Non-opioids, gout, rheum arthritis Flashcards

(82 cards)

1
Q

what are non-pharm approaches to gout & RA?

A

dietary modifications: reduce purine-rich foods, weight
PT: for RA, to improve joint mobility
acute pain management = cold/hot compresses

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2
Q

non opioid analgesic types

A

NSAIDs, acetaminophen, DMARDs, colchicine

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3
Q

fatty acid in cell membrane phospholipids
released w/ cell activation or damage by phospholipase A2 enzyme
PGs and LTs derived from this

A

arachidonic acid

pathway = leukotrienes, prostanoids

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4
Q

what drug inhibits COX enzymes that produce prostaglandins and mediate pain and inflammation

A

NSAIDs

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5
Q

non-selective NSAIDs

A

salicyclates = aspirin, topical salicyclic acid, bismuth-subsalicylate (pepto bismol)

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6
Q

cox-2 selective NSAID

A

celecoxib (celebrex)

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7
Q

other nsaids

A

classes: heteroaryl acetic acids, propionic acid derivatives, oxicam derivatives, acetic acid derivatives

ibuprofen, naproxen, diclofenac, ketoprofen, indomethacin, meloxicam, ketorolac

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8
Q

what drug is analgesic, anti-inflamm, antipyretic for RA, osteoarthritis, gout, acute pain, or closure of PDA?

A

NSAIDs

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9
Q

What are propionic acid derivative NSAIDs?

A

OTC: ibuprofen, naproxen

rx: ketoprofen, oxaprozin

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10
Q

What are propionic acid derivative NSAIDs indicated for?

A

chronic treatment of RA and OA, mild-mod acute pain and fever, closure of PDA (ibuprofen)

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11
Q

What are acetic acid derivatives NSAIDs?

A

Rx: indomethacin, sulindac

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12
Q

what are indications for acetic acid derivatives NSAIDs?

A

acute gout attack, closure of PDA

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13
Q

acetic acid derivatives NSAIDs have high toxicity with adverse effects in –

A

1/3 of patients

pancreatitis, headache, dizziness, confusion, hallucinations, thormbocytopenia and aplastic anemia

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14
Q

what are oxicam derivatives

A

RX: piroxicam, meloxicam

long half lives, meloxicam preferentially inhibiting COX-2, less GI

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15
Q

heteroaryl acetic acid NSAIDs

A

RX: diclofenac, keterolac (great for renal calculi)

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16
Q

strongest NSAIDs are

A

heteroaryl acetic acid NSAIDs

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17
Q

indications for heteroaryl acetic acid NSAIDs

A

moderate to severe pain, only can use short-term up to 5 days with risk of nephrotoxicity

  • Cr baseline, monitor w/ severe renal disease
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18
Q

—– may increase LFTs, check at baseline and monitor with heteroaryl acetic acid NSAIDs

A

diclofenac

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19
Q

selective, reversible inhibition of COX-2 with no antiplatelet effect

A

celecoxib = increased CV risks

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20
Q

celecoxib is used for

A

long term treatment of RA and OA, mild/mod acute pain

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21
Q

celecoxib ADRs

A

same black box warnings as NSAIDs, increased risk of MI/stroke (avoid in high risk), may interfere with aspirin’s antiplatelet effects

C in 1st/2nd trimester, D for DEATH in 3rd trimester

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22
Q

toxicities of NSAIDs

A

GI Toxicities - protect w/ PPI or H2 blockers, metabolized by 2C9

renal toxicities – dose adjustments needed wit kidney injuries, nephrotic syndrome, hyperkalemia

cardiovascular risk: increased risk of MI and stroke

hepatic toxicity: varying degrees of enterohepatic circulation, liver damage possible

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23
Q

non-selective, irreversible inhibition of COX
acetylsalicyclic acid –> alicylate

A

aspirin

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24
Q

use in antiplatelet effects, decreased strokes, reduced mortality w/ MI and recurrence, reduce risk with stable angina

A

aspirin

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25
aspirin ADRs
GI= discomfort, bleeding, PUD, take with food **pregnancy category X** hematologic allergic reye's syndrome (nausea, lethargy, confusion) gout = lowers renal uric acid clearance C in 1st and 2nd, D in third
26
aspirin DDIs
can displace warfarin, phenytoin, valproic acid
27
mild salicylism (ASA overdose)
N/V, dizziness, tinnitus --> hospitalize --> activated charcoal
28
moderate-severe salicyclism
restlessness, hallucination, seizures, coma, death admit, activated charcoal
29
other salicylates like
bismuth-subsalicylate (pepto bismol), anti-inflamm, antacid, part of h pylori eradication, dark stools topical salicylic acid
30
WHat are ADRs of NSAIDs
HTN due to fluid retention, edema, headaches, tinnitus, dizziness, hypersensitivity
31
ADRs of non selective NSAIDs
black box = increased CV risk, GI bleed. PUD, separate w/ ASA at least 2 hours most pregnancy B in 1st and 2nd trimesters (oxaprozin and keterolac are C) and D in 3rd trimester -- avoid!
32
highest NSAID GI risk
keterolac (ibuprofen is lowest)
33
highest NSAID CV risk
naproxen (celecoxib is lowest)
34
inhibition of COX enzymes in brain without anti-inflammatory
acetaminophen (also doesn't have antiplatelet effect)
35
acetaminophen is metabolized in the
liver, with renal excretion
36
use acetaminophen for
mild-moderate pain relief, fever reduction, DOC with viral illness, pregnancy category B
37
acetaminophen is better because of
less GI irritation, no anti-inflammatory effects
38
acetaminophen can cause
liver toxicity from toxic metabolite production (NAPQI conversion from CYP2E1)
39
overdose of acetaminophen can occur with
long term supratherapeutic doses, 4gm/day MAX -- monitor LFTs with high dose therapy
40
the bad metabolite is
NAPQI
41
treat acetaminophen toxicity with
n=acetylcysteine RF: chronic alcohol use, malnutrition, use of other drugs
42
What are the different types of RA meds?
DMARDs = methotrexate, sulfasalazine, leflunomide, hydroxychloroquine biologics = TNF-alpha inhibitors, T cell inhibitor glucocorticoids NSAIDs
43
DMARDs
disease modifying antirheumatic drugs ** prevent and slow disease progression and destruction ** takes 2 weeks - 6 months most have serious effects and cannot be used in pregnancy
44
safest RA drug in pregnancy
steroids, sulfasalazine, hydroxychloroquine
45
primary choice for RA
methotrexate 3-6 week onset
46
folic acid antagonist
methotrexate
47
methotrexate is never
dosed daily -- weekly dose, 7.5mg-22.5mg
48
ADRs of methotrexate
lots of black box warnings -- must wait 3 months after finishing drug to concieve or donate blood category X hepatotoxicity -- must test for hep B and C before therapy, monitor bone marrow suppression immunosuppression *cannot administer live vaccines* can cause lung inflammation
49
methotrexate montioring
liver function, CBC, renal function folate supplementation to reduce side effects
50
DMARD aminosalicyclate anti-inflamm COX inhibitor (5-ASA)
sulfasalazine onset 1-3 months
51
1st line for mild, mod, severe RA
sulfasalazine
52
What are ADRs of sulfasalazine
N/V, ab pain, skin rash, dyspepsia, arthralgias, myalgia, bone marrow suppression
53
sulfasalazine is CI in
ASA and sulfa allergies pregnancy category B (only if benefits outweigh risks) interferes with folate absorption, so give patient a supplement
54
DMARD: inhibiting pyrmidine synthesis with inhibiting T and B cell production
leflunomide
55
1st line for mild, mod, severe RA, onset in 4-6 weeks
leflunomide
56
ADRs of leflunomide
diarrhea, nausea, headache, alopecia, HTN, hepatotoxiity (get hep B and C tested, elevated LFTs, monitor at baseline and monthly x 6 months) rash, pruritus, allergic reaction teratogenic!!!!!!!!!!!!!!! pregnancy category X = must have negative test before starting med, and use 2 forms of BC, must have undetectable drug levels on TWO occasions before trying to get pregnant
57
cytotec causes
medical abortion
58
induce leflunomide elimination by
cholestyramine
59
less effective DMARD
hydroxychloroquine -- unclear MOA, for mild RA, effect in 3-6 months ADRs: ocular toxicity, N/V, dyspepsia, abdominal pain, dizziness, ataxia, headache category C = only if benefits outweigh risk
60
biologic RA first line
TNF inhibitors etanercept infliximab adalimumab
61
biologic RA 2nd
rituximab (CD20+ B cells) anakinra (Il-1) abatacept (T lymph inhib) tocilizumab (IL-6)
62
can give biologics with
methotrexate when severe disease w/ poor prognosis, 2ndary for resistant disease (combo of 2+ DMARDs failing to achieve low disease activity after 3 months)
63
ADRs of biologics
black box for serious infections and malignancy -- immunosuppression --> evaluate TB risk, test for latent disease at baseline and annually increased risk of malignancy, infusino reaction, HF, hepatotoxicity
64
monitor for RA meds
methotrexate: monitor LFTs, CBC, Cr biologics: infections, CBC, LFTs, renal hydroxychloroquine: retinal toxicity, eye exams
65
gout tx
NSAIDs, colchicine, steroids, urate lowering therapy (allopurinol, febuxostat, probenecid)
66
acute gout attack tx
NSAIDs = indoemthacin * , ibuprofen, naproxen, diclofenac, meloxicam colchicine steroids reduce inflammation with NSAIDs DOC
67
chronic gout tx
allopurinol, febuxostat, probenecid, lower uric acid levels
68
DOC for acute gout with no CIs (PUD, renal insufficiency, CHF)
NSAIDs = indomethacin!
69
do not use -- in gout
aspirin
70
inhibits leukocyte migration and phagoytosis, relieving pain and inflammation by reducing inflammation in joint 3A4 and PGP substrate -- strong inhibitors can lead to serious and fatal toxicity (amiodarone, clarithormycin) reduce dose!
colchicine = can take at first signs of an attack
71
use -- if NSAIDs are CI in gout
colchicine initial dose 1.2mg + additional .6mg one hour later is just as effective! narrow therapeautic index
72
ADRs of colchicine
N/V, diarrhea, caution in hepatic and renal impairment
73
monitor gout with
serum uric acid levels, joint aspiration, renal function
74
steroids in gout are
3rd line, if both previous are CId intra-articular methylprednisonlone or triamcinolone for monoarticular disease oral prednisone for polyarticular disease avoid if you have not ruled out septic joint!
75
blocks xanthine oxidase enzyme
allpurinol
76
what to use to prevent acute attacks in chronic gout?
allopurinol with 2-3+ attacks/year with continued elevation of uric acid levels not anti-inflammatory
77
ADRs of allopurinol
titrate slowly, use NSAID or colchicine in flare, cataracts allergic skin reaction GI, hepatic
78
nonpurine xanthine oxidase inhibitor and can be administered to renal insufficiency without dose adjustments
febuxostat
79
decreases uric acid reabsortion, inhibits excretion of penicillins, aspirin can decrease effectiveness
probenecid (uricosuric drugs) ADRs: titrate and use NSAID/colchicine in flares uric acid stones, must drink 2L of fluid/day during therapy
80
what are pregnancy category B drugs of this lecture
NSAIDs (1st/2nd trimester) biologics acetaminophen
81
what are category C drugs of this lecture
celebrex NSAID biologics colchicine
82
what are category X drugs of this lecture
methotrexate