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Pharmacology > Pharmacokinetics and Pharmacodynamics > Flashcards

Pharmacokinetics and Pharmacodynamics Flashcards

1
Q

3 ways of membrane crossing

A
  1. Channels and pores
  2. Transport system
  3. Direct penetration (lipid soluble only)
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2
Q

First pass effect

A

The initial metabolism in the liver of a drug absorbed from the GI tract before drug reaches systemic circulation through the bloodstream

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3
Q

Where does metabolism usually take place?

A

Liver

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4
Q

Therapeutic range

A

Between MEC and toxic

Larger range = safe

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5
Q

What factors affect absorption?

A 
Rate of dissolution
Surface area
Blood flow
Lipid solubility
Rate of administration
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6
Q

Enteric coated

A

Special coating on a drug that prevents absorption until drug reaches small intestine
Protects stomach or keeps drug from being destroyed by stomach acids

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7
Q

CYP450

A

Group of enzymes in GI tract and liver that metabolize drugs —> take fat soluble item (drug) and make it water soluble so it can be excreted

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8
Q

3 steps of renal excretion

A
  1. Glomerular filtration - filtration moves drugs from blood to urine
  2. Passive tubular reabsorption - lipid soluble drugs move back into blood while polar and ionized drugs remain in the urine
  3. Active tubular secretion - tubular pumps for organic acids and bases and moves drugs from blood to urine
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9
Q

Can ions be excreted?

A

Yes - they are not lipid soluble

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10
Q

T/F: drugs can only elicit or block normal physiologic responses

A

True

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11
Q

Intrinsic activity (efficacy)

A

Intensity of effect that the drug produces, ability of a drug to active the receptor after binding

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12
Q

Interpatient variability

A

The dose required to produce a therapeutic response can vary substantially among patients

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13
Q

ED50

A

Effective dose in 50% of population

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14
Q

LD50

A

Dose that is lethal in 50% of population

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15
Q

Drug

A

Any chemical that affects living systems

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16
Q

Is there any such thing as an ideal drug?

A

No

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17
Q

Clinical pharm

A

Study of drugs in humans

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18
Q

Therapeutics

A

Medical use of drugs to diagnose, treat and prevent

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19
Q

Ideal drug properties

A

Effectiveness, safety, selectively, reversible, predictability, ease of administration, freedom from drug interactions, low cost, chemical stability, possession of simple generic name

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20
Q

Pharmacokinetics

A

The process by which drugs are absorbed, distributed, metabolized and excreted

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21
Q

Pharmacodynamics

A

What the drug does to the body and how does it illicit a response

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22
Q

P-glycoprotein (P-gp)

A

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

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23
Q

Pka

A

Ph at which the drug is 50% ionized

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24
Q

Ion trapping

A

Occurs when a drug molecule changes from ionized to non ionized from as it moves from one body compartment to another 0 drug will accumulate on the side that favors the ionized state and cannot cross back over

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25
Q

Where will acidic drugs accumulate?

A

Alkaline side

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26
Q

Where will basic drugs accumulate?

A

Acidic side

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27
Q

Administration routes

A

enteral (GI), PO, PR (per rectum)

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28
Q

Parenteral route

A

IV, IM (not GI)

29
Q

Distribution

A

Movement of drug from blood into the interstitial spaces and cells to the site of action

30
Q

What is distribution determined by?

A

Blood flow to tissues, ability of drug to exit vascular system, ability of drugs to enter the cells

31
Q

Volume of distribution

A

Reflection of how much drug is left in vasculature

32
Q

What is a small Vd?

A

Drug is mostly held in vasculature

33
Q

What is large Vd?

A

Drug is widely distributed outside of vasculature

34
Q

What affects Vd?

A

CO, perfusion of tissues, type of capillary system, polarity of drug molecules, protein binding

35
Q

Metabolism (bio transformation)

A

How bio chemical reactions alter drugs in the body

*does not always inactivate the drug

36
Q

Consequences of metabolism

A

Accelerated renal excretion, drug inactivation to inactive metabolites, increased therapeutic action (metabolites are more effect), activation of prodrugs (inactive until metabolism), increased or decreased toxicity

37
Q

CYP450 inducers

A

Drugs that increase synthesis of enzymes —> increased enzyme concentration and increased drug metabolism —> decreased therapeutic response

38
Q

CYP450 inhibitors

A

Decrease synthesis of enzymes —> decreased drug metabolism —> increase drug effects/risk for toxicity (i.e. grape fruit juice)

39
Q

Most common excretion site

A

Renal system

40
Q

Other methods of excretion

A

Feces, sweat, saliva, breast milk, expired air

41
Q

Minimum effective concentration (MEC)

A

The plasma drug level below which therapeutic effects will not occur

42
Q

Toxic concentration

A

Level of drug that will result in serious side effects

43
Q

Half life

A

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

44
Q

Plateau

A
  • steady level achieved once repeated doses cause build up
  • amount of drug eliminated b/w doses equals amount administered
  • when a drug is administered repeatedly in the same dose, plateau will be reached in approx. 4 half lives
45
Q

Peak level

A

Highest concentration

46
Q

Trough level

A

Lowest concentration

47
Q

Zero order

A

Same amount of drug will be metabolized per hour no matter how much drug is present (i.e. alcohol)

48
Q

First order

A

% of drug metabolized is related to dose size

A larger dose = a larger amount metabolized

49
Q

Types of receptors

A
  1. Cell membrane embedded enzymes
  2. Ligand gated ion channels
  3. G protein coupled receptors
  4. Transcription factors (intracellular)
50
Q

Affinity (potency)

A

How much drug must be administered to elicit a desired effect
Strength of attract b/w drug and receptor

51
Q

Agonists

A

Mimic action of endogenous ligand and activate receptors

52
Q

Antagonists

A

Produce their effects by preventing receptor activation by endogenous regulatory molecules and drugs

53
Q

Competitive antagonists

A

Bind reversibility to receptors

54
Q

Noncompetitive antagonists

A

Drug that reduces the effect of an agonist but does not compete at the receptor site
-irreversible

55
Q

Partial agonist

A

Drugs that interact with a receptor to stimulate a response but to a lesser intensity

56
Q

Dose response curve

A

As dose increases, response becomes progressively larger

57
Q

Orthosteric sites

A

Same site as endogenous ligand

58
Q

Allosteric sites

A

Alternative site from endogenous ligand

59
Q

Upregulation with continues antagonist usage

A

Receptors will proliferate

60
Q

Downregulation w/ continuous agonist usage

A

Receptors decrease and drugs elicit less of a resposne

61
Q

Therapeutic Index (TI)

A

Measure of drug’s safety ratio (ED50/LD50)

Wider TI = safe

62
Q

Adverse drug effects

A

Any noxious, unintended, and undesired effect that occurs at normal drug doses —> can be annoying to life threatening

63
Q

Side effect

A

Nearly unavoidable effect that occurs with therapeutic doses

64
Q

Toxicity

A

Negative effects due to excessive drug doses

65
Q

Allergic reaction

A

Immune response

66
Q

Black boxed warning

A

Strongest safety warning a drug can carry and still remain on the market

67
Q

What are the highest fatal potential medication errors?

A

Wrong route, wrong drug, overdose

68
Q

T/F: nurses are required to report medication error

A

TRUE - to institution, to provider, national program exists (MER)

Pharmacology (6 decks)

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