Products
Mizolastine was commercially available in tablet form (Mizollen, 10 mg) and approved in many countries since 1996. The tablets are no longer available today. For example, fexofenadine (Telfast) or another 2nd-generation antihistamine can be used as an alternative.
Structure and properties
Mizolastine (C24H25FN6O, Mr = 432.5 g/mol) a piperidine and benzimidazole derivative. It is structurally related to astemizole (Hismanal, out of commerce).
Effects
Mizolastine (ATC R06AX25) is long-acting antihistamine, antiallergic, and anti-inflammatory. The effects are due to antagonism at histamine H1 receptors. It may have potential to prolong the QT interval; the literature is not consistent on this point.
Indications
For symptomatic treatment of hay fever, allergic rhinitis, allergic conjunctivitis, and chronic urticaria.
Dosage
According to the SmPC. The drug may be administered once daily due to its long half-life of 13 hours.
Contraindications
Mizolastine is contraindicated in hypersensitivity, treatment with macrolides and azole antifungals, treatment with drugs that prolong the QT interval, significant changes in liver function, significant cardiac disease or arrhythmias, if the QT interval is prolonged, electrolyte imbalances, hypokalemia, and significant bradycardia. For complete precautions, see the drug label.
Interactions
Mizolastine is conjugated and metabolized via CYP3A4 and other pathways. Therefore, combination with CYP3A4 inhibitors is contraindicated because an increase in concentration may occur.
Adverse effects
The most common adverse effects include diarrhea, abdominal pain, dry mouth, nausea, weakness, increased appetite, headache, drowsiness, and dizziness. Occasionally, rapid pulse, palpitations, and low blood pressure have been reported. Very rarely, severe allergic reactions may occur. Prolongation of the QT interval cannot be ruled out.
