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Metabolism and Excretion

Terms in this set (21)

Most biotransformation occurs in the _____.
Liver
Results of Biotransformation:
-activate an inactive drug
-inactivate an active drug
-convert active drug to active metabolite
-convert active drug or metabolite to toxic metabolite
T/F.
metabolites are usually more polar, H20 soluble, excreted faster than parent drug
True
What is in phase I of chemical transformation?
-oxidation
-reduction
-hydrolysis
What is in phase II of chemical transformation?
conjugation/synthesis
microsomal enzymes refer to ____
smooth ER
are microsomal enzymes inducible?...in other words, can we make more if we need them?
yes
non-microsomal enzymes are located where?
cytosol, mitochondria, and plasma
are non-microsomal enzymes inducible?...in other words, can we make more if we need them?
No
2 microsomal enzymes
NADPH-cytochrome P450 reductase
Cytochrome P450 (CYP or P450)
What is the location of NADPH-cytochrome P450 reductase and Cytochrome P450 (CYP or P450)?
smooth ER of most cells. abundant in the liver
CYP3A4:
CYP means?
cytochrome p450
CYP3A4:
3 means?
what family its in
CYP3A4:
A means?
subfamily
CYP3A4:
4 means?
isoform
4 things needed for a p450 oxidation reaction?
-NADPH-cytochrome P450 reductase (a flavoprotein)
-Cytochrome P450 (serves as the terminal oxidase)
-NADPH (the reducing agent)
-Nicotinamide adenine dinucleotide phosphate
-Molecular oxygen
Factors that influence the rate of biotransformation:
Enzyme inducers (smoking, environmental agents, drugs)
Enzyme inhibitors (competing drugs)
Age
Liver function/disease
Nutritional state
Genetics (acetylation)
Gender
Major routes of drug excretion?
Urinary excretion
Fecal excretion
Pulmonary (exhalation) excretion
Minor routes of drug excretion?
-CSF
-Milk
-Sweat and saliva
More chemicals are eliminated from the body by this route than by any other?
Urinary excretion
Finish Later
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