Brand Name
Retrovir
Generic Name
Zidovudine
View Brand Information FDA approval date: September 19, 2005
Classification: Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor
Form: Injection, Syrup, Tablet, Capsule, Solution
What is Retrovir (Zidovudine)?
Zidovudine tablets are a nucleoside analogue reverse transcriptase inhibitor indicated for: Treatment of Human Immunodeficiency Virus infection in combination with other antiretroviral agents.
Approved To Treat
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Brand Information
RETROVIR (zidovudine)
WARNING: RISK OF HEMATOLOGICAL TOXICITY, MYOPATHY, LACTIC ACIDOSIS AND SEVERE HEPATOMEGALY WITH STEATOSIS
RETROVIR (zidovudine) capsules, oral solution, and injection have been associated with hematologic toxicity including neutropenia and severe anemia, particularly in patients with advanced HIV-1 disease
Prolonged use of RETROVIR has been associated with symptomatic myopathy
Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues alone or in combination, including RETROVIR and other antiretrovirals. Suspend treatment if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity occur
1DOSAGE FORMS AND STRENGTHS
- RETROVIR capsules 100 mg (white, opaque cap and body) containing 100 mg zidovudine and printed with “Wellcome” and unicorn logo on cap and “Y9C” and “100” on body.
- RETROVIR oral solution (colorless to pale yellow, strawberry‑flavored) containing 10 mg zidovudine in each mL.
- RETROVIR injection is a clear, nearly colorless, sterile aqueous solution with a pH of approximately 5.5. Each vial contains 200 mg of zidovudine in 20 mL solution (10 mg per mL).
2CONTRAINDICATIONS
RETROVIR is contraindicated in patients who have had a potentially life-threatening hypersensitivity reaction (e.g., anaphylaxis, Stevens-Johnson syndrome) to any of the components of the formulations.
3ADVERSE REACTIONS
The following adverse reactions are discussed in greater detail in other sections of the labeling:
- Hematologic toxicity, including neutropenia and anemia
- Symptomatic myopathy
- Lactic acidosis and severe hepatomegaly with steatosis
- Hepatic decompensation in patients co-infected with HIV-1 and hepatitis C
3.1Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Adults
The frequency and severity of adverse reactions associated with the use of RETROVIR are greater in patients with more advanced infection at the time of initiation of therapy.
Table 3 summarizes adverse reactions reported at a statistically significant greater incidence for subjects receiving oral RETROVIR in a monotherapy trial.
In addition to the adverse reactions listed in
Selected laboratory abnormalities observed during a clinical trial of monotherapy with oral RETROVIR are shown in
The adverse reactions reported during IV administration of RETROVIR injection are similar to those reported with oral administration; neutropenia and anemia were reported most frequently. Long-term IV administration beyond 2 to 4 weeks has not been studied in adults and may enhance hematologic adverse reactions. Local reaction, pain, and slight irritation during IV administration occur infrequently.
Pediatrics
The clinical adverse reactions reported among adult recipients of RETROVIR may also occur in pediatric patients.
Trial ACTG 300: Selected clinical adverse reactions and physical findings with a greater than or equal to 5% frequency during therapy with EPIVIR (lamivudine) oral suspension 4 mg per kg twice daily plus RETROVIR 160 mg per m2 3 times daily compared with didanosine in therapy-naive (less than or equal to 56 days of antiretroviral therapy) pediatric subjects are listed in Table 5.
Selected laboratory abnormalities experienced by therapy-naive (less than or equal to 56 days of antiretroviral therapy) pediatric subjects are listed in
Macrocytosis was reported in the majority of pediatric subjects receiving RETROVIR 180 mg per m
Use for the Prevention of Maternal-Fetal Transmission of HIV-1
In a randomized, double-blind, placebo-controlled trial in HIV-1-infected women and their neonates conducted to determine the utility of RETROVIR for the prevention of maternal-fetal HIV-1 transmission, RETROVIR oral solution at 2 mg per kg was administered every 6 hours for 6 weeks to neonates beginning within 12 hours following birth. The most commonly reported adverse reactions were anemia (hemoglobin less than 9.0 g per dL) and neutropenia (less than 1,000 cells per mm
3.2Postmarketing Experience
The following adverse reactions have been identified during post-approval use of RETROVIR. Because these reactions are reported voluntarily from a population of unknown size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Body as a Whole
Back pain, chest pain, flu-like syndrome, generalized pain, redistribution/accumulation of body fat
Cardiovascular
Cardiomyopathy, syncope.
Eye
Macular edema.
Gastrointestinal
Constipation, dysphagia, flatulence, oral mucosa pigmentation, mouth ulcer.
General
Sensitization reactions including anaphylaxis and angioedema, vasculitis.
Hematologic
Aplastic anemia, hemolytic anemia, leukopenia, lymphadenopathy, pancytopenia with marrow hypoplasia, pure red cell aplasia.
Hepatobiliary
Hepatitis, hepatomegaly with steatosis, jaundice, lactic acidosis, pancreatitis.
Musculoskeletal
Increased CPK, increased LDH, muscle spasm, myopathy and myositis with pathological changes (similar to that produced by HIV-1 disease), rhabdomyolysis, tremor.
Nervous
Anxiety, confusion, depression, dizziness, loss of mental acuity, mania, paresthesia, seizures, somnolence, vertigo.
Reproductive System and Breast
Gynecomastia.
Respiratory
Dyspnea, rhinitis, sinusitis.
Skin and Subcutaneous Tissue
Changes in skin and nail pigmentation, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis, sweating, urticaria.
Special Senses
Amblyopia, hearing loss, photophobia, taste perversion.
Renal and Urinary
Urinary frequency, urinary hesitancy.
4OVERDOSAGE
Acute overdoses of zidovudine have been reported in pediatric patients and adults. These involved exposures up to 50 grams. No specific symptoms or signs have been identified following acute overdosage with zidovudine apart from those listed as adverse events such as fatigue, headache, vomiting, and occasional reports of hematological disturbances. Patients recovered without permanent sequelae. Hemodialysis and peritoneal dialysis appear to have a negligible effect on the removal of zidovudine while elimination of its primary metabolite, 3′-azido-3′-deoxy-5′-
5DESCRIPTION
RETROVIR is the brand name for zidovudine (formerly called azidothymidine [AZT]), a pyrimidine nucleoside analogue active against HIV-1. The chemical name of zidovudine is 3′-azido-3′-deoxythymidine; it has the following structural formula:
Zidovudine is a white to beige, odorless, crystalline solid with a molecular weight of 267.24 and a solubility of 20.1 mg per mL in water at 25°C. The molecular formula is C
RETROVIR capsules are for oral administration. Each capsule contains 100 mg of zidovudine and the inactive ingredients corn starch, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate. The 100-mg empty hard gelatin capsule, printed with edible black ink, consists of black iron oxide, dimethylpolysiloxane, gelatin, pharmaceutical shellac, soya lecithin, and titanium dioxide.
Each mL of RETROVIR oral solution contains 10 mg of zidovudine and the inactive ingredients sodium benzoate 0.2% (added as a preservative), citric acid, flavors, glycerin, and liquid sucrose. Sodium hydroxide may be added to adjust pH.
RETROVIR injection is a sterile solution for IV infusion only. Each mL contains 10 mg zidovudine in water for injection. Hydrochloric acid and/or sodium hydroxide may have been added to adjust the pH to approximately 5.5. RETROVIR injection contains no preservatives.
6CLINICAL STUDIES
Therapy with RETROVIR has been shown to prolong survival and decrease the incidence of opportunistic infections in patients with advanced HIV-1 disease and to delay disease progression in asymptomatic HIV-1-infected patients.
6.1Adults
Combination Therapy
RETROVIR in combination with other antiretroviral agents has been shown to be superior to monotherapy for one or more of the following endpoints: delaying death, delaying development of AIDS, increasing CD4+ cell counts, and decreasing plasma HIV-1 RNA.
The clinical efficacy of a combination regimen that includes RETROVIR was demonstrated in trial ACTG 320. This trial was a multi-center, randomized, double-blind, placebo-controlled trial that compared RETROVIR 600 mg per day plus EPIVIR 300 mg per day with RETROVIR plus EPIVIR plus indinavir 800 mg three times daily. The incidence of AIDS-defining events or death was lower in the triple-drug–containing arm compared with the 2-drug–containing arm (6.1% versus 10.9%, respectively).
Monotherapy
In controlled trials of treatment-naive subjects conducted between 1986 and 1989, monotherapy with RETROVIR, as compared with placebo, reduced the risk of HIV-1 disease progression, as assessed using endpoints that included the occurrence of HIV-1-related illnesses, AIDS-defining events, or death. These trials enrolled subjects with advanced disease (BW 002), and asymptomatic or mildly symptomatic disease in subjects with CD4+ cell counts between 200 and 500 cells per mm
6.2Pediatric Patients
ACTG 300 was a multi-center, randomized, double-blind trial that provided for comparison of EPIVIR plus RETROVIR to didanosine monotherapy. A total of 471 symptomatic, HIV-1-infected therapy-naive pediatric subjects were enrolled in these 2 treatment arms. The median age was 2.7 years (range: 6 weeks to 14 years), the mean baseline CD4+ cell count was 868 cells per mm
6.3Prevention of Maternal-Fetal HIV-1 Transmission
The utility of RETROVIR for the prevention of maternal-fetal HIV-1 transmission was demonstrated in a randomized, double-blind, placebo-controlled trial (ACTG 076) conducted in HIV-1-infected pregnant women with CD4+ cell counts of 200 to 1,818 cells per mm
7HOW SUPPLIED/STORAGE AND HANDLING
RETROVIR 100-mg capsules are supplied as white, opaque cap and body capsules containing 100 mg zidovudine per capsule. Each capsule is printed with “Wellcome” and unicorn logo on cap and “Y9C” and “100” on body.
Bottles of 100 (NDC 49702-211-20).
Store at 15° to 25°C (59° to 77°F) and protect from moisture.
RETROVIR oral solution is supplied as a colorless to pale yellow, strawberry-flavored solution containing 10 mg zidovudine in each mL.
Bottle of 240 mL (NDC 49702-212-48) with child-resistant cap.
Store at 15° to 25°C (59° to 77°F).
RETROVIR injection is a clear, colorless to slightly yellow aqueous solution. The strength of the presentation is 200 mg of zidovudine in 20 mL solution (10 mg per mL).
Single-dose vial (NDC 49702-213-01), Carton of 5 (NDC 49702-213-26).
Store vials at 15° to 25°C (59° to 77°F) and protect from light.
8PATIENT COUNSELING INFORMATION
Hypersensitivity Reactions
Inform patients that potentially life‑threatening hypersensitivity reactions (e.g., anaphylaxis, Stevens-Johnson syndrome) can occur while receiving RETROVIR. Instruct patients to immediately contact their healthcare provider if they develop rash, as it may be a sign of a more serious reaction. Advise patients that it is very important that they remain under a healthcare provider’s care during treatment with RETROVIR
Neutropenia and Anemia
Inform patients that the major toxicities of RETROVIR are neutropenia and/or anemia. The frequency and severity of these toxicities are greater in patients with more advanced disease and in those who initiate therapy later in the course of their infection. Advise patients that if toxicity develops, they may require transfusions or drug discontinuation. Advise patients of the extreme importance of having their blood counts followed closely while on therapy, especially for patients with advanced symptomatic HIV-1 disease
Myopathy
Inform patients that myopathy and myositis with pathological changes, similar to that produced by HIV-1 disease, have been associated with prolonged use of RETROVIR
Lactic Acidosis/Hepatomegaly with Steatosis
Advise patients that lactic acidosis and severe hepatomegaly with steatosis have been reported with use of nucleoside analogues and other antiretrovirals. Advise patients to stop taking RETROVIR if they develop clinical symptoms suggestive of lactic acidosis or pronounced hepatotoxicity
HIV-1/HCV Co-infection
Inform patients with HIV-1/HCV co-infection that hepatic decompensation (some fatal) has occurred in HIV-1/HCV co-infected patients receiving combination antiretroviral therapy for HIV-1 and interferon alfa with or without ribavirin
Immune Reconstitution Syndrome
Advise patients to inform their healthcare provider immediately of any signs and symptoms of infection as inflammation from previous infection may occur soon after combination antiretroviral therapy, including when RETROVIR is started
Lipoatrophy
Advise patients that loss of subcutaneous fat may occur in patients receiving RETROVIR and that they will be regularly assessed during therapy
Common Adverse Reactions
Inform patients that the most commonly reported adverse reactions in adult patients being treated with RETROVIR were headache, malaise, nausea, anorexia, and vomiting. The most commonly reported adverse reactions in pediatric patients receiving RETROVIR were fever, cough, and digestive disorders. Patients also should be encouraged to contact their physician if they experience muscle weakness, shortness of breath, symptoms of hepatitis or pancreatitis, or any other unexpected adverse events while being treated with RETROVIR
Drug Interactions
Advise patients that other medications may interact with RETROVIR and certain medications, including ganciclovir, interferon alfa, and ribavirin, may exacerbate the toxicity of RETROVIR
Dosage and Administration in Neonates
Due to the small volume of RETROVIR administered to neonates, advise caregivers to use an appropriate-sized syringe with 0.1-mL graduation to ensure accurate dosing of the oral solution formulation
Pregnancy
Inform pregnant women considering the use of RETROVIR during pregnancy for prevention of HIV-1 transmission to their infants that transmission may still occur in some cases despite therapy.
Pregnancy Registry
Advise patients that there is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to RETROVIR during pregnancy
Lactation
Instruct women with HIV-1 infection not to breastfeed because HIV-1 can be passed to the baby in the breast milk
Missed Dose
Instruct patients that if they miss a dose of RETROVIR, to take it as soon as they remember. Advise patients not to double their next dose or take more than the prescribed dose
EPIVIR and RETROVIR are trademarks owned by or licensed to the ViiV Healthcare group of companies.
Manufactured for:
ViiV Healthcare
Durham, NC 27701
©2024 ViiV Healthcare group of companies or its licensor.
RTR:13PI