For midterm- PD&PK

Question 1

Racemic mixture

Answer 1

50:50 mixture of both enantiomers

Question 2

True or false: Local anesthetics bind to voltage activated (gated) sodium (Na+) channels to shorten the refractory period

Answer 2

False

Question 3

Which form of transfer of drugs across membranes dominates for most drugs
A. Active transport
B.Paracellular transport
C. Facilitated transport
D.Passive diffusion

Answer 3

Passive diffusion

Question 4

Decreased clearance of a drug could ______ the elimination half life

Question 5

Decreased distribution of a drug could _____ the elimination half life

Answer 5

decrease

Question 6

Secondary structure results from

Answer 6

Protein a.a interacting with other nearby a.a’s on same protein

Question 7

Tertiary structure results from

Answer 7

Interaction of more distant a.a’s along a.a

Question 8

Quaternary structure

Answer 8

Multiple polypeptides interact

Question 9

Order of bond strength

Answer 9

Covalent > ionic > hydrogen > van der waals

Question 10

Enantiomers

Answer 10

S: left handed
R: right randed
(based on organization around chiral centre)

Question 11

Racemic mixture

Answer 11

50:50 mix of both enantiomers

Question 12

Ranitidine: what is it and what is interesting about it

Answer 12

H2 (histamine receptor) antagonist or blocker
* Reduce Hcl production
* Limited effects in body due to restriction of H2 receptors in the
stomach

Question 13

Nicotinic acetylcholine receptor: what type of channel, how does it open and where is it found?

Answer 13

Ligand-gated channel

Question 14

Most important receptor type for drugs

Answer 14

Proteins

Question 15

Ion channels have key role in

Answer 15

-neurotransmission
-sm. & sk. muscle contraction
-cardiac contraction
-secretion

Question 16

Excitatory NTs

Answer 16

ACh or glutamate

Question 17

Inhibitory NTs

Answer 17

Glycine or GABA

Question 18

What binds to channel to prolong refractory period

Answer 18

Local anesthetics

Question 19

G-protein activated by

Answer 19

NTs, eicosanoids, peptides, opioids

Question 20

G-proteins work where

Answer 20

Over 50% - sensory perception

Remainder - nerve regulation, sm muscle tension, force/rate of cardiac contraction, secretion

Question 21

Major role of G proteins

Answer 21

Activate effector molecules, produce second messengers

Question 22

Hormones of a tyrosine-kinase associated receptor

Answer 22

Growth hormone, prolactin

Question 23

Nuclear hormone receptor (intracell.)

Answer 23

Circulating steroid hormone (lipophilic) –> diffuse thru PM –> bind TF –> modify nuclear events

Question 24

NO affect on cGMP

Answer 24

NO binds N-term coluble cGMP –> enhance cGMP amp

Question 25

2 major types of D-R relationships

Answer 25

Graded: D-R of an individual Quantal: D-R of a population of individuals

Question 26

Fraction of all available receptors that are ligand bound

Answer 26

[LR]/Ro

Question 27

Affinity of a drug is most influenced by changes in the _______ rate

Answer 27

Off

Question 28

Efficacy (Emax)

Answer 28

Maximal response produced by the drug at that receptor

Question 29

Potency (EC50)

Answer 29

Drug concentration which elicits 50% of the maximal response (Emax); function of affinity and efficacy

Question 30

Therapeutic index (TD50/ED50)

Answer 30

Estimate of relative safety margin of drug

Question 31

More potent drugs have a ______ affinity (______ Kd ) for their receptors

Answer 31

Greater affinity, lower Kd

Question 32

More efficacious drugs (larger Emax ) usually cause a _________ proportion of their receptors to be activated

Answer 32

Greater

Question 33

Partial agonist

Answer 33

Not able to achieve the same maximal response at a given receptor compared to a full agonist; even with increasing [agonist] BUT MAY SHOW GREATER POTENCY

Question 34

Types of receptor agonists

Answer 34

Reversible (competitive) Irreversible (non-competitive)

Question 35

Nonreceptor antagonists

Answer 35

Chemical antagonist Physiologic antagonist

Question 36

Increase in Kd does what to potency

Answer 36

Decrease

Question 37

What do noncompetitive antagonists do

Answer 37

Depress the maximal response or efficacy (Emax ), can also decrease potency