Ketotifen eye drops 0.25mg/ml, 2p x 5ml — Made in Ukraine — Free Delivery

Brand: Pharmex Group
Product Code: Ketotifen
Availability: In Stock

$19.57

Description

Pharmacological properties

Antiallergic, membrane stabilizing, antihistamine agent. inhibits the release of histamine, leukotrienes, lymphokines and other biologically active substances from mast cells and basophils. noncompetitively blocks h1-histamine receptors, inhibits phosphodiesterase, increases the level of camp in cells. reduces sensitization of eosinophils by recombinant human cytokines and their accumulation in target organs. when administered orally, the preparation is absorbed almost completely, its bioavailability is about 50% due to the effect of primary passage through the liver.

Ketotifen is excreted from the body in two phases, and the half-life of the short phase is 3-5 hours, and the long one is 21 hours. The main part of the dose taken is excreted in the urine within 48 hours in the form of metabolites (60-70%).

Indications

Prevention and treatment of acute, subacute and chronic allergic conjunctivitis and keratoconjunctivitis, seasonal (spring) conjunctivitis, eye manifestations of hay fever. in the form of tablets are used to prevent the development of bronchospasm, asthmatic attacks and acute allergic reactions, to reduce the dose and / or cancel hormonal preparations (glucocorticosteroids) and bronchodilators when used in combination.

Application

The preparation in the form of drops for adults and children over the age of 12 is prescribed 1 drop in the conjunctival sac of each eye 2 times a day. prophylactic administration for subacute and chronic processes should be started 3 weeks before contact with the allergen. the treatment is continued during the entire period of exposure to allergens. the duration of the use of eye drops depends on the type and severity of the disease. the bottle should be carefully closed after each use.

In the form of tablets, it is prescribed for adults by mouth 1 tablet 2 times a day - in the morning and in the evening with meals. If necessary, the daily dose is increased to 4 mg, divided into 2 doses. For children over 3 years old, the preparation is prescribed 1 mg 2 times a day.

Contraindications

Hypersensitivity to ketotifen and other components of the preparation, during pregnancy and lactation; children under 3 years of age.

Side effects

A burning sensation and tingling sensation in the eyes, blurred vision immediately after instillation. irritation of the mucous membrane of the eye, skin rash around the eyes; hypersensitivity. when taking the preparation inside, drowsiness, dry mouth, dizziness, slowing down of mental reactions, which usually disappear after several days of administration, are possible. occasionally, an increase in body weight is noted due to an increase in appetite.

special instructions

In acute inflammation and during an exacerbation of a chronic process, it is possible to use the preparation in combination with corticosteroids. the patient should be warned about the need for regular use of the preparation. treatment begins before contact with the allergen and continues for the entire period of action of the allergen.

The preparation should not be used concurrently with antidiabetic agents.

When using eye drops, do not use soft contact lenses due to the presence of benzalkonium chloride in the composition. Rigid contact lenses should be removed from the eyes immediately before instilling drops and inserted no earlier than 15 minutes after using the preparation.

Use of the preparation during lactation. Recommended only as directed by a physician.

Influence on the ability to drive vehicles and control mechanisms. When using tablets, patients should refrain from performing potentially hazardous activities that require increased attention. For some time after instilling drops in the eyes, you should refrain from doing work that requires increased attention.

Interactions

With the simultaneous use of ketotifen and antihistamines, a potentiation effect is possible. simultaneous administration with oral antidiabetic preparations increases the possibility of thrombocytopenia.

Overdose

Cases of overdose in the form of drops have not been established. when taken in pill form, confusion and disorientation, tachycardia and decreased blood pressure, convulsions and increased excitability (especially in children), drowsiness and severe sedation, coma are possible. treatment: gastric lavage, monitoring of indicators of the cardiovascular system. in the case of psychomotor agitation and the development of convulsive syndrome, barbiturates with a short period of action and benzodiazepines are prescribed.

Storage conditions

In the dark place at a temperature of 15-25 ° C.

Actual information

Ketotifen as the first successful (from a preventive point of view) anti-asthma preparation was described in 1965. The scientific world learned about this new progress in the treatment of bronchial asthma, followed by research and publications in this direction. the preparation is recognized as effective for the treatment of not only bronchial asthma, but also allergic rhinitis and conjunctivitis.

Physical properties

Fine crystalline powder from white to brownish-yellow color. Let's dissolve in water; very slightly soluble in acetonitrile (acetic acid nitrile); slightly soluble in methyl alcohol.

Pharmacokinetics

Ketotifen is almost completely absorbed from the gastrointestinal tract after oral administration, but bioavailability is only about 50% due to first-pass hepatic metabolism. The maximum concentration in blood plasma after oral administration is achieved after 2–4 hours. As a rule, the preparation is excreted in the urine in the form of inactive metabolites and a small amount of the preparation unchanged; T 1/2 - about 21 hours

Application

According to the ATC classification, it belongs to the group "Antihistamines for systemic use". Ketotifen is a sedative antihistamine that also has a stabilizing effect on mast cells. It is used in the treatment of allergic conditions, including allergic rhinitis and conjunctivitis. Ketotifen is also used in the prevention of bronchial asthma, which can take several weeks to show its full therapeutic effect. It is not used for the treatment of acute attacks of bronchial asthma. It is also used in the form of eye drops.

The results of studies on the effectiveness of ketotifen in the treatment of asthma have been conflicting. Although it was found to be effective in reducing symptoms by some researchers, it also decreased the use of other anti-asthma preparations during its use, however, some studies have shown no significant benefit. In the UK asthma guidelines, ketotifen is considered ineffective. Some systematic reviews found that prescribing the preparation was effective in controlling asthma and shortness of breath in children with mild to moderate illness, but noted that the high prevalence of atopy in some studies meant that the results could not be generalized to children with bronchial asthma in general. Studies carried out with the participation of children have shown that long-term therapy with ketotifen reduces the risk of bronchial asthma.

Experimental data

The experimental data obtained provide a rationale for the use of ketotifen as a prophylactic preparation for asthma (inhibition of the release of mediators of anaphylaxis, especially SRS-A, prevention of bronchospasm caused by SRS-A in vivo, the effect of a calcium antagonist). The relevant reviews briefly discussed and reviewed the results of experimental and therapeutic studies conducted over 6 years in several countries on several thousand patients. Some important features of oral prophylaxis of asthma with ketotifen have been highlighted, namely the effect of ketotifen on the characteristic hyperreactivity of bronchial asthma, the types of asthma that respond best to treatment with ketotifen; the effect of ketotifen in reducing the concomitant use of corticosteroids and bronchodilators, comparison of ketotifen with specific antihistamines, as well as side effects and safety of the preparation with long-term use (Craps L., 1981).

Allergic conjunctivitis is an IgE-mediated inflammation of the conjunctiva. Although histamine is the main mediator in this condition, the use of topical antihistamines often provides only temporary relief. Therapies targeting the inflammatory cascades of the disease are necessary, especially in cases of prolonged and severe allergic conjunctivitis. Ketotifen has been reviewed for the treatment of allergic conjunctivitis in terms of its mechanism of action and clinical efficacy. Thus, eye drops have been recommended for the treatment of this type of disease.

As a second generation antihistamine, Ketotifen has shown anti-inflammatory properties such as inhibiting the release of histamine from mast cells, as well as interfering with the production of cytokines and adhesion molecules from umbilical cord blood and conjunctival mast cells. Several immunomodulation options are currently available for the treatment of allergic conjunctivitis. These therapeutic possibilities provide the best therapeutic result for patients with allergic conjunctivitis, especially those who are in serious condition (Pacharn R., 2013).

The therapeutic efficacy of ketotifen for prophylaxis in children and adolescents with bronchial asthma was also considered. Conclusions are drawn based on the results of 4 double-blind, placebo-controlled studies with 194 patients, 2 double-blind controlled studies with clemastine with 86 patients and 5 double-trials. Long-term use of oral ketotifen made it possible to reduce the intake of corticosteroids and bronchodilators while improving clinical symptoms and maintaining respiratory function. Optimal results were obtained after 8–12 weeks of therapy. Comparative studies with clemastine, a specific H1-blocking agent, have shown that the antihistaminic properties of ketotifen have no prophylactic effect in bronchial asthma. In addition, it has been found that for optimal results, a double dose in milligrams per kilogram of body weight, calculated based on the recommended dose for adults, or that the adult dose can be used in children, would be required. These clinical observations are consistent with the results of pharmacokinetics in children, which indicates a faster metabolism without changing the nature of biotransformation. Comparative studies between ketotifen and disodium chromoglycate have shown comparable efficacy, although this does not mean that the response pattern was the same for the two preparations. Long-term treatment with oral ketotifen was as well tolerated in children as in adults. The main adverse effect was sedation, which occurs in 6% of children at the beginning of treatment, which disappeared after several days of using the preparation (Craps L., 1983).

The efficacy and safety of Ketotifen in the treatment of recurrent bronchitis was studied in 20 Thai children, whose mean age was 5.3 years. The symptoms studied were cough, increased secretion, and dyspnea, and each symptom was assigned a rating score (maximum score of 4). The frequency, severity and duration of the disease were taken into account, and points were assigned for the dose of symptomatic preparations used. Symptoms during the use of symptomatic preparations were recorded throughout the year before ketotifen therapy and throughout the following year. Efficacy was assessed by comparing symptoms (assessed per month) and preparation effects over the study period with the average of these indicators over the previous year. Thirteen children received ketotifen throughout the year, while seven children who showed virtually no symptoms after 4 months of ketotifen treatment were observed only for 8 months. At the end of the study period for ketotifen therapy, treatment was rated very good and good in 85% of children, satisfactory in 10% and poor in 5%. Drowsiness was the only side effect reported in several cases, but only during the initial phase of therapy. There were no abnormalities in laboratory values (Suwanjutha S., 1985).

17 children with neurodermatitis aged from 2 to 14 years received Ketotifen at a dose of 1 mg 2 times a day. 7 children underwent polyvalent therapy. Ketotifen therapy produced marked relief from itching in only two weeks; patients were completely free from itching on average after 20 days. Improvements in the skin were recorded after 2 months of treatment. The patients completely recovered from skin diseases after 7-9 months. In three patients, the deterioration of the skin was caused by an infection. With regard to long-term therapy with ketotifen, no serious side effects were observed (Kikindjanin V., 1990).

In a double-blind study, half of 56 adult patients with atopic dermatitis were treated systemically for 3 months with 1 mg ketotifen capsules twice daily, while the other half received placebo. The health status of patients in the ketotifen group improved significantly during treatment according to all clinical evaluations. The overall treatment efficacy was significantly higher in the ketotifen group. No serious side effects were observed (Falk E.S., 1993).

Adverse Effects

They relate to the entire class of antihistamines: drowsiness, dry mouth and dizziness may occur at the beginning of treatment, but usually these symptoms disappear with further use of the preparation. Information has been reported regarding weight gain, as well as isolated cases of severe skin reactions, cystitis and hepatitis. Irritation, pain, and punctate keratitis are commonly observed after eye instillation. For the full therapeutic effect of Ketotifen to manifest, it is necessary to carry out therapy for several weeks. And in the case of anti-asthma treatment, it should not be abruptly canceled after starting ketotifen therapy. This preparation should not be used to treat acute attacks of asthma.

Children

Ketotifen can be prescribed to children to treat allergic conditions such as rhinitis or conjunctivitis, and is used to prevent bronchial asthma. Oral doses equivalent to 1 mg of ketotifen 2 times daily with meals can be used from 3 years of age. A dose equivalent to 500 mcg of ketotifen twice daily has been suggested for children aged 6 months to 3 years. Ketotifen is also used in the form of eye drops 2 times a day.

Overdose

An overdose of Ketotifen while taking a dose of 10–120 mg was reported in 8 patients. Symptoms included drowsiness, confusion, shortness of breath, and disorientation. The most serious manifestations were loss of consciousness, seizures, bradycardia and tachycardia, as well as a severe hypotensive reaction. In such cases, the stomach should be flushed. Further, symptomatic supportive therapy is prescribed.

Interactions

A reversible decrease in platelet counts has been observed in several patients who received ketotifen in combination with oral antidiabetic preparations, and therefore it was suggested to avoid this combination.

Dosage regimen

Adults: 1 tablet 2 times a day (morning and evening), if necessary, the daily dose of the preparation can be increased to 4 mg (this is the maximum daily dose).

Children: 1 tablet 2 times a day; at the age of 6 months - 3 years, 500 mcg 2 times a day.

Ketotifen is also used topically, as eye drops equivalent to 0.025% ketotifen, prescribed twice a day.

The therapeutic effect develops slowly. The preparation therapy is carried out within 2-3 months. Finish taking the preparation should be gradual, within 2-4 weeks.

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