Included in the formulation
АТХ:J.05.A.R.03 Tenofovir Dizoproxil + Emtricitabine
Pharmacodynamics:Tenofovir
Under the action of cellular kinases phosphorylated in the active metabolite - tenofovir diphosphate - an analogue of the nucleoside monophosphate (nucleotide) of adenosine monophosphate, which, due to competition with deoxythymidine triphosphate, suppresses the replication of the human immunodeficiency virus by inhibiting the HIV reverse transcriptase.
EmtricitabineThe synthetic analogue of cytidine under the action of cellular kinases is phosphorylated into emtricitabine-5-triphosphate, which, due to competition with deoxythymidine triphosphate, suppresses the replication of the human immunodeficiency virus by inhibiting HIV reverse transcriptase. Also violates the synthesis of viral DNA, terminating its chains, since emtricitabine does not contain in its composition a molecule of the 3-hydroxyl group, without which the extension of the DNA chain is impossible.
In addition, emtricitabine-5-triphosphate inhibits cellular DNA polymerases β and γ, significantly reducing the synthesis of mitochondrial DNA.
Pharmacokinetics:Tenofovir
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.
Emtricitabine
After ingestion, up to 93% is absorbed in the gastrointestinal tract. The connection with plasma proteins is less than 4%. The maximum concentration in the blood plasma is achieved after 2.5 hours.
Metabolism in the liver.
Half-life is 10 hours. Elimination by the kidneys.
Indications:It is used to treat patients with HIV 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:1 tablet once a day during meals.
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, cisplatin, 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.