PRIMALAN Tablet Ref.[7688] Active ingredients: Mequitazine

Source: Medicines & Healthcare Products Regulatory Agency (GB)  Revision Year: 2011  Publisher: Pierre Fabre Medicament 45, Place Abel Gance, 92100, Boulogne, France

Pharmacodynamic properties

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.

Pharmacokinetic properties

Absorption

Mequitazine is readily absorbed from the gastrointestinal tract.

Distribution

The apparent volume of distribution is high, indicating that mequitazine is extensively distributed outside the vascular compartment.

Biotransformation

Mequitazine is metabolised by the liver.

Elimination

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.

Preclinical safety data

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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