Pharmacological & Toxicological profiling

Question 1

Properties of an ideal drug:

Answer 1

1) Must be chemically stable
2) Must not be toxic
3) Good pharmacodynamic activity
4) Good pharmacokinetic activity

Question 2

Pharmacology

Answer 2

Pharmacodynamics is the biochemical & physiological effect(s) the drug has in the body. Target specificity & selectivity must be established, as should the therapeutic range.

Question 3

Absorption

Answer 3

is where the drug moves from the site of administration to a site in the body (blood). Absorption depends on the route – IV vs oral. There is a reliance on passage through membranes – transcellular or paracellular.

Question 4

The volume of distribution

Answer 4

depends on partitioning across various membranes & binding to tissue or blood components.

Question 5

Metabolism depends

Answer 5

on the location of the enzymes responsible for metabolism, whether it undergoes first-pass metabolism before systemic circulation, and the induction of metabolising enzymes (i.e. pro-drugs). During synthetic pathway, impurities may form and cause adverse effects.

Question 6

Elimination

Answer 6

is commonly via biliary (bile) or renal (urine) routes.

Question 7

• Receptor, ion channel and enzyme mediated

Answer 7

o Animal toxins can block ion channels

Question 8

• Biochemical pathways

Answer 8

o Inhibition of mitochondrial function (e.g. AZT has mitochondrial toxicity)

Question 9

• Organ-directed toxicity

Answer 9

o Hepatotoxicity
o Nephrotoxicity
* Mutagenesis and carcinogenesis
* Teratogenicity