Procyclidine

Trade Names:
Kemadrin
- Tablets 5 mg

Pharmacology

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Has atropine-like action and exerts antispasmodic effect on smooth muscle. Is potent mydriatic and inhibits salivation; normally has no sympathetic ganglion-blocking activity.

Pharmacokinetics

Absorption

Procyclidine hydrochloride is well-absorbed from the GI tract. T _max is 1.1 to 2 h. C _max is 80 mcg/L. Bioavailability is 52% to 97% (oral).

Elimination

The t _½ is 11.5 to 12.6 h.

Duration

4 h (oral).

Indications and Usage

Treatment of parkinsonism, including postencephalitic, arteriosclerotic, and idiopathic types. Usually more efficacious in relief of rigidity than of tremor and can be used alone in mild to moderate cases. Also can be given to treat drug-induced extrapyramidal symptoms of phenothiazine or rauwolfia therapy and to control sialorrhea associated with neuroleptic medication.

Contraindications

Angle closure glaucoma; pyloric and duodenal obstruction; stenosing peptic ulcers; prostatic hypertrophy; bladder neck obstruction; achalasia; myasthenia gravis; megacolon.

Dosage and Administration

PO 2.5 mg 3 times daily after meals initially. If well tolerated, dose may be gradually increased to 5 mg 3 times daily. Bedtime dose can be added if necessary.

Substitute 2.5 mg 3 times daily for all or part of original agent. Increase as needed while other drug is lowered or omitted. Individualize (max dose, 60 mg/day).

Begin with 2.5 mg 3 times daily; increase by 2.5 mg increments until symptoms are relieved. Usually 10 to 20 mg/day is adequate.

General Advice

Give with food if GI upset is experienced.

Storage/Stability

Store at room temperature in tightly closed container.

Drug Interactions

Schizophrenic symptoms may worsen, haloperidol levels may decrease and tardive dyskinesia may develop.

Actions of phenothiazines may be decreased. Anticholinergic adverse reactions may increase.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Tachycardia; palpitations; orthostatic hypotension.

CNS

Disorientation; confusion; memory loss; hallucinations; agitation; nervousness; depression; drowsiness; giddiness; lightheadedness.

Dermatologic

Rash; urticaria; decreased sweating.

EENT

Mydriasis; blurred vision.

GI

Dry mouth; nausea; vomiting; epigastric distress; constipation; paralytic ileus.

Genitourinary

Urinary retention; urinary hesitancy.

Miscellaneous

Muscle weakness; acute suppurative parotitis; hyperthermia; heat stroke.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

More susceptible to adverse reactions. Occasionally may exhibit confusion, disorientation, agitation, hallucinations, and psychotic-like symptoms.

Special Risk Patients

Use caution in concurrent illness in which anticholinergic effects may be undesirable (ie, tachycardia, urinary retention, marked prostatic hypertrophy). Closely observe hypotensive patients.

Anticholinergic effects

Administration of other drugs with anticholinergic effects will increase incidence and severity of these effects.

CNS

Psychotic episode may be precipitated in treating drug-induced extrapyramidal adverse reactions of phenothiazines or rauwolfia derivatives.

Heat illness

Give with caution during hot weather.

Ophthalmic

Incipient narrow-angle glaucoma may be precipitated.

Overdosage

Symptoms

Circulatory collapse, respiratory depression or arrest, CNS depression preceded or followed by stimulation, psychosis, stupor, coma, seizures, fever, hot/dry/flushed skin, dry mucous membranes, paralytic ileus.

Patient Information

• Advise patient to use caution in hot weather as drug increases susceptibility to heat stroke.
• Instruct patient to report the following symptoms to health care provider immediately: pounding heartbeat, eye pain, confusion or skin rash. Also tell patient to report bothersome adverse reactions, including blurred vision, urinary retention or hesitancy, nausea, vomiting, constipation, dizziness, drowsiness, or dry mouth, nose, or throat.
• Tell patient to take sips of water frequently, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
• Instruct patient to avoid intake of alcoholic beverages or other CNS depressants.
• Advise patient that drug may cause drowsiness or dizziness and to use caution while driving or performing tasks requiring mental alertness.

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