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

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Showing 21 - 30 of 56 results

Biperiden, sold under the brandname Akineton was used as an adjunct in the therapy of all forms of parkinsonism (postencephalitic, arteriosclerotic and idiopathic). Was also useful in the control of extrapyramidal disorders due to central nervous system drugs such as phenothiazines and other groups of psychotropics. Biperiden is a weak peripheral anticholinergic agent. It has, therefore, some antisecretory, antispasmodic and mydriatic effects. In addition, biperiden possesses nicotinolytic activity. Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as biperiden is considered to relate to competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance. Atropine-like side effects such as dry mouth; blurred vision; drowsiness; euphoria or disorientation; urinary retention; postural hypotension; constipation; agitation; disturbed behavior may been seen. Only limited pharmacokinetic studies of biperiden in humans are available.
Status:
US Previously Marketed
Source:
RABELLON HYOSCYAMINE HYDROBROMIDE by MSD
(1961)
Source URL:
First marketed in 1921
Source:
Hyoscyamine Hydrobromide U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Hyoscyamine as a natural plant alkaloid derivative and anticholinergic. Hyoscyamine is used to treat a variety of stomach/intestinal problems such as cramps and irritable bowel syndrome. It is also used to treat other conditions such as bladder and bowel control problems, cramping pain caused by kidney stones and gallstones, and Parkinson's disease. In addition, it is used to decrease side effects of certain medications (drugs used to treat myasthenia gravis) and insecticides. Hyoscyamine inhibits specifically the actions of acetylcholine on structures innervated by postganglionic cholinergic nerves and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. These peripheral cholinergic receptors are present in the autonomic effector cells of the smooth muscle, cardiac muscle, the sinoatrial node, the atrioventricular node, and the exocrine glands. At therapeutic doses, it is completely devoid of any action on autonomic ganglia. Side effects include dry mouth and throat, increased appetite leading to weight gain, eye pain, blurred vision, restlessness, dizziness, arrhythmia, flushing, and faintness. Additive adverse effects resulting from cholinergic blockade may occur when hyoscyamine is administered concomitantly with other antimuscarinics, amantadine, haloperidol, phenothiazines, monoamine oxidase (MAO) inhibitors, tricyclic antidepressants or some antihistamines.
Status:
US Previously Marketed
Source:
METROPINE METHYLATROPINE NITRATE by PENWALT
(1961)
Source URL:
First marketed in 1911
Source:
Eumydrin by Bayer
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



Methylatropine (methylatroponium) is a belladonna derivative. In 1902 the Bayer Company introduced atropine methonitrate, a quaternary ammonium salt of atropine (Eumydrin), as a mydriatic for dilation of the pupil during ophthalmic examination. Due to its highly polar nature it penetrates less readily into the central nervous system than atropine and was therefore introduced for relieving pyloric spasms in infants. Atropine methyl nitrate is a muscarinic acetylcholine receptor antagonist that does not cross the blood-brain barrier. Atropine methyl nitrate has been used for its peripheral muscarinic effects (targeting the bladder, respiratory tract, and to block parasympathetic signaling to the heart, among others) and to separate central from peripheral nervous system effects, or to protect against peripheral side effects when using muscarinics that do cross the blood brain barrier.
Status:
Possibly Marketed Outside US
Source:
Sultroponium-B by Biotherax [France]
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Sultroponium is an antispasmodic without strong side effects. It is a powerful neurotropic spasmolytic anticholinergic agent.
Status:
Possibly Marketed Outside US
Source:
Xenytropium bromide by Licencia Budapest
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Xenytropium is a quaternary ammonium derivative of atropine. It combines antimuscarinic and ganglionic blocking potencies. It was marketed in Eastern Europe under trade name Gastripon for the treatment of gastritis, gastric and duodenal ulcers, gallstone diseases, and other conditions.
Status:
Possibly Marketed Outside US
Source:
Canada:TRICHLORFON
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Trichlorfon (Metrifonate), the organophosphorous cholinesterase inhibitor, O,O-dimethylhydroxy-2,2,2-trichlorethyl-phosphonate, has been used sporadically in the treatment of human schistosomiasis for a decade. It has selective and variable schistosomicidal activity against S. haematobium that results from its partial metabolism to a highly active anti-cholinesterase, dichlorvos. Schistosomal cholinesterase is more susceptible to this metabolite than that of the human host, but transient reductions in both plasma and erythrocyte cholinesterase activity are demonstrable at therapeutic dosage. However, despite early concerns about its potential toxicity, metrifonate is well tolerated and has been used effectively and extensively in large-scale control programmes. Its potential to enhance central nervous system cholinergic neurotransmission led to clinical trials for the treatment of people with Alzheimer's disease (AD).
mixture
Status:
Possibly Marketed Outside US
Source:
Octaplasma by Octapharma Pharmazeutika Produktionsges M B H [Canada]
Source URL:

Class:
MIXTURE

Showing 21 - 30 of 56 results