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Composition:


active ingredient: oseltamivir;


1 capsule solid contains oseltamivir phosphate equivalent to oseltamivir 30 mg;


excipients: pre-chelated starch, talc, povidone, sodium croscarmellose, sodium stearyl fumarate, solid gelatin capsule No. 4;


capsule composition: Iron Oxide Red (E 172), iron oxide yellow (E 172), titanium dioxide (E 171), gelatin, purified water;


1 capsule solid contains oseltamivir phosphate equivalent to oseltamivir 45 mg;


excipients: pre-chelated starch, talc, povidone, sodium croscarmellose, sodium stearyl fumarate, solid gelatin capsule No. 4;


capsule composition: black iron oxide (E 172), titanium dioxide (E 171), gelatin, purified water;


1 capsule solid contains oseltamivir phosphate equivalent to oseltamivir 75 mg;


excipients: pre-chelated starch, talc, povidone, sodium croscarmellose, sodium stearyl fumarate, solid gelatin capsule No. 2;


capsule composition: Iron Oxide Red (E 172), iron oxide yellow (E 172), iron oxide Black (E 172), titanium dioxide (E 171), gelatin, purified water.


Dosage form. The capsules are solid.


Basic physical and chemical properties:


30 mg: solid gelatin capsules No. 4 with a lid and body of light yellow color, marked in blue "30 mg" on the lid and" M 53 " on the body, containing granules from white to almost white in color;


45 mg: solid gelatin capsules No. 4 with a gray lid and body, marked in Blue "45 mg" on the lid and "M 54" on the body, containing granules from white to almost white in color;


75 mg: solid gelatin capsules No. 2 with a light yellow lid and a gray body, marked in blue "75 mg" on the lid and "M 55" on the body, containing granules from white to almost white.


Pharmacotherapeutic group.


Antiviral agents for systemic use. Direct-acting antiviral agents. Neuraminidase inhibitors. Oseltamivir. ATX code J05A H02.


Pharmacological properties.


Pharmacodynamics.


Oseltamivir phosphate is a propreparation of the active metabolite (oseltamivir carboxylate), which selectively inhibits neuraminidase of influenza viruses − an enzyme that catalyzes the release of newly formed viral particles from infected cells, their penetration into uninfected cells and further spread of the virus in the body.


Oseltamivir carboxylate inhibits neuraminidase of influenza viruses types A and B in vitro. Oseltamivir phosphate inhibits viral replication and pathogenicity in vitro. Oseltamivir, when administered orally, inhibits the replication of influenza viruses of types A and B and its pathogenicity in animal models of influenza infection in vivo with antiviral exposure, which was achieved in humans with a dose of 75 mg 2 times a day.


The antiviral activity of Oseltamivir was confirmed against influenza viruses of types A and B in experimental studies in healthy volunteers.


The IC50 values of Oseltamivir for the neuraminidase enzyme of clinical isolates of influenza A viruses ranged from 0.1 to 1.3 nmol, and for influenza B viruses they were 2.6 nmol. Published study data showed higher IC50 values for influenza B viruses with an average of 8.5 nmol.


Pharmacokinetics.


Suction


After oral administration of Oseltamivir, Phosphate is easily absorbed in the digestive tract and is largely converted to the active metabolite (oseltamivir carboxylate) by hepatic esterases. At least 75% of the oral dose enters the systemic circulation in the form of an active metabolite, less than 5% – in the form of the initial drug. Plasma concentrations of both the pro-drug and the active metabolite are proportional to the dose, so they do not depend on simultaneous use with food.


Distribution


In humans, the average volume of distribution of the active metabolite at steady state is approximately 23 liters – a volume equivalent to the volume of extracellular fluid of the body. Since neuraminidase activity is extracellular, oseltamivir carboxylate reaches all major sites of influenza infection localization.


Binding of the active metabolite to human plasma proteins is low (approximately 3 %).


Metabolism


Oseltamivir phosphate is largely converted to oseltamivir carboxylate by esterases found mainly in the liver. Neither oseltamivir phosphate nor the active metabolite are substrates or inhibitors of cytochrome P450 isoenzymes in in vitro studies. No Phase 2 conjugates were detected for both compounds in vivo.


Output


Absorbed oseltamivir is mainly excreted (>90 %) by conversion to oseltamivir carboxylate, which does not undergo further transformation and is excreted in the urine. In most patients, the maximum concentration of the active metabolite in plasma decreases with a Half-Life of 6-10 hours. The fully active metabolite is excreted by the kidneys. Renal clearance (18.8 L/H) exceeds the glomerular filtration rate (7.5 L/h), which indicates that the drug is additionally excreted by tubular secretion. Less than 20% of the radiolabeled drug taken orally is excreted in the feces.


Pharmacokinetics in special groups.

Children over 1 year of age


The pharmacokinetics of Oseltamivir were studied in children aged 1 to 16 years in a single-dose pharmacokinetic study. The pharmacokinetics of repeated administration of the drug were studied in a small number of children in a clinical efficacy study. In young children, the elimination of the pro-drug and the active metabolite occurred faster than in adults, which led to lower exposure, expressed in mg/kg dose. Taking the drug at a dose of 2 mg/kg gives the same exposure to oseltamivir carboxylate, which is achieved in adults after a single dose of 75 mg of the drug (which is equivalent to approximately 1 mg per 1 kg of body weight). The pharmacokinetics of oseltamivir in children and adolescents aged 12 years and older are the same as in adults.


Elderly patients


In elderly patients (65-78 years), the exposure of the active metabolite at steady state is 25-35% higher than in younger patients(see the section "dosage and administration").


Patients with kidney damage


Taking oseltamivir phosphate 100 mg 2 times a day for 5 days in patients with varying degrees of renal damage demonstrated that exposure to oseltamivir carboxylate is inversely proportional to the decrease in renal function. For dosage, see the section "dosage and administration".


Patients with liver damage


According to the results of in vitro studies, neither a significant increase in exposure to oseltamivir nor a significant decrease in exposure to the active metabolite of oseltamivir is expected in patients with impaired liver function (see the section "dosage and administration").


Pregnant women


A summary population pharmacokinetic analysis indicates that the dosage regimen of the drug, which is described in the section "dosage and administration", leads to low exposure (on average 30% during all trimesters) of the active metabolite in pregnant women compared to non-pregnant women. However, the predicted low exposure remains higher than the inhibitory concentrations (IC95 values) and ranges of influenza virus strains at the therapeutic level. In addition, data from observational studies reflect the benefits of the current dosage regimen for this category of patients. Therefore, it is not recommended to adjust the dose for pregnant women in the treatment or prevention of influenza (see the section "use during pregnancy or lactation").


Clinical characteristics.


Indications.


Flu treatment


The drug is indicated for adults and children over 1 year of age who have flu symptoms during the circulation of the flu virus. Efficacy was demonstrated when treatment was started within 2 days of the first onset of symptoms.


Flu prevention


- prevention of influenza in adults and children over 1 year of age after contact with a person with clinically diagnosed influenza during the circulation of the influenza virus;


- the appropriate use of the drug for the Prevention of influenza should be determined on a case-by-case basis, taking into account the circumstances and taking into account the group of patients who need protection. In exceptional situations (for example, in case of discrepancies between the circulating influenza virus and the influenza virus against which vaccination was carried out, and during a pandemic), seasonal prevention can be carried out in people aged 1 year and older.


The use of the drug does not replace flu vaccination


The use of antiviral agents for the treatment and Prevention of influenza should be based on official recommendations. The decision to use oseltamivir for treatment and Prevention should be made taking into account the characteristics of circulating influenza viruses, available information about the sensitivity of influenza viruses to drugs in each season, the impact of the disease in different geographical regions and patient groups.


Contraindications.


Hypersensitivity to oseltamivir phosphate or to any component of the drug.


Interactions with other drugs and other types of interactions.


The pharmacokinetic properties of Oseltamivir, such as weak protein binding and metabolism independent of the CYP450 and glucuronidase systems (see Section "pharmacokinetics"), indicate that a clinically significant interaction with other drugs is unlikely. 


Probenecid


When Oseltamivir and probenecid are co-administered in patients with normal renal function, no dose adjustment is required. Concomitant use of probenecid, which is a potent inhibitor of the anion pathway of renal tubular secretion, leads to an increase in exposure to the active metabolite oseltamivir by approximately half.


Amoxicillin


Oseltamivir does not show a kinetic interaction with amoxicillin, which is eliminated in the same way as oseltamivir, which indicates a weak interaction with Oseltamivir in this way.


Renal excretion


Clinically important interactions with other drugs, including competition for renal tubular secretion, are unlikely due to the known safety limits of most of these drugs, the characteristics of elimination of active metabolites (glomerular filtration and anionic tubular secretion), and the volume of excretion by these pathways. However, caution should be exercised when prescribing oseltamivir to patients taking medications with a similar route of excretion and a narrow therapeutic range (for example, chlorpropamide, methotrexate, phenylbutazone).


Additional information


Pharmacokinetic interactions between Oseltamivir and its active metabolite when co-administered with paracetamol, acetylsalicylic acid, cimetidine and antacids (magnesium hydroxide and aluminum hydroxide, calcium carbonate), rimantadine or warfarin (in patients who are on stable doses of warfarin and do not have influenza) were not detected.


In Phase III clinical trials of Oseltamivir for the treatment and Prevention of influenza, the drug was prescribed with commonly used drugs, such as ACE inhibitors (enalapril, captopril), thiazide diuretics (bendrofluazide), antibiotics (penicillin, cephalosporin, azithromycin, erythromycin and doxycycline), H2-receptor blockers (Ranitidine, cimetidine), beta-blockers (propranolol), xanthines (theophylline), sympathomimetics (pseudoephedrine), opioids (codeine), corticosteroids, inhaled bronchodilators, analgesics (acetylsalicylic acid, ibuprofen and paracetamol). When using Seltavir together with the listed drugs, no changes in the safety profile and frequency of adverse reactions were reported.


There is no mechanism of interaction with oral contraceptives.

Application features.


Oseltamivir is only effective against diseases caused by influenza viruses. There are no data on the effectiveness of oseltamivir in any diseases caused by pathogens other than influenza viruses.


The use of the drug does not replace flu vaccination. The use of the drug should not affect the examination of individuals for annual flu vaccination. Protection against influenza continues only while taking the drug. Seltavir should be used for the treatment and Prevention of influenza only if there are reliable epidemiological data that indicate the circulation of the virus. It has been demonstrated that the sensitivity of circulating influenza virus strains to the drug is highly variable, so the doctor should take into account the latest information on the sensitivity of currently circulating viruses to oseltamivir before making a decision on the use of the drug.


Severe skin reactions and hypersensitivity reactions


Anaphylaxis and severe skin reactions, including Toxic Epidermal Necrolysis, Stevens-Johnson syndrome, and erythema multiforme, have been reported during post-marketing use of the drug. Seltavir should be discontinued and appropriate treatment should be prescribed if such reactions occur or are suspected of occurring.


Severe concomitant conditions


There is no information on the safety or efficacy of oseltamivir in patients with severe or unstable diseases with an unavoidable risk of hospitalization.


Immunocompromised patients


The safety and efficacy of Oseltamivir for the treatment and Prevention of influenza in immunocompromised patients have not been established.


Diseases of the heart / respiratory system


The efficacy of Oseltamivir for the treatment of people with chronic heart and/or respiratory diseases has not been established. In such patients, there was no difference in the incidence of complications between the treatment and placebo groups.


Severe renal failure


Dose adjustment of the drug when used for treatment and Prevention is recommended for adults and adolescents (≥13 years) with severe renal insufficiency. There are insufficient clinical data on the use of the drug in children over 1 year of age with renal insufficiency for dosage recommendations (see the sections "pharmacokinetics", "dosage and administration").


Neuropsychiatric disorders


Cases of neuropsychiatric disorders have been reported in patients with influenza (mainly in children and adolescents) when using the drug. Such disorders have also been reported in patients with influenza who did not use this drug. Patients should be carefully monitored for behavioral changes, and the benefits and risks of continuing treatment should be evaluated with caution for each patient (see Section "adverse reactions").


Disposal of unused and expired medicines. The supply of the drug to the external environment should be minimized. The drug should not be disposed of in wastewater or household waste. For disposal, it is necessary to use a so-called waste collection system (if any).


Use during pregnancy or lactation.


Pregnancy


Due to the fact that controlled clinical studies on the use of oseltamivir in pregnant women have not been conducted, data on the use of the drug during pregnancy were obtained in the post-marketing period and during observation (see the section "pharmacokinetics"for data on exposure in pregnant women).


The data obtained and the results of animal studies indicate that there is no direct or indirect harmful effect on the course of pregnancy, embryo/fetus development and postnatal development. Pregnant women can use the drug taking into account the available information on safety, pathogenicity of the circulating strain of influenza virus and the condition of the pregnant woman after evaluating the benefit/risk ratio.


Breast-feeding period


In lactating rats, Oseltamivir and the active metabolite pass into breast milk. There is limited information on breast-feeding in women taking Oseltamivir and on the excretion of oseltamivir in human breast milk. Limited data show that Oseltamivir and its active metabolite were found in breast milk, but their levels were low, which may lead to subtherapeutic doses in infants. Given these data, as well as the pathogenicity of the circulating influenza virus strain and the condition of a breast-feeding woman, it may be possible to consider prescribing oseltamivir after evaluating the benefit/risk ratio.


Fertility


Based on preclinical data, there is no evidence on the effect of the drug on male or female fertility.


Ability to influence the reaction rate when driving vehicles or other mechanisms.


It doesn't affect you.


Dosage and administration.


Method of application


For oral administration.


Dosage


The drug in a dose of 75 mg can be used as:


– 1 capsule of 75 mg or


– 1 capsule of 30 mg and plus one capsule of 45 mg.

Tags: Oseltamivir