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.05 Lamivudine
Pharmacodynamics:HIV refers to RNA-containing viruses, which require the creation of complementary DNA for replication. Lamivudine intracellularly phosphorylated into the active metabolite, lamivudine triphosphate, which, like natural nucleotides, is inserted into the synthesized chain of viral DNA and blocks its further elongation. Has a weak inhibitory effect on DNA polymerase (α, β and γ) in mammals. Resistance to lamivudine is associated with HIV mutations. Lamivudine It is also highly active against hepatitis B virus (HBV).
Pharmacokinetics:After oral administration lamivudine quickly and almost completely absorbed, bioavailability is 86%. The presence of food in the stomach slows down the absorption (3-3.5 times the time to reach Cmax and its value is reduced by 40%), but does not affect AUC. Binding to plasma proteins reaches 36%; on the surface of erythrocytes is adsorbed up to 57% of the dose. Apparent volume of distribution is 1.3 l / kg. It is subject to insignificant (5%) biotransformation in the liver with the formation of an inactive transulfoxide metabolite. Excreted by the kidneys mostly unchanged; partially excreted in breast milk.Half-Elimination Period (T1/2) is 3-5 hours. In case of renal failure, the clearance decreases in proportion to the drop in the glomerular filtration rate.
Indications:Treatment of HIV infection caused by HIV-1 (in combination antiretroviral therapy), in adults and children older than 3 months. Chronic viral hepatitis B on the background of viral replication.
I.B20-B24.B23.8 The disease caused by HIV, with manifestations of other specified states
I.B15-B19.B18.1 Chronic viral hepatitis B without delta-agent
I.B15-B19.B18.0 Chronic viral hepatitis B with delta-agent
Contraindications:Life-threatening allergic reactions (anaphylaxis, Stephen-Johnson syndrome) on lamivudine or any components of dosage forms.
Carefully:Lactate acidosis and severe hepatomegaly with steatosis, exacerbation of hepatitis, renal, hepatic insufficiency, pancreatitis (including in the anamnesis), peripheral neuropathy (including in the anamnesis).
Pregnancy and lactation:Action category for the fetus by FDA - FROM
It is not recommended to appoint women until the 14th week of pregnancy. If you need to use the drug before the 14th week of pregnancy, you should carefully correlate the intended benefit to the mother and the potential risk to the fetus.
Dosing and Administration:The recommended dose for adults and adolescents over 16 years is 300 mg per day (2 doses) or a single dose of 300 mg per day in combination with other antiretroviral drugs. Children aged 3 months to 16 years are recommended a dose of 4 mg / kg 2 times a day.
In patients with renal insufficiency, correction of the dosing regimen is necessary taking into account the creatinine clearance: at a level of more than 30 ml / min lamivudine apply in a dose of 150 mg once a day; at a level of 5-30 ml / min in a dose of 150 mg once a day.
Side effects:Headache, dizziness, weakness, sleep disorders, neuropathy, cough, flu-like syndrome, anorexia, nausea, diarrhea, vomiting, epigastric pain, necrotic pancreatitis (possibly fatal), myalgia, arthralgia, leukopenia, anemia, fever, sweating, alopecia, allergic reactions.
Overdose:Specific symptoms of overdose are absent. Hemodialysis and peritoneal dialysis slightly affect the excretion of lamivudine. When an overdose of lamivudine is recommended, follow-up and standard maintenance therapy.
Interaction:Increases Cmax zidovudine by 39%.Trimethoprim and sulfamethoxazole increase lamivudine AUC by 44%, reduce its overall clearance (Cl) by 29% and renal Cl by 30%.
It is not recommended to combine with zalcitabine and cladribine because of mutual inhibition of phosphorylation in the cell.
Special instructions:The use of lamivudine does not prevent the possibility of infection during sexual intercourse or through blood. Experience with lamivudine in children younger than 3 months is absent. Lamivudine should be used with caution in patients with hepatic cirrhosis due to the hepatitis B virus, given the risk of hepatitis after lamivudine withdrawal. During the treatment period, one should keep in mind the possibility of secondary infections caused by saprophytic microorganisms.
There are recommendations for HIV-infected women to avoid breastfeeding because of the risk of infection of the child. Given these recommendations, patients receiving lamivudine, breastfeeding should be prohibited.