Gout and RA drugs

Question 1

What drug is often prescribed for gout? Esp tx for first 24hrs of symptomatic problems?

Answer 1

Indomethacin; NSAIDs for first 24 hours

Question 2

What is the mechanism of colchicine?

Answer 2

antimitotic, arrests cell division in G1 by interfereing with microtubule and spindle formation; effect is largest in cells with rapid turnover

Question 3

What is the metabolism of colchicine accomplished by?

Answer 3

50% plasma protein binding, rapid but variable oral absorption.
enterohepatic circulation
Hepatic metabolism via CYP3A4

Question 4

Who is colchicine contraindicated in?

Answer 4

patients with hepatic or renal impairment requiring concomitant tx with CYP3A4 or PgP inhibitors

Question 5

What is colchicine used to treat?

Answer 5

acute attacks of gout and is effective for 2/3 of pop if taken wthin 24 hrs of initiaon

Question 6

What is the mechanism of action of allopurinol?

Answer 6

inhibits xanthine oxidase; active metabolite inhibits reduced form of xanthine oxidase

Question 7

What is the pharmokinetics of allopurinol?

Answer 7

rapid absorption; metabolized to active metabolite, oxypurinol
half life of oxypurinol is 18-30 hrs

Question 8

What is the adverse effects of allopurinol?

Answer 8

generally well tolerated

drowsiness, hypersensitivity rxns, increase gout flare at initiation of tx

Question 9

What is a therapeutic use of allopurinol?

Answer 9

effective tx for primary and secondary gout

goal of tx is to reduce the plasmic uric acid concentration

Question 10

What is the mechanism of action of febuxostat?

Answer 10

non-purine xanthine oxidase inhibitor; forms a stable complex with both the reduced and oxidized form of zanthine oxidase

Question 11

What is the pharmokinetics of febuxostat?

Answer 11

oral admin; highly plasma protein; metabolized by CYPs adn non CYP enzymees

Question 12

What are the adverse effects/contraindications?

Answer 12

liver fxn abnormalites, nausea, joint paina nd rash
liver fxn should be monitored periodically
increased gout flares after initation
increased MIs

Question 13

What is the mechanism of action of pegloticase?

Answer 13

Pegylated recombinant form of urate-oxidase enzyme. Uricase is normally absent in humans. Pegloticase converts uric acid to allantoin

Question 14

What is the pharmokinetics of pegloticase?

Answer 14

IV admin

serum half life from 6-14 days

Question 15

What does pegloticase treat?

Answer 15

refactory gout

Question 16

What is the mechanism of action of probenecid?

Answer 16

inhibition of organic acid transport in renal tubule

Question 17

What is adverse effects of probenecid?

Answer 17

well tolerated with mild GI effects; ineffective in those with renal insufficiency

Question 18

What is probenecid used to treat?

Answer 18

hyperuricemia associated with gout or gouty arthritis

Question 19

What are some effects of probenecid with diuretics?

Answer 19

enhance adverse/toxic effect of loop diuretics
decrease diuretic effect of loop diuretics
increase serum conc of loop diuretics

Question 20

What is the mechanism of action of Etanercept?

Answer 20

soluble, recombinant fully human TNF receptor fusion protein bidning ligand portion of TNFalpha receptor

Question 21

What are the adverse effects of Etanercept?

Answer 21

serious and potentially fatal infections

lymphoma and other malignancies in adolescents and children

Question 22

What is the mechanism of action of adalimumab?

Answer 22

chimeric IgG monoclonal antibody binds to both forms of TNFalpha

Question 23

Wat are the adverse effects of adalimumab?

Answer 23

injection site from subQ

infection and upper respiratory tract

Question 24

What are the therapeutic uses of adalimumab?

Answer 24

moderately to severelya ctive RA
acute juvenitle idiopathic arthritis
often used in conjuction with methotrexate

Question 25

What is the mechanism of action of infliximab?

Answer 25

a chimeric IgG antibody binds to both forms of TNFalpha

Question 26

What are hte adverse effects of infliximab?

Answer 26

acute infusion reaction infection active TB, invasive pathogens monitor closely for signs/symptoms of infection lymphoma and other malignnancies have been reported in children and adolescent pts receiving infliximab

Question 27

What are the therapeutic uses of infliximab?

Answer 27

moderate to severely active rheumatoid arthiritis

Question 28

What is the mechanism of action of abatacept?

Answer 28

selective costim modulator; inhibits T-cell activation by binding to CD80 and CD86 on APC thus blocking required CD28 interaction btw T and APCs

Question 29

What are the adverse effects associated with abatacept?

Answer 29

headache hypersensitivity increased risk of infection should not be used in combo with anakinra or TNF blocking agents

Question 30

What is the mechanism of action of Rituximab?

Answer 30

monoclonal antibody directed against CD20 on B cells; kills b cells

Question 31

What are the adverse effects of Rituximab?

Answer 31

severe ocassionally fatal infusion related reactions have been reported usually with the first infusion; fatalities have been reported within 24 hrs of infusion Tumor lysis syndrome leading to acute renal failure requirng dialysis may occur in the 12-24 hour mark

Question 32

What is the mechanism of action of Tocilizumab?

Answer 32

humanized antibody; binds to soluble and membrane-bound IL-6 receptor and inhibits the IL6 mediated signaling.

Question 33

What are the adverse effects of Tocilizumab?

Answer 33

upper resp tracts infections, headache, HTN adn elevated liver enzymes serious infections including TB, fungal viral and other infections Neutropenia and reduction in platelet counts and lipids Gi perforation

Question 34

What is the mechanism of action of Tofacitinib?

Answer 34

janus kinase inhibitor;

Question 35

What ar ethe adverse effects of tofacitinib?

Answer 35

pts high risk of infection, tb and lymphoma GI perforations associate in combo ith other antiinflammatory increase blood cholesterol levels

Question 36

What are the therapeutic uses of tofacitinib?

Answer 36

tx of moderately to severe active rheumatorid arthritis

Question 37

What is the mechanism of action of anakinra?

Answer 37

antagonist of IL1 receptor

Question 38

What is the adverse effects associated with anakinra?

Answer 38

infection or injections ite reaction