(ADM) E Flashcards

1
Q

define CL

A

the apparent volume of plasma completely cleared of drug per unit time

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2
Q

2 drugs with the same CL would only have the same half life if…

A

they have the same Vd

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3
Q

why is CL different in different drugs?

A
  • inefficient extraction through that elimination organ

- additivity of CL, some drugs are cleared in more than 1 organ

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4
Q

what are the normal blood flow values of:

  • liver
  • kidney
  • cardiac output
A

liver = 1300-1500ml/min
kidney = 1100ml/min
cardiac output = 6000ml/min

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5
Q

what value of Eh is high extraction ratio?

A

> 0.7

<0.3 is low so hardly eliminated by liver

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6
Q

what is the equation to describe F?

A

F= Fa . FG . FH

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7
Q

what does it mean that half life is a combined parameter?

A

influenced by both Vd and CL

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8
Q

why is the liver highly perfused?

A

high blood flow because has 2 blood supplies; one from hepatic artery and one from portal vein (total approx 1.5L/min)

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9
Q

how can u increase hepatic blood flow?

A

bed rest, thyrotoxicosis, isoprenaline

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10
Q

how can u decrease hepatic blood flow?

A

exercise, heart failure, propranolol

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11
Q

give an example of enzyme induction?

A

rifampicin

smoking and clozapine

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12
Q

give an example of reversible enzyme inhibition and irreversible

A

reversible: ketokonazole
irreversible: statins and furanocourmarins

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13
Q

what causes liver cirrhosis?

A

excessive alcohol

hepB and hepC

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14
Q

for a drug to be eliminated into the bile, what are the requirements?

A
  • presence of transporters as takes place by active facilitated transport
  • polar molecule
  • large molecule (>350MW)
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15
Q

give an example of a drug which is NOT metabolised in liver so excreted unchanged in the kidney?

A

metformin (by OCT1 transporters)

which also has a very high Fu (none is bound)

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16
Q

what info do you have about the perfusion of the kidney?

A

highly perfused - gets 20% of cardiac output

17
Q

what is normal GFR?

A

120ml/min

18
Q

if a drug is completely unbound, what route of renal elimination does it go down?

A

filtration - as this process is only for unbound drugs!

19
Q

GRF is …

A

usually constant and relatively indpendant of renal blood flow

20
Q

how does active tubular SECRETION work?

A

facilitates excretion by adding drug to tubular fluid and uses transporters so is a saturable process!

21
Q

what transporters are involved in secretion?

A

uptake: OAT1 (anionic e.g. penG) and OCT1 (cationic e.g. metformin)
efflux: MRP and MATE

22
Q

what enzymes are found in proximal tubule of kidney?

A

metabolic GLUT enzymes

23
Q

what is the normal urine flow value?

A

1ml/min

24
Q

reabsorption is a passive process, what does this mean?

A

doesn’t need energy to transporters etc
occurs passively for UNBOUND and NONIONISED LIPOPHILIC drugs - so drugs in this form can cross the membrane and be rebabsorbed

25
Q

in what kind of drugs is equilibrium via reabsorption hardly ever achieved?

A

in polar strong acid and basic drugs

26
Q

what is normal urine pH?

A

4.5-7.5

27
Q

give an example of an drug affected by urine pH?

A

amphetamine (people take Na bicarb with it to allow for more reabsorption)

28
Q

when is renal CL dependent on urine flow?

A

when reabsorption tends to equilibrium (so not in strong acidic or basic polar drugs)

29
Q

when is dose adjustment needed in renal disease?

A
  • if elimination for that drug is mainly via the kidney
  • if drug has narrow TW
  • if drug forms active metabolites
  • if they have impaired metabolism (as 2 probs now)
30
Q

which one mechanism of renal excretion is active rather than the other 2 which are passive?

A

secretion - uses transporters