Pharmacology I Flashcards Preview

Tim's Cards > Pharmacology I > Flashcards

Flashcards in Pharmacology I Deck (150):
1

T/F
Chinese developed drugs in 2700 BC in Doctrine of Signatures. The oldest prescription is on a Sumerian Tablet around 3000 BC.

True

2

T/F
Hippocrates big insight was that disease is from natural causes.

True

3

What was the 1st specific drug used to treat a specific disease?

Quinine from Peruvian Tree bark used to treat Malaria

4

What is the single most important drug discovery in medicine?

Acetylsalicylic Acid - aspirin - 1890's

5

What treatment/drug for Congestive Heart Failure is still isolated from the Foxglove plant?

Digitalis

6

How are arsenicals made?

Arsenic to Carbon atom attachment

7

What 2 Alkaloid substances were isolated from Atropa belladonna?

Atropine (pupil dilator)

Scopolamine (motion sickness)

8

T/F
Penicillin was used in WWI

False

not until WWII

9

How long does it take to develop and bring a new drug to market?

How much does it cost?

15 years

360 million

10

____ out of 10 compounds that are developed reach market.

Of those, ___ out of 10 have ROI.

2

3

11

How long does a Patent for a new drug last?

17 years

12

Define Margin of Safety:

LD50 divided by ED50

(lethal dose/effective dose)

13

What is an acceptable Margin of Safety?

2000 or more

14

Animal Testing and Margin of Safety (LD50/ED50) are part of ______ Testing

Short-term Toxicity

15

What is another name for Long-term toxicity studies?

Chronic Toxicity Studies

16

T/F
Chronic Toxicity Studies involve daily dosing of dogs/rats from 3 months to 2 years, than animals are killed and histopathology is studied

True

17

What are 2 Specialized animal studies done for Safety?

Reproduction (teratogen)

Carcinogenicity

18

What can be submitted if drug has adequate margin of safety in rats, there are no long-term toxicities, no carcinogenic effects, non-teatogenic?

What is the Approval Time?

IND - Investigational New Drug Application

30 days

19

In what phase are drugs evaluated in humans for the 1st time?

When does it begin?

Clinical Studies - Phase 1

Immediately after IND approval

20

Who is studied in Phase 1?

20-80 healthy male humans

21

What is determined in Clinical Studies - Phase 1?

3 things

Safety Profile

Pharmokinetics

Toxicity dose

22

At what clinical phase of the study are new drugs given to patients that have the condition for which the drug is intended?

Phase 2

23

How many subjects are in Phase 2 studies?

What is determined?

100-300 subjects

Short-term effectiveness

24

T/F
Phase 1 establishes therapeutic efficacy, dose response/range, metabolism, and adverse drug events.

False

*Phase 2

25

What Phase studied Long Term Efficacy?

Phase 3

26

How many subjects are in a Phase 3 study?

1000 - 3000

27

T/F
Phase 3 clinical studies are to confirm drug safety/efficacy and to try to detect adverse effects that are undetected in prior studies.

True

28

Phase 3 studies are always _____

Double Blind

29

Name 2 potential limitations in Phase 3 testing.

More Short term than Long term participants

Toxicities occurring less than 1 in 1000 will not be revealed

30

If Phase 3 testing is successful, what can be submitted (this is after 8 years of animal/human testing)?

NDA - New Drug Application process

31

T/F

If an NDA (New Drug Application) is accepted by the FDA, it can be sold exclusively and have a 17 year patent.

True

32

When are Phase 4 Studies done?

Post-marketing Surveillance

After FDA approval

***Drug pulled off market if new toxicities are uncovered

33

T/F
Often the result of Phase 4 study/surveillance is relabeling with new warnings and precautions

True

34

4 Phases Drug Testing Summary:
Phase 1:

Phase 2:

Phase 3:

Phase 4:

20-80, test for safety in "normals"

hundreds, Safety and Effectiveness

thousands, safety, dose, effectiveness, adverse events

Post-marketing surveillance

35

Define Chemical, Generic, and Trade name of drugs:

Chemical: structure (combo letters/numbers)

Generic: lower case, official name

Trade: marketed commercially

*all drugs have on generic name and many trade names

36

The active ingredient in Generic Drugs must enter the blood at the _____ rate as the Trade brands

Same

37

Name 8 pieces of legislation that regulate drug marketing and safety:

What do each do?

1906 Pure Food and Drug Act
(created FDA, standards purity/quality, correct/truthful labels)

Federal Food and Drug Cosmetic act of 1938
(Requires proof of safety/purity)

FDA Modernization Act of 1997

Durham-Humphery Act of 1952
(FDA authorized to determine what drugs can be sold w/o prescription)

Kefauver-Harris Amendment of 1962
(requires proof efficacy/safety of new drugs)

Controlled Substances Act of 1970
(abuse - DEA)

Dietary Supplement Health and Education Act of 1994
(FDA must demonstrate supplement unsafe before taking action against)

Federal Food, Drug, and Cosmetic Act of 2006
(supplement industry must report side effects)

38

T/F
The FDA controls OTC drugs, reviews for misbranding and adulteration, sets guidelines for safety/efficacy, and can prevent the sale and withdraw a drug from market

True

39

The Orphan Drug Amendments of _____ provides incentives to treat orphan diseases.

The Expedited Drug Approval Act of _____ allows accelerated FDA approval for drugs of significant need with detailed post-marketing _______.

The Harrison _______ act of 1914 first established regulations governing opiates and cocaine and preceded the Controlled Substances Act of 1970

1983

1992

Surveillance

Narcotic

40

A drug is a ______ substance

The are used for what 4 things?

Chemical

Diagnosis, Prevention, Treatment, Prego prevention

41

What is the study of how drugs enter the body, circulates, changes, and leaves?

Pharmacokinetics

42

What are the 4 steps the body takes a drug through?

Absorption

Distribution

Metabolism

Excretion

43

For the following describe how it influences passing a lipid bilayer:
Solubility:

Charge:

Size:

Shape:

Solubility: more soluble, passes easier

Charge: cannot pass if charged

Size: Small crosses easily

Shape: must fit through membrane

44

What is the study of biochemical and physiologic actions, and the mechanism of drug action at cell/sub-cell level?

Pharmacodynamics

45

T/F
Lipid solubility, degree of ionization (charge), size, and shape are all characteristics of drug molecules

True

46

The lower the pKa, the _____ the acid

Stronger

47

Weak Acid in Acidic =

Weak Acid in Basic =

Weak Base in Acidic =

Weak Base in Basic =

Lipid Soluble

Water Soluble

Water Soluble

Lipid Soluble

***Like with like = Lipid `

48

_____ is administered into the GI tract and ______ bypasses via injections, inhalation, topical administration

Enteral

Parenteral

49

T/F
Enteral drug administration is the cheapest and is poorly/irregularly absorbed

True

50

Inhalation, IV, IM, Topical, Subgingival, SubQ, Sublingual, and transdermal are all...

Parenteral

51

IV is the most _____ and ______.

IM has the most ______ effect.

Transdermal is more _______ than others.

Rapid, Predictable

Sustained

Concentrated

52

What route goes into the spinal or subarachnoid space?

Intrathecal

53

Tablets and Capsules are _____ and _____-

Slow

Unpredictable

54

Solution, syrup, suspension, emulsion, tincture, elixir all have a ______ control rate

Continuous

55

T/F
Ointments and Creams have problematic dosage controls

True

56

What has slow, continuous delivery and must be changed?

Transdermal patches

57

T/F
Inhalants have slow onset

False

*rapid

58

What are 3 mechanisms by which drugs penetrate biological membranes?

Diffusion - passive

Filtration - through pores

Specialized Transport - Facilitated/Active

59

T/F
Topical drugs cause systemic effects

False

*can be local or systemic, depending on dosage

60

Local anesthetics are usually delivered by what route?

Subcutaneous

61

What are 3 fast and 3 slow onset drug delivery methods?

Fast: IV, Sublingual, Inhalation

Slow: IM, Patch, Subcutaneous

62

Drug dissolved in aqueous solution:

Drug dissolved in saturated aqueous solution of sugar:

Drug dissolved in sweetened water/alcohol solution:

Drug dissolved in pure alcohol:

Drug dissolved in oil phase:

Drug not dissolved but...

Solution

Syrup

Elixir

Tincture

Emulsion

Suspension

63

T/F
IV faster than IM faster than Oral

True

64

What does the following pathway describe?

Oral - Stomach - Intestines - Portal veins - Liver

First Pass Effect

65

What is the fraction of administered drug that becomes available in the plasma?

Bioavailability

***Frequently influenced by the "vehicle" of the drug

66

What is the only type of drug administration that gives 100% bioavailability?

IV

67

T/F
The FDA mandates that generics have 90% bioavailability

True

68

What 2 forms do drugs take in the body?

*What can pass across membranes?

Bound to Plasma Proteins = Inactive

*Free = Active (passes membranes)

69

What are 2 potential barriers to drug distribution in the body?

BBB - blood brain barrier (only small, lipid soluble drugs pass through)

Placenta - most drugs pass, lipid soluble cross easiest

70

What must happen for a drug to terminate its activity?

Redistribution

***off site of action

71

What is the term for drug metabolism so it can be excreted by the kidneys?

Biotransformation

72

Biotransformation converts _____ soluble drugs to ______ soluble metabolites.

Lipid

Water

73

Where does biotransformation take place?

Liver

74

What are the 2 Phases of Biotransformation?

Phase 1 - Liver modification (redox/hydrolysis)

Phase 2 - Conjugation. Pharmacologically inactive

75

What does LMOES stand for?

Liver Microsomal Oxidation Enzyme System

76

LMOES usually occurs in what phase of biotransformation?

Phase 1

77

An electron transport system requiring NADPH and Oxygen, present in the Liver (primarily), GI tract, and kidney.

LMOES - Liver Microsomal Oxidation Enzyme System

78

What 3 factors control the rate of drug metabolism in LMOES?

Cytochrome P-450

NADPH-cytochrome C reductase

Competing substrates

79

What are the 2 general (descriptive) ways to eliminate drugs from the body?

Zero Order - constant (alcohol)

First Order - constant fraction (exponential)

80

6 routes of Drug excretion:

Kidney (urine)

Bile (feces)

Sweat

Saliva

Lungs

Breast Milk

81

What is the time needed for the plasma concentration of a drug to fall to one half its blood level?

Biological Half Life

82

If a constant fraction of drug is eliminated over time, this is _____

First Order

83

If the rate of Intake = rate of Elimination of a drug, it has reached...

Plasma steady state concentration

84

T/F
At a regular dosing frequency, a drug reaches a steady state or equilibrium because the process of elimination is concentration dependent.

True

85

T/F
Drugs only interact with receptors covalently

False

Covalent, ionic, hydrogen, hydrophobic, Van der Waals

86

What are the 2 most common ways drugs bind to receptors?

H-bonding

Ionic bonding

87

T/F
The affinity of a drug for a particular receptor and the type of binding is intimately related to the drug's chemical structure.

True

88

How long does it take for a drug to be cleared from the body?

4 to 5 half lives

89

A drug that causes a conformational change in protein is the ______ model

Induced Fit

90

T/F
Drug receptors are proteins that recognize selected molecules at the external surface and transmit information to inside the cell.

True

91

T/F
Membrane spanning protein receptors communicate with both sides of the cell, which allows drug to act without entering

True

92

A hormone, neurotransmitter, GF, or drug that binds a receptor protein/glycoprotein is called a...

Ligand

93

A conformational change that causes a signal in response to a ligand is known as...

Cell Signaling

94

Name 4 Cell Signaling substances in the body:

Hormones

Neurotransmitters

Growth Factors

Drugs

95

What are 4 examples of cellular responses that occur following cell signaling?

Ion channel opening/closing

2nd Messenger formation

Gene expression alters

Cell growth/differentiation

96

T/F
Drug interaction with receptors that control ion channels are found in excitable tissues

True

97

A drug that binds a receptor that controls ion channels will increase permeability to _____ and _____, that will determine _____ of the nerve.

Potassium, Sodium

Depolarization/hyperpolarization

98

Ligand gated ion channels, G proteins, Intracellular receptors, and Tyrosine Kinase receptors are all involved in Signal Transduction

True

99

Parasympathetic - Acytylcholine - muscarinic cholinergic receptors

Sympathetic - Norepinepherine - Adrenergic receptors

True

*these generate second messengers

100

T/F
Ligand binding causes events that generate 2nd messengers that pass message from inside the cell to effector organ

True

101

What in the internal membrane regulates the generation of 2nd Messengers?

Intracellular G-Protein Complex

102

What 3 responses can an Activated G-Protein Complex Induce?

Adenylyl Cyclase - generate cAMP

Phospholipase C - phosphorylates proteins

Membrane channel - changes ionic conductance

103

The amount of drug necessary to produce an effect is what?

Drug Potency

104

The maximum intensity of a drug's effect is the...

Drug Efficacy

*maximum response produced by the drug

105

Demerol and Morphine have similar ______, but differ greatly in ______.

Efficacy

Potency

106

A drug that is able to bind to a receptor to produce an effect is an....

Agonist

107

A drug that binds to the same receptor as an agonist but is unable to Activate the receptor (produces to effect) is what?

Antagonist

108

If an agonist and antagonist are administered together, what binds the receptor first?

Antagonist

109

T/F
An Antagonist can be either competitive or non-competitive

True

110

A Competitive Antagonist is ______ and physically blocks the receptor

Reversible

111

T/F
Administering additional agonist will displace the antagonist from the receptor

True

112

A Non-Competitive Antagonist will bind ______ and binds either the same or different sites. (both inhibit agonist)

Irreversibly

*cannot be displaced - think botox

113

A Physiological Antagonist will oppose an agonist by ______.

A Pharmacologic Antagonist will oppose an agonist by ______.

Activating pathways

Binding first and preventing pathway

114

The range of doses that elicit a therapeutic response without unacceptable side effects is known as the ______.

Therapeutic Window

115

If the Therapeutic Window is small, the blood plasma level of a drug must be closely monitored

True

116

T/F
Receptor molecules include proteins and glycoproteins

True

117

T/F
Binding of ligand to receptor occurs through induced fit

True

118

T/F
Receptors recognize ligands at external cell surface and transmit info into the cell.

Cell signaling involves Conformational Change in receptor molecule due to ligand binding

Cell signaling substances can be hormones, neurotransmitters, growth factors, and drugs

All True

119

TD50 (toxic) / ED50 (therapeutically effective), defines what?

Quantitative measure of Therapeutic Window

120

Cell and Tissue damage due to overdose that leaves permanent micro/macro and Intolerable effects is _____

Toxicity

121

Undesired effects that are tolerable, reversible, and dose related are.....

Side effects

122

Multiple medications given to a pt (5 or more), is known as....

Taking multiple supplements is known as....

Polypharmacy

Polyherbacy

123

What report, in terms of percentage of population affected, is categorized by body/organ system for each drug?

Monograph

*required by FDA

124

T/F
Hypersensitivity rxns manifest as skin rash, asthmatic rxns, rhinitis, and anaphylaxis

True

125

T/F
A person must have a previous exposure to a drug to have an allergic rxn

True

126

What are the 3 types of allergic rxns associated with drugs and what are the antibodies associated with them?

Type 1 - IgE

Type 2 - IgG, IgM

Type 3 - IgG

127

Type 1 IgE hypersensitivity rxns are the most severe and include what 4 symptoms?

Anaphylaxis

Asthma

Rhinitis

Dermatitis

128

Type 2 hypersensitivity (IgG, IgM) is manifested by what?

Hemolysis of RBC's

129

Type 3 hypersensitivity (IgG) rxs include these 3...

Arthralgia

Fever

Lymphadenopathy

130

Causing defects in developing embryo

Teratogen

131

FDA pregnancy risk categories and what they mean:

A = failed to demonstrate risk to fetus

B = animal studies no risk demonstrated

C = animal studies reveal risk to fetus, no human data

D = positive data human fetal risk, but useful benefits

X = animal and human fetal risk demonstrated (contraindicated)

132

What sedative used to relieve morning sickness caused limb defects in the 1960's?

Thalidomide

133

What is the modern use of Thalidomide?
(4 things)

Oral ulcers from AIDS

Multiple myeloma/other blood dyscrasias

Leprosy sores

Reverses wasting in AIDS

134

What field studies the genetic variability of drug effects?

Pharmacogenetics

*often by misspelled genes

135

Pharmacogenetic variability can alter pharmacokinetics seen by______, and pharmacodynamics seen by ______.

drug plasma levels

therapeutic effects of drugs

136

How do "misspelled genes" affect the following drug interactions:
Albuterol:

Prozac:

Isoniazid:

Albuterol ineffective in dilating smooth muscle in bronchioles

Prozac metabolized so slowly becomes toxic

Isoniazid (TB drug) metabolized too rapidly to be effective

137

What 4 Factors greatly influence the effectiveness and safety of drugs?

Biological variation

Hypersusceptibility

Drug idiosyncrasy

Age

138

Pediatric pts will have lower dose because of _______ kinetics

Geriatric pts will have lower dose because of _______ clearance

Increased

Decreased

139

In Liver Disease, ____ is reduced, so _____ must be reduced.

Metabolism

Dose

140

T/F
In Renal Disease, drug excretion is inhibited

True

141

A rapid development of Tolerance (e.g. - local anesthesia wears off quickly) is knows as...

Tachyphylaxis

142

What 3 effects can drug interactions have?

Enhancement

New

Inhibition

143

What are the 4 basic mechanisms of Drug Interactions?

Synergistic (similar effects)

Metabolic (induction, inhibition)

Absorption (altered pH, binding in stomach)

Displacement of plasma proteins (more active free drug in circulation)

144

Name the components of the Heading, Body, and Closing of a prescription.

Heading: name, address, tele# of presciber and pt, DATE

Body: Name, dosage size/concentration, amount dispensed, directions to pt

Closing: Presciber signature, DEA number, Refill instructions

145

In prescription writing, define Rx:

Mitte:

Sig:

Rx: Recipe

Mitte: Quantity

Sig: How should be taken

146

What are the 4 factors that determine dosage?

Age

Body Weight

Total body surface area

Usage

147

1 Tube

1 (one) 15 gm tube

Incorrect

Correct

148

Any Scheduled Drug, a prescription for a controlled substance, requires what?

DEA#

149

Define Schedule 1:

Schedule 2:

Schedule 3:

Schedule 4:

Schedule 5:

CI: high potential for abuse

CII: high abuse, severe dependence

CIII: lesser abuse, moderate dependence

CIV: low abuse, moderate dependence

CV: low abuse, moderate dependence

150

What is the best Drug Library available for a dentist?

Lexi-Comp

Decks in Tim's Cards Class (140):