Zidovudine + Lamivudine + Nevirapine (Zidovudinum + Lamivudinum + Nevirapinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
Read on
Clinical and pharmacological group: & nbsp

Means for the treatment of HIV infection

Included in the formulation
  • Zidolam-N
    pills inwards 
    Heterose Labs Limited     India
    • АТХ:

    J.05.A.R.05   Zidovudine + Lamivudine + Nevirapine

    Pharmacodynamics:

    Antiviral combination. The use of drugs in combination slows the development of virus resistance to zidovudine.

    Zidovudine

    The synthetic analogue of thymidine is phosphorylated into zidovudine monophosphate by the action of cellular kinases and then transformed into di- and triphosphate under the influence of host cell enzymes, which, due to competition with deoxythymidine triphosphate, suppresses the replication of human immunodeficiency virus by inhibiting HIV reverse transcriptase. Thus, the synthesis of mRNA and, correspondingly, the proteins of the virus is disrupted.

    Lamivudine

    The synthetic analogue of thymidine, under the action of cellular kinases, is phosphorylated into 5-phosphate, which, due to competition with deoxythymidine triphosphate, suppresses replication of the human immunodeficiency virus by inhibiting HIV reverse transcriptase. Thus, the synthesis of mRNA and, correspondingly, the proteins of the virus is disrupted. It is active against the hepatitis B virus.

    Nevirapine

    A non-nucleoside reverse transcriptase inhibitor, HIV-1, binds directly to reverse transcriptase,blocks RNA and DNA-dependent activity of DNA polymerase, which causes destruction of the catalytic center of the enzyme. It is not active against HIV-2-reverse transcriptase and human polymerases of α, β, γ and s.

    Pharmacokinetics:

    Zidovudine

    After oral ingestion, up to 65% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved after 0.5-1.5 hours. The connection with plasma proteins is 38%.

    Penetrates through the blood-brain and placental barrier. Metabolism in the liver.

    The elimination half-life is 1 hour. Elimination by the kidneys.

    Lamivudine

    After oral administration, up to 88% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 1 hour. The connection with plasma proteins is 36%.

    Penetrates through the blood-brain and placental barrier. Metabolism in the liver.

    The half-life is 5-7 hours. Elimination by the kidneys.

    Nevirapine

    After oral administration, up to 90% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 4 hours. The connection with plasma proteins is 60%. Inductor of cytochrome P450 enzymes.

    Penetrates through the blood-brain and placental barrier. Metabolism in the liver.

    The half-life is 45 hours. Elimination by the kidneys and with feces.

    Indications:

    It is used to treat HIV infection.

    ICD-10

    I.B20-B24   Disease caused by the human immunodeficiency virus [HIV]

    Contraindications:

    Violations of kidney function, neutropenia, anemia, peripheral neuropathy, individual intolerance, children under 16 years.

    Carefully:

    Dysfunction of the liver, hypersensitivity.

    Pregnancy and lactation:

    Recommendations for FDA - Category C. When pregnancy is used with caution, in those cases where the predicted benefit overcomes the risk to the fetus. According to existing recommendations, HIV-infected women are recommended to avoid breastfeeding because of the risk of infection of the child. Given these recommendations, patients receiving zidovudine, breastfeeding should be prohibited.

    Dosing and Administration:

    Inside, regardless of food intake. 1 tablet 2 times a day.

    Side effects:

    Central and peripheral nervous system: asthenia, headache, hallucinations, insomnia, paresthesia, peripheral neuropathy.

    Respiratory system: cough.

    Hemopoietic system: anemia, leukopenia, thrombocytopenia, pancytopenia.

    Digestive system: anorexia, pancreatitis, dyspepsia, flatulence, increased levels of hepatic transaminases, hepatomegaly with fatty liver dystrophy.

    Musculoskeletal system: arthralgia, myalgia.

    Dermatological reactions: hyperpigmentation of the mucous membrane of the mouth, skin, nails.

    Allergic reactions.

    Overdose:

    Increased side effects, neuropathy.

    Treatment is symptomatic, continuous hemodialysis.

    Interaction:

    Simultaneous use with myelosuppressive and nephrotoxic drugs (dapsone, pentamidine, pyrimethamine, amphotericin, co-trimoxazole, doxorubicin, ganciclovir, flucytosine, interferon, vinblastine, vincristine) increases the risk of side effects.

    Ribavirin blocks the antiviral activity of zidovudine.

    Trimethoprim increases the concentration of lamivudine by 40%.

    With the simultaneous use of nevirapine with drugs metabolized by isoenzymes CYP3A and CYP2B6, it is possible to reduce their concentration in the blood plasma.

    With the simultaneous use of nevirapine with preparations containing St. John's wort, it is possible to reduce the concentration of nevirapine.

    Nevirapine reduces the concentration of methadone.

    Special instructions:

    Monitoring of the cellular composition of peripheral blood.

    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.

    In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

    Instructions
    Up