GCU NUR 635 midterm
Pharmacokinetics includes - absorption, distribution, metabolism, elimination
absorption of drugs factors - PH changes, gastric emptying, gastric enzymes, bile acids, GI flora, food and
nutrient interactions, lipid solubility
Where is cyp450 system found - endoplasmic reticulum of hepatocytes
CYP3A4/5 - most abundant CYP450 isoform which metabolizes the most prescribed
" "drugs. Especially important for bioavailability due to its abundance in
" "cells lining the GI tract. Can be induced by a wide variety of drugs "
"and is potently inhibited by ketoconazole and erythromycin.
CYP2D6 - metabolizes 25% of prescribed drugs
*3*4*5 majority of bad metabolizers
Antidepressants
Antipsychotics
Antiarrythmics
*carvedilol, *metoprolol
*codeine → morphine
*tamoxifen to active
CYP2c8/9 - warfarin
CYP1A2 - AcetAminophen
, CRAP GPS induces my rage - carbamazepine, rifampin,
alcohol, phenytoin, griseofulun, phenobarbitone, sulfonylureas
rectal admin has what absorption - variable and erratic
steady state (SS) is usually reached within how many half-lives of a drug - 4-5
zero-order(nonlinear) pharmacokinetics means a drug is metabolized - at a constant rate per unit time
Michaelis-menten pharmacokinetics - the rate of drug elimination is directly proportion to the
concentration of free drug (phenytoin)
theraputic index - TD50 = median toxic dose
ED50 = median effective dose
window = between those doses
safe drugs have a wider or high window/index
Agonist - drugs that alter the physiology of a cell by binding to plasma membrane or intracellular
receptors
Antagonists (drugs) - These drugs block the actions caused by agonists
off-label use - a drug can be used for an unapproved indication and is legitimate if there is clinical data
supporting its use for that indication
Pharmacokinetics includes - absorption, distribution, metabolism, elimination
absorption of drugs factors - PH changes, gastric emptying, gastric enzymes, bile acids, GI flora, food and
nutrient interactions, lipid solubility
Where is cyp450 system found - endoplasmic reticulum of hepatocytes
CYP3A4/5 - most abundant CYP450 isoform which metabolizes the most prescribed
" "drugs. Especially important for bioavailability due to its abundance in
" "cells lining the GI tract. Can be induced by a wide variety of drugs "
"and is potently inhibited by ketoconazole and erythromycin.
CYP2D6 - metabolizes 25% of prescribed drugs
*3*4*5 majority of bad metabolizers
Antidepressants
Antipsychotics
Antiarrythmics
*carvedilol, *metoprolol
*codeine → morphine
*tamoxifen to active
CYP2c8/9 - warfarin
CYP1A2 - AcetAminophen
, CRAP GPS induces my rage - carbamazepine, rifampin,
alcohol, phenytoin, griseofulun, phenobarbitone, sulfonylureas
rectal admin has what absorption - variable and erratic
steady state (SS) is usually reached within how many half-lives of a drug - 4-5
zero-order(nonlinear) pharmacokinetics means a drug is metabolized - at a constant rate per unit time
Michaelis-menten pharmacokinetics - the rate of drug elimination is directly proportion to the
concentration of free drug (phenytoin)
theraputic index - TD50 = median toxic dose
ED50 = median effective dose
window = between those doses
safe drugs have a wider or high window/index
Agonist - drugs that alter the physiology of a cell by binding to plasma membrane or intracellular
receptors
Antagonists (drugs) - These drugs block the actions caused by agonists
off-label use - a drug can be used for an unapproved indication and is legitimate if there is clinical data
supporting its use for that indication
