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Valacyclovir
drug data and news
Valacyclovir drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Valacyclovir | ||
| Brand Names/Synonyms | Acyclovir; BW 256U87; Valaciclovir; Valaciclovir Hcl; Valaciclovir Hydrochloride; Valacyclover Hydrochloric; Valacyclover Hydrochloride; Valacyclovir; Valacyclovir Hydrochloride; Valtrex; Zovirax | ||
| Indication | For the treatment or suppression of cold sores (herpes labialis), herpes zoster (shingles), genital herpes in immunocompetent individuals, and recurrent genital herpes in HIV-infected individuals. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Valacyclovir is a prodrug and synthetic purine nucleoside analogue with inhibitory activity against herpes simplex virus types 1 (HSV-1), 2 (HSV-2), varicella-zoster virus (VZV), Epstein-Barr virus (EBV), and cytomegalovirus (CMV). Valacyclovir is almost completely converted to acyclovir and L-valine. The inhibitory activity of valacyclovir is highly selective due to its affinity for the enzyme thymidine kinase (TK) encoded by HSV and VZV. This viral enzyme converts acyclovir into acyclovir monophosphate, which is then converted into acyclovir diphosphate and triphosphate by cellular enzymes. Acyclovir is selectively converted to the active triphosphate form by cells infected with herpes viruses. | ||
| Mechanism Of Action | Valacyclovir is phosphorylated by viral thymidine kinase to acyclovir triphosphate (the active metabolite) which then inhibits herpes viral DNA replication by competitive inhibition of viral DNA polymerase, and by incorporation into and termination of the growing viral DNA chain. When used as a substrate for viral DNA polymerase, acyclovir triphosphate competitively inhibits dATP leading to the formation of 'faulty' DNA. This is where acyclovir triphosphate is incorporated into the DNA strand replacing many of the adenosine bases. This results in the prevention of DNA synthesis, as phosphodiester bridges can longer to be built, destabilizing the strand. | ||
| Valacyclovir News (When available) |
Recent Developments in the Treatment of Cutaneous Viral Infections Apr 20, 2006 Antiviral meds shackle shingle pain May 9, 2006 Antiviral Drugs May Fight Shingles Pain May 10, 2006 Antiviral Drugs may Help Treat Shingles May 10, 2006 Antiviral Drugs Help Relieve Enduring Shingles Pain May 9, 2006 Antiviral Drugs May Cut Shingles Pain May 8, 2006 I have herpes, is my sex life ruined? May 2, 2006 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Prodrugs; Antivirals; ATC:J05AB | ||
| Absorption | After oral administration, valacyclovir hydrochloride is rapidly absorbed from the gastrointestinal tract. The absolute bioavailability of acyclovir after administration of valacyclovir is 54.5% ± 9.1%. | ||
| Interactions | Interactions for Valacyclovir: The pharmacokinetics of digoxin was not affected by coadministration of Valacyclovir 1 gram 3 times daily, and the pharmacokinetics of acyclovir after a single dose of Valacyclovir (1 gram) was unchanged by coadministration of digoxin (2 doses of 0.75 mg), single doses of antacids (Al3+ or Mg++), or multiple doses of thiazide diuretics. Acyclovir Cmax and AUC following a single dose of Valacyclovir (1 gram) increased by 8% and 32%, respectively, after a single dose of cimetidine (800 mg), or by 22% and 49%, respectively, after probenecid (1 gram), or by 30% and 78%, respectively, after a combination of cimetidine and probenecid, primarily due to a reduction in renal clearance of acyclovir. These effects are not considered to be of clinical significance in subjects with normal renal function. Therefore, no dosage adjustment is recommended when Valacyclovir is coadministered with digoxin, antacids, thiazide diuretics, cimetidine, or probenecid in subjects with normal renal function. | ||
| Toxicity | Adverse effects of overexposure might include headache and nausea. | ||
| Organisms Affected | Not Available | ||
| Chemical IUPAC Name | 2-[(2-amino-6-oxo-3,9-dihydropurin-9-yl)methoxy]ethyl2-amino-3-methyl-butanoate | ||
| Chemical Formula | C13H20N6O4 | ||
| Molecular Weight | 324.336 g/mol | ||
| Smiles String | CC(C)C(C(=O)OCCOCN1C=NC2=C1NC(=NC2=O)N)N | ||
| Melting Point | Not Available | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | Not Available | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Valacyclovir is rapidly and almost entirely (~99%) converted to the active compound, acyclovir, and L-valine by first-pass intestinal and hepatic metabolism by enzymatic hydrolysis. Neither valacyclovir nor acyclovir is metabolized by cytochrome P450 enzymes. | ||
| Half Life | 2.5-3.3 hours | ||
| Protein Binding [%] | 13 to 18% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Valacyclovir.html http://www.rxlist.com/cgi/generic3/valacyclovir.htm http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/val1474.shtml | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00697 | ||
| CAS Registry Number | 124832-27-5 | ||
| KEGG Compound ID | C07184 | ||
| PubChem ID | SID:215420 | ||
| PharmGKB ID | PA451839 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2246559 |
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