Volume of Distribution - Examples

Examples

If you administer a dose D of a drug intravenously in one go (IV-bolus), you would naively expect it to have an immediate blood concentration which directly corresponds to the amount of blood contained in the body . Mathematically this would be:

But this is generally not what happens. Instead you observe that the drug has distributed out into some other volume (read organs/tissue). So probably the first question you want to ask is: how much of the drug is no longer in the blood stream? The volume of distribution quantifies just that by specifying how big a volume you would need in order to observe the blood concentration actually measured.

A practical example for a simple case (mono-compartmental) would be to administer D=8 mg/kg to a human. A human has a blood volume of around 0.08 l/kg . This gives a 100 µg/ml if the drug stays in the blood stream only, and thus its volume of distribution is the same as that is 0.08 l/kg. If the drug distributes into all body water the volume of distribution would increase to approximately 0.57 l/kg

If the drug readily diffuses into the body fat the volume of distribution may increase dramatically, an example is chloroquine which has a 250-302 l/kg

In the simple mono-compartmental case the volume of distribution is defined as:, where the in practice is an extrapolated concentration at time=0 from the first early plasma concentrations after an IV-bolus administration (generally taken around 5min - 30min after giving the drug).

Drug VD Comments
Warfarin 8L Reflects a high degree of plasma protein binding.
Theophylline, Ethanol 30L Represents distribution in total body water.
Chloroquine 15000L Shows highly lipophilic molecules which sequester into total body fat.
NXY-059 8L Highly-charged hydrophilic molecule.

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