The combination of lamivudine and zidovudine is used along with other medications to treat human immunodeficiency virus (HIV) infection.
Nucleoside Reverse Transcriptase Inhibitor; Antiviral
Lamivudine and Zidovudine are synthetic nucleoside analogues with activity against human immunodeficiency virus (HIV).
Lamivudine: Intracellularly, Lamivudine is phosphorylated to its active 5’-triphosphate metabolite, Lamivudine triphosphate (L-TP). The principal mode of action of L-TP is inhibition of reverse transcription (RT) via DNA chain termination after incorporation of the nucleoside analogue. Following oral administration, Lamivudine is rapidly absorbed and extensively distributed. Binding to plasma protein is low.
Zidovudine: Intracellularly, Zidovudine is phosphorylated to its active 5’-triphosphate metabolite, Zidovudine triphosphate (ZDV-TP). The principal mode of action of ZDV-TP is inhibition of RT via DNA chain termination after incorporation of the nucleoside analogue. Following oral administration, Zidovudine is rapidly absorbed and extensively distributed. Binding to plasma protein is low. Zidovudine is eliminated primarily by hepatic metabolism.
Applies to the following strengths: 150 mg-300 mg
Cross-resistance may develop when given with emtricitabine. Exacerbation of anaemia with concomitant use of zidovudine with ribavirin. Increased adverse effects to zidovudine with nephrotoxic or myelosuppressive drugs (e.g. systemic pentamide, dapsone, pyrimethamine, co-trimoxazole, amphotericin, flucytosine, ganciclovir, interferon, vincristine, vinblastine, doxorubicin). Lamivudine and zalcitabine may inhibit the intracellular phosphorylation of one another. Antagonistic effect when zidovudine is used concomitantly with stavudine or doxorubicin.
Neutrophil count <0.75x109/l; Hb levels <7.5 g/dI or 4.65 mmol/l. Lactation. Renal & hepatic impairment; poor bone marrow reserve prior to treatment; risk of opportunistic infection; patients (especially obese women) w/ risk factors for or active liver disease. Patients w/ low body wt should avoid the combined formulation. Separate formulations of lamivudine or zidovudine should not be given at the same time as the combined formulation. If dose adjustment is necessary for either component, separate formulations should be used. Monitor haematological parameters (advanced disease: 2 wkly for 1st 3 mth of treatment, then monthly; early disease: 1-3 mthly), LFTs, mean cell volume, serum creatinine kinase, viral load, CD4 counts & blood lactate levels. Patient to report any sore throat, nausea, vomiting, unexplained bruising or bleeding. Maintain adequate hydration (2-3 L/day) unless fluid restricted. Withdraw treatment if symptomatic hyperlactaemia, metabolic/ lactic acidosis. progressive heptomegaly or rapidly elevating aminotransf erase levels occur. Cases of lactic acidosis & hepatic steatosis syndrome have been reported in pregnancy. Monitor hepatic enzymes & electrolytes regularly during 3rd trimester.
Headache, malaise & fatigue, fever or chills, nausea, diarrhoea, anorexia, abdominal pain, neuropathy, insomnia & other sleep disorders, dizziness, depressive disorders, nasal signs & symptoms, skin rashes, musculoskeletal pain, myalgia, arthralgia; anaemia, neutropenia & leucopenia (particularly at high doses of zidovudine; 1200-1500 mg/ day), usually seen 4-5 wk after therapy commencing; resp symptoms eg rapid and/or deep breathing; if symptomatic hyperlactatemia, metabolic/lactic acidosis, progressive hepatomegaly, or rapidly elevating aminotransf erase levels occur, w/draw treatment; mitochondrial damage leading to hyperlactatemia & hyperlipasemia; lipodystrophy; immune reactivation syndrome, osteonecrosis. Lactic acidosis associated w/ liver failure & pancreatitis (normally after several mth of treatment); haematological toxicity (eg. neutropenia & severe anaemia).
This drug should be used during pregnancy only if the benefit outweighs the risk to the fetus. Breastfeeding is not recommended during use of this drug. If replacement feeding is not an option, the WHO recommends a triple-drug regimen for HIV-infected women who are nursing; both drugs are included in alternative regimens.
Stored at a cool and dry place, protected from light and moisture. Keep the medicine out of the reach of children.
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