Cyclizine

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Image:Cyclizine.svg
Cyclizine
Systematic (IUPAC) name
1-benzhydryl-4-methyl-piperazine
Identifiers
CAS number 82-92-8
ATC code R06AE03
PubChem 6726
DrugBank APRD00061
Chemical data
Formula C18H22N2 
Mol. mass 266.381 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism N-demethylated to inactive norcyclizine
Half life 20 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

A (Au)

Legal status

P/POM (UK)

Routes Oral, IM, IV

Overview

Cyclizine is an antihistamine drug used to treat nausea, vomiting and dizziness associated with motion sickness, vertigo and post-operative following administration of general anaesthesia and opioids.

Pharmacology

Cyclizine is a piperazine derivative with histamine H1-receptor antagonist (antihistamine) activity. The precise mechanism of action in inhibiting the symptoms of motion sickness is not well understood. It may have effects directly on the labyrinthine apparatus and on the chemoreceptor trigger zone. Cyclizine exerts a central anticholinergic (antimuscarinic) action.

Contraindications

Its antimuscarinic action warrants caution in patients with prostatic hypertophy, urinary retention, glaucoma. Liver disease exacerbates its sedative effects. It cannot be combined with diclofenac, for example in the same syringe or bag of fluids, as a crystallisation reaction occurs.

Side effects

Common (>10%) - Drowsiness

Uncommon (1% to 10%) - Headache, psychomotor impairment, and antimuscarinic effects such as urinary retention, xerostomia (dry mouth), blurred vision and gastro-intestinal disturbances.

Rare - Hypersensitivity reactions (bronchospasm, angioedema, anaphylaxis, rashes and photosensitivity reactions), extrapyramidal effects, dizziness, confusion, depression, sleep disturbances, tremor, liver dysfunction.

Formulations

As cyclizine hydrochloride 50mg tablets and cyclizine lactate solution for intramuscular or intravenous injection (Brand names: Valoid® in UK and Marezine®, Marzine® and Emoquil® in US)).

References

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Acknowledgement and Attribution Regarding Sources of Content

Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .