Term
|
Definition
| enzymatic modification of a drug |
|
|
Term
| The goal of metabolism to to convert molecules into___more suitable for___ |
|
Definition
| Polar forms for Elimination |
|
|
Term
T/F
All drugs are extensively metabolized |
|
Definition
|
|
Term
T/F
Metabloism occurs only in tissues such as the liver |
|
Definition
FALSE
it is rare but it can occur in the blood |
|
|
Term
| What are the 3 categories of metabolites that drugs are turned into? (activity) |
|
Definition
Active:Therapeutic Action
Inactive: Excretion
Toxic: Tissue damage/Cancer |
|
|
Term
T/F
Once metabolized a drug has either more/less therapuetic activity |
|
Definition
FALSE
The metabolism can have no effect on the parent drug
ex. aspirin |
|
|
Term
Phase I/II
A) Oxidation
B)Glucuronidation
C)Reduction
D)Hydrolyses |
|
Definition
Oxidation- I
Glucuronidation-II
Reducation-I
Hydrolyses-I |
|
|
Term
Which phase attaches small polar molecules?
Which attaches OH grps? |
|
Definition
Phase II-small polar molecules
Phase I- OH grps |
|
|
Term
| How can we predict drug metabolism? |
|
Definition
|
|
Term
| Which subcellular sites of metabolism are membrane bound? |
|
Definition
Smooth ER (microsomal)
Mitochondria |
|
|
Term
Microsomal, Cytoplasmic, or Mitochondrial
A) CYP enzymes
B)Alcohol metabolism
C)MAO enzymes
D) Glucuronidation |
|
Definition
A) CYP enzymes Microsomal
B)Alcohol metabolism Cytoplasmic
C)MAO enzymes Mitochondrial
D) Glucuronidation Microsomal |
|
|
Term
| What provides electrons to the CYP reductase? |
|
Definition
|
|
Term
| Each cycle of CYP adds how many O? |
|
Definition
|
|
Term
T/F
The oxene species is very electron deficient |
|
Definition
TRUE
It is highly reactive and e- deficient |
|
|
Term
| What gives the CYP enzyme its O binding ability? |
|
Definition
| The heme group in the active site |
|
|
Term
| CYP 450 catalyzes which reactions? |
|
Definition
aromatic hydroxylation
aliphatic hydroxylation
dealkylation
epoxidation
Oxidation (S, N) |
|
|
Term
| Alcohols are converted to____ and then into_____ |
|
Definition
| aldehydes then carboxylic acids |
|
|
Term
| Why is ethanol administered for methanol toxicity? |
|
Definition
| The ethanol is a competitive inhibitor for the rxn and will get metabolized before the methanol |
|
|
Term
| Which step in the rxn causes a hangover? |
|
Definition
| when ethanol is converted into acetaldehyde |
|
|
Term
T/F
MAO rxns are intended for elimination |
|
Definition
FALSE
they are not intended to be eliminated |
|
|
Term
| What reactions are catalyzed by MAO? |
|
Definition
| oxidative deamination of endogenous amines and some drugs |
|
|
Term
| What 2 enzymes are involved in alcohol metabolism? |
|
Definition
alcohol dehydrogenase
aldehyde dehydrogenase |
|
|
Term
T/F
Esterases and Amidases need water to carry out their reactions |
|
Definition
TRUE
they are hydrolysis reactions |
|
|
Term
T/F
Glucuronindation is very common and a readily available cofacter |
|
Definition
|
|
Term
T/F
Glucuronidation occurs with inversion of stereochemistry
What does this mean? |
|
Definition
TRUE
UDP is in the alpha(bottom) position and the substrate comes in from the beta (top) position and UDP is removed |
|
|
Term
| What is the purpose of adding Glucuronic Acid to a substrate? |
|
Definition
| It dramatically increases the polarity of the substrate |
|
|
Term
| Which atoms are substrates for Glucuronidation? |
|
Definition
|
|
Term
T/F
Phenol is a common site for glucuronidation |
|
Definition
|
|
Term
T/F
Glucuronidation occurs in aliphatic and aromatic Carbons |
|
Definition
FALSE
Glucuronidation is very restricted |
|
|
