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A loading dose is most useful for drugs that are eliminated from the body relatively slowly, i.e. have a long systemic half-life. Such drugs need only a low maintenance dose in order to keep the amount of the drug in the body at the appropriate therapeutic level, but this also means that, without an initial higher dose, it would take a long ...
Continuing the maintenance dose for about 4 to 5 half-lives (t 1/2) of the drug will approximate the steady state level. [1] One or more doses higher than the maintenance dose can be given together at the beginning of therapy with a loading dose. [2] A loading dose is most useful for drugs that are eliminated from the body relatively slowly ...
where De is the effective dose, B bioavailability and Da the administered dose. Therefore, if a drug has a bioavailability of 0.8 (or 80%) and it is administered in a dose of 100 mg, the equation will demonstrate the following: De = 0.8 × 100 mg = 80 mg
Consideration has to be given to what is known as "drug loading" - the ratio of the active drug to the total contents of the dose. A low drug load may cause homogeneity problems. A high drug load may pose flow problems or require large capsules if the compound has a low bulk density.
So, for example, digoxin has a half-life (or t 1 / 2 ) of 24–36 h; this means that a change in the dose will take the best part of a week to take full effect. For this reason, drugs with a long half-life (e.g., amiodarone , elimination t 1 / 2 of about 58 days) are usually started with a loading dose to achieve their desired ...
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Therefore, the dose required to give a certain plasma concentration can be determined if the V D for that drug is known. The V D is not a physiological value; it is more a reflection of how a drug will distribute throughout the body depending on several physicochemical properties, e.g. solubility, charge, size, etc.
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