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Western > Pharm 2060 > Flashcards

Pharm 2060 Flashcards

1
Q

“Pharmacology” derived from…

A

Greek: pharmakon (remedy), logos (study)

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2
Q

“Pharmacology” =

A

Study of drugs

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3
Q

4 Aspects

A

How a drug is delivered
How a drug works (MOA)
Therapeutic effect
Adverse effects

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4
Q

3 Classifications:

A

Drugs
Biologics
Natural health products

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5
Q

Drug classification: antibody

A

Biologics

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6
Q

Drug classification: hormone

A

Biologics

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7
Q

Drug classification: herbals

A

Natural health products

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8
Q

Drug classification: vitamins

A

Natural health products

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9
Q

Drug classification: minerals

A

Natural health products

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10
Q

Health Canada functions under ___?

A

Food and drug act and regulations

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11
Q

What branch of Health Canada has 3 directorates?

A

Products and food branch

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12
Q

3 directorates of HC?

A

Therapeutic products directorate
Biologics and genetic therapies directorate
Natural health products directorate

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13
Q

What is the chemical name?

A

Describes the drug structure of molecule

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14
Q

Who uses chemical name?

A

Chemists; not commonly used in pharmacology

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15
Q

What is the generic name?

A

Unique name that identifies the drug

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16
Q

Who uses the generic name?

A

Most commonly used in pharmacology; should be used by health care professionals but often isn’t

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17
Q

What is the trade name?

A

Name assigned by drug company

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18
Q

Problem with using trade name?

A

Many companies may produce same drug and therefore have many trade names.

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19
Q

How many steps of approval of marketed drugs in Canada are there?

A

7

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20
Q

Approval of marketed drugs in Canada: step 1?

A

Drug discovery and preclinical testing

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21
Q

How long does step 1/pre clinical testing for drug approval take?

A

6.5 years

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22
Q

How is step 1/pre clinical testing for drug approval carried out?

A

Cultured cells, living tissue, or experimental animals.

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23
Q

Purpose of step 1/preclinical testing of drugs?

A

Evalutate biological effects, pharmokinetics, and toxicity

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24
Q

Approval of marketed drugs in Canada: step 2?

A

Clinical trial application

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25
Q

How long does step 2/trial application of drug approval take?

A

30 days

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26
Q

How is step 2/trial application of drug approval carried out?

A

Submission of paperwork detailing all preclinical data to Health Canada

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27
Q

Approval of marketed drugs in Canada: step 3?

A

Phase I clinical trial

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28
Q

How long does step 3/phase I clinical trial take?

A

1 year

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29
Q

How is step 3/phase I clinical trial carried out?

A

20-100 healthy volunteers

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30
Q

Purpose of step 3/phase I clinical trial?

A

Evaluate phamokinetics and pharmodynamics

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31
Q

Approval of marketed drugs in Canada: step 4?

A

Phase II clinical trial

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32
Q

How long does step 4/phase II clinical trial take?

A

2 years

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33
Q

How is step 4/phase II clinical trial carried out?

A

300-500 patients with target disorder

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34
Q

Purpose of step 4/phase II clinical trial?

A

Therapeutic effectiveness, side effects and dosing information is gathered

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35
Q

Approval of marketed drugs in Canada: step 5?

A

Phase III clinical trial

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36
Q

How long does step 5/phase III clinical trial take?

A

4 years

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37
Q

How is step 5/phase III clinical trial carried out?

A

500-5000 patients with target disorder

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38
Q

Purpose of step 5/phase III clinical trial?

A

Therapeutic effectiveness verified, long term side effects assessed

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39
Q

Approval of marketed drugs in Canada: step 6?

A

New Drug Submission to Health Canada

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40
Q

How long does a new drug submission (NDS) take?

A

1.5 years

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41
Q

Components of a new drug submission?

A

Report detailing therapeutic effectiveness and safety. Includes results from pre clinical and clinical studies.

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42
Q

What does Health Canada issue after a successful new drug submission?

A

Notice of compliance (NOC)

Drug identification number (DIN)

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43
Q

Approval of marketed drugs in Canada: step 7?

A

Phase IV clinical trial

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44
Q

Purpose of phase IV clinical trial?

A

HC monitors efficacy and safety of the drug after it has been marketed. Drugs can be pulled from the market if not efficacious or safe.

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45
Q

What drug was pulled from the market in 2004?

A

Vioxx

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46
Q

“Pharmokinetics” =

A

Study of drug movement in body (what body does to drug)

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47
Q

Components of pharmokinetics:

A

Absorption
Distribution
Metabolism
Excretion

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48
Q

The majority of absorption from orally ingested drugs occurs in the ___?

A

Small intestine

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49
Q

Pathway of orally ingested drugs?

A

Stomach - small intestine - portal vein - liver - systemic circulation to tissues OR bile duct to gall bladder and LI

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50
Q

Pathway of injected drugs?

A

Systemic circulation - tissues OR liver excretion OR kidney excretion

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51
Q

Primary site of drug metabolism?

A

Liver

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52
Q

Primary site of drug excretion?

A

Kidney

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53
Q

3 Routes of administration categories?

A

Enteral, parenteral, other

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54
Q

Type of administration: oral?

A

Enteral

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55
Q

Type of administration: rectal?

A

Enteral

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56
Q

Type of administration: intravenous?

A

Parenteral

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57
Q

Type of administration: intramuscular?

A

Parenteral

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58
Q

Type of administration: subcutaneous?

A

Parenteral

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59
Q

Type of administration: creams?

A

Topical/transdermal

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60
Q

Type of administration: patches?

A

Topical/transdermal

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61
Q

Intestinal villi form ____ against oral drugs/toxins/nutrients?

A

Barrier

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62
Q

Function of nucleus?

A

Contains genetic material/DNA

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63
Q

Function of smooth ER?

A

Metabolizes drugs, carbohydrates, and steroids

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64
Q

Function of rough ER?

A

Synthesizes proteins

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65
Q

Function of golgi?

A

Processes and packages proteins and lipids

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66
Q

Function of mitochondria?

A

Produces ATP

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67
Q

Function of cell membrane?

A

Separates the intracellular and extracellular environments

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68
Q

Phospholipid: head?

A

Polar/water soluble; phosphate

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69
Q

Phospholipid: tail?

A

Lipid soluble

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70
Q

3 ways to cross cell membranes:

A

Direct penetration
Ion channels and pores
Specific transport proteins

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71
Q

Necessary drug components for direct cell membrane penetration?

A

Lipophilic

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72
Q

Necessary drug components for transmembrane travel by ion channels and pores?

A

Small (molecular weight

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73
Q

Function of uptake transporters?

A

Transport drugs from outside the cell to inside the cell.

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74
Q

What are uptake transporters important mediators for?

A

Intestinal absorption, renal excretion, reaching target sites of action inside cells.

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75
Q

Function of efflux transporters?

A

Transport drugs from inside the cell to outside the cell.

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76
Q

What are efflux transporters important for?

A

Protecting cells from exposure to drugs, protection from drug absorption across intestine

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77
Q

Where are efflux transporters found? (4)

A

Intestine, placenta, kidney, blood brain barrier

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78
Q

What are the 5 types of drug molecules?

A 
Polar
Ions
Quaternary ammonium compounds
Ionizable molecules
Lipophilic
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79
Q

Characteristics of polar molecules?

A

Water soluble, have an uneven distribution of electrical charge but have no net charge.

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80
Q

What type of molecule is water?

A

Polar

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81
Q

What type of molecule is glucose?

A

Polar

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82
Q

What type of molecule is the antibiotic ‘kanamycin’?

A

Polar

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83
Q

How do polar molecules cross cell membranes?

A

Specific transport proteins

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84
Q

What are the characteristics of an ion?

A

Have a total number of electrons that is not equal to the total number of proteins resulting in a net charge

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85
Q

How do ions cross cell membranes?

A

Ion channels

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86
Q

What are the characteristics of quaternary ammonium compounds?

A

Have at least 1 nitrogen atom, have a positive charge at all times.

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87
Q

How do quaternary ammonium compounds cross cell membranes?

A

Specific transport proteins

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88
Q

What are the characteristics of ionizable molecules?

A

Can exist in charged (weak acid/base) or uncharged form.

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89
Q

What determines whether a ionizable molecule is charged?

A

pH of the surrounding environment

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90
Q

Weak acids (ionizable molecule) is ___ in an acidic environment?

A

Non ionized

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91
Q

Weak acids (ionizable molecule) is ___ in an alkaline environment?

A

Ionized

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92
Q

Weak bases (ionizable molecule) is ___ in an acidic environment?

A

Ionized

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93
Q

Weak bases (ionizable molecule) is ___ in an alkaline environment?

A

Non ionized

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94
Q

What type of ionizable molecules are the majority of drugs?

A

Weak bases

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95
Q

Weak bases are able to cross the membrane easier in an _____ environment?

A

Alkaline

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96
Q

Weak acids are able to cross the membrane easier in an _____ environment?

A

Acidic

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97
Q

How do ionizable molecules cross the cell membrane?

A

Direct penetration *ONLY when non ionized

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98
Q

How do lipophilic molecules cross the cell membrane?

A

Direct penetration

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99
Q

When does ion trapping occur?

A

Difference in pH on different sides of the membrane

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100
Q

What type of drugs experience ion trapping?

A

Ionizable molecules

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101
Q

What side of the membrane do ionizable molecules get trapped?

A

The side that they are charged.

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102
Q

When is ion trapping clinically used?

A

Cases of drug overdose.

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103
Q

What are the 3 areas of large capillary beds?

A

Kidneys, GI tract, lungs

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104
Q

What are the gaps called between capillaries?

A

Fenestrations

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105
Q

What types of drugs can pass through fenestrations to leave the blood?

A

Hydrophilic drugs (and lipophilic)

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106
Q

What area of the body does NOT have fenestrations?

A

Blood brain barrier

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107
Q

What type of cells line the capillaries at the blood brain barrier?

A

Astrocytes

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108
Q

How can drugs enter the brain?

A

Lipophilic OR have specific transport proteins

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109
Q

What type of cells line the capillaries NOT at the blood brain barrier?

A

Tissue cells

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110
Q

Drug absorption =

A

The movement of the drug from site of administration into the blood

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111
Q

The rate of drug absorption determines ___?

A

How quickly the drug effect will occur

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112
Q

The amount of drug absorption determines ___ ?

A

How intensive the effect of the drug will be

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113
Q

What are the 6 factors that effect rate of absorption?

A 
Rate of dissolution
Surface area
Local blood flow
Lipid solubility
pH partitioning
Activity of drug transport proteins
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114
Q

Dissolution =

A

Dissolving of drugs into solution (must be disintegrated then dissolved)

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115
Q

What is the greatest determinant of drug absorption?

A

Surface area

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116
Q

How does local blood flow effect drug absorption rate?

A

Areas with high blood flow maintain a concentration gradient which drives absorption

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117
Q

In what conditions can blood flow be decreased?

A

Heart failure, severe hypotension, hypothermia, circulatory shock

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118
Q

In what way does pH partitioning effect drug absorption?

A

Absorption is greater when there’s a difference between pH at site of administration and the blood such that the drug is ionized in the blood (trapped in blood)

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119
Q

Per os =

A

By mouth (Latin) = oral administration

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120
Q

What is the most common route of administration?

A

Oral

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121
Q

What are the 3 advantages of oral administration?

A

Safe, economical, convenient

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122
Q

What is the disadvantage to oral administration?

A

Incomplete and/or varied absorption

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123
Q

The rate of drug absorption in the intestine will be ______ than the stomach even if the drug is ionized.

A

Greater

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124
Q

What is the pharmaceutical phase?

A

The disintegration phase and the dissolution phase that occurs after a drug is swallowed.

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125
Q

What is gastric emptying?

A

The movement of the stomach contents into the intestine

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126
Q

How to increase gastric emptying: stomach contents?

A

Empty

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127
Q

How to increase gastric emptying: water temperature?

A

Cold

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128
Q

How to increase gastric emptying: laying down?

A

Lay on right side

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129
Q

How to increase gastric emptying: osmolality?

A

High (tube feeding)

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130
Q

How to increase gastric emptying: GI motility?

A

Increased by taking pro kinetic drug

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131
Q

How to decrease gastric emptying: stomach contents?

A

Full/high fat meal

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132
Q

How to decrease gastric emptying: laying down?

A

Left side

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133
Q

How to decrease gastric emptying: activity?

A

Heavy exercise

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134
Q

How to decrease gastric emptying: nerve inhibitors?

A

Anticholinergic drug to inhibit vagus nerve

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135
Q

What is enteric coating? Purpose?

A

Coating on drug that prevents dissolution in acidic environment of the stomach

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136
Q

When does enteric coating dissolve?

A

Alkaline environment of duodenum

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137
Q

When is enteric coating useful?

A

If drugs are destroyed by acidic stomach OR harmful to stomach

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138
Q

What is bioavailability?

A

Fraction of dose that reaches the systemic circulation unchanged

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139
Q

What influences bioavailability? (3)

A

Drug formulation
Route of administration
Degree of liver metabolism

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140
Q

What has the highest bioavailability?

A

Aqueous solution

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141
Q

What has the lowest bioavailability?

A

Time release tablets

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142
Q

How are sublingual drugs delivered?

A

Under the tongue

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143
Q

How do sublingual drugs get absorbed?

A

Dissolves under tounge and is absorbed across oral mucosa. Venous drainage leads to superior vena cava.

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144
Q

What area of the body are sublingual drugs exceptionally useful for?

A

Heart

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145
Q

Do sublingual drugs go through first pass liver metabolism?

A

No

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146
Q

What type of drugs can be sublingual?

A

Lipophilic, uncharged

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147
Q

What characteristics must transdermal drugs have?

A

Lipophilic to pass through epidermis
Hydrophilic to pass through extra cellular fluid
Small

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148
Q

What is the advantage to transdermal drugs?

A

Provides constant plasma drug levels with minimal peaks and troughs

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149
Q

Why are transdermal drugs removed for periods of time?

A

Tolerance can develop

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150
Q

How long are transdermal [patches] removed for?

A

6-10 hours/day

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151
Q

What are the 5 factors that affect transdermal absorption?

A 
Thickness of skin 
Hydration
Hair follicles 
Application area
Integrity of barrier
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152
Q

How does thickness of skin affect transdermal absorption?

A

Inversely proportional

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153
Q

How does hydration affect transdermal absorption?

A

Proportional

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154
Q

How does hair follicles affect transdermal absorption?

A

Proportional; can bypass epidermis (can be less lipophilic)

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155
Q

How does application area affect transdermal absorption?

A

Proportional

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156
Q

How does the integrity of the barrier affect transdermal absorption?

A

Proportional

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157
Q

In what skin conditions can transdermal absorption be increased?

A

Psoriasis, burned skin, abraded skin

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158
Q

How is a rectal suppository absorbed?

A

Through rectal mucosa into blood

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159
Q

When is a rectal drug helpful?

A

Unconscious or vomiting patient

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160
Q

Do rectal drugs get metabolized in the liver?

A

50% bypass liver

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161
Q

What is the disadvantages to rectal drugs?

A

Incomplete absorption, irritate rectal mucosa

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162
Q

What is an IV bolus?

A

Single dose administered over a short period (syringe)

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163
Q

What is an IV drip?

A

Drug is administered under continuous infusion over a prolonged period - diluted in saline

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164
Q

What is the BA of IV drugs?

A

100%

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165
Q

What are the 4 advantages to IV drugs?

A

BA 100%
Precise control of drug dosage and duration of action
Poorly soluble drugs can be diluted in a large volume
Irritant drugs can be delivered slowly

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166
Q

What are 4 disadvantages to IV drugs?

A

Expensive
Invasive
Inconvenient
Drug cannot be removed after injection (final)

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167
Q

What are 3 risks with IV drugs?

A

Infection
Fluid overload
Wrong formulation (i.e. supposed to be IM)

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168
Q

What are ‘subcutaneous’ drugs short formed to?

A

SubQ , SC

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169
Q

What are the barriers to absorption for subcutaneous injections?

A

Capillary wall

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170
Q

What sort of drugs should NOT be injected subcutaneously? Why?

A

Irritants BECAUSE severe pain/tissue sloughing

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171
Q

What are the primary determinants of rate of absorption in subcutaneous injections?

A

Blood flow

Water solubility

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172
Q

What are the determinants of rate of absorption in IM injections?

A
  1. Blood flow
  2. Water solubility
  3. Small enough to fit through fenestrations
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173
Q

What are the advantages of IM injections? (2)

A

Used for poorly soluble drugs

Administer depot preparations

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174
Q

What is a depot preparation?

A

Drug is administered all at once but is absorbed slowly over time

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175
Q

What are the disadvantages of IM injections? (2)

A

Pain

Local tissue/nerve problems if done incorrectly

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176
Q

What muscle for IM injections has the highest blood flow?

A

Deltoid

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177
Q

What gets more blood flow - VL or glutes?

A

Vastus lateralis

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178
Q

What are the 3 main muscles for IM injections?

A

Deltoid
VL
Glutes

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179
Q

What type of drugs can be inhaled and absorbed by lungs?

A

Gaseous and volatile

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180
Q

How are pulmonary drugs absorbed?

A

Pulmonary epithelium into blood

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181
Q

What is the rate of absorption for pulmonary drugs?

A

Instantaneous

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182
Q

What is the rate of absorption of pulmonary drugs so fast?

A

Large lung surface area

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183
Q

What is the major advantage of pulmonary drugs?

A

Drug delivered right to site of action in pulmonary diseases

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184
Q

What type of drug administration route is used for general anesthetic?

A

Pulmonary

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185
Q

What are the 4 things drugs can do in your body?

A

Stored
Metabolized
Excreted
Exert pharmacological effect

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186
Q

How many body compartments are there?

A

7

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187
Q

What is the interstitial space?

A

Extracellular fluid that surrounds cells.

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188
Q

What sort of drugs distribute into interstitial space?

A

Small/light

Hydrophilic

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189
Q

What is the total body water?

A

Fluid from interstitial space, intracellular fluid, plasma

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190
Q

What is plasma?

A

Non-cell containing component of blood

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191
Q

What sort of drugs distribute into plasma?

A

Drugs strongly bound to proteins

Large/heavy

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192
Q

What sort of drugs distribute into adipose tissue?

A

Lipophilic

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193
Q

Do any drugs bind to muscle tissue?

A

Yes. Some drugs bind tightly to muscle.

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194
Q

How are drugs absorbed in bone?

A

Absorb into crystal surface of bone with eventual incorporation into crystal lattice

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195
Q

Drugs can be stored and slowly released from what body compartment?

A

Bone

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196
Q

Where can protein bound drugs be distributed?

A

Trapped in plasma

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197
Q

What are the 3 drug distribution factors?

A

Blood flow to tissues
Ability of drug to move out of capillaries
Ability of drug to move into cells

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198
Q

Level of blood perfusion: liver?

A

High

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199
Q

Level of blood perfusion: kidney?

A

High

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200
Q

Level of blood perfusion: brain?

A

High

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201
Q

Level of blood perfusion: skin?

A

Low

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202
Q

Level of blood perfusion: fat?

A

Low

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203
Q

Level of blood perfusion: bone?

A

Low

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204
Q

Altered level of blood flow in neonates? Outcome?

A

Limited; limited/unpredictable drug distribution

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205
Q

Poor blood flow ___ limits drug distribution in adults

A

Rarely

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206
Q

In what circumstances can poor blood flow limit drug distribution?

A

Heart failure/shock
Solid tumor
Absesses

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207
Q

Tumour blood flow?

A

High outside; progressively less moving towards middle

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208
Q

What is an abscess?

A

Infection filled with pus

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209
Q

Abscess blood supply?

A

None

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210
Q

Why are abscesses so hard to treat with antibiotics?

A

No blood supply

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211
Q

Drug movement through fenestrations/through capillaries is ___ (speed). What is the exception?

A

Fast

Brain

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212
Q

What does P-GP stand for?

A

P glycoprotien

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213
Q

What is PGP?

A

Most widely studied efflux transporter

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214
Q

Why is PGP clinically significant?

A

Role in drug distribution

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215
Q

What are the 4 areas that PGP is found?

A

Liver
Intestine
Kidney
Brain

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216
Q

What liver cells is PGP found? Where in the liver?

A

Hepatocytes

Bile canaliculus membrane

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217
Q

What is the function of liver PGP?

A

Pump drugs from hepatocytes into bile

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218
Q

What is the purpose/result of liver PGP?

A

PGP substate drugs are eliminated in bile

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219
Q

What intestine cells is PGP found? Where in intestine?

A

Enterocytes

Apical/luminal membrane

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220
Q

Where in the kidney is PGP found?

A

Proximal tubule; apical membrane

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221
Q

What is the function of kidney PGP?

A

Excrete drugs into lumen of nephron to be excreted in urine

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222
Q

Where in the brain is PGP found?

A

Neuronal cells at capillary endothelial cells

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223
Q

What is the function of brain PGP?

A

Pump drugs out of brain into blood

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224
Q

Relationship between protein bound drug and free drug?

A

Reversible/equilibrium

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225
Q

What happens if two drugs are present in the blood?

A

One drug may displace the other drug from plasma protein. Fate of free drug depends on Vd

226
Q

What are the 2 types of plasma proteins? Which one binds the most?

A

Albumin**

Alpha 1 acid glycoprotein

227
Q

Albumin has a high affinity for ____?

A

Lipophilic

Anionic (weakly acidic)

228
Q

Aging decreases what plasma protein?

A

Albumin

229
Q

Malnutrition decreases what plasma protein?

A

Albumin

230
Q

Liver disease decreases what plasma protein?

A

Albumin

231
Q

Kidney disease decreases what plasma protein?

A

Albumin

232
Q

Hepatic inflammation increases what plasma protein?

A

Alpha 1 acid glycoprotein

233
Q

Alpha 1 acid glycoprotein has a high affinity for ___?

A

Cationic (weakly basic)

Very hydrophilic

234
Q

What may decreased albumin lead to?

A

Toxicity

235
Q

What may decreased alpha 1 acid glycoprotein lead to?

A

Ineffective therapy

236
Q

Aging increases what plasma protein?

A

Alpha 1 acid glycoprotein

237
Q

Trauma increases what plasma protein?

A

Alpha 1 acid glycoprotein?

238
Q

What increases alpha 1 glycoprotein?

A

Aging
Trauma
Hepatic inflammation

239
Q

What decreases albumin?

A

Aging
Malnutrition
Liver/kidney disease

240
Q

Volume of distribution represents…?

A

Represents the apparent volume that the drug distributes into

241
Q

Vd =

A

D (total amount of drug in body) / C (plasma concentration in blood)

242
Q

How can Vd be greater than body volume?

A

Extensive tissue binding

243
Q

Amount of total body water in 70 kg person?

A

42 L

244
Q

Amount of intracellular fluid in 70 kg person?

A

28 L

245
Q

Amount of extracellular fluid in 70 kg person?

A

14 L

246
Q

Amount of interstitial fluid in 70 kg person?

A

10 L

247
Q

Amount of plasma in 70 kg person?

A

4 L

248
Q

What are the two components of total body water?

A

Intracellular fluid

Extracellular fluid

249
Q

What are the two components of extracellular fluid?

A

Interstitial fluid

Plasma

250
Q

Drugs with small Vd are:

A

Highly protein bound

Large/heavy

251
Q

Where do small Vd drugs distribute?

A

Plasma

252
Q

Drugs with intermediate Vd are:

A

Light/small
Hydrophillic
Intermediate protein binding

253
Q

Where do intermediate Vd drugs distribute?

A

Extracellular fluid

254
Q

Drugs with large Vd are:

A

Light/small
Lipophilic
Minimal protein binding

255
Q

Where do large Vd drugs distribute?

A

All body compartments

Mainly intracellular fluid

256
Q

Volume requirement for large Vd?

A

Greater than 0.2 L/kg

257
Q

“Metabolism” =

A

Enzyme mediated alteration of a drug’s structure

258
Q

Why is metabolism important?

A

Protection from environmental toxins and synthesized endogenous molecules

259
Q

What is “exogenous”?

A

Originating from outside the body

260
Q

What is “endogenous”?

A

Originating from inside the body

261
Q

What is the primary site of drug metabolism?

A

Liver

262
Q

What are the 5 sites of drug metabolism?

A 
Liver
Intestine
Stomach
Kidney
Intestinal Bacteria
263
Q

What is the site of alcohol metabolism?

A

Stomach

264
Q

What are the 5 therapeutic consequences to drug metabolism?

A 
Increase water solubility to promote excretion
Inactivate drugs
Increase drug effectiveness
Activate pro drug
Increase drug toxicity
265
Q

What order kinetics do most drugs exhibit?

A

1st

266
Q

What is 1st order kinetics?

A

Rate of drug metabolism is directly proportional to the concentration of the free drug

267
Q

In 1st order kinetics, a constant ___ of drug metabolized per unit time?

A

Fraction

268
Q

In what situation is 1st order kinetics present?

A

Concentration of drug is less than total metabolic capacity of body

269
Q

What is 0 order kinetics?

A

Drug metabolism is constant over time

270
Q

IN what situation is 0 order kinetics present?

A

Plasma drug concentration is much higher than metabolic capacity of body

271
Q

In 0 order kinetics, a constant ___ of drug metabolized per unit time?

A

Amount

272
Q

What is an example of 0 order kinetics/metabolism?

A

Ethanol/alcohol metabolism

273
Q

What is 1st pass metabolism?

A

Oral drugs that undergo sig. metabolism period to entering systemic circulation

274
Q

What is the result of 1st pass metabolism?

A

Decreased amount of parent drug in systemic circulation

275
Q

What is the one area where 1st pass metabolism does not occur?

A

Kidney

276
Q

What is the enzyme for 1st pass metabolism in the liver?

A

CYP

277
Q

What is the enzyme for 1st pass metabolism in the intestine?

A

CYP

278
Q

What is the enzyme for 1st pass metabolism in the stomach?

A

Alcohol dehydrogenase

279
Q

After alcohol is metabolized, what does it become?

A

Acetaldehyde

280
Q

What is the enzyme for 1st pass metabolism in the intestinal bacteria?

A

Bacterial enzyme

281
Q

What is the extraction ratio (ER)?

A

Amount of metabolism that occurs on the first pass through the liver

282
Q

What does high ER mean?

A

Highly metabolized in liver (1st pass)

283
Q

What does low ER mean?

A

Small amount of 1st pass liver metabolism

284
Q

What is the bioavailability of high ER drugs?

A

Low 1-20%

285
Q

High ER drugs have PO doses ___ than IV doses?

A

Much higher

286
Q

Small changes to hepatic enzyme activity produce ____ changes in BA in high ER drugs?

A

Large

287
Q

What is the bioavailability of low ER drugs?

A

High 80%+

288
Q

Low ER drugs have PO doses ___ than IV doses?

A

Similar

289
Q

Small changes to hepatic enzyme activity produce ____ changes in BA in low ER drugs?

A

Little/none

290
Q

Which ER group is highly susceptible to drug drug interactions?

A

High

291
Q

What is the purpose of phase I metabolism? How?

A

Convert lipophilic drugs to more polar molecules to facilitate excretion BY introducing/unmasking polar functional groups

292
Q

What are the 2 polar functional groups?

A

OH

NH2

293
Q

What are the 3 mediators to phase I metabolism?

A

Cytochrome P450 enzyme = CYP
Esterases
Dehydrogenases

294
Q

The metabolites formed from phase I metabolism are ___ active than the parent?

A

Less OR more OR equally

295
Q

Where are phase I metabolizing enzymes found?

A

Smooth endoplasmic reticulum

296
Q

The majority of drug metabolism in the body is done by ___ enzyme?

A

Hepatic CYP

297
Q

What do CYPs do? How?

A

Oxidize drugs BY inserting 1 atom of O into the drug

298
Q

What is the byproduct of CYP oxidation?

A

Water

299
Q

How many CYP families are there?

A

12

300
Q

How many of the CYP families account for the majority of drug metabolism?

A

3/12

301
Q

What can decrease CYP activity?

A

Malnutrition

302
Q

What is the nomenclature for CYP enzymes?

A

CYP (family) (subfamily) (isozyme)

303
Q

What CYP enzyme metabolizes the largest fraction of currently marketed drugs?

A

CYP3A4

304
Q

Percent of drugs metabolized by this enzyme: CYP3A4?

A

50

305
Q

Percent of drugs metabolized by this enzyme: CYP2D6?

A

20

306
Q

Percent of drugs metabolized by this enzyme: CYP2C9?

A

10

307
Q

Percent of drugs metabolized by this enzyme: CYP2C19?

A

10

308
Q

Percent of drugs metabolized by this enzyme: 2E1?

A

5

309
Q

Percent of drugs metabolized by this enzyme: 1A2?

A

5

310
Q

What is the purpose of phase II metabolism? How?

A

Increase polarity of lipophilic drugs by conjugation reaction to make more water soluble

311
Q

What are the conjugates for phase II metabolism?

A

Glucuronic acid (sugar)
Sulfate
Acetate
AA (glycine)

312
Q

Phase II metabolites are ___ active than parent drug? Exception?

A

Less

Morphine metabolite

313
Q

Where are phase II enzymes found? Exception?

A

Cytosol

Glucuronidation in smooth ER

314
Q

What does UGT stand for?

A

UGT

315
Q

What does GST stand for?

A

Glytathione S transferase

316
Q

What does SULT stand for?

A

Sulfotransferase

317
Q

What does NATs stand for?

A

N acetyltransferase

318
Q

What does TMPT stand for?

A

Thiopurine methyltransferase

319
Q

What phase II metabolism enzyme metabolizes the most drugs?

A

UGT

320
Q

Where is UGT found?

A

Smooth ER

321
Q

What does UGT do? Purpose?

A

Catalyze the transfer of glucuronic acid to drug

Makes more polar and more easily excreted

322
Q

What phase II enzyme has the most human types?

A

GSTs

323
Q

How many drugs does UGTs metabolize?

A

30%

324
Q

How many drugs does GSTs metabolize?

A

25%

325
Q

How many drugs does SULTs metabolize?

A

20%

326
Q

How many drugs does NATs metabolize?

A

15%

327
Q

How many drugs does TMPT metabolize?

A

1%

328
Q

Where is GST enzyme found?

A

Cytosol

Microsome

329
Q

What does GST do?

A

Catalyze transfer of glutathione to drug

330
Q

What is glutathione?

A

Intracellular anti oxidant

331
Q

If you transfer glutathione onto a reactive drug, what happens?

A

Becomes less toxic

332
Q

What is SULTs found?

A

Cytosol

333
Q

What do SULTs do? Why?

A

Catalyze transfer of sulphate group to hydroxyl group

BECAUSE more polar and more easily excreted

334
Q

How many human types of NATs are there?

A

2

335
Q

Where is NATs found?

A

Cytosol

336
Q

What do NATs do? Why?

A

Catalyze transfer of acetyl group from acetyl CoA to a drug

BECAUSE more water soluble

337
Q

What phase II enzyme is subject to genetic polymorphisms?

A

NATs and TMPTs

338
Q

Where are TMPTs found?

A

Cytosol

339
Q

What does TMPTs do?

A

Catalyze transfer of methyl group from 5 adensylmethionine to drug

340
Q

Can a drug undergo multiple pathways of metabolism at the same?

A

YES! Some drugs can directly enter phase II metabolism.

341
Q

What are the 4 factors that affect drug metabolism?

A

Age
Drug interactions
Disease state
Genetic polymorphisms

342
Q

What drug metabolism factors change with age?

A

Expression

Activity

343
Q

What is different in babies regarding drug metabolism?

A

No CYP activity until 1 yr

344
Q

At what age do babies have the same drug metabolism as adults?

A

2

345
Q

What is enzyme induction?

A

Process where a cell synthesizes an enzyme in response to a drug or other chemical

346
Q

What is the result of enzyme induction of CYPs?

A

Increased drug metabolism

347
Q

What can increased drug metabolism lead to?

A

Decreased plasma concentrations

Decreased OR increased drug activity

348
Q

What can cause enzyme induction in liver?

A

Smoking

349
Q

What disease states can decrease CYP activity?

A

Liver disease
Kidney disease
Inflammatory disease
Infection

350
Q

What is a SNP?

A

Single nucleotide polymorphism

351
Q

What does CYP2C9 do?

A

Metabolizes anticoagulant drug warfarin

352
Q

What does CYP2D6 do?

A

Metabolizes codine to morphine

353
Q

What does UGT1A1 do?

A

Inactivate/eliminate anti cancer drugs

354
Q

What does NAT2 do?

A

Acetylates isoniazid (treat TB), caffeine, cancer causing chemicals

355
Q

What does a SNP to CYP2C9 do? Result?

A

Decrease enzyme activity

Need less warfarin

356
Q

What does a SNP to CYP2D6 do? Result?

A
  1. Ultra rapid metabolizer UM
  2. Extensive metabolizer EM = normal
  3. Intermediate metabolizer IM
  4. Poor metabolizer PM
357
Q

What does a SNP to UGT1A1 do? Result?

A

Decrease activity

Increased risk of diarrhea and bone marrow suppression

358
Q

What does a SNP to NAT2 do? Result?

A
  1. Rapid acetylators

2. Slow acetylators - more susceptible to toxicity

359
Q

What is drug excretion?

A

Removal of parent drug and metabolites from body

360
Q

What are the 4 places drug excretion occurs?

A

Kidney
Bile
Breast milk
Lung

361
Q

Healthy kidneys can limit ? of drug effects?

A

Duration and intensity

362
Q

What does the nephron regulate?

A 
Water 
Electrolytes
Drug excretion
Blood volume
Blood pressure
pH
363
Q

What blood vessel brings blood to the nephron?

A

Afferent renal arteriole

364
Q

What is the basic pathway of the nephron?

A 
Renal artery
Glomerulus
Prox tubule
Loop of Henle
Dist tubule
Collecting duct
365
Q

Glomerular filtration rate =

A

120 ml/min/1.73m2 = 20% plasma flow

366
Q

What is the major determinant of drug passage through glomerulus?

A

Size

367
Q

If the drug remains in the blood after the glomerulus, it has a chance to re-enter the filtrate at the ___?

A

Proximal tubule

368
Q

Where are the transport proteins at the proximal tubule of the nephron located?

A

Basolateral (blood) side

369
Q

How does tubular secretion work? (nephron)

A

2 sets of transport proteins (weak acids and weak bases)

370
Q

Rate of tubular secretion? (nephron)

A

Rapid/high capacity

371
Q

Why are drugs reabsorbed in the nephron?

A

Filtrate concentration is higher than plasma concentration

372
Q

What drugs are able to be reabsorbed in the nephron?

A

Lipophilic

Uncharged

373
Q

What is the glomerular filtration rate in babies?

A

40 ml/min/1.73m2

374
Q

What are the characteristics of drugs that are excreted in bile?

A

Large/heavy >300 Da
Polar AND lipophilic (amiphipathic)
Glucuronidated (UGT)

375
Q

What transporters are used in biliary excretion?

A

P glycoprotein

MRP2

376
Q

What does P glycoprotein transport?

A

Amiphipathic drugs from liver to bile

377
Q

What does MRP2 transport?

A

Glucuronidated drugs from liver to bile

378
Q

What is enterohepatic recycling?

A

Process where drugs in the intestine are absorbed to the liver where they undergo phase II metabolism, released back into the intestine where intestinal bacteria cleave off the conjugate and the ‘parent’ drug is reabsorbed again.

379
Q

What are the 4 components of the hepato-biliary system?

A

Portal vein
Hepatocyte
Hepatic duct
Bile canniculus

380
Q

What is the bile canniculus?

A

Thin tube that collects bile and drugs that are excreted by the liver

381
Q

What is the hepatic duct?

A

Tube that takes stuff from the liver to the gall bladder

382
Q

What type of drug excretion is not heavily reliable on drug metabolism?

A

Pulmonary

383
Q

What are the 3 factors that effect pulmonary excretion?

A

CO
Respiration rate
Drug blood solubility (inverse)

384
Q

What percent of women take 1+ drugs in first week post partum?

A

90%

385
Q

How big is the concern for secondary drug exposure to babies through breast milk?

A

Small

386
Q

What type of drugs are excreted through breast milk?

A

Light/small
Low protein binding
Lipophilic

387
Q

What is the transporter that transports drugs into breast milk?

A

BCRP = breast cancer resistant protein

388
Q

What is the pH in breast milk vs. plasma?

A

Breast milk 6.5

Plasma 7.4

389
Q

What are the 3 minor routes of excretion?

A

Hair
Saliva
Sweat

390
Q

What is the rate of hair growth?

A

1 cm/month

391
Q

What are the 4 most important parameters for determining drug disposition?

A

Clearance
Elimination half time
Vd
BA

392
Q

What is clearance?

A

Bodies efficiency in irreversible drug elimination

393
Q

Clearance =

A

Volume blood cleared PER unit time (mL/min OR L/hr)

394
Q

Dosing rate =

A

Plasma concentration x clearance

395
Q

Why is knowing elimination half time important?

A

Time to get to SS

How long it takes drug levels to decline after administration stops

396
Q

Elimination half time =

A

Clearance

397
Q

How is drug concentration measured?

A

Plasma drug concentration (free + bound)

398
Q

Drug duration is considered ? on a plasma time curve?

A

Time over minimum effective concentration MEC

399
Q

What is it called then the rate of absorption = rate of elimination on plasma time curve?

A

Cmax

400
Q

Rate of drug elimination after an IV bolus normally follows ___ order kinetics?

A

1st

401
Q

Steady state range for PO drugs is ___ than IV bolus drugs?

A

Smaller

402
Q

If the therapeutic range is small, when is plasma concentration tested?

A

Trough

403
Q

What are 3 ways to reduce plasma drug concentration fluctuations?

A

Continuous IV infusion
Depot preparations
Change dosing interval

404
Q

When the same dose of a drug is administered repeatedly, it takes ___ half lives to reach steady state.

A

5

405
Q

Loading dose =

A

Target plasma drug concentration at SS * Vd

406
Q

How many half lives does it take to eliminate 97% of drug?

A

5

407
Q

After 5 half lives, how much drug has been eliminated from the body?

A

97%

408
Q

After 9 half lives, how much drug has been eliminated from the body?

A

100%

409
Q

What is significant about allergens and drug elimination?

A

Will still be irritant even when concentration very low.

410
Q

Pharmacodynamics =

A

Study of what the drug does to the body

411
Q

What type of curves are used to evaluate pharmacodynamics?

A

Dose response

412
Q

What are the characteristics of dose response curves?

A

Monotonic

Semi logarithmic

413
Q

How many phases of dose response curves are there?

A

3

414
Q

What is phase 1 of the dose response curve?

A

Doses are too low to elicit clinically sig. response

415
Q

What is phase 2 of dose response curve?

A

Response is graded and linear

416
Q

Phase is phase 3 of dose response curve?

A

Larger dose does not lead to greater response; may cause toxicity

417
Q

What is “efficacy”?

A

How effective a drug is at a given dose

418
Q

How is maximal efficacy determined?

A

Maximal height on a dose response curve

419
Q

What is “potency”?

A

Amount of drug required to elicit a response

420
Q

How is potency determined?

A

Dose required to produce ED50 (want low)

421
Q

How can you compare potency?

A

Drugs must produce same therapeutic effect

422
Q

What is the majority of drug targets?

A

Receptors

423
Q

What are the 4 drug targets?

A

Receptors
Ion channels
Enzymes
Transport proteins

424
Q

What is an example of a drug that does not act on a cellular target?

A

Antacids that neutralize stomach acid

425
Q

What is the main function of receptors?

A

Bind to drug

Translate extracellular signals into biological responses

426
Q

How many receptors can a selective drug bind to?

A

1

427
Q

How can selective drugs still cause side effects?

A

Receptors may be located around the body even though you only want to target 1 specific area

428
Q

What are the 4 types of receptors?

A

Ligand gated ion channels
G protein coupled receptors
Enzyme linked receptors
Intracellular receptors

429
Q

What type of receptors do neurotransmitters bind to?

A

Ligand gated ion channels

430
Q

What type of receptor is a GABA receptor?

A

Ligand gated ion channel

431
Q

When GABA binds to a GABA receptor, what moves into the cell?

A

Chlorine

432
Q

What does the activation of the GABA receptor cause?

A

Sedation and muscle relaxaiton

433
Q

What is the response and duration of ligand gated ion channels?

A

Very rapid

Milliseconds

434
Q

How many drugs mediate their effects on G protein coupled receptors?

A

50%

435
Q

What are the 3 components of a G protein coupled receptor?

A

7 transmembrane protein receptor
G protein with 3 subunits
Effector molecule/enzyme

436
Q

Bind of a ligand to the G protein coupled receptor causes ______?

A

Activation of G protein which dissociates from receptor and activates effector

437
Q

How long does the activation of a G protein coupled receptor last?

A

Seconds to minutes

438
Q

Norepinephrine, serotonin and histamine all bind to what type of receptor?

A

G protein coupled receptor

439
Q

Where is the enzyme catalytic site on an enzyme linked receptor?

A

Inside cell

440
Q

How fast is the response to an enzyme linked receptor?

A

Seconds

441
Q

What type of receptor does insulin bind to?

A

Enzyme linked

442
Q

What does insulin binding cause?

A

Enzyme mediated phosphorylation and activation of intracellular effector = increased translocation of glucose to cell membrane

443
Q

What are transcription factors AKA?

A

Intracellular receptors

444
Q

Binding of a ligand to an intracellular receptor causes… ?

A

Translocation of complex to nucleus and binding to DNA

445
Q

What happens when the ligand-receptor complex of intracellular receptors binds to the DNA?

A

Transcription of mRNA stimulated

Protein synthesis hours/days later

446
Q

What type of ligands bind to intracellular receptors?

A

Lipophilic

447
Q

What receptor do the steroid hormones (testosterone and estrogen) bind to?

A

Intracellular receptor

448
Q

What ar the two drug receptor interaction theories?

A

Single occupancy

Modified occupancy

449
Q

What is the single occupancy theory? (2)

A

Intensity of drug response is proportional to number of receptors occupied
Maximal response when all receptors occupied

450
Q

What is the modified occupancy theory? (3)

A

Intensity of drug response is proportional to number of receptors occupied
Two drugs occupying receptor can have different affinities
Two drugs occupying receptor can have different intrinsic activity

451
Q

What is affinity?

A

Attraction that a drug has for receptor

452
Q

Affinity is proportional to …

A

Potency

453
Q

Intrinsic activity is proportional to …

A

Efficacy

454
Q

What is intrinsic activity?

A

Ability of drug to activate receptor

455
Q

After a drug binds to the receptor, it can either ____ OR ____?

A

Activate receptor

Prevent other ligands from binding

456
Q

What are the 3 types of molecules that bind to receptors?

A

Agonist
Antagonist
Partial agonist

457
Q

What is an agonist?

A

Molecule that binds to receptor and activates it - mimics endogenous ligands

458
Q

What type of binding molecule is dopamine?

A

Agonist

459
Q

What occurs with low dose dopamine? What receptor does it bind to?

A

Renal artery vasodilation = Increased urine output

Dopamine receptor

460
Q

What occurs with moderate dose dopamine? What receptor does it bind to?

A

Increased CO

Beta 1 adrenergic receptor

461
Q

What occurs with high dose dopamine? What receptor does it bind to?

A

Renal artery vasoconstriction = decreased urine output

Alpha adrenergic receptor

462
Q

What is an antagonist?

A

Molecule that binds to receptor and does NOT activate it.

463
Q

What condition are antagonist molecules useful?

A

Overdoses

464
Q

What type of binding molecule are beta blockers, antihistamines, gastric acid reducers, and opioid receptor blockers?

A

Antagonists

465
Q

What do beta blockers do?

A

Block binding of epinephrine to beta 1 receptor in heart = slow HR

466
Q

What do antihistamines do?

A

Block binding of histamine to H1 histamine receptor in nasal mucosa = decrease allergy symptoms

467
Q

What do gastric acid reducers do?

A

Block binding of histamine to H2 histamine receptors in gut = decrease gastric acid secretion

468
Q

What do opioid receptor blockers do?

A

Block binding of opioids to opiate receptors = treat overdose

469
Q

What are the 3 types of antagonists?

A

Competitive
Irreversible
Allosteric

470
Q

What are competitive antagonists?

A

Binding occurs at same site as agonist; reversible based on affinity and then concentration

471
Q

How does a dose response curve change with the presence of a competitive antagonist?

A

Shift right (decrease potency/affinity)

472
Q

What are irreversible antagonists? How long do effects last?

A

Binding occurs at same site as agonist; irreversible
Until body replaces receptor
**Not common!

473
Q

How does a dose response curve change with the presence of a irreversible antagonist?

A

Shift down (decrease efficacy)

474
Q

What is an allosteric antagonist?

A

Binding occurs at different site than agonist - changes conformation of receptor so agonist can’t bind

475
Q

How does a dose response curve change with the presence of an allosteric antagonist?

A

Shift down (decrease efficacy)

476
Q

What is a partial agonist?

A

Molecules that bind to receptor but have minimal ability to activate it (decrease intrinsic activity)

477
Q

What is tolerance?

A

Response to agonist can decrease with prolonged exposure

478
Q

What are the 3 types of tolerance?

A

Desensitization
Metabolic tolerance
Tachphylaxis

479
Q

What is desensitization?

A

Continuous exposure to agonist causes receptor desensitization –> receptor internalization and destruction = decreased cell surface receptor expression = decreased drug effects

480
Q

What is metabolic tolerance?

A

Continuous exposure to drug causes induction of drug metabolizing enzymes = decrease plasma concentrator of drug

481
Q

What is tachphylaxis? How to prevent it?

A

Rapid decrease in response to drug

Have drug free time between administrations

482
Q

How is dose response tested in phase I trials?

A

Animal studies

483
Q

How is dose response tested in phase 2 trials?

A

Info over range of doses is determined

484
Q

To determine interpatient variability in response to medications, we first ____?

A

Set an endpoint

485
Q

What is ED50? When is it used?

A

Dose required to produce a response in 50% of population

Used as initial dose for therapy

486
Q

Drugs with narrow therapeutic range should have their dose ____.

A

Titrated

487
Q

How long is chronic animal testing?

A

6 mth - 2 yr

488
Q

How is drug toxicity tested?

A

Acute and chronic testing on animals - determine doses that produce toxicity and death in multiple species

489
Q

What is TD50?

A

Dose where 50% of animals experience toxicity

490
Q

What is LD50?

A

Dose where 50% of animals die

491
Q

What is the therapeutic index a measure of?

A

Drug safety (high = safe). High = large space between ED50 and TD50

492
Q

How to measure therapeutic index?

A

TD50 LD50
——– OR ———–
ED50 ED50

493
Q

How many factors affect intermittent variation in response?

A

7

494
Q

How does body weight and compensation affect inter-patient variation in response?

A

CHange Vd

Clinicians adjust drugs by body surface area

495
Q

What is the normal body surface area of adults?

A

1.73m2

496
Q

How does genetics affect inter-patient variation in response?

A

SNP

Genotype differences

497
Q

How does gender affect inter-patient variation in response? (3 examples)

A

Can be more effective in one gender vs. other
Alcohol metabolism slower in females
Opioids more effective in women
Heart dysrhythmia drugs in women cause long QT interval

498
Q

How does race affect inter-patient variation in response?

A

Hard to define

Rousuvastatin (lower cholesterol) concentrations 2-3x higher in asian vs. Caucasian

499
Q

How does kidney disease affect inter-patient variation in response?

A

Drug excretion decreased = increased half life = stronger effect = increased BA

500
Q

How does liver disease affect inter-patient variation in response?

A

Decreased metabolism = increase half life

501
Q

How can the environment affect inter-patient variation in response? (4 examples)

A

Cigarette smoke induces enzymes = less effective drugs
Alcohol increase drug toxicity
Exercise improve insulin
Pesticides induce CYPs = decrease drug response

502
Q

How many people are admitted to Cdn hospitals every year from adverse drug reactions?

A

185000

7.5% admissions

503
Q

What are side effects?
When do they occur?
Example?

A

Secondary to main therapeutic effect of drug; expected
Occur at normal doses - expected
Antihistamines cause drowsiness, dry mouth, urinary retention

504
Q

What is an allergic reaction? How does it work?

A

Mediated by immune system
Needs prior exposure
Allergen binds to IgE antibodies which cause release of chemicals/mediators

505
Q

What are the common areas of allergic reactions symptoms on body? Uncommon?

A

LOOK: Stomach, bum, under arms, top of legs

DON’T LOOK: head, hands, feet

506
Q

The intensity of allergic reactions are ___ of dosage size.

A

Independent

507
Q

What is the most common drug class to cause allergy?

A

Penicillin

508
Q

Sulfonamides and NSAID drugs can cause what type of ADR?

A

Allergy

509
Q

What is an idiosyncratic reaction?

Where do they occur?

A

Rare and unpredictable
Mainly due to polymorphism
Occur in metabolizing enzymes and transport proteins.

510
Q

What CYP enzymes have idiosyncratic reactions? Occurrence?

A

CYP2C9 15%

CYP2D6 10%

511
Q

What are the 3 other enzymes (+2 CYP) that have idiosyncratic reactions? Occurrence?

A

TMPT 10%
OATP1B1 15% - myopathy
G6PDH - hemolysis

512
Q

What drug caused carcinogenic effects?

A

Diethylstillbestrol DES

513
Q

How are drugs tested for potential mutagens?

A

Ames test on bacteria

514
Q

What are teratogenic effects?

A

Ability of drug to produce birth defects or infertility

515
Q

_% of all birth defects are caused by drugs?

A

Less than 1

516
Q

What part of the developing fetus is most sensitive to drugs?

A

CNS

517
Q

How are pregnancy risks categorized?

A

A-E

518
Q

What is a A risk pregnancy?

A

OK!

519
Q

What is a B risk pregnancy?

A

No shown harmed effect in human but ?animal harm

520
Q

What is a C risk pregnancy?

A

Animal studies = harmed fetus

521
Q

What is a D risk pregnancy?

A

Human studies = harmed fetus BUT benefits outweigh risk

522
Q

What is an E risk pregnancy?

A

Human studies = harmed fetus; risks outweigh benefits

523
Q

The most common and important organ specific toxicity is observed in the ___ and ___?

A

Liver and heart

524
Q

Patients taking hepatoxic drugs should be educated to look for signs of liver toxicity including: _____?

A 
Jaundice
Dark urine
Light coloured stool
Nausea
Vomiting
525
Q

What blood tests should you do to look for liver toxicity?

A

AST aspartate aminotransferase - want low

ALT alanine aminotransferase - want low

526
Q

QT interval prolongation is a major risk for the development of…

A

Torsades de points

527
Q

What is torsades de points?

A

Life threatening ventricular arrhythmia

528
Q

What are opiates used for?

A

Analgesia

529
Q

What is the consequence of rapid withdrawal of opiates?

A 
Anorexia
Irritability 
Nausea/vomiting
Weakness
Muscle spasm
530
Q

What are benzodiazepines used for?

A

Anxiety

531
Q

What is the consequence of rapid withdrawal of benzodiazepines?

A 
Anxiety 
Insomnia
Sweating 
Treamours
Panic
Delirium
Paranoia
Convulsions
532
Q

What are beta blockers used for?

A

Decrease HR

533
Q

What is the consequence of rapid withdrawal of beta blockers?

A 
Rebound 
Hypertension
Chest pain
Heart attack 
Arrhythmia
534
Q

What is the most common cause of adverse drug reactions?

A

Medication errors

535
Q

What is it called when a medication error is caused by a health care professional?

A

Iatrogenic error

536
Q

How many medication errors are due to drug name confusion?

A

15%

537
Q

The abbreviation IU should be written as ___

A

Units

538
Q

The abbreviation q.d. should be written as ___

A

Every day

539
Q

The abbreviation q.o.d. should be written as ___

A

Every other day

540
Q

The number 1.0 should be written as __

A

1

541
Q

The number .5 should be written as ___

A

0.5

542
Q

The abbreviation MgSO4 should be written as ___

A

Magnesium sulfate

543
Q

The abbreviation MS / MSO4 should be written as___

A

Morphine sulfate

544
Q

The risk of drug interactions increases ____ with the number of medications the patient takes.

A

Linearly

545
Q

The most common type of drug drug interactions affect ___

A

Pharmokinetics

546
Q

What are the 3 types of drug drug interaction effect?

A

Increased effects
Decreased effects
Generation of new effect

547
Q

Ampicillin and sulbactam = example of what type of drug drug interaction?

A

Increase therapeutic effect

548
Q

Aspirin and warfarin = example of what type of drug drug interaction?

A

Increased adverse effect

549
Q

Clodiogrel and omepraxole = example of what type of drug drug interaction?

A

Decreased therapeutic effect

550
Q

Morphine and naloxone = example of what type of drug drug interaction?

A

Decreased adverse effect

551
Q

Disulfiram and alcohol = example of what type of drug drug interaction?

A

Generation of new effect

552
Q

What are the 4 types of drug interactions?

A

Direct physical interaction
Pharmacokinetic interaction
Pharmodynamic interaction
Combined toxicity

553
Q

What is the most common physical drug interaction?

A

2 IVs mixed together that causes precipitate to form

554
Q

Why would it be beneficial to inject epinephrine with local anaesthetic?

A

Epinephrine cause vasoconstriction causing anaesthetic to stay at injection site.

555
Q

If the patient vomits 20-30 mins after administration of drug, it is likely that the drug absorption is ___.

A

Incomplete

556
Q

How long after exposure to an inducer does CYP induction begin?

A

2-10 days

557
Q

How long after stopped exposure to an inducer foes CYP induction stop?

A

7-10 days

558
Q

Many antibiotics and anti fungals, and grapefruit juice inhibit CYP___?

A

CYP3A4

559
Q

Both NSAIDS and beta blockers and decrease ___?

A

Renal blood flow

560
Q

What is combined toxicity?

A

2+ drugs exhibit toxicity to the same organ

561
Q

Patients on MAO inhibits must avoid foods with …

A

Tyramine = old cheese, yeast, red wine, cured meat

562
Q

What happens if patients on MAO inhibitors ingest tyramine?

A

Continue to release norepinephrine = hypertensive crisis

Western (14 decks)

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