Benzatropine
Clinical data | |
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Trade names | Cogentin, others |
Other names | benzatropine (BAN UK), benztropine (USAN US) |
AHFS/Drugs.com | Monograph |
License data |
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Pregnancy category |
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Routes of administration | By mouth, IM, IV |
ATC code | |
Legal status | |
Legal status |
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Pharmacokinetic data | |
Metabolism | Liver |
Elimination half-life | 12–24 hours |
Excretion | Urine |
Identifiers | |
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Benzatropine (
Common side effects include dry mouth, blurry vision, nausea, and constipation.
Benzatropine was approved for medical use in the United States in 1954.
Medical uses
Benzatropine is used to reduce
, a rare disorder that causes abnormal muscle contraction, resulting in twisting postures of limbs, trunk, or face.Adverse effects
These are principally anticholinergic:
- Dry mouth
- Blurred vision
- Cognitive changes
- Drowsiness
- Constipation
- Urinary retention
- Tachycardia
- Anorexia
- Severe hallucinations(in overdose)
While some studies suggest that use of anticholinergics increases the risk of tardive dyskinesia (a long-term side effect of antipsychotics),[10][11] other studies have found no association between anticholinergic exposure and risk of developing tardive dyskinesia,[12] although symptoms may be worsened.[13]
Drugs that decrease cholinergic transmission may impair storage of new information into long-term memory. Anticholinergic agents can also impair time perception.[14]
Pharmacology
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.[15]
Benzatropine analogues are atypical
Benzatropine also acts as a functional inhibitor of acid sphingomyelinase (FIASMA).[18]
Benzatropine has been also identified, by a high throughput screening approach, as a potent differentiating agent for
Other animals
In veterinary medicine, benzatropine is used to treat priapism in stallions.[20]
Naming
Since 1959, benzatropine is the official
"Benztropine" is the official United States Adopted Name (USAN), the medication naming system coordinated by the USAN Council, co-sponsored by the American Medical Association (AMA), the United States Pharmacopeial Convention (USP), and the American Pharmacists Association (APhA). It is also the Japanese Accepted Name (JAN)[22] and was used in Australia until 2015, when it was harmonized with the INN.[21]
Both names may be modified to account for the
The misspelling benzotropine is also occasionally seen in the literature.
See also
- Gaboxadol
- Propantheline bromide
- Glycopyrrolate
- Oxybutynin
References
- ^ a b World Health Organization (December 1959). "International Non-Proprietary Names for Pharmaceutical Preparations). Recommended International Non-Proprietary Names (Rec. I.N.N.): List 3º" (PDF). WHO Chronicle. 13 (12): 464. Retrieved 2020-12-01.
- ^ a b c World Health Organization. "INN: Benzatropine". WHO MedNet. Retrieved 2020-12-01.[permanent dead link]
- ^ a b c d e f g h i "Benztropine Mesylate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 9 April 2019.
- ISBN 9780876309568.
- ISBN 9780781765879.
- ^ "Benztropine (Cogentin) Use During Pregnancy". Drugs.com. Retrieved 9 April 2019.
- ^ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
- ^ "Benztropine - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
- PMID 5066.
- S2CID 10194153.
- PMID 11534539.
- PMID 9546009.
- PMID 3063514.
- S2CID 27308127.
- ^ MIMS Australia Pty Ltd. MIMS.
- PMID 24194527.
- PMID 8290678.
- PMID 21909365.
- PMID 24107995.
- PMID 1752772.
- ^ a b "Updating medicine ingredient names - list of affected ingredients". Therapeutic Goods Administration. 2015-11-23. Retrieved 2020-12-01.
- ^ a b Compound D00778 at KEGG Pathway Database.
- ISBN 978-0-85369-840-1.
External links
- "Benzatropine". Drug Information Portal. U.S. National Library of Medicine.