Mequitazine(trade name Primalan) is an H1 antagonist and antihistamine of the phenothiazine chemical class. It is used to treat allergies and rhinitis. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
This compound belongs to the class of organic compounds known as phenothiazines. These are polycyclic aromatic compounds containing a phenothiazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a para-thiazine ring.
Mequitazine is a phenothiazine derivative with antihistaminic effect, which can simultaneously act in the following four aspects:
- Blocking mast cell degranulation.
- antagonize the action of proinflammatory mediators such as histamine on peripheral H1 receptors.
- mild anticholinergic effect.
- regulate the tension of the vagus nerve and prevent the development of chronic symptoms. It has the advantages of quick effect, long-lasting efficacy, difficulty in passing the blood-brain barrier and no continued toxicity.
Oral absorption through the gastrointestinal tract is rapid, 2 to 4 hours effective, not easy to penetrate the blood-cerebrospinal fluid barrier. Eliminated from the body 38 hours after oral administration, this product is metabolized by the liver. Most are excreted by bile, and about 20% is excreted from the urine.
(Mequitazine binds to the histamine H1 receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.)
For the treatment of Hay fever, urticaria (hives) and allergic rhinitis. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
Enhances the effects of CNS depressants eg alcohol, barbiturates, hypnotics, opioid analgesics, anxiolytics and antipsychotics. Can mask signs of ototoxicity caused by aminoglycosides. QT prolongation (which can lead to torsades de pointes arrhythmia) reported with spiramycin.
Antihistamines (H 1 -receptor antagonists) are widely prescribed to treat symptoms of seasonal and perennial allergic rhinitis and chronic urticaria. (Drowsiness and impairment of cognition and psychomotor performance have been reported as adverse events in many trials, and all antihistamines appear to have some sedative properties. Sedation, however, may be a direct result of allergic rhinitis, and the degree of sedation may depend on each individual's response to antihistamine therapy, and thus cannot be predicted.)
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