Principles Of Pharmacology Flashcards

0
Q

Pharmacology

A

The study of drugs and their interactions with living systems

The study of the physical and chemical properties of drugs as well as their biochemical and physiologic effects

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1
Q

Drug

A

Any chemical that can affect the living process

All chemicals are considered drugs

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2
Q

Clinical Pharmacology

A

The study of drugs in humans

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3
Q

Therapeutics

A

The use of drugs to diagnose, prevent, or treat disease or to prevent pregnancy

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4
Q

Are there any ideal medications?

A

No, there is no such thing as a perfect drug

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5
Q

Properties of an ideal drug (3)

A

Effectiveness, Safety, Selectivity

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6
Q

Effectiveness

A

Elicits the response for which it is given

Most important property a drug can have!

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7
Q

Safety

A

Cannot produce harmful effects

There is no such thing as a safe drug

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8
Q

Selectivity

A

Elicits ONLY the response for which it is given

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9
Q

Additional Properties of an ideal drug… (7)

A
Reversible action
Predictability
Ease of Administration
Freedom from drug interactions
Low Cost 
Chemical stability
Possession of simple generic name
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10
Q

Therapeutic Objective

A

Provide maximum benefit with minimum harm

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11
Q

Factors that determine the intensity of a drug

A

Administration, Pharmacokinetics, Pharmacodynamics, Sources of Individual variation

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12
Q

Administration

A

Dosage size and route and timing of administration are important determinants of drug responses

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13
Q

Toxicity

A

Results of dosage is too high

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14
Q

Treatment failure

A

Results is dosage is too low

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15
Q

Pharmacokinetics

A

Pharmacokinetic processes determine how much of an administered dose gets to its sites of action

“Impact of the body on drugs”

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16
Q

Four Major Pharmacokinetic Processes

A
  1. Drug absorption
  2. Drug distribution
  3. Drug metabolism
  4. Drug excretion
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17
Q

Pharmacodynamics

A

Determine the nature and the intensity of the response

A patient’s “functional state” can impact pharmacodynamic processes

“impact of drugs on the body”

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18
Q

Six rights of administration

A
  1. Right drug
  2. Right patient
  3. Right dose
  4. Right route
  5. Right time
  6. Right documentation
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19
Q

Contraindication

A

A pre-existing condition that precludes use of a particular drug under all but the most desperate circumstances

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20
Q

Precaution

A

a preexisting condition that significantly increases the risk of adverse reaction to a particular drug, but not to the degree that it is life threatening

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21
Q

Three types of drug names

A
  1. Chemical Name
  2. Generic Name
  3. Trade Name
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22
Q

Chemical Name

A

Description of the drug using nomenclature of Chemistry

  • long and complex
  • inappropriate for everyday use

Example: N-acetyle-para-aminophenol

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23
Q

Generic Name

A

Name assigned by the United States Adopted Names Council

  • Each drug has only one generic name
  • Less complex than chemical names, but more complex than trade names

Example: Acetaminophen

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24
Q

Trade Name

A

Names under which a drug is marketed
-Easy to pronounce and remember

Example: Tylenol, Valorin, Q-pap, etc.

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25
Q

Three ways to cross a cell membrane

A
  1. Passage through channels or pores
  2. Passage with the aid of the transport system
  3. Direct penetration of the membrane itself
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26
Q

Passage through channels or pores

A

Very few drugs can cross membranes via channels or pores, they are extremely small and specific to certain organisms

Smallest compounds can pass through them

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27
Q

Passage through Transport Systems

A

All transport systems are selective

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28
Q

P-Glycoprotien

A

Transporter

Transmembrane protein that transports a wide variety of drugs out of cells

Present at many sites including the liver, kidney, placenta, intestine, and capillaries of the brain

Limiting access or reducing absorption

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29
Q

Direct Penetration of the membrane

A

For most drugs, movement throughout the body is dependent on the ability to directly penetrate the membrane because:

  1. most drugs are too large to pass through channels or pores
  2. most drugs lack transport systems to help them cross all of the membranes that separate them from their sites of action metabolism and excretion

In order to directly penetrate a membrane a drug MUST be lipid soluble (aka NOT polar molecules)

30
Q

Ions and polar molecules are unable to…

A

…cross cell membranes

31
Q

Quaternary Ammonium Compounds

A

Molecules that contain at least one atom of nitrogen and carry a positive charge at all times

Unable to cross membranes

32
Q

Absorption

A

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

Rate = how soon
Amount = how intense the affects will be
33
Q

Factors that affect absorption

A
  1. Rate of Dissolution (how fast it dissolves)
  2. Surface Area (larger the surface area, the faster the absorption)
    - drugs are usually absorbed through the small intestine rather than the stomach
  3. Blood Flow (absorbed more rapidly where blood flow is high)
  4. Lipid Solubility (Lipid soluble drugs are absorbed more rapidly)
  5. pH partitioning
34
Q

Routes of Administration

A

Enteral (via gastrointestinal tract) and parenteral (outside GI tract)

35
Q

Enteral

A

Tablets

36
Q

Parenteral

A

intravenous (IV), intramuscular (IM), subcutaneous (subQ)

37
Q

Distribution

A

The movement of drugs throughout the body

38
Q

Three major factors of distribution

A
  1. Blood flow to tissues
  2. The ability of a drug to exit the vascular systems
  3. The ability of a drug to enter cells (to a lesser extent)
39
Q

What two factors inhibit blood flow to the tissues?

A

abscesses and tumors

40
Q

Exiting the vascular system

A

drugs must exit the blood in order to affect the target, it is also important for metabolism and secretion

41
Q

Blood Brain Barrier (BBB)

A

Refers to the unique anatomy of capillaries in the CNS

There are tight junctions between the cells (to prevent drug passage) = only drugs that are lipid soluble or have a transport system can pass through

Also has P-glycoprotein (protective component)

42
Q

Plasma Albumin

A

Of all the drugs in which a protein can bind, plasma albumin is the most important, being the most abundant protein in plasma

Albumin always remains in the bloodstream

Binding between albumin is reversible

43
Q

Metabolism

A

Drug metabolism, also known as biotransformation, is defined as the enzymatic alteration of drug structure. Most drug metabolism takes place in the liver.

The most important consequence of drug metabolism is renal drug secretion

44
Q

P450 (aka hepatic microsomal enzyme system)

A

Most drug metabolism in the liver is performed by this

A group of 12 closely related enzyme families

45
Q

Prodrug

A

compound that is pharmacologically inactive as administered and then undergoes conversion to its active form within the body

46
Q

First-pass effect

A

refers to the rapid hepatic inactivation of certain oral drugs

Results in no therapeutic affect

47
Q

Excretion

A

Removal of drugs from the body

kidneys account for most of drug excetion

48
Q

Potential outcomes of metabolism

A
  • promote renal excretion
  • drug inactivation
  • increased effectiveness
  • activation of “pro” drugs
  • Increased/decreased toxicity
49
Q

Considerations in drug metabolism

A
  • age
  • drug metabolizing enzymes
  • first pass effect
  • nutritional status
  • competition between drugs
50
Q

Steps of Renal drug excretion

A
  1. Glomerular filtration (moves drugs from blood into tubular urine, proteins, like albumin, are too large to be filtered)
  2. Passive tubular absorption (drugs that are lipid soluble undergo passive reabsorption from the tubule back into the blood, drugs that are not lipid soluble remain in the urine)
  3. Active tubular secretion (specialized “pumps” for organic acids and bases to be moved from the blood into the urine)
51
Q

Minimum effective concentration (MEC)

A

the plasma drug level below which therapeutic effects will not occur

52
Q

Toxic Concentration

A

When plasma drug level is too high

53
Q

Therapeutic range

A

ideal range for drug

54
Q

Drug half-life

A

Time required for the amount of drug in the body to decrease by 50%

55
Q

How long does it take for a plateau to be reached?

A

Approximately four half lives

94% will be eliminated after 4 half lives of discontinuing to take it

56
Q

Highest level of drug concentration is…

A

peak concentration

57
Q

Lowest level of drug concentration is…

A

trough concentration

58
Q

Dose-response relationships

A

relationship between size of the dose and the potency

59
Q

Potency

A

drug that produces an effect at lower doses

60
Q

Maximal efficacy

A

biggest effect drug can produce

61
Q

Receptor

A

any functional macromolecule in a cell to which a drug binds to produce its effects

Drugs can be made selective or nonselective to specific receptors

Drugs mimic or block receptors

More selective = fewer side affects

62
Q

Single occupancy theory

A

the intensity of the response of the drug is proportional to the amount of receptors and a maximal response will occur when all receptors are occupied

63
Q

Modified Occupancy Theory

A

ascribes two qualities to drugs affinity and intrinsic activity are independent properties

64
Q

Affinity

A

refers to the strength of the attraction between the drug and its receptor

Drugs with high affinity are very potent

65
Q

Intrinsic Activity

A

Refers to the ability of a drug to activate a receptor upon binding

Drugs with high intrinsic activity cause intense receptor activation

reflected in maximal efficiency

66
Q

Agonists

A

Drugs that mimic the actions of endogenous regulatory molecules

High affinity and high intrinsic activity

67
Q

Antagonist

A

block the actions of endogenous regulatory molecules

affinity but no intrinsic activity

preventing the activation of receptors by agonists

68
Q

Partial agonists

A

mimic the actions of endogenous regulatory molecules, but they produce responses of intermediate intensity

moderate intrinsic activity

69
Q

Non-competitive antagonist

A

bind irreversibly to receptors

reduce maximal response

70
Q

Competitive Antagonists

A

bind reversibly to receptors

Most antagonists are competitive

71
Q

Desensitized/refractory/down-regulation

A

receptors of a cell are continually exposed to an agonist, and the cell becomes less responsive

72
Q

hypersensitive/supersensitive

A

constantly exposed to antagonists

73
Q

Therapeutic index

A

measure of drugs safety