Aciclovir

C HpNsO, 133186-23-9) see Aciclovir iV-acetyl-S-benzyloxy-DL-tryptophan (C2, H2,N204 53017-51-9) see Oxitriptan iV-aeetyl-lV,0-bis(trimethylsilyl)cytosine... [Pg.2283]

C5HiyNSi2, 999-97-3) see Aciclovir Capecitabine Ganciclovir Mecillinam Tegafur Trifluridine... [Pg.2392]

C,oH 3N504 110104-37-5) see Aciclovir mono(diphenylmethyl) 4-hydroxymalonate (QiHisO 64952-5(5-3) see .Latamoxef monoethyl adipate... [Pg.2424]

Acyclovir (aciclovir) Famciclovir r Herpes simplex and varicella zoster... [Pg.124]

Steingrimsdottir, H.,etal. Bioavailability of aciclovir after oral administration of aciclovir and its prodrug valaciclovir to patients with leukopenia after chemotherapy. Antimicrob. Agents Chemother. 2000,... [Pg.273]

Aciclovir is used extensively in prophylaxis and treatment of infections caused by herpesviruses. The L-valyl ester prodrug of aciclovir, valaciclovir, has been developed during the past decade and enhances the 20% oral bioavailability of aciclovir... [Pg.538]

When administered as valaciclovir, aciclovir is released during absorption, and 60% of the drug reaches the bloodstream, as described above. Site activation also occurs in herpesvirus-infected cells where aciclovir is biochemically transformed to the phosphorylated active drug by virus-specific thymidine kinase [74]. [Pg.539]

Fig. 22.3. Mean plasma concentration-time profiles of aciclovir following administration of 1000 mg oral valaciclovir or a 350-mg intravenous infusion of aciclovir over a 1-h period.

Fig. 22.4. Model of aciclovir and Val-aciclovir transport. The prodrug Val-aciclovir is taken up at the apical cell membrane via the di/tri-peptide transporter, hydrolyzed intracelIularly in the enterocyte, with basal exit of valine and aciclovir. (Adapted from Smith et a. [78].)...

Prodrugs provide a vehicle by which the bioavailablUity of a drug displaying poor water solubility can be enhanced or a method of targeting diseased areas of the body. Following uptake, the drug is frequently released by the action of metabolic enzymes. For example, the human enzyme believed to be primarily responsible for the rapid in vivo hydrolysis of valaciclovir to aciclovir has recently been isolated and characterized (Scheme 1.18). ... [Pg.23]

Famciclovir, which is the pro-drug of penciclovir, is indicated in acute genital herpes simplex and in the treatment of varicella zoster. Famciclovir is available as tablets. Valaciclovir is the ester of aciclovir. [Pg.30]

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