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
Intestinal Metabolism
- 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
Hepatic Metabolims
- beta blockers reduce hepatic blood flow, deompensated CHF affects liver blood flow
Know inhibitors\ allopurinal cipr cimet dilt eryth isoiz PPI
Inducers barb carb Know Inducers
Pharmacodynamics
Effect of drug on the body
Drug Drug Interactions
Nitrates with PD5 inhibitors
Digoxin
- Other meds
- Hypokalemia, often dont get dig toxic unless hypok, start on diuretic, then pt becoes dig toxic
- Other drugs
Teratogenicity
- Drugs cross placenta
- No drug completely safe
ACE ARB warfarin clearly bad Betablcoker can be used Alcohol, LI pheno cause fetal abn
Drugs in Lactation
Drug Overdose Mangement
Beta Blocker
=CCB
Caffeine
Cardiotoxicity
- CHF with anthracylines: related to cumulative dose, 400 t0 500 mg / m2, occurs in about a yr, progressive asx lv dysfxn.
may persist after dc of tx
- may progressive after dc
younger and old age at biggest death pathphys:cell death
minimize further exxposure chf tx worse with re-exposure
type 2 cardiotoxicity
reversibel re-challenge may be safe