Term
CYTOCHROMES P450
monooxygenations (?) diagram |
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Definition
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Term
CYTOCHROMES P450
monooxygenase reaction sequence
(diagram)
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Definition
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Term
CYTOCHROMES P450
two major types
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Definition
microsomal p450 enzymes
and
mitochondrial p450 enzymes |
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Term
| Microsomal p450 -> substrate |
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Definition
| NADPH ->nadph-cytochrome p450 reductase -> cytochrome p450 -> substrate |
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Term
| Mitochondrial p450 enzymes -> substrate |
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Definition
NADPH -> Adrenodoxin reductase -> adrenodoxin
-> cytochrome p450 -> substrate
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Term
Most of the human P450 belong to the
_____system.
This system include those involved in : (5) |
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Definition
Microsomal
1. drug metabolism
2. xenobiotic metabolism
3. steroid met.
4. fatty acid met.
5. elcosanoid met. |
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Term
| Human mitochondrial isoforms are found in ____ and are important for _____. |
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Definition
inner membrane of the mitchondrial matirx
steroid metabolism |
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Term
Human P450 families -> substrate
CYP:
1,2,3 |
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Definition
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Term
Human P450 families -> substrate
CYP:
4,5,8
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Definition
| fatty acids, prostaglandins, thromboxanes |
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Term
Human P450 families -> substrate
CYP:
7,11,17,19,21,24,27,39,46,51
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Definition
| steroid hormones/ cholesterol |
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Term
Human P450 families -> substrate
CYP:
20
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Definition
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Term
Human P450 families -> substrate
CYP:
26
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Definition
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Term
cytochromes p450 metabolize ____ substrates
(yeah vague) |
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Definition
| both endogenous and exogenous |
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Term
Cytochromes P450 metabolizes drugs via
2 pathways
phase I (______)
phase II (______) |
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Definition
fuctionalization reactions
biosynthetic reactions |
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Term
| describe phase I and phase II of p450 drug metabolism |
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Definition
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Term
Metabolism of drugs by c-P450
can have 1 of 3 effects |
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Definition
inactivation
activation
formation of a toxic metabolite |
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Term
Metabolism of drugs by c-P450
things to know about inactivation |
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Definition
active drug -> now inactive and lower bioavailability
can thus can lower harmful effects
for example: cyp3a4 is in the GI and Liver
and therefore there is a poor oral availability of many drugs
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Term
Metabolism of drugs by c-P450
things to know about activation |
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Definition
inactive drug is converted to its functional, desired form
for example: terfenadine is toxic to the heart but it is converted by cyp3a4 to its active form, fexofenadine. (there are substance, like grapejuice, that can inhibit cyp3a4. u can see a problem) |
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Term
Metabolism of drugs by c-P450
and formation of a toxic metabolite |
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Definition
read the tylenol story
(not sure if its important) page 69 of syl |
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Term
| What is a polymorphism effect: |
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Definition
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Term
not sure if u need to know about the polymorphism effect in ethopians and saudi arabian
(seems too specific)
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Definition
read page 70
it does help you understand the genetic polyporphisms
which is under clinical aspects |
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Term
c-p450's can be __________ by other drugs i.e. drug-drug reactions.
If the drugs are given with other drugs that are metabolized by p450 enzymes ________ |
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Definition
induced or inhibited
the lifetime of the drugs can be altered
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Term
| drug-drug example with cyp3e |
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Definition
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Term
a few of the many compounds
metabolized by p450
(11) |
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Definition
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Term
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Definition
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