Source: Health Products Regulatory Authority (IE) Revision Year: 2018 Publisher: Amdipharm Limited, Temple Chambers, 3 Burlington Road, Dublin 4, Ireland.
Pharmacotherapeutic group: Piperazine derivatives
ATC Code: R06AE03
Cyclizine is a histamine H1 receptor antagonist of the piperazine class, which is characterised by a low incidence of drowsiness. It possesses anticholinergic and antiemetic properties. The exact mechanism by which cyclizine can prevent or suppress both nausea and vomiting from various causes is unknown. Cyclizine increases lower oesophageal sphincter tone and reduces the sensitivity of the labyrinthine apparatus. It may inhibit the part of the midbrain known collectively as the emetic centre.
Cyclizine produces its antiemetic effect within 2 hours and lasts approximately 4 hours.
In healthy adult volunteers the administration of a single oral dose of 50mg cyclizine resulted in the peak plasma concentration of approximately 70ng/mL occurring at about two hours after drug administration.
The plasma elimination half-life was approximately 20 hours.
The N-demethylated derivative, norcyclizine, has been identified as a metabolite of cyclizine. Norcyclizine has little antihistaminic (H1) activity compared to cyclizine and has a plasma elimination half-life of approximately 20 hours.
After a single dose of 50 mg cyclizine given to a single adult male volunteer, urine collected over the following 24 hours contained less than 1% of the total dose administered.
Cyclizine was not mutagenic in a full Ames test, including use of S9-microsomes but can nitrosate in vitro to form mutagenic products.
No long term studies have been conducted in animals to determine whether cyclizine has a potential for carcinogenesis. However, long-term studies with cyclizine administered with nitrate have indicated no carcinogenicity.
Some animal studies are interpreted as indicating that Cyclizine may be teratogenic at dose levels up to 25 times the clinical dose level. In another study, cyclizine was negative at oral dose levels up to 65 mg/kg in rats and 75 mg/kg in rabbits. The relevance of these studies to the human situation is not known.
In a study involving prolonged administration of cyclizine to male and female rats there was no evidence of impaired fertility after continuous treatment for 90-100 days at dose levels of approximately 15 and 25 mg/kg/day. There is no experience of the effect of Valoid Tablets on human fertility.
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