Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
22 Cards in this Set
- Front
- Back
|
Why biotransforming nesc?
|
renal excretion for water soluble drugs-most drugs not, bound to plasma protein-not filtered by kidney, need conversion to more water sol for excretion
|
|
|
biotransromation
|
conversion to a different entity
|
|
|
detoxification
|
toxic to nontoxic
|
|
|
bioactivation
|
inactive to active coumpound/reactive species
|
|
|
distribution of biotrans enazymes: major
|
liver, major site, [high], hi blood flow, portal circ, drug excretion
|
|
|
distribution of biotrans enazymes: minor
|
lung, kidney, intestine
|
|
|
distribution of biotrans enazymes: some
|
skin, gonads, all organs can biotrans, local biotran – terminate local drugeffect/bioactivation
|
|
|
biotrans function: liver
|
liver drug biotrans
|
|
|
biotrans function: adrenal
|
steriod synth
|
|
|
phase one
|
add, unmask functional group, oxidative(polysub monooxygenase), reductive, hydrolysis, peptidases
|
|
|
phase two
|
conjugate a functional group with water sol entity: glucuronide conj, sulfate conj, methltransferase, glutathione transferase, acylation
|
|
|
oxidative via polysub monoxygenase
|
P450, coupled to NADPH, bind substrate/activate O2, CYP1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1, 3A4
|
|
|
cyp450 reactions
|
propranolol, ibuprofen, morphine, nic/acetaminophen, chloropromazine, ampehtamine
|
|
|
polymorphism
|
gen factors control the amount of enzyme inactivated CYP2D6 notriptyline/codeine, 2C9 warfarin
|
|
|
phase one not p450
|
amine oxidase, alcohol/aldehyde dehydrogenase, ester hydrolysis, amide hydrolysis, peptidases
|
|
|
phase two reactions
|
glucuronide conj, sulfat conj, methyltransferase, glutathione transferase, acylation
|
|
|
enterohepatic circ
|
drugs conjugated and secreted via bile in intestine, conjugate cleaved by enzymes in gut, drug reabsorbed
|
|
|
first pass
|
oral drug-portal circ/liver, if extraction hi than amount reach systemic circ lower than expected, gut may biotransform also have transport back to lumen of guy, low abs than predicted from dose
|
|
|
biotrans results
|
inactivation/reduced effect, detox/less toxic, activation/active codeine, toxifcation/acetaminophin
|
|
|
inhibition of drug metab
|
induction, many drugs inhibit 450, 2 drugs when 1 inhibits the other, one will increase in plasma, graprefruit
|
|
|
stimulation of drug metab
|
phenobarbital stims 450, more enzyme to metab drug, cleared faster, low [plasma]/therapeutic response
|
|
|
biotrans: clinical importance
|
indiv diff, genetic/polymorphism, diet/enviro – cig/charcoal CYP1A, age low at birth/decr 55, sex diff, drug interactions, disease states
|
