Retrovir: The Foundation of Effective HIV Management
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Retrovir (zidovudine) is a nucleoside reverse transcriptase inhibitor (NRTI) that has served as a cornerstone of antiretroviral therapy (ART) for decades. It works by inhibiting the reverse transcriptase enzyme, a critical component for the replication of the human immunodeficiency virus (HIV). This action impedes the virus’s ability to multiply, thereby reducing the viral load in the body and allowing the immune system to recover. It is indicated, in combination with other antiretroviral agents, for the treatment of HIV-1 infection and for the prevention of maternal-fetal HIV transmission. As a proven and extensively studied medication, Retrovir remains a vital component in tailored treatment regimens for a diverse patient population.
Features
- Active pharmaceutical ingredient: Zidovudine.
- Dosage forms: 100 mg hard gelatin capsules; 300 mg tablets; 200 mg/10 mL or 240 mg/12 mL oral syrup; 10 mg/mL intravenous (IV) infusion solution.
- Pharmacological class: Nucleoside Reverse Transcriptase Inhibitor (NRTI).
- Mechanism of Action: Acts as a thymidine analogue. It is phosphorylated to its active metabolite, zidovudine 5’-triphosphate, which competitively inhibits the incorporation of thymidine triphosphate into viral DNA by HIV reverse transcriptase. This results in chain termination and halts viral replication.
- Bioavailability: Approximately 60-70% following oral administration.
- Protein Binding: 30-38% to plasma proteins.
- Metabolism: Primarily hepatic via glucuronidation by UGT2B7 to an inactive metabolite, 3’-azido-3’-deoxy-5’-O-β-D-glucopyranuronosylthymidine (GZDV).
- Elimination Half-life: 0.5 to 3 hours for zidovudine; 1 to 2 hours for its inactive metabolite, GZDV.
- Excretion: Primarily renal (approximately 50-80% of the dose is excreted in the urine as GZDV, with 14-18% excreted as unchanged zidovudine).
Benefits
- Proven Virological Suppression: Effectively reduces HIV viral load when used in combination with other antiretroviral agents, helping to achieve and maintain an undetectable status.
- Immunological Restoration: By controlling viral replication, it facilitates the recovery of CD4 (T-cell) counts, strengthening the immune system and reducing the risk of opportunistic infections.
- Prevention of Mother-to-Child Transmission (MTCT): Significantly reduces the rate of perinatal transmission of HIV from an infected mother to her fetus/newborn when administered according to established protocols during pregnancy, labor, and to the neonate.
- Extensive Clinical History: With decades of real-world use and clinical data, its efficacy and safety profile are well-characterized, providing clinicians with a reliable and predictable therapeutic option.
- Flexible Formulations: Availability in multiple formulations (capsules, tablets, syrup, IV) allows for tailored dosing across different patient populations, including adults, pediatric patients, and those unable to take oral medications.
Common use
Retrovir is indicated for the treatment of HIV-1 infection in adults and children, always in combination with other antiretroviral agents. Combination therapy is essential to prevent the emergence of resistance. Its second primary indication is the prevention of maternal-fetal HIV transmission as part of a regimen for pregnant individuals with HIV infection and their newborns. It is not recommended for use as a monotherapy.
Dosage and direction
For the treatment of HIV infection in adults: The recommended oral dosage is 300 mg twice daily or 200 mg three times daily. The IV dosage is 1 mg/kg, infused over one hour, every four hours until oral therapy can be administered. For pediatric patients: Dosage is based on body weight and body surface area and must be calculated carefully by a healthcare provider. The oral syrup is often used for this population. For prevention of maternal-fetal HIV transmission: A specific regimen is used for the mother during pregnancy and labor, and for the newborn after birth. This typically involves oral administration to the mother starting after the first trimester and IV administration during labor, followed by oral syrup for the neonate for the first six weeks of life. Always take Retrovir exactly as prescribed by your physician. Do not alter the dose or stop taking it without consulting your doctor. It can be taken with or without food.
Precautions
- Hematologic Toxicity: Retrovir has been associated with hematologic toxicity including neutropenia and severe anemia, which may require dose interruption or discontinuation. Regular monitoring of blood counts is mandatory.
- Myopathy: Prolonged use has been associated with symptomatic myopathy and myositis.
- Lactic Acidosis: Like other NRTIs, Retrovir carries a risk of lactic acidosis and severe hepatomegaly with steatosis, which can be fatal. Use with caution in patients with known risk factors for liver disease.
- Fat Redistribution: Redistribution/accumulation of body fat (lipodystrophy) has been observed in patients receiving antiretroviral therapy.
- Immune Reconstitution Inflammatory Syndrome (IRIS): Autoimmune disorders may occur months after initiation of ART as the immune system recovers.
- Patients with impaired renal or hepatic function require dosage adjustment and close monitoring.
Contraindications
Retrovir is contraindicated in patients with a known hypersensitivity to zidovudine or any component of the formulation. It is also contraindicated for use with other drugs containing zidovudine or stavudine. Due to the risk of antagonism, concomitant use with ribavirin or stavudine is contraindicated.
Possible side effect
Common side effects may include headache, nausea, vomiting, asthenia (loss of strength), malaise, insomnia, and mild musculoskeletal pain. More serious side effects that require immediate medical attention include:
- Signs of anemia (severe fatigue, pale skin, shortness of breath)
- Signs of neutropenia/infection (fever, chills, sore throat)
- Signs of myopathy (muscle pain, weakness, tenderness)
- Signs of lactic acidosis (nausea, vomiting, stomach pain, unexplained weight loss, difficulty breathing)
- Signs of hepatotoxicity (yellowing of skin/eyes, dark urine, clay-colored stools)
- Skin rash
Drug interaction
Retrovir has the potential for significant drug interactions. Inform your doctor of all medications you are taking, including:
- Stavudine & Ribavirin: Contraindicated due to antagonistic effect.
- Other Bone Marrow Suppressants: (e.g., ganciclovir, interferon-alpha, cytotoxic chemotherapy) may increase the risk of hematologic toxicity.
- Nephrotoxic Drugs: May impair excretion of Retrovir.
- Probenecid: May inhibit the glucuronidation of Retrovir, leading to increased plasma levels and potential for toxicity.
- Phenytoin: May alter the levels of both phenytoin and Retrovir, requiring monitoring.
Missed dose
If you miss a dose, take it as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and resume your regular dosing schedule. Do not take a double dose to make up for a missed one. Maintaining a consistent schedule is crucial for efficacy.
Overdose
Cases of overdose have been reported. Symptoms may include nausea, vomiting, lethargy, and hematologic disturbances such as neutropenia. Hemodialysis and peritoneal dialysis may enhance the elimination of zidovudine and its primary metabolite. In the event of a suspected overdose, contact a poison control center or emergency room immediately for advice.
Storage
Store Retrovir capsules and tablets at room temperature (15°-30°C or 59°-86°F) in a tightly closed container, away from light, moisture, and heat. The oral syrup may be stored at room temperature or refrigerated (2°-8°C or 36°-46°F). Do not freeze. Keep all medications out of the reach of children and pets. Safely discard any expired or unused medication.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The information provided is based on the product’s labeling but may not be exhaustive.
Reviews
“Retrovir was one of the first ARVs I prescribed in the early ’90s. While newer agents have different profiles, its role in combination therapy, especially in resource-limited settings, and its proven efficacy in PMTCT, remain invaluable. Monitoring for hematologic parameters is key to its safe long-term use.” – Infectious Disease Specialist, 25 years of experience.
“As a pharmacist, I appreciate the multiple formulations of Retrovir, which allow us to create appropriate regimens for a wide range of patients, from infants to adults. Its well-documented interaction profile allows for careful management within complex ART regimens.” – Clinical Pharmacist, HIV specialty.
“After my HIV diagnosis, my regimen included Retrovir. While I experienced some initial nausea, it subsided. It’s been a stable part of my cocktail for years, and my viral load has been undetectable. Knowing its long history of use gives me confidence.” – Patient, on therapy for 8 years.