BENZTROPINE MESYLATE TABLETS, USP

Rx only

REV. 11-02
15134-04

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 C₂₁H₂₅NO•CH₄O₃S, and its structural formula is:

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

Each benztropine mesylate tablet for oral administration contains benztropine mesylate 0.5 mg, 1 mg or 2 mg.

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

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 PRECAUTIONS) due to neuroleptic drugs (e.g., phenothiazines).

Hypersensitivity to 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 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 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, in combination with phenothiazines and/or tricyclic antidepressants.

Since 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.

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.

Cardiovascular
Tachycardia.

Digestive
Paralytic ileus, constipation, vomiting, nausea, dry mouth.

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.

Nervous System
Toxic psychosis, including confusion, disorientation, memory impairment, visual hallucinations; exacerbation of preexisting psychotic symptoms; nervousness; depression; listlessness; numbness of fingers.

Special Senses
Blurred vision, dilated pupils.

Urogenital
Urinary retention, dysuria.

Metabolic/Immune or Skin
Occasionally, an allergic reaction, e.g., skin rash, develops. If this can not be controlled by dosage reduction, the medication should be discontinued.

Other
Heat stroke, hyperthermia, fever.

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 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 blistercards of 30 and 31.

As 1 mg: Compressed tablet, white, 0.231" x 0.420", oval; one side scored and debossed 832 and BM1, one side plain, in blistercards of 30, 31 and boxes of 30 for unit-dose dispensing.

As 2 mg: Compressed tablet, white, 9/32" diameter, flat beveled edge; one side scored and debossed 832 and BM2, one side plain, in blistercards of 30 and 31.

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

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

Keep out of reach of children.

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

Rev. 11-02

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

Bentropine Mesylate Tabs, USP 0.5mg

Benztropine Mesylate Tabs, USP 0.5mg 

NDC 0615-7676

Benztropine
Mesylate
Tablets, USP

1 mg

Principal Display Panel-Benztropine Mesylate Tabs, USP 1mg

NDC 0615-7277

Benztropine
Mesylate
Tablets, USP

2 mg

 Principal Display Panel-Benztropine Mesylate Tablets USP 1mg Unit Dose Label