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PHARMACOLOGY I > L2-3: Pharmacokinetics > Flashcards

L2-3: Pharmacokinetics Flashcards

(59 cards)

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1
Q

water soluble + lipid soluble drugs penetrate cellular membranes through ____ diffusion

A

passive (simple)

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2
Q

3 types of carrier-mediated trasnport

A
  • structure specific
  • competition
  • Tmax
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3
Q

a ______ drug in an acidic medium (like stomach) is ______ ionized and more lipid soluble = rapidly absorbed

A

weak acidic drug
less ionized

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4
Q

if a drug is less ionized, how does this affect its ability to be absorbed

A

less ionized = absorbed quickly

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5
Q

what happens if a weak basic drug diffuses into an acidic medium

A

drug becomes ionized and will accumulate

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6
Q

why aren’t strong acids and bases lipid souble (cannot penetrate lipid membranes by passive diffusion)

A

they are always ionized in the body
ionized = not lipid soluble

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7
Q

what is ion trapping

A

acids accumulate in basic env
bases accumulate in acidic env

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8
Q

what causes an increase in the elimination of bases in urine

A

making the urine more acidic w/ ammonium chloride

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9
Q

what causes an increase in the elimination of acids in urine

A

making the urine more basic by sodium bicarbonate

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10
Q

the amount of active drug available at the site of action

A

bioavailability

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11
Q

what is the bioavailability of IV administered drugs

A

100%

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12
Q

disadvantages of oral administration

A
  • emesis (irritation of intestinal mucosa)
  • irregularities in abs
  • metabolism by intestinal flora
  • abs drug is exposed to liver
  • gastric emptying time
  • binidng to food
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13
Q

sites in body where drugs accumulate

A

Fat, Tissues, Bone

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14
Q

what is the main goal of biotransformation

A

promotion of elimination from the body

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15
Q

what does permeability glycoprotein (Pgp) aka multidrug resistance protein 1 (MDRI) do?

A

uses ATP to pump out substrates across cellular membranes
it is extensively distributed

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16
Q

factors affecting absorption

A
  • solubility
  • dissolution
  • concentration
  • blood flow
  • absrobing surface
  • pH
  • contact time
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17
Q

bioavailability is a result of ….

A
  • decomposition/inactivation of drug in intestine
  • degree of absorption
  • metabolism in gut wall or liver
  • transport of drug by P glycoproteins back to the lumen of the gut
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18
Q

term for the initial metabolism of drug as it passes through gut and liver

A

first pass effect

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19
Q

what are the sites of drug exclusion

A
  • CSF
  • ocular fluid
  • endolymph fluid
  • fetal fluid
  • pleural fluid
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20
Q

what is the apparent volume of distribution (Vd)?

A

total amount of drug in body / concentration of drug in plasma

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21
Q

what does a very low Vd indicate about the presence of a drug

A

drug is mostly present in the plasma (blood)

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22
Q

what does a high Vd indicate about the presence of a drug

A

drug is extensively distributed and binds extensively with peripheral tissues

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23
Q

drugs with very high plasma protein binding have ______ Vd

A

low

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24
Q

common characteristics of most pharmacologically active drugs

Study These Flashcards
A
  • lipid soluble
  • unionized or partially ionized
  • storngly bound to plasma proteins and other tissues
  • not readily excreted by kidney
  • remain in body for a long time
25
Phase I reactions convert ______ soluble parent compounts into more _________ metabolites (meaning they are ______ soluble)
lipid solible compounds into more polar metabolites = less lipid solible
26
phase I metabolites are usually _______ and readily ________
inactive, excreted
27
phase I reactions usually **introduce or unmask** certain ___________
functional groups ex: OH, SH, NH2
28
what are the 2 types of Phase I reactions?
Microsomal: inducible reactions that occur in the ER Non-microsomal: non inducible
29
Phase I reactions are NOT _______ specific
compound
30
type of Phase I reactions that come from ER, layers of enzyme+lipid layers that can metabolize lipid soluble drugs
Microsomal
31
Phase II reactions make drugs...
more polar, of larger molecular weight, and more inactive
32
what is the only Phase II reaction which is microsomal (therefore inducible)
Glucuronidation
33
what are the 2 most common CYP450 enzymes
CYP 3A4 and CYP 2D6
34
Phase II reactions are the _________ of drug via __________ enzymes (Ex: glucuronidation, acetylation, sulfation, methylation, etc)
conjugation transferase
35
what type of biotransformtion (phase I or II) do glucuronidation, acetylation, sulfation, methylation fall under
phase II
36
what are the types of enzymes that fall into **non-microsomal phase I reactions**
* esterases + amidases * monoamine oxidases * alcohol and aldehyde dehydrogenases
37
endogenous amines (Catecholamines, serotonin) are what type of nonmicrosomal enzymes
monoamine oxidases
38
CYP 450 inducers ? Riley Barfs Penis Goo She just wont (swallow)
rifampin barbiturates phenytoin glucocorticoids st. john’s worts
39
what are the P450 inhibitors? Candy Dildos Keep Every Vagina Functioning
cimetidine diltiazem ketoconazole erythromycin verapamil fluoxetine
40
3 methods of renal excretion of drugs and drug metabolites
* glomerular filtration in the PT * active tubular secretion or reabsorption * passive diffusion across tubular epithelium
41
measure of the capacity of the body to remove the drug
clearancce
42
proportionality constant that relates the rate of drug elimintation to its plasma concentration
clearance
43
Explain the Two Compartment Model (biexponential) of drug pharmacokinetics
* distribution of drug is not instantaneous * Vd (distribution of volume) becomes larger until equilibrium is reached * intial decline in drug [ ] is fast due to elimination and distribution occurring * the later decline in the plasma drug [ ] is only due to elimination (slower)
44
in the two compartment model, the **intitial decline in drug [ ] is due to what?**
fast elimination and distribution
45
in the two compartment model, the **secondary decline in drug [ ] is due to what?**
elimination only (slower)
46
the elimination of most drugs from the body follows ______ kinetics, meaning that a constant proportion of the drug is eliminated per unit of time
exponential
47
what assumptions are made when describing a drug's half life ?
* body is a single compartment * body size is = to Vd * drug is distributed equally throughout body * drug in plasma is in equilibrium w/ total volume
48
what type of elimination does this graph show
zero order elimination elimination process gets saturated after a high dose
49
what type of elimination does this graph show
first order
50
to reach immediate therapeutic concentration, a ____________ dose is used
loading
51
Loading Dose = _____ x _____
Vd x TC (target concentration)
52
is a loading dose dependent on the half life or clearance of a drug?
no
53
repeated administration (same dose at same dosing intervals) results in a _________ concentration of the drug in plasma
steady state
54
it takes at least _______ half lives to obtain a steady state plasma level
5
55
shortening the _______interval will result in a higher steady state concentration
dosing
56
what is the effect on steady state concentration of the dosing interval length is increased
lower steady state
57
is the time required to reach steady state levels related to the size of the dose?
no
58
where is permeability glycoprotein (P-gp) expressed
* intestinal mucosa * hepatocytes * renal proximal tubular cells * adrenal gland * capillary endothelial cells of the BBB
59
Do Vd values represent their actual distribution in the body fluid
no Vd is a conceptual figure

PHARMACOLOGY I (21 decks)

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