Rasagiline

Rasagiline is a selective, irreversible MAO-B inhibitor indicated for the treatment of idiopathic Parkinson's disease. The results of a clinical trial designed to examine the effects of rasagiline tablets on blood pressure when it is administered with increasing doses of tyramine indicates the functional selectivity can be incomplete when healthy subjects ingest large amounts of tyramine while receiving recommended doses of rasagiline tablets. The selectivity for inhibiting MAO-B diminishes in a dose-related manner. One mechanism is believed to be related to its MAO-B inhibitory activity, which causes an increase in extracellular levels of dopamine in the striatum. The elevated dopamine level and subsequent increased dopaminergic activity are likely to mediate rasagiline’s beneficial effects seen in models of dopaminergic motor dysfunction.


myocarditis

biolink:Disease biolink:DiseaseOrPhenotypicFeature biolink:ThingWithTaxon biolink:BiologicalEntity biolink:NamedThing biolink:Entity


Bone pain

biolink:PhenotypicFeature biolink:DiseaseOrPhenotypicFeature biolink:ThingWithTaxon biolink:BiologicalEntity biolink:NamedThing biolink:Entity


Econazole

An imidazole derivative that is commonly used as a topical antifungal agent.


Mephenytoin

An anticonvulsant effective in tonic-clonic epilepsy (EPILEPSY, TONIC-CLONIC). It may cause blood dyscrasias.


Epinastine

direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell, indicated for the prevention of itching associated with allergic conjunctivitis


Estazolam

A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.


Stannous fluoride

Inorganic fluorides of tin. They include both stannic fluoride (tin tetrafluoride) and stannous fluoride (tin difluoride). The latter is used in the prevention of dental caries.


ELTROMBOPAG

an oral, nonpeptide thrombopoietin receptor agonist


Intubation, Gastrointestinal

biolink:Procedure biolink:ActivityAndBehavior biolink:NamedThing biolink:Entity biolink:Occurrent biolink:PhysicalEssenceOrOccurrent


Memantine

AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent.


Hexylresorcinol

A substituted dihydroxybenzene used topically as an antiseptic for the treatment of minor skin infections.


Buspirone

An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.


Indinavir

A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.


lanthanum carbonate

a phosphate binder used for hyperphosphatemia treatment in end-stage renal disease


Meclizine

A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.


Aspirin

The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5)


Phenolphthalein

An acid-base indicator which is colorless in acid solution, but turns pink to red as the solution becomes alkaline. It is used medicinally as a cathartic.


Penciclovir

The antiviral compound penciclovir has inhibitory activity against herpes simplex virus types 1 (HSV-1) and 2 (HSV-2). In cells infected with HSV-1 or HSV-2, the viral thymidine kinase phosphorylates penciclovir to a monophosphate form that, in turn, is converted by cellular kinases to the active form penciclovir triphosphate. Biochemical studies demonstrate that penciclovir triphosphate inhibits HSV polymerase competitively with deoxyguanosine triphosphate. Consequently, herpes viral DNA synthesis and, therefore, replication are selectively inhibited.


Suprofen

An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic.


Bicalutamide

Bicalutamide is a non-steroidal androgen receptor inhibitor. It competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue. Prostatic carcinoma is known to be androgen sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen.


Bromocriptine

A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.


Hostility

biolink:Behavior biolink:OntologyClass biolink:ActivityAndBehavior biolink:BiologicalProcess biolink:Occurrent biolink:BiologicalProcessOrActivity biolink:BiologicalEntity biolink:NamedThing biolink:Entity biolink:PhysicalEssenceOrOccurrent


Diethylpropion

A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290)


Ciclesonide

nasal spray approved for seasonal and perennial allergic rhinitis


Furazolidona

A nitrofuran derivative with antiprotozoal and antibacterial activity. Furazolidone acts by gradual inhibition of monoamine oxidase. (From Martindale, The Extra Pharmacopoeia, 30th ed, p514)


Fesoterodine

a muscarinic antagonist for treatment of overactive bladder


Gabapentin enacarbil

Gabapentin enacarbil is a prodrug of gabapentin and, accordingly, its therapeutic effects in restless legs syndrome and postherpetic neuralgia are attributable to gabapentin. In animal models of analgesia, gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli).


Dezocine

potent analgesic; RN given refers to ((5R-(5alpha,11alpha,13S*)))-isomer (dezocin); structure


Histidine

An essential amino acid that is required for the production of HISTAMINE.


bacterial infectious disease with sepsis


Propylene Glycol

A clear, colorless, viscous organic solvent and diluent used in pharmaceutical preparations.


Olsalazine

cpd with 2 salicylate molecules linked together by an azo bond


L-ornithine

An amino acid produced in the urea cycle by the splitting off of urea from arginine.


Posterior synechiae of the anterior chamber


Stavudine

A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.


Chlorphenesin carbamate

A centrally acting muscle relaxant. Its mode of action is unknown. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1203)


Cianidanol

An antioxidant flavonoid, occurring especially in woody plants as both (+)-catechin and (-)-epicatechin (cis) forms.


Nicotinic acid

A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.


Chloroethane

A gas that condenses under slight pressure. Because of its low boiling point ethyl chloride sprayed on skin produces an intense cold by evaporation. Cold blocks nerve conduction. Ethyl chloride has been used in surgery but is primarily used to relieve local pain in sports medicine.


Iopanoic acid

Radiopaque medium used as diagnostic aid.


Dronabinol

A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.


Alvimopan

mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain


Alitretinoin

A retinoid that is used for the treatment of chronic hand ECZEMA unresponsive to topical CORTICOSTEROIDS. It is also used to treat cutaneous lesions associated with AIDS-related KAPOSI SARCOMA.


Medetomidine

An agonist of RECEPTORS, ADRENERGIC ALPHA-2 that is used in veterinary medicine for its analgesic and sedative properties. It is the racemate of DEXMEDETOMIDINE.


Riluzole

The etiology and pathogenesis of amyotrophic lateral sclerosis (ALS) are not known, although a number of hypotheses have been advanced. One hypothesis is that motor neurons, made vulnerable through either genetic predisposition or environmental factors, are injured by glutamate. In some cases of familial ALS the enzyme superoxide dismutase has been found to be defective. The mode of action of riluzole is unknown. Its pharmacological properties include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release, 2) inactivation of voltage-dependent sodium channels, and 3) ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors. Riluzole has also been shown, in a single study, to delay median time to death in a transgenic mouse model of ALS. These mice express human superoxide dismutase bearing one of the mutations found in one of the familial forms of human ALS. It is also neuroprotective in various in vivo experimental models of neuronal injury involving excitotoxic mechanisms. In in vitro tests, riluzole protected cultured rat motor neurons from the excitotoxic effects of glutamic acid and prevented the death of cortical neurons induced by anoxia. Due to its blockade of glutamatergic neurotransmission, riluzole also exhibits myorelaxant, sedative, and anticonvulsant properties.


Rimantadine

An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza.


Enalapril

Enalapril, after hydrolysis to enalaprilat, inhibits angiotensin-converting enzyme (ACE) in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex. Inhibition of ACE results in decreased plasma angiotensin II, which leads to decreased vasopressor activity and to decreased aldosterone secretion.


Tesamorelin

Growth Hormone-Releasing Factor (GRF), also known as growth hormone-releasing hormone (GHRH), is a hypothalamic peptide that acts on the pituitary somatotroph cells to stimulate the synthesis and pulsatile release of endogenous growth hormone (GH), which is both anabolic and lipolytic. GH exerts its effects by interacting with specific receptors on a variety of target cells, including chondrocytes, osteoblasts, myocytes, hepatocytes, and adipocytes, resulting in a host of pharmacodynamic effects. Some, but not all these effects, are primarily mediated by IGF-1 produced in the liver and in peripheral tissues. In vitro, tesamorelin binds and stimulates human GRF receptors with similar potency as the endogenous GRF.


Lipodystrophy due to Human immunodeficiency virus infection and antiretroviral therapy


Fenoldopam

A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.


Sincalide

An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.


Erysipelothrix rhusiopathiae infectious disease


Tryptophan

An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.


Loperamide

One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.


Masoprocol

A potent lipoxygenase inhibitor that interferes with arachidonic acid metabolism. The compound also inhibits formyltetrahydrofolate synthetase, carboxylesterase, and cyclooxygenase to a lesser extent. It also serves as an antioxidant in fats and oils.


Quinacrine

An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.


Yersinia pseudotuberculosis infectious disease


Meningitis caused by Klebsiella aerogenes


Secondary malignant neoplasm of bone marrow


Methylnaltrexone

a selective antagonist of opioid binding at the mu-opioid receptor with restricted ability to cross the blood-brain barrier, function as a peripherally-acting mu‑opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids without impacting opioid-mediated analgesic effects on the central nervous system


Milrinone

A positive inotropic cardiotonic agent with vasodilator properties. It inhibits cAMP phosphodiesterase type 3 activity in myocardium and vascular smooth muscle. Milrinone is a derivative of amrinone and has 20-30 times the inotropic potency of amrinone.


Adapalene

A naphthalene derivative that has specificity for RETINOIC ACID RECEPTORS. It is used as a DERMATOLOGIC AGENT for the treatment of ACNE.


Thioctic acid

An octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.


Praziquantel

An anthelmintic used in most schistosome and many cestode infestations.


Iron(III) oxide

A glucaric acid-iron conjugate that is used in the treatment of IRON-DEFICIENCY ANEMIA, including in patients with chronic kidney disease, when oral iron therapy is ineffective or impractical.


Dehydrocholic acid

A semisynthetic bile acid made from cholic acid. It is used as a cholagogue, hydrocholeretic, diuretic, and as a diagnostic aid.


Troleandomycin

A macrolide antibiotic that is similar to ERYTHROMYCIN.


Probucol

A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).


Hyaluronic acid sodium salt

A natural high-viscosity mucopolysaccharide with alternating beta (1-3) glucuronide and beta (1-4) glucosaminidic bonds. It is found in the UMBILICAL CORD, in VITREOUS BODY and in SYNOVIAL FLUID. A high urinary level is found in PROGERIA.


Permethrin

A pyrethroid insecticide commonly used in the treatment of LICE INFESTATIONS and SCABIES.


Nalidixic acid

A synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA GYRASE.


Valacyclovir

A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES.


attention deficit hyperactivity disorder, inattentive type


Gonadorelin

A decapeptide that stimulates the synthesis and secretion of both pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. GnRH is produced by neurons in the septum PREOPTIC AREA of the HYPOTHALAMUS and released into the pituitary portal blood, leading to stimulation of GONADOTROPHS in the ANTERIOR PITUITARY GLAND.


Mepivacaine

A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168)


Tiagabine

The precise mechanism by which tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to block GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells.


superficial multifocal basal cell carcinoma


Pyrantel

Broad spectrum anthelmintic for livestock.


Aprepitant

Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV). Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions.


BALSALAZIDE

a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine


Icatibant

a potent bradykinin (B2) receptor antagonist; WIN 65365 is an L-Tic(7) stereoisomer


Right-sided Staphylococcus aureus endocarditis


Nutritional deficiency with AIDS (acquired immunodeficiency syndrome)


Betaine

A naturally occurring compound that has been of interest for its role in osmoregulation. As a drug, betaine hydrochloride has been used as a source of hydrochloric acid in the treatment of hypochlorhydria. Betaine has also been used in the treatment of liver disorders, for hyperkalemia, for homocystinuria, and for gastrointestinal disturbances. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1341)


Pramlintide

Pramlintide is an analog of human amylin. Amylin is colocated with insulin in secretory granules and cosecreted with insulin by pancreatic beta cells in response to food intake. Amylin and insulin show similar fasting and postprandial patterns in healthy individuals. In patients with type 1 and type 2 diabetes, there is reduced secretion from pancreatic beta cells of both insulin and amylin in response to food. Amylin affects the rate of postprandial glucose appearance through a variety of mechanisms, as determined by nonclinical studies. Amylin slows gastric emptying (i.e., the rate at which food is released from the stomach to the small intestine) without altering the overall absorption of nutrients. In addition, amylin suppresses glucagon secretion (not normalized by insulin alone), which leads to suppression of endogenous glucose output from the liver. Amylin also regulates food intake due to centrally-mediated modulation of appetite. In human studies, pramlintide, acting as an amylin analog, slows gastric emptying, reduces the postprandial rise in plasma glucagon, and modulates satiety leading to decreased caloric intake.


Proflavine

Topical antiseptic used mainly in wound dressings.


Distinctive exudative discoid AND lichenoid chronic dermatosis of Sulzberger and Garbe


Famciclovir

An aminopurine derivative and prodrug of penciclovir which is a competitive inhibitor of herpes simplex 2 DNA polymerase. It is used to treat HERPES SIMPLEX VIRUS INFECTION.


pyrithione zinc

dimer of two pyrithione molecules bound by zinc; ingredient of commercial anti-dandruff shampoos; Do not confuse zinc pyrithione with Raman spectrum probe dye known as zincon; antifungal and antibacterial


Dipivefrin

used in treatment of both primary & open angle glaucoma; RN given refers to (+-)-isomer


Acetohexamide

A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide.


anti-glomerular basement membrane disease


Phenprocoumon

Coumarin derivative that acts as a long acting oral anticoagulant.


Succimer

A mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them.


Trimethaphan

A nicotinic antagonist that has been used as a ganglionic blocker in hypertension, as an adjunct to anesthesia, and to induce hypotension during surgery.


Cisplatin

An inorganic and water-soluble platinum complex. After undergoing hydrolysis, it reacts with DNA to produce both intra and interstrand crosslinks. These crosslinks appear to impair replication and transcription of DNA. The cytotoxicity of cisplatin correlates with cellular arrest in the G2 phase of the cell cycle.


Glutamine

A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.


Sulfapyridine

Antibacterial, potentially toxic, used to treat certain skin diseases.


Vincamine

A major alkaloid of Vinca minor L., Apocynaceae. It has been used therapeutically as a vasodilator and antihypertensive agent, particularly in cerebrovascular disorders.


Spinosad

combination of spinosyns A and D; isolated from Saccharopolyspora spinosa


Gentian violet cation

A dye that is a mixture of violet rosanilinis with antibacterial, antifungal, and anthelmintic properties.


Acamprosate

The mechanism of action of acamprosate in maintenance of alcohol abstinence is not completely understood. Chronic alcohol exposure is hypothesized to alter the normal balance between neuronal excitation and inhibition. In vitro and in vivo studies in animals have provided evidence to suggest acamprosate may interact with glutamate and GABA neurotransmitter systems centrally, and has led to the hypothesis that acamprosate restores this balance.


Yersinia enterocolitica infectious disease


central nervous system infectious disorder


Zalcitabine

A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.


Telbivudine

A thymidine derivative and antiviral agent that inhibits DNA synthesis by HEPATITIS B VIRUS and is used for the treatment of CHRONIC HEPATITIS B.


Naftifine

allylamine der; RN given refers to unlabeled parent cpd


Phenacemide

Phenacemide (Phenurone) is an older antiepileptic agent. It is capable of relieving patients resistant to other antiepileptics, although its therapeutic effectiveness must be balanced against its toxic effects.


Enalaprilat

The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.


alveolar capillary dysplasia with misalignment of pulmonary veins


Epidermal growth factor receptor negative non-small cell lung cancer


Lactic Acid

A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed)


Pipecuronium

A piperazinyl androstane derivative which is a non-depolarizing neuromuscular blocking agent (NEUROMUSCULAR NONDEPOLARIZING AGENTS). It is used as a muscle relaxant during ANESTHESIA and surgical procedures.


Trioxsalen

Pigmenting photosensitizing agent obtained from several plants, mainly Psoralea corylifolia. It is administered either topically or orally in conjunction with ultraviolet light in the treatment of vitiligo.


Asymptomatic left ventricular systolic dysfunction


pneumonia caused by gram negative bacteria


Ursodeoxycholic acid

An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.


Oxamniquine

An anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine causes worms to shift from the mesenteric veins to the liver where the male worms are retained; the female worms return to the mesentery, but can no longer release eggs. (From Martindale, The Extra Pharmacopoeia, 31st ed, p121)


Dextrothyroxine

The dextrorotary isomer of the synthetic THYROXINE.


Nitrogen

An element with the atomic symbol N, atomic number 7, and atomic weight [14.00643; 14.00728]. Nitrogen exists as a diatomic gas and makes up about 78% of the earth's atmosphere by volume. It is a constituent of proteins and nucleic acids and found in all living cells.


Hexachlorophene

A chlorinated bisphenol antiseptic with a bacteriostatic action against Gram-positive organisms, but much less effective against Gram-negative organisms. It is mainly used in soaps and creams and is an ingredient of various preparations used for skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p797)


Metyrapone

An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.


respiratory syncytial virus infectious disease


Fosfomycin

An antibiotic produced by Streptomyces fradiae.


Carbocysteine

A compound formed when iodoacetic acid reacts with sulfhydryl groups in proteins. It has been used as an anti-infective nasal spray with mucolytic and expectorant action.


L-threonine

An essential amino acid occurring naturally in the L-form, which is the active form. It is found in eggs, milk, gelatin, and other proteins.


Amlexanox

The mechanism of action by which amlexanox accelerates healing of aphthous ulcers is unknown. In vitro studies have demonstrated amlexanox to be a potent inhibitor of the formation and/or release of inflammatory mediators (histamine and leukotrienes) from mast cells, neutrophils and mononuclear cells.


Clofibrate

A fibric acid derivative used in the treatment of HYPERLIPOPROTEINEMIA TYPE III and severe HYPERTRIGLYCERIDEMIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986)


Asthma-Chronic Obstructive Pulmonary Disease Overlap Syndrome


Tubocurarine chloride

A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae.


Carglumic acid

carglumic acid could be helpful in lowering plasma ammonia levels over 400 micromol/L more rapidly


Barbital

A long-acting barbiturate that depresses most metabolic processes at high doses. It is used as a hypnotic and sedative and may induce dependence. Barbital is also used in veterinary practice for central nervous system depression.


Matromycin

Antibiotic macrolide produced by Streptomyces antibioticus.


Methoxamine

An alpha-1 adrenergic agonist that causes prolonged peripheral VASOCONSTRICTION.


Phenylbutazone

A butyl-diphenyl-pyrazolidinedione that has anti-inflammatory, antipyretic, and analgesic activities. It has been used in ANKYLOSING SPONDYLITIS; RHEUMATOID ARTHRITIS; and REACTIVE ARTHRITIS.


Cidofovir

An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.


hereditary thrombophilia due to congenital protein C deficiency


Vidarabine

A nucleoside antibiotic isolated from Streptomyces antibioticus. It has some antineoplastic properties and has broad spectrum activity against DNA viruses in cell cultures and significant antiviral activity against infections caused by a variety of viruses such as the herpes viruses, the VACCINIA VIRUS and varicella zoster virus.


Alcaftadine

Alcaftadine is an H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.


Aluminum Chloride

A compound with the chemical formula AlCl3; the anhydrous salt is used as a catalyst in organic chemical synthesis, and hydrated salts are used topically as antiperspirants, and for the management of HYPERHYDROSIS.


Natamycin

Amphoteric macrolide antifungal antibiotic from Streptomyces natalensis or S. chattanoogensis. It is used for a variety of fungal infections, mainly topically.


Netilmicin

Semisynthetic 1-N-ethyl derivative of SISOMYCIN, an aminoglycoside antibiotic with action similar to gentamicin, but less ear and kidney toxicity.


congenital non-bullous ichthyosiform erythroderma


Ranolazine

An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.


Vitamin E

A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.


Sorbitan mono-9-octadecanoate poly(oxy-1,2-ethanediyl) derivatives; complex mixtures of polyoxyethylene ethers used as emulsifiers or dispersing agents in pharmaceuticals.


Potassium acetate

A potassium salt used to replenish ELECTROLYTES, for restoration of WATER-ELECTROLYTE BALANCE, as well as a urinary and systemic alkalizer, which can be administered orally or by intravenous infusion. Formerly, it was used in DIURETICS and EXPECTORANTS.


Glucantime

ANTIMONY salt of meglumine that is used in the treatment of LEISHMANIASIS.


Influenza due to Influenza virus, type B


Malignant melanoma with BRAF V600E mutation


Trilostane

inhibits conversion of pregnenolone to progesterone; adrenal blocking agent used in treatment of Cushing's syndrome


Dementia associated with Parkinson's Disease


Mephentermine

A sympathomimetic agent with specificity for alpha-1 adrenergic receptors. It is used to maintain BLOOD PRESSURE in hypotensive states such as following SPINAL ANESTHESIA.


Sermorelina

The biologically active fragment of human growth hormone-releasing factor, consisting of GHRH(1-29)-amide. This N-terminal sequence is identical in several mammalian species, such as human, pig, and cattle. It is used to diagnose or treat patients with GROWTH HORMONE deficiency.


Cupric Sulfate

A sulfate salt of copper. It is a potent emetic and is used as an antidote for poisoning by phosphorus. It also can be used to prevent the growth of algae.


Phenol red

Red dye, pH indicator, and diagnostic aid for determination of renal function. It is used also for studies of the gastrointestinal and other systems.


myeloid neoplasm associated with PDGFRA rearrangement


Thiethylperazine

A dopamine antagonist that is particularly useful in treating the nausea and vomiting associated with anesthesia, mildly emetic cancer chemotherapy agents, radiation therapy, and toxins. This piperazine phenothiazine does not prevent vertigo or motion sickness. (From AMA Drug Evaluations Annual, 1994, p457)


Ethinamate

short duration hypnotic with fast onset & relatively low toxicity; may cause dependence; minor descriptor (76-85); on-line & Index Medicus search CARBAMATES (76-85)


Intrathecal injection of chemotherapeutic agent


Moricizine

An antiarrhythmia agent used primarily for ventricular rhythm disturbances.


Troglitazone

A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity.


Benzyl Alcohol

A colorless liquid with a sharp burning taste and slight odor. It is used as a local anesthetic and to reduce pain associated with LIDOCAINE injection. Also, it is used in the manufacture of other benzyl compounds, as a pharmaceutic aid, and in perfumery and flavoring.


Isosorbide

1,4:3,6-Dianhydro D-glucitol. Chemically inert osmotic diuretic used mainly to treat hydrocephalus; also used in glaucoma.


Mazindol

Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.


Herpes zoster with AIDS (acquired immunodeficiency syndrome)


Tocainide

An antiarrhythmic agent which exerts a potential- and frequency-dependent block of SODIUM CHANNELS.


Selective decontamination of the digestive tract


Pelvic inflammatory disease due to Mycoplasma hominis


hantavirus hemorrhagic fever with renal syndrome


Contact dermatitis caused by urushiol from Pacific poison oak


Testolactone

An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer.


bacterial meningitis caused by gram-negative bacteria


Metocurine

from Chinese herb Cyclea hainanensis Mrr


multiple acyl-CoA dehydrogenase deficiency


Calcium Carbonate

Carbonic acid calcium salt (CaCO3). An odorless, tasteless powder or crystal that occurs in nature. It is used therapeutically as a phosphate buffer in hemodialysis patients and as a calcium supplement.


Pargyline

A monoamine oxidase inhibitor with antihypertensive properties.


Pemoline

A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.


Glycerol

A trihydroxy sugar alcohol that is an intermediate in carbohydrate and lipid metabolism. It is used as a solvent, emollient, pharmaceutical agent, or sweetening agent.


Uterine perforation by intrauterine contraceptive device


Ketotifen

A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.


Enzalutamide

Enzalutamide is an androgen receptor inhibitor that acts on different steps in the androgen receptor signaling pathway. Enzalutamide has been shown to competitively inhibit androgen binding to androgen receptors and inhibit androgen receptor nuclear translocation and interaction with DNA. A major metabolite, N‑desmethyl enzalutamide, exhibited similar in vitro activity to enzalutamide. Enzalutamide decreased proliferation and induced cell death of prostate cancer cells in vitro, and decreased tumor volume in a mouse prostate cancer xenograft model.


Tofacitinib

Tofacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression. Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.


Tafluprost

a prostaglandin analog is a selective FP prostanoid receptor agonist which is believed to reduce intraocular pressure by increasing uveoscleral outflow


Axitinib

A benzamide and indazole derivative that acts as a TYROSINE KINASE inhibitor of the VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR. It is used in the treatment of advanced RENAL CELL CARCINOMA.


Ingenol mebutate

protein kinase C agonist and antineoplastic


Vismodegib

inhibits the hedgehog pathway and ABC transporters; has antineoplastic activity


Lucinactant

a pulmonary surfactant composed of sinapultide, colfosceril palmitate, palmitoyloleaoylphosphatidylglycerol, and palmitic acid; Aerosurf is for inhalation


Strontium ranelate

an uncoupling agent containing strontium prevents bone loss by depressing bone resorption & maintaining bone formation in estrogen-deficient rats


STIBOPHEN

antimony compound used as treatment of schistosomiasis


Teduglutide

an analogue of human glucagon-like peptide-2 (GLP-2) preserves mucosal integrity by promoting repair and normal growth of the intestine through an increase of villus height and crypt depth


Lomitapide

an anticholesteremic agent and microsomal triglycide transfer protein inhibitor


Apixaban

Apixaban is a selective inhibitor of FXa. It does not require antithrombin III for antithrombotic activity. Apixaban inhibits free and clot-bound FXa, and prothrombinase activity. Apixaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development.


4-Aminopyridine derivative that acts as a POTASSIUM CHANNEL blocker to increase release of ACETYLCHOLINE from nerve terminals. It is used in the treatment of CONGENITAL MYASTHENIC SYNDROMES.


Methylprednisolone acetate

Methylprednisolone derivative that is used as an anti-inflammatory agent for the treatment of ALLERGY and ALLERGIC RHINITIS; ASTHMA; and BURSITIS; and for the treatment of ADRENAL INSUFFICIENCY.


Dabrafenib

Dabrafenib is an inhibitor of some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. Dabrafenib also inhibits wild-type BRAF and CRAF kinases with IC50 values of 3.2 and 5.0 nM, respectively, and other kinases such as SIK1, NEK11, and LIMK1 at higher concentrations. Some mutations in the BRAF gene, including those that result in BRAF V600E, can result in constitutively activated BRAF kinases that may stimulate tumor cell growth. Dabrafenib inhibits cell growth of various BRAF V600 mutation-positive tumors in vitro and in vivo.


Trametinib

a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 activation and of MEK1 and MEK2 kinase activity. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation


Carbetocin

carbetocin selectively binds to oxytocin receptors in the smooth muscle of the uterus, stimulates rhythmic contractions of the uterus, increases the frequency of existing contractions, and raises the tone of the uterus musculature


Obidoxime

Cholinesterase reactivator occurring in two interchangeable isomeric forms, syn and anti.


Trabectedin

A complex structure that includes isoquinolines joined by a cyclic ester; it is a DNA-binding agent and guanine N2 alkylator derived from the marine tunicate, Ecteinascidia turbinata. Trabectedin is used for the treatment of advanced soft-tissue SARCOMA, after failure of ANTHRACYCLINES or IFOSFAMIDE drug therapy.


Bosutinib

a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases


Crizotinib

Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins. The formation of ALK fusion proteins results in activation and dysregulation of the gene's expression and signaling which can contribute to increased cell proliferation and survival in tumors expressing these proteins. Crizotinib demonstrated concentration-dependent inhibition of ALK, ROS1, and c-Met phosphorylation in cell-based assays using tumor cell lines and demonstrated antitumor activity in mice bearing tumor xenografts that expressed echinoderm microtubule-associated protein-like 4 (EML4)- or nucleophosmin (NPM)-ALK fusion proteins or c-Met.


Pirfenidone

pyridone, indicated for the treatment of idiopathic pulmonary fibrosis


Bazedoxifene

an estrogen agonist/antagonist that acts as an agonist in some estrogen-sensitive tissues and an antagonist in others


Avanafil

a selective inhibitor of cGMP-specific PDE5 has no direct relaxant effect on isolated human corpus cavernosum, but enhances the effect of NO by inhibiting PDE5, which is responsible for degradation of cGMP in the corpus cavernosum


Gimeracil

a biochemical and pharmacological modulator of 5-FU


Aclidinium

a long-acting, inhaled antimuscarinic; in phase I trial 8/2008


Ibrutinib

Ibrutinib is a small-molecule inhibitor of BTK. Ibrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. BTK's role in signaling through the B-cell surface receptors results in activation of pathways necessary for B-cell trafficking, chemotaxis, and adhesion. Nonclinical studies show that ibrutinib inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro.


Dapoxetine

selective serotonin reuptake inhibitor (SSRI) that was designed specifically for premature ejaculation


Moxisylyte

An alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312)


Clobutinol

was minor as SILOMAT mapped to AMINO ALCOHOLS (63-79)


Sofosbuvir

A uridine monophosphate analog inhibitor of HEPATITIS C VIRUS (HCV) polymerase NS5B that is used as an ANTIVIRAL AGENT in the treatment of CHRONIC HEPATITIS C.


Simeprevir

Oral HCV-PROTEASE INHIBITOR effective against hepatitis C virus (HCV) serine protease NS3/4A. It is used in the treatment of chronic hepatitis C (Antivirals) genotype 1 infection in adults with compensated liver disease, including CIRRHOSIS.


Luliconazole

an antifungal that belongs to the azole class, luliconazole appears to inhibit ergosterol synthesis by inhibiting the enzyme lanosterol demethylase, inhibition of this enzyme’s activity by azoles results in decreased amounts of ergosterol, a constituent of fungal cell membranes, and a corresponding accumulation of lanosterol


Olodaterol

a long-acting beta2-adrenergic agonist (LABA), activation of beta2 receptors in the airways results in a stimulation of intracellular adenyl cyclase, an enzyme that mediates the synthesis of cyclic-3',5' adenosine monophosphate (cAMP), elevated levels of cAMP induce bronchodilation by relaxation of airway smooth muscle cells


Artesunic acid

A water-soluble, semi-synthetic derivative of the sesquiterpene lactone artemisinin with anti-malarial, anti-schistosomiasis, antiviral, and potential anti-neoplastic activities. Artesunate (AS) contains an endoperoxide bridge that is activated by heme iron, resulting in the generation of free radicals that alkylate parasite proteins and ultimately lead to cell death. Dihydroartemisinin (DHA, also known as artenimol), the active metabolite of artesunate, was found to specifically increase oxidative stress in P. falciparum-infected erythrocytes but not uninfected cells, by reduction of antioxidants.


Naftidrofuryl

A drug used in the management of peripheral and cerebral vascular disorders. It is claimed to enhance cellular oxidative capacity and to be a spasmolytic. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1310) It may also be an antagonist at 5HT-2 serotonin receptors.


Polidocanol

An alkyl polyglycol ether of LAURYL ALCOHOL, chemically defined as an alcohol ethoxylate having an average alkyl chain of 12–14 carbon atoms, and an ethylene oxide chain of 9 ethylene oxide units. It is used as a detergent, and medically as a local anesthetic, and as a sclerosing agent for the treatment of ESOPHAGEAL AND GASTRIC VARICES and VARICOSE VEINS.


Clobazam

A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME.  It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY.


Trichomycin

major descriptor (78-85); on-line search ANTIBIOTICS, ANTIFUNGAL (66-85); Index Medicus search TRICHOMYCIN (63-77); HACHIMYCIN (78-85)


Levamisole

An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6)


Lixisenatide

A synthetic GLUCAGON-LIKE PEPTIDE-1 RECEPTOR (GLP-1) agonist that binds GLP-1 receptor that is used to control blood sugar levels in patients with TYPE 2 DIABETES; amino acid sequence is H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSK KKKKK-NH2 (ZP10A).


Vitamin E

A natural tocopherol and one of the most potent antioxidant tocopherols. It exhibits antioxidant activity by virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus. It has four methyl groups on the 6-chromanol nucleus. The natural d form of alpha-tocopherol is more active than its synthetic dl-alpha-tocopherol racemic mixture.


Rilmenidine

Oxazole derivative that acts as an agonist for ALPHA-2 ADRENERGIC RECEPTORS and IMIDAZOLINE RECEPTORS. It is used in the treatment of HYPERTENSION.


Tegafur

Congener of FLUOROURACIL with comparable antineoplastic action. It has been suggested especially for the treatment of breast neoplasms.


Molsidomine

A morpholinyl sydnone imine ethyl ester, having a nitrogen in place of the keto oxygen. It acts as NITRIC OXIDE DONORS and is a vasodilator that has been used in ANGINA PECTORIS.


Umeclidinium

a long-acting antimuscarinic agent with similar affinity to the subtypes of muscarinic receptors M1 to M5, in the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation


alpha-Lactose

A disaccharide of GLUCOSE and GALACTOSE in human and cow milk. It is used in pharmacy for tablets, in medicine as a nutrient, and in industry.


Betamethasone valerate

Betamethasone valerate has anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.


Docosahexaenoic acid

a mixture of fish oil and primrose oil; used as a high-docosahexaenoic acid fatty acid supplement


Deferoxamine

Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.


Butethal

Butobarbital should be distinguished from Butabarbital (a synonym for Secbutabarbital)


Metahexamide

major descriptor (64-83); on-line search SULFONYLUREA COMPOUNDS (64-83); Index Medicus search METAHEXAMIDE (64-83); RN given refers to parent cpd; structure


Benzoin

A white crystalline compound prepared by condensation of benzaldehyde in potassium cyanide and used in organic syntheses. This should not be confused with benzoin gum from STYRAX.


sodium phosphate, monobasic, monohydrate


Tyropanic acid

A diagnostic aid as a radiopaque medium in cholecystography.


Formaldehyde

A highly reactive aldehyde gas formed by oxidation or incomplete combustion of hydrocarbons. In solution, it has a wide range of uses: in the manufacture of resins and textiles, as a disinfectant, and as a laboratory fixative or preservative. Formaldehyde solution (formalin) is considered a hazardous compound, and its vapor toxic. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p717)


Dihydroergocornine

A 9,10alpha-dihydro derivative of ERGOTAMINE that contains isopropyl sidechains at the 2' and 5' positions of the molecule.


Levoleucovorin

A folate analog consisting of the pharmacologically active isomer of LEUCOVORIN.


Adenosine monophosphate

Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.


Pyrethrins

The active insecticidal constituent of CHRYSANTHEMUM CINERARIIFOLIUM flowers. Pyrethrin I is the pyretholone ester of chrysanthemummonocarboxylic acid and pyrethrin II is the pyretholone ester of chrysanthemumdicarboxylic acid monomethyl ester.


Undecylenic acid

a fatty acid with a terminal double bond


Aminohippuric acid

The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.


Peramivir

Peramivir is an inhibitor of influenza virus neuraminidase, an enzyme that releases viral particles from the plasma membrane of infected cells.


Colestilan

a 2-methylimidazole-epichlorohydrin polymer; bile acid and methotrexate anion-exchange resin


Prussian blue

antidote to thallium poisoning; RN given refers to Fe(+3)[3:4] salt; structure


Levomilnacipran

a selective serotonin and norepinephrine reuptake inhibitor (SNRI), mechanism of the antidepressant action of levomilnacipran is unknown, but is thought to be related to the potentiation of serotonin and norepinephrine in the central nervous system


Diphenidol

shows anti-arrhythmic activity; RN given refers to unlabeled parent cpd


Nadifloxacin

(R)-isomer does not induce chromosomal aberrations, unlike (S)-isomer; structure given in first source


Furazidine

Nitrofuran derivative anti-infective agent used for urinary tract infections.


Thiosemicarbazone

A thiosemicarbazone that is used in association with other antimycobacterial agents in the initial and continuation phases of antituberculosis regimens. Thiacetazone containing regimens are less effective than the short-course regimen recommended by the International Union Against Tuberculosis and are used in some developing countries to reduce drug costs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p217)


Vorapaxar

Vorapaxar is a reversible antagonist of the protease-activated receptor-1 (PAR-1) expressed on platelets, but its long half-life makes it effectively irreversible. Vorapaxar inhibits thrombin-induced and thrombin receptor agonist peptide (TRAP)-induced platelet aggregation in vitro studies. Vorapaxar does not inhibit platelet aggregation induced by adenosine diphosphate (ADP), collagen or a thromboxane mimetic and does not affect coagulation parameters ex vivo. PAR-1 receptors are also expressed in a wide variety of cell types, including endothelial cells, neurons, and smooth muscle cells, but the pharmacodynamic effects of vorapaxar in these cell types have not been assessed.


Nitrazepam

A benzodiazepine derivative used as an anticonvulsant and hypnotic.


Premarin

A pharmaceutical preparation containing a mixture of water-soluble, conjugated estrogens derived wholly or in part from URINE of pregnant mares or synthetically from ESTRONE and EQUILIN. It contains a sodium-salt mixture of estrone sulfate (52-62%) and equilin sulfate (22-30%) with a total of the two between 80-88%. Other concomitant conjugates include 17-alpha-dihydroequilin, 17-alpha-estradiol, and 17-beta-dihydroequilin. The potency of the preparation is expressed in terms of an equivalent quantity of sodium estrone sulfate.


Piperaquine

The exact mechanism of action of piperaquine is unknown, but it likely mirrors that of chloroquine, a close structural analogue. Chloroquine binds to toxic haeme (derived from the patient’s haemoglobin) within the malaria parasite, preventing its detoxification via a polymerisation step.


Alaxin

Artenimol is able to reach high concentrations within the parasitized erythrocytes. Its endoperoxide bridge is thought to be essential for its antimalarial activity, causing free-radical damage to parasite membrane systems.


Thiosalicylic acid

a degradation product of thimerosal; RN given refers to parent cpd


Benzylhydrochlorothiazide

thiazide diuretic used as a blood pressure-lowering agent


Simetride

a analgesic agent indicated for low back pain, symptomatic neuralgia, headache, menstrual pain, pharyngalgia/earache due to inflammation, toothache, postoperative pain, combined with caffeine


Icosapent ethyl

Icosapent ethyl is a stable ethyl ester of the omega-3 fatty acid, eicosapentaenoic acid (EPA). The mechanisms of action contributing to reduction of cardiovascular events with icosapent ethyl are not  completely understood. The mechanisms are likely multi-factorial including improved lipoprotein profile with reduction of triglyceride-rich lipoproteins, anti-inflammatory, and antioxidant effects, reduction of macrophage accumulation, improved endothelial function, increased fibrous cap thickness/stability, and antiplatelet effects. Each of these mechanisms   can beneficially alter the development, progression, and stabilisation of atherosclerotic plaque, as well as the implications of plaque rupture, and preclinical and clinical studies support such benefits with EPA. Systemic and localised anti-inflammatory effects of EPA may result from displacement of pro-inflammatory arachidonic acid (AA), directing catabolism away from eicosanoids (2-series prostaglandins and thromboxanes, and 4-series leukotrienes) to non- or anti-inflammatory mediators. However, the direct clinical meaning of individual findings is not clear.


Betahistine

A histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.


Nicorandil

A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.


Asunaprevir

an NS3 protease inhibitor against hepatitis C virus


Luseogliflozin

an antidiabetic agent that inhibits sodium-dependent glucose cotransporter 2 (SGLT2)


TALAPORFIN

effective tumor localizer that brings about the selective degradation of tumor tissue following light exposure; structure given in first source


Tipiracil

tipiracil increases trifluridine exposure by inhibiting its metabolism by thymidine phosphorylase


Iguratimod

a methanesulfonanilide disease-modifying antirheumatic drug that has been developed exclusively in Japan and China


Teneligliptin

A long-acting, orally bioavailable, pyrrolidine-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Teneligliptin may also reduce plasma triglyceride levels through a sustained increase in GLP-1 levels.


Anagliptin

anagliptin hydrochloride salt is the active compound


Methylprednisolone hemisuccinate

A water-soluble ester of METHYLPREDNISOLONE used for cardiac, allergic, and hypoxic emergencies.


Edoxaban

An orally active inhibitor of coagulation factor Xa (activated factor X) with anticoagulant activity. Edoxaban is administered as edoxaban tosylate. This agent has an elimination half-life of 9-11 hours and undergoes renal excretion.


Mitiglinide

a rapid and short-acting hypoglycemic agent; acts on sulfonylurea receptor closing KATP channels; considered one of the glinides-an imprecise grouping; structure given in first source


Pegaptanib

a pegylated modified oligonucleotide that binds with high specificity and affinity to extracellular Vascular Endothelial Growth Factor (VEGF165) inhibiting its activity, VEGF is a secreted protein that induces angiogenesis, vascular permeability and inflammation, all of which are thought to contribute to the progression of the neovascular (wet) form of AMD


Mozavaptan

Mozavaptan is a benzazepine derivative that antagonizes the binding of arginine vasopressin (AVP) to vasopressin receptors. Mozavaptan can inhibit the antidiuretic action of AVP promoting aquaresis.


Levosimendan

A hydrazone and pyridazine derivative; the levo-form is a phosphodiesterase III inhibitor, calcium-sensitizing agent, and inotropic agent that is used in the treatment of HEART FAILURE.


Toloxatone

oxazolidinone derivative; psychotropic drug; structure


Moclobemide

A reversible inhibitor of monoamine oxidase type A (RIMA) that has antidepressive properties.


Pranlukast

SRS-A antagonist; leukotriene D4 receptor antagonist


Tranilast

antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis; structure


Olaparib

Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. PARP enzymes are involved in normal cellular homeostasis, such as DNA transcription, cell cycle regulation, and DNA repair. Olaparib has been shown to inhibit growth of select tumor cell lines in vitro and decrease tumor growth in mouse xenograft models of human cancer both as monotherapy or following platinum-based chemotherapy. Increased cytotoxicity and anti-tumor activity following treatment with olaparib were noted in cell lines and mouse tumor models with deficiencies in BRCA. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complex, resulting in disruption of cellular homeostasis and cell death.


Tiquizium

antispasmodic; RN refers to bromide (trans)-isomer


Acotiamide

A prokinetic agent with gastrointestinal (GI) motility-enhancing activity. Although the exact mechanism by which acotiamide exerts its effect has yet to be fully elucidated, this agent appears to inhibit acetylcholinesterase (AchE), an enzyme responsible for the breakdown of acetylcholine (Ach). Increased Ach concentrations lead to an improvement of gastric emptying and GI motility and eventually to a reduction of dyspepsia symptoms.


ALEMTUZUMAB

Alemtuzumab binds to CD52, an antigen present on the surface of B and T lymphocytes, a majority of monocytes, macrophages, NK cells, and a subpopulation of granulocytes. A proportion of bone marrow cells, including some CD34+ cells, express variable levels of CD52. The proposed mechanism of action is antibody-dependent cellular-mediated lysis following cell surface binding of alemtuzumab to the leukemic cells.


Felypressin

A synthetic analog of LYPRESSIN with a PHENYLALANINE substitution at residue 2. Felypressin is a vasoconstrictor with reduced antidiuretic activity.


Trimetazidine

A vasodilator used in angina of effort or ischemic heart disease.


Almitrine

A respiratory stimulant that enhances respiration by acting as an agonist of peripheral chemoreceptors located on the carotid bodies. The drug increases arterial oxygen tension while decreasing arterial carbon dioxide tension in patients with chronic obstructive pulmonary disease. It may also prove useful in the treatment of nocturnal oxygen desaturation without impairing the quality of sleep.


Amisulpride

A benzamide derivative that is used as an antipsychotic agent for the treatment of schizophrenia. It is also used as an antidepressive agent.


Dasabuvir

Dasabuvir is a non-nucleoside inhibitor of the HCV RNA-dependent RNA polymerase encoded by the NS5B gene, which is essential for replication of the viral genome. In a biochemical assay, dasabuvir inhibited a panel of genotype 1a and 1b NS5B polymerases. Based on drug resistance mapping studies of HCV genotypes 1a and 1b, dasabuvir targets the palm domain of the NS5B polymerase, and is therefore referred to as a non-nucleoside NS5B-palm polymerase inhibitor.


Fendiline

Coronary vasodilator; inhibits calcium function in muscle cells in excitation-contraction coupling; proposed as antiarrhythmic and antianginal agents.


RAMUCIRUMAB

Ramucirumab is a vascular endothelial growth factor receptor 2 antagonist that specifically binds VEGF Receptor 2 and blocks binding of VEGFR ligands, VEGF-A, VEGF-C, and VEGF-D. As a result, ramucirumab inhibits ligand-stimulated activation of VEGF Receptor 2, thereby inhibiting ligand-induced proliferation, and migration of human endothelial cells. Ramucirumab inhibited angiogenesis in an in vivo animal model.


Dosulepin

A tricyclic antidepressant with some tranquilizing action.


Lofepramine

A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE.


Carbutamide

A sulfonylurea antidiabetic agent with similar actions and uses to CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277)


Glisoxepide

oral sulfonylurea hypoglycemic agent which stimulates insulin secretion; minor descriptor (75-85); on-line & Index Medicus search SULFONYLUREA COMPOUNDS (75-85); RN given refers to parent cpd


Becaplermin

A recombinant human platelet-derived growth factor B-chain dimer used to promote WOUND HEALING by stimulating PHYSIOLOGIC ANGIOGENESIS.


Neuropathic ulcer of foot due to diabetes mellitus


Sulpiride

A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed)


ALBIGLUTIDE

A long-acting glucagon-like peptide-1 (GLP-1) receptor agonist, with antihyperglycemic activity. Albiglutide is composed of a GLP-1 (7-36) dimer fused to recombinant human albumin. Upon subcutaneous administration, this agent has a half-life of 4-7 days and resists degradation by dipeptidyl peptidase-4 (DPP-4).


History of medullary carcinoma of thyroid


Urofollitropin

A protein extract of human menopausal urine in which LUTEINIZING HORMONE has been partially or completely removed. Urofollitropin represents FOLLICLE STIMULATING HORMONE from the urine.


Thyrotropin alfa

A highly purified recombinant glycoprotein form of human THYROID-STIMULATING HORMONE, produced by recombinant DNA technology comprising two non-covalently linked subunits, an alpha subunit of 92 amino acid residues containing two N-linked glycosylation sites, and a beta subunit of 118 residues containing one N-linked glycosylation site. The amino acid sequence of thyrotropin alfa is identical to that of human pituitary thyroid stimulating hormone.


Corticotropin

A hormone made in the pituitary gland. ACTH acts on the outer part of the adrenal gland to control its release of corticosteroid hormones. More ACTH is made during times of stress.


IMIGLUCERASE

A glycosidase that hydrolyzes a glucosylceramide to yield free ceramide plus glucose. Deficiency of this enzyme leads to abnormally high concentrations of glucosylceramide in the brain in GAUCHER DISEASE. EC 3.2.1.45.


secukinumab

Secukinumab is a human IgG1 monoclonal antibody that selectively binds to the interleukin-17A (IL-17A) cytokine and inhibits its interaction with the IL-17 receptor. IL-17A is a naturally occurring cytokine that is involved in normal inflammatory and immune responses. Secukinumab inhibits the release of proinflammatory cytokines and chemokines.


Carbenicillin indanyl

acid stable indanyl ester of carbenicillin for oral use; same side-effects as carbenicillin; minor descriptor (75-86); on line & INDEX MEDICUS search CARBENICILLIN/AA (75-86); RN given refers to (mono-Na salt(2S-(2alpha,5alpha,6beta))-isomer)


PALIVIZUMAB

A humanized monoclonal antibody and ANTIVIRAL AGENT  that is used to prevent RESPIRATORY SYNCYTIAL VIRUS INFECTIONS in high risk pediatric patients.


Alectinib

Alectinib is a tyrosine kinase inhibitor that targets ALK and RET. In nonclinical studies, alectinib inhibited ALK phosphorylation and ALK-mediated activation of the downstream signaling proteins STAT3 and AKT, and decreased tumor cell viability in multiple cell lines harboring ALK fusions, amplifications, or activating mutations. The major active metabolite of alectinib, M4, showed similar in vitro potency and activity.


Ripasudil

Rho-associated kinase inhibitor for the treatment of glaucoma and ocular hypertension


inhibits hepatitis C virus NS3/4a protease


BASILIXIMAB

Basiliximab functions as an IL-2 receptor antagonist by binding with high affinity to the alpha chain of the high affinity IL-2 receptor complex and inhibiting IL-2 binding. Basiliximab is specifically targeted against IL-2Ralpha, which is selectively expressed on the surface of activated T-lymphocytes. This specific high affinity binding of basiliximab to IL-2Ralpha competitively inhibits IL-2-mediated activation of lymphocytes, a critical pathway in the cellular immune response involved in allograft rejection.


Dextromoramide

An opioid analgesic structurally related to METHADONE and used in the treatment of severe pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1070)


Garenoxacin

a des-fluoro(6) quinolone with antibacterial activity


DINUTUXIMAB

a human-mouse chimeric monoclonal antibody directed against disialoganglioside (GD2); used for treatment of refractory neuroblastoma & osteosarcoma


belimumab

monoclonal antibody directed against human BLyS protein (B lymphocyte stimulator) for treatment of autoimmune diseases


Abciximab

A Fab fragment of the chimeric monoclonal antibody 7E3 that binds to the glycoprotein IIb-IIIa receptor of human platelets, and blocks PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX, potently inhibiting PLATELET AGGREGATION. It is used in treatment of refractory unstable angina, and for prevention of ischemic complications in patients undergoing percutaneous coronary procedures such as ANGIOPLASTY; ATHERECTOMY; or stenting.


Dimethyl Ether

Ofatumumab is a human monoclonal antibody (IgG1) that binds specifically to a distinct epitope encompassing both the small and large extracellular loops of the CD20 molecule. The CD20 molecule is a transmembrane phosphoprotein expressed on B lymphocytes from the pre-B to mature B lymphocyte stage and on B cell tumours. The binding of ofatumumab to the membrane-proximal epitope of the CD20 molecule induces recruitment and activation of the complement pathway at the cell surface, leading to complement dependent cytotoxicity and resultant lysis of tumour cells. Ofatumumab has been shown to induce appreciable lysis of cells with high expression levels of complement defence molecules.


CANAKINUMAB

a human anti-interleukin-1beta monoclonal antibody for treatment of cryopyrin-associated periodic syndrome


systemic-onset juvenile idiopathic arthritis


Daclizumab

An anti-TAC (INTERLEUKIN-2 RECEPTOR ALPHA SUBUNIT) humanized monoclonal antibody (immunoglobulin G1 disulfide with human-mouse monoclonal clone 1H4 light chain, dimer) that is used in the treatment of ACUTE RELAPSING MULTIPLE SCLEROSIS.


Methyl 4,7,10,13,16-docosapentaenoate

A chimeric monoclonal antibody that functions as an ANTINEOPLASTIC AGENT through its binding to the EPIDERMAL GROWTH FACTOR RECEPTOR, where it prevents the binding and signaling action of cell growth and survival factors.


Tiocarlide

major descriptor (68-85); on-line search PHENYLTHIOUREA/AA (68-85); Index Medicus search THIOCARLIDE (68-85); Antitubercular Agent


panitumumab

Recombinant human monoclonal antibody that binds to and inhibits the function of the EPIDERMAL GROWTH FACTOR RECEPTOR. It is used in the treatment of EGFR-expressing metastatic colorectal cancer that expresses wild-type ras gene (see GENES, RAS).


metastatic malignant neoplasm in the colon


bevacizumab

An anti-VEGF humanized murine monoclonal antibody. It inhibits VEGF RECEPTORS and helps to prevent PATHOLOGIC ANGIOGENESIS.


Nonsquamous nonsmall cell neoplasm of lung


PERTUZUMAB

a humanized HER-2 monoclonal antibody; prevents ERBB2 receptor protein from binding (dimerizing) to other receptors in the HER family


ipilimumab

An anti-CTLA-4 ANTIGEN monoclonal antibody initially indicated for the treatment of certain types of metastatic MELANOMA. Its mode of actions may include blocking of CTLA-4 mediated inhibition of CYTOTOXIC T LYMPHOCYTES, allowing for more efficient destruction of target tumor cells.


EFALIZUMAB

a humanized anti-CD11anti-adhesion monoclonal antibody


Insulin degludec

insulin degludec is a long-acting basal human insulin analog for subcutaneous injection, differs from human insulin in that the amino acid threonine in position B30 has been omitted and a side-chain consisting of glutamic acid and a C16 fatty acid has been attached


raxibacumab

is a human IgG1lambda monoclonal antibody directed against protective antigen, a component of the anthrax toxin.


BRENTUXIMAB VEDOTIN

a CD30-directed antibody-drug conjugate consisting of three components: the chimeric IgG1 antibody cAC10, specific for human CD30, the microtubule disrupting agent MMAE, and a protease-cleavable linker that covalently attaches MMAE to cAC10


Anaplastic large T-cell systemic malignant lymphoma


DENOSUMAB

A humanized monoclonal antibody and an inhibitor of the RANK LIGAND, which regulates OSTEOCLAST differentiation and bone remodeling. It is used as a BONE DENSITY CONSERVATION AGENT in the treatment of OSTEOPOROSIS.


Ustekinumab

A humanized monoclonal antibody that binds to IL-12 and IL-23 and is used as a DERMATOLOGIC AGENT in the treatment of patients with plaque PSORIASIS who have not responded to other therapies.


GOLIMUMAB

Golimumab plus MTX effectively reduces the signs and symptoms of RA and is generally well tolerated in patients with an inadequate response to MTX.


CERTOLIZUMAB PEGOL

A polyethylene-glycolated Fab' fragment of TUMOR NECROSIS FACTOR antibody that binds specifically to TNF-ALPHA and neutralises it in a dose-dependent manner. It also inhibits the production of lipopolysaccharide-induced TNF-ALPHA and IL-1 BETA and is used to treat RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.


eculizumab

a recombinant humanized monoclonal IgG2/4k antibody produced by murine myeloma cell culture, specifically binds to the complement protein C5 with high affinity, thereby inhibiting its cleavage to C5a and C5b and preventing the generation of the terminal complement complex C5b-9


Ketanserin

A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.


Natalizumab

A humanized monoclonal immunoglobulin G4 antibody to human INTEGRIN ALPHA4 that binds to the alpha4 subunit of INTEGRIN ALPHA4BETA1 and integrin alpha4beta7. It is used as an IMMUNOLOGIC FACTOR in the treatment of RELAPSING-REMITTING MULTIPLE SCLEROSIS and CROHN'S DISEASE.


RANIBIZUMAB

A recombinant humanized monoclonal antibody fragment that binds VEGF-A to prevent its binding to VEGFR-1 and VEGFR-2 receptors. This activity reduces vessel permeability and angiogenesis in the treatment of neovascular age-related MACULAR DEGENERATION.


Omalizumab

An anti-IgE, recombinant, humanized monoclonal antibody which specifically binds to the C epsilon3 domain of IMMUNOGLOBULIN E, the site of high-affinity IgE receptor binding. It inhibits the binding of IgE to MAST CELLS and BASOPHILS to reduce the severity of the allergic response and is used in the management of persistent allergic ASTHMA.


Tucidinostat

An orally bioavailable benzamide-type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Chidamide binds to and inhibits HDACs, leading to an increase of acetylation levels of histone proteins. This agent also inhibits the expression of kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. HDACs, a class of enzymes that deacetylate chromatin histone proteins, are upregulated in many tumor types and play key roles in gene expression. Compared to some other benzamide-type HDAC inhibitors, chidamide is more stable, more resistant to degradation and has a longer half-life.


INFLIXIMAB

Infliximab products neutralize the biological activity of TNF-alpha by binding with high affinity to the soluble and transmembrane forms of TNF-alpha and inhibit binding of TNF-alpha with its receptors. Infliximab products do not neutralize TNF-beta (lymphotoxin-alpha), a related cytokine that utilizes the same receptors as TNF-alpha. Biological activities attributed to TNF-alpha include: induction of pro-inflammatory cytokines such as interleukins (IL) 1 and 6, enhancement of leukocyte migration by increasing endothelial layer permeability and expression of adhesion molecules by endothelial cells and leukocytes, activation of neutrophil and eosinophil functional activity, induction of acute phase reactants and other liver proteins, as well as tissue degrading enzymes produced by synoviocytes and/or chondrocytes. Cells expressing transmembrane TNF-alpha bound by infliximab products can be lysed in vitro or in vivo. Infliximab products inhibit the functional activity of TNF-alpha in a wide variety of in vitro bioassays utilizing human fibroblasts, endothelial cells, neutrophils, B and T-lymphocytes and epithelial cells. The relationship of these biological response markers to the mechanism(s) by which infliximab products exert their clinical effects is unknown. Anti-TNF-alpha antibodies reduce disease activity in the cotton-top tamarin colitis model, and decrease synovitis and joint erosions in a murine model of collagen-induced arthritis. Infliximab products prevent disease in transgenic mice that develop polyarthritis as a result of constitutive expression of human TNF-alpha, and when administered after disease onset, allow eroded joints to heal.


RITUXIMAB

A murine-derived monoclonal antibody and ANTINEOPLASTIC AGENT that binds specifically to the CD20 ANTIGEN and is used in the treatment of LEUKEMIA; LYMPHOMA and RHEUMATOID ARTHRITIS.


GEMTUZUMAB OZOGAMICIN

Immunotoxin that consists of an anti-CD33 (CD33 ANTIGEN) monoclonal antibody conjugated to CALICHEAMICIN. It is used for the treatment of ACUTE MYELOID LEUKEMIA.


INSULIN ASPART PROTAMINE RECOMBINANT

Insulin that has been modified to contain an ASPARTIC ACID instead of a PROLINE at position 38 of the B-chain.


vedolizumab

a humanized monoclonal antibody that targets the 4beta7 integrin exclusively, and modulates inflammation in the gastrointestinal tract


OBINUTUZUMAB

anti-CD20 mAb for treating B-cell lymphoid cancers


IBRITUMOMAB TIUXETAN

90Y-labeled anti-CD20 monoclonal antibody for radioimmunotherapy for patients with relapsed B-cell non-Hodgkin's lymphoma


Insulin detemir

A recombinant long-acting insulin and hypoglycemic agent in which a MYRISTIC ACID is conjugated to a LYSINE at position B29. It is used to manage BLOOD GLUCOSE levels in patients with DIABETES MELLITUS.


Vonoprazan

a potassium-competitive proton pump blocker for the treatment of acid-related disorders. Its potential to combat cytokine release syndrome (CRS) in patients with severely ill COVID-19 was investigated. Accordingly, it is recommended to use tocilizumabin combination with dexamethasone (or another corticosteroid at an equivalent dose) in certain hospitalized patients who are exhibiting rapid respiratory decompensation caused by COVID-19.


Eluxadoline

Eluxadoline is a mu-opioid receptor agonist; eluxadoline is also a delta opioid receptor antagonist and a kappa opioid receptor agonist. The binding affinities (Ki) of eluxadoline for the human mu and delta opioid receptors are 1.8 nM and 430 nM, respectively. The binding affinity (Ki) of eluxadoline for the human kappa opioid receptor has not been determined; however, the Ki for guinea pig cerebellum kappa opioid receptor is 55 nM. In animals, eluxadoline interacts with opioid receptors in the gut.


insulin lispro

Insulin that has been modified so that the B-chain contains a LYSINE at position 28 instead of a PROLINE and a PROLINE at position 29 instead of a LYSINE. It is used to manage BLOOD GLUCOSE levels in patients with TYPE 2 DIABETES.


INSULIN SUSP ISOPHANE RECOMBINANT HUMAN

Insulin (51 aa, ~6 kDa) is encoded by the human INS gene. This protein is involved in the direct regulation of glucose metabolism.


Rebamipide

Rebamipide is a mucosal protective agent and is postulated to increase gastric blood flow, prostaglandin biosynthesis and decrease free oxygen radicals.


Cholecystokinin

A peptide, of about 33 amino acids, secreted by the upper INTESTINAL MUCOSA and also found in the central nervous system. It causes gallbladder contraction, release of pancreatic exocrine (or digestive) enzymes, and affects other gastrointestinal functions. Cholecystokinin may be the mediator of satiety.


Eledoisin

A peptide extracted from the posterior salivary glands of certain small octopi (Eledone spp., Mollusca), or obtained by synthesis. Its actions resemble those of SUBSTANCE P; it is a potent vasodilator and increases capillary permeability. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1364)


Cangrelor

Cangrelor is a direct P2Y12 platelet receptor inhibitor that blocks ADP-induced platelet activation and aggregation. Cangrelor binds selectively and reversibly to the P2Y12 receptor to prevent further signaling and platelet activation.


Buformin

An oral hypoglycemic agent that inhibits gluconeogenesis, increases glycolysis, and decreases glucose oxidation.


mecasermin

Recombinant form of endogenous Insulin-like Growth Factor 1 exhibiting mitogenic activity. Clinical Use: Diabetes Mellitus and Amyotrophic Lateral Sclerosis.


Amineptine

used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure


Deoxycholic acid

A bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent.


ocriplasmin

consists or two polypeptide chains connected by disulfide bonds; one chain is the B chain of plasmin consisting of 230 amino acids, the other peptide is the COOH-terminal portion of the A chain of plasmin consisting of 31 amino acid residues; MW 28.635kDa


Lumacaftor

Lumacaftor improves the conformational stability of F508del-CFTR, resulting in increased processing and trafficking of mature protein to the cell surface.


Ivacaftor

Ivacaftor is a potentiator of the CFTR protein. The CFTR protein is a chloride channel present at the surface of epithelial cells in multiple organs. Ivacaftor facilitates increased chloride transport by potentiating the channel-open probability (or gating) of the CFTR protein.


ALDESLEUKIN

a recombinant human IL-2, marketed for the treatment of metastatic renal cell carcinoma; BAY 50-4798 is a variant


Piribedil

A dopamine D2 agonist. It is used in the treatment of parkinson disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist.


TROPISETRON

An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.


sebelipase alfa

a recombinant form of human lysosomal acid lipase (rhLAL)


alglucosidase alfa

Defects in the gene for this protein cause glycogen storage disease II, also known as Pompe disease, RefSeq NM_000152


MOGAMULIZUMAB

a defucosylated humanized anti-CCR4 antibody under phase I clinical trials (2010)


Thiocolchicoside

used in combination with glafenine and meprobamate to tranquilize patients undergoing hysterosalpingography; structure


Hyaluronidase

An enzyme that catalyzes the random hydrolysis of 1,4-linkages between N-acetyl-beta-D-glucosamine and D-glucuronate residues in hyaluronate. (From Enzyme Nomenclature, 1992) There has been use as ANTINEOPLASTIC AGENTS to limit NEOPLASM METASTASIS.


PROTAMINE SULFATE

A group of simple proteins that yield basic amino acids on hydrolysis and that occur combined with nucleic acid in the sperm of fish. Protamines contain very few kinds of amino acids. Protamine sulfate combines with heparin to form a stable inactive complex; it is used to neutralize the anticoagulant action of heparin in the treatment of heparin overdose. (From Merck Index, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p692)


ergoloid mesylates

A mixture of the mesylates (methane sulfonates) of DIHYDROERGOCORNINE; DIHYDROERGOCRISTINE; and the alpha- and beta-isomers of DIHYDROERGOCRYPTINE. The substance produces a generalized peripheral vasodilation and a fall in arterial pressure and has been used to treat symptoms of mild to moderate impairment of mental function in the elderly.


CARIPRAZINE

The efficacy of cariprazine could be mediated through a combination of partial agonist activity at central dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors.


technetium (99mTc) nofetumomab merpentan

a Fab fragment of the murine pancarcinoma antibody NR-LU-10 labeled with Tc-99m; used as a diagnostic imaging agent in staging patients with lung cancer


Chymotrypsin

A serine endopeptidase secreted by the pancreas as its zymogen, CHYMOTRYPSINOGEN and carried in the pancreatic juice to the duodenum where it is activated by TRYPSIN. It selectively cleaves aromatic amino acids on the carboxyl side.


somatrem

was MH (1997-2002), demoted; an analog of the synthetic human growth hormone (human somatropin) in which a methionyl amino-acid residue is added. It may be produced in bacteria from recombinant DNA. It is used in therapy for growth hormone deficiency. Do not confuse somatrem with sometribove (methionyl bovine somatotropin).


Sucrase

A glycoside hydrolase found primarily in PLANTS and YEASTS. It has specificity for beta-D-fructofuranosides such as SUCROSE.


RETEPLASE

mutant form of tissue plasminogen activator used in treatment of myocardial infarct


Aripiprazole lauroxil

prodrug of aripiprazole, following intramuscular injection is converted by enzyme-mediated hydrolysis to N-hydroxymethyl aripiprazole which is then hydrolyzed to aripiprazole


Terodiline

Terodiline relaxes the smooth muscle and used to reduce bladder tone in treatment of urinary frequency and incontinence. Muscle relaxation caused by terodiline, is probably due to its anticholinergic and calcium antagonist activity


Glymidine

was MH 1975-92 (see under SULFONAMIDES 1975-90); GLIDIAZINE & GLYCODIAZINE were see GLYMIDINE 1975-92; use SULFONAMIDES to search GLYMIDINE 1975-92; a sulfonamide hypoglycemic agent which stimulates insulin secretion


idarucizumab

an anticoagulant reversal agent that targets dabigatran


Drug-induced coagulation inhibitor disorder


insulin glulisine

Insulin glulisine [rDNA origin] is a rapid-acting human insulin analog used to lower blood glucose. Insulin glulisine is produced by recombinant DNA technology utilizing a non-pathogenic laboratory strain of Escherichia coli (K12). Insulin glulisine differs from human insulin in that the amino acid asparagine at position B3 is replaced by lysine and the lysine in position B29 is replaced by glutamic acid.


mepolizumab

Mepolizumab is an interleukin-5 antagonist (IgG1 kappa). IL-5 is the major cytokine responsible for the growth and differentiation, recruitment, activation, and survival of eosinophils. Mepolizumab binds to IL-5 with a dissociation constant of 100 pM, inhibiting the bioactivity of IL-5 by blocking its binding to the alpha chain of the IL-5 receptor complex expressed on the eosinophil cell surface.


Vinpocetine

whole issue of Arzneim Forsch (23 articles) discuss this drug; Arzneim Forsch 26(10a);1976; RN given refers to parent cpd with unspecified isomeric designation


Osimertinib

Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) at approximately 9-fold lower concentrations than wild-type. In cultured cells and animal tumor implantation models, osimertinib exhibited anti-tumor activity against NSCLC lines harboring EGFR-mutations (T790M/L858R, L858R, T790M/exon 19 deletion, and exon 19 deletion) and, to a lesser extent, wild-type EGFR amplifications.


Bencyclane

A vasodilator agent found to be effective in a variety of peripheral circulation disorders. It has various other potentially useful pharmacological effects. Its mechanism may involve block of calcium channels.


Clomethiazole

A sedative and anticonvulsant often used in the treatment of alcohol withdrawal. Chlormethiazole has also been proposed as a neuroprotective agent. The mechanism of its therapeutic activity is not entirely clear, but it does potentiate GAMMA-AMINOBUTYRIC ACID receptors response and it may also affect glycine receptors.


Dichloroacetic acid

A derivative of ACETIC ACID that contains two CHLORINE atoms attached to its methyl group.


PATIROMER

binds potassium ions in the gastrointestinal tract to lower serum potassium levels


Ferric maltol

potential use as an oral therapy for iron deficiency anemia


Selexipag

an oral prostacyclin receptor (IP receptor) agonist that is structurally distinct from prostacyclin, indicated for the treatment of pulmonary arterial hypertension, selexipag is hydrolyzed by carboxylesterase 1 to yield its active metabolite, which is approximately 37-fold as potent as selexipag, selexipag and the active metabolite are selective for the IP receptor versus other prostanoid receptors (EP1-4, DP, FP and TP)


Lobeglitazone

putative antidiabetic agent for type 2 diabetes


Viloxazine

A morpholine derivative used as an antidepressant. It is similar in action to IMIPRAMINE. The mechanism of action of viloxazine in the treatment of ADHD is unclear; however, it is thought to be through inhibiting the reuptake of norepinephrine.


belatacept

Belatacept, a selective T-cell (lymphocyte) costimulation blocker, binds to CD80 and CD86 on antigen-presenting cells thereby blocking CD28 mediated costimulation of T lymphocytes. In vitro, belatacept inhibits T lymphocyte proliferation and the production of the cytokines interleukin-2, interferon-gamma, interleukin-4, and TNF-alfa. Activated T lymphocytes are the predominant mediators of immunologic rejection


A primary source of energy for living organisms. It is naturally occurring and is found in fruits and other parts of plants in its free state. It is used therapeutically in fluid and nutrient replacement.


Defibrotide

Single-stranded polydeoxyribonucleotide extracted from mammalian organs and used in the treatment of HEPATIC VENO-OCCLUSIVE DISEASE in patients with kidney or lung abnormalities following HEMATOPOIETIC STEM CELL TRANSPLANTATION. The compound is a sodium salt.


OBILTOXAXIMAB

A monoclonal antibody that neutralizes toxins produced by BACILLUS ANTHRACIS. It is used to treat inhalational ANTHRAX.


Thallous chloride TL-201

non-pyrogenic diagnostic radiopharmaceutical for intravenous administration


reslizumab

Reslizumab is an interleukin-5 antagonist (IgG4, kappa). IL-5 is the major cytokine responsible for the growth and differentiation, recruitment, activation, and survival of eosinophils. Reslizumab binds to IL-5 with a dissociation constant of 81 pM, inhibiting the bioactivity of IL-5 by blocking its binding to the alpha chain of the IL-5 receptor complex expressed on the eosinophil surface. Inflammation is an important component in the pathogenesis of asthma. Multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) are involved in inflammation. Reslizumab, by inhibiting IL-5 signaling, reduces the production and survival of eosinophils; however, the mechanism of reslizumab action in asthma has not been definitively established.


galsulfase

a recombinant form of N-acetylgalactosamine-4-sulfatase


SUTILAINS

used in treatment of burns; derived from filtration of cultures of a strain of Bacillus subtilis


Acrisorcin

A topical anti-fungal agent. Acrisorcin is comprised of two active ingredients, 9-aminoacridine and 4-hexylresorcinol, but its clinical use has been discontinued.


rilonacept

an anti-arthritis agent derived from IL-1R and IL-1RAcP


Nonoxinol

Nonionic surfactant mixtures varying in the number of repeating ethoxy (oxy-1,2-ethanediyl) groups. They are used as detergents, emulsifiers, wetting agents, defoaming agents, etc. Nonoxynol-9, the compound with 9 repeating ethoxy groups, is a spermatocide, formulated primarily as a component of vaginal foams and creams.


BERACTANT

a bovine lung extract that contains mostly phospholipids; modified by the addition of dipalmitoylphosphatidylcholine, palmitic acid, and tripalmitin


UROKINASE

A proteolytic enzyme that converts PLASMINOGEN to FIBRINOLYSIN where the preferential cleavage is between ARGININE and VALINE. It was isolated originally from human URINE, but is found in most tissues of most VERTEBRATES.


Migalastat

Migalastat is a pharmacological chaperone that is designed to selectively and reversibly bind with high affinity to the active sites of certain mutant forms of alpha-Gal A, the genotypes of which are referred to as amenable mutations. Migalastat binding stabilizes these mutant forms of alpha-Gal A in the endoplasmic reticulum and facilitates their proper trafficking to lysosomes where dissociation of migalastat restores alpha-Gal A activity, leading to the catabolism of GL-3 and related substrates.


Technetium ((sup 99m)Tc) Methylenediphosphonate

A radiopharmaceutical containing methylene diphosphonate (medronate; MDP) complexed with the gamma-emitting radionuclide technetium Tc 99m with radioisotopic activity and hydroxyapatite affinity. Upon intravenous administration, skeletal uptake of technetium Tc 99m methylene diphosphonate occurs as a function of skeletal blood flow and osteogenic activity. The MDP moiety of this agent has affinity for hydroxyapatite crystals in bone with abnormal accumulation at sites with increased osteoid mineralization; labeling of MDP with Tc 99m allows scintigraphic imaging of areas of abnormal osteogenesis associated with malignant bone lesions.


Sucroferric oxyhydroxide

an oral phosphate binder for treatment of hyperphosphatemia


Technetium (99mTc) sestamibi

A technetium imaging agent used to reveal blood-starved cardiac tissue during a heart attack.


Omega-3 carboxylic acid

Fish oil-derived free fatty acids including multiple omega-3 fatty acids, eicosapentaenoic acid [EPA] and docosahexaenoic acid [DHA] being the most abundant. The mechanism of action of omega-3-carboxylic acids is not completely understood. Potential mechanisms of action include inhibition of acyl-CoA:1,2-diacylglycerol acyltransferase, increased mitochondrial and peroxisomal beta-oxidation in the liver, decreased lipogenesis in the liver, and increased plasma lipoprotein lipase activity. Omega-3-carboxylic acids may reduce the synthesis of triglycerides in the liver because EPA and DHA are poor substrates for the enzymes responsible for TG synthesis, and EPA and DHA inhibit esterification of other fatty acids.


Ferric carboxymaltose

effective for treatment of postpartum anemia


alglucerase

modified form of human placental glucocerebrosidase; oligosaccharide units of glucocerebrosidase are sequentially deglycosylated to yield a mannose-terminated preparation which is targeted to the mannose lectin on the macrophage plasma membrane


ATEZOLIZUMAB

A monoclonal antibody that targets programmed death-ligand 1 (CD274 ANTIGEN) and is used to treat urothelial carcinoma, the most common type of bladder cancer.


CONESTAT ALFA

recombinant human complement component 1 (C1) esterase inhibitor (rhC1INH), is an analogue of human C1INH and is obtained from the milk of rabbits expressing the gene encoding for human C1INH, the amino acid sequence of conestat alfa is identical to that of endogenous C1INH


a radiotracer containing a synthetic amino acid analogue of L-leucine radiolabeled with fluorine F 18 with diagnostic imaging use


Velpatasvir

pan-genotypic NS5A inhibitor for the treatment of chronic genotype 1-6 hepatitis C virus (HCV) infection


Terguride

pronounced antifertility agent in rats; lactation suppressor in other species; serotonin antagonist; RN given refers to parent cpd; structure


Gallium Ga 68 dotatate

A radioactive diagnostic agent used for POSITRON EMISSION TOMOGRAPHY (PET) imaging of SOMATOSTATIN RECEPTOR positive neuroendocrine tumors and malignant abdominal paraganglioma.


Carbenoxolone

An agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise the drug is low in toxicity.


Mebhydrolin

see also record for mebhydroline, RN: 524-81-2


An opioid analgesic used similarly to MORPHINE in the control of moderate to severe pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1097)


NELTENEXINE

elastase inhibitor; may be useful for preventing pulmonary emphysema


Obeticholic acid

obeticholic acid is an agonist for FXR, a nuclear receptor expressed in the liver and intestine


Spiperone

A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.


Azidocillin

antibiotic similir to ampicillin; minor descriptor (75-86); on line & INDEX MEDICUS search PENICILLIN G/AA (75-86); RN given refers to (2S-(2alpha,5alpha,6beta(S*))-isomer)


Butriptyline

a tricyclic antianxiety and antidepressive agent similar to, but with less side effects than amitriptyline; minor descriptor (75-86); on line & INDEX MEDICUS search DIBENZOCYCLOHEPTENES (75-86); RN given refers to parent cpd


BUTYLSCOPOLAMINE

Antimuscarinic quaternary ammonium derivative of scopolamine used to treat cramps in gastrointestinal, urinary, uterine, and biliary tracts, and to facilitate radiologic visualization of the gastrointestinal tract.


Ethanol

A clear, colorless liquid rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in ALCOHOLIC BEVERAGES.


a tertiary hexanol with hypnotic/sedative and anticonvulsant effects, was used for the treatment of insomnia


Choline

A basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.


Betazole

A histamine H2 agonist used clinically to test gastric secretory function.


Meptazinol

A narcotic antagonist with analgesic properties. It is used for the control of moderate to severe pain.


epoetin beta

A recombinant therapeutic agent that is chemically identical to or similar to the endogenous cytokine human erythropoietin (EPO). Produced primarily by cells of the peritubular capillary endothelium of the kidney in response to hypoxia, circulating EPO binds to EPO receptors on the surface of committed erythroid progenitors in the bone marrow resulting in their replication and maturation into functional erythrocytes.


Endothal-disodium

A standardized enzyme concentrate containing the pancreatic enzymes, lipase, protease and amylase used in enzyme substitution therapy. Lipase, protease and amylase break down fat, protein, and starches, respectively in the small intestine, thereby promoting digestion. Pancrelipase is used to reduce malabsorption when the pancreas is unable to secrete sufficient amounts of these enzymes.


NADROPARIN CALCIUM

A low molecular weight heparin (LMWH) composed of a heterogeneous mixture of sulfated polysaccharide glycosaminoglycan chains obtained by depolymerisation of porcine mucosal sodium heparin, extraction/purification and conversion to the calcium salt. Nadroparin binds to antithrombin III (ATIII) and inhibits the activity of activated factor X (factor Xa), thereby inhibiting the final common pathway of the coagulation cascade and preventing the formation of a cross-linked fibrin clot


peginterferon alfa-2b

A covalent conjugate of recombinant interferon alpha, subtype 2b, and polyethylene glycol (PEG), used as an antiviral and antineoplastic agent. The biological activity of this agent is derived from its interferon alpha-2b protein moiety. Interferons alfa bind to specific cell-surface receptors, leading to the transcription and translation of genes whose protein products mediate antiviral, antiproliferative, anticancer, and immune-modulating effects. The PEG moiety lowers the clearance of interferon alpha-2b, thereby extending the duration of its therapeutic effects, but may also reduce the interferon-mediated stimulation of an immune response


METHOXY POLYETHYLENE GLYCOL-EPOETIN BETA

A pegylated form of recombinant human erythropoietin, a glycosylated protein naturally produced in the kidney that stimulates erythrocyte production in the bone marrow. Methoxypolyethylene glycol epoetin beta may reverse anemias induced by cancer therapy


MOROCTOCOG ALFA

Human coagulation factor VIII produced by recombinant DNA technology in Chinese hamster ovary (CHO) cells. Moroctocog alfa is a glycoprotein with 1438 amino acids with a sequence that is comparable to the 90 + 80 kDa form of factor VIII (i.e. B-domain deleted) and similar post-translational modifications to those of the plasma-derived molecule


LENOGRASTIM

A glycosylated form of a recombinant therapeutic agent which is chemically identical to or similar to an endogenous human granulocyte colony-stimulating factor (G-CSF). Produced endogenously by monocytes, fibroblasts, and endothelial cells, G-CSF binds to and activates specific cell surface receptors, stimulating neutrophil progenitor proliferation and differentiation and selected neutrophil functions.


Eldecalcitol

an analog of vitamin D for the treatment of osteoporosis


epoetin zeta

a copy of human erythropoietin and works in exactly the same way as the natural hormone to stimulate red blood cell production


Clopenthixol

A thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors.


Egualen

a stable azulene derivative, antiulcer agent


CALCIUM DOBESILATE

A drug used to reduce hemorrhage in diabetic retinopathy.


Cyclophosphamide

Precursor of an alkylating nitrogen mustard antineoplastic and immunosuppressive agent that must be activated in the LIVER to form the active aldophosphamide. It has been used in the treatment of LYMPHOMA and LEUKEMIA. Its side effect, ALOPECIA, has been used for defleecing sheep. Cyclophosphamide may also cause sterility, birth defects, mutations, and cancer.