15.3
Administered drugs begin to act once the minimum effective plasma level, Cmin, is attained. They remain effective as long as the concentration stays above Cmin.
The duration of drug action depends on the dose size, the drug removal rate, tissue binding, and route of administration.
With an increase in dose, Cmin is achieved rapidly, leading to the drug’s quicker onset and longer duration of action.
As per one-compartment kinetics, the following equation provides plasma drug concentration after an IV bolus. If plasma concentration is Cmin, then t becomes td or duration of the drug effect. Rearranging the equation yields td, with the resulting plot between td and log dose being linear.
As a result, doubling the dose increases the effect duration by one half-life.
However, for drugs having a narrow therapeutic index, doubling the dose may cause toxic effects. Instead, the same dose can be repeated when the drug levels fall.
For drugs producing a quantal response, onset occurs when plasma concentration reaches a minimum effective level (Cmin). The drug's action duration de…
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