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Foundations of Clinical Medicine > Foundations: Pharmacology > Flashcards

Foundations: Pharmacology Flashcards

1
Q

How would you describe a selective drug?

A

One that only interacted with its intended molecular target over its therapeutic range

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2
Q

Define selective toxicity.

A

Describes a drug aimed at killing something (parasites, tumor) without harming the host

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3
Q

How long does it take to design a new drug?

A

7-10 years

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4
Q

How much does it cost to design a new drug?

A

> $250 million

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5
Q

When writing a prescription, should the generic or brand name of a drug be used?

A

The generic name (allows pharmacist to choose most economical form of drug)

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6
Q

When writing scientific publications, should the generic or brand name of a drug be used?

A

The generic name

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7
Q

What is the generic name for Coumadin?

A

Warfarin

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8
Q

What is the generic name for Lamisil?

A

Terbinafine

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9
Q

What is the generic name for Lasix?

A

Furosemide

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10
Q

What is the generic name for Glucophage?

A

Metformin

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11
Q

If the drug concentration and % biological effect are plotted on a linear scale, what relationship is expressed?

A

A hyperbolic dose relationship

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12
Q

If the drug concentration and % biological effect are plotted on a semilog scale, what relationship is expressed?

A

A sigmoidal dose relationship

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13
Q

What is the effective concentration/dose?

A

That which elicits the biological response in 50% of individuals (ED50)

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14
Q

What is the toxic dose?

A

That which elicits toxicity in 50% of individuals (TD50)

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15
Q

What is the lethal dose, and how is it determined?

A

That which causes death in 50% of individuals

Determined statistically

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16
Q

What is the therapeutic index, and how is it calculated?

A

The range where a drug will be effective but not toxic

TI = TD50/ED50

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17
Q

Does a large therapeutic index mean a safer or more dangerous drug?

A

A larger TI means a safer drug

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18
Q

What is an example of a drug with a small TI?

A

Warfarin… higher doses produce anticoagulation leading to hemorrhage

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19
Q

What is an example of a drug with a large TI?

A

Penicillin

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20
Q

Define potency.

A

The amount of drug needed to produce an effect that is 50% of the maximum (EC50)

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21
Q

Define efficacy.

A

The maximum response that can be achieved by a drug (ECmax).
It’s the inherent ability of the drug to couple receptor activation to production of a biological effect.

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22
Q

Which is more important, potency or efficacy?

A

Efficacy

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23
Q

How does an agonist activate receptors?

A

By mimicking natural ligands

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24
Q

How does a partial agonist differ from an agonist?

A

The partial agonist binds to the receptor to elicit a lesser response (decreased efficacy)

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25
Q

Define antagonism.

A

When a drug binds to a receptor but elicits no response. The drug has full affinity but no efficacy.

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26
Q

How does competitive antagonism change the dose-response relationship?

A

The agonist must be present in higher concentrations to produce the same efficacy. The potency of the agonist shifts.

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27
Q

Is competitive antagonism reversible?

A

Yes. Binding the agonist and the antagonist is reversible.

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28
Q

How does irreversible antagonism change the dose-response relationship?

A

The antagonist binds irreversibly to the same receptor as the agonist, and no amount of agonist can overcome the antagonist’s effects. The efficacy of the agonist decreases.

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29
Q

What is an example of a competitive/reversible antagonist?

A

Tolazoline (anti-depressant)

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30
Q

What is an example of an irreversible antagonist?

A

Dibenamine (anti-depressant)

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31
Q

How does a non-competitive/allosteric antagonist change the dose-response relationship?

A

The antagonist binds to the receptor near the agonist’s binding site to cause a conformational change in the receptor. The efficacy of the agonist is decreased.

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32
Q

Define physiologic antagonism.

A

When two molecules have opposite effects that are mediated through different mechanisms.

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33
Q

What is an example of physiologic antagonism?

A

The antagonism of histamine-induced vasodilation by epinephrine-induced vasoconstriction

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34
Q

Define chemical antagonism.

A

The antagonist removes the drug being antagonized to inhibit its ability to reach the target.

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35
Q

What is an example of chemical antagonism?

A

Dimercaprol is a chelator (binds up the compound to render it ineffective) of lead and other toxic methods

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36
Q

Define pharmacodynamics.

A

What the drug does to the body.

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37
Q

What is the fundamental principle of pharmacodynamics?

A

Drugs are not able to generate responses de novo. They either block or stimulate a response that is already present.

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38
Q

What are the immediate targets for most drugs (molecular level effects)?

A

Receptors
Ion channels
Enzymes

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39
Q

What type of receptor is the most prevalent target for drugs?

A

Rhodopsin-like G-protein coupled receptors (GPCR)

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40
Q

Describe the structure of the GPCR.

A

Made of 7 transmembrane helices that are linked to G-proteins (3 subunits)

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41
Q

What happens to the GPCR after being active for awhile?

A

Desensitization - it will shut down even if the ligand is still around

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42
Q

What are some examples of GPCR?

A 
Taste receptors
Olfactory receptors
Chemokine receptors
Regulators of mood and behavior
Control of automatic  functions (BP, HR, digestion)
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43
Q

How does the GPCR interact with the G-proteins?

A

When the GPCR is occupied, it undergoes a conformational change and interacts with the G-protein

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44
Q

How does the G-protein initiate a signal to be sent?

A

The alpha subunit dissociates and activates adenylyl cyclase

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45
Q

What type of receptor is the second most prevalent target for drugs?

A

Nuclear receptors

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46
Q

Where are nuclear receptors located?

A

Inside the cell

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47
Q

What process does nuclear receptors regulate?

A

Gene expression

48
Q

Describe Type 1 Nuclear Receptor Steroid signaling.

A

The steroid receptor is bound to a Hsp90 protein in the cytoplasm. When a steroid crosses the cell membrane to bind to the receptor, it releases the Hsp90 and moves into the nucleus to bind to the gene regulatory sequence to activate transcription.

49
Q

Describe Type 2 Nuclear Receptor Non-steroid signaling using the thyroid hormone receptor.

A

The thyroid hormone receptor is in the nucleus sitting on the DNA. When hormone binds, it activates the receptor to activate transcription.

50
Q

What is the role of the Tyrosine Kinase receptors?

A

Regulate growth and cell differentiation

51
Q

What are some tyrosine kinase receptor agonists?

A

Insulin
EGF
PDGF
FGF

52
Q

What are some examples of receptor operated channels (ligand gated ion channels)?

A

Nicotinic receptor

GABA receptor

53
Q

Describe the nicotinic acetylcholine receptor.

A

When acetylcholine binds to the nicotinic receptor, the receptor undergoes a conformational change to allow Na+ to influx and initiate an AP in the neuromuscular junction

54
Q

Describe the GABA receptor.

A

When GABA binds to the receptor, the receptor undergoes a conformational change to allow Cl- ions into the cell to decrease Vm and make it harder to generate an AP
**major molecular target for drugs in the brain

55
Q

How can drugs affect voltage operated/gated channels?

A

Drugs can change voltage dependence or cause the channel to be blocked

56
Q

What is an example of a voltage operated/gated channel?

A

The voltage gated Na+ channel in neurons and in cardiac and skeletal muscle

57
Q

What is an example of an antiporter?

A

The Na+/Ca++ exchange

58
Q

What is an example of an energy dependent channel?

A

The Na+/K+ ATPase pump

59
Q

What drug affects the Na+/K+ ATPase pump?

A

Digoxin

60
Q

What differentiates the action of competitive and noncompetitive enzyme inhibitors?

A

Competitive inhibitors interfere with the active site

Noncompetitive inhibitors binds to a different site to change the shape of the enzyme

61
Q

How does Metformin work on a molecular level?

A

Binds to Complex 1 in mitochondria

62
Q

How does Metformin work on a cellular level?

A

Acts on AMP Kinase, which is involved in neoglucogenesis

63
Q

How does Metformin work on a tissue level?

A

Decreases the amount of sugar made by the liver

64
Q

How does Metformin work on a systemic level?

A

Lowers plasma glucose
Prevents cardio complications associated with diabetes
People tend to lose weight

65
Q

Define pharmacokinetics.

A

What the body does to the drug.

66
Q

What is the most common route of drug administration?

A

Per oral

67
Q

What is the major site of entry into systemic circulation?

A

The duodenum

68
Q

What are some advantages of oral drug administration?

A

Convenient
Cheap
Variety of forms

69
Q

What are some disadvantages of oral drug administration?

A

Can be inefficient
May be only partially absorbed
First-pass effect

70
Q

What are some advantages of sublingual drug administration?

A

Avoids first-pass
Rapid access to circulation
Drug stability due to neutral pH in mouth

71
Q

What are some disadvantages of sublingual drug administration?

A

Inconvenient

Can only accommodate small doses

72
Q

What is an example of a sublingual drug?

A

Nitroglycerin, used to relieve acute attack of angina

73
Q

What are some advantages of rectal drug administration?

A

Half of rectal drainage bypasses first-pass
Avoids GI enzyme breakdown
Good for those unable to take drugs orally

74
Q

What are some disadvantages of rectal drug administration?

A

Erratic and often incomplete absorption

Social stigma

75
Q

What form of drug administration provides the most dose control?

A

Parenteral administration

76
Q

What are some advantages to intravenous drug administration?

A

Rapid

Max control over dose of drug

77
Q

What are some disadvantages to intravenous drug administration?

A

Can’t remove it if the patient has a toxic reaction
Requires trained personnel
Expensive

78
Q

What is an advantage to intramuscular drug administration?

A

Drug can be delivered fast or slow

79
Q

What is a disadvantage to intramuscular drug administration?

A

Requires trained personnel

80
Q

What are some advantages to subcutaneous drug administration?

A

Patient can give drug to self

Slow but complete absorption

81
Q

What are some disadvantages to subcutaneous drug administration?

A

Can hurt
Tissue damage can result at site of administration
Can only inject a limited dose

82
Q

What is an advantage to inhaled drugs?

A

Convenient/effective route, especially if the lungs are the target

83
Q

What is an example of an inhaled drug?

A

Glucocorticosteroids, to treat asthma

84
Q

What are some advantages to intranasal drug administration?

A

Great for drugs that would be eliminated by first-pass if taken orally
Can deliver potent drugs to elicit systemic effects
Easy to administer
Good compliance

85
Q

What are some examples of topically administered drugs?

A

Sunscreen
Eye drops
Antiseptic

86
Q

What are some advantages to transdermal drug administration?

A

Systemic effects
Controlled release
Prompt termination

87
Q

What is the main disadvantage of transdermal drug administration?

A

Only very small drug molecules can penetrate the skin

88
Q

What are the 4 basic pharmacokinetic processes?

A

Absorption
Distribution
Metabolism
Elimination

89
Q

How does size affect absorption?

A

The smaller the molecule, the better it is absorbed (doesn’t matter if molecule is uncharged)

90
Q

How does the pH of the environment affect absorption?

A

The pH determines the fraction of drug available in non-ionized form, which is the only form that can get across the membrane

91
Q

In what environment is an acidic drug best absorbed?

A

An acidic pH (lower #)

92
Q

In what environment is a basic drug best absorbed?

A

A basic pH (higher #)

93
Q

What is the Partition Coefficient?

A

The solubility of a drug molecule in a lipid solvent in comparison to its solubility in water

94
Q

Will a drug with a greater partition coefficient have a greater or weaker solubility in lipid?

A

Greater lipid solubility

Will move rapidly across the membrane

95
Q

What is an example of a drug with a particularly high partition coefficient?

A

Thiopental (580) used to quickly induce anesthesia

96
Q

What is an example of a drug with a particularly low partition coefficient?

A

Phenobarbitol (3) used for treatment of chronic epilepsy

97
Q

If you wanted rapid gastric emptying, would you recommend the drug to be taken with or without food?

A

Without food, with only a glass of water

98
Q

If you wanted delayed gastric emptying, would you recommend a drug be taken with or without food?

A

With food

99
Q

Is plasma protein (albumin) binding of a drug beneficial or detrimental to distribution?

A

Can be either

Drug will not be accessible for metabolism or for function

100
Q

What 3 factors affect the distribution of a drug?

A

Size of the drug
Plasma protein binding
Permeability of the cell membrane

101
Q

What organ is a major site for metabolism?

A

The liver

102
Q

Describe first order elimination kinetics.

A

Drug has not saturated the body’s capacity to eliminate it.

Loss of drug from body is proportional to the drug concentration in the plasma.

103
Q

After how many half lives is a drug gone?

A

5

104
Q

Describe zero order elimination kinetics.

A

The drug has saturated the body’s ability to eliminate it with a very low concentration.
The loss of drug from body is constant over time. The concentration of the drug does not matter.

105
Q

What is an example of a drug that displays zero order elimination kinetics?

A

Ethanol

106
Q

What elimination process do normal doses of Aspirin exhibit?

A

Between first and zero order.

Once first order is saturated, elimination switches to zero order.

107
Q

How do Phase 1 reactions affect drug metabolism?

A

Oxidation and hydrolysis provide functional groups to increase the polarity of a drug

108
Q

What enzyme usually induces oxidation, and where is it found?

A

Cytochrome P-450 (CYP) in microsomes of the liver

109
Q

How do Phase 2 reactions affect drug metabolism?

A

Attach large chemical groups to increase water solubility and excretion from body

110
Q

How is most drug excretion accomplished?

A

Renal excretion (urine)

111
Q

How can you measure renal function directly?

A

24 hour creatinine clearance

112
Q

Describe entero hepatic circulation.

A

A drug secreted in bile is hydrolyzed in the lower intestine to release the original drug. The drug is reabsorbed into the blood stream with a prolonged half life.

113
Q

What type of drugs are mainly excreted via the lungs?

A

General anesthetics in gaseous or vapor form

114
Q

What other substance can be excreted via the lungs in minor amounts?

A

Ethanol (basis for the breathalyzer test)

115
Q

What are the 3 methods of drug excretion?

A

Renal (urine)
Liver (bile, feces)
Lungs (exhaled air)

Foundations of Clinical Medicine (5 decks)

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