Valacyclovir hydrochloride pharmacokinetics

Valacyclovir hydrochloride is the forerunner of acyclovir into acyclovir anatomize in vivo to arrest the virus. Adjoin HSV Ⅰ (HSV-Ⅰ) and canker canker virus Ⅱ (HSV-Ⅱ) able inhibition of varicella zoster virus, EB virus and cytomegalovirus anemic inhibition. The apparatus is to absolute the viral DNA amalgam and arrest its replication. Valacyclovir hydrochloride rapidly captivated afterwards articulate administering and adapted to acyclovir, acyclovir affectionate claret aiguille time of 0.88-1.75hr. Articulate bioavailability was 67 ± 13%, is 3-5 times acyclovir. Valacyclovir hydrochloride articulate assimilation broadly distributed, can be broadcast to all the 14 kinds of tissues, including the stomach, baby intestine, kidney, liver, lymph nodes and derma tissue in the accomplished concentration, the everyman assimilation of academician tissue. Valacyclovir hydrochloride in vivo afterwards articulate administering is rapidly captivated absolutely into acyclovir, metabolites mainly alone in urine, which accounted for 46% -59% acyclovir 8 - hydroxy-9 - guanine accounted for 25 % -30%, 9 - hydroxy-methoxy-methyl guanine accounted for 11% -12%. Affectionate acyclovir afterwards articulate administering of single-phase abolishment half-life of 2 advantageous volunteers demography the artefact 250 ~ 2000mg, into the claret aggregate and aiguille claret assimilation (Cmax) and dose-linear. The assimilation of ACV, articulate 200 ~ 400mg, the beeline relationship,> 600mg saturated curve, oral> 800mg, captivated into the bloodstream best dosing increases. Added articulate dosage (600mg) of VACV and ACV, aiguille time (Tmax) were 2.10 and 3.27h; aiguille concentrations were 5.03 and 1.53mg / L. ACV VACV in the physique into locations by the liver, its above metabolite in the urine, which accounted for 46% of ACV to 59%, 8 - hydroxy Acyclovir accounted for 25% to 30%, 9 - hydroxy-methoxy-A guanine abject accounted for 11% to 12%. Claret protein bounden bulk is actual low, calmly through the biofilm. ACV afterwards articulate abolishment half-life of affectionate 3h.

Valacyclovir hydrochloride into the animal physique rapidly addle into L-valine and acyclovir. The above is complex in accustomed physiological and biochemical metabolism of the body, the closing is the canker virus-infected cells, viral thymidine kinase phosphorylation to become a individual phosphate compound, again the beef become diphosphate kinase phosphorylation and triphosphate compounds. Triphosphate compounds are anti-viral substances, can arrest the viral DNA polymerase, abortion of DNA synthesis, appearance antiviral efficacy. Since the amino acerbic ester of ACV artefact is no chargeless hydroxyl accumulation to phosphorylation, which is not adapted to ACV before, no antiviral activity, which it is not like the added forerunner drugs such as valaciclovir (desciclovir), etc. an added baneful to cells. Someone in Vero beef in vitro antiviral archetypal observed, including VACV, including amino acerbic esters of acyclovir adjoin canker canker virus blazon Ⅰ (HSV-1) accept a assertive effect, IC50 bulk of 0.84 ~ 10.5μmol / L, which , VACV0.84μmol / L, ACV0.1μmol / L [4]. HSV-1 was able application mice or dissection archetypal of HSV-2 infection, the use of VACV treatment, while ACV as a control. VACV accepted above ability of ACV, and the HSV-1 and HSV-2 agnate sensitivity, and added appropriate treatment, the beneath bulk of virus infection, the better. Has been begin that acyclovir triphosphate inhibits HBV, woodchuck hepatitis and avoid hepatitis B DNA polymerase, thereby interfering with viral DNA replication, and in vitro abstracts ACV does not arrest the virus. Clinically, this artefact is now acclimated for the blockage and analysis of patients with assorted allowed deficiencies canker virus infections. Late H Ⅳ and accompanied by abbreviation the amount of CD4 lymphocytes in patients decumbent to accelerating or alternate mucocutaneous canker virus infections, ACV has apparent accretion resistance, as analytic problems, use the artefact afterwards The bearings has been decidedly improved.

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from: biomedicine