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304 > General Principles of Pharmacology > Flashcards

General Principles of Pharmacology Flashcards

1
Q

pharmacology

A

branch of medicine that deals with interaction of drugs with the systems and processes of living animals

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2
Q

drugs

A

broadly defined as any chemical agent that affects living processes

  • affects mind/body
  • used to diagnose, treat, prevent
  • used recreationally for effects on CNS
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3
Q

pharmacology derived from Greek word..

A

pharmakon; a magic charm for tearing disease

-later came to mean a remedy or drug

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4
Q

different drug names

A
  • brand
  • generic
  • pre market manufacturer code
  • chemical
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5
Q

pharmacokinetics

A
  • what the body does to the drug

- process of absorption, distribution, metabolism/biotransformation, and excretion

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6
Q

pharmacodynamics

A
  • what the drug does to the body

- processes of receptor binding, signal transduction, biological effect

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7
Q

Most drugs are supposed to be …. because ….

A

beneficial; they are prescribed based on known mechanism of action

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8
Q

side effects

A

secondary effect due to known mechanism; expected

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9
Q

adverse effects

A

due to interactions of some UNKNOWN mechanisms; unexpected

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10
Q

iatrogenic effect

A

and adverse effect or complication caused by a physician resulting from medical treatment or device

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11
Q

enteral

A

through the digestive tracts

-oral, sublingual, rectal

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12
Q

parenteral

A

a route other than the digestive tract

-intravenous, intramuscular, subcutaneous, intraatrerial, intrathecal, intraperitoneal

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13
Q

intravenous

A

100% bioavailability

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14
Q

drug absorption

A

the passage of drug from site of administration into general circulation

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15
Q

better absorbed

A

non-ionized, small molecules, lipid soluble drugs

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16
Q

two organs where cell layer is interrupted (fenestrations/pores)

A
  • capillary beds in kidney glomerulus (tubular space in nephron, gaps between endothelial cells)
  • liver (interstitial space in organ)
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17
Q

sites that act as a barrier created by uninterrupted cell layers

A

GI tract epithelium, capillary beds

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18
Q

pKa

A

the pH at which half o the drug is ionized

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19
Q

acid/acidic

A
  • proton donor
  • more protons
  • protonated form is charged and better absorbed (non ionized)
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20
Q

base/alkaline

A
  • proton acceptors
  • less protons
  • protonated form is charged and not well absorbed (ionized)
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21
Q

ion trapping

A

-an acidic drug would accumulate on more basic side of membrane and a basic to the more acidic side

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22
Q

To increase excretion of acidic drugs such as phenobarbital…

A

intravenous sodium bicarbonate is given

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23
Q

To increase excretion of basic drugs such as amphetamine..

A

ammonium chloride or ascorbic acid may be given

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24
Q

bioavailability

A

the fraction of an ORALLY given drug that reaches the circulation (fraction between 0 and 1)

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25
Q

bioavailability =

A

quantity of drug reaching systemic circulation / quantity of drug administered

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26
Q

Metabolizing enzymes in…

A

intestinal wall and/or liver

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27
Q

Everything taken orally must go through…

A

the liver

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28
Q

If taking drugs sublingually, they go straight to..

A

the heart and bypass metabolism through the liver

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29
Q

cheese-wine rxn

A
  • tyramine in cheese and wine, metabolized by monoamine oxidases
  • when patient takes MAO inhibitor, tyramine will be absorbed, reach circulation and nerve terminals and release NE
  • NE stimulates adrenergic receptors causing tachycardia and high BP
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30
Q

Most drugs exists as …… or …..

A

free drug, bound drug (bound to plasma proteins)

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31
Q

factors affecting drug distribution

A
  • ionization
  • capillary permeability
  • blood flow
  • plasma protein binding
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32
Q

drugs in the capillaries of liver and spleen

A

regardless or whether they are poorly lipid soluble, charged, or polar, drugs leave the capillaries

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33
Q

In the liver and spleen, the capillaries are very…

A

leaky

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34
Q

capillaries in the brain

A

-have tight junction, only lipophilic drugs diffuse across unless actively transported

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35
Q

Tissues that receive more …. receive more drug.

A

blood flow

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36
Q

Drugs reach the majority of tissues via..

A

the general circulation

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37
Q

Rate at which drugs distribute from bloodstream to tissues depends on..

A

relative blood flow to various tissues

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38
Q

total body water

A

2/3 in ICF, 1/3 in ECF (1/3 is intravascular/plasma)

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39
Q

adult blood volume

A

~5L

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40
Q

Vd

A

volume of distribution

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41
Q

volume of distribution

A

a theoretical volume in which the total amount of administered drug should be uniformly distributed throughout the body and to account for its plasma or blood conc.

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42
Q

Vd =

A

dose administered / plasma concentration

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43
Q

We normally take … of a drug to calculate Vd.

A

plasma samples

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44
Q

high Vd

A

indicates that most of the drug is in the extravascular compartment

45
Q

low Vd

A

indicates that most of the drug is in the vascular compartment (plasma)

46
Q

drug metabolism

A

chemical modification of drugs by enzymes, to make them more polar and therefore readily excretable by the kidneys

47
Q

drug metabolizing enzymes present in…

A
  • liver
  • gastrointestinal wall
  • lungs
  • kidneys
  • skin
  • blood
  • brain
48
Q

phase I of biotransformation

A

making drug more polar thru oxidation, reduction, and hydrolytic reactions

49
Q

phase II of biotransformation

A

conjugation to polar groups resulting in most drugs inactivation and rapid excretion
-a chemical group such as glucuronic acid, sulphate, glutathione, amino acids, or acetate is added to the drug

50
Q

phase I main enzymes

A

microsomal Cytochrome P450 MonoOxygenase family

51
Q

Cytochrome P450 MonoOxygenase

A
  • located in the ER
  • require O2
  • metabolize widest range of drugs
  • rxns inactivate a drug
52
Q

90% of drug oxidation by cytochrome enzymes can be attributed to..

A

isoforms

  • CYP1A2
  • CYP2C9
  • CYP2C19
  • CYP2D6
  • CYP2E1
  • CYP3A4
53
Q

CYP3A4

A

primary enzyme for metabolism of about HALF of ALL drugs

-inhibited or induced by many drugs, which can cause drug-drug interactions

54
Q

A drug can interact (stimulate or inhibit) with..

A

drugs, foods, herbals/medicines

55
Q

Induction or inhibition of phase I enzymes (especially CYT P450) can cause..

A

drug interactions when two or more drugs that are metabolized by the same enzyme are given

56
Q

inducers

A
  • cause expression of more enzymes and faster elimination of drugs
  • lower than expected drug levels can cause treatment failure
57
Q

examples of inducers

A

rifampin, barbiturates, st johns wort

58
Q

inhibitors

A
  • inhibit activity of enzymes and reduce elimination of substrate drugs
  • higher than expected drug levels can cause drug toxicity
59
Q

examples of inhibitors

A
  • grapefruit juice
  • cimetidine
  • erythromycin
  • intraconazole
60
Q

one of the most commonly prescribed antibiotics

A

erythromycin

61
Q

Most common P450 polymorphism in Caucasians is the lack of…expression

A

CYP2D6

62
Q

CYP2D6

A

metabolizes codeine to morphine for the analgesic effect; for people lacking expression of CYP2D6, codeine is almost ineffective

63
Q

Enzymes for Phase II rxns are mostly located in..

A

the cell cytosol

64
Q

50% of Americans and 60% of Europeans have reduced expression of..

A

acetylating enzymes N-acetyl transferase which cause slow metabolism of drugs such as isoniazid (antiTB drug), procainamide (anti-arhythmic drug) and caffeine

65
Q

factors affecting drug metabolism

A
  • lipid solubility
  • 1st order or zero order rate of metabolism
  • blood flow to liver
  • maturation of metabolizing enzymes
  • diseases of liver and kidney
66
Q

prodrugs

A

inactive precursor with favourable pharmacokinetics, which metabolize into the active drug in the body
-useful for when certain drugs do not reach their site of action because of pharmacokinetic obstacles

67
Q

omeprazole and lansoprazole

A

prodrugs used to reduce stomach acid secretion

-proton pump inhibitors

68
Q

levo-dopa

A

a prodrug that is converted into the active compound dopamine used for Parkinson’s disease

69
Q

P-glycoprotein

A
  • an EFFLUX pump that uses ATP to remove compounds for INSIDE to OUTSIDE and protects CNS
  • has a broad substrate specificity, located at many site on luminal surfaces (cancer tissue)
  • can be induced and inhibited
70
Q

P-glycoprotein expression is induced by..

A

St. John’s Wort, rifampin

71
Q

P-glycoprotein is inhibited by …

A

verapamil, quinidine, macrolide, antibiotics, antifungals

72
Q

clinical significance or P-glycoprotein

A
  • plays a role in drug resistance to cancer chemotherapeutic agents
  • pumps out anticancer drugs
73
Q

phenothiazine and cyclosporin A

A

calcium channel clockers that inhibit P-glycoprotein and may be useful to reverse resistance

74
Q

enterohepatic recirculation

A

a phenomenon that prolongs the duration of action (half-life) of a drug and allows recycling of bile salts

75
Q

95% of bile salts are…

A

reabsorbed and used in cholesterol systhesis

76
Q

cycle of estrogen during enter-hepatic recirculation

A
  • conjugation of estrogen to estrogen glucuronide
  • excreted as bile
  • deconjugation in the intestines by bacterial enzymes
  • reabsorption via circulation
77
Q

affecting factors of excretion

A
  • lipid solubility
  • first order or zero order
  • blood flow to kidney/GFR
  • maturation of metabolizing enzymes
  • dises of liver + kidney
  • competition for transport systems in renal tubules
  • pH of blood and urine
  • plasma protein binding
78
Q

clearance

A

volume of blood from which a drug is irreversibly removed

79
Q

Use for knowing clearance values?

A

useful to calculate maintenance dose (rate of administration) of a drug

80
Q

rate of administration/ maintenance dose should be equal to..

A

rate of elimination

81
Q

filtration

A
  • passive

- only free drug is filtered at glomerulus (not protein-bound drugs)

82
Q

drugs that are strong acids and strong bases are secreted through… and is an … process

A

proximal tubule, active

83
Q

net removal =

A

filtered + secreted - reabsorbed

84
Q

most drugs are eliminated according to ..

A

a first order rate process

85
Q

first-order rate process

A

a CONSTANT FRACTION of a drug is eliminated per unit of time

86
Q

metabolizing enzymes located in..

A

liver

87
Q

how much of a drugs metabolized?

A

1/5th

88
Q

zero-order rate process

A

a CONSTANT AMOUNT of a drug is eliminated per unit of time

89
Q

How does the zero-order process determine the constant amount?

A

it is the maximum rate of elimination when the pathway for ELIMINATION IS SATURATED

90
Q

half-life

A

time required for the blood or plasma conc. of a drug to be reduced by 50%

91
Q

If a FIXED dose is given repeatedly at fixed intervals, it takes… half-lives for that drug to achieve steady state conc. in the plasma (for about 97% of a drug to be effectively eliminated from the body.

A

5

92
Q

finding half-life applies to drugs that are eliminated by …. order rate

A

first

93
Q

Time to steady state or elimination is independent of..

A

dosage

94
Q

Increased effect from a drug interaction can cause..

A

toxicity

95
Q

Decreased effect in a drug interaction can cause…

A

treatment failure

96
Q

Drug use is greatesr among…

A

frail elderly, hospitalized patients, and nursing home residents

97
Q

drug-drug interaction

A

between two drugs metabolized by the same CYP isoform

98
Q

drug-food interaction example

A

drugs metabolized by CYP enzymes and grapefruit juice

99
Q

drug-herb interaction example

A

drugs metabolized by CYP enzymes and St. Johns Wort

100
Q

pharmacodynamic interaction

A

two drugs affecting the same system (effect on the organism)

101
Q

pharmacokinetic interaction

A

one drug changes the absorption, distribution, metabolism, excretion of another.

102
Q

absorption DDI example

A

antacids reduce absorption of tetracycline

-calcium supplements reduce absorption of thyroxine

103
Q

Distribution DDI example

A

-competition for plasma protein binding by non-steroidal anti-inflammatory drugs (NSAIDs) and warfarin (anticoagulant)

104
Q

excretion DDI example

A

probenecid reduces excretion of penicillin by competition for the kidney tubule transport system

105
Q

most common reason for DDI?

A

one drug affecting the metabolism of another drug

106
Q

liver and kidney affects?

A

metabolism and excretion and plasma levels of many drugs

107
Q

When should the possibility of DDIs be considered?

A

when a patient is taking two or more drugs

108
Q

When taking a single drug metabolized by the cytochrome P450 enzyme, what should be considered?

A

interactions with food items or herbal medecines

109
Q

In cases of drug toxicity or treatment failure, what should be considered?

A

genetic variation of metabolizing enzymes

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