Exam 1: Metabolism of Drugs

Question 1

The Chemical alteration of the drug molecule by the cells of the animal

Answer 1

Metabolism of drugs

Question 2

What are the 2 main effects of drug biotransformation

Answer 2

1. change in physicochemical properties of the drug

2. change in pharmacologic activity

Question 3

What is more common, Bioinactivation or bioactivation

Answer 3

Bioinactivation

Question 4

What is the main site of Biotransformation

Answer 4

Liver

Question 5

Other than the liver list some other tissues capable of biotransformation

Answer 5

Nervous tissue, Kidney, GI, lungs, skin, plasma

Question 6

What are the 4 types of biotransformation

Answer 6

1. Active drug to inactivated
2. Active drug to active metabolite
3. inactive drug to active metabolite
4. Nontoxic drug to toxic metabolite

Question 7

What are the two toxic metabolites in Antifreeze toxicity

Answer 7

Glycoaldehyde and glycoxylate

Question 8

Refers to large groupings of enzymes that tackle a variety of chemical substances

Answer 8

Microsomal enzymes

Question 9

T/F. Enzymatic rxns are not saturable

Answer 9

F

Question 10

Enzymes can be ____ or _____ by other drugs

Answer 10

induced or inhibited

Question 11

Microsomal enzymes cause what 4 things to glucuronic acid

Answer 11

1. Oxidation
2. reduction
3. hydrolysis
4. conjugation

Question 12

What are the 2 types of metabolic Rxns

Answer 12

1. Phase 1 rxns

2. Phase 2 rxns

Question 13

what are the 3 types of phase 1 rxns

Answer 13

1. Oxidation
2. Reduction
3. Hydrolysis

Question 14

What is the only type of phase 2 rxn.

Answer 14

conjugation

Question 15

What is another name for phase 2 rxns.

Answer 15

Synthetic

Question 16

What is another name for phase 1 rxn.

Answer 16

Nonsynthetic

Question 17

The loss of one or more electrons

Answer 17

oxidation

Question 18

The gain of one or more electrons

Answer 18

Reduction

Question 19

The splitting of a molecule into fragments by the addition of water

Answer 19

Hydrolysis

Question 20

Oxidation or reduction

Gain O2 or remove H+

Answer 20

Oxidation

Question 21

Oxidation or reduction

Gain H+ or Remove O2

Answer 21

Reduction

Question 22

What is the most common biotransformation

Answer 22

Oxidation

Question 23

T/F. all phase 1 products move on to phase 2

Answer 23

F

Question 24

Which type of drug must go through phase 2 prior to excretion

Answer 24

Lipid soluble

Question 25

What is a conjugation rxn.

Answer 25

combination of a drug or its metabolite with an endogenous substance

Question 26

Who is deficient in conjugation rxns.

Answer 26

Cats and neonates

Question 27

Metabolite conjugates are usually ____, _____, and _____

Answer 27

Inactive, Water soluble, and Non-toxic

Question 28

What is the one conjugation rxn that is microsomal

Answer 28

Glucuronidation

Question 29

Conjugation to ____ is the most common conjugation reaction

Answer 29

Glucuronic Acid

Question 30

Dogs are deficient in ____

Answer 30

Acetylating enzymes

Question 31

Ruminants have less plasma ______ than horses, dogs, or cats

Answer 31

pseudocholinesterase

Question 32

Pigs are deficient in ____ enzymes

Answer 32

sulfate conjugatin

Question 33

Birds lack ___ enzymes

Answer 33

Oxidative

Question 34

What is the 3 criteria of hepatic first pass metabolism

Answer 34

1. drug must go to liver before circ. 2. drug must be metabolized by the liver 3. must have high hepatic extraction ratio

Question 35

what is the result of hepatic first pass metabolism

Answer 35

drug metabolized before distribution

Question 36

Drug that stimulates the liver to produce more metabolic enzymes

Answer 36

Enzyme inducers

Question 37

Drugs that inhibit liver production of metabolic enzymes

Answer 37

Enzyme inhibitors

Question 38

Bioactivation transforms the drug into an _____ compound first

Answer 38

Active

Question 39

Lethal transformation transforms nontoxic drugs into ____

Answer 39

toxic

Question 40

T/F First pass metabolism results in dec. oral drug bioavailability

Answer 40

T