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
N2 
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 opioids.

Pharmacology

Cyclizine is a 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

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.