Pharmacology of Drugs Used to Treat Inflammation

Question 1

Hallmarks of Inflammation

Answer 1

Redness, Swelling, Increased temp, pain

Question 2

NSAID MOA

Answer 2

COX-1 inhibition- decr. prostaglandin that protects GI and maintains RBF, reduction in thromboxane that induces platelet aggregation
COX-2 inhibition- reduction in prostaglandins involved in inflammation

Question 3

Non-Selective NSAID

Answer 3

aspirin, Toradol, Motrin, Naprosyn, Ketoporfen, Indocin

Question 4

COX-2 Selective

Answer 4

Sight- Piroxicam/Sulindac
Likely- Lodine/Mobic/Relafen (nabumetone)/Diclofenac
Selective- Celebrex

Question 5

NSAID clinical uses

Answer 5

OA, RA, Gout, musculoskeletal pain, HA, body aches, menstrual cramps, Closure of ductus arteriosus

Question 6

NSAID ADE

Answer 6

NV, ulcers, bleeding, ranal failure, HA, tinnitus, dizziness, hypertension (fluid retention) abnormal LFT

Question 7

CV and GI Risks

Answer 7

CV risks increase with high doses, naproxen lowest, GI risk highest with piroxicam and ketorolac (Celebrex and Mobic best for GI ADE)

Question 8

Celebrex

Answer 8

less GI more CV risk, some renal toxicity, very COX-2 selective

Question 9

Motrin

Answer 9

used for closure of ductus arteriosus, high doses need for anti-inflammatory effects (600-800 tid-qid)

Question 10

Relafen

Answer 10

Nabumetone, prodrug, long half-life, dosed daily

Question 11

Feldene

Answer 11

Piroxicam, long half-life, once daily, high risk for GI ulcers

Question 12

Mobic

Answer 12

meloxicam, mostly Cox-2, long half-life

Question 13

Indocin

Answer 13

indomethacin, used for gout, closure of ductus arteriosus, GI effects @ high doses

Question 14

Toradol

Answer 14

ketorolac, post surgical pain for up to 5 days, SIGNIFICANT GI and renal toxicities with longer durations

Question 15

Other NSAIDs

Answer 15

Voltaren, Lodine, Nalfon, Ansaid (flurbiprofen), Clinoril (sulindac), Daypro (oxprazosin), ketoprofen

Question 16

DMARDs

Answer 16

onset= weeks to months, slow progression of disease, some are biologics

Question 17

Methotrexate

Answer 17

DMARD, first line for RA, inhibits proliferation and stimulates apoptosis of immune-inflammatory cells, folic acid antagonist, used for lupus erythematosis, cancer

Question 18

Methotrexate ADE

Answer 18

NVD, stomatitis, hepatotixicity, thrombocytopenia, teratogenic, when taken with folic acid GI and liver toxicities reduced

Question 19

Hydroxychloroquine

Answer 19

DMARD, Plaquenil, MOA unclear: inhibits lymphocyte responses, stabilizes lysosomal enzymes, Inhibits DNA and RNA synthesis, traps free radicals, 3-6 mo. for response

Question 20

Plaquenil Clinical Uses

Answer 20

less for RA, malaria, lupus erythematosis

Question 21

Plaquenil ADE

Answer 21

NVD, rash, alopecia, Ocular toxicity

Question 22

Sulfasalazine

Answer 22

DMARD, Azulfidine, MOA: suppress t-cell response and inhibit b-cell proliferation, for RA and ankylosing spondylitis

Question 23

Sulfasalazine ADE

Answer 23

NVD, anorexia, rash, leukopenia, alopecia, stomatitis, elevated liver enzymes

Question 24

Leflunomide

Answer 24

DMARD, Arava, works like sulfasalazine, for RA and psoriasis, ADE: Diarrhea, hepatotoxicity, alopecia, leukopenia

Question 25

Nonbiologic DMARD

Answer 25

Azathioprine, cyclophosphamide, cyclosporine, penicillamine, minocycline, mycophenolate

Question 26

Biologic DMARDs: TNF-a Inhibitors

Answer 26

Enbrel (entanercept), Humira (adalimumab), Remicade (infliximab), Symponi, Cimzia

Question 27

TNF-a inhibitor Clinical Uses

Answer 27

RA, Ankylosing spondylitis, psoriatic arthritis, Crohn’s disease

Question 28

ADE of TNF-a inhibitors

Answer 28

injection site reactions, demyelinating syndromes, lupus-like syndrome, heart failure exacerbation, infection, malignancy

Question 29

Gout

Answer 29

characterized by hyperuricemia and urate crystals in joints

Question 30

XOI

Answer 30

hypoxanthine to xanthine to uric acid via xanthine oxidase

Question 31

Gout acute attacks

Answer 31

First line is NSAIDs (Indocin and Motrin), inhibit prostaglandin synthase

Question 32

Gout acute attacks

Answer 32

Colcrys- MOA: inhibit leukocyte migration and phagocytosis, prophylaxis of gout

Question 33

Colchicine ADE

Answer 33

NVD & abdominal pain, rare- bone marrow suppression, alopecia

Question 34

Uricosuric Agents

Answer 34

Probenecid (Benuryl), Sulfinpyrazone (Anturane), MOA: inhibit reabsorption of uric acid in proximal tubule, to prevent recurrent episodes, ADE: GI, rash, renal stones

Question 35

Allopurinol

Answer 35

Zyloprim, XOI, prevent recurrent gout attacks, antiprotozoal, ADE: gout flare, NVD, HA

Question 36

Febuxostat

Answer 36

Uloric, XOI, prevent recurrent episodes, ADE: NVD, HA, LFT elevation, can be used in those with allopurinol hypersensitivity

Question 37

Krystexxa

Answer 37

pegloticase, IV only, MOA: converts uric acid to allantoin

Question 38

Adrenocorticosteroids

Answer 38

Glucocorticoids, Mineralocorticoids, Androgens and Estrogens

Question 39

Cortisol

Answer 39

natural glucocorticoid, hydrocortisone, released in response to ACTH from pituitary, has mineralocorticoid action, metabolic effects on sugars, inhibits glucose uptake

Question 40

Cortisol catabolic effects

Answer 40

decreased muscle mass and weakness, skin thinning, peripheral fat redistribution

Question 41

Cortisol

Answer 41

reduces COX-2 expression, inhibits macrophages

Question 42

Glucocorticoid Clinical uses

Answer 42

Addisons Disease, Diagnose Cushings syndrome

Question 43

Glucocorticoid ADE

Answer 43

not common w/ tx less than two weeks, taper over weeks or months to avoid adrenal insufficiency

Question 44

Glucocorticoid ADE

Answer 44

weight gain, moon faces, buffalo hump, acne, hyperglycemia and diabetes, bone loss, ulcer and GI bleeding, cataracts, hypertension