抗病毒藥品
1. Treatment of acute herpes zoster (shingles), herpes labialis (cold sores), recurrent episodes of genital herpes in immunocompetent patients
2. Treatment of recurrent orolabial/genital (mucocutaneous) herpes simplex in adult patients with HIV
藥理
Antiviral Agent
Famciclovir undergoes rapid biotransformation to the active compound, penciclovir (prodrug), which is phosphorylated by viral thymidine kinase in HSV-1, HSV-2, and VZV-infected cells to a monophosphate form; this is then converted to penciclovir triphosphate and competes with deoxyguanosine triphosphate to inhibit HSV-2 polymerase, therefore, herpes viral DNA synthesis/replication is selectively inhibited.
藥動學
1. Metabolism: Famciclovir is rapidly deacetylated and oxidized to penciclovir
2. Bioavailability: (Penciclovir) 69% to 85%
3. Protein binding:<20%
4. Excretion: Urine (73% primarily as penciclovir)
5. Elimination half-life: (Penciclovir) 2-4 hours; prolonged in renal impairment
禁忌症
Known hypersensitivity to famciclovir, penciclovir or other constituents
Herpes simplex virus infection (Immunocompetent patients):
1. Recurrent: 1 g twice daily for 1 day or 500 mg as a single dose, followed by 250 mg twice daily for 2 days or 125 mg twice daily for 5 days
2. Suppressive (eg, for severe and/or frequent recurrences): 250 mg twice daily Herpes zoster (Immunocompetent patients):
500 mg every 8 hours for 7 days; 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
小兒調整劑量
腎功能調整劑量
1. CrCl ≥30 mL/min/1.73 m2: No dosage adjustment necessary
2. CrCl 10-29 mL/min/1.73 m2: 125 mg Q8H
3. Hemodialysis: 250 mg after each dialysis session (herpes zoster ); 125 mg after each dialysis session (genital HSV infection)
肝功能調整劑量
1. Mild-to-moderate impairment: No dosage adjustment is necessary
2. Severe impairment: No dosage adjustment provided (has not been studied); However, a 44% decrease in the Cmax of penciclovir (active metabolite) was noted in patients with mild-to-moderate impairment