procyclidine hydrochloride tablet Monarch Pharmaceuticals, Inc.
KEMADRIN® (procyclidine hydrochloride)
5 mg Scored Tablets
KEMADRIN (procyclidine hydrochloride) is a synthetic antispasmodic
compound of relatively low toxicity. It has been shown to be useful for the
symptomatic treatment of parkinsonism (paralysis agitans) and extrapyramidal
dysfunction caused by tranquilizer therapy. Procyclidine hydrochloride was
developed at The Wellcome Research Laboratories as the most promising of a
series of antiparkinsonism compounds produced by chemical modification of
antihistamines. Procyclidine hydrochloride is a white crystalline substance
which is soluble in water and almost tasteless. It is known chemically asα-cyclohexyl-α-phenyl-1-pyrrolidinepropanol hydrochloride and
has the following structural formula:
is available in tablet form for oral administration. Each scored tablet contains5 mg procyclidine hydrochloride and the inactive ingredients corn and potato
starch, lactose, and magnesium stearate.
Pharmacologic tests have shown that procyclidine hydrochloride
has an atropine-like action and exerts an antispasmodic effect on smooth muscle.
It is a potent mydriatic and inhibits salivation. It has no sympathetic ganglion-
blocking activity in doses as high as 4 mg/kg, as measured by the lack of
inhibition of the response of the nictitating membrane to preganglionic electrical
The intravenous LD50 in mice
was about 60 mg/kg. Subcutaneously, doses of 300 mg/kg were not toxic. In
dogs, the intraperitoneal administration of procyclidine hydrochloride in
doses of 5 mg/kg caused maximal dilation of the pupil and inhibition of salivation,
but had no toxic action. When the dose was increased to 20 mg/kg, the same
symptoms occurred, and in addition there were tremors and ataxia lasting 4
to 5 hours. In one animal, convulsions occurred which were controlled by pentobarbital.
In all animals behavior returned to normal within 24 hours.
toxicity tests in rats showed that the compound caused only a very slight
retardation in growth, and no change in the erythrocyte count or the histological
appearance of the lungs, liver, spleen, and kidney when as much as 10 mg/kg
body weight was given subcutaneously daily for 9 weeks.
KEMADRIN (procyclidine hydrochloride) is indicated in the
treatment of parkinsonism including the postencephalitic, arteriosclerotic,
and idiopathic types. Partial control of the parkinsonism symptoms is the
usual therapeutic accomplishment. Procyclidine hydrochloride is usually more
efficacious in the relief of rigidity than tremor; but tremor, fatigue, weakness,
and sluggishness are frequently beneficially influenced. It can be substituted
for all the previous medications in mild and moderate cases. For the control
of more severe cases, other drugs may be added to procyclidine therapy as
Clinical reports indicate that
procyclidine often successfully relieves the symptoms of extrapyramidal dysfunction
(dystonia, dyskinesia, akathisia, and parkinsonism) which accompany the therapy
of mental disorders with phenothiazine and rauwolfia compounds. In addition
to minimizing the symptoms induced by tranquilizing drugs, the drug effectively
controls sialorrhea resulting from neuroleptic medication. At the same time,
freedom from the side effects induced by tranquilizer drugs, as provided by
the administration of procyclidine, permits a more sustained treatment of
the patient’s mental disorder.
in the treatment of parkinsonism indicate that most patients experience subjective
improvement characterized by a feeling of well-being and increased alertness,
together with diminished salivation and a marked improvement in muscular coordination
as demonstrated by objective tests of manual dexterity and by increased ability
to carry out ordinary self-care activities. While the drug exerts a mild atropine-like
action and therefore causes mydriasis, this may be kept minimal by careful
adjustment of the daily dosage.
Procyclidine hydrochloride should not be used in angle-closure
glaucoma although simple type glaucomas do not appear to be adversely affected.
Use in Children: Safety
and efficacy have not been established in the pediatric age group; therefore,
the use of procyclidine hydrochloride in this age group requires that the
potential benefits be weighed against the possible hazards to the child.
Pregnancy Warning: The safe use of this drug in
pregnancy has not been established; therefore, the use of procyclidine hydrochloride
in pregnancy, lactation, or in women of childbearing age requires that the
potential benefits be weighed against the possible hazards to the mother and
Conditions in which inhibition of the parasympathetic nervous
system is undesirable, such as tachycardia and urinary retention (such as
may occur with marked prostatic hypertrophy), require special care in the
administration of the drug. Hypotensive patients who receive the drug should
be observed closely. Occasionally, particularly in older patients, mental
confusion and disorientation may occur with the development of agitation,
hallucinations, and psychotic-like symptoms.
with mental disorders occasionally experience a precipitation of a psychotic
episode when the dosage of antiparkinsonism drugs is increased to treat the
extrapyramidal side effects of phenothiazine and rauwolfia derivatives.
Anticholinergic effects can be produced by therapeutic doses
although these can frequently be minimized or eliminated by careful dosage.
They include: dryness of the mouth, mydriasis, blurring of vision, giddiness,
lightheadedness, and gastrointestinal disturbances such as nausea, vomiting,
epigastric distress, and constipation. Occasionally an allergic reaction such
as a skin rash may be encountered. Feelings of muscular weakness may occur.
Acute suppurative parotitis as a complication of dry mouth has been reported.
Dosage and Administration
For Parkinsonism: The
dosage of the drug for the treatment of parkinsonism depends upon the age
of the patient, the etiology of the disease, and individual responsiveness.
Therefore, the dosage must remain flexible to permit adjustment to the individual
tolerance and requirements of each patient. In general, younger and postencephalitic
patients require and tolerate a somewhat higher dosage than older patients
and those with arteriosclerosis.
Patients Who Have Received No Other Therapy: The usual dose of procyclidine
hydrochloride for initial treatment is 2.5 mg administered three times daily
after meals. If well tolerated, this dose may be gradually increased to 5
mg three times a day and occasionally 5 mg given before retiring. In some
cases smaller doses may be employed with good therapeutic results.
a patient is encountered who cannot tolerate a bedtime dose of the drug. In
such cases it may be desirable to adjust dosage so that the bedtime dose is
omitted and the total daily requirement is administered in three equal daytime
doses. It is best administered during or after meals to minimize the development
of side reactions.
Patients to KEMADRIN from Other Therapy: Patients who have been
receiving other drugs may be transferred to procyclidine hydrochloride. This
is accomplished gradually by substituting 2.5 mg three times a day for all
or part of the original drug. The dose of procyclidine is then increased as
required while that of the other drug is correspondingly omitted or decreased
until complete replacement is achieved. The total daily dosage may then be
adjusted to the level which produces maximum benefit.
For Drug-Induced Extrapyramidal Symptoms: For treatment
of symptoms of extrapyramidal dysfunction induced by tranquilizer drugs during
the therapy of mental disorders, the dosage of procyclidine hydrochloride
will depend on the severity of side effects associated with tranquilizer administration.
In general, the larger the dosage of the tranquilizer, the more severe will
be the associated symptoms, including rigidity and tremors. Accordingly, the
drug dosage should be adjusted to suit the needs of the individual patient
and to provide maximum relief of the induced symptoms. A convenient method
to establish the daily dosage of procyclidine is to begin with the administration
of 2.5 mg three times daily. This may be increased by 2.5 mg daily increments
until the patient obtains relief of symptoms. In most cases excellent results
will be obtained with 10 to 20 mg daily.
White, scored tablets containing 5 mg procyclidine hydrochloride,
imprinted with “KEMADRIN” and “S3A” in bottles
of 100 (NDC 61570-059-01).
Store at 15° to 25°C
(59° to 77°F) in a dry place.