Cardiovascular pharmacology
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
Scope
- 5% of questions of the boards
Pharmacokinetics
- Potency vs Efficacy: Potency is meaningless, effect of drug per mg. Efficacy is the clinical effectiveness of drug.
- PK is effect of the body on the drug.
- Drug distribution: muscle high in water content. Women have less muscle mass. Older patients have less muscle mass. Elderly women have less total body water. Water soluble drugs are associated with a higher drug effect (eaxample alcohool). Do not diffuse into brain. Very important in beta blockers, they are hydrophilic.
- Lipophilic drugs:Cross into CNS. Lopressor, propranolol
Hydrophilic
- In intravascular space
- Cleared by kidney
- Dont cross blood brain barrier
Atenolol, hadolol, sotalol
Metabolism
- Liver C34 in half patients
- grapefruit juice affects intestinal system, but not liver. Intestinal cytochrome CYP3A4. (dihydropiridine CCBs,
lova, simva, cyclosporine, tacrolimus, sildenafil can be affected. May increase drug levels