I.A. Introduction: The Nature of Drugs & Drug Development & Regulation

Question 1

can be defined as the study of substances that
interact with living systems through chemical processes

Answer 1

Pharmacology

Question 2

defined as the science of substances used to prevent, diagnose, and
treat disease

Answer 2

medical pharmacology

Question 3

the branch of pharmacology that deals with the undesirable effects of chemicals on living systems, from individual cells to humans to complex ecosystems

Answer 3

Toxicology

Question 4

aimed at understanding the actions of drugs as chemicals on individualorganisms, especially humans and domestic animals

Answer 4

medical pharmacology and toxicology

Question 5

deals with the absorption, distribution, and elimination of drugs

Answer 5

Pharmacokinetics

Question 6

concerns the actions of the chemical on the organism

Answer 6

Pharmacodynamics

Question 7

concerned with the effects of chemicals on all organisms and their survival in groups and as species

Answer 7

environmental toxicology

Question 8

the science of drug preparation and the medical uses of drugs

Answer 8

materia medica

Question 9

the relation of the individual’s genetic makeup to his or her response to specific drugs

Answer 9

Pharmacogenomics

Question 10

T/F

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

Answer 10

true

Question 11

defined as any substance that brings about a change in biologic function through its chemical actions

Answer 11

drug

Question 12

the drug molecule interacts as an ___ or ___ with a specific target molecule that plays a regulatory role in the biologic system.

Answer 12

agonist (activator) or antagonist (inhibitor)

Question 13

target molecule is called a ___

Answer 13

receptor

Question 14

are drugs that have almost exclusively harmful effects

Answer 14

Poisons

Question 15

defined as poisons of biologic origin

Answer 15

Toxins

Question 16

most drugs have molecular weights between ___

Answer 16

100 and 1000

Question 17

Drugs interact with receptors by means of ___

Answer 17

chemical forces or bond

Question 18

3 major types of bonds

Answer 18

covalent
electrostatic
hydrophobic

Question 19

___ bonds are very strong and in many cases
not reversible under biologic conditions.

Answer 19

Covalent

Question 20

___ is much more common than covalent
bonding in drug-receptor interactions

Answer 20

Electrostatic bonding

Question 21

are usually quite weak and are probably important in the interactions of highly lipid-soluble drugs with
the lipids of cell membranes and perhaps in the interaction of drugs with the internal walls of receptor “pockets.”

Answer 21

Hydrophobic bonds

Question 22

drugs that bind through weak bonds to their receptors are generally more ___ than drugs that bind by means of very strong bonds

Answer 22

selective

[because weak bonds require a very precise fit of the drug to its receptor
if an interaction is to occur]

Question 23

a drug that interacts with adrenoceptors

Answer 23

carvedilol

Question 24

Area of pharmacology concerned with the use of
chemicals in the prevention, diagnosis, and
treatment of disease, especially in humans

Answer 24

MEDICAL PHARMACOLOGY

Question 25

Area of pharmacology concerned with the undesirable effects of chemicals, whether it is a drug or poison, on biologic systems

Answer 25

TOXICOLOGY

Question 26

the relation of the individual’s genetic makeup to his or her response to specific drugs

Answer 26

PHARMACOGENOMICS

Question 27

Any substance that brings about a change in biologic function through chemical actions

Answer 27

DRUG

Question 28

Hydrophobic bonds are usually quite ___

Answer 28

weak

Question 29

___ MW For selective binding

Answer 29

100

Question 30

___ MW For traversing to different barriers of the body

Answer 30

1000

Question 31

Cannot move within the body because of impediments ____ MW

Answer 31

>1000

Question 32

Aspirin binds to the ___

Answer 32

platelets

Question 33

The tendency of a drug that binds to a receptor via a covalent bond is to have a ___ bond

Answer 33

permanent

Question 34

a process to prevent and stop bleeding in the body.

Answer 34

Hemostasis

Question 35

Activates receptor-effector system to the maximum extent (Ra-D pool){activated form}

Answer 35

Full agonist

Question 36

Binds to the same receptors and activate them in the same way but do not evoke as great a response

Answer 36

Partial agonist

Question 37

Binds to a site on the receptor molecule separate from the agonist binding site

Answer 37

Allosteric modulators

Question 38

Enzymes are a class of ___

Answer 38

receptors

Question 39

they could bind together with the agonist

Answer 39

allosteric modulators

Question 40

Results in effects that are opposite of the effects produced by conventional agonists

Answer 40

Inverse agonist

Question 41

Binds to a receptor, compete with and prevent binding by other molecules

Answer 41

Antagonist

Question 42

They need to be activated by passing through the liver

Answer 42

Prodrug

Question 43

types of permeation

Answer 43

○ Aqueous diffusion ○ Lipid diffusion ○ Transport by special carriers ○ Endocytosis ○ Exocytosis

Question 44

movement of molecules through the watery extracellular and intracellular spaces

Answer 44

AQUEOUS DIFFUSION

Question 45

AQUEOUS DIFFUSION occurs within...

Answer 45

LARGER aqueous compartments of the body (eg: interstitial space, cytosol, etc.) and across epithelial membrane tight junctions and the endothelial lining of blood vessels

Question 46

Movement of molecules through membranes and other lipid structures

Answer 46

LIPID DIFFUSION

Question 47

LIPID DIFFUSION is governed by ___

Answer 47

Fick's law

Question 48

TRANSPORT BY SPECIAL CARRIERS 2 TYPES

Answer 48

1. Active transport 2. Facilitated diffusion

Question 49

NET (norepinephrine transporter) 1. Physiologic Function 2. Pharmacologic Significance

Answer 49

1. Norepinephrine reuptake from synapse 2. Target of cocaine and some tricyclic antidepressants

Question 50

SERT (serotonin reuptake transporter) 1. Physiologic Function 2. Pharmacologic Significance

Answer 50

1. Serotonin reuptake from synapse 2. Target of selective serotonin reuptake inhibitors and some tricyclic antidepressants

Question 51

VMAT (vesicular monoamine transporter) 1. Physiologic Function 2. Pharmacologic Significance

Answer 51

1. Transport of dopamine and norepinephrine into adrenergic vesicles in nerve endings 2. Target of reserpine and tetrabenazine

Question 52

MDR1 (multidrug resistance protein - 1) 1. Physiologic Function 2. Pharmacologic Significance

Answer 52

1. Transport of many xenobiotics out of cells 2. Increased expression confers resistance to certain anticancer drugs; inhibition increases blood levels of digoxin

Question 53

MRP1 (multidrug resistance-associated protein -1) 1. Physiologic Function 2. Pharmacologic Significance

Answer 53

1. Leukotriene secretion 2. Confers resistance to certain anticancer and antifungal drugs

Question 54

the process by which the substance is bound at a cell-surface receptor, engulfed by the cell membrane, and carried into the cell by pinching off of the newly formed vesicle inside the membrane

Answer 54

ENDOCYTOSIS

Question 55

Expulsion (or secretion) of membrane-encapsulated material from the cell

Answer 55

EXOCYTOSIS

Question 56

Predicts the movement of molecules across a barrier

Answer 56

FICK’S LAW OF DIFFUSION

Question 57

Drug absorption is faster in organs with larger ___

Answer 57

surface areas

Question 58

Drug absorption is faster from organs with ___ membrane barriers

Answer 58

thin

Question 59

The passive flux of molecules down a concentration gradient is governed by ___

Answer 59

Fick’s law

Question 60

Water soluble drugs are (polar/nonpolar)

Answer 60

polar (they follow the water diffusion)

Question 61

Lipid soluble drugs are (polar/nonpolar)

Answer 61

nonpolar

Question 62

Aqueous solubility of a drug is a function of the ___ (degree of ionization, polarity) of the molecule

Answer 62

electrostatic charge

Question 63

Lipid solubility of a molecule is ___ proportional to its charge

Answer 63

inversely

Question 64

Clinically important when it is necessary to estimate or alter the partition of drugs between compartments of different pH

Answer 64

THE HENDERSON-HASSELBACH EQUATION

Question 65

amount absorbed into the systemic circulation

Answer 65

BIOAVAILABILITY

Question 66

When the drug passes through the ___, it is metabolized and when the drug goes to the blood circulation, it will be less than 100% of what you administered

Answer 66

liver

Question 67

Instantaneous and complete absorption

Answer 67

INTRAVENOUS (IV) / PARENTERAL ABSORPTION

Question 68

Absorption maybe slower, and less complete

Answer 68

ORAL (swallowed)

Question 69

Absorption is often faster and more complete (higher bioavailability) than oral

Answer 69

INTRAMUSCULAR (IM) ABSORPTION

Question 70

___ cannot be given by IM, causes bleeding in the muscle

Answer 70

heparin

Question 71

Most vaccines are administered through ___

Answer 71

intramuscular injection

Question 72

___ are injected subcutaneously to avoid being recycled by the liver

Answer 72

Insulin

Question 73

Slower absorption than IM route

Answer 73

SUBCUTANEOUS ABSORPTION

Question 74

____ drugs are pressed under the tongue and the buccal

Answer 74

Nitroglycerin antianginal

Question 75

Application to the skin or mucous membrane of the eye, nose, throat, airway, or vagina for local effect

Answer 75

TOPICAL

Question 76

Application to the skin for systemic effect

Answer 76

TRANSDERMAL

Question 77

ABSORPTION OF DRUGS ROUTES OF ADMINISTRATION (9)

Answer 77

1. ORAL (swallowed) 2. INTRAVENOUS (IV) / PARENTERAL 3. INTRAMUSCULAR (IM) 4.. SUBCUTANEOUS 5. BUCCAL AND SUBLINGUAL 6. RECTAL (suppository) 7. INHALATION 8. TOPICAL 9. TRANSDERMAL

Question 78

(high/low) blood flow maintains a high drug depot-to-blood concentration gradient

Answer 78

high

Question 79

Major determinant of the rate of absorption (Fick's law)

Answer 79

CONCENTRATION

Question 80

DETERMINANTS OF DISTRIBUTION

Answer 80

SIZE OF THE ORGAN BLOOD FLOW SOLUBILITY BINDING

Question 81

determines the concentration gradient between blood and the organ

Answer 81

Size of the organ

Question 82

Important determinant of the rate of uptake

Answer 82

BLOOD FLOW

Question 83

If the drug is very soluble in cells, the concentration in the perivascular space will be ___ and diffusion from the vessel into the extravascular tissue will be ___

Answer 83

lower facilitated

Question 84

Binding of drugs to macromolecules in the blood or tissue compartment will tend to ___ the drug's concentration in that compartment

Answer 84

increase

Question 85

Amount of drug in the body to the concentration in the plasma

Answer 85

Vd

Question 86

Drug elimination is the same as drug excretion (T/F)

Answer 86

FALSE *A drug maybe eliminated by metabolism long before the modified molecules are excreted from the body

Question 87

For most drugs, excretion is by way of the ___

Answer 87

kidneys

Question 88

Rate of elimination is proportionate to the concentration

Answer 88

FIRST ORDER ELIMINATION

Question 89

Drug’s concentration in plasma ___ exponentially with time

Answer 89

decreases