Distribution: Widely; CSF acyclovir concentration is ~50% of plasma concentrations.
Protein binding: 9% to 33%.
Metabolism: Converted by viral enzymes to acyclovir monophosphate, and further converted to diphosphate then triphosphate (active form) by cellular enzymes.
Excretion: Urine (62% to 91% as unchanged drug and metabolite).
禁忌症
Hypersensitivity to acyclovir, valacyclovir, or any component of the formulation.
懷孕分類
C; Acyclovir crosses the placenta.
哺乳分類
Acyclovir is present in breast milk.
副作用
>10%:
Hematologic & oncologic: Decreased hemoglobin (neonates: 13%), decrease in absolute neutrophil count (neonates: 3% to 16%).
1% to 10%:
Dermatologic: Pruritus (≤2%), skin rash (≤2%), urticaria (≤2%).
Gastrointestinal: Diarrhea (<1%), nausea (≤7%), vomiting (≤7%).
Hematologic & oncologic: Thrombocytopenia (<1%).
Hepatic: Increased serum bilirubin (4%), increased serum transaminases (1% to 2%).
Local: Inflammation at injection site (≤9%), injection site phlebitis (≤9%).
Nervous system: Headache (≤2%).
Renal: Increased blood urea nitrogen (5% to 10%), increased serum creatinine (5% to 10%).
劑量和給藥方法
1. Cytomegalovirus, prevention in low-risk allogeneic hematopoietic cell transplant recipients (alternative agent) (off-label use): IV: 500 mg/m2/dose every 8 hours for up to 4 weeks or until hospital discharge, followed by oral therapy.
2. Herpes simplex virus, central nervous system infection (encephalitis or meningitis):IV: 10 mg/kg/dose every 8 hours. Duration for encephalitis is 14 to 21 days and for meningitis is 10 to 14 days.
3. Herpes simplex virus, mucocutaneous infection: Genital: IV: 5 to 10 mg/kg/dose every 8 hours.
4. Herpes simplex virus, prevention in immunocompromised patients (off-label use): 250 mg/m2/dose every 12 hours.
5. Herpes zoster (shingles), treatment: Disseminated zoster (extensive cutaneous lesions or visceral involvement): IV: 10 mg/kg/dose every 8 hours.
6. Herpes zoster ophthalmicus (off-label use): IV: 10 mg/kg/dose every 8 hours for 7 days.
7. Varicella (chickenpox), treatment: Severe or complicated infection: IV: 10 mg/kg/dose every 8 hours for 7 to 10 days.
8. Varicella zoster virus, acute retinal necrosis (off-label use): IV: 10 mg/kg/dose every 8 hours for 10 to 14 days, followed by ~6 weeks of valacyclovir.
9. Varicella zoster virus, encephalitis (off-label use): IV: 10 mg/kg/dose every 8 hours.
小兒調整劑量
腎功能調整劑量
1. If the usual dose is 5 mg/kg/dose every 8 hours:
>50 mL/minute/1.73 m2: No dosage adjustment necessary.
25 to 50 mL/minute/1.73 m2: 5 mg/kg/dose every 12 hours.
10 to <25 mL/minute/1.73 m2: 5 mg/kg/dose every 24 hours.
<10 mL/minute/1.73 m2 (not on dialysis): 2.5 mg/kg/dose every 24 hours.
2. If the usual dose is 10 mg/kg/dose every 8 hours:
>50 mL/minute/1.73 m2: No dosage adjustment necessary.
25 to 50 mL/minute/1.73 m2: 10 mg/kg/dose every 12 hours.
10 to <25 mL/minute/1.73 m2: 10 mg/kg/dose every 24 hours.
<10 mL/minute/1.73 m2 (not on dialysis): 5 mg/kg/dose every 24 hours.