FINAL Flashcards
(125 cards)
First order kinetics
- constant FRACTION of drug eliminated/unit time
- clearance directly proportional to concentration
- most drugs
- curved graph
Zero order kinetics
- constant AMOUNT of drug eliminated/unit time
- independent of concentration
- ETOH, ASA, dilantin
- linear graph
Half life
Amount of time it takes for 1/2 of drug to be cleared
Steps for determining degree of ionization of drug
1) is drug acidic or basic?
2) what is the pH of the tissue?
3) what is the pKa of the drug?
4) Is the pKa becoming more acidic or basic?
5) if 1 and 4 are the same= more unionized; if different= ionized
What % of the drug is nonionized and ionized if pKa and pH are the same?
50/50
what is pKa?
dissociation constant
What processes are in phase 1 reactions and what do they do?
- oxidation- lose electron
- reduction- gain electron
- hydrolysis- split apart and add H2O
What carries out phase 1 reactions and what is the final product?
CP450- converts drug into polar metabolite
What is the phase 2 reaction?
Conjugation- adds polar, water soluble substrate to molecule to make it biologically inactive and ready for excretion
What are the enzymes involved in phase 2 reactions?
glucuronic acid, GST, N-acetyl-transferase, sulfotransferases
full agonist
drug has effect on receptor- high receptor affinity and high intrinsic activity- full effect
inverse agonist
binds to receptor and causes opposite effect
partial agonist
has high receptor affinity but only partial intrinsic activity
agonist-antagonist
partial agonists that also have antagonistic activity (may decrease effects of full agonists)
Antagonist
binds to receptor but blocks effect (no response)
Competitive vs non-competitive antagonist
competitive (can be reversed- ex Narcan); noncompetitive (cannot be reversed)
What tests evaluate effectiveness of heparin?
aPTT- normal is 30-35, therapeutic is 1.5-2x baseline)
ACT- normal is 90-120; therapeutic >300, <180 inadequate (measure baseline, 3 min out, and q30m after)
What tests evaluate effectiveness of warfarin?
PT- normal 10-14 seconds
INR- therapeutic 2-3
What monitors effectiveness of ASA?
no lab value- ASA is irreversible and lasts for lifetime of platelet (d/c 4-7 days preop)
What is bleomycin used for?
testicular cancer (blue balls)
What is a complication of bleomycin?
pulmonary toxicity (blebs)
Oxygen consideration with bleomycin?
maintain FiO2 below 30%
What is doxorubicin (adriamycin) used for?
mainly metastatic breast cancer (and others)
What is a complication of doxorubicin?
cardiotoxicity- may potentiate myocardial depressant effects of anesthetics