Description
Influcaine Pharmacodynamics
Mechanism of action
Antiviral drug. Oseltamivir phosphate is a prodrug, its active metabolite (oseltamivir carboxylate, OC) is an effective and selective inhibitor of influenza virus neuraminidase type A and B – the enzyme that catalyzes the release of newly formed virus particles from infected cells, their penetration into respiratory epithelial cells and further spread of the virus in the body.
Inhibits the growth of influenza virus in vitro and suppresses viral replication and pathogenicity in vivo, reduces the release of influenza A and B viruses from the body. Studies of clinical influenza virus isolates have shown that the concentration of OC needed to inhibit neuraminidase by 50% (IC50) is 0.1-1.3 nM for influenza A virus and 2.6 nM for influenza B virus. According to published studies, the median IC50 value for influenza B is slightly higher at 8.5 nM.
Indications
– Flu treatment for adults and children over one year of age.
– Influenza prophylaxis for adults and children over 12 years of age in groups at high risk of contracting the virus (in military units and large work collectives, in patients who are weakened).
– Flu prevention for children over 1 year of age.
Contraindications
– Hypersensitivity to oseltamivir phosphate or any component of the drug;
– Terminal stage of renal failure (creatinine clearance ?10 ml/min);
– children under 1 year of age;
– severe hepatic insufficiency.
Dosage and administration
- Orally, with a meal or regardless of the meal. Tolerability may be improved if taken with meals.
- If there are signs of capsule aging (e.g., increased fragility or other physical disorders), it is necessary to open the capsule and pour its contents into a small amount (maximum 1 teaspoon) of suitable sweetened food (chocolate syrup with normal or no sugar content, honey, light brown sugar or table sugar dissolved in water, sweet dessert, condensed milk with sugar, apple puree or yogurt) in order to conceal the bitter taste. The mixture should be thoroughly mixed and given to the patient whole. The mixture should be swallowed immediately after preparation. Detailed recommendations are given in the subsection “Extemporaneous preparation of the suspension”.
- Standard dosing regimen
- Treatment
- It is necessary to begin taking the drug within 2 days from the date of development of symptoms.
- Adults and teenagers aged ? 12 years old.
By 75 mg 2 times per day orally for 5 days. Increase of the dose more than 150 mg/day does not lead to strengthening of the effect. - Children with body weight >40 kg or at the age of 8 to 12 years
- Children who are able to swallow capsules may also be treated by taking one 75 mg capsule twice daily for 5 days.
- Children 1 to 8 years of age
Extemporally prepared suspension may be used (see subsection “Extemporally prepared suspension”). - Prevention
- Administration should begin within 2 days after exposure.
- Adults and adolescents aged ? 12 years old.
- By 75 mg 1 time per day orally for at least 10 days after contact with a patient. During seasonal influenza epidemics, 75 mg once daily for 6 weeks. The prophylactic effect lasts as long as the drug intake lasts.
- Children with body weight >40 kg or in age from 8 to 12 years
- Children who can swallow the capsules may also receive prophylactic therapy by taking one 75 mg capsule 1 time per day for 10 days.
- Children from 1 to 8 years of age
- It is possible to use extemporally prepared suspension (see subsection “Extemporal preparation of suspension”).
