Meclozin

Products

Meclozine is marketed as a fixed combination with caffeine and the vitamin pyridoxine in the form of capsules and suppositories (Itinerol B6). It has been approved in many countries since 1953. In some countries, the active ingredient is also called. Itinerol dragées went out of commerce in 2015.

Structure and properties

Meclozine (C25H27ClN2, Mr = 390.9 g/mol) is present in drugs as meclozine dihydrochloride, a white to yellowish crystalline powder that is sparingly soluble in water. It is a racemate and a piperazine derivative. Meclozine is structurally related to other antihistamines, such as hydroxyzine and cetirizine.

Effects

Meclozine (ATC R06AE05) has antihistamine, antiemetic, anticholinergic, and depressant properties. The effects are due in part to antagonism at histamine receptors and muscarinic acetylcholine receptors. Effects occur within about one hour and last 12 to 24 hours. Meclozine has a half-life of 5 to 6 hours.

Indications

For the prevention and treatment of:

Meclozine could also be used to treat allergic diseases, but it is not approved for that purpose.

Dosage

According to the SmPC. To prevent motion sickness, the drug should be administered one hour before the planned activity.

Contraindications

Meclozin is contraindicated in hypersensitivity. It should be used with caution in narrow-angle glaucoma or benign prostatic enlargement. Meclozin may cause drowsiness and therefore should not be taken when full attention is required, such as when driving or operating heavy machinery. It should not be administered concomitantly with alcohol. For complete precautions, see the drug label.

Interactions

Meclozine is biotransformed by CYP2D6 and corresponding drug-drug interactions are possible. Centrally depressant drugs such as sedatives, antidepressants, and neuroleptics, as well as stimulants such as alcohol, may increase side effects.

Adverse effects

Possible adverse effects include:

First-generation antihistamines should be administered with caution to children and the elderly because of the potential for side effects.