Bioavailability, ADME, and Therapeutic Equivalence

ADME
absorption – determined by route
distribution – from route to target site. Affected by molecular size, blood flow rates, polarity
(fat / water) and ability to cross the blood-brain barrier.
Metabolism – chemical transformation by the body
excretion – expelled from by through urine, feces or exhalation

Toxicity – can be a problem through any ADME stage.

Bioavalability – percentage of a drug that reaches the systemic circulation (after metabolism)
IV has near 100% bioavalability.
Affected by Physical properties of the drug, diseases, age, gender, food, and drug formulation.
First-pass effect – matabolized by liver and released into bloodstream. EYP 450 enzomes involved.
Prodrugs – drugs designed to created active ingredient through metabolism process.

Bioequivalence – drugs that demonstrate the same clinical and biological effects, including
bioavailability.