Instruction for use: Ketotifen

Trade name of the drug – Ketotifen

International nonproprietary name: ketotifen

Dosage Form: pills
Composition:
Ingredients: 1 tablet contains:
Active ingredient: Ketotifen fumarate - 1.3 mg (equivalent to 1 mg ketotifen).

Excipients: 

potato starch, lactose (milk sugar), magnesium stearate.
Description:

Tablets white, odorless or with a faint odor, round.
Pharmacotherapeutic group:

antiallergic agent, mast cell stabilizer.

ATX Code R06AX17

Pharmacological Properties
Pharmacodynamics.

Mast cell stabilizer, has a moderate activity gistaminoblokiruyuschey-H1 to inhibit the release of histamine, leukotrienes from basophils and neutrophils, reduces the accumulation of eosinophils in the airway response to histamine and suppress early and late asthmatic responses to allergen. It prevents the development of bronchospasm, has no bronchodilatory effect. Inhibits phosphodiesterase, thereby increasing cAMP in adipose tissue cells.
The therapeutic effect is fully manifested in 1.5-2 months. from the start of therapy.

Pharmacokinetics.

Absorbability - virtually complete bioavailability - about 50% (because of the "first pass" effect in the liver). Time to maximum concentration (Tcmax) - 2-4 hours, the connection with plasma proteins - 75%. It passes through the blood-brain barrier. Penetrates into breast milk.It is metabolized in the liver. Excreted by the kidneys as metabolites (the main metabolite - ketotifen N-glucuronide pharmacologically inactive). Within 48 hours the kidneys displayed basic part of the dose (1% - unchanged, and 60-70% - as metabolites). Withdrawal - biphasic: half-life of the first phase - 3-5 h, the second - 21 hours.
Pharmacokinetics in children older than 3 years is not different from adults.

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

Contraindications
Hypersensitivity, pregnancy, lactation, children under 3 years.

Be wary - epilepsy, liver failure.

Dosing and Administration
Inside, during a meal, adults - 1 mg 2 times a day, morning and evening. If necessary, the dose was increased to 2 mg 2 times a day. Children from 3 years and over - 1 mg 2 times a day.
Duration of treatment - at least 3 months. Abolition of therapy is carried out gradually, within 2-4 weeks.

Side effects
From the nervous system: drowsiness, dizziness, slow reaction rate (disappear after a few days of therapy), sedation, fatigue; rare - anxiety, sleep disorders, anxiety (especially in children).
From the digestive system: dry mouth, increased appetite, nausea, vomiting, gastralgia, constipation.
From the urine: dysuria, cystitis.
Other: thrombocytopenia, weight gain, allergic skin reactions.

Overdose
Symptoms: drowsiness, confusion, disorientation, or bradi- tachycardia, decreased blood pressure, shortness of breath, cyanosis, convulsions, irritability, coma. Treatment: gastric lavage (if little time has passed since the reception), symptomatic treatment, the development of seizures - barbiturates or benzodiazepines. Dialysis is ineffective.

Interaction with other drugs

It enhances the effect of sleeping pills, antihistamines, ethanol.
In combination with hypoglycemic drugs increases the likelihood of developing thrombocytopenia.

Special instructions
In the period of treatment should refrain from driving motor vehicles and activities potentially hazardous activities that require high concentration and psychomotor speed reactions.
Bad abrupt withdrawal prior treatment of beta-agonists, corticosteroids, adrenocorticotropic hormone (ACTH) in patients with bronchial asthma and bronchospastic syndrome after joining ketotifen therapy, cancellation is carried out for at least 2 weeks, gradually reducing the dose. Treatment stopped gradually over 2-4 weeks (possible recurrence of asthma symptoms).Individuals sensitive to the sedative effect, in the first 2 weeks of the drug is prescribed in small doses.
Not intended for the relief of asthma attack.
Patients receiving both oral hypoglycemics, should control the number of platelets in peripheral blood.

Release Form
Tablets 1 mg, 10 tablets in blisters. 1, 2, 3, 4, 5, along the contour of cellular packages are placed in the instruction stack of the cardboard.
Storage conditions
List B. In dry the dark place at a temperature no higher than 25 ° C.
Keep out of the reach of children.
Shelf life
3 years. Do not use beyond the expiration date printed on the package.
Conditions of supply at the pharmacy
On prescription.