Pharm Ii: Drugs Against Inflammation

Front 1

asprin

Back 1

asa, hydrolyzed to salicylic acid, accumulated in stomach lining
cox 1 & 2

Front 2

acetaminophen

Back 2

non-specific cox inhibitor
tylonal
no anti-inflamm, no anticoag
OD: for overdose you want to give acetylcyctein stat

Front 3

ibuprofin

Back 3

non-selective cox inhib
nsaid
most potent/expensive than asprin
milder GI effect

Front 4

naproxin

Back 4

non-selective cox inhib
nsaid
most potent/expensive than asprin
milder GI effect

Front 5

indomethacin

Back 5

nsaid, very power, serious untoward effects
used short term: gout, ankylosing spodylitis, pericarditis, pleurisy

Front 6

celecoxib

Back 6

selective for COX2
no more effective and more expensive than non-selective
lower GI problems
a SULFA derivatice

Front 7

misoprostol

Back 7

synthetic prostaglandin
can prevent ulcers when used concurrently with nsaids
SE: diarhhea, cannot be used in pregnancy!!

Front 8

methotrxate

Back 8

dmard
standard of care
inhibits dihydrofolate reductase --> thymidine deficiency
teratogenic
decreases lymphocytes and pmns
SEs: GI, hematological, hepatic... folic acid suppliments do NOT mitigate marrow toxicity

Front 9

hydroxychloroquine

Back 9

malaria and ameba infestation (gets into the acidic vacuole) and dmard
reduces chemotaxis, phagocytosis, superoxide production
effects on RA take 3-6 months... rare untoward effects
don't give with g6pdh defic.
ok in preg

Front 10

sulfasalazine

Back 10

sulfonamide
used in IBS
MOA unknown
SE: rash, dissiness, GI upset, photosens

Front 11

leflunomide

Back 11

heparic metabolism
inhibits dihydroorotate dehydrogenase
diarrhea, hair loss, hepatic damage
cyp2c9 inhibited (many drugs, including NSAID, are metabolized by this p450)

Front 12

azathioprine

Back 12

inhibits dna synthesis
bioavailibilty NOT controlled by 3A4

Front 13

what are the TNF inhibitors? and what is special about them?

Back 13

etanercept: fusion protein, scavenges TNF
imfliximab (remicade): chimeric human-mouse ab, inactivates TNF
adalimumab: human ab, like imfliximab

Front 14

what are se's of tnf inhib?

Back 14

tb, infections, tumors? ms rare

Front 15

abatacept

Back 15

inhibits t-cell activity, binds CD80/86 on apcs, inhibits CD28 on lymphocytes binding
used when tnf-inhib fail
should NOT be given with tnf inhib (serious infection risk increases greatly)
pts w/ COPD may hay increased pulmonary effects

Front 16

rituximab

Back 16

monoclonal ab, targets bcell ag CD20
used against a variety of autoimmune reactions.. iv infusion rxns are SEs

Front 17

what are the drugs against gout?

Back 17

colchicine, allopruinol, probenicid
(what did the anus say when it had it's tempurature taken? ALLO COLD PROB)

Front 18

what dose colchicine do?

Back 18

binds to TUBULIN in leukocytes and reduces their moblility and ability to phagocytose, only used to control acute gout

Front 19

what does allopurinol do?

Back 19

inhibits xanthine oxidase! both steps. PREVENTATIVE.
SE: allergic skin reactions (3% pts)
GI,, marrow depression, neuritis occur infrequently

Front 20

what is the uric acid reaction?

Back 20

xanthine --> hypoxyanthine --> uric acid, enzyme in both steps = xanthine oxidase

Front 21

tell me about probenicid.

Back 21

inhibits both active excretion and reabsorption and results in net loss of uric acid... can be given chronically.
aplastic anemia rarely occur.
also preventative
inhibits Prox tubule secretion of some other drugs

Front 22

please list three glucocorticoids

Back 22

predisone, corisol, dexamthasone

Front 23

what are the three main effects of glucocorticoids, and which one is only really important pharmalogically (as oposed to phys)?

Back 23

antiinflammitory (ding ding), metabolic effect, and Na+ retention

Front 24

what are some wierdo SE of glucocorticoids?

Back 24

cataracts, thin skin, peptic ulcer, psychosis........ adrenal atrophy! (reason for taper)

Front 25

where is cox 1 localized?

Back 25

stomach, platelets and many other tissues

Front 26

where is cox 2 localized?

Back 26

cells involved in inflammation, vascular endothelium and renal JG apparatus

Front 27

SEs of asprin?

Back 27

gastric irritation, bleeding, gouty attacks, reye's syndrom in kids, renal disease exacerbation, bronchospasm

Front 28

SEs of acetomenaphine?

Back 28

hepato and renal toxicity, tx with acetylcysteine reduces hepatotoxicity

Front 29

what can NSAIDs decrease effectivness of?

Back 29

ABCDE

Ace inhib, Beta blocker, aCe inhib, Diuretics, acE inhib

Front 30

what is interesting about glucocorticoids and toxicity?

Back 30

very time and dose dependant... a large dose over short about of time is well tolerated (think cortisol shot?) and small amounts over long period of time can be not tolerated well at all.

Front 31

prednisone

Back 31

5 times more potent as anti-inflamm (and gluconeogenesis) than cortisol, but with only 30% of Na+ retaining properties

Front 32

dexamethasone

Back 32

30 times more potent than cortisol as an anti-inflamm, 0.04% Na+ retaining property

Front 33

metabolism of GCs?

Back 33

p450

Front 34

anti-leukemic effects of glucocorticoids?

Back 34

a single dose can cause lymphocyotopenia that can persist for 24 hours..... lymphos are sequestered in the spleen
certian elements destroyed by GCs