Flashcards in Drug metabolism Deck (116)
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1
Processes that prevent continuous drug action
elimination/excreation
metabolism
2
Drug metabolites are usually more ________ then the drug ingested thus easliy excreated
poloar
3
most drugs enter the body _______ thus are difficult to excrete
lipophilic
4
In most cases metabolism will take active drug-->
inactive metabolite
5
A drug that is converted to active form by drug metabolizing enZ
prodrug
6
a prodrug is inactive until
metabolized
7
the more drugs we take the more at risk we are for
adverse affects
8
Drugs withdrawn from the market often d/t this reason
drug-drug interactions d/t drug metabolism
9
These guys do oxidation, reduction, dealkylation or hydrolysis
Phase I enZ
10
This enZ will often introdue or reaveal a functional group
Phase I enZ
11
Phase I enZ actions
oxidation, reduction, dealkylation or hyrolysis and introduce or reveal a functional group
12
These guys have conjugation of durg or durg metaboliet to endogenous substrate molecule
Phase II enZ
13
responsible for : Drug + conjugant--> Drug-conjugant
Phase II enZ
14
CYPs are examples of
Phase I enx
15
CYPs will often
make lipophilic drugs more soluble in water
16
These guys add large, polar conjugates to make drug super water soluble
phase II
17
Common location for drug metabolizing agents
portals of entry/exit
liver (HIGHEST)
GI, kidneys, lungs
18
Subcellularly where are the Phase I enZ located ?
In the SER microsomes
19
Subcellularly, where are phase II enZ located?
most are cytosilc
20
What venous system will take drugs to liver from the GI system
portal venous sytem
21
What drug administration is exposed to 1st pass effect
orally administered
22
Significant drug metabolism can occur before reaching general circulation d/t
first pass in intestines and liver
23
Drugs exposed to 1st pass will need _____ dose
higher
24
bioavialibty will ______ d/t first pass
lower F
25
F for IV administration
1 or 100%
26
What are two reasons for poor F
poor absorption or large first pass effect
27
Morphines's F d/t first pass
.33
28
If i gave IV dose of 10 mg of morphine to relieve pain, what oral dose would i need to match that?
30 mg
29
Two key Phase I enZ
Cytochrome P450s = CYPs
Flavin-containing monooxygenases
30
