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Pharmacology Exam 1 > Lecture 2: Pharmacokinetics > Flashcards

Lecture 2: Pharmacokinetics Flashcards

1
Q

ADME

A

absorption
distribution
metabolism
excretion/elimination

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2
Q

actions of the body on a drug

A

pharmacokinetics

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3
Q

ionization

A

many drugs are weak acids

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4
Q

partition coefficient

A

amount in oil vs. amount in water

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5
Q

what is the pH in the stomach

A

1-2

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6
Q

will weak acid drugs be ionized in the stomach?

A

probably not (favors absorption)

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7
Q

when pH = pKa..

A

50% is ionized

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8
Q

if a weak acid drug is in a solution 3 pH units below its pKa, almost 100% will be

A

non-ionized (protonated)

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9
Q

pH trapping

A

drug in stomach, favors absorption
* reaching plasma, gets stuck in plasma because cannot cross back through membrane

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10
Q

local anesthetics block _ that carry AP down the axon

A

voltage-gated Na+ channels

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11
Q

a drug molecule must diffuse from _, through _, into _

A

extracellular fluid, membrnae, cytosol

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12
Q

most capillaries are

A

leaky

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13
Q

blood-brain barrier has

A

tight junctions

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14
Q

_ generally enhances ability of drugs to enter brain

A

lipid solubility

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15
Q

metabolism/biotransformation

A

inactivation of drug by enzymes

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16
Q

primary metabolism organ

A

liver

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17
Q

excretion

A

removal of metabolites or the unchanged active drug from the body
* kidneys (urine)
* liver (bile salts)
* lungs (exhaled)

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18
Q

three “families” of cytochrome P450s:

A

CYP1, CYP2, CYP3

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19
Q

subfamilies of cytochrome P450

A

denoted by letter; speicifc enzymes by number

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20
Q

CYP3A4

A

most common metabolic enzyme involved in drug interactions

21
Q

phase I metabolism

A

oxidation, reduction, hydrolysis

22
Q

phase II metabolism

A

conjugation with glucuronic acid

23
Q

zero order drug metabolic reactions

A

drug concentration does not affect metabolic rate

24
Q

first order kinetics

A

drug concentration affects rate
* higher conc. = higher rate
* exponential drop in drug concentration

25
Q

factors affecting drug metabolism

A
  • enzyme induction
  • inhibtion/competition
  • genetic polymorphisms
26
Q

acetaminophen dose

A

3 g/day (used to be 4)

27
Q

when does acetaminophen toxicity occur

A

7-10 g/day

28
Q

signs of acetaminophen toxicity

A
  • initial flu-like symptoms
  • liver failure: jaundice, decreased blood clotting, death possible
29
Q

antidote for acetaminophen toxicity

A

N-acetylcysteine

30
Q

prodrugs

A

administered in an active form
* require metabolic activiation by the body

31
Q

codeine is a _ of morphine

A

prodrug

32
Q

free drug molecules are filtered at the

A

glomerulus

33
Q

lipid-solible are reabsorbed in _ by passive diffusion

A

renal tubules

34
Q

ionized (charged) or hydrophilic drugs can’t be reabsorbed are therefore excreted in

A

urine

35
Q

alkalization of urine (increasing pH) will facilitate excretion of

A

weak acids

36
Q

intrinsic toxicity

A
  • reproducible - all patients at risk
  • dose-dependent (drug overdose)
  • sensitivity can vary from patient to patient
  • result of actions at target receptor or effects at other receptors
37
Q

idiosyncratic

A
  • not widely reproducible
  • low incidence
  • occurrence is the result of interaction with patient attributes
38
Q

enteral

A

administration into the systemic circulation via the alimentary canal

39
Q

parenteral

A

adminstration into the systemic circulation via routes other than the alimentary canal

40
Q

topical

A

aministration by direct application onto the skin or associated membranes

40
Q

topical

A

aministration by direct application onto the skin or associated membranes

41
Q

clearance

A

a way to collectively quantify all of the processes that make active drug disappear from the body
* expressed at the amount of plasma per unit of time that would be completely cleared of the drug

42
Q

volume of distribution (Vd)

A

theoretical volume in which a drug is dissolved in the body
* Vd = D/C0 (dose given/concentration in plasma)

43
Q

half-life (t1/2)

A

time is takes for drug concentration to decrease by half
* 50% of drug is lost in one half-life
* 75% lost in 2
* 87.5% lost in 3

44
Q

bioavailability

A

fractio of original dose that reaches systemic circulation

45
Q

obstacles of oral administration

A
  • variations in stomach emptying time
  • acidity/alkalinity
  • interactions with food
  • absorption across gut epithelium
  • liver - first pass effect
46
Q

inhibition of P450 enzymes

A

decreased enzymatic capacity
* less metabolism
* drug accumulation

47
Q

excretion =

A

filtration + secretion - reabsorption

Pharmacology Exam 1 (15 decks)

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