Antiviral drugs are used for a variety of infections, including herpes, hepatitis B and C, and influenza. Human immunodeficiency virus (HIV) infection was first reported in 1981. The search for effective anti-HIV treatment began in 1987 with zidovudine (AZT) as a single-agent regimen. In 1994, the first protease inhibitor, saquinavir, was introduced. More agents and different classes of antiretroviral agents were developed later (Table II–12).
Table II-12 Antiviral and Antiretroviral Drugs |Favorite Table|Download (.pdf)
Table II-12 Antiviral and Antiretroviral Drugs
Toxic Dose or Serum Level
High-dose chronic therapy has caused crystalluria and renal failure, leukopenia. Coma, seizures, renal failure after large acute overdoses. Hallucinations and confusion after IV administration.
16.3 and 17.4 mg/kg (case reports)
No renal dysfunction after treatment with probenecid and IV hydration.
Headache, nasopharyngitis, cough, pyrexia, upper abdominal pain, fatigue, diarrhea, lactic acidosis, hepatomegaly.
Prodrug metabolized to active penciclovir.
1.14–8 times recommended dose (average, 4 times)
Seizures, renal impairment. One patient had seizures and died after receiving 12.5 g daily for 3 days.
3.5 h (IV)
4.8 h (oral)
Adults: 5–7 g or 25 mg/kg IV
Neutropenia, thrombocytopenia, pancytopenia, increased serum creatinine; 9 mg/kg IV caused a seizure; 10 mg/kg IV daily caused hepatitis.
Children: 1 g instead of 31 mg in a 21-month-old had no toxic effect; an 18-month-old received 60 mg/kg IV, was treated with exchange transfusion, and had no effect; a 4-month-old received 500 mg, was treated with peritoneal dialysis, and had no effect; 40 mg in a 2-kg infant caused hepatitis.
Extensive intracellular metabolism.
Up to 20 g acute ingestion
Hemolytic anemia, neutropenia, thrombocytopenia; suicidal ideation.
15–30 mg/kg IV
Reversible bone marrow toxicity reported after 3–5 courses of IV treatment. Systemic absorption is negligible after ophthalmic instillation. Ingestion of contents of one bottle (7.5 mL, 75 mg) unlikely to cause any adverse effects.
Prodrug promptly converted to acyclovir.
Rapidly converted to ganciclovir.
Rapid deamination to ara-hypoxanthine metabolite, whose half-life is 2.4–3.3 h
Chronic 1–20 mg/kg/d IV for 10–15 d
Nausea, vomiting, diarrhea, dizziness, ataxia, tremor, confusion, hallucinations, psychosis; decreased Hct, Hgb, WBC, platelets; increased AST, ALT, LDH. Poorly absorbed orally; no toxicity expected if one tube (3.5 g, 105 mg) ingested.
Nucleoside (NRTIs) or nucleotide (NtRTIs) reverse transcriptase inhibitors
Lactic acidosis, mitochondrial toxicity, hepatotoxicity.
1.54 ± 0.63 h
Diarrhea, nausea, vomiting; hypersensitivity (fatal reactions reported); perioral paresthesias.
1.5 ± 0.4 h
Diarrhea, pancreatitis, peripheral neuropathy, salt overload with buffered product.
Lactic acidosis and severe hepatomegaly with steatosis.
1.15 h IV
1.44 h PO
Hepatic steatosis, lactic acidosis, ...