Pharmacokinetics (PK) simply stated is ‘‘what the body does to the drug’’ (ie, how the drug is absorbed, eliminated and metabolized). Pharmacodynamics or PD is ‘‘what the drug does to the body.’’ Absorption: After single oral-dose administration of tadalafil, the maximum observed plasma concentration (Cmax) is achieved between 30 minutes and 6 hours (median time of 2 hours), although an erectogenic effect is not predicated on the need to reach Cmax. The time to reach Cmax is referred to as Tmax. Neither the rate nor the extent of absorption of tadalafil is influenced by food. Thus tadalafil may be taken with or without food. Metabolism: Tadalafil is predominantly metabolized by CYP3A4 to a methyl catechol glucuronide metabolite. In vitro data suggest that metabolites are not expected to be pharmacologically active following a dose of tadalafil. Elimination: The mean elimination half-life (also sometimes referred to as ‘‘terminal halflife’’) for tadalafil is 17.5 hours in healthy subjects. The half-life is the time it takes for the plasma concentration of drug in the body to be reduced by 50%. Tadalafil is excreted predominately as inactive metabolites, mainly in the feces and to a lesser extent, urine.
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