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Acyclovir is an antiviral for herpes simplex and varicella-zoster viruses that compounding pharmacies prepare as topical creams, oral suspensions, capsules and other forms by prescription.
Acyclovir is a synthetic purine nucleoside analogue antiviral. In cells infected with herpes simplex or varicella-zoster virus, a viral enzyme (thymidine kinase) activates it, and the activated form blocks the virus's DNA polymerase and ends the growing DNA chain, so the virus cannot copy itself; uninfected cells activate very little of it. Manufactured products include generic acyclovir tablets, capsules and oral suspension, Zovirax cream and ointment, Sitavig buccal tablets, and acyclovir injection. The oral products are FDA-approved for herpes zoster (shingles), initial and recurrent genital herpes, and chickenpox; Zovirax ointment for initial genital herpes and limited mucocutaneous HSV in immunocompromised patients. A prescriber may order acyclovir compounded when a patient needs a different topical strength or base, a combination with another ingredient, or a flavored or sugar-free oral liquid. Compounded acyclovir preparations are not FDA-approved and require a prescription.
Acyclovir carries no boxed warning. The oral label warns that kidney failure, sometimes fatal, has occurred, especially with dehydration, kidney disease or other kidney-toxic drugs, so adequate hydration matters; thrombotic thrombocytopenic purpura/hemolytic uremic syndrome has occurred in immunocompromised patients; and severe skin reactions have been reported, so a painful rash with mouth sores means stop and get help. It is contraindicated with a significant allergy to acyclovir or valacyclovir. Probenecid raises acyclovir levels. Older adults and people with reduced kidney function are more prone to confusion and hallucinations. The ointment must not be used in the eye. There are no adequate pregnancy studies; a registry found birth defect rates similar to the general population, and the label advises use only if the benefit justifies the risk. Milk levels are far below an infant dose, and acyclovir is considered a treatment of choice for herpes during breastfeeding. Common side effects are nausea, vomiting, diarrhea and malaise. Acyclovir does not clear the virus from the body or fully prevent spreading it. For decreased urination, confusion or blistering skin, talk to your prescriber or pharmacist.
Acyclovir is phosphorylated by viral thymidine kinase to the monophosphate, then by cellular kinases to acyclovir triphosphate, which competitively inhibits viral DNA polymerase and causes chain termination; selectivity arises from preferential activation in infected cells. Oral bioavailability is 10 to 20 percent and decreases with increasing dose; protein binding is 9 to 33 percent; plasma half-life is 2.5 to 3.3 hours with normal renal function and can extend up to tenfold in renal impairment. Elimination is largely unchanged by glomerular filtration and tubular secretion, so dose adjustment follows creatinine clearance. Systemic absorption after topical ointment is minimal. Labeled indications: acute herpes zoster, initial and recurrent genital herpes, and varicella (oral acyclovir); initial genital herpes and limited non-life-threatening mucocutaneous HSV in immunocompromised patients (Zovirax ointment); HSV encephalitis, neonatal HSV, mucocutaneous HSV in immunocompromised patients, severe initial genital herpes and zoster in immunocompromised patients (acyclovir injection). Prescribers have ordered compounded acyclovir for mucocutaneous HSV, HSV keratitis and prophylaxis in transplant recipients, uses StatPearls describes beyond the oral label; recurrent herpes labialis is the labeled indication of Sitavig buccal tablets. Dosing is per prescriber. Monitor renal function, hydration status and neurologic changes, particularly in older adults, obese patients and those receiving vancomycin or other nephrotoxins. Acyclovir is not a controlled substance.
Compounded at Bayview
Patient guides for the preparations we make most often. Each one is compounded to order and requires a prescription.
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Every preparation in our formulary that contains this ingredient. Strength, base and dose form are set by the prescription.
Other salt forms of this molecule, and ingredients commonly compounded alongside it.
This page describes an active pharmaceutical ingredient, not a finished drug product. Bayview Pharmacy compounds preparations containing it only on a prescriber's order for an individual patient.
Compounded preparations are not FDA-approved, and the FDA has not evaluated them for safety, effectiveness, or manufacturing quality. Nothing on this page is a claim that any preparation is effective for any condition.
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