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A Comprehensive Guide Describing The Properties Of The Drugs By Generic Origin
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Cyclizine Hcl  ( Antihistamines, Systemic.... )
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Mode Of Action

Cyclizine is a piperazine derivative with histamine H1-receptor antagonist (antihistamine) activity. The precise mechanism of action in inhibiting the symptoms of motion sickness is not well understood. It may have effects directly on the labyrinthine apparatus and on the chemoreceptor trigger zone. Cyclizine exerts a central anticholinergic (antimuscarinic) action.

Pharmacokinetics

The pharmacokinetics of cyclizine, a piperazine derivative useful in the prevention and treatment of nausea and vomiting, was investigated in six healthy male volunteers following an intravenous bolus dose. The drug is extensively distributed with a mean volume of distribution of 16.50 ± 3.33 l/kg and a mean total clearance of 0.870 ± 0.105 l/h per kg. Urinary excretion data showed that less than one percent of the dose was excreted up to 36 h as unchanged drug in the urine. The extremely low mean renal clearance (0.005 ± 0.002 l/h per kg) for the parent drug comprised only a small proportion of total clearance indicating that urinary excretion of parent drug is not a major route of elimination for cyclizine. The drug appears to exhibit biexponential pharmacokinetics and has a terminal elimination half-life of approximately 13 h.

Indications

Cyclizine is an antihistamine drug used to treat nausea, vomiting and dizziness associated with motion sickness, vertigo and post-operatively following administration of general anaesthesia and opioids. It is also used recreationally as an opiate/opioid-enhancing antihistamine booster and separately for its anticholinergic effects.

Contraindications

Its antimuscarinic action warrants caution in patients with prostatic hypertrophy, urinary retention, or glaucoma. Liver disease exacerbates its sedative effects. It cannot be combined with diclofenac, for example in the same syringe or bag of fluids, as a crystallisation reaction occurs.

Side Effects

Common (over 10%) – Drowsiness, xerostomia (dry mouth)
Uncommon (1% to 10%) – Headache, psychomotor impairment, and antimuscarinic effects such as urinary retention, diplopia (blurred vision), dermatitis, and gastro-intestinal disturbances.
Rare – Hypersensitivity reactions (bronchospasm, angioedema, anaphylaxis, rashes and photosensitivity reactions), extrapyramidal effects, dizziness, confusion, depression, sleep disturbances, tremor, liver dysfunction and hallucinations.

Drug Interactions

Avoid use in combinaations with alcohol or » CNS depression–producing medications, anticholinergics or other medications with anticholinergic activity and apomorphine.

Precautions

Patient should observe caution while driving or performing other task requiring alertness because it may produce dizziness. Cyclizine should be used with caution in patients with asthma, glaucoma, obstructive disease of gastrointestinal tract.

Usage in Pregnancy & Lactation

Pregnancy: Problems in humans have not been documented.
It is not known whether cyclizine is distributed into breast milk. However, problems in humans have not been documented. Because of its anticholinergic actions, cyclizine may inhibit lactation.

Dosage & Administration

Adult Dosage (>12 years):
50mg 8 hourly, PO,IV,IM
Paedriatic Dosage (20 Kg):
2.500 mg/kg or As recommended, Oral/injectable, as required.

Brands Available in Pakistan
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