U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1211 - 1220 of 4027 results

Mepenzolate is a postganglionic parasympathetic inhibitor. It decreases gastric acid and pepsin secretion and suppresses spontaneous contractions of the colon. It specifically antagonizes muscarinic receptors. Mepenzolate is marketed under the brand name CANTIL. CANTIL is indicated for use as adjunctive therapy in the treatment of peptic ulcer. It has not been shown to be effective in contributing to the healing of peptic ulcer, decreasing the rate of recurrence, or preventing complications.
Promazine (Sparine) is a phenothiazine neuroleptic used for short-term management of moderate to severe psychomotor agitation and treatment of agitation and restlessness in the elderly. Promazine is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors. Promazine's antipsychotic effect is due to antagonism at dopamine and serotonin type 2 receptors, with greater activity at serotonin 5-HT2 receptors than at dopamine type-2 receptors. This may explain the lack of extrapyramidal effects. Promazine does not appear to block dopamine within the tuberoinfundibular tract, explaining the lower incidence of hyperprolactinemia than with typical antipsychotic agents or risperidone. Antagonism at muscarinic receptors, H1-receptors, and alpha(1)-receptors also occurs with promazine. Promazine is not approved for human use in the United States. It is available in the US for veterinary use under the names Promazine and Tranquazine.
Iproniazid is a non-selective, irreversible monoamine oxidase inhibitor (MAO) of the hydrazine class. It was originally developed for the treatment of Tuberculosis, but in 1952, its antidepressant properties were discovered when researchers noted that patients given isoniazid became inappropriately happy. Iproniazid is no longer clinically prescribed and has been withdrawn due to incidences of hepatotoxicity.
Status:
US Previously Marketed
First approved in 1955
Source:
Vanquin by Parke-Davis
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pyrvinium (Viprynium) is an anthelmintic effective for pinworms. Pyrvinium is used in the treatment of enterobiasis caused by Enterobius vermicularis (pinworm). Pyrvinium has being shown to be a potent inhibitor of Wnt signaling (EC(50) of ∼10 nM). Pyrvinium binds all casein kinase 1 (CK1) family members in vitro at low nanomolar concentrations and pyrvinium selectively potentiates casein kinase 1α (CK1α) kinase activity. Pyrvinium pamoate (PP) is a potent noncompetitive inhibitor of the androgen receptor (AR). A noncompetitive AR inhibitor pyrvinium has significant potential to treat CRPC, including cancers driven by ligand-independent AR signaling.
Status:
US Previously Marketed
First approved in 1955

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Potassium Aminosalicylate is the potassium salt form of aminosalicylic acid, an analog of aminobenzoic acid used to treat tuberculosis. There are two mechanisms responsible for aminosalicylic acid's bacteriostatic action against Mycobacterium tuberculosis. Firstly, aminosalicylic acid inhibits folic acid synthesis (without potentiation with antifolic compounds). The binding of para-aminobenzoic acid to pteridine synthetase acts as the first step in the folic acid synthesis. Aminosalicylic acid binds pteridine synthetase with greater affinity than para-aminobenzoic acid, effectively inhibiting the synthesis of folic acid. As bacteria are unable to use external sources of folic acid, cell growth and multiplication slow. Secondly, aminosalicylic acid may inhibit the synthesis of the cell wall component, mycobactin, thus reducing iron uptake by M. tuberculosis. Specifically, Potassium Aminosalicylate is used to treat active drug-resistant tuberculosis together with other antituberculosis medications. Potassium Aminosalicylate t has also been used as a second line agent to sulfasalazine in people with inflammatory bowel disease such as ulcerative colitis and Crohn's disease.
Status:
US Previously Marketed
Source:
Synatan by Irwin, Neisler (Mallinckrodt)
(1955)
Source URL:
First approved in 1955
Source:
Synatan by Irwin, Neisler (Mallinckrodt)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


DEXTROAMPHETAMINE TANNATE is a salt of dextroamphetamine, amphetamine enantiomer. It is used as CNS stimulant in the treatment of attention deficit hyperactivity disorder.
Status:
US Previously Marketed
Source:
METATENSIN #2 by SANOFI AVENTIS US
(1982)
Source URL:
First approved in 1954

Class (Stereo):
CHEMICAL (ABSOLUTE)



Reserpine is an alkaloid, isolated from the Rauwolfia serpentina plant and developed by Ciba pharma. Reserpine was approved by FDA for the treatment of hypertension and psychotic disorders. The drug exerts its effect by blocking two vesicular monoamine transporters, VMAT1 and VMAT2. The blockade results in vesicles that lose their ability to store neurotransmitter molecules. Neurotransmitters, thus retained in cytosol, are then neutralized by MAO.
Status:
US Previously Marketed
First approved in 1954

Class (Stereo):
CHEMICAL (ABSOLUTE)



Digoxin is a cardiac glycoside derived from the purple foxglove flower. In 1785, the English chemist, botanist, and physician Sir William Withering published his findings that Digitalis purpurea could be used to treat cardiac dropsy (congestive heart failure; CHF). Digoxin has been in use for many years, but was not approved by the FDA for treatment of heart failure (HF) until the late 1990s. Another FDA indication for digoxin is atrial fibrillation (AF). Digoxin also has numerous off-label uses, such as in fetal tachycardia, supra-ventricular tachycardia, cor pulmonale, and pulmonary hypertension. Digitoxin inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations. Increased intracellular concentrations of calcium may promote activation of contractile proteins (e.g., actin, myosin). Digoxin also has Para sympathomimetic properties. By increasing vagal tone in the sinoatrial and atrioventricular (AV) nodes, it slows the heart rate and AV nodal conduction.
Status:
US Previously Marketed
Source:
Dactil by lakeside (MerrellNational)
(1954)
Source URL:
First approved in 1954
Source:
Dactil by lakeside (MerrellNational)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Piperidolate hydrochloride is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs. It’s usually used to kill the cramp-like pain of gastric/duodenal ulcer, gastritis, enteritis, gallstones, cholecystitis and biliary tract dyskinesia and to improve some symptoms in threatened miscarriage/premature delivery. Piperidolate blocked the contraction of ACh, Ba ++ and electrical stimulations on the isolated rat, mouse and guinea-pig ileum and trachea. In guinea-pig teania caeci, piperidolate like papaverine blocked specifically the tonic response, however, piperidolate in high doses completely blocked both spike and tonic responses. These results indicate that spasmolytic action of piperidolate like that of papaverine may depend upon inhibition of the release of store Ca++. Moreover piperidolate, given at high doses, may inhibit the contractile elements in the smooth muscle. In the rat uterus pretreated with sex hormones, piperidolate nonspecifically blocked the contraction of ACh, Ba ++ and oxytocin and sex hormones had no influence on the spasmolytic action of piperidolate.
Thiamylal is a barbiturate that is administered intravenously for the production of complete anesthesia of short duration, for the induction of general anesthesia, or for inducing a hypnotic state. Thiamylal, a barbiturate, is used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia. Thiamylal binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.

Showing 1211 - 1220 of 4027 results