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

Excipients: sorbitol 1750 mg, methyl parahydroxybenzoate 5 mg, propyl parahydroxybenzoate 1 mg, citric acid monohydrate 9 mg, sodium hydrogen phosphate dodecahydrate 30 mg, ethanol 96% 100 mg, sodium saccharinate 1 mg, strawberry flavor (liquid essence "Strawberry") 15 mg, water purified to 5 ml.

Description:

Transparent viscous liquid from colorless to light yellow color with a specific smell of strawberry.

Pharmacotherapeutic group:Antiallergic agent - stabilizer of membranes of mast cells

ATX: & nbsp

S.01.G.X.08 Ketotifen

R.06.A.X.17 Ketotifen

Pharmacodynamics:

Ketotifen belongs to the group of cycloheptathiophenones and has a pronounced antihistamine effect. Does not apply to bronchodilator antiasthmatics. The mechanism of action is associated with inhibition of the release of histamine and other mediators from mast cells, the blocking of histamine H₁receptors and inhibition of the enzyme phosphodiesterase, resulting in an increased level of cAMP (cyclic adenosine monophosphate) in mast cells. Suppress effects PAF (thrombocyte-activating factor). It does not stop asthmatic attacks, but prevents their appearance and leads to a decrease in their duration and intensity, and in some cases they completely disappear. It facilitates sputum production.

Pharmacokinetics:

Almost completely absorbed from the gastrointestinal tract, bioavailability is about 50% due to the effect of "first passage" through the liver. The maximum level in blood plasma is reached between 2-4 hours. Binding to plasma proteins is about 75%.Passes through the blood-brain barrier, penetrates into breast milk. The volume of distribution is 2.7 l / kg.

About 60% of the dose is metabolized in the liver in three ways: demethylation, N-oxidation, N-glucuroconjugation, to the following metabolites: ketotifen - N-glucuronide (pharmacologically inactive), norketotifen (with pharmacological activity, similar ketotifen activity), N-Ketotifen oxide and 10-hydroxy-ketotifen (with unknown pharmacological activity).

Metabolism in children does not differ from that in adults, except for a faster clearance, so children over 3 years of age need a daily dose for adults.

It is excreted by the kidneys - about 70% in the form of inactive metabolites, 0.8% - in unchanged form. The elimination is biphasic: the half-life of the first phase is 3 to 5 hours, the second - about 21 hours.

Indications:

- Atopic bronchial asthma (as part of complex therapy);

- allergic rhinitis, conjunctivitis.

Contraindications:

- Hypersensitivity to the active substance or any of the excipients of the drug;

- I trimester of pregnancy, lactation period;

- Children's age up to 6 months;

- deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption.

Carefully:

Epilepsy, episodes of seizures in the anamnesis, hepatic insufficiency.

Pregnancy and lactation:

In the first trimester of pregnancy, the use of the drug is contraindicated. In the II and III trimesters of pregnancy ketotifen Use with caution and only if the intended benefit to the mother exceeds the potential risk to the fetus.

Ketotifen excreted in breast milk, so women should stop breastfeeding if necessary to use the drug during lactation.

Dosing and Administration:

Inside.

Adults: 5 ml (1 mg) 2 times a day, morning and evening, with meals.

For patients who have a significant sedative effect, a slow increase in dose is recommended during the first week, starting with 2.5 ml (0.5 mg) in the evening before bedtime, until the therapeutic dose is gradually reached. If necessary, the daily dose can be increased to 4 mg - 10 ml 2 times a day. At a higher dose, a more rapid onset of therapeutic effect can be expected.

Children from 3 to 18 years old: 5 ml (1 mg) 2 times a day, morning and evening, with meals.

Children from 6 months to 3 years: 2.5 ml (0.5 mg) 2 times a day, morning and evening. Apply on the advice of a doctor.

Application the elderly patients

There are no special requirements for elderly patients.

Duration of treatment

The treatment is long, the therapeutic effect is achieved after several weeks of therapy. Treatment should be performed for at least 2-3 months, especially in patients who have not had an effect in the first weeks.

Simultaneous application β2-adrenomimetics and ketotifen can reduce the frequency of bronchodilators.

Discontinuation of treatment

Stop treatment with Ketotifen Sopharma gradually, within 2-4 weeks, to avoid the risk of exacerbation of bronchial asthma.

Side effects:

The following side effects are classified by organs and systems and by frequency. Side effects are classified by frequency as follows: very often (≥ 1/10), frequent (≥ 1/100 and <1/10), infrequently (≥ 1/1 000 and <1/100), rarely (≥ 1/10 000 and <1/1 000), very rarely (<1/10 000), with an unknown frequency (based on existing data, it is impossible to make an estimate).

Infections: infrequently - cystitis.

Immune system disorders: very rarely - severe skin reactions, erythema multiforme exudative, Stevens-Johnson syndrome.

Disorders from the metabolism and nutrition: rarely - weight gain.

Mental disorders: often - arousal, irritability, insomnia, anxiety.

Disturbances from the nervous system: infrequently - dizziness, headache; rarely - sedation (relaxation, slowing down the reaction); very rarely - cramps.

Disorders from the gastrointestinal tract: infrequent - dry mouth, nausea, vomiting, diarrhea.

Hepatobiliary disorders: very rarely - increased activity of hepatic enzymes, hepatitis.

At the beginning of the treatment, dry mouth and dizziness may appear, but they usually pass spontaneously during the treatment. In rare cases, there are symptoms of central nervous system stimulation, such as irritation, irritability, insomnia and anxiety, especially in children, nervousness, fatigue, drowsiness.

Overdose:

Symptoms: drowsiness, confusion, nystagmus, dizziness, disorientation, brady- or tachycardia, arterial hypotension, nausea, vomiting, dyspnea, cyanosis, increased excitability, coma, children may have seizures.

Treatment: gastric lavage (if a little time has passed since the time of taking), symptomatic treatment, with the development of convulsive syndrome, the use of barbiturates or benzodiazepines, the reception of activated charcoal. If necessary, symptomatic treatment and monitoring of cardiac activity is recommended. Dialysis is ineffective.

Interaction:

With the simultaneous use of ketotifen and oral antidiabetics, there is a risk of developing reversible thrombocytopenia. Such patients are advised to monitor the number of platelets.

Ketotifen may enhance the effects of other drugs that suppress the central nervous system (sedatives, hypnotics).

Simultaneous use of ketotifen with other antihistamines may lead to mutual enhancement of their effects.

During treatment with ketotifen, alcohol should be avoided, since it increases the inhibitory effect of ketotifen on the central nervous system.

Special instructions:

The drug is not prescribed for relief of an attack of bronchial asthma.

At the beginning of the treatment with ketotifenum, you can not abruptly stop therapy with other anti-asthmatic drugs,especially systemic glucocorticosteroids. In patients with steroid dependence, adrenal insufficiency may develop.

In the case of intercurrent infection, specific anti-infective therapy should be carried out.

After joining the therapy of ketotifen, the abolition of the previous treatment is carried out for a minimum of 2 weeks, gradually reducing the dose.

Ketotifen lowers the threshold of convulsive activity, so it must be administered with extreme caution to patients with episodes of seizures in the anamnesis.

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

Ketotifen Sopharma syrup contains as auxiliary substances methyl- and propyl parahydroxybenzoates, which can cause allergic reactions (possibly delayed).

Ketotifen Sopharma syrup contains as an auxiliary substance sorbitol (a dose of 10 ml - up to 3.5 g of sorbitol). Patients with rare hereditary problems of fructose intolerance should not take this medication (gastric irritation and diarrhea are possible).

The drug contains 2.46% by volume ethanol (alcohol), which can harm patients suffering from alcoholism.This should also be taken into account when applying the drug to pregnant and breast-feeding women, children, as well as in patients with a high risk group (with liver disease or epilepsy).

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Syrup 1 mg / 5 ml.

Packaging:

For 100 ml of the drug in bottles of dark glass, ukuporennyh aluminum caps or caps made of polyethylene type "Pylfer-proof" or in bottles of dark polyethylene terephthalate, sealed with caps of polyethylene type "Pilfer-proof."

Each vial with a measuring spoon (5 ml) or a measuring cup (20 ml) and instructions for use are placed in a cardboard pack.

Storage conditions:

AT dry, protected from light at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Shelf life after the first opening of the bottle: 1 month.

Terms of leave from pharmacies:On prescription

Registration number:П N012663 / 02

Date of registration:17.03.2009 / 09.11.2016

Expiration Date:Unlimited

The owner of the registration certificate:Sopharma, AOSopharma, AO Bulgaria

Manufacturer: & nbsp

SOPHARMA, AD Bulgaria

Representation: & nbspSOFARMA SA SOFARMA SA Bulgaria

Information update date: & nbsp08.01.2018

Illustrated instructions

Instructions

Ketotifen Sopharma (Ketotifen Sopharma)