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 Nucleosides - reverse transcriptase inhibitors
J.05.A.F.04 Stavudine
Pharmacodynamics:The synthetic analogue of thymidine under the action of cellular kinases is phosphorylated in stavudine triphosphate, which, due to competition with deoxythymidine triphosphate, suppresses the replication of the human immunodeficiency virus by inhibiting the HIV reverse transcriptase. Also violates the synthesis of viral DNA, terminating its chains, since stavudine 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, stavudine triphosphate inhibits cellular DNA polymerases β and γ, greatly reducing the synthesis of mitochondrial DNA.
Pharmacokinetics:After ingestion, up to 86% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 1 hour, it penetrates the blood-brain barrier.
Metabolism in the liver by phosphorylation to the active metabolite - stavudine triphosphate.
Half-life is 1.5 hours. Elimination by the kidneys, about 40% unchanged.
Indications:It is used to treat patients with HIV infection who received zinovudine for a long time.
I.B20-B24 Disease caused by the human immunodeficiency virus [HIV]
Contraindications:Impaired renal function, peripheral neuropathy, individual intolerance.
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:Children with body weight less than 30 kg at 2 mg / kg 2 times / day with an interval of 12 hours.
Children with a body weight of more than 30 kg - appoint adult doses.
Adults
Patients with a body weight of less than 60 kg at 30 mg 2 times / day, more than 60 kg - 40 mg 2 times / day.
The highest daily dose: 40 mg.
The highest single dose: 80 mg.
Side effects:Central and peripheral nervous system: asthenia, headache, hallucinations, insomnia, peripheral neuropathy.
The system of hematopoiesis: anemia.
Digestive system: anorexia, pancreatitis, dyspepsia, increased level of hepatic transaminases.
Musculoskeletal system: arthralgia, myalgia.
Allergic reactions.
Overdose:Increased side effects, neuropathy.
Treatment is symptomatic - dose reduction or drug withdrawal.
Interaction:Simultaneous use with didanosine, chloramphenicol, cisplastin, hydralazine, vincristine, isoniazid, zalcitabine, metronidazole increases the risk of peripheral neuropathy.
Special instructions:Taking 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.