Zyclidine

Uses

Zyclidine is used for the adjunctive treatment of all forms of parkinsonian syndrome. It is mainly used for the symptomatic treatment of idiopathic (paralysis agitants), postencephalitic and arteriosclerotic parkinsonian. It is used to control troublesome extrapyramidal symptoms including pseudoparkinsonian, acute dystonic reactions and akathisia induced by neuroleptic drugs such as phenothiazine derivatives.

Zyclidine is also used to associated treatment for these conditions: Parkinsonian Syndromes, Extrapyramidal reaction

How Zyclidine works

The mechanism of action is unknown. It is thought that Zyclidine acts by blocking central cholinergic receptors, and thus balancing cholinergic and dopaminergic activity in the basal ganglia. Many of its effects are due to its pharmacologic similarities with atropine. Zyclidine exerts an antispasmodic effect on smooth muscle, and may produce mydriasis and reduction in salivation.

Dosage

Zyclidine dosage

Oral administration:

Adults: Zyclidine tablet is administered orally, preferably after meals.

• Parkinsonism: Initially 2.5 mg 3 times a day, then 5 mg 3 times a day and occasionally 5 mg at bed time. The dosage being adjusted as tolerated or until the total daily dose reaches 20 to 30 mg divided into 3 to 4 doses.
• Drug induced extrapyramidal symptom: Initially 2.5 mg 3 times a day. The dosage being increased by 2.5 mg increment per day as needed and tolerated.

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 children.

IM or IV administration:

By intramuscular or intravenous injection, 5-10 mg, repeated if necessary after 20 minutes; maximum 20 mg daily can be given.

Side Effects

At usual dosage levels dryness of the mouth is generally the only adverse effect. Mydriasis, blurred vision and adverse G.I. effects (nausea, vomiting, epigastric distress, constipation) occur occasionally. An allergic reaction (e.g. rash) or muscular weakness may occasionally occur. High doses may cause vertigo and possibly confusion and hallucination. Adverse effect may usually be minimized by adjustment of dosage and administration after meal.

Toxicity

LD₅₀=60 mg/kg (IV in mice)

Precaution

Precaution should be taken in case of hepatic & renal impairment, children, elderly, pregnancy and lactation condition. Patients with mental disorders occasionally experience a precipitation of a psychotic episode when Zyclidine is administered for the treatment of the extrapyramidal side-effects of neuroleptic. Zyclidine should not be withdrawn abruptly as rebound Parkinsonism symptoms may occur.

Interaction

The anticholinergic activity of procyclidine may be increased by agents having anticholinergic amantadine. The absorption of ketoconazole may be reduced by concomitant administration of procyclidine.

Food Interaction

• Take with or without food. Taking with food may reduce the adverse effects of procyclidine.

Zyclidine Alcohol interaction

[Moderate] GENERALLY AVOID:

Use of anticholinergic agents with alcohol may result in sufficient impairment of attention so as to render driving and operating machinery more hazardous.

In addition, the potential for abuse may be increased with the combination.

The mechanism of interaction is not established but may involve additive depressant effects on the central nervous system.

No effect of oral propantheline or atropine on blood alcohol levels was observed in healthy volunteers when administered before ingestion of a standard ethanol load.

However, one study found impairment of attention in subjects given atropine 0.5 mg or glycopyrrolate 1 mg in combination with alcohol.

Alcohol should generally be avoided during therapy with anticholinergic agents.

Patients should be counseled to avoid activities requiring mental alertness until they know how these agents affect them.

Zyclidine Hypertension interaction

[Minor] Cardiovascular effects of anticholinergics may exacerbate hypertension.

Therapy with anticholinergic agents should be administered cautiously in patients with hypertension.

Zyclidine Drug Interaction

Moderate: aripiprazole, citalopram, divalproex sodium, diazepam, gabapentin, oxycodone, risperidone, carbidopa / levodopa, valproic acid, alprazolam, olanzapineMinor: acetaminophenUnknown: isotretinoin, aspirin, nifedipine, amphetamine / dextroamphetamine, bisacodyl, albuterol, multivitamin, ascorbic acid

Zyclidine Disease Interaction

Major: autonomic neuropathy, GI obstruction, glaucoma, obstructive uropathy, tardive dyskinesia, infectious diarrheaModerate: cardiac disease, liver diseaseMinor: hypertension, hyperthyroidism

Pregnancy & Breastfeeding use

The safe use of this drug in pregnancy, lactation or in women of childbearing age requires that the potential benefits be weighed against the possible hazards to the mother and child.

Contraindication

It should be given with caution in children and geriatric patients. It is advisable to be cautious in giving Zyclidine to patients with diarrhoea and cardiovascular disease, glaucoma, urinary retention, hepatic or renal impairment. The safety of using procyclidine during pregnancy has not been established. No data are available on the excretion of this drug in breast milk.

Storage Condition

Store between 15-30° C. Protect from moisture.

Innovators Monograph

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