Cyclizine
| 180px | |
| Cyclizine
| |
| Systematic (IUPAC) name | |
| 1-benzhydryl-4-methyl-piperazine | |
| Identifiers | |
| CAS number | |
| ATC code | R06 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C18H22N2 |
| Mol. mass | 266.381 g/mol |
| SMILES | & |
| 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
- British National Formulary 45 March 2003
Deliriants (anticholinergic hallucinogens) | |
|---|---|
| Tropanes | Atropine, Hyoscyamine, Scopolamine |
| Benzilates | Benactyzine, Dicyclomine, N-Ethyl-3-piperidyl benzilate, N-Methyl-3-piperidyl benzilate, 3-Quinuclidinyl benzilate |
| Antihistamines | Cyclizine, Dimenhydrinate, Diphenhydramine, Doxylamine, Promethazine |
| Others | Benzydamine, Biperiden, Trihexyphenidyl |
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