Trade Names:Acyclovir- Injection 50 mg/mL (as sodium)- Powder for injection 500 mg/vial (as sodium)- Powder for injection 1,000 mg/vial (as sodium)
Trade Names:Zovirax- Tablets 400 mg- Tablets 800 mg- Capsules 200 mg- Suspension 200 mg per 5 mL- Ointment 5%- Cream 5%
Apo-Acyclovir (Canada)Gen-Acyclovir (Canada)Nu-Acyclovir (Canada)ratio-Acyclovir (Canada)Inhibits viral DNA replication by interfering with viral DNA polymerase.
Bioavailability is 10% to 20%. C max is 0.83 to 1.61 mcg/mL (200 to 800 mg at steady state).
IVC max is 9.8 mcg/mL (5 mg/kg dose), 22.9 mcg/mL (10 mg/kg).
TopicalSystemic absorption is minimal.
9% to 33% protein bound.
IVCSF concentrations are about 50% of plasma values.
The t ½ is 2.5 to 3.3 h. Cl and t ½ are dependent on renal function.
IV62% to 91% is excreted unchanged in the urine. Cl is 5.1 mL/min/kg.
Total body Cl and t ½ are dependent on renal function. Dosage adjustment recommended.
ElderlyIncreased plasma concentrations. Dosage adjustment may be required.
Treatment of initial or recurrent mucosal and cutaneous herpes simplex viruses (HSV) and varicella zoster (shingles) infections in immunocompromised patients; treatment of herpes simplex encephalitis; treatment of severe initial clinical episodes of genital herpes; treatment of neonatal herpes infections.
OralTreatment of initial and recurrent episodes of genital herpes in certain patients; acute treatment of shingles and chickenpox.
TopicalTreatment of initial episodes of herpes genitalis and nonlife-threatening mucotaneous HSV infections in immunocompromised patients (ointment); recurrent herpes labialis (cold sores) (cream).
Treatment of cytomegalovirus and HSV infection after bone marrow or renal transplant; treatment of infectious mononucleosis, varicella pneumonia, chickenpox, and other HSV infections.
Hypersensitivity to acyclovir or valacyclovir.
For IV infusion only; rapid or bolus IV must be avoided.
Herpes Simplex Infections in Immunocompromised Patients Adults and adolescents 12 yr of age and olderIV 5 mg/kg infused at a constant rate over 1 h every 8 h for 7 days.
Children younger than 12 yr of ageIV 10 mg/kg infused at a constant rate over 1 h every 8 h for 7 days.
Severe Initial Genital Herpes Adults and adolescents 12 yr of age and olderIV 5 mg/kg at a constant rate over 1 h every 8 h for 5 days.
Varicella Zoster Infections in Immunocompromised Patients Adults and adolescents 12 yr of age and olderIV 10 mg/kg infused at a constant rate over 1 h every 8 h for 7 days.
Children younger than 12 yr of ageIV 20 mg/kg infused at a constant rate over 1 h every 8 h for 7 days.
Herpes Simplex Encephalitis Adults and adolescents 12 yr of age and olderIV 10 mg/kg infused at a constant rate over 1 h every 8 h for 10 days.
Children 3 mo to 12 yr of ageIV 20 mg/kg infused at a constant rate over 1 h every 8 h for 10 days.
Neonatal Herpes Infections (CDC Recommendations)IV Disseminated and CNS disease: 20 mg/kg every 8 h for 21 days. Mucocutaneous disease: 20 mg every 8 h for 14 days.
OralChickenpox Adults and children (greater than 40 kg)PO 800 mg 4 times daily for 5 days.
Children 2 yr of age and older (40 kg or less)PO 20 mg/kg 4 times daily for 5 days.
Herpes Zoster AdultsPO 800 mg every 4 h 5 times/day for 7 to 10 days.
Initial Genital Herpes AdultsPO 200 mg every 4 h 5 times/day for 10 days.
Suppressive Therapy for Recurrent Genital Herpes AdultsPO 400 mg bid for up to 12 mo.
Intermittent Therapy for Recurrent Genital Herpes AdultsPO 200 mg every 4 h 5 times/day for 5 days at earliest sign or symptom of recurrence.
TopicalInitial Genital Herpes and Herpes Simplex Infections in Immunocompromised Patients AdultsOintment Apply sufficient quantity to cover all lesions every 3 h, 6 times/day, for 7 days.
Recurrent Herpes Labialis (Cold Sores) Adults and children 12 yr of age and olderCream Apply to lesion 5 times/day for 4 days.
Store tablets, capsules, and suspension at controlled room temperature (59° to 77°F). Protect from moisture.
TopicalStore ointment at controlled room temperature (59° to 77°F). Store cream at controlled room temperature (59° to 86°F).
InjectionStore powder for injection at controlled room temperature (59° to 77°F). Use reconstituted solution within 12 h. Refrigeration of reconstituted solution may result in formation of a precipitate that will redissolve at room temperature. Use diluted solution within 24 h.
IV acyclovir plasma levels may be increased, and the duration of action prolonged, while the urinary excretion and renal Cl may be reduced.
ZidovudineIncreased propensity for lethargy.
Precipitation may occur with bacteriostatic water. Do not add acyclovir to biologic or colloidal fluids.
None well documented.
Phlebitis at injection site (9%); hypotension (postmarketing).
Headache, agitation, coma, confusion, delirium, dizziness, hallucinations, obtundation, psychosis, seizure, somnolence (postmarketing).
Itching, rash, hives (2%); alopecia, erythema multiforme, photosensitive rash, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria (postmarketing).
Visual abnormalities.
Nausea, vomiting (7%); diarrhea, GI distress, abdominal pain (postmarketing).
Transient elevations of serum creatinine or BUN (5% to 10%); renal failure, elevated blood urea nitrogen, elevated creatinine.
Anemia, neutropenia, thrombocytopenia, thrombocytosis, leukocytosis, neutrophilia (less than 1%); leukopenia (postmarketing).
Disseminated intravascular coagulation, hemolysis, lymphadenopathy (postmarketing).
Elevated transaminases (1% to 2%); hepatitis, jaundice (postmarketing).
Myalgia (postmarketing).
Anaphylaxis, fever, pain, peripheral edema (postmarketing).
Category B .
Excreted in breast milk.
Safety and efficacy in children under 2 yr of age not established.
TopicalSafety and efficacy not established in pediatric patients.
Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Dosage adjustment may be needed. With parenteral use, acyclovir may precipitate as crystals in renal tubules.
Chickenpox in otherwise healthy children is usually a self-limiting disease of mild to moderate severity; however, adolescents and adults tend to have more severe disease.
Care must be taken to avoid getting drug in eyes.
Patients with underlying neurologic abnormalities or severe hypoxia may have increased risk of neurotoxic effects.
Sexual intercourse must be avoided when lesions are present. Use of acyclovir does not prevent transmission.
There are no data on treatment started more than 72 h after the onset of the rash.
Ensure that patient receiving IV acyclovir is well hydrated during therapy and that max dose of 20 mg/kg every 8 h is not exceeded.
May occur and has resulted in death in immunocompromised patients.
Increased BUN and serum creatinine, renal failure, convulsions, lethargy, acyclovir precipitation, renal tubules, agitation, coma.
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