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Cyclizine Drug Information Provided by Lexi-Comp

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Pronunciation

(SYE kli zeen)

Generic Available (U.S.)

No

Index Terms

  • Cyclizine Hydrochloride
  • Cyclizine Lactate

U.S. Brand Names

  • Bonine® for Kids [OTC]
  • Marezine® [OTC]

Pharmacologic Category

  • Histamine H1 Antagonist
  • Histamine H1 Antagonist, First Generation
  • Piperazine Derivative

Pharmacologic Category Synonyms

  • Antihistamine
  • Antihistamine, H1 Selective
  • H1 Antagonist
  • H1 Blocker
  • First Generation H1 Antagonist

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

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. Management: For patients being treated with hydroxyzine, a reduction in the dose of any other CNS depressants that are to be used in combination is recommended. With concurrent use, monitor patients closely for excessive response to the combination. 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.

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]

International Brand Names

  • Cyclizine FNA (NL)
  • Echnatol (AT)
  • Fortravel (AT)
  • Maremal (ES)
  • Marzine (CH, DK, FI, IT, NL, NO, SE)
  • Nausicalm (NZ)
  • Norizine (ZA)
  • Valoid (GB, IE)

Lexi-Comp.com

Last full review/revision May 2011

Content last modified May 2011

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