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PRIN > PRIN 12 Pharmacology > Flashcards

PRIN 12 Pharmacology Flashcards

1
Q

QD

A

every day

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2
Q

QID

A

4 times daily

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3
Q

TID

A

3 times daily

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4
Q

BID

A

twice daily

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5
Q

PO

A

Oral

per orum

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6
Q

PRN

A

as needed

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7
Q

–oxetine

A

antidepressants

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8
Q

–mycin

A

macrolide antibiotics

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9
Q

–azole

A

azole antifungals

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10
Q

ADME process

A

Absorption
Distribution
Metabolism
Excretion

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11
Q

sl

A

Sublingual

most gets absorbed into capillary network under tongue

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12
Q

pr

A

rectal

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13
Q

sc

A

Subcutaneous

aka “subQ”

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14
Q

How to give sc?

A

Subcutaneous

45 degree angle

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15
Q

How to give intradermal?

A

10-15 degree angle

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16
Q

What is Transdermal?

A

“Patch”
Drug is absorbed through the skin and enters blood.
Enables steady, consistent release

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17
Q

How are most drugs absorbed?

A

Passive Diffusion

Influenced by:

  • *conc gradient
  • *size
  • *lipid solubility
  • *UNCHARGED
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18
Q

How does the body irreversibly bio-transform drugs to increase their likelihood of excretion?

A

LIVER: 2 steps:

PHASE 1: Oxidation, Reduction, Hydrolysis

PHASE 2: Conjugation

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19
Q

What is Cyp?

A

Superfamily of enzymes:
Cytochrome P450

MOA: add or uncover chemical groups to make them MORE POLAR … increase excretion

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20
Q

What can inhibit Cyp?

What is the result?

A

Grapefruit Juice

RESULT: drug is not broken down by body as usual rate and therefore we have a heightened dose of drug

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21
Q

What can promote Cyp?

What is the result?

A

Alcohol - induces the Cyp pathway

RESULT: drug is broken down too quickly and is warranted less therapeutic

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22
Q

What is Phase II?

A

Conjugative Enzymes

Covalently add large, polar, endogenous molecules to drug molecule … promote excretion

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23
Q

Why are Oral doses so much higher than IV doses?

A

100% of drug by IV is made available

HOWEVER, oral drugs are reduced because liver breaks lots of it down before the drug has even been circulated around the body

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24
Q

What are necessary characteristics of a drug in order to undergo passive glomerular filtration?

A

Small
Unbound drug
<20kDa

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25
Q

How are large or protein-bound drugs excreted?

A

ACTIVE tubular secretion

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26
Q

Once in the filtrate, what happens to uncharged drugs?

A

May be reabsorbed due to being driven by conc. gradient

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27
Q

How can the liver prolong the lifetime of a drug?

A

Enterohepatic Recirculation

Drug undergoes Gluc-uron-idation in liver to become polar … passes through bile duct … enters duodenum … gets hydrolyzed by bacterial gluc-uro-nidase to become no longer polar … gets absorbed into capillary network … carried to liver

BOTTEM LINE: drug gets regenerated in the GI and reabsorbed

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28
Q

Oral Contraceptives rely on Enterohepatic Recirculation …. what might be the effect of prescribing Antibiotics?

A

Antibiotics will decrease bacteria in gut that are necessary to regenerate drug for reaborption.

RESULT: drug will leave body prematurely and the therapeutic dose of the OC will not be achieved … babies …

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29
Q

MTC

A

Max Toxic Concentration

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30
Q

MEC

A

Min Effective Concentration

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31
Q

Formula for half-life

A

T-half life = ln2/k

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32
Q

How long does it take to completely void the body of drug?

A

5 half-lives

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33
Q

How do k and T(1/2) relate to Route of Administration>

A

k and T(1/2) are INDEPENDENT of administration route. They are always the same.

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34
Q

When is steady state attained?

A

After 5 half-lives

Time to reach steady state is ALWAYS the same

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35
Q

Css = ?

A

Steady-State Mean

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36
Q

What are the two approaches used in getting to steady state?

A

(1) Exponential Approach: give small, repeat doses at intervals equal to the half-life … steady state reached after 5 rounds
(2) LD followed by MD

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37
Q

In the formula for Loading Dose, what is Vd?

LD = C-target x Vd

A

Vd = Volume of Distribution of Drug

38
Q

First Order VS Zero Order Kinetics

A

FIRST ORDER:
elimination processes not saturated at therapeutic drug conc.
*drug is eliminated by a constant FRACTION

ZERO ORDER:

  • elimination processes become saturated
  • drug is eliminated in LINEAR / constant fashion
39
Q

What is Therapeutic Drug Monitoring?

When is it Used?

A

Provides patient-specific dosing info

Useful for drugs with narrow therapeutic range and special populations

40
Q

During distribution of drug, in what order is it delivered throughout the tissues?

A

(1) Plasma
(2) Brain, heart, liver, kidneys
(3) Skeletal Muscle, Skin
(4) Adipose Tissue

41
Q

What can occur in the plasma that radically affects the rate at which the drug can be distributed?

A

Protein Binding … this makes the drugs big and prevents them from diffusing into tissues

42
Q

In plasma protein binding, what can weak acids bind to?

A

Albumin

43
Q

In plasma protein binding, what can weak bases bind to?

A

a1-acid glycoprotein

44
Q

What is Vd?

A

Volume of Distribution

LARGE Vd:
drug distributes outside blood and boyd fluids into tissues

SMALL Vd:
drug has limited distribution, typically restricted to blood or physiological fluids

45
Q

What is the most understood reason for differences in drug metabolism?

A

Cyp 450 polymorphisms

46
Q

What are “normal metabolizers” called?

A

Extensive Metabolizers

47
Q

Why do Asians have a harder time with alcohol?

A

They have a lower amount of ACDH

Alcohol
**ADH
Acetaldehyde (toxic)
**ACDH
Acetate
48
Q

Pediatric Age Groups

A

Neonate: birth - 28 days
Infant: 29 days - 12 months\
Child: > 1 year

49
Q

What is the effect of gastric acid quantity in drug absorption for pediatrics and geriatrics?

A

Both have less stomach acid. Therefore, pH is higher.
Weak Acid Drugs will be LESS absorbed
Weak Base Drugs will be MORE absorbed

50
Q

What is important to know about kids and Per-cutaneous Delivery?

A

Kids have a thinner Stratum Corneum

Therefore, more is absorbed … MUST lower dose

51
Q

How are kids unique in Vd?

A

Vd = Volume Distribution

Kids are MORE water … need lower dose

Kids are LESS protein … need lower dose since drug is less bound by protein and more is available to be absorbed

52
Q

How are pediatrics unique in Metabolism?

A

Phase I & II is decreased

Therefore, increased drug half-life … must lower dose

53
Q

How are pediatrics unique in Excretion?

A

GFR is reduced … therefore, less is excreted … must lower dose

54
Q

Geriatric Age Groups

A

“Young” Old: 65-84

“Old” Old: 85 & older

55
Q

How is Absorption affected in Geriatrics?

A

Increased gastric pH … acid drugs are less absorbed / weak bases are more absored

Decreased GI emptying & decreased gastric flow: decrease in absorption

56
Q

How is Distribution affected in Geriatrics?

A

Increased Adipose Tissue:

Decreased TBW: drug less distributed

Decreased Serum Albumin: drug more absorbed

57
Q

How is Metabolism affected in Geriatrics?

A

Phase 1 enzymes have lower activity
Phase 2 enzymes are the same

THEREFORE … when possible, choose drugs metabolized only by Phase II system

58
Q

Geriatrics & Liver

A

Decreased liver mass

Decreased hepatic flow

59
Q

How is Excretion affected in Geriatrics?

A

Kidney is smaller and less functional … excretion is impaired … increased drug half-life

60
Q

What is Amitryptyline?

What is it used for?

A

Antidepressant from Class: Tricyclic

61
Q

What is a chelator?

A

Organic chemical that bonds with and removes free metal ions from solutions

62
Q

What is an example of an agent that chelates a drug?

A

Ca2+ chelates Tetracycline

(result: BOTH become inaccessible to the patient

63
Q

How may a drug reduce absorption of another drug?

A

DIRECTLY:
by binding other drugs

INDIRECTLY:
by altering - 
(1) gastric pH
(2) GI motitlity
(3) transport proteins such as P-glycoprotein
64
Q

What is the effect of Anti-cholinergics on absorption?

A

Anti-cholinergics slow down GI motility by delaying gastric emptying

Result: lowers therapeutic effect

65
Q

What is the most important factor involved in drug absorption?

A

Activity level of p-glycoprotein

P-gp can be inhibited or induced

66
Q

What is the most important factor involved in drug metabolism?

A

Cytochrome P450 enzymes
3A4

(perform Phase 1 oxidative metabolism of substrates)

67
Q

Although not as important, Phase II reactions contribute to drug metabolism. What family of enzymes performs such reactions?

A

Uridine 5’-diphosphate gluo-urono-syl-transferases

68
Q

What is the name of the “drug recycling program?

A

Enterohepatic Recirculation

Inactivated in liver and reactivated in gut by bacteria

69
Q

What is the function of MAO?

A

MOA breaks down amines such as:

NE, dopamine, serotonin, Tyramine

70
Q

What does Tyramine do?

A

Circulating Tyramine releases NE

71
Q

What is the “Wine Cheese Reaction”

A

Aged foods contain high levels of Tyramine, which when ingested in high quantities, would result in an adverse effect for patients taking an MAO inhibitor for treatment of depression

72
Q

Give an example of a synergistic pharmacodynamic interaction.

A

Warfarin & ASA / ginkgo

Alcohol & CNS depressant

73
Q

Give an example of an antagonistic pharmacodynamic interaction.

A

Salbutamol & B-Blocker

74
Q

What does Vitamin K do?

A

Promotes coagulation

75
Q

What is the interaction between Warfarin & Vit K?

A

Warfarin inhibits Vit K
Warfarin is an ANTI-coagulant

(best to have consistent moderate intake of cruciferous veggies rather than occasional huge intake)

76
Q

What are the common CYP 450 enzyme inhibitors?

A

Fluoxetine
Erythromycin
Ketoconazole
Grapefruit Juice

77
Q

What are the common CYP 450 enzyme inducers?

A 
Rifampin
Caramezepine
Phenytoin
St John's Wort
Ethanol
Cigg Smoke
78
Q

What is the effect of Fluoxetine on CYP 450?

A

CYP 450 Inhibitor

Antidepressant
other: paroxetine

79
Q

What is the effect of Erythromycin on CYP 450?

A

CYP 450 Inhibitor

Macrolide Antibiotic
other: Clarithromycin

80
Q

What is the effect of Ketoconazole on CYP 450?

A

CYP 450 Inhibitor

Anzole Antofungal
other: Fluconazole

81
Q

For some people, what can play a significant role in drug interaction?

A

Genetics!

82
Q

What is Cyclosporin for?

A

Immuno-suppressant

Common anti-rejection drug used in transplants

83
Q

What is Mycophenolate for?

A

Immuno-suppressant

Common anti-rejection drug used in transplants

84
Q

What is Prednisone for?

A

Immuno-suppressant

Common anti-rejection drug used in transplants

85
Q

What was interaction between between cyclosporin & fluconazole?

A

Fluconazole inhibits Cyp P450.

Result: Cyclosporin is not metabolized fast enough and reaches toxic levels

86
Q

What is Amitriptyline for?

A

Antidepressant (Class: Tricyclic)

Has Anticholinergic effects:
eg) dry mouth, difficulty peeing
Inhibits reuptake of Serotonin & NE

87
Q

What is Anhedonia?

A

lack of pleasure

not caring

88
Q

What was interaction between between cyclosporin & St John’s Wort?

A

St John’s Wort induces Cyp 450 AND p-glycoprotein.

Result: Cyclosporin is metabolized TOO fast and is no longer therapeutic …. immunosuppression is lifted … transplant rejection

89
Q

What is “first pass?”

A

Drugs that undergo extensive hepatic metabolism

90
Q

Herbal products are currently regulated under which piece of legislation?

A

Natural Health Product Regulations

91
Q

What’s the problem with broccoli and Warfarin?

A

Broccoli contains Vitamin K, which opposes the pharmacodynamic actions of Warfarin, a Vitamin K antagonist

PRIN (13 decks)

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