Ovirelis (Capsules) Instructions for Use

Marketing Authorization Holder

Obnovlenie Pfc, JSC (Russia)

ATC Code

J05AH02 (Oseltamivir)

Active Substance

Oseltamivir (Rec.INN registered by WHO)

Dosage Form

Ovirelis

Capsules 75 mg: 10 or 30 pcs.

Dosage Form, Packaging, and Composition

Capsules hard gelatin, size No. 1, with a white body and cap; the capsule contents are a white or white with a yellowish tint powder.

Excipients : Capsule contents corn starch pregelatinized, talc, croscarmellose sodium, povidone K30, calcium stearate.
Capsule body titanium dioxide (E171), gelatin.
Capsule cap titanium dioxide (E171), gelatin.

10 pcs. – blister pack (1) – cardboard packs.
10 pcs. – blister pack (3) – cardboard packs.

Clinical-Pharmacological Group

Antiviral drug

Pharmacotherapeutic Group

Systemic antiviral agents; direct-acting antiviral agents; neuraminidase inhibitors

Pharmacological Action

Antiviral agent. It is a prodrug, whose active metabolite (Oseltamivir carboxylate) selectively inhibits the neuraminidase of influenza virus types A and B. Neuraminidase is a glycoprotein that catalyzes the cleavage of the bond between the terminal sialic acid and sugar, thereby promoting the spread of the virus in the respiratory tract (the release of virions from the infected cell and penetration into the cells of the respiratory tract epithelium, preventing the inactivation of the virus by epithelial mucus). Oseltamivir carboxylate acts outside cells and competitively inhibits viral neuraminidase.

It inhibits the growth of the influenza virus in vitro and suppresses virus replication and its pathogenicity in vivo. Reduces the release of influenza A and B viruses from the body.

Does not affect the production of antibodies in response to the administration of an inactivated influenza vaccine.

The frequency of resistance of clinical virus isolates is 2%.

Efficacy for treatment has been proven when therapy is initiated within two days of the onset of disease symptoms.

Pharmacokinetics

After oral administration, it is almost completely absorbed from the gastrointestinal tract; absorption does not depend on food intake. It has a “first-pass” effect through the liver. Under the action of intestinal and hepatic esterases, it is converted into an active metabolite. 75% of the orally administered dose enters the systemic circulation as the active metabolite, less than 5% as the parent substance. Plasma concentrations of both the prodrug and the active metabolite are dose-proportional.

The mean V_d of the active metabolite is 23 L. Plasma protein binding is 3%.

It is excreted as the active metabolite primarily by the kidneys via glomerular filtration and tubular secretion. T_1/2 of oseltamivir is 1-3 hours. Oseltamivir carboxylate is not further metabolized and is excreted by the kidneys, its T_1/2 is 6-10 hours. Renal clearance is 18.8 L/h. Excreted via the intestine – less than 20%.

In elderly patients (65-78 years), the steady-state concentration of the active metabolite is 25-35% higher than in younger patients. In patients with renal failure, the excretion rate of oseltamivir carboxylate is inversely proportional to the creatinine clearance value.

Indications

Treatment of influenza in the presence of typical influenza symptoms during the period of influenza virus circulation in the general population.

For the treatment of influenza in adults and children, including full-term newborns, in the presence of typical influenza symptoms during the period of influenza virus circulation in the general population.

For post-exposure prophylaxis of influenza in adults and children aged 1 year and older after contact with a clinically diagnosed influenza case during the period of influenza virus circulation in the general population.

For post-exposure prophylaxis of influenza in children under 1 year of age during an influenza pandemic outbreak.

ICD codes

Dosage Regimen

Take orally.

For the treatment of influenza in adults: 75 mg twice daily for 5 days; in immunocompromised patients – including after organ or tissue transplantation, use for 10 days is recommended. Treatment should be started as early as possible: within the first two days from the onset of influenza symptoms.

Prophylaxis of influenza in adults and adolescents (aged 13-17 years): after contact with a sick person – 75 mg once daily for at least 10 days; during seasonal influenza epidemic – 75 mg once daily for up to 6 weeks or up to 12 weeks in immunocompromised patients. The protective effect lasts only as long as the drug is being taken.

In case of impaired renal function, dose adjustment is carried out according to a special scheme.

In children, the dose is set depending on age, body weight, and indications.

Adverse Reactions

Infections and infestations frequent – bronchitis, infections caused by Herpes simplex, nasopharyngitis, upper respiratory tract infections, sinusitis. In children frequent – otitis media.

Blood and lymphatic system disorders rare – thrombocytopenia.

Immune system disorders uncommon – hypersensitivity reactions; rare – anaphylactic reactions, anaphylactoid reactions.

Psychiatric disorders rare – agitation, abnormal behavior, anxiety, confusion, delirium, hallucinations, nightmares, self-injury.

Nervous system disorders very common – headache (frequent in children); common – insomnia; uncommon – altered consciousness, seizures.

Eye disorders rare – visual disturbance. In children common – conjunctivitis (including eye redness, discharge, and pain).

Ear and labyrinth disorders in children common – earache; uncommon – tympanic membrane disorders.

Cardiac disorders uncommon – arrhythmia.

Respiratory, thoracic and mediastinal disorders common – cough, sore throat, rhinorrhea (including in children); in children very common – cough, nasal congestion.

Gastrointestinal disorders very common – nausea; common – vomiting (very common in children), abdominal pain (including upper abdominal pain) (including in children), dyspepsia; rare – gastrointestinal bleeding, hemorrhagic colitis; in children very common – vomiting, common – abdominal pain (including upper abdominal pain).

Hepatobiliary disorders uncommon – increased liver enzyme activity; rare – fulminant hepatitis, hepatic failure, hepatitis.

Skin and subcutaneous tissue disorders uncommon – eczema, dermatitis, rash, urticaria; rare – angioedema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. In children uncommon – dermatitis (including allergic and atopic dermatitis).

General disorders and administration site conditions common – pain, dizziness (including vertigo), fatigue, pyrexia, limb pain.

Contraindications

Chronic renal failure (creatinine clearance less than 10 ml/min), hepatic failure, hypersensitivity to oseltamivir.

Use in Pregnancy and Lactation

Oseltamivir should be used during pregnancy and breastfeeding only if the expected clear benefit to the nursing mother outweighs the risk to the child.

Use in Hepatic Impairment

Dose adjustment is not required for the treatment and prevention of influenza in patients with impaired liver function. Studies in pediatric patients with impaired liver function have not been conducted.

Use in Renal Impairment

In adult patients and adolescents (13-17 years) with severe renal failure, dose adjustment is recommended for the treatment and prevention of influenza. Clinical data for dose adjustment in infants and children (aged 1 year and older) with renal impairment are lacking.

Pediatric Use

Used in children according to indications, in recommended doses, in an appropriate dosage form.

Data for determining the dose in premature infants (postconceptional age 36 weeks) are lacking.

Geriatric Use

Dose adjustment is not required, except for elderly patients with moderate or severe renal impairment.

Special Precautions

The use of oseltamivir does not replace vaccination against influenza.

The use of antiviral drugs for the treatment and prevention of influenza should be determined based on official recommendations. Decisions regarding the use of oseltamivir for the treatment and prevention of influenza should be made taking into account data on circulating influenza viruses, available information on drug susceptibility patterns for each season, and the impact of the disease in different geographical regions and patient populations.

Oseltamivir is effective only against disease caused by the influenza virus. Data on the efficacy of oseltamivir in the therapy of diseases caused by other agents are lacking.

The use of oseltamivir should not affect the evaluation of patients during annual influenza vaccination.
Protection against influenza lasts only as long as Oseltamivir is being taken.

Oseltamivir should be used only for the treatment and prevention of influenza and only if reliable epidemiological data indicate that the influenza virus is circulating in the general population.

The sensitivity of circulating strains of the influenza virus to oseltamivir can vary significantly.
Therefore, when prescribing the drug, the most recent available information on the sensitivity of the circulating virus to oseltamivir must be taken into account.

Patients should be carefully monitored for behavioral changes; the risk and benefit of continuing therapy should be assessed for each patient individually.

Drug Interactions

Drugs that block tubular secretion increase the concentration of the active metabolite by 2-3 times (due to inhibition of the process of active tubular secretion in the kidneys), which does not require dose adjustment.

Use Oseltamivir with caution in combination with drugs that have a narrow therapeutic index (for example, chlorpropamide, methotrexate, phenylbutazone).

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.