Bioavailability

In the discussion of extravascular administration, it mentioned that it is possible that not all of the administered dose of a drug is absorbed. The percentage of the dose that is absorbed and reaches the circulation is called the bioavailability (F). A drug's bioavailability is typically less than 100. This can be due to poor absorption, or more commonly, metabolic degradation prior to the reaching the systemic circulation. Drugs given enterally pass through the portal vein and the liver prior to reaching the systemic circulation.

 

 

 

The bioavailability can be calculated by giving a drug both intravenously and orally. When the AUC is calculated (see calculating clearance) in both situations, and when it can be assumed that intravenous clearance is the same as oral clearance, this will allow calculation of the amount absorbed.

F = AUCoral / AUCintravenous

See how bioavailability effects the AUC by clicking here and selecting the AUC (module 3).

 

 

1

A certain drug can be administered intravenously and orally. The oral bioavailability is 0.5. What is expected if that drug is taken orally instead of intravenously? (Multiple answers possible)

2

For a drug with Foral = 0.5, the maximum concentration (Cmax) is always 50% of the Cmax of intravenous administration

3

A new drug is tested using 2 different administration routes:
- 80 mg oral
- 20 mg intravenous

The AUC's of both administered drugs are:
- oral: 1200 ng/mL*h
- intravenous: 1500 ng/mL*h

What is the oral bioavailability of this drug?