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Cyclizine



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 search in 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) OTC (NL)

Routes Oral, IM, IV

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.

Additional recommended knowledge

Contents

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 hypertrophy, 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, xerostomia (dry mouth)

Uncommon (1% to 10%) - Headache, psychomotor impairment, and antimuscarinic effects such as urinary retention, diplopia (blurred vision), dermatitis, 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)).

Abuse

In the UK the drug was removed from the shelves as an OTC preparation in the mid 80s because of it's interaction with opiates. It served to increase the 'flash' of injected opiates. Since opiate users would regularly use high doses, the number of ER room admissions due to seizures became a notable public health risk. Even so, the drug remains available on the internet and pockets of abuse still exist in the UK.

References

  • British National Formulary 53 2007

Lexi-Online drug database http://online.lexi.com/crlsql/servlet/crlonline

 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Cyclizine". A list of authors is available in Wikipedia.
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