Overview
| Generic Names: | 9-Hyroxyethoxymethylguanine; AC2; Aciclovier; Aciclovir Sodium; Acycloguanosine; Acyclovir; Acyclovir Sodium; Wellcome-248u |
|---|---|
| Trade Names: | Alti-Acyclovir; Avirax; Vipral; Virorax; Zovir; Zovirax; Zovirax Injection (Zovirax sodium) |
| PharmGKB Accession Id: | PA448045 |
Description
A guanosine analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes. PubChem (source: Drug Bank)
Indication
For the treatment and management of herpes zoster (shingles), genital herpes, and chickenpox (source: Drug Bank)
ATC Therapeutic Categories
- D06BB:Antivirals
- J05AB:Nucleosides and nucleotides excl. reverse transcriptase inhibitors
- S01AD:Antivirals
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Viral (HSV-1, HSV-2 and VZV) thymidine kinase converts aciclovir to the aciclovir monophosphate, which is then converted to the diphosphate by cellular guanylate kinase, and finally to the triphosphate by phosphoglycerate kinase, phosphoenolpyruvate carboxykinase, and pyruvate kinase. Aciclovir triphosphate competitively inhibits viral DNA polymerase and competes with the natural deoxyguanosine triphosphate, for incorporation into viral DNA. Once incorporated, aciclovir triphosphate inhibits DNA synthesis by acting as a chain terminator. (source: Drug Bank)
Pharmacology
Aciclovir (INN) or acyclovir (USAN, former BAN) is a synthetic deoxyguanosine analog and it is the prototype antiviral agent that is activated by viral thymidine kinase. The selective activity of aciclovir is due to its affinity for the thymidine kinase enzyme encoded by HSV and VZV. (source: Drug Bank)
Food Interactions
Increase liquid intake.
Take without regard to meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic, the only major urinary metabolite that has been detected is 9-carboxymethoxymethylguanine. (source: Drug Bank)
Protein Binding
9%-33% (source: Drug Bank)
Absorption
Oral: bioavailability 10 to 20% (source: Drug Bank)
Toxicity
Aciclovir may cause nephrotoxicity (crystallization of aciclovir within renal tubules, elevation of serum creatinine, transient), and neurotoxicity (coma, hallucinations, lethargy, seizures, tremors). Nephrotoxicity and neurotoxicity usually resolve after cessation of aciclovir therapy. However, there is no well-defined relationship between aciclovir concentrations in the blood and these adverse effects. (source: Drug Bank)
Isomeric SMILES Code:
c1nc2c(=O)[nH]c(nc2n1COCCO)N (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
|
SLC22A1 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| NP |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| theophylline |
|
Increases the effect and toxicity of theophylline (source: Drug Bank) |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
