Basic Principles of Pharmacology Flashcards

1
Q

pharmacokinetics

A

How drugs move through the body (moves)

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2
Q

pharmacodynamics

A

the effects of drugs and the mechanism of their action (effects)

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3
Q

4 parts of taking medicine

A

Absorption, distribution, metabolism and excretion

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4
Q

AUC/MIC, T>MIC, Cmax/MIC

A

?

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5
Q

P-glycoprotein inhibitors

A

?

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6
Q

Therapeutic drug monitoring: Drugs that exhibit narrow therapeutic indices

A

?

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7
Q

Therapeutic drug monitoring: Timing of appropriate serum drug levels

A

?

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8
Q

Absorption-

A

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

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9
Q

3 Factors that affect absorption

A
  1. Route of administration can effect
  2. Bioavailability
  3. Concentration
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10
Q

Factors that affect absorption: Route of administration can effect 4 things

A

Compliance, bioavailability, onset of action and duration of action

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11
Q

Factors that affect absorption: Bioavailability

A

The percentage of administered drug that enters the blood

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12
Q

Factors that affect absorption: Concentration

A

Higher concentration of drug at site of action may increase absorption

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13
Q

Rectal administration may be useful in

A

presence of nausea, vomiting, pediatric

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14
Q

Topical administration includes skin,

A

lungs, eyes, ears, nasal

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15
Q

Factors that affect absorption: Bioavailability: If bioavailability is low,

A

higher doses may be required

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16
Q

Factors that affect absorption: Concentration: Rapid absorption may lead to

A

higher concentrations/ peaks

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17
Q

Distribution-

A

the process of drugs moving throughout the body after absorption

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18
Q

Factors that affect distribution: 4 things

A
  • Size of the organ
  • Blood flow (well perfused tissue tend to have higher tissue concentrations)
  • Solubility
  • Binding (highly plasma protein bound drugs stay in the vascular compartment)
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19
Q

Factors that affect distribution: explain the effect of binding

A

highly plasma protein bound drugs stay in the vascular compartment

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20
Q

Factors that affect distribution: explain the effect of Blood flow

A

well perfused tissue tend to have higher tissue concentrations

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21
Q

Metabolism occurs primarily

A

in the liver

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22
Q

Metabolism can ___ the action of the drug

A

activate or terminate the action of the drug

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23
Q

Metabolism some drugs are metabolized and converted to an ____ metabolite before excretion

A

inactive

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24
Q

Some drugs are metabolized and converted to an inactive metabolite before excretion. 2 example:

A

Sympathomimetics, phenothiazines

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25
Q

Prodrugs are

A

inactive until they are metabolized in the body

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26
Q

Prodrugs: 2 example

A

Levodopa, minoxidil

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27
Q

Unlike prodrugs, Other drugs are

A

active when administered and have active metabolites

28
Q

Unlike prodrugs, Other drugs are active when administered and have active metabolites. 2 examples:

A

Morphine, benzodiazepines

29
Q

Unlike prodrugs, Other drugs are active when administered and have active metabolites. There are also drugs that

A

do not get metabolized and remain active until excretion

30
Q

There are drugs that do not get metabolized and remain active until excretion, for example

A

Lithium

31
Q

Excretion (for MOST drugs) occurs primarily in the

A

kidneys

32
Q

Volatile anesthetic gases are excreted primarily by the

A

lungs (unlike most other drugs that are done by the kidneys)

33
Q

Drugs that are not metabolized-> excretion is the mode of elimination

A

?

34
Q

Metabolism is often needed to ensure

A

elimination of drugs and to facilitate excretion

35
Q

Metabolism: Phase I reactions

A

Converts parent drug to a more polar (water-soluble) form

36
Q

Metabolism: Phase 2 reactions

A

Increase water solubility by conjugation of the drug molecule with a polar moiety

37
Q

Glucuronate, acetate, or sulfate

A

?

38
Q

CYP isoenzymes

A

?

39
Q

P-glycoprotein

A

An ATP-dependent transport molecule that expels drug molecules from the cytoplasm into the extracellular space.

40
Q

Drug-receptor binding is r____, s___, and g____

A

reversible, selective and graded

41
Q

Drug-receptor binding: The higher the number of drug bound receptors,

A

the greater the pharmacological response

42
Q

Drugs that are bound to the receptors may be: (3 things)

A

Agonists, Partial agonists, Antagonists

43
Q

Agonists

A

a drug capable of activating the receptor upon binding to it

44
Q

Partial agonists

A

Produces less than the full effect

45
Q

In the presence of a full agonist, the partial agonist

A

acts as an inhibitor

46
Q

A pharmacological antagonist interacts with

A

the same receptor as the drug it is meant to inhibit

47
Q

Dose-response curve

A

depicts the relationship between the drug dose and magnitude of effect

48
Q

Dose-response curve: Doses below the curve

A

do not produce a pharmacological response

49
Q

Dose-response curve: Doses above the curve

A

do not produce much additional pharmacological response

50
Q

Dose-response curve: Therapeutic index (TI) is

A

the ratio between the lethal dose (LD) and the effective dose (ED). The larger the ratio, the safer the drug.

51
Q

Therapeutic index (TI) is the ratio between the lethal dose (LD) and the effective dose (ED). The larger the ratio,

A

the safer the drug. (larger means you have more room to mistake, therefore safer)

52
Q

Loading doses may help achieve therapeutic drug levels…

A

quicker

53
Q

Generally takes ___ half-lives of the drug to achieve steady state

A

4 ½ - 5

54
Q

Steady state

A

when the amount of drug going in equals the amount of drug going out to keep the blood levels “steady”

55
Q

When should serum drug levels for TDM should be taken

A

after steady state is achieved

56
Q

Many drugs that have a narrow therapeutic index may require TDM. 3 examples:

A

Digoxin, aminoglycosides, lithium

57
Q

Drug - Drug Interactions: Enzyme induction: Produces

A

an increased rate and extent of metabolism of drugs

58
Q

Drug - Drug Interactions: Enzyme induction: Produces an increased rate and extent of metabolism of drugs. often associated with

A

cytochrome P450 enzymes

59
Q

Drug - Drug Interactions: Enzyme induction: Drugs that increase enzyme activity are known as

A

inducers

60
Q

Drug - Drug Interactions: Enzyme Inhibition: The inhibitors of drug metabolism include, but are not limited to,

A

grapefruit juice*, amiodarone, and protease inhibitors

61
Q

Drug - Drug Interactions: Enzyme induction: Since inducers increase metabolism,

A

less drug becomes available → decreased drug effect

62
Q

Drug - Drug Interactions: P-glycoprotein inhibitors: Drugs that inhibit P-glycoprotein

A

increase bioavailability of the drug and can result in toxic levels of drugs when given at normal dosages.

63
Q

Drug - Drug Interactions: P-glycoprotein inhibitors: P-glycoprotein inhibitors include

A

Verapamil, grapefruit juice*

64
Q

Drug - Drug Interactions: P-glycoprotein inhibitors: Drugs that can become toxic when given with a P-glycoprotein inhibitor

A

Digoxin, cyclosporine

65
Q

Drug - Drug Interactions: P-glycoprotein inhibitors: Furanocoumarin

A

is the component in grapefruit juice that is responsible for these effects