Benztropine (Monograph)
Brand name: Cogentin
Drug class: Anticholinergic Agents
VA class: AU350
CAS number: 132-17-2
Introduction
Antimuscarinic antiparkinsonian agent.157 200 201
Uses for Benztropine
Parkinsonian Syndrome
Symptomatic management of all forms of parkinsonian syndrome, including idiopathic parkinson disease and parkinsonism resulting from encephalitis (postencephalitic parkinsonism).200 201 c
Has been used as monotherapy or adjunctive therapy in the treatment of parkinson disease.123 157 158
Levodopa is currently the most effective drug for relieving motor symptoms of parkinson disease; however, long-term use associated with motor complications.101 115 123 157 To avoid these complications, may initiate treatment with other antiparkinsonian agents first and postpone use of levodopa.115 123 157 Some clinicians state that anticholinergic agents (e.g., trihexyphenidyl, benztropine) may be particularly useful for initial therapy in patients <60 years of age with resting tremors as their only or most prominent symptom.115 123
Although main use of anticholinergic agents in parkinson disease is to control tremors, evidence of a benefit largely anecdotal.123 157 158
Drug-induced Extrapyramidal Reactions
Control of extrapyramidal symptoms (EPS) induced by antipsychotic agents (e.g., phenothiazines).200 201
Anticholinergic agents (e.g., benztropine, trihexyphenidyl) are used traditionally to restore acetylcholine and dopamine imbalance in patients with antipsychotic-induced EPS; however, evidence supporting a benefit is lacking or inconsistent and the drugs are associated with a variety of adverse effects.160 161 162
In general, use cautiously and for minimum duration necessary to control EPS.160 162
Benztropine does not alleviate symptoms of tardive dyskinesia, and in some instances may aggravate them.200 201 c Use not recommended.200 201 c
Benztropine Dosage and Administration
Administration
Administer orally or by IM injection.200 201
Also may be given IV.200 Because onset of effect is similar with IV and IM route, manufacturer states there usually is no need to administer IV and does not provide specific instructions for IV administration.200
Oral Administration
Administer as a single dose at bedtime or in divided doses 2–4 times daily.201
IM Administration
Reserve for patients who cannot take oral medication or for emergency situations (e.g., acute dystonia).200 201 c
Dosage
Available as benztropine mesylate; dosage is expressed in terms of the salt.200 201
Adjust dosage carefully according to individual requirements and response.200 201 Initiate with low dosage and increase gradually to minimum effective dosage.200 201
Dosing guidelines are the same for oral and IM administration; oral administration preferred whenever possible.200
Pediatric Patients
Manufacturers make no specific dosage recommendations for children ≥3 years of age.200 201 (See Pediatric Use under Cautions.)
Adults
Parkinsonian Syndrome
May require periodic dosage adjustments to maintain optimum symptomatic relief in patients receiving concomitant levodopa-carbidopa therapy.200 201
If used to replace or supplement other antiparkinsonian drugs, change should be gradual, with dosage of previous medication reduced as benztropine dosage is increased.200 201
Avoid abrupt discontinuance of concomitantly administered antiparkinsonian drugs.200 201
Idiopathic Parkinsonian Syndrome
OralInitially, 0.5–1 mg as a single daily dose at bedtime.201 Dosage may be increased by 0.5-mg increments at 5- or 6-day intervals based on response and tolerability up to a maximum of 6 mg daily.201
Usual dosage: 1–2 mg daily (range: 0.5–6 mg daily).201
IMInitially, 0.5–1 mg as a single dose at bedtime.200 Dosage may be increased by 0.5-mg increments at 5- or 6-day intervals based on response and tolerability up to a maximum of 6 mg daily.200
Usual dosage: 1–2 mg daily (range: 0.5–6 mg daily).200
For emergency situations, 1–2 mg normally will provide quick relief; repeat dose if parkinsonian symptoms return.200
Postencephalitic Parkinsonian Syndrome
OralInitially, 2 mg daily, given in 1 or more divided doses.201 In highly sensitive patients, may give a single 0.5 mg-dose at bedtime.201 Dosage may be increased by 0.5-mg increments at 5- to 6-day intervals up to a maximum of 6 mg daily.201
Usual dosage: 1–2 mg daily (range: 0.5–6 mg daily).201
IMInitially, 2 mg daily, given in 1 or more divided doses.200 In highly sensitive patients, may give a single 0.5 mg-dose at bedtime. Dosage may be increased by 0.5-mg increments at 5- or 6-day intervals up to a maximum of 6 mg daily.200
Usual dosage: 1–2 mg daily (range: 0.5–6 mg daily).200
For emergency situations, 1–2 mg normally will provide quick relief; repeat dose if parkinsonian symptoms return.200
Drug-Induced Extrapyramidal Reactions
Oral
1–4 mg once or twice daily.160 201
For EPS that develops shortly after initiation of antipsychotic therapy, 1–2 mg 2 or 3 times daily usually provides relief within 1 or 2 days.201 Evaluate need for continued therapy after 1–2 weeks.201
IM
1–4 mg once or twice daily.160 200
For EPS that develops shortly after initiation of antipsychotic therapy, 1–2 mg 2 or 3 times daily usually provides relief within 1 or 2 days.200 Evaluate need for continued therapy after 1–2 weeks.200
Acute Dystonia
IM followed by Oral1–2 mg, as a single IM dose, followed by 1–2 mg orally twice daily to prevent recurrence.200 201
Prescribing Limits
Adults
Parkinsonian Syndrome
Oral
Maximum 6 mg daily.201
IM
Maximum 6 mg daily.200
Special Populations
Hepatic Impairment
No specific dosage recommendations at this time.200 201
Renal Impairment
No specific dosage recommendations at this time.200 201
Geriatric Patients
Geriatric patients generally cannot tolerate high dosages of the drug; select dosage with caution, starting at low end of dosing range and increasing only as needed.200 201 (See Geriatric Use under Cautions.)
Low Body Weight
Patients with less than average body weight generally cannot tolerate high dosages of the drug.200 201
Cautions for Benztropine
Contraindications
Warnings/Precautions
Warnings
Pregnancy
Safe use during pregnancy has not been established.200 201
Cognitive/Physical Impairment
Risk of impaired mental alertness or physical coordination required for performing hazardous tasks (e.g., driving or operating machinery).200 201
Drug Interactions
Concomitant use with phenothiazines or tricyclic antidepressants associated with potentially fatal paralytic ileus, hyperthermia, or heat stoke.200 201 Advise patients to promptly notify clinicians if adverse GI effects, fever, or heat intolerance occur if used concomitantly with these drugs or other drugs with anticholinergic or antidopaminergic (e.g., haloperidol) effects.200 201 (See Interactions.)
Anhidrosis
Possibly severe anhidrosis and fatal hyperthermia.200 201 Use with caution in hot weather, particularly when given concomitantly with other anticholinergic drugs to chronically ill or alcoholic patients, those who have CNS disease, and those engaged in manual labor.200 201 Decrease dosages as needed to maintain ability to perspire.200 201
General Precautions
Adequate Patient Monitoring
Has cumulative effects; continue to monitor patients, particularly those with tendency toward tachycardia or with prostatic hypertrophy.200 201
Musculoskeletal Effects
Possible complaints of weakness and inability to move particular muscle groups, particularly at large dosages; adjust dosage as required.200 201
CNS Effects
Possible mental confusion and excitement, particularly with large dosages or in susceptible patients.200 201 Visual hallucinations also possible.200 201 (See Dosage under Dosage and Administration.)
Risk of intensification of mental symptoms or precipitation of toxic psychosis in patients with mental disorders receiving phenothiazines, especially at beginning of therapy or during dosage adjustment; monitor closely.200 201 (See Specific Drugs under Interactions.)
Tardive Dyskinesia
Not recommended for use in patients with tardive dyskinesia.200 201 (See Drug-induced Extrapyramidal Reactions under Uses.)
Renal Effects
Possible dysuria or urinary retention.200 201
Glaucoma
Consider risks of glaucoma.200 201 Probably should not be used in patients with angle-closure glaucoma.200 201 e
Specific Populations
Pregnancy
Safe use during pregnancy not established.200 201
Geriatric Use
Possibility exists of greater sensitivity to the drug in some geriatric individuals.200 201 Careful dosage selection necessary.200 201 Some experts state to avoid use in geriatric patients because of unfavorable balance of benefits and risks compared with alternative treatments.157 159
Pediatric Use
Safety and efficacy not established in children <3 years of age.200 201 (See Cautions: Contraindications.)
Use with caution in children >3 years of age because of adverse anticholinergic effects.200 201
Common Adverse Effects
Dry mouth, blurred vision, mydriasis, nausea, nervousness, tachycardia, paralytic ileus, constipation.c e
Drug Interactions
Specific Drugs
Drug |
Interaction |
Comments |
---|---|---|
Anticholinergic agents |
||
Antidepressants, tricyclics |
Potentially fatal paralytic ileus, hyperthermia, or heat intolerance200 201 |
Advise patients to promptly notify clinicians if adverse GI effects, fever, or heat intolerance occurs200 201 |
Haloperidol |
Potentially fatal paralytic ileus, hyperthermia, or heat intolerance200 201 |
Advise patients to promptly notify clinicians if adverse GI effects, fever, or heat intolerance occurs200 201 |
Phenothiazines |
Potentially fatal paralytic ileus, hyperthermia, or heat intolerance200 201 Possible intensification of mental symptoms or precipitation of toxic psychosis in patients with mental disorders200 201 |
Advise patients to promptly notify clinicians if adverse GI effects, fever, or heat intolerance occurs200 201 Observe carefully, especially at beginning of therapy or during dosage adjustment200 201 |
Stability
Storage
Oral
Tablets
20–25°C.201
Parenteral
Injection
20–25°C.200
Compatibility
Drug Compatibility
For information on IV injection of benztropine, see Administration under Dosage and Administration.
Compatible |
---|
Cloxacillin sodium |
Fluconazole |
Tacrolimus |
Compatible |
---|
Chlorpromazine HCl |
Fluphenazine HCl |
Metoclopramide HCl |
Variable |
Haloperidol lactate |
Actions
-
Possesses both anticholinergic and antihistaminic effects, although only the former have been established as therapeutically important in management of parkinsonism.200 201
Advice to Patients
-
Potential for drug to impair mental alertness or physical coordination; use caution when driving or operating machinery until effects on individual are known.200 201
-
Importance of promptly notifying clinicians of adverse GI effects, fever, or heat intolerance, particularly if also receiving phenothiazines, haloperidol, or other drugs with anticholinergic or antidopaminergic activity.200 201
-
Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.200 201
-
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as concomitant illnesses.200 201
-
Importance of informing patients of other important precautionary information.200 201 (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes |
Dosage Forms |
Strengths |
Brand Names |
Manufacturer |
---|---|---|---|---|
Oral |
Tablets |
0.5 mg* |
Benztropine Mesylate Tablets |
|
1 mg* |
Benztropine Mesylate Tablets |
|||
2 mg* |
Benztropine Mesylate Tablets |
|||
Parenteral |
Injection |
1 mg/mL* |
Benztropine Mesylate Injection |
|
Cogentin |
Akorn |
AHFS DI Essentials™. © Copyright 2025, Selected Revisions February 17, 2022. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
References
101. Olanow CW, Watts RL, Koller WC. An algorithm (decision tree) for the management of Parkinson’s disease (2001): treatment guidelines. Neurology. 2001; 56:S1-S88.
115. Lewitt PA. Levodopa for the treatment of Parkinson's disease. N Engl J Med. 2008; 359:2468-76. https://pubmed.ncbi.nlm.nih.gov/19052127
123. Connolly BS, Lang AE. Pharmacological treatment of Parkinson disease: a review. JAMA. 2014 Apr 23-30; 311:1670-83. https://pubmed.ncbi.nlm.nih.gov/24756517
157. . Drugs for Parkinson's disease. Med Lett Drugs Ther. 2017; 59:187-194. https://pubmed.ncbi.nlm.nih.gov/29136401
158. Katzenschlager R, Sampaio C, Costa J et al. Anticholinergics for symptomatic management of Parkinson's disease. Cochrane Database Syst Rev. 2003; :CD003735. https://pubmed.ncbi.nlm.nih.gov/12804486
159. By the 2019 American Geriatrics Society Beers Criteria Update Expert Panel. American Geriatrics Society 2019 Updated AGS Beers Criteria for Potentially Inappropriate Medication Use in Older Adults. J Am Geriatr Soc. 2019; 67:674-694. https://pubmed.ncbi.nlm.nih.gov/30693946
160. Salem H, Nagpal C, Pigott T et al. Revisiting Antipsychotic-induced Akathisia: Current Issues and Prospective Challenges. Curr Neuropharmacol. 2017; 15:789-798. https://pubmed.ncbi.nlm.nih.gov/27928948
161. Rathbone J, Soares-Weiser K. Anticholinergics for neuroleptic-induced acute akathisia. Cochrane Database Syst Rev. 2006; :CD003727. https://pubmed.ncbi.nlm.nih.gov/17054182
162. Ogino S, Miyamoto S, Miyake N et al. Benefits and limits of anticholinergic use in schizophrenia: focusing on its effect on cognitive function. Psychiatry Clin Neurosci. 2014; 68:37-49. https://pubmed.ncbi.nlm.nih.gov/24102938
200. Akorn. Cogentin (benztropine mesylate) injection prescribing information. Lake Forest, IL; 2016 Sept.
201. Bayshore Pharmaceuticals. Benztropine mesylate tablets prescribing information. Short Hills, NJ; 2017 Nov.
c. AHFS drug information 2021. Snow EK, ed. Benztropine mesylate. Bethesda, MD: American Society of Health-System Pharmacists; 2021.
e. AHFS drug information 2021. Snow EK, ed. Antimuscarinics/Antispasmodics General Statement. Bethesda, MD: American Society of Health-System Pharmacists; 2021.
HID. ASHP’s interactive handbook on injectable drugs. McEvoy, GK, ed. Bethesda, MD: American Society of Health-System Pharmacists, Inc; Accessed Jan 29, 2020. From HID website. http://www.interactivehandbook.com
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