Module 2 Jan 26 Flashcards
Drug altered Response - 4
Tolerance - after giving drug, body adjusts, need more to get same effect
Tachyphylaxis - tolerance after short term admin
Down regulation - cell response, remove some receptors, desensitize
Up regulation - cell response, add receptors, more sensitive
Why need to know pharmacodynamics - 6
Drug delivery timing High quality care Communication w/other health care providers Monitoring Patient education/questions Questions and clarifications
Drug legislation history - 5
1938 Food Drug Cosmetic Act - Basic Safety
1962 - Kefauver-Harris, required effectiveness, rigorous testing
1970 - Controlled substances act, Schedule 1-5, abuse. Narcotic means schedule 1, controlled with no medical use.
1984 - Hatch-Waxman - availability of generic drugs
1994 - Dietary supplement - restrictions on labelling supplements
Drug development phases - 5
Preclinical - test on animals, toxicology
Phase 1 - Toxicology on healthy humans, 1 year
Phase 2 - Effects and safety, 2 years
Phase 3 - Safety and effectiveness, 3 years
Phase 4 - Post Marketing
Drug labelling, naming - 6
Prescribing Information (PI)
What FDA approved, note could have off-brand uses
Black Box warnings - cause specific problems
Drug names: Chemical name, Generic Name, Brand Name(s)
Pharmacodynamics - 3, pharmacokinetics - 5
Pharmacokinetics - Action of body on drug - Absorb, distribute, metabolize, excrete
Pharmacodynamics - Action of the drug on the body, drug + receptor, Biological response
Drug-receptor interactions, relative speed - 2
Ligand-Receptor - fast
Intracellular - slow
Drug - Receptor interactions - 2 types, stereoisomers, binding - 2
Agonist, antagonist
Same formula, different orientation R and S, mirror image
Me Too drugs often use stereoisomers to re-patent
Binding - lock and key - reversible or non-reversible
2nd messengers common - 5
cAMP cGMP Ca++ Diacylglycerol IP3
Drug effects additive, synergistic, antagonistic, potentiation
Additive - Sum of effects
Synergistic - More than the sum of effects
Antagonistic - Less than the individual parts
Potentiation - One has no effect except to enhance the other
Agonist/Antagonist/Affinity/Intrinsic activity 2 types (blocking) Antagonist
Affinity - really attracted to receptor (Agonist, Antagonist)
Intrinsic activity - really activates receptor on binding (Agonist)
Partial Agonist - binds and activates, lower maximal effect
Antagonist Competitive - can be overcome by lots of agonist
Irreversible - will not leave receptor
Dose-response curve, ED50, efficacy, potency
Dose horizontal log scale, response vertical, S curve
ED50 is dose required for 50% maximal response
Efficacy - max response produced by drug.
Potency - smaller dose for same result. Don’t care
Therapeutic index - 2
Space between efficacy curve and toxic curve
Narrow causes clues like a slow titration, be in hospital for titration, med change