United States - English - NLM (National Library of Medicine)
BENZTROPINE MESYLATE- benztropine mesylate tablet
Rebel Distributors Corp
BENZTROPINE MESYLATE TABLETS USP
0.5 mg, 1 mg and 2 mg
DESCRIPTION: Benztropine mesylate is a synthetic compound containing structural features found in
atropine and diphenhydramine.
It is a crystalline white powder, very soluble in water. It is designated chemically as 3α-
(Diphenylmethoxy)-1αH, 5αH-tropane methanesulfonate. Its molecular formula is C
CH O S, and its structural formula is:
Each tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg of benztropine mesylate. Each tablet
contains the following inactive ingredients: magnesium stearate, microcrystalline cellulose, povidone
and pregelatinized starch.
CLINICAL PHARMACOLOGY: Benztropine possesses both anticholinergic and antihistaminic
effects, although only the former have been established as therapeutically significant in the management
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
In laboratory animals, its antihistaminic activity and duration of action approach those of pyrilamine
INDICATIONS AND USAGE: 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).
CONTRAINDICATIONS: Hypersensitivity to benztropine mesylate 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.
WARNINGS: 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 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 in combination with phenothiazines and/or tricyclic antidepressants.
Since benztropine 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 has cumulative action, continued supervision is advisable. Patients with a
tendency to tachycardia and patients with prostatic hypertrophy should be observed closely during
Dysuria may occur, but rarely becomes a problem. Urinary retention has been reported with
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
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
Antipsychotic drugs such as phenothiazines or haloperidol; tricyclic antidepressants (see
Because of the atropine-like side effects, benztropine mesylate should be used with caution in pediatric
patients over three years of age (see CONTRADICTIONS ).
ADVERSE REACTIONS: 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.
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.
Toxic psychosis, including confusion, disorientation, memory impairment, visual hallucinations;
exacerbation of pre-existing psychotic symptoms; nervousness; depression; listlessness; numbness of
Blurred vision, dilated pupils.
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.
Heat stroke, hyperthermia, fever.
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;
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. Induce emesis or perform gastric lavage (contraindicated in
precomatose, convulsive, or psychotic states). 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.
DOSAGE AND ADMINISTRATION: 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
Duvoisin, R.C.; Katz, R.J.; Amer. Med. Ass. 206: 1963-1965, Nov. 25, 1968.
desired than can be obtained with 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.
Postencephalitic and Idiopathic Parkinsonism — The usual daily dose is 1 to 2 mg with a range of 0.5 to
6 mg orally or 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 by taking 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 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 may be used concomitantly with carbidopa-levodopa, or with levodopa, in which
case periodic 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 orally or parenterally.
Dosage must be individualized according to the need of the patient. Some patients require more than
recommended; others do not need as much.
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 tablets two or three
times a day usually provides relief within one or two days. After one or two weeks, the drug should be
withdrawn to determine the continued need for it. If such disorders recur, benztropine mesylate can be
Certain drug-induced extrapyramidal disorders that develop slowly may not respond to benztropine.
Benztropine mesylate tablets USP 2 mg - Each white, round compressed tablet is scored and debossed
with identification logo cor and 145 on one side.
NDC 21695-286-30 in bottles of 30 tablets
Store at controlled room temperature 15° - 30°C (59° - 86°F) (see USP).
Dispense in well-closed container as defined in the USP.
Middlesex, NJ 08846
MF # 276-03
Rising Pharmaceuticals, Inc.
Allendale, NJ 07401
Rev. July 2009
Rebel Distributors Corp
Thousand Oaks, CA 91320
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benztropine mesylate tablet
Product T ype
HUMAN PRESCRIPTION DRUG
Ite m Code (Source )
NDC:216 9 5-28 6 (NDC:6 49 8 0 -113)
Route of Administration
Active Ingredient/Active Moiety
Basis of Strength
Stre ng th
BENZTRO PINE MESYLATE (UNII: WMJ8 TL7510 ) (BENZTROPINE - UNII:1NHL2J4X8 K)
Stre ng th
MAGNESIUM STEARATE (UNII: 70 0 9 7M6 I30 )
CELLULO SE, MICRO CRYSTALLINE (UNII: OP1R32D6 1U)
PO VIDO NE (UNII: FZ9 8 9 GH9 4E)
STARCH, CO RN (UNII: O8 232NY3SJ)
Rebel Distributors Corp
S hap e
ROUND (ro und)
S iz e
c o r;145
Marketing Start Date
Marketing End Date
NDC:216 9 5-28 6 -30
30 in 1 BOTTLE, PLASTIC
Marke ting Cate gory
Application Numbe r or Monograph Citation
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Marke ting End Date
ANDA0 7226 6
0 8 /13/20 0 2
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