DV
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DV (DV).
Nucleoside reverse transcriptase inhibitor; inhibits HIV-1 reverse transcriptase by competing with natural deoxynucleotides and causing chain termination after incorporation into viral DNA.
| Metabolism | Metabolized via intracellular phosphorylation to its active metabolite; not significantly metabolized by CYP450 enzymes. Renal elimination of unchanged drug via tubular secretion and glomerular filtration. |
| Excretion | Primarily renal excretion of unchanged drug (70-80%) and glucuronide conjugate (10-15%); biliary/fecal elimination accounts for approximately 5-10%. |
| Half-life | Terminal elimination half-life is 3-5 hours in healthy adults; prolonged to 10-20 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 98% bound primarily to albumin; minor binding to alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.2-0.3 L/kg, indicating distribution mainly in extracellular fluid. |
| Bioavailability | Oral: 75-85% (first-pass metabolism ~15-25%); Rectal: 50-60%; Intramuscular: 90-100%. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes; Intramuscular: 15-30 minutes. |
| Duration of Action | Oral: 4-6 hours; Intravenous: 2-4 hours; Intramuscular: 3-5 hours. |
2 mg/kg IV every 8 hours for 14 days; or 2 mg/kg IM every 8 hours for 14 days; or 1.5 mg/kg IV every 6 hours for 14 days.
| Dosage form | CREAM |
| Renal impairment | GFR >50 mL/min: no adjustment. GFR 30-50 mL/min: 2 mg/kg IV every 12 hours. GFR 10-29 mL/min: 2 mg/kg IV every 24 hours. GFR <10 mL/min: 2 mg/kg IV every 48 hours. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: reduce dose by 75%. |
| Pediatric use | Neonates: 2.5 mg/kg IV every 8 hours. Infants and children: 2 mg/kg IV every 6-8 hours. Maximum: 150 mg/day. |
| Geriatric use | No specific adjustment; monitor renal function and adjust based on creatinine clearance using Cockcroft-Gault equation. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DV (DV).
| Breastfeeding | Excreted in breast milk. M/P ratio not established. Due to potential for serious adverse reactions in nursing infants, contraindicated during breastfeeding. |
| Teratogenic Risk | FDA Category X. Contraindicated in pregnancy. First trimester: High risk of neural tube defects, cardiovascular malformations, and cleft palate. Second and third trimesters: Risk of fetal growth restriction, oligohydramnios, premature closure of ductus arteriosus, and neonatal persistent pulmonary hypertension. |
| Fetal Monitoring |
■ FDA Black Box Warning
Risk of lactic acidosis and severe hepatomegaly with steatosis, including fatal cases; post-treatment acute exacerbation of hepatitis B in co-infected patients.
| Serious Effects |
Hypersensitivity to drug or components; co-administration with drugs that compete for renal tubular secretion (e.g., emtricitabine, lamivudine).
| Precautions | Lactic acidosis and severe hepatomegaly; acute exacerbation of hepatitis B upon discontinuation; renal impairment; bone mineral density reduction; immune reconstitution syndrome; lipoatrophy. |
Loading safety data…
| For inadvertent exposure: serial fetal ultrasound for growth and anatomy, amniotic fluid index, and Doppler studies of ductus arteriosus. Maternal monitoring of renal function and blood pressure. |
| Fertility Effects | May impair female fertility by disrupting ovulation and menstrual cycle. In males, may reduce sperm count and motility. Reversible upon discontinuation. |