抗病毒藥品
1. Initial and recurrent episodes of genital herpes
2. Acute treatment of herpes zoster (shingles)
3. Treatment of varicella (chickenpox)
藥理
Antiviral Agent
藥動學
Absorption:
1. Poorly absorbed; absorption improves with multiple small doses compared to one large daily dose
2. Bioavailability: 10% to 20% with normal renal function (bioavailability decreases with increased dose) Distribution:
1. Widely (eg, brain, kidney, lungs, liver, spleen, muscle, uterus, vagina, CSF); CSF acyclovir concentration is ~50% of plasma concentrations
2. 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
Acyclovir has been shown to cross the human placenta
Herpes zoster (shingles):
800 mg 5 times daily for 7 days, Initiate at earliest sign or symptom; treatment is most effective when initiated ≤72 hours after rash onset, but may initiate treatment >72 hours after rash onset if new lesions are continuing to appear Varicella (chickenpox):
800 mg 5 times daily for >5 to 7 days and until all lesions have crusted
小兒調整劑量
Herpes zoster (shingles):
800 mg every 4 hours (5 doses per day) for 5 to 7 days Varicella (chickenpox):
20 mg/kg/dose 4 times daily for 5 days; maximum 3,200 mg/day
腎功能調整劑量
1. If the usual dose is 400 mg every 12 hours or 200 mg 5 times daily:
(1) CrCl >25: No dosage adjustment necessary
(2) CrCl 10-25: No dosage adjustment necessary or reduce to 200 mg Q12H
(3) CrCl<10: 200 mg Q12H
2. If the usual dose is 800 mg 5 times daily:
(1) CrCl >25: No dosage adjustment necessary.
(2) CrCl 10-25: 800 mg Q8H
(3) CrCl<10: 200 mg every 12 hours or 400 mg every 12 hours
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling; use caution in patients with severe impairment.