Learn more about the mechanism, dosage, side effects, and interactions of acyclovir from this book chapter on the NCBI Bookshelf
Pharmacokinetics of acyclovir and its metabolites in cerebrospinal fluid and systemic circulation after administration of high-dose valacyclovir in subjects with normal and impaired renal function
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5h Acyclovir levels in cerebrospinal fluid are approximately 50 percent of corresponding plasma levels
Viral DNA Polymerase Viral DNA synthesis is inhibited 20, 55, and 100% by incubation of HSV-I-infected Acyclovir kinetics are described by a two-compartment open model
Acyclovir is an oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9
Serum concentrations of acyclovir and its metabolite 9-(carboxymethoxymethyl) guanine were mainly analyzed on day 5 after the initiation of treatment before the morning dose (trough concentration Acyclovir (ACV) is an effective and selective antiviral drug, and the study of its toxicology and the use of appropriate detection techniques to control its toxicity at safe levels are extremely important for medicine efforts and human health
Acyclovir's main metabolite 9‐carboxymethoxymethylguanine is a presumptive neurotoxin and should be monitored in patients with impaired renal function or in cases with neurotoxic symptoms
However, these compounds were competitive inhibitors of this Objective: To obtain information on the serum concentrations of acyclovir and its metabolite in routine health care with respect to the renal function
Acyclovir phosphorylation was inhibited by exogenously added nucleosides
Acyclovir is mainly excreted in the urine, mostly unchanged, but partly as its main metabolite 9-Carboxymethoxymethylguanine (CMMG, 10-15%)
Acyclovir / analysis Acyclovir / metabolism* Adolescent Adult Age Factors Animals Biological Availability Child Child, Preschool Humans For decades, acyclovir-induced nephrotoxicity was believed to be secondary to crystalluria
This selectivity is due to the initial activation of the drug by A simple and rapid ultra-high-performance liquid chromatography coupled with mass spectrometry method was developed for acyclovir and its metabolite 9-carboxymethoxymethylguanine in human serum
After intravenous dosing of patients with normal renal function, 8 to 14% of the dose is recovered in A screening program for antiviral drugs begun at Burroughs Wellcome in the 1960s resulted in the discovery of acyclovir in 1974
Acyclovir will not cure herpes, but it can lessen the symptoms of the infection
Acyclovir (ACV) and ganciclovir (GCV) are acyclic analogs of guanosine that were approved for medical use in 1982 and 1989, respectively
Comparison of amenamevir with acyclovir and valaciclovir indicates that the Fa value is the differentiating factor for the Pharmacokinetics of acyclovir and its metabolites in cerebrospinal fluid and systemic circulation after administration of high-dose valacyclovir in subjects with normal and impaired renal function
07% of the rate with Guo)
This metabolite of acyclovir is the most potent inhibitor of purine nucleoside phosphorylase reported to date
Its elimination is mainly renal through filtration and tubular excretion; therefore, kidney damage can cause drug accumulation and systemic adverse effects
This knowledge can further be utilized to design novel prodrugs with optimum physicochemical properties and better pharmacokinetic profiles
Serious neurological adverse side effects have occurred during ACV treatment in patients with renal failure, but the cause of the symptoms remains unknown
ymethoxymethylguanine was the only signtftcant urinarry metabolite of acyclovir accounting for 8
Crystal-induced acute kidney injury (AKI) is caused by the intratubular precipitation of crystals, which results in obstruction
Although generally safe, it can cause AKI from intratubular crystal deposition when administered intravenously, particularly at high doses
Each 400 Acyclovir [9-(2-hydroxyethoxymethyl) guanine] is a synthetic acyclic purine nucleoside analogue that lacks the 3′-hydroxyl group of nucleosides
Oral administration of valaciclovir yields systemic aciclovir through uptake by dipeptide transporters in the gut lumen and hydrolysis by esterases present in the gut lumen, intestinal wall and liver
After intracellular uptake, it is converted to acyclovir monophosphate by virally-encoded thymidine kinase
BREAST FEEDING COMPATIBILITY
The pka's of acyclovir are 2
The oral bioavailability when taking acyclovir is only 10-20%, while the oral bioavailability of valacyclovir is as high as 54%
Penciclovir-triphosphate has a prolonged in vitro intracellular half-life of 10 to 20 hours in HSV-1-and HSV-2-infected cells, respectively, and 9 to 14 hours in VZV-infected cells
2 percent of dose) had the retention time of 8- hydroxy-9-(2-hydroxyethoxymethyl)guanine
2 micrograms/ml) were also achieved at 0
To the best of our knowledge, the acyclovir aldehyde metabolite has not been measured in any human biologic specimens, including plasma and urine
518-524
Profiling NNA drugs, we identify acyclovir (ACV) and ganciclovir (GCV) as two new NNAs metabolized by NUDT15
8 to 7
Studies on the disposition of acyclovir, during the course of its preclinical and clinical development, indicated significant species differences in the absorption, metabolism
The level of phosphorylation of acyclovir was
Patients were divided into two subgroups according to the
Metabolism
This metabolite of acyclovir is the most potent inhibitor of purine nucleoside phospho rylase reported to date
Serious neurological adverse side effects have occurred during ACV treatment in patients with renal failure, but the cause of the symptoms remains unknown
This selectivity is due to the initial activation of the drug by The metabolism of acyclovir to its mono-, di-, and triphosphate derivatives was examined in uninfected and virus-infected cells
This would give insight into the prodrug metabolism, major metabolite(s) formed, elimination pathway, and renal elimination kinetics of intact prodrug as well as the metabolites
10mg/kg IV q8h x 10 d
Acyclovir must first be taken up by virus-infected cells and phosphorylated to an active triphosphate metabolite that subsequently inhibits viral DNA synthesis
Valacyclovir has greater oral bioavailability than acyclovir and has similar activity against herpes viruses Aciclovir is an anti-viral frequently used for herpes virus infections
Each 800-mg tablet of acyclovir contains 800 mg of acyclovir and the inactive ingredients corn starch, microcrystalline cellulose, magnesium stearate, and sodium starch glycolate