|Trade names||Cogentin, others|
|Other names||Benztropine, benztropine (BAN UK), benztropine (USAN US)|
|Main uses||Dystonia, parkinsonism|
|Side effects||Dry mouth, blurry vision, nausea, constipation|
|By mouth, IM, IV|
|Defined daily dose||2 mg|
|Elimination half-life||12-24 hours|
|Chemical and physical data|
|Molar mass||307.437 g·mol−1|
|3D model (JSmol)|
Benzatropine, sold under the brand name Cogentin among others, is a medication used to treat a type of movement disorder due to antipsychotics known as dystonia and parkinsonism. It is not useful for tardive dyskinesia. It is taken by mouth or by injection into a vein or muscle. Benefits are seen within two hours and last for up to ten hours.
Common side effects include dry mouth, blurry vision, nausea, and constipation. Serious side effect may include urinary retention, hallucinations, hyperthermia, and poor coordination. It is unclear if use during pregnancy or breastfeeding is safe. Benzatropine is an anticholinergic which works by blocking the activity of the muscarinic acetylcholine receptor.
Benzatropine was approved for medical use in the United States in 1954. It is available as a generic medication. In the United States the wholesale cost is about US$6 per month. In 2017, it was the 226th most commonly prescribed medication in the United States, with more than two million prescriptions.
Benzatropine is used to reduce extrapyramidal side effects of antipsychotic treatment. Benzatropine is also a second-line drug for the treatment of Parkinson's disease. It improves tremor, and may alleviate rigidity and bradykinesia. Benzatropine is also sometimes used for the treatment of dystonia, a rare disorder that causes abnormal muscle contraction, resulting in twisting postures of limbs, trunk, or face.
These are principally anticholinergic:
- Dry mouth
- Blurred vision
- Cognitive changes
- Urinary retention
- Fast heartrate
- Loss of appetite
- Delirium and hallucinations (in overdose)
While some studies suggest that use of anticholinergics increases the risk of tardive dyskinesia (a long-term side effect of antipsychotics), other studies have found no association between anticholinergic exposure and risk of developing tardive dyskinesia, although symptoms may be worsened.
Drugs that decrease cholinergic transmission may impair storage of new information into long-term memory. Anticholinergic agents can also impair time perception.
Benzatropine is a centrally acting anticholinergic/antihistamine agent. It is a selective M1 muscarinic acetylcholine receptor antagonist. Benzatropine partially blocks cholinergic activity in the basal ganglia and has also been shown to increase the availability of dopamine by blocking its reuptake and storage in central sites, and as a result, increasing dopaminergic activity. Animal studies have indicated that anticholinergic activity of benzatropine is approximately one-half that of atropine, while its antihistamine activity approaches that of mepyramine. Its anticholinergic effects have been established as therapeutically significant in the management of Parkinsonism. Benzatropine antagonizes the effect of acetylcholine, decreasing the imbalance between the neurotransmitters acetylcholine and dopamine, which may improve the symptoms of early Parkinson's disease.
Benzatropine has been also identified, by a high throughput screening approach, as a potent differentiating agent for oligodendrocytes, possibly working through M1 and M3 muscarinic receptors. In preclinical models for multiple sclerosis, benzatropine decreased clinical symptoms and enhanced re-myelination.
Society and culture
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