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pharm L4 drug action metabolism.txt
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Four characteristics of active drugs
lipid soluble
unionized
plasma protein bound
not excreted easily by kidneys
What is a highlight of Phase III drugs?
They are secreted back into the gut via P glycoproteins
What % of a drug is commonly an inactive metabolite?
90%
Why is Isoniazid (INH) a special drug when it comes to Phase I & II rxns.?
It goes through phase II then Phase I
What is the main organ that biotransforms drugs?
Liver
what are the roles of Phase I and Phase II rxns on drugs?
Phase 1
: modification of molecule
Phase II
: conjugation of molecule
T/F A Lipid soluble molecule will become less polar after Phase I modification?
F, it will become more polar (less lipid soluble)
What are three outcomes of a drug after a phase II rxn.?
Larger molecule
More Polar molecule
Less biological activity
What happens to drugs with a molecule weight >350 and <350?
>350 = excreted into bile, metabolized and reabsorbed by gut (possibly)
<350 = excreted into blood, kidney, and removed
Organ that metabolizes
chlorpromazine & Clonazepam?
Intestine
Organ that metabolizes
Penicillin-G & Erythromycin
?
Stomach (gastric acid)
Organ that destroys
Insulin & Polypeptides
?
Stomach (Gastric juices)
Organ that inactivates
epi & norepi & other catecholamines
?
Intestinal Wall
What is a
Microsomal Rxn
?
Phase I Rxn
** microsomal = chopped ER
What is the bodies main microsomal Rxn?
Cytochrome P450
What does CYP1A2 do in the Cytochrome P450 system?
Metabolizes smoke, acetaminophen, grilled foods, etc...
What is the largest Cytochrome P450 metabolizer of drugs?
CYP3A4
What phase Rxn are non-microsomal metabolites that are non-inducible?
Phase 1
Are Esterases/Amidases microsomal or non-microsomal?
Non
2 Examples of Esterase and Amidase?
Pseudocholinesterase - genetic polymorphism
Lidocaine
Are Monoamine oxidase non-microsomal or microsomal?
Non
Main example of monoamine oxidases?
Endogenous amine - Tyramine (cured foods)
Are Alcohol & aldehyde dehydrogenase non-microsomal or microsomal?
Non
What is the cellular result of Phase II rxns?
Large molecule
More polar
inactive
What is the only Phase II rxn that is microsomal and inducible?
Glucoronidation
Name the 7 types of Phase II Rxns
Glucoronidation
Acetylation
Methylation
Glutathione conjugation
Glycine conjugation
Sulfate conjugation
Water conjugation
How does enterohepatic circulation help with drug reabsorption?
Bacterial enzymes split conjugate for reabsorption
increase drug half-life
Do you increase or decrese a drug dose for a fast or slow metabolizer?
Fast metabolizer = more drug
Slow metabolizer = less drug
What are four drugs that require biological variation?
INH
Mephenytoin
Warfarin
Succinylcholine
Why do young children react differently to drugs?
Permeable BBB
Decreased liver function
Decreased renal excretion
In the elderly, what is the path of reduced drug metabolism?
Kidney > phase I > Phase II in Liver
What is the Sex difference for ethanol?
Ethanol concentration in males is higher than females b/c we have more water
What are the two main diseases that modify drug metabolism?
Liver and Renal disease
Common pathway of metabolites in kidneys?
Glomerular filtration
Secretion or reabsorption
Diffusion across tubular epithelium
Author
matthewgraff
ID
103832
Card Set
pharm L4 drug action metabolism.txt
Description
pharm 4
Updated
2011-09-23T15:59:50Z
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