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Pharmacology > module 1 pharmacodynamics and pharmacokinetics > Flashcards

module 1 pharmacodynamics and pharmacokinetics Flashcards

1
Q

lipophilicity

A

ability to dissolve in fats, oils, lipids, and non-polar solvents
- drug affinity for lipid environment

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2
Q

therapeutic window

A

efficacy without unacceptable toxicity

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3
Q

ED50

A

dose where 50% of people have therapeutic effect

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4
Q

TD50

A

dose where 50% have toxic effect

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5
Q

LD50

A

dose where 50% die (lethal)

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6
Q

High therapeutic index

A

wide window

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7
Q

low therapeutic index

A

small window

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8
Q

Receptors natural state

A

non-active

- become active when bound with drug or natural agonist

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9
Q

inverse agonist

A

binds to receptors who have a natural active state and inactive it.

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10
Q

full agonist

A

elicits maximal response

stabilizes DR*(active)

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11
Q

partial or mixed agonist-antagonist

A

activates receptor but not with maximal efficacy

stabilized DR and DR*

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12
Q

Antagonists

A

inhibition of agonist activity

- stabilization of DR; prevention of DR*

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13
Q

competitive antagonist

A

reversible binding

competes for same active site

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14
Q

noncompetitive antagonist

A

irreversible binding to active site

or allosteric site

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15
Q

allosteric site

A

site other than active site

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16
Q

non-receptor antagonist

A

chemical: binds to agonist and inactivates it
physiologic: mediates opposite response of agonist

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17
Q

competitive antagonist and drug response

A

Will eventually get to full drug response but it takes longer due to fighting for binding sites.

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18
Q

noncompetitive antagonist and drug response

A

drug response will not reach 100% d/t antagonist binding to allosteric site
- non-reversible

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19
Q

pharmacokinetics

A

what body does to the drug

20
Q

pharmacokinetics 4 topics

A

absorption
distribution
metabolism
excretion

21
Q

absorption

A

from compartment to circulation

22
Q

metabolism

A

free drug-> metabolism -> metabolites (active and inactive) -> excretion

23
Q

free drug can bind to

A

receptors
tissue reservoirs
proteins

24
Q

physiochemical properties for drug transfer

A

size and shape
solubility at absorption site
degree of ionization
relative lipid solubility (ionized vs nonionized)

25
Q

passive diffusion

A

small

hydrophobic/ lipophillic

26
Q

facilitated diffusion

A

transporter

no ATP required

27
Q

active transport

A

transporter

ATP required

28
Q

endocytosis

A

engulfment

29
Q

nonionized molecules

A

lipid soluble, easily penetrate

30
Q

ionized molecules

A

hydrophilic, difficulty penetrating

31
Q

pKa

A

pH at which 50% of drug is ionized

32
Q

pH trapping

A

determined by pKa and pH gradient across membrane

  • weak acid in stomach becomes non-ionized and will cross to plasma
    • in plasma becomes ionized and will not cross back.
33
Q

CNS penetration

A

small and hydrophobic
active transport
facilitated transport
intrathecal

34
Q

pharmacodynamics

A

what drug does to receoptor/body

35
Q

efficacy

A

ability of drug-receptor complex to produce intended response

36
Q

potency

A

amount of drug needed to produce effect

- strength

37
Q

potency and efficacy relationship

A

drug that requires less to produce the same response (potency) has higher efficacy.
- drugs can have same efficacy but different potency

38
Q

water-soluble: hydro..

A

hydrophilic

39
Q

polar, usually ionized: hydro…

A

hydrophilic

40
Q

lipophilic: hydro..

A

hydrophobic

41
Q

water insoluble: hydro..

A

hydrophobic

42
Q

renal excretion: hydro..

A

hydrophilic

43
Q

requires transport mechanism to cross membranes: hydro…

A

hydrophilic

44
Q

passively diffuses across membranes: hydro..

A

hydrophobic

45
Q

Forms H+ bonds: hydro..

A

hydrophilic

46
Q

non-polar, unusually not ionized: hydro..

A

hydrophobic

Pharmacology (78 decks)

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