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

Details

Stereochemistry ACHIRAL
Molecular Formula C21H25NO
Molecular Weight 307.4293
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BENZTROPINE

SMILES

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

InChI

InChIKey=GIJXKZJWITVLHI-PMOLBWCYSA-N
InChI=1S/C21H25NO/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/h2-11,18-21H,12-15H2,1H3/t18-,19+,20+

HIDE SMILES / InChI
Molecular Formula C21H25NO
Molecular Weight 307.4293
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 3 / 3
E/Z Centers 0
Optical Activity UNSPECIFIED

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.
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:14:44 GMT 2023
Edited
by admin
on Fri Dec 15 16:14:44 GMT 2023
Record UNII
1NHL2J4X8K
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BENZTROPINE
HSDB   MI   VANDF  
Common Name English
BENZATROPINE
INN   WHO-DD  
INN  
Official Name English
BENZTROPINE [VANDF]
Common Name English
8-AZABICYCLO(3.2.1)OCTANE, 3-(DIPHENYLMETHOXY)-8-METHYL-, (3-ENDO)-
Systematic Name English
BENZTROPINE [HSDB]
Common Name English
benzatropine [INN]
Common Name English
COBRENTIN
Brand Name English
NK-02
Code English
Benzatropine [WHO-DD]
Common Name English
BENZTROPINE [MI]
Common Name English
1.ALPHA.H,5.ALPHA.H-TROPANE, 3.ALPHA.-(DIPHENYLMETHOXY)-
Common Name English
Classification Tree Code System Code
NDF-RT N0000175370
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
NDF-RT N0000175750
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
NDF-RT N0000175574
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
LIVERTOX NBK548408
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
NDF-RT N0000000207
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
NCI_THESAURUS C29704
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
WHO-VATC QN04AC01
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
WHO-ATC N04AC01
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
Code System Code Type Description
IUPHAR
7601
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
EPA CompTox
DTXSID9022659
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
INN
292
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
LACTMED
Benztropine
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
DRUG BANK
DB00245
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
HSDB
3014
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
ChEMBL
CHEMBL1201203
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
DRUG CENTRAL
333
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
CHEBI
3048
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
MESH
D001590
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
DAILYMED
1NHL2J4X8K
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
NCI_THESAURUS
C61649
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
SMS_ID
100000086381
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
MERCK INDEX
m2394
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY Merck Index
RXCUI
1424
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY RxNorm
WIKIPEDIA
BENZATROPINE
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
FDA UNII
1NHL2J4X8K
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
CAS
86-13-5
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
EVMPD
SUB05742MIG
Created by admin on Fri Dec 15 16:14:44 GMT 2023 , Edited by admin on Fri Dec 15 16:14:44 GMT 2023
PRIMARY
Related Record Type Details
Structure of BENZTROPINE MESYLATE
SALT/SOLVATE -> PARENT
Structure of Benztropine hydrobromide
SALT/SOLVATE -> PARENT
Related Record Type Details
Structure of BENZTROPINE
ACTIVE MOIETY
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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