Adult: For the prevention and treatment of cases associated with motion sickness or radiotherapy: As cyclizine lactate: 50 mg up to tid via IM or slow IV inj. Treatment recommendations may vary among countries (refer to specific local guidelines).
Intramuscular, Intravenous Postoperative nausea and vomiting
Adult: As cyclizine lactate: 50 mg up to tid via IM or slow IV inj; 1st dose should be given via slow IV inj 20 minutes before the anticipated end of surgery. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Intravenous Prophylaxis of acid aspiration during general anaesthesia
Adult: For patients undergoing emergency surgery: As cyclizine lactate: 25 mg prior to induction of general anaesthesia. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Oral Motion sickness
Adult: As cyclizine hydrochloride: Treatment: 50 mg up to tid. Prevention: 50 mg up to tid; 1st dose should be given at least 1-2 hours before travelling. Dosing recommendations may vary among individual products and between countries (refer to specific product guidelines). Child: As cyclizine hydrochloride: 6-12 years Treatment: 25 mg up to tid. Prevention: 25 mg up to tid; 1st dose should be given at least 1-2 hours before travelling. >12 years Same as adult dose.
Oral Nausea and vomiting
Adult: For the prevention and treatment of cases associated with radiotherapy or postoperative period: As cyclizine hydrochloride: 50 mg up to tid. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines). Child: For the prevention and treatment of cases associated with radiotherapy or postoperative period: As cyclizine hydrochloride: 6-12 years 25 mg up to tid; >12 years Same as adult dose. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Incompatibility
Cyclizine lactate: May be incompatible with oxytetracycline hydrochloride, chlortetracycline hydrochloride, benzylpenicillin and solutions with a pH of ≥6.8.
Contraindications
Acute alcohol intoxication.
Special Precautions
Patient with severe heart failure or acute MI, hypertension, gastrointestinal obstruction, glaucoma, underlying neuromuscular disorders, phaeochromocytoma, prostatic hyperplasia or urinary retention, compromised respiratory function (including asthma or COPD), epilepsy, history of drug abuse or acute alcohol disorder. Avoid use in patients with porphyria. Concomitant use with other CNS depressants (e.g. anaesthetics, hypnotics, tranquillisers). Hepatic impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Anticholinergic effects (e.g. constipation, xerostomia, blurred vision, urinary retention), CNS effects (e.g. drowsiness, sedation, restlessness, excitation, nervousness, tremors, seizures, insomnia); extrapyramidal symptoms and dystonic reactions. Cardiac disorders: Tachycardia, palpitations, arrythmias. Ear and labyrinth disorders: Tinnitus. Eye disorders: Oculogyric crisis. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain. General disorders and administration site conditions: Asthenia. Hepatobiliary disorders: Hepatic dysfunction, cholestatic jaundice, cholestatic hepatitis. Immune system disorders: Hypersensitivity reactions including anaphylaxis. Metabolism and nutrition disorders: Loss of appetite. Musculoskeletal and connective tissue disorders: Twitching, muscle spasms. Nervous system disorders: Transient speech disorders, paraesthesia, chorea. Psychiatric disorders: Auditory and visual hallucinations, disorientation, euphoria. Respiratory, thoracic and mediastinal disorders: Bronchospasm, apnoea. Skin and subcutaneous tissue disorders: Urticaria, rash, angioedema, fixed drug eruption, allergic skin reaction, photosensitivity. Vascular disorders: Hypertension, hypotension.
Patient Counseling Information
This drug may cause CNS effects which may impair motor skills, if affected, do not drive or operate machinery.
Monitoring Parameters
Assess for CNS effects (including sedation, extrapyramidal symptoms) and relief of symptoms.
Overdosage
Symptoms: Peripheral anticholinergic effects (e.g. blurred vision, tachycardia, urinary retention; dry mouth, nose, and throat) and CNS effects (e.g. drowsiness, dizziness, incoordination, ataxia, weakness, hyperexcitability, impaired judgment, disorientation, hallucinations, hyperkinesia, extrapyramidal motor disturbances, convulsion, hyperpyrexia, respiratory depression). Management: Perform gastric lavage and supportive measures for respiration and circulation if needed. Administer parenteral anticonvulsant medication in case of convulsions.
Drug Interactions
May cause additive effects with other CNS depressants (e.g. hypnotics, tranquillisers, anaesthetics, antipsychotics, barbiturates). Enhanced soporific effect of pethidine. May counteract the haemodynamic benefits of opioid analgesics. Additive anticholinergic action with other anticholinergic drugs (e.g. atropine, some antidepressants [TCAs and MAOIs]). May mask the signs of ototoxicity caused by ototoxic drugs (e.g. aminoglycoside antibacterials).
Food Interaction
May enhance the CNS depressant effect of alcohol.
Lab Interference
May suppress the wheal and flare reactions to skin test antigens.
Action
Description: Mechanism of Action: Cyclizine, a piperazine derivative, is a histamine H1 receptor antagonist with anticholinergic and antiemetic properties. The exact mechanism by which it can prevent nausea and vomiting is unknown; however, it may inhibit the part of the midbrain collectively referred to as the emetic centre. In addition, it also increases lower oesophageal sphincter tone and decreases labyrinth apparatus sensitivity. Onset: Within 2 hours. Duration: Approx 4 hours. Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract (oral). Bioavailability: Approx 40% (oral). Time to peak plasma concentration: 4 ± 2 hours (oral); approx 2 hours (IV). Distribution: Enters breast milk. Metabolism: Metabolised in the liver via N-demethylation to form the relatively inactive metabolite, norcyclizine. Excretion: Via urine (<1%, as unchanged drug). Elimination half-life: 26 ± 7 hours (oral); 13.53 ± 2.33 hours (IV).
Chemical Structure
Cyclizine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6726, Cyclizine. https://pubchem.ncbi.nlm.nih.gov/compound/Cyclizine. Accessed June 25, 2024.