Benztropine

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Benztropine
Systematic (IUPAC) name
3-benzhydryloxy-8-methyl-8-azabicyclo[3.2.1]octane
Identifiers
CAS number 86-13-5
ATC code N04AC01
PubChem 1201549
DrugBank APRD00748
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:

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. Benztropine 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]

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. 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.

Side effects

These are principally anticholinergic:

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]

References

  1. ^ MIMS Australia Pty Ltd. MIMS.
  2. ^ "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.
  3. ^ 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:10.1037/1064-1297.9.3.285. PMID 11534539. 
  4. ^ 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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  • This page was last modified on 17 August 2008, at 02:15.

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