Question
Define bioavailability. What are the factors that affect bioavailability of drugs (1+5)
Q4 6 marks Short Essays ★ ✓
Answer
Bioavailability is the fraction (or percentage) of an administered dose of a drug that reaches the systemic circulation in an unchanged, active form. For an IV dose, bioavailability is 100% by definition; for other routes it is calculated by comparing the area under the plasma concentration-time curve (AUC) for that route against the AUC for an equal IV dose.
Factors affecting bioavailability :
First-pass (presystemic) metabolism — drugs absorbed from the GI tract pass through the liver via the portal circulation before reaching systemic circulation; extensive hepatic metabolism at this stage (e.g. propranolol, lignocaine) can drastically reduce oral bioavailability compared to parenteral routes.
Drug formulation — particle size, disintegration and dissolution rate, and the specific salt/ester form all affect how much drug is actually absorbed; poorly formulated tablets may pass through the gut without fully dissolving.
Physicochemical properties of the drug — lipid solubility, degree of ionization at gut pH, and molecular size all affect membrane permeability and absorption.
GI factors — gastric emptying rate, intestinal motility, presence of food (can enhance or reduce absorption depending on the drug), and gut pH all influence how much drug is absorbed before it is eliminated.
Route of administration — parenteral (especially IV) routes bypass first-pass metabolism and absorption barriers entirely, generally giving higher bioavailability than oral administration for drugs with significant first-pass loss.
1 Pharmacokinetics
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