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PKPD > Metabolism & Clearance > Flashcards

Metabolism & Clearance Flashcards

1
Q

glucuronidation

A

UDP-glucuronosyltransferase
UGT

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2
Q

sulfation

A

sulfotransferases
SULT

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3
Q

acetylation

A

N-acetyltransferases
NAT

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4
Q

Amino acid conjugation

A

ex. glycine
low activity in newborns, fatal benzyl acid toxicity

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5
Q

glutathione conjugation

A

glutathione-S-transferase

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6
Q

methylation

A

catechol O-methyl transferase or thiopurine methyl transferase
COMT or TPMT

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7
Q

CYP2D6 activity & polymorphism

A

absent or ultrarapid
no activity or buildup of codeine

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8
Q

CYP2C19 activity & polymorphism

A

defective (race dependent)
metabolizes prodrug for clopidogrel

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9
Q

TPMT activity & polymorphism

A

Caucasians have diminished or deficient activity
severe myelosuppression with azathiopurine

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10
Q

solute carriers (SLCs)

A

OAT, OCT, OATPs, & MATE

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11
Q

transporters responsible for bioavailability

A

OATP2B1
P-gp (ABCB1, MDR1)
MCT
PEPT1

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12
Q

OATP2B1 location & activity

A

uptake in gut, liver, and systemic circulation
large MW organic anions
P1B3 and P1B1 are liver specific

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13
Q

P-gp location & activity

A

kidney, liver, & BBB
protects and eliminates compounds from cells

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14
Q

MCT location & activity

A

intestine
transports low MW organic anions
can improve oral absorption

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15
Q

PEPT1 location & activity

A

intestine
transports peptides
can improve oral absorption

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16
Q

transporters responsible for liver activity

A

OATPs
BCRP (ABCG2)
P-gp

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17
Q

BCRP location & activity

A

intestine, liver, BBB, and some cancers
protects and eliminates compounds from cells

18
Q

transporters responsible for renal activity

A

OAT
OCT
MATE

19
Q

OAT location & activity

A

renal secretion (uptake)
organic anion transporter

20
Q

OCT location & activity

A

renal secretion (uptake)

21
Q

MATE location & activity

A

apical membrane of kidney
recognize cations for efflux

22
Q

transporters with activity in the BBB

A

BCRP & P-gp

23
Q

Equilibriative nucleoside transporters (ENTs)

A

transport nucleosides, regulate uptake of purines and pyrimidines

24
Q

where does renal secretion occur

A

proximal tubules

25
Q

where does renal reabsorption occur

A

along the nephron

26
Q

when CLr > CLrf (excretion exceeds filtration)

A

secretion occurs

27
Q

when CLr < CLrf (filtration exceeds excretion)

A

reabsorption occurs

28
Q

what induces CYP1A2

29
Q

what induces CYP2C19

A

rifampin, secobarbital

30
Q

what induces CYP2E1

A

ethanol, isoniazid

31
Q

what induces CYP3A4

A

carbamazepine, phenobarbital, rifampicin, phenytoin, SJW, troglitazone

32
Q

what does carbamazepine do acutely and chronically

A

acute- inhibit 3A4
chronic- induce 3A4

33
Q

SJW induces 3A4 & P-gp (ABCB1) which

A

increases clearance of indinavir
reduces bioavailability of talinolol

34
Q

fluoxetine (prozac) inhibits CYP2C9

A

warfarin metabolism is lost, conc increases

34
Q

itraconazole inhibits CYP3A4

A

increases CYP3A4 substrates

34
Q

fluvoxamine (luvox) inhibits CYP1A2

A

increases CYP1A2 substrates

35
Q

cyclosporine inhibits OATP1B1

A

prevents CL and leads to accumulation of rosuvastatin

35
Q

talinolol is a P-gp inhibitor

A

leads to accumulation of digoxin

36
Q

probenecid is a OAT1 inhibitor

A

reduces renal secretion, given with cidofovir (vistide) to reduce accumulation

37
Q

clarithromycin inactivates CYP3A4

A

midazolam concentrations rise

38
Q

furanocoumarins in GFJ inhibit CYP3A4 intestinal metabolism

A

increased bioavailability and systemic concentrations of CYP3A4 substrates
felodipine

39
Q

naringin in GFJ is an OATP inhibitor

A

reduces bioavailability of fexofenadine

PKPD (2 decks)

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