Pharmacology

Question 1

Initial enzyme-substrate interactions in active sites are typically ________

Answer 1

Non covalent (H-bonding, VDW, hyrdophobic, electrostatic)

Question 2

Active site excludes ______

Answer 2

bulk solvent which would reduce cat.

Question 3

Species Specificity (differential)

Answer 3

The likeliness of a drug to attack enzyme isoform in one species while leaving the host alone

Question 4

Two fundamental phenomena behind drug resistance

Answer 4

1. reduced intracellular concentration of drug

2. changes in drug target

Question 5

A flexible drug avoids

Answer 5

Drug resistance

Question 6

What mechanisms may cause reduced intracelluar concentration of a drug?

Answer 6

Drug inactivation, Prevention of drug uptake, Drug efflux

Question 7

What mechanisms are classisfied as target-based mechanisms

Answer 7

Altered drug target (receptor mutates), Bypassing metabolic requirements, insensitivity to apoptosis

Question 8

Activation of the receptor to signal as a result of binding

Answer 8

Agonists

Question 9

Drugs that bind to a receptor and block agonist from binding

Answer 9

antagonists

Question 10

Bind to an active receptor and turn it to an inactive/tense for

Answer 10

inverse agonist

Question 11

Pro-drug

Answer 11

utilizes a specific enzyme to transform inactive molecule to active form in vivo.

Question 12

Why use a pro-drug?

Answer 12

When absorption/cell permeation or manufacturing are issues. Also, used to target specific tissues

Question 13

Pharmacodynamic DDI

Answer 13

a drug-drug interaction that occurs at the receptor [additive, synergistic, antagonistic] (e.g. competitive inhibitor)

Question 14

Pharmacokinectic DDI

Answer 14

Affects the metabolism, absorption, excretion, or distribution of the drug.

Question 15

Suicide Inhibitors

Answer 15

bind covalently to the enzyme and reders it ineffective.

Question 16

Two phases of drug metabolism

Answer 16

(1) reactions (Redox, hydrolysis) to increase aqueous solubility accerates elimination
(2) reactions conjugate drug or metabolite to an endogenous substrate (acetice acid, amino acid, etc.)

Question 17

PM

Answer 17

poor metabolizers

Question 18

EM

Answer 18

extensive metabolizers

Question 19

IM

Answer 19

intermediate metabolizers

Question 20

Acute drug toxicity will most likely affect what organs?

Answer 20

liver, kidney, brain, heart

Question 21

Between an inhibitor and an inducer, which effects would be seen first?

Answer 21

Inhibitor. Inducer must bind to a promoter and upregulate protein synthesis at a target gene. (exception - suicide inhibitor)

Question 22

Ligand-Receptor binding creates

Answer 22

Hyperbolic saturation binding curve

Question 23

Enzyme Reaction creates

Answer 23

Hyperbolic Michaelis-Menten Plot

Question 24

Positive cooperativity

Answer 24

refers to ligand-receptor, increases binding aff. of OTHER SUBUNITS

Question 25

Allosteric activation

Answer 25

refers to enzyme reactions, increase affinity of active site on SAME SUBUNIT

Question 26

Negative cooperativity

Answer 26

ligand-receptor, decrease binding ability on OTHER SUBUNITS

Question 27

Allosteric inhibition

Answer 27

enzyme reaction, decreases binding ability on SAME SUBUNITS