1t is a chemical reaction that occur in the body to
maintain life.
METABOLISM
2Breaks down organic matter
Catabolism
3It uses energy to build up or
construct components of cells
such a proteins and nucleic
acids.
Anabolism
4DRUG METABOLISM aka
biotransformation
5Their pharmacologically active parent
compounds become detoxicated.
Inactive
Metabolites
6in Inactive
Metabolites
Hydrolysis of procaine to paminobenzoic acid and diethylamine
results in
loss of anesthetic acivity
7in Inactive
Metabolites
Oxidation of 6-mercaptopurine to 6-
mercatopuric acid results in
anticancer activity
8Retain the pharmacologic activity of
their parent compounds to a greater
or lesser degree
Metabolites
that retain
similar
activity
9what is the chemical reaction of procaine
hydrolysis
10what is the chemical reaction of 6 mercaptopurine
oxidation
11what is the chemical reaction of imipramine
demethylated
12what is the chemical reaction of acetohexamide
reduced
13what is the chemical reaction of codeine
demethylated
14what is the chemical reaction of antidepressant iproniazid
dealkylated
15what is the chemical reaction of vitamin a
isomerized
16what is the chemical reaction of vitamin retinoic acid
isomerized
17what is the chemical reaction of enalapril
hydrolyzed
18what is the chemical reaction of sulindac
reduced
19what is the chemical reaction of antiparkinsonian Levodopa
decarboxylated
20what is the therapeutic and product of procaine
para amino benzoic acid + diethylamine = loss of anesthetic
21what is the therapeutic and product of 6 mecaptopurine
6 mecaptopuric acid = loss of anticancer
22what is the therapeutic and product of imipramine
desipramine = antidepressant
23what is the therapeutic and product of acetohexamide
1 hydoxyhexamide = more hypoglycemic
24what is the therapeutic and product of iproniazifd
isoniazid= antitubercular
25what is the therapeutic and product of vitamin retinoic acid
isotretinoin acid = anti acne agent
26what is the therapeutic and product of enalapril
enalaprilat = potent antihypertensive
27what is the therapeutic and product of sulindac
sulfide
28what is the therapeutic and product of antiparkinsonian Levodopa
dopamine
29Develop different activity from that
of their parent compound
Metabolites
with altered
activity
30Pharmacologically inactive parent
compounds are converted to active
species within the body.
Bioactivated
metabolites
31parent compound aka
prodrugs
32in oxidation Majority occurs in the _____
liver
336 mammalian families are involved in the ______ and
bile _____ metabolism: and innumerate the 6 mammalian families
steroid and bile acid, CYP7, CYP11, CYP17, CYP21, CYP27
344 mammalian families are involved in _______ or _____: and innumerate the 4 mamalian
xenobiotics or drug, CYP1, CYP2, CYOP3, CYP4
35phase 1 in oxidation,it is Catalyzed by __________ bound to smooth ER
of the liver and require both _______ and a _______
cytochrome P450
,NADPH, porphyrin
prosthetic group.
36Enzyme responsible for transferring an Oxygen atom
to the substrate is called
cytochrome P450
37Plays a vital role in oxidation of
lipophilic xenobiotics
CYTOCHROME P-450
38Metabolizes almost unlimited
number of diverse substrates by
a
variety
of
oxidative
transformation
CYTOCHROME P-450
39CYTOCHROME P-450 is located in
Endoplasmic Reticulum
40Bacteria in the GIT are involved in the ______ and ______
reductions.
Azo , nitro
41To create more polar functional groups that can be
eliminated in the urine
reduction
42Addition of water across a bond resulting a more
polar metabolites.
ENZYMATIC HYDROLYSIS
43nonspecific and catalyze de-esterification, hydrolyzing
nonpolar to 2 polar, more water soluble compounds;
alcohol & aci; prodrugs into active forms
Esterase enzymes
44amides into amines and acids (deamination), occurs in
the liver
Amidase enzymes
45what are the common endogenous ?
sulfate, glycine , glucoronic acid
46Most conjugates are very polar resulting in __________
rapid drug
elimination