Lecture 1: Nature of Drugs & Drug Development

Question 1

Pharmacology definition

Answer 1

the study of substances that interact with living systems through chemical process, especially by binding to regulatory molecules and improving or impressing normal function

Question 2

define medical pharmacology

Answer 2

the science of substances uses to prevent, diagnose and treat disease

Question 3

define toxicology

Answer 3

the branch of pharmacology that deal with undesirable effects of chemicals on living things

Question 4

pharmacodynamics

Answer 4

describes the action of the drug on the body (physical, molecular, and biochemical level)

Question 5

pharmacokinetics

Answer 5

investigates the effects of the body drugs (ADME)

Question 6

Drug definition

Answer 6

any substance that causes alteration in cellular / biopic effect

Question 7

therapeutic agent

Answer 7

a drug used to treat a medical condition or disease

Question 8

prophylactic agent

Answer 8

a drug used to prevent a medical condition or disease

Question 9

pharmacy

Answer 9

the profession of preparing, compounding, and dispensing chemicals for medical use

Question 10

pharmacogenetics/genomics

Answer 10

examines the role of genetics on different drug responses

Question 11

medicinal chemistry

Answer 11

design and synthesis of drug compounds

Question 12

pharmaceutics

Answer 12

design and synthesis of drug formulations (ex: extended release)

Question 13

what was the start of early drug development in the 1800s

Answer 13

isolation of natural products

Question 14

morphine is purified from ___

Answer 14

opium found in products

Question 15

who was credited with developing early experimental physiology and pharmacology?

Answer 15

Francois magendie and Claude Bernard

Question 16

what is the drug regulatory body in the US

Answer 16

FDA

Question 17

what is a serendipitous drug discovery?

Answer 17

drug found by accident or when trying to accomplish something different

Question 18

give an example of serendipitous discovery

Answer 18

Alexander Flemming discovering penicillin in the 1920’s

Question 19

what is intelligent (rational) drug design?

Answer 19

identifying the target and designing a drug to modulate this target

Question 20

give an example of a drug therapy that is the result of intelligent (rational) drug development

Answer 20

reverse transcriptase inhibitors (HIV therapy)

Question 21

What is high throughput screening?

Answer 21

testing large libraries of compounds to determine “hits”

Question 22

what are “me-too” drugs?

Answer 22

additional related drugs that are produced after the discovery of the first

Question 23

what are the main goals of the pre-clinical phase?

Answer 23

identify target, determine mechanism of action

Question 24

what are the goals of phase 1 of clinical trial?

Answer 24

determine limits of safe dosing, predict toxicity, discover pharmacokinetic measurements

Question 25

who are then volunteers in phase 1 of a clinical trial?

Answer 25

healthy volunteers (do not have disease of interest)

Question 26

who are the volunteers in phase 2 of a clinical trial?

Answer 26

volunteers with the disease of interest

Question 27

which phase of a clinical trial has the highest rate of failure?

Answer 27

phase 2

Question 28

what are the goals of phase 2 of a clinical trial

Answer 28

determine efficacy of drug in diseased patients and continue determining toxicity and dosage

Question 29

what are the goal of phase 3 clinical trial?

Answer 29

confirm safety and efficacy and minimize placebo effects

Question 30

what happens if a clinical trial passes the third phase?

Answer 30

application is sen for review if it can be marketed for sale (can take several years)

Question 31

what are randomized control trials?

Answer 31

trial in which participants are randomly assigned to a treatment group

Question 32

what are single and double blind procedure? what is their use?

Answer 32

single blind: patient does not know which treatment group they are in; Double blind: neither patient or researcher knows which group patient is in. Eliminates subconscious bias and placebo

Question 33

what are some examples of drugs that may be exceptions to the clinical trial rules?

Answer 33

drugs for life-threatening illnesses such as cancer, HIV etc

Question 34

what are the 3 components in the application process to manufacture and sell a generic version of a known drug?

Answer 34

1. must show quality manufacturing 2. the active ingredient must be present in listed amount 3. other components of formulation may differ from the original

Question 35

what is the chemical name of a drug?

Answer 35

the IUPAC name of the compound

Question 36

what is the Generic name of a drug? Example?

Answer 36

the universal name of a drug; EX: ibuprofen and acetaminophen

Question 37

what is the brand name of a drug?

Answer 37

name chosen by the manufacturer, usually different across the world

Question 38

materia-medica

Answer 38

the science of drug preparation and medical use of drugs

Question 39

___ is the biological substrate of drug action

Answer 39

drug receptor

Question 40

what are orphan receptors?

Answer 40

no ligand has been discovered for them so their function can only be guessed at

Question 41

osmotic agents are drugs that ___

Answer 41

interact almost exclusively with water

Question 42

chemical antagonist drugs are drugs that __

Answer 42

interact directly with other drugs

Question 43

drugs made in the body

Answer 43

hormones

Question 44

chemical not made in the human body are called __

Answer 44

xenobiotics

Question 45

what are toxins? Example?

Answer 45

poisons of biologic origin; arsenic

Question 46

to interact with a receptor, a drug must have the correct __, ___, ___, and ___

Answer 46

size, shape, charge, atomic composition

Question 47

provide three qualities of a useful drug

Answer 47

1. is able to be transported in the body 2. can be inactivated/ecreted from the body 3. react at a reasonable rate to have the effects last for a desired duration

Question 48

drugs should usually be at least ___-MW units inside

Answer 48

100

Question 49

what is a potential con of large drugs?

Answer 49

need to be able to move through the body

Question 50

a drug greater than ___ MW units in size needs to be administered directly to action site

Answer 50

1000

Question 51

a drug can bind to a receptor through what sort of bonds?

Answer 51

covalent, H bonds, electrostatics

Question 52

covalent bonds are reversible or irreversible under biological conditions?

Answer 52

irreversible

Question 53

which drugs are more selective? those that bind strongly or those that bind weakly?

Answer 53

those that bind weakly

Question 54

more than __ % of drugs are chiral

Answer 54

50

Question 55

t/f when stereochemistry is involved, typically there is one isomer which is more potent as a drug than the other

Answer 55

true

Question 56

enzymes are ___ , therefore one enantiomer of a drug is more susceptible to drug metabolizing enzymes

Answer 56

stereoselective

Question 57

t/f the effector may be part of the receptor, a separate molecule, responsible for final change in function

Answer 57

true

Question 58

allosteric drugs are those which __

Answer 58

bind to the same receptor as the agonist, but do not prevent binding of agonist

Question 59

t/f allosteric drugs can enhance or inhibit action the agonist

Answer 59

true

Question 60

role of competitive inhibitor

Answer 60

mimic agonist

Question 61

what is constitutive activity?

Answer 61

when a receptor can exist in both active and inactive forms and can sometimes become activated without against

Question 62

role of full agonists

Answer 62

cause activation of almost all receptors

Question 63

role of partial agonists

Answer 63

can't illicit as great a response, no mater the concentration

Question 64

partial agonists are said to be drugs with low ___

Answer 64

intrinsic activity

Question 65

what is neutral antagonism?

Answer 65

an antagonist at the receptor site blocks the agonists

Question 66

inert binding site

Answer 66

non-regulatory molecule, binding to it will result in no change in biological function

Question 67

prodrug

Answer 67

precursor to the active form of the drug

Question 68

permeation can proceed through what 3 methods?

Answer 68

1. passive diffsuion 2. vehicles to transport 3. end/exocytosis

Question 69

most new drugs are developed through what 4 processes?

Answer 69

1. identification of new drug target 2. rational drug design, based on biological mechanisms and receptor structure 3. screening for biological activity of a large # products and banks 4. chemical modification of pre-existing drugs (me-too_

Question 70

molecular drug screenings involve __

Answer 70

screening for receptor binding activity

Question 71

cellular drug screening involves __

Answer 71

determining if the drug will act as an agonist, antagonist, partial inverse etc

Question 72

whole animal drug screening involves __

Answer 72

screening the effect on organ systems and disease models

Question 73

the desired result of drug screening is a __ compound

Answer 73

lead

Question 74

t/f some chemicals can be deemed completely safe

Answer 74

false

Question 75

what is the "no effect dose"?

Answer 75

the max dose at which a specified toxic effect is not seen

Question 76

what is the minimum lethal dose?

Answer 76

the smallest dose observed to kill an experimental animal

Question 77

Median lethal dose (LD50)

Answer 77

dose expected to kill 50 % of experimental animals (can be extrapolated to human dosing)

Question 78

some conditions can wax and wane in severity, when developing a trial to administer a drug to treat these diseases what sort of method should be used to reduce confounding variables?

Answer 78

cross over technique ( alternating periods of administration)

Question 79

what is the fourth phase of a clinical trial?

Answer 79

monitoring for safety