pharmacopeia
GET
/api/v1/drug/zidovudine

Boxed warning

WARNING: RISK OF HEMATOLOGICAL TOXICITY, MYOPATHY, LACTIC ACIDOSIS AND SEVERE HEPATOMEGALY WITH STEATOSIS Zidovudine tablets have been associated with hematologic toxicity including neutropenia and severe anemia, particularly in patients with advanced HIV-1 disease [see Warnings and Precautions ( 5.1 )]. Prolonged use of zidovudine has been associated with symptomatic myopathy [see Warnings and Precautions ( 5.3 )]. Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues alone or in combination, including zidovudine and other antiretrovirals. Suspend treatment if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity occur [see Warnings and Precautions ( 5.4 )]. WARNING: RISK OF HEMATOLOGICAL TOXICITY, MYOPATHY, LACTIC ACIDOSIS AND SEVERE HEPATOMEGALY WITH STEATOSIS See full prescribing information for complete boxed warning. • Hematologic toxicity including neutropenia and severe anemia have been associated with the use of zidovudine. ( 5.1 ) • Symptomatic myopathy associated with prolonged use of zidovudine. ( 5.3 ) • Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported with the use of nucleoside analogues including zidovudine.

Mechanism of action

Sourced from openFDA

Zidovudine is an antiretroviral agent [see Microbiology ( 12.4 )].

Nucleoside Reverse Transcriptase

Indications

Sourced from openFDA
  • & USAGE Zidovudine tablets are a nucleoside analogue reverse transcriptase inhibitor indicated for: •Treatment of Human Immunodeficiency Virus (HIV-1) infection in combination with other antiretroviral agents. ( 1.1 ) • Prevention of maternal-fetal HIV-1 transmission.ICD-10: B20

Contraindications

Sourced from openFDA
  • Zidovudine tablets are 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. Hypersensitivity to zidovudine or any of the components (e.g., anaphylaxis, Stevens-Johnson syndrome).contraindicated

Dosage & administration

Sourced from openFDA

DOSAGE & ADMINISTRATION • Treatment of HIV-1 infection: Adults: Recommended oral dosage is 300 mg twice a day with other antiretroviral agents. ( 2.1 ) Pediatric patients (aged 4 weeks to less than 18 years): Dosage should be calculated based on body weight not to exceed adult dose. ( 2.2 ) • Prevention of maternal-fetal HIV-1 transmission: Specific dosage instructions for mother and infant. ( 2.3 ) • Patients with severe anemia and/or neutropenia: Dosage interruption may be necessary. ( 2.4 ) • Renal impairment: Recommended oral dosage in hemodialysis or peritoneal dialysis or in patients with creatinine clearance (CrCl) less than mL per minute is 100 mg every 6 to 8 hours. ( 2.5 ) 2.1 Adults - Treatment of HIV-1 Infection Oral Dosing The recommended oral dose of zidovudine is 300 mg twice daily in combination with other antiretroviral agents. 2.2 Pediatric Patients (Aged 4 Weeks to Less than 18 Years) Healthcare professionals should pay special attention to accurate calculation of the dose of zidovudine, transcription of the medication order, dispensing information, and dosing instructions to minimize risk for medication dosing errors. Prescribers should calculate the appropriate dose of zidovudine for each child based on body weight (kg) and should not exceed the recommended adult dose. Before prescribing zidovudine tablets, children should be assessed for the ability to swallow tablets. If a child is unable to reliably swallow a zidovudine tablet, the zidovudine syrup formulation should be prescribed.

Warnings & precautions

Sourced from openFDA

• See boxed warning for information about the following: hematologic toxicity, myopathy, and lactic acidosis and severe hepatomegaly ( 5.1 , 5.3 , 5.4 ) • Exacerbation of anemia has been reported in HIV-1/HCV co-infected patients receiving ribavirin and zidovudine. Coadministration of ribavirin and zidovudine is not advised. ( 5.5 ) • Hepatic decompensation, (some fatal), has occurred in HIV-1/HCV co-infected patients receiving combination antiretroviral therapy and interferon alfa with/without ribavirin. Discontinue zidovudine as medically appropriate and consider dose reduction or discontinuation of interferon alfa, ribavirin, or both. ( 5.5 ) • Immune reconstitution syndrome ( 5.6 ) and lipoatrophy ( 5.7 ) have been reported in patients treated with combination antiretroviral therapy. 5.1 Hematologic Toxicity/Bone Marrow Suppression Zidovudine should be used with caution in patients who have bone marrow compromise evidenced by granulocyte count less than 1,000 cells per mm 3 or hemoglobin less than 9.5 g per dL. Hematologic toxicities appear to be related to pretreatment bone marrow reserve and to dose and duration of therapy. In patients with advanced symptomatic HIV-1 disease, anemia and neutropenia were the most significant adverse events observed. In patients who experience hematologic toxicity, a reduction in hemoglobin may occur as early as 2 to 4 weeks, and neutropenia usually occurs after 6 to 8 weeks. There have been reports of pancytopenia associated with the use of zidovudine, which was reversible in most instances after discontinuance of the drug.

Adverse reactions

Sourced from openFDA

The following adverse reactions are discussed in greater detail in other sections of the labeling: • Hematologic toxicity, including neutropenia and anemia [see Boxed Warning, Warnings and Precautions ( 5.1 )]. • Symptomatic myopathy [see Boxed Warning, Warnings and Precautions ( 5.3 )]. • Lactic acidosis and severe hepatomegaly with steatosis [see Boxed Warning, Warnings and Precautions ( 5.4 )]. • Hepatic decompensation in patients co-infected with HIV-1 and hepatitis C [see Warnings and Precautions ( 5.5 )]. The following adverse reactions are discussed in greater detail in other sections of the labeling: • Hematologic toxicity, including neutropenia and anemia [see Boxed Warning, Warnings and Precautions ( 5.1 )]. • Symptomatic myopathy [see Boxed Warning, Warnings and Precautions ( 5.3 )]. • Lactic acidosis and severe hepatomegaly with steatosis [see Boxed Warning, Warnings and Precautions ( 5.4 )]. • Hepatic decompensation in patients co-infected with HIV-1 and hepatitis C [see Warnings and Precautions ( 5.5 )]. To report SUSPECTED ADVERSE REACTIONS, contact Hetero Labs Limited at 1-866-495-1995 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical 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.

Use in specific populations

Sourced from openFDA

• Lactation: Women infected with HIV should be instructed not to breastfeed due to potential for HIV transmission. ( 8.2 ) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to zidovudine during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Available data from the APR show no difference in the overall risk of birth defects for zidovudine compared with the background rate for birth defects of 2.7% in the Metropolitan Atlanta Congenital Defects Program (MACDP) reference population (see Data). The APR uses the MACDP as the U.S. reference population for birth defects in the general population. The MACDP evaluates women and infants from a limited geographic area and does not include outcomes for births that occurred at less than 20 weeks' gestation. The rate of miscarriage is not reported in the APR. The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15% to 20%. The background risk for major birth defects and miscarriage for the indicated population is unknown. Hyperlactatemia, which may be due to mitochondrial dysfunction, has been reported in infants with in utero exposure to zidovudine-containing products.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption and Bioavailability In adults, following oral administration, zidovudine is rapidly absorbed and extensively distributed, with peak serum concentrations occurring within 0.5 to 1.5 hours. The AUC was equivalent when zidovudine was administered as zidovudine tablets or syrup compared with zidovudine capsules.

Overdosage

Sourced from openFDA

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'-O-β-D-glucopyranuronosylthymidine (GZDV), is enhanced. If overdose occurs, the patient should be monitored for evidence of toxicity and given standard supportive treatment as required.

Approval history

Sourced from openFDA
  • Mar 19, 1987NDANDA019655Viiv Hlthcare
  • Sep 28, 1989NDANDA019910Viiv Hlthcare
  • Feb 2, 1990NDANDA019951Viiv Hlthcare
  • Sep 26, 1997NDANDA020857Viiv Hlthcare
  • Sep 19, 2005ANDAANDA077267Aurobindo
  • Sep 19, 2005ANDAANDA077268Aurobindo
  • Mar 27, 2006ANDAANDA078128Aurobindo Pharma Ltd
  • Apr 25, 2008ANDAANDA090092Hetero Labs Ltd Iii

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
19,864 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Foetal Exposure During Pregnancy2,63513%
  2. 2Drug Exposure During Pregnancy1,9309.7%
  3. 3Anaemia1,2796.4%
  4. 4Premature Baby9794.9%
  5. 5Virologic Failure9124.6%
  6. 6Pain8734.4%
  7. 7Exposure During Pregnancy8654.4%
  8. 8Maternal Exposure During Pregnancy8304.2%
  9. 9Anxiety8164.1%
  10. 10Drug Resistance7964.0%
  11. 11Emotional Distress7803.9%
  12. 12Pyrexia7343.7%
  13. 13Anhedonia7023.5%
  14. 14Viral Mutation Identified6583.3%
  15. 15Pathogen Resistance6573.3%

Literature

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Recent PubMed references pinned to Zidovudine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 522 ClinicalTrials.gov registrations naming Zidovudine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Zidovudine work?
Zidovudine is an antiretroviral agent [see Microbiology ( 12.4 )].
What is Zidovudine used for?
According to FDA labeling, Zidovudine carries indications including: & USAGE Zidovudine tablets are a nucleoside analogue reverse transcriptase inhibitor indicated for: •Treatment of Human Immunodeficiency Virus (HIV-1) infection in combination with other antiretroviral agents. ( 1.1 ) • Prevention of maternal-fetal HIV-1 transmission.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Zidovudine?
Zidovudine is classified as Nucleoside and nucleotide reverse transcriptase inhibitors, Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor, Nucleoside Reverse Transcriptase Inhibitors, Decreased Reverse Transcription to DNA.
What are the brand names for Zidovudine?
Zidovudine is marketed under brand names including Combivir, Retrovir, Trizivir.
What are the contraindications for Zidovudine?
Zidovudine labeling lists contraindications including: Zidovudine tablets are 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. Hypersensitivity to zidovudine or any of the components (e.g., anaphylaxis, Stevens-Johnson syndrome).. Always consult the full prescribing information and a clinician.
Note. Data for zidovudine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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