Lamivudin-ZTS 150 mg, 60 pcs.

The antiviral agent is a nucleoside reverse transcriptase inhibitor. Penetrating into cells, it is metabolized to 5-triphosphate, which inhibits HIV reverse transcriptase, which leads to suppression of viral replication. It is active against zidovudine-resistant strains, and when used in combination it slows the development of virus resistance to zidovudine (in previously untreated patients).

It has higher therapeutic index in vitro (inhibits bone marrow progenitor cells weaker than zidovudine, and also has less cytotoxic effect on lymphocytes of peripheral blood, lymphocytic and monocytic-macrophage cell lines). Slightly affects cellular deoxynucleotide metabolism and DNA content in mitochondria of intact cells.

Lamivudine is highly active against hepatitis B virus (HBV) in all cell lines studied and in all experimentally infected animals.

Indications

Treatment of HIV infection in adults and children (as part of combination therapy with other antiretroviral drugs).

Chronic viral hepatitis B against HBV replication in patients aged 16 years and older.

Active ingredient

Lamivudine

Interaction

Concomitant use of lamivudine increases the duration of action of zidovudine by 13% and its C_max in plasma by 28%. Zidovudine does not affect the pharmacokinetics of lamivudine.

Synergism with zidovudine and other antiviral agents used in the treatment of HIV infections has been noted with respect to HIV replication in cell culture.

Concomitant use with didanosine, sulfonamides, zalcitabine increases the risk of pancreatitis.

Concomitant use with dapsone, didanosine, isoniazid, stavudine, zalcitabine increases the risk of peripheral neuropathy.

Trimethoprim increases the plasma concentration of lamivudine.

Directions for use

The dose and regimen of treatment are established depending on the indications.

Special Instructions

With caution is used in patients with impaired renal function. Dose adjustment is necessary if CKR is less than 50 ml/min.

As lamivudine is excreted almost exclusively by the kidneys, dosage regimen adjustment is not required in patients with hepatic impairment. However, caution should be used in patients with severe hepatitis B virus-associated cirrhosis, given the risk of exacerbation of the disease after withdrawal of lamivudine.

Lamivudine is not used in combination with zidovudine if there is neutropenia (neutrophil count is less than 750/μL) or anemia (hemoglobin less than 7.5 g/dL or 4.65 mmol/L).

If abdominal pain, nausea, vomiting or elevated plasma pancreatic enzyme levels occur, lamivudine should be stopped and not restarted until the diagnosis of pancreatitis is excluded.

The use of lamivudine does not prevent the possibility of infection through sexual contact or through blood.

The possibility of secondary infection should be kept in mind during treatment.

Pediatric use

There is no experience with lamivudine in children under 3 months of age. In children with impaired renal function, adjustment of the dosing regimen is recommended in the same proportions as in adults.

Features

It is rapidly absorbed from the gastrointestinal tract. Bioavailability is 80-88%. C_max in blood plasma is reached 1 hour after intake. Lamivudine penetrates through the HEB, placental barrier. Binding to plasma proteins is 36%. Metabolized by phosphorylation to form 5-triphosphate. T_1/2 is 5-7 h. 68-71% is excreted unchanged in the urine.

Contraindications

Hypersensitivity to lamivudine.

Side effects

Digestive system disorders: pain and discomfort in the epigastric region, nausea, vomiting, diarrhea, decreased appetite, increased liver transaminase activity.

CNS disorders: increased fatigue, headache.

Respiratory system: respiratory tract infections.

Others: general malaise.

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Similarities

Zeffix, Lamivudine