Benztropine
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Benztropine
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| Systematic (IUPAC) name | |
| 3-benzhydryloxy-8-methyl-8-azabicyclo[3.2.1]octane | |
| Identifiers | |
| CAS number | |
| ATC code | N04 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C21H25NO |
| Mol. mass | 307.429 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | 36 hours |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
C(US) |
| Legal status | |
| Routes | oral, IM, IV |
Benztropine mesylate (INN: benzatropine mesilate; marketed as Cogentin) is an anticholinergic drug principally used for the treatment of:
- Drug-induced parkinsonism, akathisia and acute dystonia;
- Parkinson disease; and
- Idiopathic or secondary dystonia.
Benztropine is a centrally acting anticholinergic agent with antihistaminic properties resulting from the combination of the tropine portion of the atropine molecule and the benzohydryl portion of diphenhydramine. Animal studies have indicated that anticholinergic activity of benztropine is approximately one-half that of atropine, while antihistaminic activity approaches that of pyrilamine. Its anticholinergic effects have been established as therapeutically significant in the management of parkinsonism. Benztrop antagonises the effect of acetylcholine, decreasing the imbalance between the neurotransmitters acetylcholine and dopamine, which may improve the symptoms of early Parkinson's disease. [1]
[edit] Indications
It is used in patients to reduce the side effects of antipsychotic treatment, such as parkinsonism and akathisia.
Benztropine is also a second-line drug for the treatment of Parkinson's disease. It improves tremor but not rigidity or bradykinesia.
Benztropine 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.
[edit] Side effects
These are principally anticholinergic:
- Dry mouth
- Blurred vision
- Cognitive changes
- Constipation
- Urinary retention
- Tachycardia
- Anorexia
- Psychosis (usually in overdose)
Some studies suggest that use of anticholinergics increases the risk of tardive dyskinesia, a long-term side effect of antipsychotics.[2][3]
Other studies have found no association between anticholinergic exposure and risk of developing tardive dyskinesia.[4]
[edit] References
- ^ MIMS Australia Pty Ltd. MIMS.
- ^ Arch Gen Psychiatry -- Abstract: Tardive dyskinesia: prevalence and risk factors, 1959 to 1979, April 1982, Kane and Smith 39 (4): 473. Retrieved on 2007-08-14.
- ^ Wszola BA, Newell KM, Sprague RL (2001). "Risk factors for tardive dyskinesia in a large population of youths and adults". Experimental and clinical psychopharmacology 9 (3): 285-96. doi:. PMID 11534539.
- ^ van Harten PN, Hoek HW, Matroos GE, Koeter M, Kahn RS (1998). "Intermittent neuroleptic treatment and risk for tardive dyskinesia: Curaçao Extrapyramidal Syndromes Study III". The American journal of psychiatry 155 (4): 565-7. PMID 9546009.
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