Ketotifen Sopharma, syrup 100 ml

Ketotifen has a pronounced antihistamine, weakly antiserotonin action, without anticholinergic effect. In higher doses it has a slightly depressing effect on the central nervous system.

Pharmacodynamics

The mechanism of action of Ketotifen is related to the ability to inhibit the release of histamine and other inflammatory mediators from mast cells due to membrane stabilization and also due to blockade of histamine H1 receptors. Ketotifen inhibits phosphodiesterase enzyme, as a result of which the level of cyclic adenosine monophosphate in mast cells increases.

The drug reduces or suppresses skin and bronchial reactions caused by the antigen, which leads to its use for prophylactic purposes. When used as monotherapy it does not stop asthma attacks, but leads to reduction of the number, duration and intensity of these attacks, and in some cases they completely disappear.

Limits eosinophilia, reduces the need and frequency of use of anti-asthmatic drugs: corticosteroids, bronchodilators, etc.

Pharmacokinetics

The drug is characterized by good and rapid resorption, without the danger of cumulation in the body. Bioavailability is approximately 50%, which is associated with metabolism during “first passage” through the liver. Time to reach maximum plasma concentration is 2-4 hours, and binding to plasma proteins is 75%. There are two phases of excretion, and most of the single dose is eliminated in the urine within 48 hours. Therapeutic effect occurs after 2 weeks of using the drug.

Indications

Active ingredient

How to take, the dosage

Overly, with meals.

Adults – 5 ml of syrup 2 times a day (morning and evening). For patients with significant sedative effects, a slow increase in dose over the first week is recommended, starting with 0.5 mg (2.5 ml of syrup) in the evening before bedtime until the therapeutic dose is gradually reached.

In children over 3 years of age, 5 ml of syrup 2 times a day (morning and evening); from 6 months to 3 years of age, 2.5 ml of syrup (0.5 mg) 2 times a day, morning and evening.

The duration of treatment. Treatment is prolonged; therapeutic effect is achieved after several weeks of therapy. Treatment should be carried out for at least 2-3 months, especially in patients who had no effect in the first weeks. Treatment with ketotifen should be discontinued gradually over a period of 2-4 weeks.

Interaction

The use of ketotifen by patients who have been systemically treated with corticosteroids requires a gradual reduction of prior corticosteroid therapy, since there is a risk of adrenal insufficiency.

The combination with oral antidiabetic agents sometimes leads to the development of thrombocytopenia.

The simultaneous use of Ketotifen and sedatives, hypnotics, antihistamines and alcohol may increase their effects.

Special Instructions

Patients taking ketotifen should refrain from potentially dangerous activities involving increased attention (e.g., driving). The drug may be used during lactation only if necessary, because it penetrates into the breast milk.

Contraindications

There are no absolute contraindications.

Do not take the drug in pregnancy, simultaneously with taking oral antidiabetic drugs, which may lead to thrombocytopenia; with sedatives and alcohol.

Hypersensitivity to the components of the drug.

Side effects

Drowsiness, dry mouth, mild dizziness, fatigue, slowed mental reactions may occur in the first few days, usually disappearing after a few days. A lower dose (5 ml per day) for the first week is recommended. Increased appetite and associated weight gain are less common.

Patients taking ketotifen should refrain from potentially hazardous activities involving increased attention (such as driving).

The drug may only be used during lactation if necessary because it passes into breast milk.

Overdose

Mild limb tremors, restlessness, and tachycardia may occur with increasing doses, but these may go away after decreasing the dose.

Pregnancy use

While no effects on pregnancy and peri- and postnatal development have been noted in animal experiments when Ketotifen is used in doses that are tolerated in animals, its safety in pregnancy in humans has not been established.

Therefore, Ketotifen should only be prescribed during pregnancy if absolutely necessary.

Ketotifen is also thought to be excreted with women’s breast milk, so mothers taking Ketotifen should not breastfeed.