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Pronunciation
(SYE kli zeen)
Generic Available (U.S.)
No
Index Terms
Brand Names: U.S.
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Prevention and treatment of nausea, vomiting, and vertigo associated with motion sickness
Pregnancy Risk Factor
B
Contraindications
Hypersensitivity to cyclizine or any component of the formulation
Warnings/Precautions
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Other warnings/precautions:
• Self-medication (OTC use): Prior to self medication (OTC use) patients with asthma, glaucoma, prostatic hyperplasia, or respiratory disease should consult healthcare provider. Consult healthcare provider prior to frequent or prolonged use. Do not exceed recommended dose.
Adverse Reactions
>10%:
Central nervous system: Drowsiness
Gastrointestinal: Xerostomia
1% to 10%:
Central nervous system: Headache
Dermatologic: Dermatitis
Gastrointestinal: Nausea
Genitourinary: Urinary retention
Ocular: Diplopia
Renal: Polyuria
Metabolism/Transport Effects
None known.
Drug Interactions
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.
Storage
Store at 15°C to 25°C (59°F to 77°F). Protect from light.
Mechanism of Action
Cyclizine is a piperazine derivative with properties of histamines. The precise mechanism of action in inhibiting the symptoms of motion sickness is not known. It may have effects directly on the labyrinthine apparatus and central actions on the labyrinthine apparatus and on the chemoreceptor trigger zone. Cyclizine exerts a central anticholinergic action.
Pharmacodynamics/Kinetics
Distribution: Vd: 17 L/kg (range: 13-20 L/kg) (Walker, 1996)
Metabolism: Hepatic; Undergoes demethylation to inactive metabolites (norcyclizine and norchlorcyclizine) (Paton, 1985)
Half-life elimination: Cyclizine: ~14 hours; Norcyclizine: ~24 hours; Norchlorcyclizine: ~6 days (Paton, 1985; Walker, 1996)
Excretion: Urine (<1% as unchanged drug) (Walker, 1996)
Dosage
Oral: Motion sickness (prophylaxis and treatment):
Children 6-11 years: 25 mg 1 hour before travel or at onset of symptoms; repeat dose every 6-8 hours (maximum: 3 tablets/day)
Children ≥12 years and Adults: 50 mg taken 30 minutes before departure; may repeat in 4-6 hours if needed, up to 200 mg/day
Geriatric Considerations
Due to anticholinergic action, use lowest dose in divided doses to avoid side effects and their inconvenience; limit use if possible; may cause confusion or aggravate symptoms of confusion in those with dementia; constipation and difficulty voiding urine may occur
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Drowsiness is common
Mental Health: Effects on Psychiatric Treatment
Concurrent use with psychotropics may exacerbate the dry mouth and sedation commonly seen with cyclizine
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, oral, as hydrochloride:
Marezine®: 50 mg
Tablet, chewable, oral, as hydrochloride:
Bonine® for Kids: 25 mg [scored; berry blast flavor]
References
Paton DM and Webster DR, "Clinical Pharmacokinetics of H1-Receptor Antagonists (The Antihistamines)," Clin Pharmacokinet, 1985, 10(6):477-97.
Walker RB and Kanfer I, "Pharmacokinetics of Cyclizine Following Intravenous Administration to Human Volunteers," Eur J Pharm Sci, 1996, 4(5):301-6.
International Brand Names
Lexi-Comp.com
Last full review/revision February 2012
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