Chapters 4, 5, & 9 Flashcards
Pharmacokinetics
Study of what happens to the med, how it reaches target cells, how the body handles the drug.
Absorption
Distribution
Metabolism
Excretion
Absorption
Stomach to blood
Skin to blood
Mucus membrane to blood
IVs or intra arterial administration does not use absorption
Distribution
Affected by: amount of blood flow, ability of tissues to store drug, drug and protein binding, blood brain barrier.
Metabolism (bio transformation)
How body chemically changes drug molecule
Liver primary site of metabolism
Changes is structure of drug
Some meds increase metabolic activity in liver (enzyme induction) causing increased metabolism
CYP-450 could alter metabolism in certain drugs
CYP-450
Hepatic microsomal enzyme system
Determines speed of metabolism
Drugs may compete with binding sites on CYP isozyme- responsible for drug-drug interactions
Excretion
Most excreted by kidney (bowmans capsule, renal tubule)
Some excreted by lungs
Some in saliva, sweat, breast milk
Rarely in bile or feces
Receptor theory
Receptor is cellular molecule to which a med binds, usually a protein
More receptors=more binding=greater effect
Binding either enhances or inhibits normal cellular function
High intrinsic activity is great binding, strong action
When drugs work without receptors, they change cell membrane or depress membrane excitability
Agonist
Binds to and activates receptor
Antagonist
Binds to receptor and keeps cell from functioning normally
Antagonist competes with agonist for binding sites
Potency
How much is needed to produce therapeutic effect
Determined by drugs affinity for a receptor on cell
Efficacy
Measures the greatest effect produced by the drug
The more potent (the greater the efficacy) the more intense the adverse effects