Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2011 Publisher: Pierre Fabre Medicament 45, Place Abel Gance, 92100, Boulogne, France
Pharmacotherapeutic group: Antihistamines for systemic use
ATC code: R06AD07
Mequitazine is a phenothiazine derivative with the actions and uses of antihistamines. Antihistamines diminish or abolish the main actions of histamine in the body by competitive, reversible blockade of histamine receptor sites on tissues; they do not inactivate histamine or prevent its synthesis or release. Antihistamines are used for palliative treatment of allergic reactions. Mequitazine is reported to cause less sedation than promethazine.
Mequitazine is readily absorbed from the gastrointestinal tract.
The apparent volume of distribution is high, indicating that mequitazine is extensively distributed outside the vascular compartment.
Mequitazine is metabolised by the liver.
The apparent elimination half-life is 18 hours.
The excretion of mequitazine and its metabolites is principally via the bile. The amount of unchanged mequitazine in the urine is very low.
No teratogenic effects were observed in animal studies with mequitazine.
Other preclinical effects were observed only at exposure considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use.
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