Cyclizine

(sye-kli-zeen)

PCaution when used during lactation : Caution when used during pregnancy

LCaution when used during lactation : Caution when used during lactation

Molecule Info

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Indication(s) & Dosage

Oral route

Nausea and vomiting  Adult: As hydrochloride: 50 mg orally up to tid, up to 200 mg/day.  For prevention of motion sickness, 1st dose should be given 30 min before travelling.  Child: 6-12 yr: As hydrochloride: 25 mg orally up to tid.  For prevention of motion sickness, 1st dose should be given 30 min before travelling.  

Renal impairment: Dose reductions may be needed.

Hepatic impairment: Avoid in severe liver disease.  

Parenteral route

Treatment and prophylaxis of motion sickness  Adult: As lactate: 50 mg IV/IM every 4-6 hr.  1st dose should be given 30 min before travelling.  Child: As lactate: 25 mg IV/IM up to tid.  For prevention of motion sickness, 1st dose should be given 30 min before travelling.  

Renal impairment: Dose reductions may be needed.

Hepatic impairment: Avoid in severe liver disease.  

Prophylaxis of postoperative nausea and vomiting  Adult: As lactate: 50 mg up to tid, may be given via IV or IM admin.  1st dose should be given 20 min before anticipated end of surgery.  Max: 200 mg/24 hr.  Child: 6-12 yr: As lactate: 25 mg up to tid, may be given via IV or IM admin.  1st dose should be given 20 min before anticipated end of surgery.  Max: 50 mg tid.  

Renal impairment: Dose reductions may be needed. Hepatic impairment: Avoid in severe liver disease.

Special Populations: Prevention of motion sickness: Give 30 min before traveling.

Incompatibility: Cyclizine lactate may be incompatible with oxytetracycline hydrochloride, chlortetracycline hydrochloride, benzylpenicillin and solutions with a pH ≥6. 8. 

Overdosage

Dry mouth, blurred vision, tachycardia, urinary retention, drowsiness, dizziness, inco-ordination, ataxia, weakness, hyperexcitability, disorientation, impaired judgement, hallucinations, hyperkinesia, extrapyramidal motor disturbances, convulsions, hyperpyrexia and respiratory depression.  Gastric lavage followed by supportive measures for respiration and circulation.

Contraindications

Premature or full-term neonates.

Special Precautions

Angle closure glaucoma; urinary retention; prostatic hypertrophy; pyloroduodenal obstruction; epilepsy, severe CV disorders; known or suspected QT interval prolongation; hypokalaemia or other electrolyte imbalances; asthma; hepatic impairment.  May impair ability to drive or operate machinery.  Tolerance with prolonged use.  Broken or eczematous skin.  Pregnancy and lactation.  Elderly.  Children <6 yr.  Dependence.

Adverse Drug Reaction(s)

CNS depression e. g.  drowsiness to deep sleep, lassitude, dizziness and incoordination.  Headache, psychomotor impairment, dry mouth, thickening of mucous secretions, blurred vision, difficult or painful urination, constipation and increased gastric reflux.  Occasionally, GI disturbances, palpitations and arrhythmias.  Rashes and hypersensitivity reactions.  Blood dyscrasias.  Convulsions, sweating, myalgia, paraesthesias, extrapyramidal effects, tremor, sleep disturbances, tinnitus, hypotension and hair loss.

Drug Interactions

Enhanced sedative effects of alcohol, barbiturates, hypnotics, opioid analgesics, anxiolytic sedatives, antipsychotics.  Additive antimuscarinic actions with other antimuscarinic drugs and some antidepressants.  May mask ototoxicity symptoms caused by aminoglycoside antibiotics.

Pregnancy Category (FDA)

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect that was not confirmed in controlled studies in women in the 1sttrimester.

Pharmacology

Cyclizine is a sedative antihistamine with antimuscarinic activity. Onset: Within 2 hr upon GI absorption. Duration: Approximately 4 hr.  Absorption: Absorbed from the GI tract.  Metabolism: Hepatically metabolised to relatively inactive metabolite.  Excretion: Plasma elimination half-lives of 20 hr.

ATC Classification

R06AE03 - cyclizine; Belongs to the class of piperazine derivatives used as systemic antihistamines.

 

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