Mizolastine is an active substance that belongs to the so-called H1 antihistamines. The drug is used in the vast majority of cases for the treatment of hay fever, urticaria and allergic inflammation of the conjunctiva. The treatment of the respective symptoms, not their causes, is in the foreground.
Causes of hay fever
The active ingredient mizolastine is primarily characterized by its anti-allergic effects. In addition, it belongs to the pharmaceutical category of second-generation antihistamines. The drug is usually administered orally in the form of tablets. The most common indications for prescription of the drug are hay fever, urticaria and allergic rhinitis. In the course of treatment with the drug mizolastine, side effects such as headache or digestive problems may occur. The drug mizolastine is metabolized by CYP3A4. In addition, the active ingredient mizolastine is thought to lead to QT time prolongation in some cases. The active ingredient mizolastine is also sometimes referred to by the synonymous term mizolastinum. The drug is available, for example, under the trade names Mizollen or Telfast. The latter is an antihistamine that belongs to the second generation. Basically, the active ingredient mizolastine is a derivative of benzimidazole and piperidine. In addition, the drug has a structural relationship with astemizole. The drug is available on the German market in a dosage of ten milligrams. These are film-coated tablets to be prescribed by the physician. Since there is a lack of empirical data and studies, the drug should not be used during pregnancy and breastfeeding. Currently, the drug mizolastine is prescribed relatively rarely. Reasons for this are possibly the high price of the drug as well as the lack of corresponding generics, since patent protection is currently still in effect.
Pharmacological action
The mechanism of action of mizolastine is characteristic of the substance. Basically, the drug is absorbed after a comparatively short time. In this way, the highest concentrations in the blood plasma occur after one to one and a half hours. Due to a relatively long half-life, the effect of the drug persists for about 24 hours. The active ingredient mizolastine is characterized by a particularly high affinity to the H1 receptors. In principle, the drug mizolastine is unable to cross the blood–brain barrier. For this reason, the drug only exerts its effect at the so-called peripheral H1 receptors. Therefore, it has virtually no sedative effects and thus differs from other types of antihistamines. However, transient drowsiness is possible. In addition, it is suspected that the active ingredient mizolastine also impairs the formation of leukotrienes. This results in the anti-inflammatory effect of the drug. In individual cases, prolongations of the QT interval are also seen. However, the actual effect of mizolastine on QT time and its influence on arrhythmias are still largely unclear according to current medical knowledge. P450 isozymes also participate in the metabolism of the drug mizolastine. For this reason, concomitant use of CYP3A4 inhibitors should be avoided. These include, for example, the substances erythromycin and ketoconazole. Basically, the drug mizolastine is characterized by its anti-allergic, antihistamine and anti-inflammatory properties. These result primarily from the antagonism that the drug forms at the H1 receptors for histamine.
Medicinal use and use for treatment and prevention.
The drug mizolastine is used for the treatment of various health complaints and diseases. Primarily, the drug is used for symptomatic therapy of hay fever, allergic conjunctivitis and rhinitis, and hives with chronic course. The dosage of the active ingredient is principally carried out according to the enclosed specialist information. Since the drug is characterized by a very long half-life, it is possible to take the drug once a day.
Risks and side effects
In the course of therapy with the drug mizolastine, specific undesirable side effects may occur.The most common symptoms are nausea, pain in the abdominal area and diarrhea. Weakness, dry mouth, headache and fatigue are also possible. In addition, some patients experience dizziness and increased appetite. Sometimes there is low blood pressure and an increased pulse. In rare cases, patients suffer from severe allergic reactions to the drug. In addition to the potential side effects, some contraindications should be considered before prescribing and taking the drug mizolastine. For example, it should not be taken if there is a known hypersensitivity to the active ingredient. Also, if azole antifungals are being taken, administration of the drug should be avoided. In addition, mizolastine is not suitable for patients with impaired liver function, certain heart diseases, and cardiac arrhythmias. Hypokalemia, bradycardia, a prolonged QT interval, and impaired electrolyte balance are also contraindications. In addition, care should be taken not to administer inhibitors of the CYP3A4 gene during therapy with mizolastine. This is because these usually cause an increase in the concentration of the active substance. It is at the patient’s discretion to report any side effects that occur to the physician.
