zidovudine (Rx)

Brand and Other Names:Retrovir, ZDV (formerly AZT)
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 100mg

tablet

  • 300mg

syrup

  • 50mg/5mL

injectable solution

  • 10mg/mL

HIV Infection Treatment

300 mg PO q12hr OR 200 mg PO q8hr (600 mg/day)

IV: 1 mg/kg/dose q4hr (6 times daily)

Prevention of Perinatal HIV Transmission

Indicated for prevention of maternal-fetal HIV-1 transmission

This indication is based on dosing regimens that includes antepartum and intrapartum therapy of HIV-1 infected mothers, and also postpartum therapy of HIV-1 exposed neonates

Instruct women to continue taking their antepartum combination PO antiretroviral agents (ART) on schedule as much as possible during labor and before scheduled cesarean delivery

Regardless of antepartum regimen or mode of delivery, administer by continuous IV infusion, near delivery in women with HIV RNA >1,000 copies/mL or unknown HIV RNA status; may also be considered in women with HIV RNA between 50 and 999 copies/mL

Discontinue intrapartum IV infusion if oral zidovudine was part of the antepartum regimen

Women receiving combination retroviral therapy with HIV RNA <50 copies/mL near delivery do not require zidovudine IV if there are no concerns related to adherence with oral ART regimen

IV administration (preferred)

  • During labor and delivery: 2 mg/kg loading dose followed by continuous IV infusion of 1 mg/kg/hr until umbilical cord clamped  
  • Scheduled cesarean delivery: Begin IV zidovudine 3 hr before surgery
  • Unscheduled cesarean delivery resulting from maternal or fetal complications: Consider administering loading dose then proceed to delivery

Oral administration (if IV not an option)

  • 600 mg loading dose followed by 400 mg orally every 3 hr

Dosage Modifications

Renal impairment (CrCl <15 mL/min; maintained on hemodialysis or peritoneal dialysis): 100 mg PO or 1 mg/kg IV q6-8 hr; alternatively 100 mg PO qDay or 300 mg/day PO

Renal impairment

  • CrCl ≥15 mL/min: Dose adjustment not necessary
  • CrCl <15 mL/min, hemodialysis, or peritoneal dialysis
    • Oral: 100 mg q6-8hr
    • IV: 1 mg/kg q6-8hr

Hepatic impairment

  • Primarily eliminated by hepatic metabolism and zidovudine concentrations appear to be increased in patients with impaired hepatic function
  • Frequent monitoring of hematologic toxicities advised
  • Data are insufficient to recommend dose adjustment

Dosing Considerations

Monitor: CBC with differential (monitor frequently in patients with poor bone marrow reserve), Hgb, serum creatinine, LFTs, HIV viral load and CD4

Anemia: (Hgb <7.5 g/dL or decline >25% from baseline) discontinue drug until recovery of marrow evident

Neutropenia: (granulocyte <750 cells/mm³ or decline >50% from baseline) discontinue drug until recovery of marrow evident

Dosage Forms & Strengths

capsule

  • 100mg

tablet

  • 300mg

syrup

  • 50mg/5mL

injectable solution

  • 10mg/mL

HIV Infection Treatment

Indicated for treatment of HIV infection in combination with other antiretroviral agents

Oral

  • GA ≥35 weeks
    • Birth to 4 weeks: 4 mg/kg PO BID
    • >4 weeks: 12 mg/kg PO BID
  • GA ≥30 to <35 weeks
    • Birth to 2 weeks: 2 mg/kg PO BID
    • 2 weeks: 3 mg/kg PO BID
    • >6-8 weeks: 12 mg/kg PO BID
  • GA <30 weeks
    • Birth to 4 weeks: 2 mg/kg PO BID
    • 4 to 8 weeks: 3 mg/kg PO BID
    • >8-10 weeks: 12 mg/kg PO BID
  • Infants born at or near term (GA ≥35 weeks)
    • 4 to <9 kg: 12 mg/kg PO BID
    • 9 to <30 kg: 9 mg/kg PO BID
    • ≥30 kg: 300 mg PO BID
  • Adolescents
    • 300 mg PO BID
  • Body surface area based dosing
    • 180-240 mg/m² PO BID

IV

  • GA ≥35 weeks
    • Birth to 4 weeks: 3 mg/kg IV BID
    • >4 weeks: 9 mg/kg IV BID
  • GA ≥30 to <35 weeks
    • Birth to 2 weeks: 1.5 mg/kg IV BID
    • 2-6 weeks: 2.3 mg/kg IV BID
    • >6-8 weeks: 9 mg/kg IV BID
  • GA <30 weeks
    • Birth to 4 weeks: 1.5 mg/kg IV BID
    • 4-8 weeks: 2.3 mg/kg IV BID
    • >8-10 weeks: 9 mg/kg IV BID
  • Infants ≥3 months
    • 120 mg/m²/dose IV q6h; not to exceed 160 mg/dose
  • Adolescents ≥30 kg
    • 1-2 mg/kg IV q4hr

HIV Perinatal Transmission Prevention

Indicated to prevent mother-to-child HIV transmission in all HIV-exposed infants

2 mg/kg PO q6hr or 1.5 mg/kg IV q6hr for 4-6 weeks as determined by risk  

Consultation is available from the National Perinatal HIV Hotline (888-448-8765)

Low risk of perinatal HIV transmission

  • Mother who received ART during pregnancy with sustained viral suppression near delivery and no concerns related to adherence
  • Give zidovudine for 4 weeks

Higher risk of perinatal HIV transmission

  • High risk includes
    • Mothers who received neither antepartum nor intrapartum ARV drugs
    • Mothers who received only intrapartum ARV drugs
    • Mothers who received antepartum and intrapartum ARV drugs, but who have detectable viral load near delivery, particularly if delivery was vaginal
    • Mothers with acute or primary HIV infection during pregnancy or breastfeeding (in which case, the mother should discontinue breastfeeding)
  • Neonatal ARV
    • 2-drug ARV prophylaxis with zidovudine for 6 weeks and 3 doses of nevirapine (prophylactic dosage given within 48 hr of birth, 48 hr after first dose, and 96 hr after second dose) OR
    • Empiric HIV therapy using either zidovudine, lamivudine, and nevirapine (treatment dosage) OR zidovudine, lamivudine, and raltegravir from birth to age 6 weeks

Presumed newborn HIV exposure

  • Mothers with unknown HIV status who test HIV positive at delivery or postpartum or whose newborns have a positive HIV antibody test
  • Neonatal ARV
    • ARV management as above (for higher risk of perinatal HIV transmission)
    • Discontinue neonate ARV treatment immediately if supplemental testing confirms that the mother does not have HIV

Newborn with HIV

  • Positive newborn HIV virologic test
  • Give 3-drug ARV regimen using treatment doses

Oral dosage as determined by gestational (GA in weeks) and birth age

  • GA <30 weeks
    • Birth to 4 weeks: 2 mg/kg PO BID  
    • >4 weeks: 3 mg/kg PO BID
  • GA ≥30 to <35 weeks
    • Birth to 2 weeks: 2 mg/kg PO BID  
    • >2 weeks: 3 mg/kg PO BID
  • GA ≥35 weeks
    • 4 mg/kg/dose PO BID  
  • Infants <6 weeks (GA≥35 weeks)
    • Mother received standard antiretroviral therapy during pregnancy, viral suppression was sustained, maternal adherence not a concern: 4-week course recommended
    • Intravenous weight based dosing: 2 mg/kg/dose q12hr

IV dosage as determined by gestational (GA in weeks) and birth age

  • GA <30 weeks
    • Birth to 4 weeks: 1.5 mg/kg IV BID
    • >4 weeks: 2.3 mg/kg IV BID
  • GA ≥30 to <35 weeks
    • Birth to 2 weeks: 1.5 mg/kg IV BID
    • >2 weeks: 2.3 mg/kg IV BID
  • GA ≥35 weeks
    • 3 mg/kg/dose IV BID
  • Infants born prematurely (GA<35 weeks)
    • Use neonate dosing; standard infant dosing may be excessive in infants who were born prematurely
  • Infants <6 weeks (GA≥35 weeks)
    • Mother received standard antiretroviral therapy during pregnancy, viral suppression was sustained, maternal adherence not a concern: 4-week course recommended
    • IV weight based dosing: 2 mg/kg/dose q12hr

Dosing Considerations

Monitor CBC, Hgb

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Interactions

Interaction Checker

and zidovudine

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            Contraindicated (1)

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              zidovudine, elvitegravir/cobicistat/emtricitabine/tenofovir DF. Other (see comment). Contraindicated. Comment: Elvitegravir/cobicistat/emtricitabine/tenofovir is a complete regimen for HIV and should not be administered with other antiretrovirals.

            Serious - Use Alternative (10)

            • cabotegravir

              zidovudine, cabotegravir. Other (see comment). Avoid or Use Alternate Drug. Comment: Cabotegravir plus rilpivirine is a complete regimen. Coadministration with other antiretroviral medications for treating HIV-1 infection is not recommended.

            • cidofovir

              cidofovir, zidovudine. Either increases levels of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: When cidofovir is administered concurrently with probenecid, zidovudine clearance may be decreased. Reduce dose of zidovudine by 50% on days of cidofovir/probenecid administration. .

            • clozapine

              clozapine, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Increased risk of myelosuppression.

            • deferiprone

              deferiprone, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.

            • ganciclovir

              ganciclovir increases toxicity of zidovudine by pharmacodynamic synergism. Contraindicated.

            • pretomanid

              pretomanid will increase the level or effect of zidovudine by Other (see comment). Avoid or Use Alternate Drug. In vitro studies demonstrated that pretomanid significantly inhibits OAT3; monitor for increased adverse effects and consider dosage reduction for OAT3 substrates.

            • ribavirin

              ribavirin decreases effects of zidovudine by Other (see comment). Avoid or Use Alternate Drug. Comment: Mechanism: Competition for thymidine kinase for conversion to active form.

            • ropeginterferon alfa 2b

              ropeginterferon alfa 2b, zidovudine. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.

            • stavudine

              zidovudine decreases effects of stavudine by Other (see comment). Contraindicated. Comment: Mechanism: Competition for thymidine kinase for conversion to active form.

            • valganciclovir

              valganciclovir increases toxicity of zidovudine by pharmacodynamic synergism. Contraindicated.

            Monitor Closely (54)

            • abacavir

              abacavir and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • acalabrutinib

              acalabrutinib, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may increase risk of myelosuppressive effects.

            • atazanavir

              atazanavir and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • azathioprine

              azathioprine, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • carboplatin

              carboplatin, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • cidofovir

              cidofovir, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • cisplatin

              cisplatin, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • clarithromycin

              clarithromycin increases toxicity of zidovudine by unknown mechanism. Use Caution/Monitor. Increased risk of myelosuppression.

              clarithromycin, zidovudine. Mechanism: unknown. Use Caution/Monitor. Clarithromycin may increase or decrease levels of zidovudine. Literature describes conflicting reports. Separate administration by minimum 2 to 4 hours. .

            • clofarabine

              clofarabine, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • conivaptan

              conivaptan increases levels of zidovudine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • dasatinib

              dasatinib, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • dexrazoxane

              dexrazoxane, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • doxorubicin

              zidovudine increases toxicity of doxorubicin by pharmacodynamic synergism. Use Caution/Monitor. Inreased risk of myelosuppression.

              doxorubicin decreases effects of zidovudine by Other (see comment). Use Caution/Monitor.

            • doxorubicin liposomal

              zidovudine increases toxicity of doxorubicin liposomal by pharmacodynamic synergism. Use Caution/Monitor. Inreased risk of myelosuppression.

              doxorubicin liposomal decreases effects of zidovudine by Other (see comment). Use Caution/Monitor. Comment: Concomitant administration of zidovudine and doxorubicin should be avoided since an antagonistic relationship has been demonstrated in vitro.

            • efavirenz

              efavirenz and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • emtricitabine

              emtricitabine and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • enfuvirtide

              enfuvirtide and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • fosamprenavir

              fosamprenavir and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • hydroxyurea

              hydroxyurea, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

              zidovudine, hydroxyurea. Other (see comment). Use Caution/Monitor. Comment: Combination may increase risk of myelosuppression.

            • ibritumomab tiuxetan

              ibritumomab tiuxetan, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • ifosfamide

              ifosfamide, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Ifosfamide may enhance the toxicities of myelosuppressive agents. Monitor for increased risk of myelosuppression.

            • imatinib

              imatinib, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • indinavir

              indinavir and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • interferon alfa 2b

              interferon alfa 2b increases levels of zidovudine by decreasing metabolism. Use Caution/Monitor.

            • interferon alfa n3

              interferon alfa n3 increases levels of zidovudine by decreasing metabolism. Use Caution/Monitor. Interferons may enhance potential for adverse effects. Patients should be monitored for signs and symptoms of increased myelosuppression and liver decompensation.

            • interferon beta 1a

              interferon beta 1a increases levels of zidovudine by decreasing renal clearance. Use Caution/Monitor. Interferons may enhance potential for adverse effects. Patients should be monitored for signs and symptoms of increased myelosuppression and liver decompensation.

            • interferon beta 1b

              interferon beta 1b increases levels of zidovudine by decreasing renal clearance. Use Caution/Monitor. Interferons may enhance potential for adverse effects. Patients should be monitored for signs and symptoms of increased myelosuppression and liver decompensation.

            • ketoconazole

              ketoconazole increases levels of zidovudine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • lamivudine

              lamivudine and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • lenalidomide

              lenalidomide, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • levoketoconazole

              levoketoconazole increases levels of zidovudine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • methotrexate

              methotrexate, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • mitomycin

              mitomycin, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • nelfinavir

              nelfinavir and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • nevirapine

              nevirapine and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • nirmatrelvir

              nirmatrelvir will decrease the level or effect of zidovudine by unknown mechanism. Use Caution/Monitor.

            • nirmatrelvir/ritonavir

              nirmatrelvir/ritonavir will decrease the level or effect of zidovudine by unknown mechanism. Use Caution/Monitor.

            • orlistat

              orlistat will decrease the level or effect of zidovudine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Loss of virological control reported in HIV-infected patients taking orlistat concomitantly. Exact mechanism is unclear, but may include a drug-drug interaction that inhibits systemic absorption of the antiretroviral drug. Monitor HIV RNA levels frequently and if increased HIV viral load confirmed, discontinue orlistat.

            • oxaliplatin

              oxaliplatin, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • peginterferon alfa 2b

              peginterferon alfa 2b will increase the level or effect of zidovudine by Other (see comment). Use Caution/Monitor. Interferons may enhance adverse effects of zidovudine including increased myelosuppression.

            • primaquine

              primaquine, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • probenecid

              probenecid increases levels of zidovudine by decreasing metabolism. Use Caution/Monitor.

            • rifabutin

              rifabutin will decrease the level or effect of zidovudine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rifampin

              rifampin decreases levels of zidovudine by increasing metabolism. Use Caution/Monitor.

            • ritonavir

              ritonavir and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • saquinavir

              saquinavir and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • stavudine

              stavudine and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • tenofovir DF

              tenofovir DF and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

            • thiotepa

              thiotepa, zidovudine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of myelosuppression.

            • tipranavir

              tipranavir and zidovudine both increase risk of immune reconstitution syndrome. Use Caution/Monitor.

              tipranavir decreases levels of zidovudine by unspecified interaction mechanism. Use Caution/Monitor.

            • tobramycin inhaled

              tobramycin inhaled and zidovudine both increase nephrotoxicity and/or ototoxicity. Modify Therapy/Monitor Closely. Avoid concurrent or sequential use to decrease risk for ototoxicity

            • tocilizumab

              tocilizumab decreases levels of zidovudine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Interaction applies to inflammatory conditions, such as rheumatoid arthritis, associated with increased levels of IL-6.

            • trimethoprim

              trimethoprim increases levels of zidovudine by decreasing renal clearance. Use Caution/Monitor. Potential for increased toxicity. .

            • valproic acid

              valproic acid increases levels of zidovudine by decreasing metabolism. Use Caution/Monitor. Potential for increased toxicity. .

            Minor (18)

            • amphotericin B deoxycholate

              zidovudine increases toxicity of amphotericin B deoxycholate by pharmacodynamic synergism. Minor/Significance Unknown.

            • black cohosh

              black cohosh increases toxicity of zidovudine by pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of hepatoxicity.

            • cyanocobalamin

              zidovudine decreases levels of cyanocobalamin by unspecified interaction mechanism. Minor/Significance Unknown.

            • dapsone

              zidovudine, dapsone. Either increases toxicity of the other by pharmacodynamic synergism. Minor/Significance Unknown. Increased bone marrow toxicity.

            • didanosine

              zidovudine increases levels of didanosine by decreasing renal clearance. Minor/Significance Unknown.

            • fluconazole

              fluconazole increases levels of zidovudine by decreasing metabolism. Minor/Significance Unknown.

            • flucytosine

              zidovudine increases toxicity of flucytosine by pharmacodynamic synergism. Minor/Significance Unknown.

            • food

              food decreases levels of zidovudine by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

            • kava

              kava increases toxicity of zidovudine by pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of hepatoxicity.

            • lamivudine

              lamivudine increases effects of zidovudine by pharmacodynamic synergism. Minor/Significance Unknown. Beneficial synergism.

            • methadone

              methadone increases levels of zidovudine by decreasing renal clearance. Minor/Significance Unknown.

            • pentamidine

              zidovudine increases toxicity of pentamidine by pharmacodynamic synergism. Minor/Significance Unknown.

            • pyrimethamine

              zidovudine, pyrimethamine. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased bone marrow toxicity.

            • sulfamethoxazole

              zidovudine increases toxicity of sulfamethoxazole by pharmacodynamic synergism. Minor/Significance Unknown.

              sulfamethoxazole increases levels of zidovudine by decreasing renal clearance. Minor/Significance Unknown.

            • valacyclovir

              valacyclovir increases effects of zidovudine by unknown mechanism. Minor/Significance Unknown. Monitor for lethargy and fatigue.

            • vinblastine

              zidovudine increases toxicity of vinblastine by pharmacodynamic synergism. Minor/Significance Unknown.

            • vincristine

              zidovudine increases toxicity of vincristine by pharmacodynamic synergism. Minor/Significance Unknown.

            • vincristine liposomal

              zidovudine increases toxicity of vincristine liposomal by pharmacodynamic synergism. Minor/Significance Unknown.

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            Adverse Effects

            >10%

            Anemia (23% in children)

            Anorexia (11%)

            Diarrhea (17%)

            Fever (16%)

            Granulocytopenia (39% in children)

            Headache, severe (42%)

            Leukopenia (39%)

            Nausea (46-61%)

            Pain (20%)

            Rash (17%)

            Vomiting (6-25%)

            Weakness (19%)

            1-10%

            Malaise (8%)

            Dizziness (6%)

            Insomnia (5%)

            Somnolence (8%)

            Hyperpigmentation of nails (bluish-brown)

            Dyspepsia (5%)

            Changes in platelet count

            Paresthesia (6%)

            Postmarketing Reports

            Reproductive System and Breast: Gynecomastia

            Skin and Subcutaneous Tissue: Changes in skin and nail pigmentation, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis, sweating, urticaria

            Renal and Urinary: Urinary frequency, urinary hesitancy

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            Warnings

            Black Box Warnings

            Neutropenia and severe anemia reported, particularly in patients with advanced HIV disease

            Myopathy associated with prolonged use

            Lactic acidosis and severe hepatomegaly with steatosis (including fatal cases) reported with use of nucleoside analogues alone or in combination

            Contraindications

            Hypersensitivity

            Cautions

            Vial stoppers for injection contain dry natural rubber (a latex derivative) which may cause allergic reactions in latex-sensitive individuals

            Risk of severe anemia and bone marrow depression; use with caution in patients with bone marrow compromise; hemoglobin reduction may occur 2-4 weeks and neutropenia may occur 6-8 weeks after initiating therapy; monitor blood counts; dose interruption may be required in patients who develop anemia or neutropenia

            Female sex and obesity may be risk factors for development of lactic acidosis and severe hepatomegaly with steatosis in patients treated with antiretroviral nucleoside analogues

            Monitor CBC with differentials (patients with poor bone marrow reserve require more frequent monitoring); perform CD4 count every 3-6 months; liver function tests recommended every 6-12 months

            (All NRTIs): Risk of potentially fatal lactic acidosis and severe hepatomegaly with steatosis when used alone or in combination with other antiretrovirals; suspend treatment in any patient who develops clinical or laboratory findings suggestive of lactic acidosis or hepatotoxicity (elevation of transaminase with or without hepatomegaly and steatosis may occur)

            Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs; further evaluation and treatment may be required; autoimmune disorders (such as Graves’ disease, polymyositis, and Guillain-Barré syndrome) reported to occur in setting of immune reconstitution; time to onset is more variable, and can occur many months after initiation of treatment

            Lipoatrophy, causing loss of subcutaneous fat, especially in the face and buttocks may occur; incidence and severity associated with cumulative exposure; may be only partially reversible improvement may take months or years after switching to regimen that does not contain zidovudine; monitor for signs of lipoatrophy and consider switching to non-zidovudine-containing regimen if lipoatrophy occurs

            Myopathy and myositis with pathological changes, similar to that produced by HIV-1 disease,associated with prolonged use of therapy

            Hematologic toxicity/ bone marrow suppression

            • Therapy should be used with caution in patients who have bone marrow compromise evidenced by granulocyte count < 1,000 cells per mm3 or hemoglobin < 9.5 g/dL
            • Hematologic toxicities appear to be related to pretreatment bone marrow reserve and to doseand 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 2-4 weeks, and neutropenia usually occurs after 6-8 weeks
            • There have been reports of pancytopenia, which was reversible in most instances after discontinuance of drug; however, significant anemia, in many cases requiring dose adjustment, discontinuation, and/or blood transfusions, has occurred during treatment with therapy alone or in combination with other antiretrovirals
            • Frequent blood counts are strongly recommended to detect severe anemia or neutropenia in patients with poor bone marrow reserve, particularly in patients with advanced HIV-1 disease who are treated with this medication
            • For HIV-1–infected individuals and patients with asymptomatic or early HIV-1 disease, periodic blood counts are recommended. If anemia or neutropenia develops, dosage interruption may be needed

            Drug interaction overview

            • Exacerbation of anemia due to ribavirin reported when zidovudine is part of HIV regimen; coadministration of ribavirin and zidovudine is not advised
            • Consideration should be given to replacing zidovudine in established combination HIV-1/HCV therapy, especially in patients with known history of zidovudine-induced anemia
            • 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
            • Patients receiving interferon alfa with or without ribavirin and zidovudine should be closely monitored for treatment-associated toxicities, especially hepatic decompensation, neutropenia, and anemia
            • Discontinuation of this medication should be considered medically appropriate; dose reduction or discontinuation of interferon alfa, ribavirin, or both should also be considered if worsening clinical toxicities are observed, including hepatic decompensation (eg, Child-Pugh >6)
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            Pregnancy & Lactation

            Pregnancy

            Available data from the APR show no difference in the overall risk of birth defects for lamivudine or zidovudine compared with background rate for birth defects of 2.7% in the Metropolitan Atlanta Congenital Defects Program (MACDP) reference population; APR uses the MACDP as the U.S. reference population for birth defects in the general population; 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; rate of miscarriage is not reported in the APR

            Hyperlactatemia, which may be due to mitochondrial dysfunction, reported in infants with in utero exposure to zidovudine-containing products; events were transient and asymptomatic in most cases; developmental delay, seizures, and other neurological disease also reported; a causal relationship between these events and exposure to zidovudine-containing products in utero or peri-partum not established

            Drug has been shown to cross placenta and concentrations in neonatal plasma at birth were essentially equal to those in maternal plasma at delivery; mild, transient elevations in serum lactate levels reported, which may be due to mitochondrial dysfunction, in neonates and infants exposed in utero or peri-partum to zidovudine-containing products; clinical relevance of transient elevations in serum lactate is unknown

            Lactation

            The Centers for Disease Control and Prevention recommend that HIV-1-infected mothers in the United States not breastfeed infants to avoid risking postnatal transmission of HIV-1 infection; lamivudine is present in human milk; there is no information on effects of lamivudine or zidovudine on breastfed infant or effects of drugs on milk production; because of potential for (1) HIV-1 transmission (in HIV-negative infants), (2)developing viral resistance (in HIV-positive infants), and (3) serious adverse reactions in a breastfed infant, instruct mothers not to breastfeed if they are receiving therapy

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Inhibits thymidine kinase

            Nucleoside Reverse Transcriptase Inhibitor (NRTI)

            Use with 3TC inhibits resistance

            Distribution

            Penetrates CNS well

            Protein binding: 25-38%

            Vd: 1-2.2 L/kg

            Metabolism

            Liver

            Elimination

            Half-life: 1 hr

            Excretion: Urine

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            Administration

            IV Preparation

            Dilute to not to exceed 4 mg/mL with D5W

            IV Administration

            Infuse over 1 hr

            Also given continuous infusion

            Do NOT give IVP or IM

            IV Incompatibilities

            Additive: Meropenem (may be dependent on meropenem concentration)

            Y-Site: Meropenem (may be dependent on meropenem concentration)

            IV Compatibilities

            Solution: D5W, NS

            Y-site (partial list): acyclovir, allopurinol, cefepime, clindamycin, dopamine, erythromycin, fluconazole, heparin, imipenem-cilastatin, linezolid, lorazepam, morphine, KCl, TMP-SMX, vancomycin

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            zidovudine oral
            -
            300 mg tablet
            zidovudine oral
            -
            100 mg capsule
            zidovudine oral
            -
            10 mg/mL syrup
            zidovudine oral
            -
            300 mg tablet
            Retrovir intravenous
            -
            10 mg/mL vial
            Retrovir intravenous
            -
            10 mg/mL vial
            Retrovir oral
            -
            10 mg/mL syrup
            Retrovir oral
            -
            100 mg capsule
            Retrovir oral
            -
            100 mg capsule

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Select a drug:
            Patient Education
            zidovudine oral

            ZIDOVUDINE (AZT) - ORAL

            (zye-DOE-vue-deen)

            COMMON BRAND NAME(S): Retrovir

            WARNING: Zidovudine has caused severe blood problems including a decrease in red blood cells (anemia) and white blood cells (neutropenia). They occur more frequently in people with advanced HIV disease (AIDS). Blood problems may require blood transfusions or stopping your medication. Your doctor will order blood tests to monitor for this. Keep all medical appointments. Seek immediate medical attention if you develop signs of anemia (unusual tiredness, breathing problems, weakness, bluish fingernails/lips, pale skin, fast heartbeat). Low white blood cells can make you more likely to get serious (sometimes fatal) infections. Get medical help right away if you develop signs of infection such as cough that doesn't go away, fever, chills, breathing problems, or sore throat.This medication may also cause muscle problems (myopathy). Seek immediate medical attention if you develop symptoms of myopathy (such as wasting or decrease in muscle size, muscle weakness/pain/tenderness, weight loss).Rarely, zidovudine has caused severe (sometimes fatal) liver problems and a certain metabolic problem (lactic acidosis). Tell your doctor right away if you develop symptoms of liver problems (such as nausea that doesn't go away, stomach/abdominal pain, dark urine, yellowing eyes/skin) or lactic acidosis (such as rapid breathing, drowsiness, muscle aches). These serious side effects may occur more often in women and obese patients.

            USES: This drug is used with other HIV medications to help control HIV infection. It helps to decrease the amount of HIV in your body so your immune system can work better. This lowers your chance of getting HIV complications (such as new infections, cancer) and improves your quality of life. Zidovudine belongs to a class of drugs known as nucleoside reverse transcriptase inhibitors-NRTIs.Zidovudine is used in pregnant women to prevent passing the HIV virus to the unborn baby. This medication is also used in newborns born to mothers infected with HIV to prevent infection in the newborns.Zidovudine is not a cure for HIV infection. To decrease your risk of spreading HIV disease to others, continue to take all HIV medications exactly as prescribed by your doctor. Use an effective barrier method (latex or polyurethane condoms/dental dams) during sexual activity as directed by your doctor. Do not share personal items (such as needles/syringes, toothbrushes, and razors) that may have contacted blood or other body fluids. Consult your doctor or pharmacist for more details.

            HOW TO USE: Take this medication by mouth with or without food as directed by your doctor, usually 2 to 3 times daily. Take this medication with a full glass of water (8 ounces/240 milliliters) unless your doctor directs you otherwise. If you are using the liquid form of this medication, carefully measure the dose using a special measuring device/spoon. Do not use a household spoon because you may not get the correct dose.The dosage is based on your medical condition and response to treatment. For children, the dosage is also based on weight. Pregnant women may need to take this medication 5 times a day. Newborns are usually given the liquid form every 6 hours for 6 weeks after birth to prevent infection.Take this medication 2 hours before or after taking clarithromycin. Clarithromycin may prevent your body from fully absorbing zidovudine.For the best effect, take this medication at evenly spaced times. To help you remember, take this medication at the same times every day.It is very important to continue taking this medication (and other HIV medications) exactly as prescribed by your doctor. Do not skip any doses. Refill your medication before you run out.Do not take more or less of this drug than prescribed or stop taking it (or other HIV medicines) even for a short time unless directed to do so by your doctor. Skipping or changing your dose without approval from your doctor may cause the amount of virus to increase, make the infection more difficult to treat (resistant), or worsen side effects.

            SIDE EFFECTS: See also Warning section.Headache, nausea, vomiting, trouble sleeping, or loss of appetite may occur. If any of these effects last or get worse, notify your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.As your immune system gets stronger, it can begin to fight off infections you already had, possibly causing disease symptoms to come back. You could also have symptoms if your immune system becomes overactive. This reaction may happen at any time (soon after starting HIV treatment or many months later). Get medical help right away if you have any serious symptoms, including: unexplained weight loss, severe tiredness, muscle aches/weakness that doesn't go away, headaches that are severe or don't go away, joint pain, numbness/tingling of the hands/feet/arms/legs, vision changes, signs of infection (such as fever, chills, swollen lymph nodes, trouble breathing, cough, non-healing skin sores), signs of an overactive thyroid (such as irritability, nervousness, heat intolerance, fast/pounding/irregular heartbeat, bulging eyes, unusual growth in the neck/thyroid known as a goiter), signs of a certain nerve problem known as Guillain-Barre syndrome (such as unsteadiness, loss of coordination, trouble swallowing/speaking/chewing, trouble moving your eyes).Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as depression, anxiety, confusion), easy bruising/bleeding, skin/fingernail color changes.Get medical help right away if you have any very serious side effects, including: seizures.Loss of body fat (such as in the face, arms, legs, and buttocks) may occur while you are taking this medication. This effect may be permanent. Tell your doctor right away if you notice any changes in body fat.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: Before taking zidovudine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney problems, liver problems (such as hepatitis B or C, cirrhosis), alcohol use, low red/white blood cells.Liquid products may contain sugar. Caution is advised if you have diabetes or any other condition that requires you to limit sugar in your diet. Ask your doctor or pharmacist about using this product safely.Before having surgery, tell your doctors or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Tell your doctor if you are pregnant before using this medication. Treatment can lower the risk of passing HIV infection to your baby. Discuss the risks and benefits with your doctor.This medication passes into breast milk. Because breast milk can transmit HIV, do not breast-feed.

            DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: orlistat, probenecid, ribavirin, stavudine, drugs that may suppress bone marrow function (such as ganciclovir, dapsone, trimethoprim, chemotherapy including doxorubicin, vincristine).Other medications can affect the removal of zidovudine from your body, thereby affecting how zidovudine works. These drugs include methadone, rifampin, and some drugs used to treat seizures (such as phenytoin, valproic acid). This is not a complete list.This medication must not be taken with other medications that contain zidovudine. Check the labels on all your other prescription medications to make sure they do not contain zidovudine. If you have any questions, consult your doctor or pharmacist.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include extreme drowsiness/tiredness, confusion, seizures.

            NOTES: Do not share this medication with others.Lab and/or medical tests (such as blood counts, liver tests, viral load, T-cell counts) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.

            MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            Information last revised May 2022. Copyright(c) 2022 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.