Drug target interactions and clinical effect Flashcards
Pharmacokinetics
What body does to a drug
Pharmacodynamics
Effects of drugs on the body
Absorption
- Molecular weight
- Ionisation,
- Solubility
- Formulation
- Liberation
Factors affecting absorption
- Route of administration
- Gastric pH
- Contents of GI tract
Plasma protein binding
- Bound drugs do not cross membranes
- Malnutrition = decrease of albumin, increase of free drug
Digoxin
Na-K ATPase inhibitor
Digoxin properties
- Cardiac glycoside
- 70 to 80% of oral dose absorbed
- Distributed in tissue
Metabolism reactions
- Phase 1: Cytochrome P450
- Phase 2
Statins
Atorvastatin
Lovastatin
Simvastatin
Atherogenesis
- Process of forming plaques in the intima layer of arteries
Atherosclerosis
- Hypertension
- Diabetes
- Pro-inflammatory status
- ACS, angina, MI
Treatment
Life-style modifications
- Diet, exercise, stress reduction, smoking cessation
-Reduce cardiac workload
-Reduce blood pressure
-Manage blood fluid volume and electrolyte balance
CVD Elimination
Pulmonary - expired
Bile - excreted in faeces
Renal - glomerular filtration, tubular reabsorption, tubular secretion
Prescribing-dosage ACE
Efficacy
Potency
Effective concentration 50%
Lethal dose 50%
Therapeutic index
Margin safety
Ion channel linked
Millisecond
Nicotinic acetylcholine receptor
Removing hand from water
G protein linked
Seconds
B-Adrenergic receptor
Airway smooth muscle relaxation
Tyrosine kinase linked
Minutes
Insulin receptor
Glucose uptake into cells
DNA linked
Hours to days
Steroid receptor
Cellular proliferation
Glycoproteins
Cell surface, cytoplasm
Finite number if receptors in a given
Drug receptors
Ion channel is opened or closed
Second messenger is activated
cAMP, cGMP, Ca2+, Inositol phosphate
