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Benzatropine

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Benzatropine
File:Benztropin.png
Clinical data
Routes of
administration		Oral, IM, IV
ATC code
Identifiers
  • (3-endo)-3-(diphenylmethoxy)-8-methyl-8-azabicyclo[3.2.1]octane
CAS Number
PubChem CID
DrugBank
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H25NO
Molar mass307.429 g/mol g·mol−1
3D model (JSmol)
  • CN4[C@@H]1CC[C@H]4C[C@H](C1)OC(c2ccccc2)c3ccccc3
  (verify)

Benzatropine (INN), also known as benztropine (USAN, BAN), is an anticholinergic marketed under the trade name Cogentin which is used in the treatment of Parkinson's disease, parkinsonism, akathisia, and dystonia.

Indications

Benzatropine 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.[1][2]

Other studies have found no association between anticholinergic exposure and risk of developing tardive dyskinesia.[3]

Pharmacology

Benztropine is a centrally acting anticholinergic/antihistamine agent 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 its antihistamine activity approaches that of mepyramine. 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. [4] Benztropine also acts as a dopamine reuptake inhibitor, which may further substantiate its efficacy in treating Parkinson's.[5]

References

  1. ^ "Arch Gen Psychiatry -- Abstract: Tardive dyskinesia: prevalence and risk factors, 1959 to 1979, April 1982, Kane and Smith 39 (4): 473". Retrieved 2007-08-14.
  2. ^ 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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  3. ^ 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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  4. ^ MIMS Australia Pty Ltd. MIMS.
  5. ^ Schmitt KC, Zhen J, Kharkar P; et al. (2008). "Interaction of cocaine-, benztropine-, and GBR12909-like compounds with wild-type and mutant human dopamine transporters: molecular features that differentially determine antagonist-binding properties". Journal of Neurochemistry. 107 (4): 928–40. doi:10.1111/j.1471-4159.2008.05667.x. PMC 2728472. PMID 18786172. {{cite journal}}: Explicit use of et al. in: |author= (help); Unknown parameter |month= ignored (help)CS1 maint: multiple names: authors list (link)


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