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zidovudine (Rx)Brand and Other Names:Retrovir, ZDV (formerly AZT)

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 100mg

tablet

  • 300mg

syrup

  • 50mg/5mL

injectable solution

  • 10mg/mL
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HIV Infection

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

IV: 1 mg/kg/dose 5-6x/day

Maternal Dosing to Prevent Fetal HIV Transmission

FDA-approved regimen

  • 100 mg PO 5x/day until start of labor, in combination with other ART agents
  • During labor and delivery: 2 mg/kg IV over 1 hr, THEN
  • 1 mg/kg/hr IV continuous infusion until umbilical cord clamping 

NIH perinatal guidelines

  • Indicated during labor and delivery for women who have received antepartum ART and their HIV RNA levels are >400 copies/mL, or in women who have not received antepartum ART
  • 2 mg/kg IV loading dose infused over 1 hr, THEN 1 mg/kg/hr until umbilical cord clamping 
  • Women who have received antepartum ART and their HIV RNA levels are <400 copies/mL do not require IV zidovudine
  • IV would be preferred to oral administration in the United States; in situations where IV administration is not possible, oral administration can be considered

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

Hepatic Impairment

Reduction in daily dose or extension of dosing interval may be necessary

Administration

Monitor: CBC, Hgb

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
more...

HIV Infection, Treatment

4 weeks-18 years

240 mg/m² PO q12hr or 160 mg/m² PO q8hr, OR use mg/kg dosing

4 to <9 kg: 12 mg/kg PO q12hr or 8 mg/kg PO TID

≥ 9 to <30 kg: 9 mg/kg PO q12hr or 6 mg/kg PO TID

≥30 kg: 300 mg PO q12hr or 200 mg PO TID

IV intermittent infusion: 120 mg/m² IV q6h

IV continuous infusion: 20 mg/m²/hr IV 

HIV Perinatal Transmission Prevention

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

FDA approved regimen

  • 2 mg/kg PO q6hr or 1.5 mg/kg IV q6hr 

NIH perinatal guidelines (July 2012)

  • <30 weeks’ gestation: 2 mg/kg PO or 1.5 mg/kg IV BID; after age 4 weeks, advance to 3 mg/kg PO or 2.3 mg/kg IV q12hr 
  • ≥30 to <35 weeks’ gestation: 2 mg/kg PO BID; after age 15 days, advance to 3 mg/kg PO or 2.3 mg/kg IV q12hr
  • ≥35 weeks’ gestation: 4 mg/kg PO or 3 mg/kg IV BID x6 weeks

Administration, perinatal transmission prevention

  • Initiate as soon after delivery as possible (preferably within 6-12 hr) and continue through age 6 weeks
  • If IV administered, infuse over 30 minutes
  • Additional antiretroviral prophylaxis needed (ie, nevirapine) for HIV-exposed infants of women who received no antepartum ART prophylaxis

Monitoring

CBC, Hgb

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Interactions

Interaction Checker

zidovudine and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            Sort by :  
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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%)

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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

            Risk of severe anemia & bone marrow depression

            Monitor CBC with differentials qMonth x2, then q1-3month; LFTs q6-12week

            (All NRTIs): Risk of potentially fatal lactic acidosis & severe hepatomegaly with steatosis when used alone or in combination with other antiretrovirals

            Risk of immune reconstitution syndrome if used in combination w/ other antiretroviral drugs

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: HIV+ women are advised not to breastfeed

            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

            Pharmacokinetics

            Distribution: Penetrates CNS well

            Half-Life: 1 hr

            Vd: 1-2.2 L/kg

            Protein binding: 25-38%

            Metabolism: Liver

            Excretion: Urine

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            Administration

            IV Preparation

            Dilute to not to exceed 4 mg/mL w/ 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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            Formulary

            FormularyPatient Discounts

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            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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