BIKARFEN 50 mg tablets

Transcription

1 TRANSLATION FROM LATVIAN SAM Summary of Product Characteristics 1. NAME OF THE MEDICINAL PRODUCT BIKARFEN 50 mg tablets 2. QUALITATIVE AND QUANTITATIVE COMPOSITION Active substance : sequifenadine hydrochloride (Sequifenadini hydrochloridum) 50 mg. Excipients: Each Bikarfen 50 mg tablet contains 302 mg of lactose. The list of excipients see in section PHARMACEUTICAL FORM Tablets. Description: white or almost white round, flat tablets with bevelled edge and breaking line on one side of a tablet. 4. CLINICAL PARTICULARS 4.1. Therapeutic indications Acute and chronic allergic diseases: pollinosis, allergic rhinitis, rinosinusopathy; medicines, foodstuffs, chemicals, dust, animal hair, insect bites, air pollution or other allergen-induced allergy. Allergic origin itchy skin and other diseases with itching (allergic and atopic dermatitis, vasculitis, neurodermatitis, red flat lichen, etc.). Allergy prevention (before seasonal exacerbations) and supportive therapy. 4.2 Posology and method of administration Bikarfen 50 mg tablets is taken orally right after meals drinking water. Adults: Acute and chronic allergic diseases: single dose is mg 2-3 times a day. Usually the therapeutic effect is observed after 3 days from the start of treatment with Bikarfen. Treatment course lasts 5-15 days, if necessary the course of treatment may be repeated. Prophylaxis and supportive therapy: 50 mg twice a day. For prophylaxis the preparation should be taken 2 weeks before the expected allergic reaction. Bikarfen 50 mg tablets may be used alone or in combination with preparations of local administration (nasal drops, eye drops and ointments) Contraindications Hypersensitivity to active substance or any excipients of the preparation. Pregnancy or breast-feeding.

2 lpp. 2. no 6 MAO inhibitors administration Special warnings and special precautions for use Patients with impaired renal function (treatment begins with the lowest level), severe cardiovascular, gastrointestinal or liver diseases should use the medicine with caution. Bikarfen tablets contains 302 mg of lactose. This medicine should not be used in patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption. There are no clinical studies on the preparation of children and the elderly Interaction with other medicinal products and other forms of interaction Antihistamines including sequifenadine are contraindicated in patients taking monoamine oxidase (MAO) inhibitors. Sequifenadine does not increase the hypnotic effect of alcohol and soporifics effects on the central nervous system (CNS), however, during the treatment it is not advisable to drink alcohol Pregnancy and lactation Use is contraindicated. During studies on animals that received very high doses of sequifenadine the embryotoxicity was observed. The potential risk for humans is unknown. Antihistamines should not be taken during breast-feeding because of the potential adverse effects on the infant's CNS Effects on ability to drive and use machines It is necessary to determine in advance whether the medicine causes sedation or sleep effects in the professionals whose work requires quick mental or physical reactions (e.g., drivers). It is not advisable to drive for the people who feel it Undesirable effects Classification of frequency of side effects is given in the table below.

3 lpp. 3. no 6 Very common Common Uncommon Very rare > 1/10 > 1/100, < 1/10 > 1/1 000, > 1/10 000, < 1/ < 1/100 < 1/1 000 MedDRA classification of organs system Blood and lymphatic systen disorders Nervous system disorders Frequency Common Adverse effects Decreased eosinophil leucocytes quantity in blood Sleepiness (average % of patients) is a dosedependent. If the dose is 150 mg per day, drowsiness is found in 1.97% of patients when the dose increased to 400 mg per day in 24.6% of patients. In most cases, drowsiness disappears after 2-5 days of treatment. Bikarfen can improve sleep of patients suffering from insomnia due to itching. Gastro-intestinal disorders tract Uncommon Common Uncommon Headache Agitation, insomnia, which often can be associated with high doses. Mouth dryness Weak epigastria s pain, dyspeptic phenomena, in particular, dosing on an empty stomach. This will increase the likelihood of adverse events in patients with chronic gastrointestinal diseases. Adverse reactions disappear during the first days of treatment and there is no need to stop the use or significantly reduce the dose. Renal and urinary disorders Reproductive system and breast disorders Very rare Increased appetite Light diuretic effect Menstrual disorders 4.9. Overdose The cases of overdose are not known. Symptoms: Adverse reactions may increase: dry mouth, headache, vomiting, epigastrial pain and other dyspeptic phenomena, Treatment: In case of overdose symptomatic treatment should be performed. No specific antidote is available.

4 lpp. 4. no 6 5. PHARMACOLOGICAL PROPERTIES Pharmacotherapeutic group: other antihistamines for systemic use (quinuclidyl carbinol derivative). ATC code: R06AX Pharmacodynamic properties Sequifenadine hydrochloride (hereinafter in the text sequifenadine) is a H 1 -receptor antagonist, it also moderately inhibits HT 1 receptors of serotonin, thus decreasing the activity of allergy mediators histamine and serotonin. Histamine causes clinical manifestations of allergic inflammation: oedema (capillary permeability increases), skin hyperemia (vessels widening), skin itching and ache. Bicarphen is not only H 1 -receptor antagonist, but it activates enzyme diaminoxidase that splits endogenous histamine due to this decreasing quantity of histamine in tissues. In case of allergic diseases, the level of serotonin is increased in blood. Serotonin has an effect on the specific serotoninergic receptors, increases blood pressure, causes bronchospasm, increases vascular permeability and forms edema many times more active than histamine. Furthermore, serotonin enhances histamine, bradykinin and other allergic mediators toxic activity and causes rhinitis. Sequifenadine prevents or decreases the histamine and serotonin intoxication, bronchoconstrictive activity of histamine and spasmogenic effect of histamine on smooth musculature of bronchus, intestines, vessels; disturbances of vascular permeability and oedema development. Sequifenadine has pronounced prolonged antipruritic and antiexudative qualities. Sequifenadine has an effect on immunologic reactivity of the organism, decreasing the quantity of cells forming antibodies and rosette forming cells in spleen, marrow, glands, and also it decreases elevated concentration of A and G classes immunoglobulin. Insignificant quantity of sequifenadine crosses blood-brain barrier. It does not have pronounced CNS inhibiting effect, though there could be observed a moderate sedative effect in separate cases of individual increased sensitivity.

5 lpp. 5. no 6 Sequifenadine does not change blood and urine biochemical characteristics, does not have an effect on blood pressure, ECG characteristics, sugar and cholesterol concentration in blood and characteristics of electroencephalogram Pharmacokinetic properties Absorption. Sequifenadine is rapidly absorbed in gastrointestinal tract. Maximal active substance blood plasma concentration is achieved during 1-2 hours. Sequifenadine is accumulated mainly in the lungs, liver; the lowest concentration of the drug is in the brains. It is metabolized by oxidation forming pharmacologically inactive metabolite, which is 2 times less toxic and pharmacologically inactive compared to sequifenadine Elimination. After administration of single 50 mg dose the elimination half-life of the active substance from blood plasma is 12 hours, and after administration of repeated doses the elimination half-life is decreased till 5.8 hours, i.e. the preparation is not accumulated in the body. 50 % of the dose is excreted in the bile, over 20 % -in the urine. Approximately 30 % of the dose is excreted unchanged, but % - in the form of metabolites Preclinical safety data Acute toxicity. When administered orally, the LD50 in mice is mg / kg, in rats - from 1480 to 1500 mg / kg, guinea pigs mg / kg. Intoxication is manifested by tonicclonic seizures, respiratory impairment. Chronic toxicity. Studies in laboratory animals (rats, guinea pigs, rabbits, dogs), which from 8 weeks to 6 months were administered orally 10, 25 and 50 mg / kg of sequifenadine doses, dystrophy processes in the liver and kidneys were observed in 50 mg/kg group. Carcinogenicity. Data on the sequifenadine carcinogenicity are not available. Mutagenecity. Mutagenic potential of sequifenadine was not found. Embryotoxicity. In a study with rats that received 100 and 630 times higher doses than the recommended therapeutic dose in humans, the high dose group showed embryotoxicity (embriogenesis abnormalities and embryonic death). Clinical data on sequifenadine use in pregnant women are not available. The results obtained with animals have shown that sequifenadine should not be used during pregnancy.

6 lpp. 6. no 6 6. PHARMACEUTICAL PARTICULARS 6.1. List of excipients Lactoze (302 mg), microcrystalline cellulose, pregelatinized maize starch, magnesium stearate and colloidal silicon dioxide Incompatibilities Not known Shelf life 4 years Special precautions for storage Store at below 25 C. Protect from light and moisture 6.5. Nature and contents of container 10 tablets in the blister from white PVC film and lacquered aluminium foil; two blisters (20 tablets) with patient s leaflet in a carton pack Special precautions for disposal and other handling Not applicable. 7. MARKETING AUTHORISATION HOLDER JSC Olainfarm. Address: 5, Rupnicu St., Olaine, LV-2114, Latvia. 8. MARKETING AUTHORISATION NUMBER DATE OF FIRST AUTHORISATION / DATE OF REVISION OF THE TEXT Translation from Latvian according to the original document Translation is carried out by Larisa Želnina Regulatory Affairs Senior specialist Date: