Unit 1

Question 1

Study of substances that interact with living systems through chemical processes by binding to regulatory molecules and activating/inhibiting normal body processes

Answer 1

Pharmacology

Question 2

Science of substances used to prevent/diagnose/treat disease

Answer 2

Medical Pharmacology

Question 3

Branch of pharmacology dealing with undesirable effects of chemicals on living systems

Answer 3

Toxicology

Question 4

Body to Drug; Absorption, distribution, elimination of drugs

Answer 4

Phamacokinetics

Question 5

Actions of chemical on organism

Answer 5

Pharmacodynamics

Question 6

Science of drug preparation and the medical uses of drugs, precursor to pharmacology developed around end of 17th century

Answer 6

Material Medica

Question 7

Developed experimental physiology and pharmacology

Answer 7

Francoi Magendi

Question 8

began to develop the methods of experimental physiology and pharmacology

Answer 8

François Magendie and his student Claude Bernard

Question 9

Biological substrate of drug action

Answer 9

Receptor

Question 10

Receptors for which no ligand has been discovered and whose function can only be surmised

Answer 10

Orphan Receptor

Question 11

Relation of individuals genetic makeup and response to specific drugs, relationships between receptor families and evolution of receptor proteins

Answer 11

Pharmacogenomics

Question 12

(2) small segments of RNA that interfere with protein synthesis with extreme selectivity

Answer 12

SiRNAs and miRNAs
Small interfering RNAs and micro RNAs

Question 13

short nucleotide chains synthesized to be complementary to natural RNA/DNA, can interfere with readout of genes and transcription of RNA

Answer 13

ANOs
Antisense oligonucleotides

Question 14

Any substance that brings about change in biological function through chemical actions

Answer 14

Drug

Question 15

Interact with other drugs directly

Answer 15

Chemical Antagonist

Question 16

Interact exclusively with water molecules

Answer 16

Osmotic Agents

Question 17

Drugs that are exclusively harmful

Answer 17

Poison

Question 18

Poisons of biological origin, synthesized by plants/animals

Answer 18

Toxin

Question 19

Very weak, important for highly lipid soluble drugs

Answer 19

Hydrophobic Bonds

Question 20

True or False: drugs that bind weakly to receptors are more selective

Answer 20

True

Question 21

Drugs with 2 chiral centers have __ diastereomers

Answer 21

4

Question 22

True or False: an entantiomer has different potency than another according to best fit and duration

Answer 22

True

Question 23

True or False: most drugs are one active isomer rather than a racemic mixture

Answer 23

False

Question 24

Kd, concentration for 50% saturation of receptors, inversely proportional to affinity of drug for receptors

Answer 24

dissociation constant

Question 25

Makes final change and may be in receptor molecule or separate, sometimes with a coupling mechanism

Answer 25

Effector

Question 26

Bind and activate receptor to directly/indirectly cause effect

Answer 26

Agonist

Question 27

Bind receptor to compete and prevent binding by other molecules

Answer 27

Antagonist

Question 28

True or False: action of the antagonist can be overcome by increasing dosage of the agonist

Answer 28

True

Question 29

Bind to same receptor but don't prevent agonist from binding; may enhance or inhibit action of agonist

Answer 29

Allosteric Drugs

Question 30

True or False: action of allosteric drug can be overcome by increasing agonist concentration

Answer 30

False

Question 31

Thermodynamic property; in absence of agonist some receptors are in active form and have same effect as agonist-induced activity

Answer 31

Constitutive Activity

Question 32

Constitutive activity depends on receptor _____, concentration of ____ molecules, and number of _____

Answer 32

Density, coupling, effectors

Question 33

At saturating concentration activate receptor-effector systems to max extent and shift all receptors to active pool

Answer 33

Full Agonist

Question 34

Bind same receptors and activate but do not evoke same response regardless of concentration, don't fully stabilize active receptor form as effectively, low intrinsic activity of

Answer 34

Partial Agonist

Question 35

True or False: partial agonists act as agonists if no full agonist is present or antagonist if full agonist is present

Answer 35

True

Question 36

Fix fraction of active and inactive receptor in same amounts as if there were no drug present, no change in activity is observed, prevent agonist action

Answer 36

Antagonist

Question 37

Drug has stronger affinity for inactive receptor than active, reduced constitutive activity and result in opposite effect of agonists

Answer 37

Inverse Agonist

Question 38

Not until the concepts of rational therapeutics, especially that of the __________, were reintroduced into medicine—only about 60 years ago—did it become possible to adequately evaluate therapeutic claims.

Answer 38

controlled clinical trial

Question 39

3 General Principles

Answer 39

1) that all substances can under certain circumstances be toxic; 2) that the chemicals in botanicals (herbs and plant extracts, “nutraceuticals”) are no different from chemicals in manufactured drugs except for the much greater proportion of impurities in botanicals; and 3) that all dietary supplements and all therapies promoted as health-enhancing should meet the same standards of efficacy and safety as conventional drugs and medical therapies

Question 40

T/F: there should be artificial separation between scientific medicine and “alternative” or “complementary” medicine.

Answer 40

False, there should be no artificial separation

Question 41

To interact chemically with its receptor, a drug molecule must have the (4)

Answer 41

appropriate size, electrical charge, shape, and atomic composition.

Question 42

aspirin, atropine

Answer 42

solid drugs

Question 43

nicotine, ethanol

Answer 43

liquid drugs

Question 44

nitrous oxide, nitric oxide, xenon

Answer 44

gaseous drugs

Question 45

fluoride, lithium, iron, and heavy metals

Answer 45

inorganic elements

Question 46

T/F Many organic drugs are weak acids or bases

Answer 46

True

Question 47

What is the range of MW most drugs have?

Answer 47

100 - 1000

Question 48

To achieve such selective binding, it appears that a molecule should in most cases be at least __ MW units in size

Answer 48

100

Question 49

T/F Drugs much larger than MW 1000 do not diffuse readily between compartments

Answer 49

True

Question 50

T/F: Very large drugs (usually proteins) must often be administered orally into the compartment where they have their effect

Answer 50

False, it is administered directly

Question 51

3 Major types of Chemical forces/bonds:

Answer 51

Covalent, Electrostatic, Hydrophobic

Question 52

vary from relatively strong linkages between permanently charged ionic molecules to weaker hydrogen bonds and very weak induced dipole interactions

Answer 52

Electrostatic Bonds

Question 53

the phenomenon of _____ is so common in biology that more than half of all useful drugs are chiral molecules; that is, they can exist as enantiomeric pairs.

Answer 53

chirality (stereoisomerism)

Question 54

implies the ability to predict the appropriate molecular structure of a drug on the basis of information about its biologic receptor.

Answer 54

Rational drug design

Question 55

Drug (D) + ___ → drug-receptor-effector complex → effect

Answer 55

receptor-effector (R)

Question 56

D + R → drug-receptor complex → __ → effect

Answer 56

effector molecule

Question 57

D + R → D-R complex → activation of __ → effector molecule → effect

Answer 57

coupling molecule

Question 58

Inhibition of metabolism of __ → increased activator action on an effector molecule → increased effect

Answer 58

endogenous activator

Question 59

final change in function is accomplished by an__.

Answer 59

effector mechanism

Question 60

Some drugs mimic agonist drugs by __ the molecules responsible for terminating the action of an endogenous agonist

Answer 60

inhibiting

Question 61

This effect, occurring in the absence of agonist, is termed

Answer 61

constitutive or basal activity

Question 62

the presence of the antagonist at the receptor site will block access of agonists to the receptor and prevent the usual agonist effect. Such blocking action can be termed as

Answer 62

neutral antagonism

Question 63

the drug will reduce any constitutive activity, thus resulting in effects that are the opposite of the effects produced by conventional agonists at that receptor. Such drugs are termed as

Answer 63

inverse agonists

Question 64

To function as a receptor, an __ molecule must first be selective in choosing ligands (drug molecules) to bind

Answer 64

endogenous

Question 65

an inactive precursor chemical that is readily absorbed and distributed must be administered and then converted to the active drug by biologic processes—inside the body. Such a precursor chemical is called a

Answer 65

prodrug

Question 66

This requires that the drug be __ into the blood from its site of administration and __ to its site of action, __ through the various barriers that separate these compartments.

Answer 66

absorbed, distributed, permeating

Question 67

__ can be very important in facilitating transport and permeation, eg, by encapsulating the active agent in liposomes and in regulating release, as in slow release preparations.

Answer 67

Drug vehicles

Question 68

Drugs may diffuse passively through (4)

Answer 68

1. Aqueous Diffusion 2. Lipid Diffusion 3. Special Carriers 4. Endocytosis and Exocytosis

Question 69

This diffusion occurs within the larger aqueous compartments of the body (interstitial space, cytosol, etc) and across epithelial membrane tight junctions and the endothelial lining of blood vessels

Answer 69

Aqueous Diffusion

Question 70

most important limiting factor for drug permeation because of the large number of lipid barriers that separate the compartments of the body

Answer 70

Lipid diffusion

Question 71

These exist for many substances that are important for cell function and too large or too insoluble in lipid to diffuse passively through membranes, eg, peptides, amino acids, and glucose

Answer 71

Special carrier molecules

Question 72

This process is responsible for the transport of vitamin B12, complexed with a binding protein (intrinsic factor) across the wall of the gut into the blood.

Answer 72

Endocytosis

Question 73

responsible for the secretion of many substances from cells.

Answer 73

exocytosis