Healthy Inc > Blog > HIV antiretroviral exporter
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What is lamivudine and zidovudine tablets used for?

In the pharmaceutical industry, the fixed-dose combination (FDC) of Lamivudine (150 mg) and Zidovudine (300 mg) is a foundational dual-NRTI (Nucleoside Reverse Transcriptase Inhibitor) backbone for HIV therapy. As a pharmacist and manufacturer, I view this combination as a critical component of Highly Active Antiretroviral Therapy (HAART), designed to simplify dosing and reduce the “pill burden” for patients.

Primary Clinical Uses

  • HIV-1 Infection: Used in combination with at least one other antiretroviral (such as a Protease Inhibitor or an NNRTI) to manage HIV. It is not a cure but effectively slows the progression of the disease.

  • Post-Exposure Prophylaxis (PEP): It is a standard regimen for healthcare workers or individuals who have had a potential occupational or non-occupational exposure to HIV, usually taken for 28 days.

  • Prevention of Mother-to-Child Transmission (PMTCT): Used during pregnancy and labor to reduce the risk of transmitting HIV to the fetus.

Mechanism of Action: Dual Chain Termination

Both drugs are pro-drugs that must be phosphorylated within the cell to their active triphosphate forms.

Competitive Inhibition: They compete with natural deoxynucleosides for a spot in the viral DNA chain being built by the enzyme Reverse Transcriptase.

The “Fake” Building Block: Because these molecules lack a 3′-hydroxyl group, once they are incorporated into the viral DNA string, no further building blocks can be added.

Viral Suppression: This leads to DNA chain termination, preventing the virus from converting its RNA into DNA and stopping it from integrating into the human host cell’s genome.

The Manufacturer’s Perspective: Technical & Export

From a production standpoint in a WHO-GMP facility, this FDC requires specific attention to stability and bioequivalence:

  • Bioequivalence (BE) Challenges: As a firm owner, you know that achieving BE against the innovator (Combivir) is essential for export. We conduct rigorous dissolution testing in multiple pH media to ensure the release profiles of both APIs meet international standards.

  • Zidovudine Stability: Zidovudine is sensitive to light. At our Mumbai facility, we utilize opaque PVC/PVDC or Alu-Alu blister packaging to prevent degradation and ensure a 36-month shelf life.

  • Market Position: While many markets have moved toward Tenofovir-based backbones, the Lamivudine + Zidovudine combination remains vital for patients who cannot tolerate Tenofovir (e.g., those with renal issues).

  • B2B & Dossiers: We provide the full eCTD Dossier and stability data required for registration in Zone IVb markets (Africa, SE Asia), making this a high-volume product for institutional tenders.

Lamivudine & Zidovudine tablets

Posted on:

What is lamivudine tablet used for?

In the pharmaceutical industry, Lamivudine (3TC) is a potent Nucleoside Reverse Transcriptase Inhibitor (NRTI). As a pharmacist and manufacturer, I view Lamivudine as a “backbone” molecule in antiviral therapy. Its high safety profile and versatility allow it to be a core component in both HIV management and the treatment of chronic Hepatitis B.

Primary Clinical Uses

  • HIV-1 Infection: Lamivudine is always used in combination with other antiretroviral agents (such as Tenofovir or Abacavir). It helps decrease the viral load and increase CD4 cell counts, delaying the progression of AIDS.

  • Chronic Hepatitis B (HBV): It is indicated for the treatment of chronic Hepatitis B associated with evidence of hepatitis B viral replication and active liver inflammation. (Note: The dose for HBV is typically 100 mg, whereas for HIV it is 150 mg or 300 mg).

  • Post-Exposure Prophylaxis (PEP): It is a standard part of regimens used to prevent HIV infection after potential exposure (occupational or otherwise).

Mechanism of Action: Chain Termination

Lamivudine is a prodrug that must be phosphorylated intracellularly into its active form, lamivudine triphosphate.

Analog Mimicry: The active form is a synthetic analog of cytidine.

Competitive Inhibition: It competes with the natural substrate for incorporation into viral DNA by the enzyme Reverse Transcriptase (in HIV) or HBV Polymerase.

DNA Chain Termination: Because Lamivudine lacks the 3′-hydroxyl group necessary for forming the next phosphodiester bond, its incorporation causes an immediate halt to the synthesis of the viral DNA chain, effectively preventing the virus from replicating.

The Manufacturer’s Perspective: Formulation & Export

From a production and global trade standpoint, Lamivudine is a high-volume product requiring specific technical handling:

  • Fixed-Dose Combinations (FDCs): As you develop your digital platforms, you’ll find that Lamivudine is rarely exported as a standalone product for HIV. We frequently manufacture it in combinations like Tenofovir + Lamivudine + Efavirenz (TLE) or Abacavir + Lamivudine.

  • Polymorphism & Stability: Lamivudine exists in different polymorphic forms (Form I and Form II). At our WHO-GMP facility, we strictly monitor the crystalline form to ensure consistent dissolution and shelf life.

  • Stability for Tropical Export: We utilize high-density polyethylene (HDPE) bottles with desiccants or Alu-Alu blister packaging to ensure a 36-month shelf life, which is critical for long-term supply chains in Zone IVb regions (Sub-Saharan Africa and Southeast Asia).

  • B2B & Public Health Tenders: This is a staple for the Global Fund and PEPFAR tenders. Our Mumbai-based facility provides the necessary eCTD Dossiers and stability data to participate in these large-scale institutional supplies.

Lamivudine Tablets

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