Instructions for use Ketotifen Sopharma tablets 1 mg blister No. 30
Composition
active ingredient: ketotifen hydrofumarate;
1 tablet contains 1.38 mg of ketotifen hydrofumarate, which is equivalent to 1 mg of ketotifen;
excipients: calcium hydrogen phosphate anhydrous, microcrystalline cellulose, wheat starch, magnesium stearate.
Dosage form
Pills.
Main physicochemical properties: round flat tablets with a bevel, with a dividing line on one side, 7 mm in diameter, from white to white with a gray tint; odorless.
Pharmacotherapeutic group
Antihistamines for systemic use. ATX code R06A X17.
Pharmacological properties
Pharmacodynamics
Ketotifen belongs to the group of cycloheptothiophenones and has a pronounced antihistamine effect. It belongs to the group of non-bronchodilating anti-asthmatic drugs. The mechanism of its action is associated with the inhibition of the release of histamine and other mediators from mast cells, with the blocking of histamine H1 receptors and the inhibition of the enzyme phosphodiesterase, as a result of which the level of cAMP in mast cells increases. Inhibits the effects of PAF (platelet-activating factor). When used alone, it does not stop attacks of bronchial asthma, but prevents their occurrence and leads to a reduction in their duration and intensity, while in some cases they disappear completely. Has a beneficial effect on sputum discharge.
Pharmacokinetics
Absorption: characterized by almost complete absorption from the gastrointestinal tract. Maximum plasma levels are reached after 2-4 hours. Steady state is achieved after taking the minimum daily dose, which is 2 mg.
Distribution: approximately 75% bound to plasma proteins. Volume of distribution is 2.7 l/kg.
Metabolism: About 60% of the administered dose is metabolized in the liver by three pathways: demethylation, N-oxidation, N-glucuronide to the following metabolites: ketotifen-N-glucuronide (pharmacologically inactive), nor-ketotifen (with pharmacological activity similar to that of unchanged ketotifen), ketotifen N-oxide and 10-hydroxy-ketotifen (with unknown pharmacological activity).
Metabolism in children is no different from that in adults, except for faster clearance.
Elimination: Excreted biphasically, with a short half-life of 3 to 5 hours and a longer half-life of 21 hours. About 1% of the substance is excreted unchanged in the urine within 48 hours, and 60-70% in the form of metabolites.
Indication
Prophylactic treatment of bronchial asthma, especially atopic. In the symptomatic treatment of allergic conditions, including allergic rhinitis and conjunctivitis.
Contraindication
Hypersensitivity to the active substance or to any of the excipients of the drug.
Avoid concomitant use of ketotifen and oral antidiabetic agents (risk of reversible thrombocytopenia) until this phenomenon is sufficiently studied.
Interaction with other medicinal products and other types of interactions
There is a risk of reversible thrombocytopenia when ketotifen is used concomitantly with oral antidiabetic agents. In such patients, monitoring of platelet counts is recommended.
The simultaneous use of atropine, agents with atropine-like action and ketotifen increases the risk of adverse reactions such as urinary retention, constipation, and dry mouth.
Ketotifen may potentiate the effects of other drugs that depress the central nervous system (sedatives, hypnotics).
Concomitant use of ketotifen with other antihistamines may lead to mutual potentiation of their effects.
During treatment with ketotifen, alcohol consumption should be avoided, as ethanol enhances the depressant effect of ketotifen on the central nervous system.
Application features
The drug is ineffective in the treatment of acute allergic reactions and is not used to relieve asthma attacks (asthma attacks).
The maximum therapeutic effect of the drug occurs after several weeks of systematic use.
Normalization of the function of the pituitary-adrenal system may take up to one year, therefore, in the first weeks of ketotifen use, it is recommended to continue the previous treatment and then cancel it gradually and for a long time.
At the beginning of long-term treatment with ketotifen, treatment with other anti-asthmatic drugs, especially corticosteroids, should not be abruptly discontinued. In patients with steroid dependence, the development of adrenocortical insufficiency may occur.
In case of intercurrent infection, specific anti-infective therapy is necessary.
In very rare cases, convulsions have been reported during treatment with ketotifen. Since ketotifen lowers the seizure threshold, it should be used with extreme caution in patients with a history of seizures. During treatment with the drug, it is necessary to be under the supervision of a doctor, taking into account the possibility of seizures.
Alcohol should not be consumed during treatment with ketotifen, as it enhances the depressive effect of ketotifen on the central nervous system.
The drug should be discontinued 10-14 days before skin tests to determine allergies.
If treatment with ketotifen needs to be discontinued, the dose should be gradually reduced over 2-4 weeks to prevent the recurrence of asthma symptoms.
Caution should be exercised when administering ketotifen to patients with impaired liver function.
Given that concomitant use with oral hypoglycemic agents may cause thrombocytopenia, this combination should be avoided or platelet levels should be closely monitored if such treatment is recommended.
The wheat starch in the tablet may contain only traces of gluten and is considered safe for patients with celiac disease.
Ability to influence reaction speed when driving vehicles or other mechanisms
At the beginning of treatment, Ketotifen Sopharma may slow down the speed of reactions, which requires the patient to be especially careful when driving vehicles and working with automated mechanisms.
Use during pregnancy or breastfeeding
In animal studies, no embryotoxic and teratogenic effects of ketotifen were detected. Controlled clinical studies in pregnant women have not been conducted. During pregnancy, ketotifen is contraindicated for use in the I trimester of pregnancy. In the II and III trimesters of pregnancy, it should be prescribed only after a strict assessment of the presence of direct indications, in cases where the expected benefit of treatment outweighs the potential risk to the fetus.
Ketotifen passes into breast milk, so women should stop breastfeeding if the drug is necessary.
Method of administration and doses
Take the tablets orally during meals, with water.
Dosage
Adults: 1 tablet (1 mg) 2 times a day, morning and evening with meals. For patients who experience significant sedation, a slow dose increase is recommended during the first week, starting with 0.5 mg 2 times a day, and gradually increasing it until the therapeutic dose is reached. If necessary, the daily dose can be increased to 4 mg (4 tablets) of 2 tablets 2 times a day. When using a higher dose, a faster onset of therapeutic effect can be expected.
Children:
Children from 6 months to 3 years of age: use ketotifen in a different dosage form (syrup).
Children over 3 years of age: 1 tablet (1 mg) 2 times a day, morning and evening, during meals.
Duration of treatment
The treatment is long-term, with the therapeutic effect being achieved after several weeks of therapy. Treatment should last at least 2-3 months, especially in patients who have not experienced improvement in their well-being in the first weeks.
Concomitant bronchodilator therapy: Concomitant use of ketotifen with bronchodilators may reduce the frequency of bronchodilator use.
Discontinuation of therapy
Ketotifen treatment should be discontinued gradually, over 2-4 weeks, to avoid the risk of recurrence of asthmatic symptoms.
Elderly patients.
There are no special requirements for elderly patients.
Children
Use for children aged 3 years and over.
Clinical observations support the pharmacokinetic properties and indicate that children may require a higher mg/kg dose than adults to achieve optimal results. Higher doses are as well tolerated as lower doses.
Overdose
Symptoms: significant impairment of psychomotor reactions, drowsiness to severe sedation, confusion, headache, disorientation, tachycardia, decreased blood pressure, in children - hyperexcitability or convulsions, reversible coma. Bradycardia, arrhythmia, depression of the respiratory center, nystagmus are also observed.
In case of the above symptoms, the patient should be carefully examined.
Treatment: general measures to remove unabsorbed drug from the digestive tract: induce vomiting, wash the stomach. The use of activated charcoal may have a beneficial effect. If necessary, symptomatic treatment and monitoring of the cardiovascular and respiratory systems are recommended. In cases of agitation, short-acting barbiturates or benzodiazepines can be used.
Adverse reactions
The following adverse reactions are classified by system organ class and frequency. Adverse reactions are classified by frequency as follows: very common (≥ 1/10), common (≥ 1/100 and <1/10), uncommon (≥ 1/1,000 and <1/100), rare (≥ 1/10,000 and <1/1,000), very rare (<1/10,000), not known (frequency cannot be estimated from the available data).
Infections and infestations:
infrequently - cystitis.
On the part of the immune system:
very rarely - severe skin reactions, erythema multiforme, Stevens-Johnson syndrome; with an unknown frequency - skin rashes.
From the side of metabolism and nutrition:
rarely - weight gain due to increased appetite.
Mental disorders:
often - psychomotor agitation, irritability, insomnia, restlessness, nervousness; with an unknown frequency - disorientation, drowsiness.
From the nervous system:
From the gastrointestinal tract:
infrequently - dry mouth; with unknown frequency - stomach pain, constipation, nausea, vomiting, dyspeptic disorders.
From the hepatobiliary system:
very rarely - increased liver enzymes, hepatitis.
From the kidneys and urinary tract:
with an unknown frequency - dysuria.
Dry mouth and dizziness may occur at the beginning of treatment, but they usually resolve spontaneously during treatment. Symptoms of CNS stimulation such as agitation, irritability, insomnia and anxiety are rare, especially in children.
Expiration date
3 years.
Storage conditions
Keep out of reach of children.
Store in the original packaging at a temperature not exceeding 25 °C.
Packaging
10 tablets in a PVC film/aluminum foil blister, 3 blisters in a cardboard pack.
Vacation category
According to the recipe.
Producer
JSC "Sopharma".
Location of the manufacturer and its business address
16 Ilienskoe Shose St., Sofia, 1220, Bulgaria.
