|
This information has been developed and provided by an independent third-party source. Merck & Co., Inc. does not endorse and is not responsible for the accuracy of the content, or for practices or
standards of non-Merck sources.
Pronunciation
(MEK li zeen)
Generic Available (U.S.)
Yes
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Prevention and treatment of symptoms of motion sickness; management of vertigo with diseases affecting the vestibular system
Pregnancy Risk Factor
B
Pregnancy Considerations
No data available on crossing the placenta. Probably no effect on the fetus (insufficient data). Available evidence suggests safe use during pregnancy.
Lactation
Excretion in breast milk unknown/not recommended
Contraindications
Hypersensitivity to meclizine 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).
Disease-related concerns:
• Asthma: Use with caution in patients with asthma.
• Glaucoma: Use with caution in patients with narrow-angle glaucoma; condition may be exacerbated by cholinergic blockade. Screening is recommended.
• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture.
• Pyloric/duodenal obstruction: Use with caution in patients with pyloric or duodenal obstruction.
Special populations:
• Elderly: Use with caution in the elderly; may be more sensitive to adverse effects.
• Pediatrics: Safety and efficacy have not been established in children <12 years of age.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Other warnings/precautions:
• Lack of response: If vertigo does not respond in 1-2 weeks, it is advised to discontinue use.
Adverse Reactions
>10%:
Central nervous system: Slight to moderate drowsiness
Respiratory: Thickening of bronchial secretions
1% to 10%:
Central nervous system: Headache, fatigue, nervousness, dizziness
Gastrointestinal: Appetite increase, weight gain, nausea, diarrhea, abdominal pain, xerostomia
Respiratory: Pharyngitis
<1%: Palpitation, hypotension, depression, sedation, photosensitivity, rash, angioedema, urinary retention, hepatitis, myalgia, tremor, paresthesia, blurred vision, bronchospasm, epistaxis
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.
Mechanism of Action
Has central anticholinergic action by blocking chemoreceptor trigger zone; decreases excitability of the middle ear labyrinth and blocks conduction in the middle ear vestibular-cerebellar pathways
Pharmacodynamics/Kinetics
Onset of action: ~1 hour (Wang, 2011a)
Duration: ~24 hours (Wang, 2011a)
Distribution: Vd: 7 L/kg (Wang, 2011a)
Metabolism: Hepatic to norchlorcyclizine (Wang, 2011a)
Half-life elimination: 5 hours (Wang, 2011a; Wang, 2011b)
Time to peak, plasma: 3 hours (Wang, 2011a; Wang, 2011b)
Excretion: Urine and feces as unchanged drug and metabolites (Wang, 2011a)
Dosage
Children >12 years and Adults: Oral:
Motion sickness: 12.5-25 mg 1 hour before travel, repeat dose every 12-24 hours if needed; doses up to 50 mg may be needed
Vertigo: 25-100 mg/day in divided doses
Patient Education
Avoid alcohol. You may experience dizziness, drowsiness, blurred vision, dry mouth, constipation, or heat intolerance. Report CNS change (hallucination, confusion, nervousness), sudden or unusual weight gain, unresolved nausea or diarrhea, chest pain or palpitations, muscle pain, or changes in urinary pattern.
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. If vertigo does not respond in 1-2 weeks, discontinue use.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Slight to moderate drowsiness, thickening of bronchial secretions, significant 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; may cause dizziness or nervousness; may rarely cause sedation or depression
Mental Health: Effects on Psychiatric Treatment
Concurrent use with psychotropic may produce additive sedation and dry mouth
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Caplet, oral, as hydrochloride: 12.5 mg
Tablet, oral, as hydrochloride: 12.5 mg, 25 mg
Antivert®: 12.5 mg, 25 mg, 50 mg
Dramamine® Less Drowsy Formula: 25 mg
Medi-Meclizine: 25 mg
Trav-L-Tabs®: 25 mg
Tablet, chewable, oral, as hydrochloride: 25 mg
Bonine®: 25 mg [scored; raspberry flavor]
Pricing: U.S. (www.drugstore.com)
Tablets (Antivert)
12.5 mg (30): $30.09
25 mg (30): $44.09
50 mg (30): $69.45
Tablets (Meclizine HCl)
12.5 mg (30): $12.99
25 mg (30): $19.99
References
Oosterveld WJ, “Vertigo: Current Concepts in Management,” Drugs, 1985, 30(3):275-83.
Park J, Logan R, and Pottage A, “Drug-Induced Extrapyramidal Signs in Chronic Liver Disease - A Case Report,” Clin Toxicol, 1977, 11(1):117-20.
Wang Z, Lee B, Pearce D, et al, "Meclizine Metabolism and Pharmacokinetics: Formulation on Its Absorption," J Clin Pharmacol, 2011a, [epub ahead of print]
Wang Z, Qian S, Zhang Q, et al, "Quantification of Meclizine in Human Plasma by High Performance Liquid Chromatography-Mass Spectrometry," J Chromatogr B Analyt Technol Biomed Life Sci, 2011b, 879(1):95-9.
International Brand Names
Lexi-Comp.com
Last full review/revision February 2012
|
