h2n n

deoxy-guanosine triphosphate (dGTP)


FIGURE 49-2 Conversion of acyclovir to acyclovir triphosphate leading to DNA chain termination. Acyclovir is converted to the monophosphate (MP) derivative by a herpes virus thymidine kinase. Acyclovir-MP is then phosphory-lated to acyclovir-DP and acyclovir-TP by cellular enzymes. Uninfected cells convert very little or no drug to the phos-phorylated derivatives. Thus, acyclovir is selectively activated in cells infected with herpesviruses that code for appropriate thymidine kinases. Incorporation of acyclovir-MP from acyclovir-TP into the primer strand during viral DNA replication leads to chain termination and formation of an inactive complex with the viral DNA polymerase. (Adapted from Elion, 1982, with permission.)

Acyclovir distributes widely in body fluids, including vesicular fluid, aqueous humor, and cerebrospinal fluid (CSF). Compared with plasma, salivary concentrations are low, and vaginal secretion concentrations vary widely. Acyclovir is concentrated in breast milk, amniotic fluid, and placenta. Newborn plasma levels are similar to maternal ones. Percutaneous absorption of acy-clovir after topical administration is low.

The plasma elimination half-life of acyclovir is ~2.5 hours in adults with normal renal function, 4 hours in neonates, and 20 hours in anuric patients. Renal excretion of unmetabolized acy-clovir by glomerular filtration and tubular secretion is the principal route of elimination.

Was this article helpful?

0 0
Diabetes 2

Diabetes 2

Diabetes is a disease that affects the way your body uses food. Normally, your body converts sugars, starches and other foods into a form of sugar called glucose. Your body uses glucose for fuel. The cells receive the glucose through the bloodstream. They then use insulin a hormone made by the pancreas to absorb the glucose, convert it into energy, and either use it or store it for later use. Learn more...

Get My Free Ebook

Post a comment