Pharmacokinetics

- what the body does to a drug

1. Absorption

- Passive Diffusion

Travels from high to low concentration

(e.g water soluble requires help and lipid soluble drug does not requires help)

- Facilitated Diffusion

Needs help from the carrier protein

Travels from high to low concentration

- Active Transport

Energy from this process derived from ATP

When ATP -> ADP (Hydrolysis) there is a high energy of breaking the phosphate bond

- Endocytosis

Large sized drugs get transported via engulfment by cell membrane

NOTE!! ABSORPTION DEPENDS ON PH, SURFACE AREA AND BLOOD FLOW

Bioavailability – simply AUC (area under the curve) for the oral drug over AUC for the IV drug times 100

2. Distribution (outside and inside the cell)

Factors affecting the distribution:

- Lipophilicity drug will dissolve through some membrane easier than the hydrophilic drug

- Blood flow (brain receives more blood flow than skin)

- Capillary Permeability (capillaries in the liver has lots of slit junctions through which large proteins can
pass, while in brain no slit junctions more difficult for a drug to pass through)

- Plasma and Tissue Binding (many drug will bind to albumin – major drug binding protein that will
significantly slow the distribution process)

Volume Distribution

- theoretical volume a drug would have to occupy in order to produce the concentration that is present
on blood plasma

- amount of drug in the body over concentration of blood in plasma

- helps predict whether the drug will concentrate largely in the blood or in the tissue

3. Metabolism (liver - biotransformed)

4. Elimination

- refers to clearing of a drug from the body mainly through hepatic renal and biliary route so the total
body clearance is simply the sum

- total body clearance = sum of individual clearance processes

First Order Kinetic

Where most drugs are eliminated – amount of drug eliminated over time is directly proportional to the
concentration of drug in the body

Pharmacodynamics