Ketotifen - instructions for use, dose, side effects, contraindications

Stabilizer of mast cell membranes,has moderate H1-histaminoblocking activity, inhibits the release of histamine, leukotrienes from basophils and neutrophils, reduces the accumulation of eosinophils in the respiratory tract and response to histamine, suppresses early and late allergic reactions to the allergen. It prevents the development of bronchospasm, does not have bronchodilator effect. Inhibits phosphodiesterase, resulting in increased, the content of cyclic adenosine monophosphate (cAMP) in adipose tissue cells.

Therapeutic effect is fully manifested after 1.5-2 months from the beginning of therapy.

Pharmacokinetics:

Absorption is almost complete, bioavailability is about 50% (due to the presence of the "first pass" effect through the liver). Time to reach the maximum concentration (TC_mOh) - 2-4 h, the connection with plasma proteins - 75%. Passes through the blood-brain barrier. Penetrates into breast milk.

Metabolised in the liver. It is excreted by the kidneys in the form of metabolites (the main metabolite - ketotifen N-glucuronide is pharmacologically inactive). Within 48 hours the kidneys display the bulk of the dose (1% in unchanged form and 60-70% in the form of metabolites).The elimination is biphasic: the half-life of the first phase is 3-5 h, the second - 21h.

Pharmacokinetics in children older than 3 years does not differ from adults.

Indications:

Atopic bronchial asthma, pollinosis (hay fever), allergic rhinitis, allergic conjunctivitis, atopic dermatitis, urticaria.

Contraindications:

Hypersensitivity, pregnancy, lactation, children under 3 years.

Carefully:

Epilepsy, hepatic insufficiency.

Pregnancy and lactation:The use of the drug during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

Inside, with food.

Adults: 1 mg 2 times a day in the morning and in the evening. If necessary, increase the dose to 2 mg 2 times a day.

Children from 3 years and older: 1 mg 2 times a day.

The course of treatment is 8-12 weeks. If necessary, drug cancellation should be done gradually for 2-4 weeks.

Side effects:

From the nervous system: drowsiness, dizziness, slow reaction (disappear after a few days of therapy), sedation, fatigue; anxiety, sleep disorders, nervousness (especially in children).

From the digestive system: dryness of the oral mucosa, increased appetite, nausea, vomiting, gastralgia, constipation.

From the side of urination: dysuria, cystitis.

Other: thrombocytopenia, weight gain, allergic skin reactions.

Overdose:

Symptoms: drowsiness, confusion, disorientation, bradycardia or tachycardia, lowering of blood pressure, dyspnea, cyanosis, convulsions, increased excitability, coma.

Treatment: gastric lavage, symptomatic treatment, with the development of convulsive syndrome - short-acting barbiturates and benzodiazepines. Dialysis is ineffective.

Interaction:

Strengthens the effect of hypnotics, antihistamines, ethanol.

In combination with hypoglycemic drugs, the probability of thrombocytopenia increases.

Special instructions:

It is undesirable to abruptly abolish the previous treatment with beta-adrenostimulants, glucocorticosteroids, adrenocorticotropic hormones in patients with bronchial asthma and bronchospastic syndrome after adherence to ketotifen therapy, and cancel for at least 2 weeks, gradually reducing the dose.

Treatment is stopped gradually, within 2-4 weeks (a relapse of asthmatic symptoms is possible).

Persons sensitive to sedation, in the first 2 weeks, the drug is prescribed in small doses.

It is not intended for arresting an attack of bronchial asthma.

In patients concomitantly receiving oral hypoglycemic agents should monitor the number of platelets in the peripheral blood.

Effect on the ability to drive transp. cf. and fur:During the period of treatment it is necessary to refrain from driving motor vehicles and engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets 1 mg.

Packaging:

10 tablets per contour cell pack.

3 contour squares with instructions for use are placed in a pack of cardboard.

Storage conditions:

Store in a dry place protected from light.

Keep out of the reach of children.

Shelf life:

3 years.

Those should be used after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-005338/08

Date of registration:08.07.2008 / 09.08.2017

Expiration Date:Unlimited

The owner of the registration certificate:AVEKSIMA, JSC AVEKSIMA, JSC Russia

Manufacturer: & nbsp

IRBITSK HFZ, OJSC Russia

Representation: & nbspAVEKSIMA, JSC AVEKSIMA, JSC Russia

Information update date: & nbsp07.01.2018

Illustrated instructions

Instructions

Ketotifen (Ketotifen)