Pharmacokinetics

Pharmacodynamics: Effect of drug on the body.

Full agonists are exogeneous ligands that mimic the endogenous effect of a naturally
occurring chemical at the same receptor site.
Pharmacokinetics: Effect of body on the drug. Study of drug’s journey as it is absorbed into,
distributed through, metabolised in and excreted from an organism.

Therapeutic index:
Therapeutic index value is a ratio. Ratio of lethal dose of drug:beneficial dose of drug
Therapeutic index value is 100:1

Lipid-soluble compounds can traverse through membrane, but water-soluble compounds

cannot.
Passive transport – using concentration gradient
Active transport – using energy from ATP to push substances against concentration gradient

Absorption looks at the movement of a drug from its site of administration to the plasma.
Approx. 75% of drugs administered orally are absorbed withing 1-3hrs
Factors affecting gastrointestinal (GI) absorption include:
1. Gastric motility
2. Presence of food/liquids
3. Particle size & formulation

Drug efflux
Drug efflux proteins: Protein-mediated transport systems fuelled by ATP. Eg P-glycoprotein
transporter.
Drug efflux proteins use energy to push drugs back into intestine, limiting absorption of fat-
soluble drugs via intestinal wall.
Plasma binding: Once drug reaches systemic circulation in blood plasma, not all of it is
available to exert an effect as it binds to plasma proteins.
Only the unbound drug can produce a pharmacological effect.

Factors that can affect plasma protein binding:

1. Concentration of free drug
2. Affinity of drug for plasma protein binding site
3. Concentration of plasma protein.

Binding sites on plasma albumin may bind to many different drugs – drug competition.

Effects of protein binding:

Highly bound drugs require larger loading dose.
Highly bound drugs have limited tissue distribution.
Changes in available plasma protein may have a profound effect on free drug availability.
Once the free drug leaves the circulation, and the target tissue has been identified , the drug
attaches itself to a receptor/other drug targets and stimulates site of action = producing
pharmacological effect.