Description
Latin name
Acid acetyrlfrf48 flu
Release form
Capsules.
Packing
10 pcs
Pharmacological action
Tamiflu – an antiviral drug. Oseltamivir phosphate is a prodrug, its active metabolite (oseltamivir carboxylate) competitively and selectively inhibits influenza A and B neuraminidase, an enzyme that catalyzes the release of newly formed virus particles from infected cells, their penetration into the cells of the respiratory tract epithelium and the further spread of the virus in organism.
Oseltamivir carboxylate acts outside the cells. It inhibits the growth of the influenza virus in vitro and inhibits the replication of the virus and its pathogenicity in vivo, reduces the release of influenza A and B viruses from the body. Its concentrations necessary to suppress enzyme activity by 50% (IC50) are located at the lower boundary of the nanomolar range.
Indications
– Treatment of influenza caused by type A and B viruses in adults and children over 1 year old.
Typical flu symptoms occur suddenly and include fever, cough, headache, severe weakness, muscle pain, and sore throat.
– Prevention of influenza in adults and adolescents over the age of 12 years, those at high risk of infection with the virus (in military units and large production teams, in debilitated patients).
Contraindications
– Hypersensitivity to oseltamivir phosphate or any component of the drug.
– Chronic renal failure (persistent hemodialysis, chronic peritoneal dialysis, creatinine clearance <10 ml / min). Special instructions Seizures and delirium-like neuropsychiatric disorders have been reported in patients (mainly children and adolescents) who took Tamiflu ® for the treatment of influenza. These cases were rarely accompanied by life-threatening actions. The role of Tamiflu ® in the development of these phenomena is unknown. Similar neuropsychiatric disorders are also noted in patients with influenza who have not received Tamiflu ®. Careful monitoring of the behavior of patients, especially children and adolescents, is recommended. in order to identify signs of abnormal behavior. There is no data on the effectiveness of Tamiflu ® for any diseases caused by pathogens other than influenza A and B viruses. In the treatment and prevention of influenza in patients with creatinine clearance of 10 to 30 ml / min dose adjustment is required. Recommendations for dose adjustment in patients receiving hemodialysis or peritoneal dialysis, and in patients with creatinine clearance of 10 ml / min are absent. Do not administer Tamiflu ® to children under 1 year of age. Composition of Oseltamivir Excipients: pregelatinized starch, povidone K30, croscarmell sodium sodium. Dosage and administration of Tamiflu is taken orally, with food, or regardless of food intake. Taking Tamiflu with meals or with a small amount of milk reduces possible gastric discomfort. Treatment should be started on the first or second day of the onset of flu symptoms. Adults and children over 12 years of age are prescribed 75 mg 2 times a day by mouth for 5 days. Increasing the dose of more than 150 mg / day does not increase the effect. Children over 40 kg or over 8 years of age who can swallow capsules can also receive treatment by taking one 75 mg capsule 2 times a day, as an alternative to the recommended dose of Tamiflu suspension (see below). Children over 1 year of age are recommended a suspension for oral administration within 5 days: children weighing less than 15 kg are prescribed 30 mg 2 times a day children weighing 15-23 kg – 45 mg 2 times a day children weighing 23-40 kg – 60 mg 2 times a day children over 40 kg – 75 mg 2 times a day. Side effects Clinical trials for the treatment of adult influenza The most common adverse events in 2107 patients (including patients receiving Tamiflu ® 75 mg 2 times a day and 150 mg 2 times a day, placebo) in phase III studies were nausea and vomiting. They were transient in nature, arose, as a rule, after taking the first dose and in most cases did not require discontinuation of the drug. When taking the recommended dose (75 mg 2 times a day), nausea was the reason for dropping out of the study in three patients and vomiting in three patients. In phase III trials in adults, the incidence of certain adverse events with Tamiflu ® was higher than with placebo. prevention studies A total of 3434 volunteers (adolescents, adults without concomitant diseases and the elderly and senile) participated in phase III studies on influenza prevention, 1480 of which received the recommended dose of the drug (75 mg once daily) 6 weeks. Despite the long duration of taking the drug, the adverse event profile was very similar to that in treatment studies (Table 1). Patients taking Tamiflu ® for prophylaxis were slightly more likely than in the placebo group, and more often than in the therapy studies, pains of various localization, rhinorrhea, dyspepsia, and upper respiratory tract infections were noted. However, the differences in the frequency of these adverse events between the Tamiflu ® and placebo groups were less than 1%. The safety profile in 942 elderly and senile patients receiving Tamiflu ® and placebo did not clinically differ from that in younger patients. Treatment studies in children A total of 1,032 children aged 1 12 years (including 698 children without concomitant diseases aged 1 12 years and 334 patients with bronchial asthma aged 6 12 participated in phase III trials for the treatment of influenza) years). 515 patients received Tamiflu ® suspension. Vomiting was the most common adverse event. Other phenomena most commonly encountered in the Tamiflu ® group were abdominal pain, nosebleeds, hearing impairment, and conjunctivitis. These phenomena occurred suddenly, stopped independently, despite continued treatment, and in the vast majority of cases did not cause a cessation of treatment. Prevention studies in children Children aged 1-12 years (222 and 134 patients, respectively) took part in the study after contact with a sick family member or someone from a permanent environment. The most common adverse events were symptoms of the gastrointestinal tract, especially vomiting. Tamiflu ® was well tolerated in this study, the reported symptoms were consistent with those previously encountered (Table 2). Post-marketing observation The following categories are used to assess the frequency of undesirable effects: very often (? 1/10) often (? 1/100,% 26lt% 3B1 / 10) infrequently (? 1/1000,% 26lt% 3B1 / 100) rarely (? 1/10000,% 26lt% 3B1 / 1000) is very rare (% 26lt% 3B1 / 10000) and the frequency is not known (the frequency cannot be determined from the available data). From the skin and subcutaneous fat: rarely – hypersensitivity reactions: dermatitis, skin rash, eczema, urticaria, very rarely – exudative erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis rarely – anaphylactic and anaphylactoid reactions, Quincke’s edema. From the liver: very rarely – hepatitis, an increase in the activity of liver enzymes in patients with flu-like symptoms who received Tamiflu ®. From the side of the neuropsychic sphere: in patients (mainly in children and adolescents) who took Tamiflu ® for the treatment of influenza, convulsions and delirium were recorded (including symptoms such as impaired consciousness, disorientation in time and space, abnormal behavior, delirium, hallucinations, agitation, anxiety, nightmares). These cases were rarely accompanied by life-threatening actions. The role of Tamiflu ® in the development of these phenomena is unknown. Similar neuropsychiatric disorders are also noted in patients with influenza who have not received Tamiflu ®. From the gastrointestinal tract: cases of gastrointestinal bleeding have rarely been observed after taking Tamiflu ® (in particular, the relationship between hemorrhagic colitis and taking Tamiflu ® cannot be ruled out, since these phenomena disappeared both after the patient recovered from the flu and after withdrawal drug). From the side of the organ of vision: visual impairment (frequency not known). From the side of the heart: cardiac arrhythmia (frequency not known). Drug Interactions Information obtained in pharmacological and pharmacokinetic studies of oseltamivir phosphate suggests that clinically significant drug interactions are unlikely. Drug interactions due to competition for active esterase centers that convert oseltamivir phosphate to an active substance are not described in detail in the literature. The low degree of binding of oseltamivir and the active metabolite to proteins does not suggest that there are interactions associated with the displacement of drugs from communication with proteins. In vitro experiments have demonstrated that neither oseltamivir phosphate, neither the active metabolite is the preferred substrate for polyfunctional oxidases of the cytochrome P450 system or for glucuronyl transferases. There is no formal basis for interaction with hormonal oral contraceptives. Cimetidine, a non-specific inhibitor of isoenzymes of the cytochrome P450 system, competing in the process of tubular secretion with alkaline preparations with cationic properties, does not affect the concentration of oseltamivir and its active metabolite in plasma. Clinically significant drug interactions based on competition in the process of tubular renal secretion are unlikely, due to the peculiarities of elimination of the active metabolite (glomerular filtration and anionic tubular secretion) and the excretory ability of these two pathways, as well as the large safety margin of Tamiflu. The simultaneous administration of probenecid leads to an approximately 2-fold increase in the AUC of the active metabolite due to inhibition of active tubular secretion in the kidneys. However, dose adjustment with simultaneous use with probenecid is not required. Concomitant use of Tamiflu with paracetamol does not affect plasma concentrations of oseltamivir, its active metabolite, and paracetamol. In clinical trials of the III phase, Tamiflu was prescribed together with ACE inhibitors (enalapril, captopril), thiazide diuretics, penicillin, cephalosporins, azithromycin, erythromycin, doxycycline, histamine H2 receptor blockers (ranididinoline, cyanogen, bimidinolitin-bimetan, bimidinolithin-bimetan-bimetan-b-receptor, (theophylline), sympathomimetics (pseudoephedrine), codeine, GCS, inhaled bronchodilators, antipyretic analgesics and NSAIDs (acetylsalicylic acid, ibuprofen and paracetamol). No changes in the nature or frequency of adverse events were observed. Overdose There are currently no cases of overdose. Nausea and / or vomiting were observed when taking single doses of Tamiflu ® up to 1000 mg. Therefore, suspected symptoms of an acute overdose may be nausea and / or vomiting. Dizziness may also occur. Storage Conditions At a temperature not exceeding 30 ° C. Shelf life 5 years. Deystvuyushtee substance Oselytamivir Conditions of sale from pharmacies Prescription dosage form capsules Indications Indications Flu, Influenza Prevention F. Hoffmann-La Roche Rhttf55 Switzerland 19 Pharmstandard-Leksredstva, Switzerland
