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.Pharmacology > Lecture 1: Nature of Drugs & Drug Development > Flashcards

Lecture 1: Nature of Drugs & Drug Development Flashcards

1
Q

Pharmacology definition

A

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

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2
Q

define medical pharmacology

A

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

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3
Q

define toxicology

A

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

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4
Q

pharmacodynamics

A

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

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5
Q

pharmacokinetics

A

investigates the effects of the body drugs (ADME)

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6
Q

Drug definition

A

any substance that causes alteration in cellular / biopic effect

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7
Q

therapeutic agent

A

a drug used to treat a medical condition or disease

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8
Q

prophylactic agent

A

a drug used to prevent a medical condition or disease

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9
Q

pharmacy

A

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

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10
Q

pharmacogenetics/genomics

A

examines the role of genetics on different drug responses

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11
Q

medicinal chemistry

A

design and synthesis of drug compounds

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12
Q

pharmaceutics

A

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

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13
Q

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

A

isolation of natural products

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14
Q

morphine is purified from ___

A

opium found in products

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15
Q

who was credited with developing early experimental physiology and pharmacology?

A

Francois magendie and Claude Bernard

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16
Q

what is the drug regulatory body in the US

A

FDA

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17
Q

what is a serendipitous drug discovery?

A

drug found by accident or when trying to accomplish something different

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18
Q

give an example of serendipitous discovery

A

Alexander Flemming discovering penicillin in the 1920’s

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19
Q

what is intelligent (rational) drug design?

A

identifying the target and designing a drug to modulate this target

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20
Q

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

A

reverse transcriptase inhibitors (HIV therapy)

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21
Q

What is high throughput screening?

A

testing large libraries of compounds to determine “hits”

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22
Q

what are “me-too” drugs?

A

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

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23
Q

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

A

identify target, determine mechanism of action

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24
Q

what are the goals of phase 1 of clinical trial?

A

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

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25
Q

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

A

healthy volunteers (do not have disease of interest)

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26
Q

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

A

volunteers with the disease of interest

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27
Q

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

A

phase 2

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28
Q

what are the goals of phase 2 of a clinical trial

A

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

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29
Q

what are the goal of phase 3 clinical trial?

A

confirm safety and efficacy and minimize placebo effects

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30
Q

what happens if a clinical trial passes the third phase?

A

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

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31
Q

what are randomized control trials?

A

trial in which participants are randomly assigned to a treatment group

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32
Q

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

A

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

33
Q

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

A

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

34
Q

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

A
  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
35
Q

what is the chemical name of a drug?

A

the IUPAC name of the compound

36
Q

what is the Generic name of a drug? Example?

A

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

37
Q

what is the brand name of a drug?

A

name chosen by the manufacturer, usually different across the world

38
Q

materia-medica

A

the science of drug preparation and medical use of drugs

39
Q

___ is the biological substrate of drug action

A

drug receptor

40
Q

what are orphan receptors?

A

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

41
Q

osmotic agents are drugs that ___

A

interact almost exclusively with water

42
Q

chemical antagonist drugs are drugs that __

A

interact directly with other drugs

43
Q

drugs made in the body

A

hormones

44
Q

chemical not made in the human body are called __

A

xenobiotics

45
Q

what are toxins? Example?

A

poisons of biologic origin; arsenic

46
Q

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

A

size, shape, charge, atomic composition

47
Q

provide three qualities of a useful drug

A
  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
48
Q

drugs should usually be at least ___-MW units inside

A

100

49
Q

what is a potential con of large drugs?

A

need to be able to move through the body

50
Q

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

A

1000

51
Q

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

A

covalent, H bonds, electrostatics

52
Q

covalent bonds are reversible or irreversible under biological conditions?

A

irreversible

53
Q

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

A

those that bind weakly

54
Q

more than __ % of drugs are chiral

A

50

55
Q

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

A

true

56
Q

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

A

stereoselective

57
Q

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

A

true

58
Q

allosteric drugs are those which __

A

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

59
Q

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

A

true

60
Q

role of competitive inhibitor

A

mimic agonist

61
Q

what is constitutive activity?

A

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

62
Q

role of full agonists

A

cause activation of almost all receptors

63
Q

role of partial agonists

A

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

64
Q

partial agonists are said to be drugs with low ___

A

intrinsic activity

65
Q

what is neutral antagonism?

A

an antagonist at the receptor site blocks the agonists

66
Q

inert binding site

A

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

67
Q

prodrug

A

precursor to the active form of the drug

68
Q

permeation can proceed through what 3 methods?

A
  1. passive diffsuion
  2. vehicles to transport
  3. end/exocytosis
69
Q

most new drugs are developed through what 4 processes?

A
  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_
70
Q

molecular drug screenings involve __

A

screening for receptor binding activity

71
Q

cellular drug screening involves __

A

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

72
Q

whole animal drug screening involves __

A

screening the effect on organ systems and disease models

73
Q

the desired result of drug screening is a __ compound

A

lead

74
Q

t/f some chemicals can be deemed completely safe

A

false

75
Q

what is the “no effect dose”?

A

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

76
Q

what is the minimum lethal dose?

A

the smallest dose observed to kill an experimental animal

77
Q

Median lethal dose (LD50)

A

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

78
Q

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?

A

cross over technique ( alternating periods of administration)

79
Q

what is the fourth phase of a clinical trial?

A

monitoring for safety

.Pharmacology (55 decks)

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