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

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Showing 271 - 280 of 816 results

Tridihexethyl is a synthetic anticholinergic agent which was marketed under the brand name Pathilon as an adjunct in the treatment of peptic ulcer disease. However, it is no longer available in the US market. Tridihexethyl may block all three types of muscarinic receptors including M-1 receptors in the CNS and ganglia, M-2 receptors in the heart, and M-3 receptors. The muscarinic acetylcholine receptors mediate various cellular responses including inhibition of adenylate cyclase, the breakdown of phosphoinositides, and modulation of potassium channels through the action of G proteins. Tridihexethyl inhibits vagally mediated reflexes by antagonizing the action of acetylcholine. This, in turn, reduces the secretion of gastric acids in the stomach. Tridihexethyl was also examined for effect on patients with acquired nystagmus where four out of six patients showed improvement, but due to the profile usage of Tridihexethyl to treat nystagmus was limited.
Status:
US Previously Marketed
First approved in 1954
Source:
Ansolysen by Wyeth
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Pentolinium (brand name Ansolysen) is a ganglionic cholinergic antagonist, acting on alpha 3 beta 4 neuronal nicotinic acetylcholine receptors (nAChRs). It was used as an antihypertensive drug during surgery or to control hypertensive crises, but Ansolysen was discontinued. Pentolinium inhibits release of adrenaline and noradrenaline from adrenergic nerves.
Status:
US Previously Marketed
First approved in 1953

Class (Stereo):
CHEMICAL (RACEMIC)



CYCRIMINE is an antispasmodic drug used for the treatment of Parkinson's disease (PD). It binds the muscarinic acetylcholine receptor M1, effectively reducing levels of acetylcholine. This decrease in acetylcholine restores the normal dopamine-acetylcholine balance and relieves the symptoms of PD.
Status:
US Previously Marketed
Source:
CENTRINE/PHENOBARBITAL AMINOPENTAMIDE HYDROGEN SULFATE by BRISTOL LABS
(1961)
Source URL:
First approved in 1953
Source:
Centrine by Bristol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Aminopentamide is a potent antispasmodic agent. As a cholinergic blocking agent for smooth muscle, its action is similar to atropine. Aminopentamide hydrogen sulfate is marketed under the brand name Centrine indicated in the treatment of acute abdominal visceral spasm, pylorospasm or hypertrophic gastritis and associated nausea, vomiting and/or diarrhea of the dogs and cats. Centrine effectively reduces the tone and amplitude of colonic contractions to a greater degree and for a more extended period than does atropine. Centrine effects a reduction in gastric secretion, a decrease in gastric acidity and a marked decrease in gastric motility. Aminopentamide is a nonselective muscarinic cholinergic .
Status:
US Previously Marketed
Source:
Provell Maleate by Lilly
(1953)
Source URL:
First approved in 1953
Source:
Provell Maleate by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Protoveratrine A, the principal alkaloid of Veratrum album, has been used in the treatment of hypertension but has largely been replaced by drugs with fewer adverse effects.
Propantheline is an antimuscarinic agent used for the treatment of excessive sweating (hyperhidrosis), cramps or spasms of the stomach, intestines (gut) or bladder, and involuntary urination (enuresis). It can also be used to control the symptoms of irritable bowel syndrome and similar conditions. Propantheline is one of a group of antispasmodic medications which work by blocking the action of the chemical messenger acetylcholine, which is produced by nerve cells, to muscarinic receptors present in various smooth muscular tissues, in places such as the gut, bladder, and eye. Normally, the binding of acetylcholine induces involuntary smooth muscular contractions. Varying degrees of drying of salivary secretions may occur as well as decreased sweating. Ophthalmic side effects include blurred vision, mydriasis, cycloplegia, and increased ocular tension. Other reported adverse reactions include urinary hesitancy and retention, tachycardia, palpitations, loss of the sense of taste, headache, nervousness, mental confusion, drowsiness, weakness, dizziness, insomnia, nausea, vomiting, constipation, bloated feeling, impotence, suppression of lactation, and allergic reactions or drug idiosyncrasies including anaphylaxis, urticaria and other dermal manifestations.
Status:
US Previously Marketed
Source:
Parsidol HCl by Warner /Chilcott
(1953)
Source URL:
First approved in 1953
Source:
Parsidol HCl by Warner /Chilcott
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Ethopropazine is an anticholinergic drug. Ethopropazine is an inhibitor of butyrylcholinesterase and non-selective muscarinic acetylcholine receptor antagonist. Ethopropazine has been used for the treatment of parkinsonism and drug-induced extrapyramidal reactions. Also It used for the symptomatic treatment of hepatolenticular degeneration and congenital athetosis.
Status:
US Previously Marketed
Source:
Antrenyl Bromide by Ciba
(1952)
Source URL:
First approved in 1952
Source:
Antrenyl Bromide by Ciba
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Oxyphenonium bromide is a quaternary ammonium anticholinergic agent, which was used under brand name antrenyl, to relieve visceral spasms and as an adjunct in the treatment of peptic ulcer. In addition, Oxyphenonium inhibits gastrointestinal propulsive motility and decreases gastric acid secretion and controls excessive pharyngeal, tracheal and bronchial secretions. Action is achieved via a dual mechanism: a specific anticholinergic effect (antimuscarinic) at the acetylcholine-receptor sites and a direct effect upon smooth muscle. Oxyphenonium bromide also been used in the form of eye drops for mydriatic effec
Status:
US Previously Marketed
Source:
Quotane by Smith Kline & French
(1951)
Source URL:
First approved in 1951
Source:
Quotane by Smith Kline & French
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Dimethisoquin (also known as Quinisocaine and QUOTANE) is a topical anesthetic used as an antipruritic. It was shown that dimethisoquin inhibits nicotinic acetylcholine receptors (alpha4/beta4 and alpha4/beta2) with the maximum inhibition potency occurring for the α4β4 subtype.
Status:
US Previously Marketed
Source:
Flaxedil by Lederle
(1951)
Source URL:
First approved in 1951
Source:
Flaxedil by Lederle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Gallamine triethiodide is a synthetic nondepolarizing blocking drug, which is allosteric antagonist of muscarinic M2 acetylcholine receptor and inhibitor of acetylcholinesterase. It was used under brand name flaxedil to stabilize muscle contractions during surgical procedures. However, this usage was discontinued. It was shown, that gallamine caused tachycardia by depressing the vagus nerve and, occasionally, hypertension and increased cardiac output.

Showing 271 - 280 of 816 results