Yes

Antiviral Agent

Dental: Treatment of initial and prophylaxis of recurrent mucosal and cutaneous herpes simplex (HSV-1 and HSV-2) infections

Medical: Treatment of initial and prophylaxis of recurrent mucosal and cutaneous herpes simplex (HSV-1 and HSV-2) infections; herpes simplex encephalitis; herpes zoster; genital herpes infection; varicella-zoster infections in healthy, nonpregnant persons >13 years of age, children >12 months of age who have a chronic skin or lung disorder or are receiving long-term aspirin therapy, and immunocompromised patients; for herpes zoster, acyclovir should be started within 72 hours of the appearance of the rash to be effective; acyclovir will not prevent postherpetic neuralgias

C

Hypersensitivity to acyclovir, valacyclovir, or any component

Use with caution in patients with pre-existing renal disease or in those receiving other nephrotoxic drugs concurrently; maintain adequate urine output during the first 2 hours after I.V. infusion; use with caution in patients with underlying neurologic abnormalities, serious hepatic or electrolyte abnormalities, or substantial hypoxia. Use with caution in immunocompromised patients; thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS) has been reported

>10%: Local: Inflammation at injection site

1% to 10%:

Central nervous system: Lethargy, dizziness, seizures, confusion, agitation, coma, headache

Dermatologic: Rash

Gastrointestinal: Nausea, vomiting

Neuromuscular & skeletal: Tremor

Renal: Impaired renal function

<1%: Mental depression, insomnia, anorexia, elevated LFT, sore throat, hallucinations, leukopenia, thrombocytopenia, anemia, anaphylaxis, agitation, delirium, seizures, psychosis, somnolence, thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS), diarrhea, hepatitis, jaundice, myalgia, alopecia, erythema multiforme, photosensitization, pruritus, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria, visual disturbances, renal failure, increased BUN, increased serum creatinine, hematuria

Symptoms of overdose include seizures, somnolence, confusion, elevated serum creatinine, and renal failure

In the event of an overdose, sufficient urine flow must be maintained to avoid drug precipitation within the renal tubules. Hemodialysis has resulted in up to 60% reductions in serum acyclovir levels.

Increased CNS side effects with zidovudine and probenecid

Incompatible with blood products and protein-containing solutions; reconstituted solutions remain stable for 24 hours at room temperature; do not refrigerate reconstituted solutions as they may precipitate; in patients who require fluid restriction, a concentration of up to 10 mg/mL has been infused, however, concentrations >10 mg/mL (usual recommended concentration: <7 mg/mL in D₅W) increase the risk of phlebitis

Acyclovir is converted to acyclovir monophosphate by virus-specific thymidine kinase then further converted to acyclovir triphosphate by other cellular enzymes. Acyclovir triphosphate inhibits DNA synthesis and viral replication by competing with deoxyguanosine triphosphate for viral DNA polymerase and being incorporated into viral DNA.

Absorption: Oral: 15% to 30%; food does not appear to affect absorption

Distribution: Widely distributed throughout the body including brain, kidney, lungs, liver, spleen, muscle, uterus, vagina, and CSF

Protein binding: <30%

Metabolism: Small amount of hepatic metabolism

Half-life, terminal phase: Neonates: 4 hours; Children 1-12 years: 2-3 hours; Adults: 3 hours

Time to peak serum concentration: Oral: Within 1.5-2 hours; I.V.: Within 1 hour

Elimination: Primary route is the kidney (30% to 90% of a dose excreted unchanged); hemodialysis removes ~60% of the dose while removal by peritoneal dialysis is to a much lesser extent (supplemental dose recommended)

Dosing weight should be based on the smaller of lean body weight or total body weight

Treatment of herpes simplex virus infections: Children >12 years and Adults: I.V.:

Mucocutaneous HSV or severe initial herpes genitalis infection: 750 mg/m²/day divided every 8 hours or 5 mg/kg/dose every 8 hours for 5-10 days

HSV encephalitis: 1500 mg/m²/day divided every 8 hours or 10 mg/kg/dose for 10 days

Treatment of genital herpes simplex virus infections: Adults:

Oral: 200 mg every 4 hours while awake (5 times/day) for 10 days if initial episode; for 5 days if recurrence (begin at earliest signs of disease)

Topical: 1/2 " ribbon of ointment for a 4" square surface area every 3 hours (6 times/day)

Treatment of varicella-zoster virus (chickenpox) infections:

Oral:

Children: 10-20 mg/kg/dose (up to 800 mg) 4 times/day for 5 days; begin treatment within the first 24 hours of rash onset

Adults: 600-800 mg/dose every 4 hours while awake (5 times/day) for 7-10 days or 1000 mg every 6 hours for 5 days

I.V.: Children and Adults: 1500 mg/m²/day divided every 8 hours or 10 mg/kg/dose every 8 hours for 7 days

Treatment of herpes zoster (shingles) infections:

Oral:

Children (immunocompromised): 250-600 mg/m²/dose 4-5 times/day for 7-10 days

Adults (immunocompromised): 800 mg every 4 hours (5 times/day) for 7-10 days

I.V.:

Children and Adults (immunocompromised): 10 mg/kg/dose or 500 mg/m²/dose every 8 hours

Older Adults (immunocompromised): 7.5 mg/kg/dose every 8 hours

If nephrotoxicity occurs: 5 mg/kg/dose every 8 hours

Prophylaxis in immunocompromised patients:

Varicella zoster or herpes zoster in HIV-positive patients: Adults: Oral: 400 mg every 4 hours (5 times/day) for 7-10 days

Bone marrow transplant recipients: Children and Adults: I.V.:

Allogeneic patients who are HSV seropositive: 150 mg/m²/dose (5 mg/kg) every 12 hours; with clinical symptoms of herpes simplex: 150 mg/m²/dose every 8 hours

Allogeneic patients who are CMV seropositive: 500 mg/m²/dose (10 mg/kg) every 8 hours; for clinically symptomatic CMV infection, consider replacing acyclovir with ganciclovir

Chronic suppressive therapy for recurrent genital herpes simplex virus infections: Adults: 200 mg 3-4 times/day or 400 mg twice daily for up to 12 months, followed by re-evaluation

Dosing adjustment in renal impairment:

Oral: HSV/varicella-zoster:

Cl_cr 10-25 mL/minute: Administer dose every 8 hours

Cl_cr <10 mL/minute: Administer dose every 12 hours

I.V.:

Cl_cr 25-50 mL/minute: 5-10 mg/kg/dose: Administer every 12 hours

Cl_cr 10-25 mL/minute: 5-10 mg/kg/dose: Administer every 24 hours

Cl_cr <10 mL/minute: 2.5-5 mg/kg/dose: Administer every 24 hours

Hemodialysis: Dialyzable (50% to 100%); administer dose postdialysis

Peritoneal dialysis: Dose as for Cl_cr <10 mL/minute

Continuous arteriovenous or venovenous hemofiltration (CAVH/CAVHD) effects: Dose as for Cl_cr <10 mL/minute

May be taken with food; food does not appear to affect absorption

Urinalysis, BUN, serum creatinine, liver enzymes, CBC

May see lethargy, confusion, or agitation; rarely may see depression or insomnia

Usually not a problem, may see additive sedation with sedating psychotropics

No information available to require special precautions

No effects or complications reported

This is not a cure for herpes (recurrences tend to appear within 3 months of original infection), nor will this medication reduce the risk of transmission to others when lesions are present. Take as directed for full course of therapy; do not discontinue even if feeling better. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake) to prevent renal complications. Avoid use of other topical creams, lotions, or ointments unless approved by prescriber. You may experience nausea or vomiting (small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); lightheadedness or dizziness (use caution when driving or engaging in tasks that require alertness until response to drug is known); headache, fever, muscle pain (an analgesic may be recommended). Report persistent lethargy, acute headache, severe nausea or vomiting, confusion or hallucinations, rash, or difficulty breathing. Pregnancy precautions: Inform prescriber if you are or intend to be pregnant.

Wear gloves when applying ointment for self-protection

Capsule: 200 mg

Powder for Injection: 500 mg (10 mL); 1000 mg (20 mL)

Ointment, topical: 5% [50 mg/g] (3 g, 15 g)

Suspension, oral (banana flavor): 200 mg/5 mL

Tablet: 400 mg, 800 mg

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