World Library  
Flag as Inappropriate
Email this Article

Benzatropine

Article Id: WHEBN0000185844
Reproduction Date:

Title: Benzatropine  
Author: World Heritage Encyclopedia
Language: English
Subject: Etybenzatropine, Thioridazine, Solanaceae, Cyproheptadine, Diphenylpyraline
Collection: Dopamine Reuptake Inhibitors, Ethers, Muscarinic Antagonists, Tardive Dyskinesia, Tropanes
Publisher: World Heritage Encyclopedia
Publication
Date:
 

Benzatropine

Benzatropine
Systematic (IUPAC) name
(3-endo)-3-(Diphenylmethoxy)-8-methyl-8-azabicyclo[3.2.1]octane
Clinical data
Trade names Cogentin
AHFS/Drugs.com
Pregnancy
category
  • US: C (Risk not ruled out)
Legal status
Routes of
administration
Oral, IM, IV
Pharmacokinetic data
Metabolism Hepatic
Biological half-life 12-24 hours
Excretion Urine
Identifiers
CAS Registry Number  Y
ATC code N04
PubChem CID:
IUPHAR/BPS
DrugBank  N
ChemSpider  Y
UNII  Y
ChEBI  Y
ChEMBL  N
Synonyms Benztropine
Chemical data
Formula C21H25NO
Molecular mass 307.429 g/mol
 N   

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, and dystonia.

Contents

  • Medical uses 1
  • Adverse effects 2
  • Pharmacology 3
  • See also 4
  • References 5

Medical uses

Benzatropine is an anticholinergic drug used in patients to reduce the side effects of antipsychotic treatment. Benzatropine is also a second-line drug for the treatment of Parkinson's disease. It improves tremor, but not 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.

Adverse effects

These are principally anticholinergic:

While 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] although symptoms may be worsened.[4]

Drugs that decrease cholinergic transmission may impair storage of new information into long-term memory. Anticholinergic agents can also impair time perception.[5]

Pharmacology

Benzatropine is a centrally acting anticholinergic/antihistamine agent. It is a selective M1 muscarinic acetylcholine receptor antagonist. Benztropine 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.[6]

Benzatropine analogues are atypical dopamine reuptake inhibitors,[7] which might make them useful for people with extrapyramidal symptoms who take antipsychotics.

Benzatropine also acts as a functional inhibitor of acid sphingomyelinase (FIASMA).[8]

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.[9]

See also

References

  1. ^ Kane JM, Smith JM (1982). "Tardive dyskinesia: Prevalence and risk factors, 1959 to 1979". Archives of General Psychiatry 39 (4): 473–81.  
  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.  
  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.  
  4. ^ Yassa R (1988). "Tardive dyskinesia and anticholinergic drugs. A critical review of the literature". L'Encephale 14 (Spec No): 233–9.  
  5. ^ Gelenberg AJ, Van Putten T, Lavori PW, Wojcik JD, Falk WE, Marder S, Galvin-Nadeau M, Spring B, Mohs RC, Brotman AW. (1989). "Anticholinergic effects on memory: benztropine versus amantadine.". Clinical Psychopharmacology 9 (3): 180–5.  
  6. ^ MIMS Australia Pty Ltd. MIMS.
  7. ^ Hiranita T, Kohut SJ, Soto PL, Tanda G, Kopajtic TA, Katz JL. (2014). "Preclinical efficacy of N-substituted benztropine analogs as antagonists of methamphetamine self-administration in rats". J Pharmacol Exp Ther. 348 (1): 174–91.  
  8. ^ Kornhuber J, Muehlbacher M, Trapp S, Pechmann S, Friedl A, Reichel M, Mühle C, Terfloth L, Groemer T, Spitzer G, Liedl K, Gulbins E, Tripal P (2011). "Identification of novel functional inhibitors of acid sphingomyelinase". PLoS ONE 6 (8): e23852.  
  9. ^ Deshmukh VA, Tardif V, Lyssiotis CA, Green CC, Kerman B, Kim HJ, Padmanabhan K, Swoboda JG, Ahmad I, Kondo T, Gage FH, Theofilopoulos AN, Lawson BR, Schultz PG, Lairson LL. (2013). "A regenerative approach to the treatment of multiple sclerosis". Nature 502 (7471): 327–332.  
This article was sourced from Creative Commons Attribution-ShareAlike License; additional terms may apply. World Heritage Encyclopedia content is assembled from numerous content providers, Open Access Publishing, and in compliance with The Fair Access to Science and Technology Research Act (FASTR), Wikimedia Foundation, Inc., Public Library of Science, The Encyclopedia of Life, Open Book Publishers (OBP), PubMed, U.S. National Library of Medicine, National Center for Biotechnology Information, U.S. National Library of Medicine, National Institutes of Health (NIH), U.S. Department of Health & Human Services, and USA.gov, which sources content from all federal, state, local, tribal, and territorial government publication portals (.gov, .mil, .edu). Funding for USA.gov and content contributors is made possible from the U.S. Congress, E-Government Act of 2002.
 
Crowd sourced content that is contributed to World Heritage Encyclopedia is peer reviewed and edited by our editorial staff to ensure quality scholarly research articles.
 
By using this site, you agree to the Terms of Use and Privacy Policy. World Heritage Encyclopedia™ is a registered trademark of the World Public Library Association, a non-profit organization.
 


Copyright © World Library Foundation. All rights reserved. eBooks from Project Gutenberg are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.