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Benztropine (Monograph)

Brand name: Cogentin
Drug class: Anticholinergic Agents
VA class: AU350
CAS number: 132-17-2

Medically reviewed by Drugs.com on Feb 7, 2024. Written by ASHP.

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
Oral

Initially, 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

IM

Initially, 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
Oral

Initially, 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

IM

Initially, 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 Oral

1–2 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

Increased risk of adverse anticholinergic effects200 201

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.

Y-Site CompatibilityHID

Compatible

Cloxacillin sodium

Fluconazole

Tacrolimus

Compatibility in SyringeHID

Compatible

Chlorpromazine HCl

Fluphenazine HCl

Metoclopramide HCl

Variable

Haloperidol lactate

Actions

Advice to Patients

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

Benztropine Mesylate

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 2024, 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. http://www.ncbi.nlm.nih.gov/pubmed/19052127?dopt=AbstractPlus

123. Connolly BS, Lang AE. Pharmacological treatment of Parkinson disease: a review. JAMA. 2014 Apr 23-30; 311:1670-83. http://www.ncbi.nlm.nih.gov/pubmed/24756517?dopt=AbstractPlus

157. . Drugs for Parkinson's disease. Med Lett Drugs Ther. 2017; 59:187-194. http://www.ncbi.nlm.nih.gov/pubmed/29136401?dopt=AbstractPlus

158. Katzenschlager R, Sampaio C, Costa J et al. Anticholinergics for symptomatic management of Parkinson's disease. Cochrane Database Syst Rev. 2003; :CD003735. http://www.ncbi.nlm.nih.gov/pubmed/12804486?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/30693946?dopt=AbstractPlus

160. Salem H, Nagpal C, Pigott T et al. Revisiting Antipsychotic-induced Akathisia: Current Issues and Prospective Challenges. Curr Neuropharmacol. 2017; 15:789-798. http://www.ncbi.nlm.nih.gov/pubmed/27928948?dopt=AbstractPlus

161. Rathbone J, Soares-Weiser K. Anticholinergics for neuroleptic-induced acute akathisia. Cochrane Database Syst Rev. 2006; :CD003727. http://www.ncbi.nlm.nih.gov/pubmed/17054182?dopt=AbstractPlus

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. http://www.ncbi.nlm.nih.gov/pubmed/24102938?dopt=AbstractPlus

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