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Pathology and MuscSkel > Gout and RA drugs > Flashcards

Gout and RA drugs Flashcards

1
Q

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

A

Indomethacin; NSAIDs for first 24 hours

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2
Q

What is the mechanism of colchicine?

A

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

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3
Q

What is the metabolism of colchicine accomplished by?

A

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

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4
Q

Who is colchicine contraindicated in?

A

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

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5
Q

What is colchicine used to treat?

A

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

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6
Q

What is the mechanism of action of allopurinol?

A

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

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7
Q

What is the pharmokinetics of allopurinol?

A

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

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8
Q

What is the adverse effects of allopurinol?

A

generally well tolerated

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

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9
Q

What is a therapeutic use of allopurinol?

A

effective tx for primary and secondary gout

goal of tx is to reduce the plasmic uric acid concentration

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10
Q

What is the mechanism of action of febuxostat?

A

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

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11
Q

What is the pharmokinetics of febuxostat?

A

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

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12
Q

What are the adverse effects/contraindications?

A

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

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13
Q

What is the mechanism of action of pegloticase?

A

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

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14
Q

What is the pharmokinetics of pegloticase?

A

IV admin

serum half life from 6-14 days

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15
Q

What does pegloticase treat?

A

refactory gout

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16
Q

What is the mechanism of action of probenecid?

A

inhibition of organic acid transport in renal tubule

17
Q

What is adverse effects of probenecid?

A

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

18
Q

What is probenecid used to treat?

A

hyperuricemia associated with gout or gouty arthritis

19
Q

What are some effects of probenecid with diuretics?

A

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

20
Q

What is the mechanism of action of Etanercept?

A

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

21
Q

What are the adverse effects of Etanercept?

A

serious and potentially fatal infections

lymphoma and other malignancies in adolescents and children

22
Q

What is the mechanism of action of adalimumab?

A

chimeric IgG monoclonal antibody binds to both forms of TNFalpha

23
Q

Wat are the adverse effects of adalimumab?

A

injection site from subQ

infection and upper respiratory tract

24
Q

What are the therapeutic uses of adalimumab?

A

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

25
Q

What is the mechanism of action of infliximab?

A

a chimeric IgG antibody binds to both forms of TNFalpha

26
Q

What are hte adverse effects of infliximab?

A

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

27
Q

What are the therapeutic uses of infliximab?

A

moderate to severely active rheumatoid arthiritis

28
Q

What is the mechanism of action of abatacept?

A

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

29
Q

What are the adverse effects associated with abatacept?

A

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

30
Q

What is the mechanism of action of Rituximab?

A

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

31
Q

What are the adverse effects of Rituximab?

A

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

32
Q

What is the mechanism of action of Tocilizumab?

A

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

33
Q

What are the adverse effects of Tocilizumab?

A

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

34
Q

What is the mechanism of action of Tofacitinib?

A

janus kinase inhibitor;

35
Q

What ar ethe adverse effects of tofacitinib?

A

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

36
Q

What are the therapeutic uses of tofacitinib?

A

tx of moderately to severe active rheumatorid arthritis

37
Q

What is the mechanism of action of anakinra?

A

antagonist of IL1 receptor

38
Q

What is the adverse effects associated with anakinra?

A

infection or injections ite reaction

Pathology and MuscSkel (15 decks)

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