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Musculoskeletal > Pharm: DMARDS and NSAIDS > Flashcards

Pharm: DMARDS and NSAIDS Flashcards

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1
Q

NSAIDs

A

non-steroidal anti-inflammatory drugs: anti-inflammatory, analgesic, antipyretic
COX inhibitors
hepatic metabolism
effects: reduce urinary metabolites of PGI2 and TXA2, inhibit platelets
AE: GI, RENAL, increase bleeding time, increase BP, increase CV risk in those on aspirin regimen, liver (low risk in most)
CI: decrease clearance of lithium and methotrexate
monitor: LFTs, serum creatinine/BUN, stool guaiac
*does not slow progression of RA

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2
Q

DMARDs (non-biological)

A

disease modifying anti rheumatic drugs
AE: BLOOD DYSCRASIA
monitor: CBC

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3
Q

biological DMARDs

A

DMARDs with specific epitopes
AE: immunosuppression, infection
other: blood dyscrasia and malignancy
CI: vaccine

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4
Q

acetaminophen

A

NSAID
NO anti-inflammatory effect
NOT used for arthritis
AE: GI in IV use, renal rarely, HEPATIC

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5
Q

aspirin

A

NSAID
irreversibly acetylates COX
platelet does not have a nucleus and cannot regenerate COX-1
MI prophylaxis
AE: hepatic (Reye’s: flu), salicylate poisoning
monitor: serum salicylate

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6
Q

diclofenac

A

NSAID
short acting
low GI risk
AE: high dose: vascular event

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7
Q

ibuprofen

A

NSAID
COX inhibitor
AE: high risk GI, high dose: vascular event

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8
Q

indomethacin

A

NSAID

AE: most adverse effects of all NSAIDs

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9
Q

ketoprofen

A

NSAID

short acting

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10
Q

ketorolac

A

NSAID

COX-1 inhibitor

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11
Q

naproxen

A

NSAID
AE: high risk GI
*NO CV risk increase even with high dose

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12
Q

piroxicam

A

NSAID

LONG ACTING

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13
Q

sulindac

A

NSAID

AE: HEPATIC (hypersensitive)

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14
Q

celecoxib

A

NSAID
selective COX-2 inhibitor
low GI risk
AE: vascular event

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15
Q

methotrexate

A

DMARD (non-biological)
DHFR inhibitor, adenosine inhibition
polyglutamation to remain intracellular
AE: bleeding, opportunistic infections, malignant lymphoma, GI, fatal dermatologic rxns, PULMONARY, TERATOGEN
CI: liver problems, alcoholic, renal failure, vaccinations (suboptimal), pregnancy, breast feeding
monitor: LFT, serum uric acid, serum creatinine/BUN

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16
Q

hydroxychloroquine

A 
DMARD (non-biological)
intracellular vacuole alkalization (need acidic for assembly of MHC)
AE: blood dycrasias, CNS, EYE
CI: liver, alcoholism, EYE 
Tx: malaria, RA, SLE
monitor: OPHTHALMOLOGIC exam
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17
Q

leflunomide

A

DMARD (non-biological)
inhibits dihydroorotate dehydrogenase: inhibits pyrimidine synthesis
urocosic effect
AE: LFT, TERATOGEN
CI: immune suppression, infection
monitor: LFT, pregnancy test, electrolytes

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18
Q

sulfasalazine

A

DMARD (non-biological)
metabolized by colon bacteria to mesalamine that inhibits PG and LT produciton
acetylated
CI: renal, hypersensitivity to salicylate or sulfonamide
monitor: LFT, serum creatinine/BUN, urinalysis

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19
Q

betamethasone

A

DMARD
POTENT
long T1/2: poor solubility
corticosteroid

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20
Q

cortisone

A

DMARD

corticosteroid

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21
Q

dexamethasone

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A

DMARD
POTENT
long t1/2: poor solubility
corticosteroid

22
Q

hydrocortisone

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A

DMARD
low potency
SHORT t1/2
corticosteroid

23
Q

methylprednisolone

Study These Flashcards
A

DMARD

corticosteroid

24
Q

prednisolone

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A

DMARD

corticosteroid

25
prednisone
DMARD | corticosteroid
26
triamcinolone
DMARD | corticosteroid
27
abatacept
CTLA4 binds CD80/86 to prevent T-cell co-stimulatory signal engaging with CD28 AE: maltose complicates blood glucose test
28
adalimumab
TNFa mAb
29
anakinra
IL-1 antagonist | AE: blood dycrasias
30
certolizumab
TNFa mAb AE lacking?: CV AE: blood dycrasias
31
etanercept
TNFa inhibitor: false TNF receptor AE lacking?: CV Postlewaite uses this TNFa inhibitor before others: variable suppression so less infection
32
golimumab
TNFa mAb AE lacking?: lupus like syndrome AE: LFT
33
infliximab
TNFa mAb CI: HEART FAILURE AE: LFT
34
apremilast
oral PDE4 inhibitor CYP substrate Pgp Tx: psoriatic arthritis and plaque psoriasis AE: WEIGHT LOSS, depression, suicide ideation
35
rituximab
CD20 mAb (B cell) need CONTRACEPTION (up to 4-6 mo. after ending) AE: Steven-Johnson syndrome, epidermal necrolysis, CV, blood dycrasias CI: PREGNANCY
36
tocilizumab
IL-6 mAb AE: blood dycrasias monitor: LFT, serum lipids
37
PGE2
activation of inflammatory cells cytoprotective mucus secretion, bicarb release, initiation of repair
38
How do COX-2 selective inhibitors differ from traditional NSAIDs?
inhibit prostacyclin without thromboxane inhibition: pro-thrombotic state NO: GI toxicity, platelet inhibition, increase bleeding time, normal urinary TXA2 metabolites
39
How do NSAIDs damage the gastric mucosa?
direct chemical irritation and inhibition of PGE2 | causes: ulceration and gastric bleeds
40
risk factors for adverse GI events with NSAIDs
1. prolonged use, max dose 2. age, male 3. GI Hx 4. comorbidity: CV, HTN, diabetes, hepatic, renal 5. alcohol, smoking 6. use of aspirin, warfarin, oral corticosteroids, SSRIs, venlafaxine, duloxetine
41
ways to reduce GI toxicity of NSAIDs
1. enteric coating 2. FDA says: milk/ food Sweatman says: empty stomach to reduce doses 3. PG analog (misoprostol) 4. H2 antagonist 5. PPI (BEST)
42
COX-1
platelet TXA2 production prothrombotic
43
COX-2
endothelial PGI2 (prostacyclin) production antithrombotic
44
How can NSAIDs cause RENAL toxicity?
PGI2 and E2 are released in abnormal conditions and maintain renal blood flow and GFR inhibition of PGs can damage kidney Sx: hematuria, pyuria, white cell casts, proteinuria, etc.
45
salicylate poisoning
ASPIRIN overdose stimulate medullary respiratory system: hyperventilation RESPIRATORY ALKALOSIS uncoupling of oxidative phosphorylation: METABOLIC ACIDOSIS cerebral and pulmonary edema, CV collapse sign: RINGING of EARS prolonged prothrombin time
46
Tx for RA | What if this Tx fails?
early aggressive therapy 1. DMARD: methotrexate (or hydroxychoroquine: less AE) 2. addition: NSAID and corticosteroid 3. failure with traditional approach: biological as mono therapy or with methotrexate
47
How does adenosine inhibition help in RA?
METHOTREXATE inhibits lymphocyte proliferation and suppresses IL-1, IFN-y and TNF increase IL-4
48
corticosteroids
inhibit: Nf-kb, AP-1, NF-AT: reduced TNFa, IL-1, IL-6 upregulate: RANKL, M-CSF Src inhibition; intercalate plasma and mitochondrial membrane Tx: RA AE: osteoporosis, cushingoid, diabetes, obesity, lipid profile (reduce with localized injection depot), hyperglycemia, weight gain monitor: osteoporosis, fasting blood sugar levels, glaucoma risk, ankle edema
49
TNFa inhibitors AE
malignancy lupus-like syndrome CV: CHF, hypotension, angina, dysrhythmia
50
Drugs with AE of blood dyscrasias
``` anakinra certolizumab rituximab tocilimumab non-biologic DMARDs ```
51
Drugs need to monitor LFT
golimumab infliximab tocilimumab
52
Drugs self-administered SC
``` injection site rotation abatacept adalimumab anakinra certolizumab etanercept golimumab ```

Musculoskeletal (13 decks)

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