Brand and Other Names:Retrovir, ZDV (formerly AZT)
- Classes: HIV, NRTIs
Dosing & Uses
Dosage Forms & Strengths
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
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
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
Reduction in daily dose or extension of dosing interval may be necessary
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
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
HIV Perinatal Transmission Prevention
Indicated to prevent mother-to-child HIV transmission in all HIV-exposed infants
NIH perinatal guidelines (July 2012)
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
Serious - Use Alternative
Significant - Monitor Closely
Anemia (23% in children)
Granulocytopenia (39% in children)
Headache, severe (42%)
Hyperpigmentation of nails (bluish-brown)
Changes in platelet count
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
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
Pregnancy & Lactation
Pregnancy Category: C
Lactation: HIV+ women are advised not to breastfeed
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.
Mechanism of Action
Inhibits thymidine kinase
Nucleoside Reverse Transcriptase Inhibitor (NRTI)
Use with 3TC inhibits resistance
Distribution: Penetrates CNS well
Half-Life: 1 hr
Vd: 1-2.2 L/kg
Protein binding: 25-38%
Dilute to not to exceed 4 mg/mL w/ D5W
Infuse over 1 hr
Also given continuous infusion
Do NOT give IVP or IM
Additive: Meropenem (may be dependent on meropenem concentration)
Y-Site: Meropenem (may be dependent on meropenem concentration)
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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