Pharm Exam 1 (1-2)

Question 1

MoA

Answer 1

a cell signaling system or process that is impacted by a drug through its interaction with a specific molecular target

Question 2

There are of three major types of chemical forces or bonds

Answer 2

covalent (strong bonds)
electrostatic (ionic bonds)
hydrophobic (weak bonds)

Question 3

affect a single organ or system (e.g.,digoxin, sleep aids)

Answer 3

Highly selective drugs

Question 4

affect targeted areas (e.g., NSAIDs such asaspirinandibuprofen

Answer 4

Relatively selective drugs

Question 5

affect many different tissues or organs (e.g.,atropine)

Answer 5

Relatively nonselective drugs

Question 6

the degree to which a drug acts on a given site relative to other sites

Answer 6

Drug selectivity

Question 7

poisons of biologic origin, synthesized by plants or animals

Answer 7

Toxins

Question 8

a term used to describe the processes of metabolism and excretion

Answer 8

Biodisposition

Question 9

“-cillin” “-olol” “-mab”

Answer 9

group is all penicillins (antibiotics)
group is all the β-blockers
monoclonalantibodies

Question 10

mumab, zumab, ximab, omab, -ib

Answer 10

For monoclonal antibodies, the two letters preceding the “mab” are used to indicate whether the antibody is fully humanized (-mumab), has the antigen-binding region from a mouse antibody (-zumab), is a chimeric with human and mouse parts (-ximab), or is entirely mouse (-omab) - the two letters before these are supposed to indicate the organ system that is the target for the antibody
You should be able to identify that the drug is a monoclonal antibody or kinase inhibitor
“-ib” drugs (most commonly -nib), which are (mostly) kinase inhibitors and sometimes called small molecule inhibitors

Question 11

The Interaction (bond) Types

Answer 11

1. Covalent Bonds (see next slide)
2. Non-covalent Bonds
   a. Ionic Bonds
   b. Dipole Interactions
   c. Hydrogen Bonds: a specialized type of Dipole-Dipole bond
   d. van der Waals Interactions
   e. Hydrophobic Bonding
   f. Chelation and Complexation
   g. Charge Transfer Interactions

Question 12

dihydrofolate reductase, the receptor for the antineoplastic drug methotrexate is what

Answer 12

Enzyme

Question 13

ligand gated channels and voltage gated channels are what

Answer 13

Ionotropic receptors or ion channels

Question 14

G-protein coupled receptors that bind to endogenously produced hormones, neurotransmitters are what

Answer 14

Metabotropic receptors

Question 15

receptors for various growth factors and thus for some anticancer drugs are what

Answer 15

Kinase linked and related receptors

Question 16

receptors for thyroid hormone, some fat-soluble vitamins and steroids are what

Answer 16

Nuclear receptors

Question 17

tubulin, the receptor for colchicine, an anti-inflammatory agent are what

Answer 17

Cytoskeletal or structural proteins

Question 18

Na+-K+ ATPase, the receptor for cardiac glycosides is what

Answer 18

Transporters or carrier proteins

Question 19

Nucleic acids (DNA, RNA), membranes, and fluid compartments are what

Answer 19

non-protein receptors

Question 20

Emax

Answer 20

Maximal Response

Question 21

EC50

Answer 21

the concentration of drug producing 50% of Emax

Question 22

agonists such as ______ could produce a maximal tissue response at extremely low receptor occupancies

Answer 22

histamine

Question 23

The overall transduction process that links drug occupancy of receptors and pharmacologic response is called _____
______ is also determined by “downstream” biochemical events that transduce receptor occupancy into cellular response.

Answer 23

Coupling

Question 24

a measure of the favorability of a drug–receptor interaction

Answer 24

Affinity

Question 25

mimic the physiologic agonist, e.g., isoproterenol (β-adrenergic agonist).

Answer 25

Full agonists

Question 26

activate receptors but are unable to elicit the maximal response of the receptor system; e.g., Dobutamine (β-adrenergic receptor).

Answer 26

Partial agonists

Question 27

cause constitutively active targets to become inactive; e.g., antihistamines are considered as ______ of H1 receptor

Answer 27

Inverse agonists

Question 28

Examples: ACEI, rennin inhibitors, angiotensin receptor inhibitors.

Answer 28

Competitive inhibitor occupies the active site and prevents binding of the physiological (i.e. endogenously produced) ligands

Question 29

inhibitors of acetylcholine esterase such as physostigmine, neostigmine etc., cyclooxygenase (COX) inhibition by aspirin, phenoxybenzamine antagonism of α-adrenergic receptor.

Answer 29

Non-competitive or irreversible inhibitor covalently binds at the active site of the enzyme and irreversibly inhibits it

Question 30

nonnucleotide reverse transcriptase inhibitors, antihistamines binding to histamine H1 receptor

Answer 30

Allosteric inhibitor binds at sites other than the active site, causing a conformational change in the enzyme that prevents it from binding to its physiological substrate

Question 31

Aspirin and proton pump inhibitors (esomeprazole, omeprazole)

Answer 31

Irreversible Antagonism

Question 32

histamine acts on receptors of the parietal cells of the gastric mucosa to stimulate acid secretion, while omeprazole blocks this effect by inhibiting the proton pump; the two drugs can be said to act as _________

Answer 32

Physiological antagonists

Question 33

(e.g., Phenobarbital reducing the anticoagulant effect of warfarin this way), impaired absorption from GI tract or enhancement of renal excretion.

Answer 33

Pharmacokinetic antagonists

Question 34

This mixed “agonist-antagonist” property of

Answer 34

Partial agonists 

Question 35

refers to the concentration (EC50) or dose (ED50) of a drug required to produce 50% of that drug’s maximal effect. 

Answer 35

Potency

Question 36

defined as the ratio of the TD50 to the ED50 

Answer 36

Therapeutic Index (TI)

Question 37

The range between the minimum toxic dose and the minimum therapeutic dose is called the 

Answer 37

therapeutic window 

Question 38

unusual and infrequent response mostly due to genetic factors

Answer 38

Idiosyncratic drug response