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HLSC 220 > Principles of Pharmacology > Flashcards

Principles of Pharmacology Flashcards

1
Q

Pharmacodynamics

A

What the drug does to the body
-the connection between drug concentration and effect

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2
Q

Pharmakinetics

A

What the drug does to the body
-How the drug concentration in plasma changes over time

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3
Q

What does pharmakinetics provide information to

A
  1. extent and duration
  2. preferred dose and dosing interval
  3. Preferred route of administration
  4. how to optimize therapies
  5. how to avoid toxicities
  6. how to avoid drug interactions
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4
Q

4 Stages of pharmakinetics

A

Administration
Distribution
Metabolism
Excretion
(ADME)

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5
Q

Administration

(3)

A
  1. can affect how quick + how much drug enters systemic circulation
  2. Not all routes of administration are suitable for all drugs
  3. drug must be administered to reach site of administration
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6
Q

Formulations for administration depend on:

A
  1. Route of admission
  2. Time course of action
  3. Active drug concentration
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7
Q

How quick and how much drug enter systemic circulation are important factors for

A
  1. Determining peak plasma concentrations + duration of drug
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8
Q

Chosen route of drug depends on

A

desired outcome

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9
Q

Enteral administration

A

Entry through the GI tract

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10
Q

Where is enteral administration absorbed

A
  1. between the mouth and anus
  2. Usually stomach or small intestine
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11
Q

How much drug is absorbed through enteral absorption

A

Less then 100% due to first pass metabolism

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12
Q

Enteral absorption depends on

A
  1. disintegration/solubility
  2. acidity of GI tract
  3. GI blood flow
  4. drug stability
  5. gastric emptying and motility
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13
Q

Enteral administration benefits

A
  1. Easy, safe, cheap
  2. No need for sterility/purity
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14
Q

Enteral administration Drawbacks

A
  1. Acid sensitive + protein drugs are unstable
  2. Ph must be conscious and cooperative
  3. variable absorption + bioavailability
  4. possible upper GI irritation
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15
Q

First pass metabolism is also called

A

pre-systemic elimination

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16
Q

First pass metabolism

A

drugs passing through liver before entering systemic circulation

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17
Q

what does the liver do during first pass metabolism

A
  1. Site of drug metabolism
  2. drug concentration can dramatically decrease
  3. extent of drug metabolism varies for different drugs
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18
Q

What does liver damage do to first pass metabolism

A
  1. decreased liver metabolism
  2. creates unpredictable drug metabolism and concentrations
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19
Q

What does metabolism do to drugs

A

changes molecules
eg. Codeine becomes morphine

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20
Q

When does first pass metabolism occur

A

with enteral administration
-especially PO

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21
Q

Rectal (PR) Administration

A

Absorption through rectal mucosa

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22
Q

Rectal (PR) Benefits

A
  1. Rapid absorption
  2. cheap, easy
  3. Useful if pt. can’t or won’t swallow
  4. Less first pass effect
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23
Q

Rectal (PR) drawbacks

A
  1. often incomplete absorption
  2. irritation on mucosal lining
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24
Q

Sublingual (SL) Administration

A

Drug is placed under tongue to dissolve and absorbe

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25
Q

Sublingual (SL) Benefits

A
  1. Rapid
  2. no first pass effect
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26
Q

What does no first pass effect mean

A

drug enters systemic blood immediately

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27
Q

Sublingual (SL) drawbacks

A
  1. many drugs taste bad
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28
Q

Buccal Administration

A

drug placed between gums and lip to be absorbed

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29
Q

Types of enteral Administration

A
  1. PO
  2. PR
  3. SL
  4. Buccal
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30
Q

Enteral administration formulations

A
  1. Tablets
  2. Capsules
  3. Liquids
  4. Buccal film
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31
Q

Parenteral Administration

A

Not absorbed through GI tract

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32
Q

Subcutaneous Injection (SC)

A

Drug is injected under skin

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33
Q

Subcutaneous injection benefits

A
  1. Rapid effect due to general circulation
  2. useful for local injection/delivery
  3. easy self administration
  4. easy to control
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34
Q

Subcutaneous injection drawbacks

A
  1. requires sterile drug
  2. some pts don’t like injections
  3. absorption affected by blood flow and injection volume
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35
Q

Intramuscular Injection (IM)

A

Drugs injected into skeletal muscle

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36
Q

Intramuscular injection benefits

A
  1. cane be into a large muscle mass
  2. self administered
  3. absorption into systemic circulation can be controlled
  4. oil based formulation allow for slower absorption (depot bolus)
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37
Q

Intramuscular injection drawbacks

A
  1. can be painful
  2. must be sterile
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38
Q

Intravenous (IV)

A

Drugs injected directly into vein as a rapid bolus (Push) or continuous infusion (Drip)

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39
Q

Intravenous benefits

A
  1. all drug enters the bloodstream
  2. rapid distribution + onset of drug
  3. large drug volumes
  4. very predictable
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40
Q

Intravenous drawbacks

A
  1. requires skilled administration + close monitoring
  2. Drug must be sterile
  3. greater cost
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41
Q

Inhalation

A

drug inhaled into airways

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42
Q

Inhalation benefits

A
  1. useful for local action (bronchodilators) but also into pulmonary circulation
  2. no first pass effect
    3.useful for gasses
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43
Q

Inhalation drawbacks

A
  1. limited absorption of large proteins
  2. possible irritation of lung lining
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44
Q

Inhalation formulations

A
  1. gasses or gas mixtures
  2. inhalers for pulmonary use
  3. pressurized aerosol and other containers allow unused product to remain uncontaminated for later use
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45
Q

Types on inhalers

A
  1. particulate powders
  2. nebulized (mists)
46
Q

Other parenteral routes

A
  1. intraarticular injection (joints)
  2. intracardiac injection (cardiac)
    3.epidural injection
  3. spinal injection (spinal fluid)
47
Q

Topical Administration

A

applied on surfaces

48
Q

Topical administration locations

A
  1. skin
  2. eyes
  3. ears
  4. nose
  5. vagina
49
Q

Transdermal Administration

A
  1. Absorbed through the skin
  2. Local and systemic effects
50
Q

Transdermal benefits

A
  1. cheap and easy
  2. simple local administration
  3. no first pass effect
51
Q

Transdermal drawbacks

A
  1. not suitable for many drugs (fat insoluble)
  2. absorption affected by skin hydration
52
Q

Transdermal formulations

A
  1. creams, gels, ointments
  2. absorption can be enhanced by suspension in an oily vehicle
  3. controlled by release patched (nicotine)
  4. topical aerosol spray
53
Q

Absorption

A

Entry of drug into circulating system

54
Q

Example of absorption

A
  1. Drug must pass through the epithelial cells of the GI tract
  2. Then into blood flowing through the capillaries of the gut wall
55
Q

Chemical factors affecting drug absorption

A
  1. Drug size
  2. Lipid solubility
  3. Drug charge
  4. Bioavailability
56
Q

Bioavailability

A

The proportion of drug that passes into systemic circulation post administration, taking into account both absorption and metabolic degradation

57
Q

Bioavailability for enteral routes

A

Less then 100%

58
Q

Bioavailability for parenteral routes

A

High

59
Q

What affects bioavailability

A
  1. first pass effect
  2. drug absorption
60
Q

What factors of drug absorption affect bioavailability

A
  1. Solubility of drug
  2. Stability of drug
  3. Formulation of drug
61
Q

Distribution

A
  1. follows absorption
  2. mixed into blood quick
62
Q

3 Determining factors of distribution

A
  1. Blood flow to tissues
  2. Exiting the vascular system
  3. Entering cells
63
Q

Initial distribution

A

rapid in the first few minutes, depends entirely of rate of blood flow to given tissues

64
Q

Tissues with high bloodflow

A

exposed to drug more quickly then those with less

65
Q

Rapid distribution goes to

A

heart, liver, kidneys

66
Q

slow distribution goes to

A

muscles, skin, fat

67
Q

Second distribution

A
  1. slower
  2. depends on where drugs like to be
68
Q

What affects distribution

A
  1. lean mass (watery environment)
  2. fat solubility of drug accumulation
  3. Plasma protein binding
69
Q

Plasma protein binding

A
  1. most drug molecules don’t float freely in blood
  2. often bound to plasma proteins (up to 90%)
  3. Albumin
  4. only free drugs create effects
70
Q

Albumin

A
  • most common plasma protein
  • major carrier drug
71
Q

liver disease affect on distribution

A

decreases blood albumin- more free drug molecules to create effects

72
Q

Metabolism

A
  1. modification/change of drug molecule by enzymes
  2. mostly occur in liver, gut, kidney, lungs, plasma, placenta
  3. metabolized by cytochrome enzymes
    4.varies between people
  4. inhibiting cyps can be dangerous
  5. cyp enzyme induction
73
Q

What inhibits CYPs

A

-grape fruit juice
-other drugs

74
Q

CYP enzyme induction

A

cells stimulated to make more enzymes

75
Q

Therapeutic consequences of drug metabolism

A
  1. accelerated renal drug excretion
  2. drug inactivation
  3. increased therapeutic action
  4. activation of prodrugs
  5. increased or decreased drug toxicity
76
Q

Accelerated renal drug excretion

A
  1. most common effect
  2. acids water solubility
77
Q

Drug excretion

A
  1. removal from body
  2. mostly through kidney
  3. some may be excreted in an altered form
  4. most drugs must be metabolized before they work
  5. Drug enters tubular fluid
78
Q

Excretion depends on

A
  1. Plasma protein binding
  2. Drug fat solubility
79
Q

Excretion is through

A
  1. Kidney
  2. GI tract
  3. Sweat
  4. Breast milk
80
Q

Drug enters tubular fluid

A
  1. filtration through glomular capillaries
  2. active transport through specialized carriers
81
Q

What can be excreted in unaltered formes

A

some antibiotics

82
Q

Why do most drugs need to be metabolized first

A
  1. renders the drug active
  2. makes the drug more water soluble/less fat soluble
83
Q

Dosage Regimes

A

Effective treatment requires effective dosage regimes
-dose size
-dose frequency

84
Q

Time course of drugs

A

duration of effects is determined by the combination of metabolism + excretion

85
Q

Drug steady state

A

When there is a consistent level of drug in the body

86
Q

What does drug steady state depend on

A

Half life of the drug

87
Q

Half life

A
  1. time required for the amount of drug in the body to decrease 50%
88
Q

What does half life measure

A

the rate drugs are removed from the body

89
Q

A long half life takes

A

a long time to reach steady state with multiple doses

90
Q

A short half life takes

A

a short amount of time to reach steady state with multiple doses

91
Q

How many half lives does it take to reach steady state

A

4-5

92
Q

Most drugs get metabolized/excreted according to

A

principles of percentage loss of drug over time

93
Q

Very few drugs leave the body at a consistent rate: what are 2 examples

A
  1. Ethanol (alcohol)
  2. Phenytoin
94
Q

Pharmacodynamics is the

A

relationship between drug concentration at the site of action and its biological effect

95
Q

Drug receptors

A
  1. to elicit an effect on the body drugs must interact directly with cells
  2. usually binding to specific targets
96
Q

drug receptors are

A

protein targets

97
Q

drugs exhibit selectively for their receptors: meaning

A
  1. they interact with their target molecules, cell, or tissues
  2. high concentrations they lose this selectively
98
Q

2 common possibilities of drug action

A
  1. response
  2. no response
99
Q

What does drug binding depend on

A

the affinity or stickiness of the drug for its target

100
Q

Agonist

A

elicits a response

101
Q

Antagonist

A

Prevents a response to an endogenous or neurotransmitter agent

102
Q

Dose response relationship

A
  1. relationship between size of administered dose and intensity of response produced
103
Q

Dose response relationship is determined by

A
  1. minimum amount of drug to be used
  2. maximum response a drug can elicit
  3. how much to increase the dose to increase the desired effect
104
Q

Onset

A

Time it takes for the drug to elicit a therapeutic response

105
Q

Peak

A

Time it takes for a drug to reach max therapeutic response
-Troughs and MEC

106
Q

Trough

A

lowest blood level of the drug
- too low drug becomes ineffective

107
Q

MEC

A

Minimum effective communication

108
Q

Minimum effective communication (MEC)

A

plasma drug level that must be reached for therapeutic effect

109
Q

Duration

A

time for which a drug concentration is sufficient to elicit a therapeutic response

110
Q

Therapeutic Index

A
  1. Measures drug safety
  2. Ratio of the drug toxic: effective drug concentration
  3. Smaller the therapeutic index the less safe the drug
111
Q

Be extra careful with drugs with a _____ Therapeutic index, ____ dangerous

A

Narrow, more dangerous

112
Q

Non-receptor Drugs

A

simple physical or chemical interactions with other molecules
-Antacid, saline laxatives, chelating agents

HLSC 220 (10 decks)

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