Benztropine Mesylate Injection, USP

General: Since benztropine mesylate injection, USP has cumulative action, continued supervision is advisable. Patients with a tendency to tachycardia and patients with prostatic hypertrophy should be observed closely during treatment.

Dysuria may occur, but rarely becomes a problem. Urinary retention has been reported with benztropine mesylate injection, USP.

The drug may cause complaints of weakness and inability to move particular muscle groups, especially in large doses. For example, if the neck has been rigid and suddenly relaxes, it may feel weak, causing some concern. In this event, dosage adjustment is required.

Mental confusion and excitement may occur with large doses, or in susceptible patients. Visual hallucinations have been reported occasionally. Furthermore, in the treatment of extrapyramidal disorders due to neuroleptic drugs (e.g., phenothiazines), in patients with mental disorders, occasionally there may be intensification of mental symptoms. In such cases, antiparkinsonian drugs can precipitate a toxic psychosis. Patients with mental disorders should be kept under careful observation, especially at the beginning of treatment or if dosage is increased.

Tardive dyskinesia may appear in some patients on long-term therapy with phenothiazines and related agents, or may occur after therapy when these drugs have been discontinued. Antiparkinsonism agents do not alleviate the symptoms of tardive dyskinesia, and in some instances may aggravate them. Benztropine mesylate injection, USP is not recommended for use in patients with tardive dyskinesia.

The physician should be aware of the possible occurrence of glaucoma. Although the drug does not appear to have any adverse effect on simple glaucoma, it probably should not be used in angle-closure glaucoma.

Drug Interactions: Antipsychotic drugs such as phenothiazines or haloperidol; tricyclic antidepressants (see WARNINGS).

Pediatric use: Because of the atropine-like side effects, benztropine mesylate injection, USP should be used with caution in pediatric patients over three years of age (see CONTRAINDICATIONS).

Geriatric Use: Clinical studies of benztropine mesylate did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should start at the low end of the dosing range (see DOSAGE AND ADMINISTRATION) and the dose should be increased only as needed with monitoring for the emergence of adverse events (see PRECAUTIONS and ADVERSE REACTIONS).

Postencephalitic and Idiopathic Parkinsonism: The following dosing guidelines were written in reference to both benztropine mesylate tablets and COGENTIN Injection. Benztropine mesylate tablets should be used when patients are able to take oral medication.

The usual daily dose is 1 to 2 mg, with a range of 0.5 to 6 mg parenterally.

As with any agent used in parkinsonism, dosage must be individualized according to age and weight, and the type of parkinsonism being treated. Generally, older patients, and thin patients cannot tolerate large doses. Most patients with postencephalitic parkinsonism need fairly large doses and tolerate them well. Patients with a poor mental outlook are usually poor candidates for therapy.

In idiopathic parkinsonism, therapy may be initiated with a single daily dose of 0.5 to 1 mg at bedtime. In some patients, this will be adequate; in others 4 to 6 mg a day may be required.

In postencephalitic parkinsonism, therapy may be initiated in most patients with 2 mg a day in one or more doses. In highly sensitive patients, therapy may be initiated with 0.5 mg at bedtime, and increased as necessary.

Some patients experience greatest relief when given the entire dose at bedtime; others react more favorably to divided doses, two to four times a day. Frequently, one dose a day is sufficient, and divided doses may be unnecessary or undesirable.

The long duration of action of this drug makes it particularly suitable for bedtime medication when its effects may last throughout the night, enabling patients to turn in bed during the night more easily, and to rise in the morning.

When benztropine mesylate injection, USP is started, do not terminate therapy with other antiparkinsonian agents abruptly. If the other agents are to be reduced or discontinued, it must be done gradually. Many patients obtain greatest relief with combination therapy.

Benztropine mesylate injection, USP may be used concomitantly with, SINEMET (Carbidopa-Levodopalevodopa), or with levodopa, in which case dosage adjustment may be required in order to maintain optimum response.

Drug-Induced Extrapyramidal Disorders: In treating extrapyramidal disorders due to neuroleptic drugs (e.g., phenothiazines), the recommended dosage is 1 to 4 mg once or twice a day parenterally. Dosage must be individualized according to the need of the patient. Some patients require more than recommended; others do not need as much.

In acute dystonic reactions, 1 to 2 mL of the injection usually relieves the condition quickly.

When extrapyramidal disorders develop soon after initiation of treatment with neuroleptic drugs (e.g., phenothiazines), they are likely to be transient. One to 2 mg of benztropine mesylate injection, USP two or three times a day usually provides relief within one or two days. If such disorders recur, COGENTIN can be reinstituted.

Certain drug-induced extrapyramidal disorders that develop slowly may not respond to benztropine mesylate injection, USP.

Manifestations: May be any of those seen in atropine poisoning or antihistamine overdosage: CNS depression, preceded or followed by stimulation; confusion; nervousness; listlessness; intensification of mental symptoms or toxic psychosis in patients with mental illness being treated with neuroleptic drugs (e.g., phenothiazines); hallucinations (especially visual); dizziness; muscle weakness; ataxia; dry mouth; mydriasis; blurred vision; palpitations; tachycardia; elevated blood pressure; nausea; vomiting; dysuria; numbness of fingers; dysphagia; allergic reactions, e.g., skin rash; headache; hot, dry, flushed skin; delirium; coma; shock; convulsions; respiratory arrest; anhidrosis; hyperthermia; glaucoma; constipation.

Treatment: Physostigmine salicylate, 1 to 2 mg, SC or IV, reportedly will reverse symptoms of anticholinergic intoxication.** A second injection may be given after 2 hours if required. Otherwise treatment is symptomatic and supportive. Maintain respiration. A short-acting barbiturate may be used for CNS excitement, but with caution to avoid subsequent depression; supportive care for depression (avoid convulsant stimulants such as picrotoxin, pentylenetetrazol, or bemegride); artificial respiration for severe respiratory depression; a local miotic for mydriasis and cycloplegia; ice bags or other cold applications and alcohol sponges for hyperpyrexia, a vasopressor and fluids for circulatory collapse. Darken room for photophobia.

** Duvoisin, R.C.; Katz, R.J.; Amer. Med. Ass. 206: 1963-1965, Nov. 25, 1968

Storage: Store at 20º to 25ºC (68º to 77ºF) [see USP Controlled Room Temperature].

Akorn

Distributed by: Akorn, Inc.

Lake Forest, IL 60045

BZ00N Rev. 09/16