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The Acyclovir
Molecule
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Pharmacology
Mechanism of action
Microbiology
Acylovir is active against most species in the herpesvirus family. In descending
order of activity:[1]. Herpes simplex virus type I (HSV-1) ; Herpes simplex virus
type II (HSV-2) ; Varicella zoster virus (VZV) ; Epstein-Barr virus (EBV)
;Cytomegalovirus (CMV)
Pharmacokinetics
Acylovir is poorly water soluble and has poor oral bioavailability (10-20%),
hence intravenous administration is necessary if high concentrations are
required. When orally administered, peak plasma concentration occurs after 1-
2 hours. Acylovir has a high distribution rate, only 30% is protein-bound in
plasma. The elimination half-life of aciclovir is approximately 3 hours. It is
renally excreted, partly by glomerular filtration and partly by tubular secretion.
Indications
Acylovir is indicated for the treatment of HSV and VZV infections, including:[3]
It has been claimed that the evidence for the effectiveness of topically applied
cream for recurrent labial outbreaks is weak.[4] Likewise oral therapy for
episodes is inappropriate for most non-immunocompromised patients, whilst
there is evidence for oral prophylactic role in preventing recurrences.[5]
Dosage forms
Aciclovir is commonly marketed as tablets (200 mg, 400 mg and 800 mg),
topical cream (5%), intravenous injection (25 mg/mL) and ophthalmic ointment
(3%). Cream preparations are used primarily for labial herpes simplex. The
intravenous injection is used when high concentrations of aciclovir are required.
The ophthalmic ointment preparation is only used for herpes simplex keratitis.
Topical therapy
Aciclovir topical cream is commonly associated with: dry or flaking skin and/or
transient stinging/burning sensations. Infrequent adverse effects include
erythema and/or itch.[3]
When applied to the eye, aciclovir is commonly associated with transient mild
stinging. Infrequently ophthalmic aciclovir is associated with superficial
punctate keratitis and/or allergic reactions.[3]
Toxicity
Footnotes
Further reading
Questions or Comments?