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PHAR370- Fundamentals of Pharmacology and Therapeutics > Module 1- Introduction to pharmacology > Flashcards

Module 1- Introduction to pharmacology Flashcards

1
Q

What is pharmacology

A

Study of substances that affect or alter living systems through chemical processes

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2
Q

Drug

A

Any substance received by a biological system that is not received for nutritive purposed (i.e. chemicals, biologicals, and herbals)

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3
Q

Pharmacodynamics

A

Effects of a drug on the body (mechanism of action that causes these effects)

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4
Q

Pharmacokinetics

A

How the body handles the drug (absorption, distribution, metabolism, and excretion)

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5
Q

what are the 2 reasons drugs are administered

A
  1. to achieve a beneficial effect on an individual
  2. to exert a selectively toxic effect on the individual
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6
Q

What are the two areas of pharmacology?

A
  1. Pharmacodynamics
  2. Pharmacokinetics
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7
Q

Most drugs influence biological systems by…

A

interacting with and binding to receptors

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8
Q

What are endogenous ligands

A

Substances ordinarily found in the body (i.e., hormones and neurotransmitters)

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9
Q

Where do receptors bind

A

Bound to and activated by endogenous ligands

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10
Q

What are 4 types of receptors

A
  1. Regulatory proteins
  2. Transporters
  3. Enzymes
  4. Structural proteins
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11
Q

Regulatory Proteins

A

Proteins that mediate the actions of endogenous chemical signals

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12
Q

What is meant by signalling mechanisms

A

Once an endogenous ligand or drug binds to and activates its receptor, the activated receptor triggers a series of biochemical events that results in the pharmacological effect

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13
Q

What are the 4 common signalling mechanisms

A
  1. ligand gated ion channels
  2. G-protein coupled receptors
  3. regulated transmembrane enzymes
  4. intracellular receptors
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14
Q

Ligand gated ion channels

A

Regulatory proteins used to transport sodium, chloride, and other ions across the cell membrane when an endogenous ligand or drug binds to the receptor

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15
Q

G-protein coupled receptor

A

Receptors that undergo a conformational change when an endogenous ligand or drug binds, activating a second messenger system

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16
Q

Regulated Transmembrane Enzymes

A

Receptors that activate an enzyme inside the cell when an endogenous ligand or drug binds

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17
Q

Intracellular Receptor

A

Receptors that move into the nucleus when bound to an endogenous ligand or drug increasing gene expression

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18
Q

Transporters

A

Proteins that transport endogenous substances across cell membranes

Note: Drugs targeting transporters often inhibit the function of the transporter

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19
Q

Enzymes

A

Proteins that catalyze biological reactions

Note: drugs targeting enzymes often inhibit the catalytic function of the enzymes

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20
Q

Structural Proteins

A

Proteins that contribute to the cell structure

Note: Drugs can bind to structural proteins in a cell and disrupt their normal function

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21
Q

Antacids

A

Commonly used to neutralize stomach acids through a simple acid-base neutralization

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22
Q

Chemotherapy Drugs

A

a # of chemo drugs do not bind to specific receptors, but kill cancer cells by chemically disrupting normal cell function

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23
Q

5 drug classifications

A
  1. Agonists
  2. Partial agonists
  3. Allosteric activator
  4. Competitive antagonist
  5. Non-competitive antagonist
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24
Q

Agonist

A

Binds to and activates the receptor, producing a full response

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25
Q

Partial Agonist

A

Binds to the receptor and activates it, but produces a weak response

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26
Q

Allosteric Activator

A

Binds to a different area of the receptor than the agonist, but makes the receptor easier to activate

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27
Q

Competitive antagonist

A

Reversibly binds to the same receptor site as an agonist, but does not activate it

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28
Q

Non-competitive antagonist

A

irreversibly binds to an blocks the receptor

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29
Q

Dose-response relationship

A

Intensity of the pharmacological effects produced by a drug increases in proportion to the dose

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30
Q

What does ED50 mean?

A

Dose that results in 50% of the maximal effect

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31
Q

What is threshold effect?

A

You need a certain amount of drug binding to an activator, to activate a certain amount of receptors before you see a response in the body

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32
Q

Efficacy vs potency

A

Efficacy: max pharmalogical response that can be produced by a specific drug

Potency: amount of drug required to obtain a particular response

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33
Q

Clinically, which is more important, efficacy or potency?

A

Efficacy is more important than potency; because the max effectiveness of a drug is generally what determined which drug is chosen to treat a specific conditions.

Note: potency does not matter as much, as the dose can be adjusted to achieve a desired response

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34
Q

The dose response curve of a drug w low potency is shifted ______ compared to the dose response curve of a drug with high potency

A

right

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35
Q

The dose response curve of a drug w low efficacy is __________ compared to the dose response curve of a drug w high efficacy

A

condensed

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36
Q

Drug disposition

A

process involved in the journey of a drug through the body

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37
Q

what does ADME stand for?

A

Absorption
Distribution
Metabolism
Excretion

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38
Q

What physical-chemical properties can a drug have?

A

Solids
Liquids
Gas at room temp

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39
Q

Bioavailability

A

actual measure of what is detected in systemic blood stream after consumption of the ingredient

Note: can only be properly determined in pharmacokinetic trials

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40
Q

Absorption

A
  1. release of drug from dosage form
  2. drug must dissolve in GI fluids before it can be absorbed into the blood
  3. Must cross biological membranes to be absorbed into blood and distributed to the sites of action, storage, and excretion
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41
Q

Diffusion through lipid

A

Lipid soluble drugs pass through the membranes by dissolving in the lipid portion of the membrane and flowing down a concentration gradient to the other side of the cell membrane

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42
Q

Membrane permeability

A

ability of a drug to cross a membrane and be absorbed depending on its lipid solubility

43
Q

Un-ionized form

A

Lipid soluble; can readily cross lipid membranes

44
Q

Ionized form

A

water-soluble; does not readily cross the lipid membrane

45
Q

What does the degree of ionization depend on?

A

the pH of the environment and the pka

46
Q

what it the pKa of a drug?

A

the pH where a drug is 50% unionized and 50% ionized

47
Q

Weak acids

A

drug that is a neutral molecule and can dissociate into a negatively charged molecule and a proton

Example: aspirin

48
Q

Weak bases

A

drug that is a neutral molecule and can combine w protons to form a positively charged molecule

example: norepinephrine

49
Q

Acidic environment

A

an excess of protons are available, so the unionized form of a weak acid, and ionized form of a weak base will predominate

50
Q

basic environment

A

few protons are available, so the ionized form of a weak acid, and the unionized form of a weak base will predominate

51
Q

Under acidic conditions, which drug is lipid soluble?

A

Weak acid

52
Q

under basic conditions, which drug is lipid soluble?

A

weak base

53
Q

Distribution

A

for a drug to act, it must move from its site of absorption to other areas of the body, including sites of action

Recall: if the concentration in the blood drops below the concentration at any of the distribution sites, the drug will move from that site into the blood to maintain equilibrium

54
Q

At all sites of distribution, drugs exist in what 2 forms

A
  1. free drug
  2. drug bound to protein

Note: when a drug is bound to protein in the blood, it is not able to cross membranes and is therefore unable to produce its pharmacological effects or be readily excreted by the kidney

55
Q

3 organ-specific distribution sites

A
  1. blood brain barrier- limits the access of many drugs to the brain/ spinal cord
  2. placenta- very permeable to drugs + most drugs reach the fetal tissue
  3. fat soluble drugs will accumulate in Fat cells, and since blood flow to fatty tissue is limited drugs will leave fat tissue slowly
56
Q

Metabolism

A

The conversion of a drug to a different chemical compound

A drug will undergo biotransformation if it needs to be converted into another compound so it can exert its effects or be eliminated from the body

57
Q

Biotransformation in the liver

A

These reactions involve the conversion of drugs into more water-soluble compounds

  • once water soluble, the drug can be eliminated from the body by the kidneys
58
Q

What happens without biotransformation?

A

Some chemicals that are very lipid soluble would never be excreted from the body

59
Q

Where can biotransformation occur?

A

Liver, kidneys, intestines, lungs, skin, and most other organs

60
Q

Phase 1 of biotransformation reactions

A

purpose add or unmask a functional group so that the phase 2 reaction can add a large water-soluble component to allow excretion by the kidney

61
Q

What are 3 phase 1 reactions

A
  1. oxidative reactions via Cytochrome P450
  2. Other oxidative reactions
  3. hydrolysis of esters and amides
62
Q

Oxidative reactions via Cytochrome P450

A

are a family of enzymes located primarily on the smooth endoplasmic reticulum in the liver

CYPs- bind the substrate and activte oxygen

63
Q

Other oxidative reactions

A

Not mediated by CYPs are oxidation of amines and dehydrogenation of alcohol –>mediated by the enzyme monoamine

64
Q

Hydrolysis of Esters and Amides

A

these drugs are converted to the acid and the corresponding alcohol or amine by carboxyl esterase’s found in the liver, blood, GI tract and other tissues

65
Q

phase 2 biotransformation reactions

A

add a large water-soluble moiity to the phase 1 biotransformation product, making the metabolite water-soluble for excretion via kidney

66
Q

Four main phase 2 conjugation enzymes are

A
  1. UDP- glucuronosyltransferase (UGT): forms a glucuronide
  2. Sulfotransferase (SULT): forms a glucuronide
  3. Glutathione transferase (GST): forms a glutathione conjugate
  4. N-acetyl transferase (NAT): forms an N-acetylated metabolite
67
Q

First pass effect

A

the biotransformation and inactivation of a drug during absorption from the intestine

68
Q

Factors affecting biotransformation

A

Drug interactions can occur when two drugs are competing for the same enzyme, or when one drug inhibits the biotransformation of another drug

  1. age
  2. genetic factors
  3. disease states
69
Q

Excretion

A

Moving a drug and its metabolites out of the body

70
Q

Drug excretion via kidney

A

Kidney’s receive about 20% of the blood from the heart (cardiac output), and are very efficient in excreting water-soluble drugs and metabolites

71
Q

Process of renal excretion

A
  1. glomerular filtration: most drugs pass from glomerulus into Bowman’s capsule and then into the proximal tubule of the kidney
  2. passive tubular reabsorption: concentration is higher in renal tubules than in the blood, so some lipid soluble drugs can be reabsorbed back into the blood as they are moving down the concentration gradient
  3. active tubular secretion: active transporters in renal tubule move drugs from the blood into the urine to be excreted
72
Q

Other routes of Drug Excretion

A
  1. gastrointestinal tract
  2. other bodily fluids (milk, saliva, sweat)
  3. through the lungs
73
Q

Apparent Volume of Distribution (Vd)

A

The volume of which a drug appears to be distributed

Vd= dose of drug / concentration of drug in plasma

V= apparent; does not represent an actual volume somewhere in the body

74
Q

Clearance of a drug

A

process of removing a drug from the body

Clearance = rate of elimination / drug concentration in blood

75
Q

First order elimination

A

Constant fraction of drug eliminated over a set period of time

If concentration is high, more drug is excreted, as the liver and kidney have higher amounts of drug available to eliminate

If concentration is low, the opposite it true

76
Q

Zero order kinetics

A

a constant amount of drug is eliminated in a set period of time (instead of a constant proportion), as the enzymes responsible for elimination are saturated and there is more drug than can be transformed

77
Q

Elimination half-life

A

time needed for the liver and kidney to remove 50% of the drug from the blood

78
Q

The plateau principle

A

When a drug is administered repeatedly, the plasma concentration of the drug will increase until the rate of administration is equal to the rate of elimination

drug input = drug output

79
Q

How long does it typically take for drug input = drug ouput?

A

5 elimination half lives

80
Q

Compliance with therapy

A

a drug is not effective if the patient does not take the drug correctly

81
Q

What is compliance when medication is self-administered

A

between 20%-90%

82
Q

Calculating drug doses

A

administered by weight or volume

83
Q

other drug measurements

A
  1. household measures (i.e. teaspoon)
  2. units (based on biological activity of drug)
  3. surface area (body weight)
84
Q

Therapeutic index

A

TI = TD50 / ED50

Note: the higher the therapeutic index, the safer the drug

When a drug has a low TI, its more likely toxicities will occur

85
Q

What is TD50?

A

The dose that is toxic to 50% of a population

86
Q

What is ED50?

A

the dose that is effective in 50% of a population

87
Q

Adverse Drug Reactions

A
  1. extension of therapeutic effect
  2. effects in non-target tissues or organs
  3. unrelated to main drug action
  4. drug idiosyncrasy
  5. allergic reactions
  6. adverse biotransformation reactions
  7. tolerance, withdrawal, addiction
  8. teratogenesis (birth defects)
88
Q

Extension of therapeutic effect

A

occurs when too much of drug is in the blood (common w drug overdose)

i.e. benzodiazepines- taken for sedative effects; an overdose will produce over-sedation

89
Q

Effects in non-target tissues or organs

A

when receptors for the drug exists in more areas than the target tissues, you can observe effects in these non-target tissues/organs

i.e. morphine - produces analgesic effects by acting on opioid receptors but acts on GI receptors also

90
Q

Unrelated to main drug action

A

effects that are unexpected and unrelated to the intended pharmacological action of the drug

i.e. digitalis- treat heart failure; causes nausea, vomiting, and abnormal vision (unrelated to heart)

91
Q

Drug idiosyncrasy

A

Genetic- refers to an unusual response to a drug that is only observed in a small number of people

i.e. succinylcholine- produces muscle relaxation but approx 1 in 3000 patients lack the enzyme that normally inactivates the drug

92
Q

allergic reactions

A

mediated by immune system

i.e. penicillin

93
Q

adverse biotransformation reactions

A

occurs when a drug is converted into a chemically reactive metabolite that can bind to tissue components and cause tissue or organ damage

i.e. acetaminophen- at recommended doses is converted but overdose leads to production of chemically reaction metabolites

94
Q

tolerane, withdrawal, and addiction

A

tolerance/withdrawal =. unwanted physiological effects

addiction= psychological effect

95
Q

teratogenesis (birth defect)

A

multifactorial and depends on the drug, usually refers to drug-induced defects in the developing fetus

96
Q

Why is drug toxicity hard to predict?

A
  1. adverse effect is rare
  2. toxic reaction only appears after prolonged use
  3. toxic effect is not detectable in animals
  4. adverse effect is unique to a particular period or circumstance
97
Q

who is at risk for an adverse reaction?

A

Age:
- newborns and individuals >60
- immature or damaged organs

Genetics:
- enzymes that bio transform and inactivate drugs can exist in different forms based on genes that code for enzymes

Multiple diseases in the same patient:
- the presence of more than one disease can increase chances

98
Q

drug-drug interactions

A

Modifications of the pharmacological effect of one drug by the presence of another drug in the body

the potential increases as the number of drugs taken by the patient increases

98
Q

Types of drug-drug interactions

A

Addictive: combined pharmacological effect of the 2 is the sum of the individual effects

Synergistic: pharmacological effect of 2 drugs is greater than the sum of individual

Potentiation: pharmacological effect of one drug is increased by a second drug, even tho the second drug is devoid of the intended therapeutic effect

antagonism: one drug reuced pharmacological effect of another drug by binding to and competing for the same receptor

altered physiology: one drug my alter the physiology of the body so the response to another drug is altered

99
Q

Drug to food interactions

A

Grapefruit:
- contains compounds that inhibit CYP 3A4, one of the p450s found in GI cells which contributes to first pass effect
- when inhibited it increases pharmacological effect normally observed with that dose

Tyramine:
- antidepressants of the monoamine oxidase inhibitor class and any food containing tyramine, such as ages cheddar cheese
- monoamine oxidase inhibitors prevent the inactivation of tyramine, and tyramine can cause a large increase in blood pressure leading to a hypersensitive crisis

100
Q

Drug discovery and development

A
  1. identify biological target
  2. identify pharmacological effects
  3. conduct more studies

drug development: can take ~2-8 years and up to 25 000 different chemical compounds

101
Q

Stages of Drug development: 25,000 compounds (3-6 years)

A

Preclinical studies:
1. pharmacological studies
2. toxicology studies
a. acute toxicity study
b. sub-chronic study
c. chronic toxicity study

102
Q

stages of drug development: 30 compounds (6-7 years)

A

Clinical trials
1. Phase 1: determining safe dosages
2. phase 2: determining the initial efficacy
3. phase 3: conducting randomized control trials

103
Q

Stages of drug development: 1 FDA approved drug (0.5-2 years)

A
  1. health canada review
  2. manufacturing: genetic vs brand name
    a. bioavailability studies

phase 4: post market surveillance

PHAR370- Fundamentals of Pharmacology and Therapeutics (5 decks)

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