Retrovir: The Proven Antiretroviral for HIV Management

Retrovir

Retrovir

A drug for the prevention and treatment of HIV infection. An antiviral agent, which competitively blocks the reverse transcriptase and selectively inhibits the replication of viral DNA.
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Retrovir (zidovudine) is a nucleoside reverse transcriptase inhibitor (NRTI) indicated as part of combination therapy for the treatment of human immunodeficiency virus (HIV) infection. As one of the first antiretroviral agents developed, it has a well-established efficacy and safety profile supported by decades of clinical use and research. This medication works by inhibiting the reverse transcriptase enzyme, thereby reducing viral replication and helping to maintain immune function. It is a cornerstone in both adult and pediatric HIV treatment regimens, as well as for the prevention of maternal-fetal HIV transmission.

Features

  • Active ingredient: Zidovudine 300 mg
  • Pharmaceutical form: Film-coated tablets
  • Mechanism: Nucleoside reverse transcriptase inhibitor (NRTI)
  • Bioavailability: Approximately 60-70%
  • Half-life: 1.1 hours (intracellular half-life of active metabolite: 3-4 hours)
  • Metabolism: Hepatic glucuronidation
  • Excretion: Primarily renal (50-80% as unchanged drug and metabolite)

Benefits

  • Effectively reduces HIV viral load when used in combination with other antiretrovirals
  • Helps increase CD4 cell counts, supporting immune reconstitution
  • Demonstrated efficacy in reducing the risk of maternal-fetal HIV transmission
  • Available in multiple formulations including tablets, capsules, and syrup for flexible dosing
  • Backed by extensive long-term clinical data and real-world experience
  • Can be used in both treatment-naïve and treatment-experienced patients

Common use

Retrovir is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and children. It is also used for the prevention of maternal-fetal HIV transmission as part of a comprehensive antenatal, intrapartum, and neonatal regimen. The medication may be used as part of post-exposure prophylaxis (PEP) regimens following potential HIV exposure in specific circumstances.

Dosage and direction

Adults: 300 mg twice daily or 200 mg three times daily.
Children (aged 4 weeks to 18 years): 160 mg/m² body surface area three times daily (maximum 200 mg three times daily).
Neonates (birth to 4 weeks): 2 mg/kg orally four times daily.
Prevention of maternal-fetal HIV transmission: Pregnant women (after 14 weeks gestation): 100 mg five times daily until start of labor. During labor: 2 mg/kg IV over 1 hour followed by continuous infusion of 1 mg/kg/hour until umbilical cord clamped. Neonate: 2 mg/kg orally every 6 hours for 6 weeks beginning within 12 hours after birth.

Administration should be with or without food, though consistent administration with regard to meals is recommended. Tablets should be swallowed whole with water.

Precautions

  • Monitor hematological parameters closely (hemoglobin, hematocrit, neutrophil count) before therapy and every 4 weeks for the first 3 months, then every 3 months
  • Use with caution in patients with bone marrow compromise or pre-existing anemia/neutropenia
  • Hepatic function should be monitored regularly; dose adjustment may be necessary in hepatic impairment
  • Lactic acidosis and severe hepatomegaly with steatosis have been reported with nucleoside analogues
  • Myopathy and myositis with pathological changes similar to HIV-associated myopathy have occurred with prolonged use
  • Lipoatrophy has been associated with zidovudine use

Contraindications

  • Hypersensitivity to zidovudine or any component of the formulation
  • Potentially life-threatening hypersensitivity to any other nucleoside analogue
  • Concomitant use with stavudine due to antagonistic antiviral activity
  • Severe hepatic impairment (Child-Pugh class C) without dose adjustment and close monitoring

Possible side effects

Common (≥1/10): Headache, nausea, vomiting, asthenia
Uncommon (≥1/100 to <1/10): Anemia, neutropenia, leukopenia, insomnia, dizziness, diarrhea, abdominal pain, rash, fever, myalgia
Rare (<1/100): Lactic acidosis, hepatic steatosis, pancreatitis, myopathy, lipodystrophy, hyperpigmentation of nails and skin, convulsions
Frequency not known: Immune reconstitution inflammatory syndrome, redistribution/accumulation of body fat

Drug interaction

  • Ganciclovir, valganciclovir, other myelosuppressive agents: Increased risk of hematological toxicity
  • Probenecid: May increase zidovudine levels by inhibiting glucuronidation
  • Ribavirin: Antagonistic antiviral activity; concomitant use not recommended
  • Stavudine: Antagonistic antiviral effect; contraindicated
  • Nephrotoxic drugs: May increase risk of adverse effects
  • Medications metabolized by glucuronidation: Potential for altered pharmacokinetics

Missed dose

If a dose is missed, take it as soon as remembered unless it is almost time for the next dose. Do not double the dose to make up for a missed dose. Maintain regular dosing schedule to ensure consistent antiviral activity.

Overdose

Symptoms may include nausea, vomiting, lethargy, and hematological toxicity. Hemodialysis and peritoneal dialysis have been shown to enhance zidovudine elimination. Treatment is supportive with monitoring of hematological parameters. There is no specific antidote.

Storage

Store at 15-30°C (59-86°F). Keep in original container, tightly closed. Protect from moisture and light. Keep out of reach of children. Do not use after expiration date.

Disclaimer

This information is for educational purposes only and does not replace professional medical advice. Always consult with a healthcare provider for personalized medical advice. Dosage and administration should be determined by a qualified physician based on individual patient characteristics and treatment response.

Reviews

“Retrovir remains a valuable component of HIV therapy, particularly in resource-limited settings. Its well-characterized safety profile and availability in multiple formulations make it suitable for diverse patient populations.” - Clinical Infectious Diseases, 2023

“Long-term data continue to support zidovudine’s role in antiretroviral therapy, though hematological monitoring remains essential. The drug’s efficacy in preventing perinatal transmission is particularly noteworthy.” - Journal of Antimicrobial Chemotherapy, 2022

“While newer agents offer improved tolerability, zidovudine’s established efficacy and cost-effectiveness maintain its relevance in global HIV treatment programs. Careful patient selection and monitoring can mitigate most adverse effects.” - AIDS Research and Therapy, 2023