Acyclovir is used to treat herpes infections of the skin, lip, and genitals; herpes zoster (shingles); and chickenpox. It does not cure herpes infections but decreases pain and itching and promotes healing. Topical Acyclovir does not prevent the recurrence of sores but may decrease pain and itching if applied when the earliest symptoms first appear. Oral Acyclovir decreases the frequency and severity of recurrent sores, but it is used only by people with severe herpes infections because of possible adverse effects. This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.
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Acylovir differs from previous nucleoside analogues in that it contains only a partial nucleoside structure: the sugar ring is replaced by an open-chain structure. It is selectively converted into acyclo-guanosine monophosphate (acyclo-GMP) by viral thymidine kinase, which is far more effective (3000 times) in phosphorylation than cellular thymidine kinase. Subsequently, the monophosphate form is further phosphorylated into the active triphosphate form, acyclo-guanosine triphosphate (acyclo-GTP), by cellular kinases. Acyclo-GTP is a very potent inhibitor of viral DNA polymerase; it has approximately 100 times greater affinity for viral than cellular polymerase. As a substrate, acyclo-GMP is incorporated into viral DNA, resulting in chain termination. It has also been shown that viral enzymes cannot remove acyclo-GMP from the chain, which results in inhibition of further activity of DNA polymerase. Acyclo-GTP is fairly rapidly metabolised within the cell, possibly by cellular phosphatases.
In sum, aciclovir can be considered a prodrug: it is administered in an inactive (or less active form) and is metabolised into a more active species after administration.
Acyclovir is used to treat herpes infections of the skin, mouth, mucous membranes, genital herpes, herpes zoster (shingles), and chickenpox in some individuals. This medication does not cure herpes, but relieves the pain and may make the infection clear faster.Begin taking Acyclovir as soon as symptoms appear. Take Acyclovir as directed. Ask your doctor or pharmacist if you have any questions. Try to take the medication at evenly spaced intervals throughout the day and night. This will ensure a constant blood level of the medication and is most effective.
No serious side effects are expected during treatment with Acyclovir topical. If you suspect an allergic reaction (difficulty breathing; rash; hives; itching; swelling of your lips, tongue, or face) seek emergency medical attention. Other less serious side effects may be more likely to occur. Continue to use Acyclovir topical and talk to your doctor if you experience itching, stinging, burning, or a rash. These side effects should resolve quickly. Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome.
Overdoses involving ingestion of up to 100 capsules (20 g) have
been reported. Adverse events that have been reported in association
with overdosage include agitation, coma, seizures, and lethargy.
Precipitation of acyclovir in renal tubules may occur when the solubility
(2.5 mg/mL) is exceeded in the intratubular fluid. Overdosage has
been reported following bolus injections or inappropriately high
doses and in patients whose fluid and electrolyte balance were not
properly monitored. This has resulted in elevated BUN and serum
creatinine and subsequent renal failure. In the event of acute renal
failure and anuria, the patient may benefit from hemodialysis until
renal function is restored.
Acyclovir Cream is contra-indicated in patients known to be hypersensitive to acyclovir or propylene glycol. Acyclovir is most effective if it is started within 48 hours of when the rash first appears. Follow the directions for using Acyclovir provided by your doctor.