Drug/Small Molecule:
benztropine

2D structure

Overview

Generic Names: Benzatropina [INN-Spanish]; Benzatropine; Benzatropine mesilate; Benzatropinum [INN-Latin]; Benztropine Mesylate; Benztropinum; Tropine Benzohydryl Ether
Trade Names: Akitan; Apo-Benztropine; Cobrentin; Cogentin; Cogentine; Cogentinol; PMS Benztropine
PharmGKB Accession Id: PA448591

Description

A centrally active muscarinic antagonist that has been used in the symptomatic treatment of parkinson disease. Benztropine also inhibits the uptake of dopamine. PubChem (source: Drug Bank)

Indication

For use as an adjunct in the therapy of all forms of parkinsonism and also for use in the control of extrapyramidal disorders due to neuroleptic drugs. (source: Drug Bank)

ATC Therapeutic Category

  • N04AC:Ethers of tropine or tropine derivatives

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Benztropine is a selective M1 muscarinic acetylcholine receptor antagonist. It is able to discriminate between the M1 (cortical or neuronal) and the peripheral muscarinic subtypes (cardiac and glandular). Benztropine partially blocks cholinergic activity in the CNS, which is responsible for the symptoms of Parkinson's disease. It is also thought to increase the availability of dopamine, a brain chemical that is critical in the initiation and smooth control of voluntary muscle movement. (source: Drug Bank)

Pharmacology

Benztropine is an anticholinergic used in the symptomatic treatment of all etiologic groups of parkinsonism and drug induced extrapyramidal reactions (except tardive dyskinesia). Benztropine possesses both anticholinergic and antihistaminic effects, although only the former has been established as therapeutically significant in the management of parkinsonism. Benztropine's anticholinergic activity is about equal to that of atropine. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Take with food to reduce irritation. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Toxicity

Signs of overdose include confusion, nervousness, listlessness, hallucinations, dizziness; muscle weakness, ataxia, dry mouth, mydriasis, blurred vision, palpitations, tachycardia, elevated blood pressure, nausea, vomiting, dysuria, numbness of fingers, headache, delirium, coma, shock, convulsions, respiratory arrest, anhidrosis, hyperthermia, glaucoma, and constipation. (source: Drug Bank)

Isomeric SMILES Code:

CN1[C@@H]2CC[C@@H]1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C19
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2D6
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  • PK
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Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
CHRM1 Uncurated Annotation (source: Drug Bank)
SLC6A3 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
donepezil Uncurated Annotation Possible antagonism of action (source: Drug Bank)
galantamine Uncurated Annotation Possible antagonism of action (source: Drug Bank)
haloperidol Uncurated Annotation The anticholinergic increases the risk of psychosis and tardive dyskinesia (source: Drug Bank)
rivastigmine Uncurated Annotation Possible antagonism of action (source: Drug Bank)

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00245
KEGG Compound ID:
C06846
PubChem Compound ID:
6832
PubChem Substance ID:
9064

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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