Chickenpox: Treatment should begin within 24 hours of appearance of rash; oral route not recommended for routine use in otherwise healthy children with varicella, but may be effective in patients at increased risk of moderate to severe infection (>12 years of age, chronic cutaneous or pulmonary disorders, long-term salicylate therapy, corticosteroid therapy).
Genital herpes: Physical contact should be avoided when lesions are present; transmission may also occur in the absence of symptoms. Treatment should begin with the first signs or symptoms.
Herpes labialis: For external use only to the lips and face; do not apply to eye or inside the mouth or nose. Treatment should begin with the first signs or symptoms.
Herpes zoster: Acyclovir should be started within 72 hours of appearance of rash to be effective.
Systemic: Oral:
1% to 10%:
Central nervous system: Lightheadedness, headache
Gastrointestinal: Diarrhea, nausea, vomiting, abdominal pain
Systemic: Parenteral:
>10%:
Central nervous system: Lightheadedness
Gastrointestinal: Anorexia
1% to 10%:
Dermatologic: Hives, itching, rash
Gastrointestinal: Nausea, vomiting
Hepatic: Liver function tests increased
Local: Inflammation at injection site or phlebitis
Renal: Acute renal failure, BUN increased, creatinine increased
Topical:
>10%: Mild pain, burning, or stinging
1% to 10%: Itching
All forms: <1%, postmarketing, and/or case reports: Abdominal pain, aggression, agitation, alopecia, anaphylaxis, anemia, angioedema, anorexia, ataxia, coma, confusion, consciousness decreased, delirium, diarrhea, dizziness, dysarthria, encephalopathy, erythema multiforme, fatigue, fever, gastrointestinal distress, hallucinations, hematuria, hepatitis, hyperbilirubinemia, insomnia, jaundice, leukocytoclastic vasculitis, leukopenia, local tissue necrosis (following extravasation), mental depression, myalgia, paresthesia, peripheral edema, photosensitization, pruritus, psychosis, renal failure, seizure, somnolence, sore throat, Stevens-Johnson syndrome, thrombocytopenia, thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS), toxic epidermal necrolysis, tremor, urticaria, visual disturbances
Capsule, tablet: Store at controlled room temperature of 15°C to 25°C (59°F to 77°F); protect from moisture.
Cream, suspension: Store at controlled room temperature of 15°C to 25°C (59°F to 77°F).
Ointment: Store at controlled room temperature of 15°C to 25°C (59°F to 77°F) in a dry place.
Injection: Store powder at controlled room temperature of 15°C to 25°C (59°F to 77°F). Reconstitute acyclovir 500 mg with SWFI 10 mL; do not use bacteriostatic water containing benzyl alcohol or parabens. For intravenous infusion, dilute to a final concentration of
7 mg/mL. Concentrations >10 mg/mL increase the risk of phlebitis. Reconstituted solutions remain stable for 12 hours at room temperature. Do not refrigerate reconstituted solutions as they may precipitate. Once diluted for infusion, use within 24 hours.
Stable in D5W, D5NS, D5 1 /4NS, D5 1 /2NS, LR, NS.
Y-site administration: Compatible: Allopurinol, amikacin, amphotericin B cholesteryl sulfate complex, ampicillin, cefamandole, cefazolin, cefoperazone, cefotaxime, cefoxitin, ceftazidime, ceftizoxime, ceftriaxone, cefuroxime, chloramphenicol, cimetidine, clindamycin, co-trimoxazole, dexamethasone, dimenhydrinate, diphenhydramine, docetaxel, doxorubicin liposome, doxycycline, erythromycin lactobionate, etoposide, famotidine, filgrastim, fluconazole, gatifloxacin, gentamicin, granisetron, heparin, hydrocortisone sodium succinate, hydromorphone, imipenem/cilastatin, linezolid, lorazepam, magnesium sulfate, melphalan, methylprednisolone sodium succinate, metoclopramide, metronidazole, multivitamins, nafcillin, oxacillin, paclitaxel, penicillin G potassium, pentobarbital, perphenazine, piperacillin, potassium chloride, propofol, ranitidine, remifentanil, sodium bicarbonate, tacrolimus, teniposide, theophylline, thiotepa, ticarcillin, tobramycin, vancomycin, zidovudine. Incompatible: Amifostine, amsacrine, aztreonam, cefepime, dobutamine, dopamine, fludarabine, foscarnet, gemcitabine, idarubicin, levofloxacin, ondansetron, piperacillin/tazobactam, sargramostim, vinorelbine. Variable (consult detailed reference): Cisatracurium, diltiazem, meperidine, meropenem, morphine, TPN.
Compatibility when admixed: Compatible: Fluconazole. Incompatible: Dobutamine, dopamine. Variable (consult detailed reference): Meropenem.
Absorption: Oral: 15% to 30%
Distribution: Widely (ie, brain, kidney, lungs, liver, spleen, muscle, uterus, vagina, CSF)
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
Bioavailability: Oral: 10% to 20% with normal renal function (bioavailability decreases with increased dose)
Half-life elimination: Terminal: Neonates: 4 hours; Children 1-12 years: 2-3 hours; Adults: 3 hours
Time to peak, serum: Oral: Within 1.5-2 hours
Excretion: Urine (62% to 90% as unchanged drug and metabolite)
Genital HSV:
I.V.: Children
12 years and Adults (immunocompetent): Initial episode, severe: 5 mg/kg every 8 hours for 5-7 days
Oral:
Children:
Initial episode (unlabeled use): 40-80 mg/kg/day divided into 3-4 doses for 5-10 days (maximum: 1 g/day)
Chronic suppression (unlabeled use; limited data): 80 mg/kg/day in 3 divided doses (maximum: 1 g/day), re-evaluate after 12 months of treatment
Adults:
Initial episode: 200 mg every 4 hours while awake (5 times/day) for 10 days (per manufacturer's labeling); 400 mg 3 times/day for 5-10 days has also been reported
Recurrence: 200 mg every 4 hours while awake (5 times/day) for 5 days (per manufacturer's labeling; begin at earliest signs of disease); 400 mg 3 times/day for 5 days has also been reported
Chronic suppression: 400 mg twice daily or 200 mg 3-5 times/day, for up to 12 months followed by re-evaluation (per manufacturer's labeling); 400-1200 mg/day in 2-3 divided doses has also been reported
Topical: Adults (immunocompromised): Ointment: Initial episode: 1 /2" ribbon of ointment for a 4" square surface area every 3 hours (6 times/day) for 7 days
Herpes labialis (cold sores):
Topical: Children
12 years and Adults: Cream: Apply 5 times/day for 4 days
Herpes zoster (shingles):
Oral: Adults (immunocompetent): 800 mg every 4 hours (5 times/day) for 7-10 days
I.V.:
Children <12 years (immunocompromised): 20 mg/kg/dose every 8 hours for 7 days
Children
12 years and Adults (immunocompromised): 10 mg/kg/dose or 500 mg/m
2
/dose every 8 hours for 7 days
HSV encephalitis: I.V.:
Children 3 months to 12 years: 20 mg/kg/dose every 8 hours for 10 days (per manufacturer's labeling); dosing for 14-21 days also reported
Children
12 years and Adults: 10 mg/kg/dose every 8 hours for 10 days (per manufacturer's labeling); 10-15 mg/kg/dose every 8 hours for 14-21 days also reported
Mucocutaneous HSV:
I.V.:
Children <12 years (immunocompromised): 10 mg/kg/dose every 8 hours for 7 days
Children
12 years and Adults (immunocompromised): 5 mg/kg/dose every 8 hours for 7 days (per manufacturer's labeling); dosing for up to 14 days also reported
Oral: Adults (immunocompromised, unlabeled use): 400 mg 5 times a day for 7-14 days
Topical: Ointment: Adults (nonlife-threatening, immunocompromised): 1 /2" ribbon of ointment for a 4" square surface area every 3 hours (6 times/day) for 7 days
Neonatal HSV: I.V.: Neonate: Birth to 3 months: 10 mg/kg/dose every 8 hours for 10 days (manufacturer's labeling); 15 mg/kg/dose or 20 mg/kg/dose every 8 hours for 14-21 days has also been reported
Varicella-zoster (chickenpox): Begin treatment within the first 24 hours of rash onset:
Oral:
Children
2 years and
40 kg (immunocompetent): 20 mg/kg/dose (up to 800 mg/dose) 4 times/day for 5 days
Children >40 kg and Adults (immunocompetent): 800 mg/dose 4 times a day for 5 days
I.V.:
Children <1 year (immunocompromised, unlabeled use): 10 mg/kg/dose every 8 hours for 7-10 days
Children
1 year and Adults (immunocompromised, unlabeled use): 1500 mg/m
2
/day divided every 8 hours or 10 mg/kg/dose every 8 hours for 7-10 days
Prevention of HSV reactivation in HIV-positive patients, for use only when recurrences are frequent or severe (unlabeled use): Oral:
Children: 80 mg/kg/day in 3-4 divided doses
Adults: 200 mg 3 times/day or 400 mg 2 times/day
Prevention of HSV reactivation in HSCT (unlabeled use): Note: Start at the beginning of conditioning therapy and continue until engraftment or until mucositis resolves (~30 days)
Oral: Adults: 200 mg 3 times/day
I.V.:
Children: 250 mg/m 2 /dose every 8 hours or 125 mg/m 2 /dose every 6 hours
Adults: 250 mg/m 2 /dose every 12 hours
Bone marrow transplant recipients (unlabeled use): I.V.: Children and Adults: Allogeneic patients who are HSV and CMV seropositive: 500 mg/m 2 /dose (10 mg/kg) every 8 hours; for clinically-symptomatic CMV infection, consider replacing acyclovir with ganciclovir
Dosing adjustment in renal impairment:
Oral:
Clcr 10-25 mL/minute: Normal dosing regimen 800 mg every 4 hours: Administer 800 mg every 8 hours
Clcr<10 mL/minute:
Normal dosing regimen 200 mg every 4 hours, 200 mg every 8 hours, or 400 mg every 12 hours: Administer 200 mg every 12 hours
Normal dosing regimen 800 mg every 4 hours: Administer 800 mg every 12 hours
I.V.:
Clcr 25-50 mL/minute: Administer recommended dose every 12 hours
Clcr 10-25 mL/minute: Administer recommended dose every 24 hours
Clcr<10 mL/minute: Administer 50% of recommended dose every 24 hours
Hemodialysis: Administer dose after dialysis
Peritoneal dialysis: No supplemental dose needed
CAVH: 3.5 mg/kg/day
CVVHD/CVVH: Adjust dose based upon Clcr 30 mL/minute
Oral: May be administered with or without food.
I.V.: Avoid rapid infusion; infuse over 1 hour to prevent renal damage; maintain adequate hydration of patient; check for phlebitis and rotate infusion sites
Topical: Not for use in the eye. Apply using a finger cot or rubber glove to avoid transmission to other parts of the body or to other persons.
Topical: Apply as directed. Use gloves or finger cot when applying.
Capsule: 200 mg
Cream, topical: 5% (2 g)
Injection, powder for reconstitution, as sodium: 500 mg, 1000 mg
Zovirax®: 500 mg
Injection, solution, as sodium [preservative free]: 25 mg/mL (20 mL, 40 mL); 50 mg/mL (10 mL, 20 mL)
Ointment, topical: 5% (15 g)
Suspension, oral: 200 mg/5 mL (480 mL) [banana flavor]
Tablet: 400 mg, 800 mg
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