Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
АТХ:J.05.A.F.07 Tenofovir
Pharmacodynamics:Tenofovir disoproxil fumarate is a prodrug that is hydrolyzed to tenofovir, dizoproxil, then to tenofovir, which is an analogue of nucleosides. Phosphorylated to tenofovirdiophosphate - obligate terminator of the DNA chain. Due to antagonism with natural deoxyadenosine triphosphate inhibits RNA-dependent DNA polymerase of HIV and DNA polymerase of hepatitis B virus - interruption of DNA synthesis of these viruses. Weak inhibitor of cellular DNA polymerases α, β and γ mammals. In a dose of less than 300 μmol / l in vitro does not affect the synthesis of mitochondrial DNA and the formation of lactic acid.
Pharmacokinetics:After ingestion with meals, up to 40% is absorbed in the gastrointestinal tract.The maximum concentration in the blood plasma is reached after 1.5 hours.
Metabolism in the liver.
The half-life is 17-24 hours. Elimination by the kidneys.
Indications:It is used to treat patients with HIV-1 infection.
I.B20-B24 Disease caused by the human immunodeficiency virus [HIV]
Contraindications:Impaired renal function, peripheral neuropathy, individual intolerance, children under 18 years of age.
Carefully:
Dysfunction of the liver.
Pregnancy and lactation:Recommendations for FDA - category is not defined. It is used in pregnancy according to vital indications, it is contraindicated in lactation period.
Dosing and Administration:Inside 300 mg once a day.
The highest daily dose: 300 mg.
The highest single dose: 300 mg.
Side effects:Central and peripheral nervous system: asthenia, headache, hallucinations, insomnia, peripheral neuropathy.
Respiratory system: dyspnoea.
Hemopoietic system: anemia.
Digestive system: anorexia, pancreatitis, dyspepsia, increased level of hepatic transaminases.
Musculoskeletal system: arthralgia, myalgia, rhabdomyolysis, myopathy.
Urinary system: acute renal failure, nephrogenic diabetes insipidus.
Allergic reactions.
Overdose:Increased side effects, neuropathy.
Treatment is symptomatic - dose reduction or drug withdrawal.
Interaction:Admission of fatty foods improves the absorption of the drug in the gastrointestinal tract.
Simultaneous use with didanosine, chloramphenicol, cisplatinum, hydralazine, vincristine, isoniazid, zalcitabine, metronidazole increases the risk of peripheral neuropathy.
Special instructions:Admission of the drug does not prevent the development of opportunistic infections and does not reduce the risk of HIV infection through the blood and during sexual intercourse.