Benztropine mesylate (Benztropine mesylate) is a synthetic compound containing structural features found in atropine and diphenhydramine.

It is designated chemically as 3∝-(Diphenylmethoxy)-1∝H, 5∝H-tropane methanesulfonate. Its molecular formula is CHNO•CHOS, and its structural formula is:

Benztropine mesylate (Benztropine mesylate) is a crystalline white powder, very soluble in water, and has a molecular weight of 403.54.

Each Benztropine mesylate (Benztropine mesylate) tablet for oral administration contains Benztropine mesylate (Benztropine mesylate) 0.5 mg, 1 mg or 2 mg.

Inactive ingredients: croscarmellose sodium, anhydrous lactose, magnesium stearate, povidone.

Benztropine mesylate (Benztropine mesylate) possesses both anticholinergic and antihistaminic effects, although only the former have been established as therapeutically significant in the management of parkinsonism.

In the isolated guinea pig ileum, the anticholinergic activity of this drug is about equal to that of atropine; however, when administered orally to unanesthetized cats, it is only about half as active as atropine.

In laboratory animals, its antihistaminic activity and duration of action approach those of pyrilamine maleate.

For use as an adjunct in the therapy of all forms of parkinsonism.

Useful also in the control of extrapyramidal disorders (except tardive dyskinesia - see ) due to neuroleptic drugs (e.g., phenothiazines).

Hypersensitivity to Benztropine mesylate (Benztropine mesylate) tablets or to any component of the tablets.

Because of its atropine-like side effects, this drug is contraindicated in pediatric patients under three years of age, and should be used with caution in older pediatric patients.

Safe use in pregnancy has not been established.

Benztropine mesylate (Benztropine mesylate) may impair mental and/or physical abilities required for performance of hazardous tasks, such as operating machinery or driving a motor vehicle.

When Benztropine mesylate (Benztropine mesylate) is given concomitantly with phenothiazines, haloperidol, or other drugs with anticholinergic or antidopaminergic activity, patients should be advised to report gastrointestinal complaints, fever or heat intolerance promptly. Paralytic ileus, hyperthermia and heat stroke, all of which have sometimes been fatal, have occurred in patients taking anticholinergic-type antiparkinsonism drugs, including Benztropine mesylate (Benztropine mesylate) , in combination with phenothiazines and/or tricyclic antidepressants.

Since Benztropine mesylate (Benztropine mesylate) contains structural features of atropine, it may produce anhidrosis. For this reason, it should be administered with caution during hot weather, especially when given concomitantly with other atropine-like drugs to the chronically ill, the alcoholic, those who have central nervous system disease, and those who do manual labor in a hot environment. Anhidrosis may occur more readily when some disturbance of sweating already exists. If there is evidence of anhidrosis, the possibility of hyperthermia should be considered. Dosage should be decreased at the discretion of the physician so that the ability to maintain body heat equilibrium by perspiration is not impaired. Severe anhidrosis and fatal hyperthermia have occurred.

Since Benztropine mesylate (Benztropine mesylate) 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 (Benztropine mesylate) .

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 with these drugs has been discontinued. Antiparkinsonism agents do not alleviate the symptoms of tardive dyskinesia, and in some instances may aggravate them. Benztropine mesylate (Benztropine mesylate) 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.

The adverse reactions below, most of which are anticholinergic in nature, have been reported and within each category are listed in order of decreasing severity.

If dry mouth is so severe that there is difficulty in swallowing or speaking, or loss of appetite and weight, reduce dosage, or discontinue the drug temporarily.

Slight reduction in dosage may control nausea and still give sufficient relief of symptoms. Vomiting may be controlled by temporary discontinuation, followed by resumption at a lower dosage.

Manifestations -

Treatment -

Benztropine mesylate (Benztropine mesylate) tablets should be used when patients are able to take oral medication.

The injection is especially useful for psychotic patients with acute dystonic reactions or other reactions that make oral medication difficult or impossible. It is recommended also when a more rapid response is desired than can be obtained with the tablets.

Because of cumulative action, therapy should be initiated with a low dose which is increased gradually at five or six-day intervals to the smallest amount necessary for optimal relief. Increases should be made in increments of 0.5 mg, to a maximum of 6 mg, or until optimal results are obtained without excessive adverse reactions.

Benztropine mesylate (Benztropine mesylate) Tablets, USP, for oral use, are supplied in the following forms:

As 0.5 mg: Compressed tablet, white, 1/4" diameter, flat beveled edge; one side scored and debossed 832 and BM05, one side plain, in bottles of 100.

As 1 mg: Compressed tablet, white, 0.231" x 0.420", oval; one side scored and debossed 832 and BM1, one side plain, in bottles of 100 and 1000.

As 2 mg: Compressed tablet, white, 9/32" diameter, flat beveled edge; one side scored and debossed 832 and BM2, one side plain, in bottles of 100 and 1000.

Store at controlled room temperature 15 - 30° C (59 - 86° F).

Dispense in well-closed containers as defined in the USP.

-------------------------

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

Rev. 11-02

Manufactured by: UPSHER-SMITH LABORATORIES, INC. Minneapolis, MN 55447

Repackaged by: Contract Pharmacy Services-PA125 Titus Ave Suite 200Warrington, PA 18976 USA

Original--06/2010--NJW