U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C21H25NO.CH4O3S
Molecular Weight 403.535
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BENZTROPINE MESYLATE

SMILES

CS(O)(=O)=O.CN1[C@H]2CC[C@@H]1C[C@@H](C2)OC(C3=CC=CC=C3)C4=CC=CC=C4

InChI

InChIKey=CPFJLLXFNPCTDW-BWSPSPBFSA-N
InChI=1S/C21H25NO.CH4O3S/c1-22-18-12-13-19(22)15-20(14-18)23-21(16-8-4-2-5-9-16)17-10-6-3-7-11-17;1-5(2,3)4/h2-11,18-21H,12-15H2,1H3;1H3,(H,2,3,4)/t18-,19+,20+;

HIDE SMILES / InChI

Description
Curator's Comment: Description was created based on several sources, including http://www.drugbank.ca/drugs/DB00245

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. Benztropine also inhibits dopamine reuptake via the dopamine transporter at nerve terminals. 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. Used 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.

CNS Activity

Originator

Approval Year

1954
117
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
Inhibitor
8297
 312.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
COGENTIN

Approved Use

For use as an adjunct in the therapy of all forms of parkinsonism Useful also in the control of extrapyramidal disorders (except tardive dyskinesia) due to neuroleptic drugs (e.g., phenothiazines).

Launch Date

1959
Secondary
Approved
8429
COGENTIN

Approved Use

For use as an adjunct in the therapy of all forms of parkinsonism Useful also in the control of extrapyramidal disorders (except tardive dyskinesia) due to neuroleptic drugs (e.g., phenothiazines).

Launch Date

1959
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.5 ng/mL
OTHER GOV
https://pdf.hres.ca/dpd_pm/00029138.PDF
1.5 mg single, oral
dose: 1.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BENZTROPINE unknown
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7 h
OTHER GOV
https://pdf.hres.ca/dpd_pm/00029138.PDF
1.5 mg single, oral
dose: 1.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BENZTROPINE unknown
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
5%
OTHER GOV
https://pdf.hres.ca/dpd_pm/00029138.PDF
1.5 mg single, oral
dose: 1.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BENZTROPINE unknown
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
2 mg 3 times / day multiple, oral
Recommended
Dose: 2 mg, 3 times / day
Route: oral
Route: multiple
Dose: 2 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/791573
unhealthy, 20-66
n = 19
Health Status: unhealthy
Condition: neuroleptic-induced extrapyramidal symptoms
Age Group: 20-66
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/791573
Other AEs: Dry mouth, Visual disturbance...
Other AEs:
Dry mouth (grade 1-2, 26%)
Visual disturbance (grade 1-2, 32%)
Constipation (grade 1-2, 10.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/791573
2.25 mg 2 times / day multiple, oral (max)
Studied dose
Dose: 2.25 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2.25 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
unhealthy, 21 - 80
n = 19
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 21 - 80
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
Other AEs: Confusion, Memory disturbance...
Other AEs:
Confusion (32%)
Memory disturbance (26%)
Lightheadedness (16%)
Blurred vision (10.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
2.25 mg 2 times / day multiple, oral (max)
Studied dose
Dose: 2.25 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2.25 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
unhealthy, 21 - 80
n = 19
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 21 - 80
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
Other AEs: Dry mouth...
Other AEs:
Dry mouth (63%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
2 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 2 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 2 mg, 1 times / day
Co-administed with::
phenothiazines
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Disc. AE: Paralytic ileus...
AEs leading to
discontinuation/dose reduction:
Paralytic ileus (grade 3-5)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
2 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 2 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 2 mg, 1 times / day
Co-administed with::
tricyclic antidepressants
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Disc. AE: Paralytic ileus...
AEs leading to
discontinuation/dose reduction:
Paralytic ileus (grade 3-5)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
2 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 2 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Other AEs: Mental impairment...
Other AEs:
Mental impairment
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Other AEs: Appetite lost, Dry mouth...
Other AEs:
Appetite lost (33%)
Dry mouth (24%)
Constipation (29%)
Listlessness (24%)
Urinary retention (19%)
Blurred vision (19%)
Muscle weakness (19%)
Excitement (10.5%)
Sweating decreased (14%)
Mental confusion (10.5%)
Skin rash (10.5%)
Nausea (10.5%)
Vomiting (10.5%)
Nervousness (10.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
6 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 6 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 6 mg, 1 times / day
Co-administed with::
phenothiazines
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Other AEs: Hyperthermia, Heat stroke...
Other AEs:
Hyperthermia (grade 3-5)
Heat stroke (grade 3-5)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
6 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 6 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 6 mg, 1 times / day
Co-administed with::
tricyclic antidepressants
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Other AEs: Hyperthermia, Heat stroke...
Other AEs:
Hyperthermia (grade 3-5)
Heat stroke (grade 3-5)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
6 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 6 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Other AEs: Physical impairment, Anhidrosis...
Other AEs:
Physical impairment
Anhidrosis (grade 3-5)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Constipation grade 1-2, 10.5%
2 mg 3 times / day multiple, oral
Recommended
Dose: 2 mg, 3 times / day
Route: oral
Route: multiple
Dose: 2 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/791573
unhealthy, 20-66
n = 19
Health Status: unhealthy
Condition: neuroleptic-induced extrapyramidal symptoms
Age Group: 20-66
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/791573
Dry mouth grade 1-2, 26%
2 mg 3 times / day multiple, oral
Recommended
Dose: 2 mg, 3 times / day
Route: oral
Route: multiple
Dose: 2 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/791573
unhealthy, 20-66
n = 19
Health Status: unhealthy
Condition: neuroleptic-induced extrapyramidal symptoms
Age Group: 20-66
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/791573
Visual disturbance grade 1-2, 32%
2 mg 3 times / day multiple, oral
Recommended
Dose: 2 mg, 3 times / day
Route: oral
Route: multiple
Dose: 2 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/791573
unhealthy, 20-66
n = 19
Health Status: unhealthy
Condition: neuroleptic-induced extrapyramidal symptoms
Age Group: 20-66
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/791573
Blurred vision 10.5%
2.25 mg 2 times / day multiple, oral (max)
Studied dose
Dose: 2.25 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2.25 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
unhealthy, 21 - 80
n = 19
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 21 - 80
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
Lightheadedness 16%
2.25 mg 2 times / day multiple, oral (max)
Studied dose
Dose: 2.25 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2.25 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
unhealthy, 21 - 80
n = 19
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 21 - 80
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
Memory disturbance 26%
2.25 mg 2 times / day multiple, oral (max)
Studied dose
Dose: 2.25 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2.25 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
unhealthy, 21 - 80
n = 19
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 21 - 80
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
Confusion 32%
2.25 mg 2 times / day multiple, oral (max)
Studied dose
Dose: 2.25 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2.25 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
unhealthy, 21 - 80
n = 19
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 21 - 80
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
Dry mouth 63%
2.25 mg 2 times / day multiple, oral (max)
Studied dose
Dose: 2.25 mg, 2 times / day
Route: oral
Route: multiple
Dose: 2.25 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
unhealthy, 21 - 80
n = 19
Health Status: unhealthy
Condition: Parkinson's disease
Age Group: 21 - 80
Sex: M+F
Population Size: 19
Sources:
https://pubmed.ncbi.nlm.nih.gov/9109903
Paralytic ileus grade 3-5
Disc. AE
2 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 2 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 2 mg, 1 times / day
Co-administed with::
phenothiazines
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Paralytic ileus grade 3-5
Disc. AE
2 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 2 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 2 mg, 1 times / day
Co-administed with::
tricyclic antidepressants
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Mental impairment
2 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 2 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 2 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Excitement 10.5%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Mental confusion 10.5%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Nausea 10.5%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Nervousness 10.5%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Skin rash 10.5%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Vomiting 10.5%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Sweating decreased 14%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Blurred vision 19%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Muscle weakness 19%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Urinary retention 19%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Dry mouth 24%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Listlessness 24%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Constipation 29%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Appetite lost 33%
2 mg 2 times / day steady, oral
Recommended
Dose: 2 mg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
unhealthy
n = 21
Health Status: unhealthy
Condition: Schizophrenia|Drug-Induced Extrapyramidal Disorders
Sex: M+F
Population Size: 21
Sources:
https://pubmed.ncbi.nlm.nih.gov/5066
Heat stroke grade 3-5
6 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 6 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 6 mg, 1 times / day
Co-administed with::
phenothiazines
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Hyperthermia grade 3-5
6 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 6 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 6 mg, 1 times / day
Co-administed with::
phenothiazines
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Heat stroke grade 3-5
6 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 6 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 6 mg, 1 times / day
Co-administed with::
tricyclic antidepressants
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Hyperthermia grade 3-5
6 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 6 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 6 mg, 1 times / day
Co-administed with::
tricyclic antidepressants
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Physical impairment
6 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 6 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Anhidrosis grade 3-5
6 mg 1 times / day multiple, parenteral (max)
Recommended
Dose: 6 mg, 1 times / day
Route: parenteral
Route: multiple
Dose: 6 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
unhealthy
Health Status: unhealthy
Condition: Parkinsonism|Extrapyramidal disorders due to neuroleptic drugs
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012015s027lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C19
991
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP2C19
991
 yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
ABI Chem
AC1Q3XL3
Amadis Chemical
A806390
Angene
AGN-PC-0V2SW3
http://www.angenechemical.com/productshow/AGN-PC-0V2SW3.html
Bide Pharmatech
BD1513
BioSynth
Q-200694
Chemieliva Pharmaceutical Co., Ltd
PBCM1439177
Hairui
HR143302
http://www.hairuichem.com/en/product/86-13-5.html
IBScreen
BB_NC-02710
IBScreen
Bio-0891
MuseChem
R044799
https://www.musechem.com/product/R044799.html
NCI Diversity
42199
NCI Plated 2007
169913
NCI Plated 2007
42199
NCI Plated 2007
63912
Pharmeks
PHAR266808
TimTec
ST50997629
Yick-Vic Chemicals & Pharmaceuticals (HK) Ltd.
PH-0814AA
ZINC
ZINC000000968360
http://zinc15.docking.org/substances/ZINC000000968360
eNovation Chemicals
D671977
https://www.enovationchem.com/ProductDetails.asp?ProductID=D671977
iChemical
EBD71620
http://www.ichemical.com/products/86-13-5.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
PubMed

PubMed

TitleDatePubMed
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.
1995 Sep 29
Intermittent neuroleptic treatment and risk for tardive dyskinesia: Curaçao Extrapyramidal Syndromes Study III.
1998 Apr
Risk factors for tardive dyskinesia in a large population of youths and adults.
2001 Aug
Synthesis and reactions of some new substituted pyridine and pyrimidine derivatives as analgesic, anticonvulsant and antiparkinsonian agents.
2005 Sep
A cell protection screen reveals potent inhibitors of multiple stages of the hepatitis C virus life cycle.
2010 Feb 23
Selective inhibition of hepatitis C virus infection by hydroxyzine and benztropine.
2014 Jun
Patents

Patents

JP2007525670A
148
JP2009519467A
53
JP2009526755A
447
JP3035346B2
5

Sample Use Guides

In Vivo Use Guide
The usual daily dose is 1 to 2 mg, with a range of 0.5 to 6 mg parenterally.
Route of Administration: Parenteral
In Vitro Use Guide
Benztropine inhibited veratridine-induced efflux of K+, membrane depolarization and release of amino acid neurotransmitters with Kd of 2 uM.
Name Type Language
BENZTROPINE MESYLATE
ORANGE BOOK   USP   USP-RS   VANDF  
Common Name English
BENZTROPINE MESYLATE [VANDF]
Common Name English
3.ALPHA.-(DIPHENYLMETHOXY)-1.ALPHA.H,5.ALPHA.H-TROPANE METHANESULPHONATE
Common Name English
3α-(Diphenylmethoxy)-1αH,5αH-tropane methanesulfonate
Common Name English
8-AZABICYCLO(3.2.1)OCTANE, 3-(DIPHENYLMETHOXY)-, ENDO, METHANESULPHONATE
Common Name English
8-AZABICYCLO(3.2.1)OCTANE, 3-(DIPHENYLMETHOXY)-8-METHYL-, (3-ENDO)-, METHANESULFONATE (1:1)
Common Name English
BENZTROPINE MESYLATE [USP MONOGRAPH]
Common Name English
BENZTROPINE METHANESULFONATE [MI]
Common Name English
8-AZABICYCLO(3.2.1)OCTANE, 3-(DIPHENYLMETHOXY)-, ENDO, METHANESULFONATE
Common Name English
BENZTROPINE MESILATE
JAN  
Common Name English
BENZATROPINE MESILATE [MART.]
Common Name English
BENZATROPINE MESILATE
MART.   WHO-DD  
Common Name English
Benzatropine mesilate [WHO-DD]
Common Name English
BENZTROPINE MESYLATE [USP IMPURITY]
Common Name English
BENZTROPINE MESYLATE [ORANGE BOOK]
Common Name English
NSC-169913
Code English
BENZTROPINE MESYLATE [USP-RS]
Common Name English
BENZTROPINE MESILATE [JAN]
Common Name English
COGENTIN
Brand Name English
Classification Tree Code System Code
NCI_THESAURUS C29704
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
Code System Code Type Description
NSC
169913
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
RS_ITEM_NUM
1061005
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
ECHA (EC/EINECS)
205-048-8
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
NCI_THESAURUS
C28864
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
RXCUI
18927
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY RxNorm
EVMPD
SUB31964
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
DAILYMED
WMJ8TL7510
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
CAS
132-17-2
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
CHEBI
3049
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
ChEMBL
CHEMBL1201203
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
FDA UNII
WMJ8TL7510
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
MERCK INDEX
m2394
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY Merck Index
EPA CompTox
DTXSID0045096
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
DRUG BANK
DBSALT000894
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
SMS_ID
100000124563
Created by admin on Sat Dec 16 04:54:44 GMT 2023 , Edited by admin on Sat Dec 16 04:54:44 GMT 2023
PRIMARY
ACTIVE MOIETY
Structure of BENZTROPINE
SUBSTANCE RECORD
Structure of BENZTROPINE MESYLATE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
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