Medicinal Chemistry Lec 7

Front 1

Any substance foreign to the body can undergo metabolism.

Back 1

(xenobiotic)

Front 2

Drug metabolism occurs primarily in the ________.

Back 2

Liver

Front 3

Drug metabolism may also occur in extrahepatic sites such as:

Back 3

intestine, kidney, lungs, nervous tissues, brain or plasma

Front 4

What is the purpose of phase I&II Rxns?

Back 4

Phase I & II reactions convert lipophilic molecules → more water-soluble metabolites for excretion in urine

Front 5

What is the principal organ for elimination of drugs?

Back 5

Kidney

Front 6

drug metabolism can be predicted & relies on nature of functional group(s) present in drug molecule. T/F?

Back 6

True

Front 7

Chemical modification (hydroxylation, etc) to enable addition functional group for conjugation (introduction of new functional group to molecule)

Back 7

Phase I

Front 8

Conjugation of –OH (glucoronidation/sulfonation. etc) -> water-soluble compound excreted in urine

Back 8

Phase II

Front 9

Which part of drug metabolism is (mostly cytochrome P450 (P450 or CYP) enzyme catalyzed)?

Back 9

Phase I

Front 10

In all cases phase I Rxns proceeds phase II Rxns. T/F?

Back 10

False
In most cases phase I reactions precede phase II reactions but not all

Front 11

Several factors influencing drug metabolism include:

Back 11

Genetic factors
Physiological factors
Pharmacodynamic factors
Environmental factors

Front 12

Study that links individual’s genotype and individual’s ability to metabolize a xenobiotic

Back 12

Pharmacogenetics

Front 13

What prosthetic group is linked to P450? and how is it linked?

Back 13

Heme linked via cystine

Front 14

What is the Major alcohol-oxidizing enzyme?

Back 14

ADH

Front 15

important metabolic reaction of drugs whose structure contain ester & amide groups

Back 15

Hydrolysis via Hydrolases

Front 16

Phase II metabolic reactions are usually catalyzed by a specific ________.

Back 16

transferase enzyme

Front 17

Which Rxn is the most important of all phase II reactions ?

Back 17

Glucoronidation

Front 18

_________ conjugates a wide variety of drugs/xenobiotics possessing electrophilic centers

Back 18

Glutathione

Front 19

What is the end product of Glutathione Conjugation which gets eliminated from the body?

Back 19

Mercapturic acid derivatives

Front 20

What is an alternative metabolic route of phenols & occasionally some alcohols & amines?

Back 20

Sulfate conjugation

Front 21

Which Rxn is important for metabolizing, solubilizing and eliminating Carboxylic Acids through urine?

Back 21

Amino Acid Conjugation

Front 22

Which Rxn(s) reduce pharmacologic activity rather than improving solubility?

Back 22

Methylation & Acetylation