RA and Gout Drugs Flashcards

1
Q

Tylenol- Clinical Use

A

Pain relief in OA or RA

no anti-inflammatory effects

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2
Q

Capsaicin- Mech of Action

A

Deplete substance P

topical

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3
Q

Capsaicin- Clinical Use

A

Pain relief in OA or RA

no anti-inflammatory effects

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4
Q

NSAIDS- Available Drugs

A

Aspirin
Ibuprofen
Naproxen
Indomethacin

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5
Q

NSAIDS- Clinical Use

A

Pain relief in OA
DOC for initial reduction of inflammation and relief of pain in RA
Pain relief in gout

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6
Q

NSAIDS- Adverse Effects/Contraindications

A

Do not use aspirin or salicylates in gout- may exascerbate the symptoms

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7
Q

Glucocorticoids (Dexamethasone)- Absorption, Distribution

A

injectable directly into joint, PO, IV

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8
Q

Glucocorticoids (Dexamethasone)- Clinical Use

A

OA alternative for patients unresponsive to acetaminophen and NSAIDs

decrease joint pain and tenderness, and increase grip strength in RA

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9
Q

Glucocorticoids (Dexamethasone)- Adverse Effects/Contraindications

A

Chronic Use- weight gain, HTN, osteoporosis, diabetes, increased risk of infection, and suppression of the HPA axis

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10
Q

DMARDS (Disease Modifiying Anti-Rheumatic Drugs)- Available Drugs

A

Hydroxychloroquine
Sulfasalzine
Methotrexate
Leflunomide

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11
Q

Hydroxycholoroquine- Mech of Action

A

inhibit TLR signaling in dendritic/B cells
inhibit antigen presentation to T cells

often combined with other DMARDS

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12
Q

Hydroxycholoroquine- Absorption, Distribution

A

3-6 months to be effective

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13
Q

Hydroxycholoroquine- Clinical Use

A

MILD RA

Malaria

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14
Q

Hydroxycholoroquine- Adverse Effects/Contraindications

A

RARE OCCULAR TOXICITY

SAFE DURING PREGNANCY AND LACTATION

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15
Q

Sulfasalazine- Mech of Action

A

unclear, may involve T and B cell interference

prodrug
often combined w/ other DMARDS (hydroxycholoraquine)

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16
Q

Sulfasalazine- Absorption, Distribution

A

1-3 months

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17
Q

Sulfasalazine- Clinical Use

A

MILD RA

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18
Q

Sulfasalazine- Adverse Effects/Contraindications

A

SAFE DURING PREGNANCY
agranulocytosis (very rare)
hepatotoxicity (reversible)

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19
Q

Methotrexate- Mech of Action

A

increase adenosine- downregulate immune rxns (different MOA in chemotherapy)

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20
Q

Methotrexate- Absorption, Distribution

A

Used at 100-1000x lower doses when used for RA than when used for chemo
4-6wks

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22
Q

Methotrexate- Elimination

A

Renal excretion

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23
Q

Methotrexate- Clinical Use

A

DOC FOR ACTIVE MODERATE/SEVERE RA

chemotherapy

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24
Q

Methotrexate- Adverse Effects/Contraindications

A

CONTRAINDICATED IN PREGNANCY AND BREASTFEEDING
hepatotoxicity (abstain from EtOH)
pulmonary toxicity, bone marrow suppression, increased risk of lymphoma, not recommended in liver or renal disease

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25
Q

Leflunomide- Mech of Action

A

inhibit dihydroorotate dehydrogenase which is resonsible for Uridine synthesis–> G1 cycle arrest–> inhibit T cell proliferation and B cell autoantibody production

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26
Q

Leflunomide- Absorption, Distribution

A

1-2 months

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27
Q

Leflunomide- Clinical Use

A

alternative to Methotrexate for moderate/severe RA

low cost oral alternative for TNF inhibitors

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28
Q

Leflunomide- Adverse Effects/Contraindications

A

CONTRAINDICATED IN PREGNANCY AND BREASTFEEDING AND LIVER DISEASE
hypertension especially if used with NSAIDS
diarrhea, nausea, rash, hepatotoxicity

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29
Q

Uncommon DMARDS- Available Drugs

A
Azathioprine
D-penicillamine
Gold salts
Cyclosporin A
Cyclophosphamide
30
Q

Uncommon DMARDS- Clinical Use

A

RESERVED FOR REFRACTORY RA OR LIFE THREATENING SYMPTOMS SUCH AS VASCULITIS

31
Q

Uncommon DMARDS- Adverse Effects/Contraindications

A

SIGNIFICANT TOXICITIES

32
Q

Eternercept, Infliximab, Adalimumab- Mech of Action

A

Antibody-like structure that binds and interferes with TNF-a

33
Q

Eternercept, Infliximab, Adalimumab- Absorption, Distribution

A

Sub-Q, IV

1-4wks

34
Q

Eternercept, Infliximab, Adalimumab- Clinical Use

A

reduce joint pain and swelling
decrease formation of new bone erosions
slow the progression of structural joint damage in RA

USED AS MONOTHERAPY OR IN COMBO WITH METHOTREXATE FOR ACTIVE RA
screen for latent TB and HBV

35
Q

Eternercept, Infliximab, Adalimumab- Adverse Effects/Contraindications

A

INCREASED RISK OF INFECTION (FUNGAL AND BACTERIAL)

REACTIVATION OF LATENT TB OR VIRUSES (HBV)

CHF EXACERBATION
DEMYELINATINGNDISEASE (MS)
MALIGNANCIES (LYMPHOMA)

CONTRAINDICATED IN PTS WITH ACUTE OR CHRONIC INFECTIONS, CHF, MS, HX OF CANCER

36
Q

Abatacept- Mech of Action

A

T-cell inhibitor

Block CD80/86 on APC, blocking CD 28 co-stimulatory signal necessary for T-cell activation

37
Q

Abatacept- Clinical Use

A

Slows damage to bone and cartilage, relieve symptoms of RA

Effective in pts non-responsive to TNF-a inhibitors
Screen for latent TB and HBV

38
Q

Abatacept- Adverse Effects/Contraindications

A

INCREASED RISK OF SERIOUS INFECTION, LATENT INFECTIONS (TB, HBV)

39
Q

Abatacept- Drug Rxns

A

Do not give in combination with TNF-a inhibitor= shuts down the immune system

40
Q

Rituximab- Mech of Action

A

B-cell inhibitor
Binds CD20 on B cells
Decreases antigen presentation to T-cells, decrease formation of autoantibodies

41
Q

Rituximab- Clinical Use

A

reduce progression of RA, decrease signs and symptoms

Effective in pts non-responsive to TNF-a inhibitors
Screen for latent TB and HBV

42
Q

Rituximab- Adverse Effects/Contraindications

A

INCREASE RISK OF SERIOUS INFECTION, LATENT INFECTIONS (TB, HBV)

RARE PROGRESSIVE MULTIFOCAL LEUKOENCEPHALOPATHY (PML)= a rare demylinating disease associated with reactivation of JC virus

43
Q

Anakinra- Mech of Action

A

IL-1 receptor antagonist

44
Q

Anakinra- Absorption, Distribution

A

Sub-Q

45
Q

Anakinra- Elimination

A

Shorter half-life given daily

46
Q

Anakinra- Clinical Use

A

RA patients non-responsive to TNF-a inhibitors or used in combo w/ Methotrexate

Less effective than TNF-a agents
Screen for latent TB and HBV

47
Q

Anakinra- Adverse Effects/Contraindications

A

SERIOUS INFECTION

neutropenia

48
Q

Anakinra- Drug Rxns

A

more serious complications when given with TNF-a agents

49
Q

Tocilizumab- Mech of Action

A

IL-6 receptor antagonist

50
Q

Tocilizumab- Clinical Use

A

RA patients non-responsive to TNF-a inhibitors or used in combo w/ Methotrexate

screen for latent TB and HBV

51
Q

Tocilizumab- Adverse Effects/Contraindication

A
BONE MARROW SUPPRESSION
SERIOUS INFECTION
HEPATOTOXICITY
INCREASED CHOLESTEROL LEVELS
increased risk of malignancy

Contraindicated in acute/chronic infection, liver disease, low blood counts, immunosuppressed

52
Q

Tocilizumab- Drug Rxns

A

do not combine with other BRMs/Biologics

53
Q

Tofacitinib- Mech of Action

A

JAK tyrosine kinase inhibitor

blocks immune cell cytokine signaling

54
Q

Tofacitinib- Clinical Use

A

RA

Screen for latent TB and HBV

55
Q

Tofacitinib- Adverse Effects/Contraindications

A
BONE MARROW SUPPRESSION
SERIOUS INFECTION
HEPATOTOXICITY
INCREASED CHOLESTEROL LEVELS
increased risk of malignancy

Contraindicated in acute/chronic infection, liver disease, low blood counts, immunosuppressed

56
Q

Colchicine- Mech of Action

A

block leukocyte migration and phagocytosis

can be used in prophylaxis with other anti-gout drugs

57
Q

Colchicine- Clinical Use

A

Gout
Anti-inflammatory
NO ANALGESIA

58
Q

Colchicine- Adverse Effects/Contraindications

A

diarrhea, nausea, vomiting

59
Q

Probenecid- Mech of Action

A

Inhibits anion transporter in renal proximal tubule= decreased uric acid reabsorption= increased excretion

60
Q

Probenecid- Clinical Use

A

gout in patients that undersecrete uric acid

61
Q

Probenecid- Adverse Effects/Contraindications

A

Contraindicated during acute attack- can make worse or prolong

Contraindicated in patients that overproduce uric acid= PRECIPITATE KIDNEY STONES

Contraindicated in renal insufficiency or kidney stones

62
Q

Allopurinol, Febuxostat- Mech of Action

A

Inhibit Xanthine Oxidase= prevents production of uric acid

63
Q

Allopurinol, Febuxostat- Clinical Use

A

Gout in patients that overproduce uric acid

Uric acid kidney stones
Tophi
gout in renal insufficiency

64
Q

Allopurinol, Febuxostat- Adverse Effects/Contraindications

A

Allopurinol hypersensitivity syndrome (life threatening; most likely in high doses with pre-existing renal failure)
Can induce acute attack if NSAID prophylaxis not provided
Rash, leukopenia, thrombocytopenia, fever, elevated liver enzymes

65
Q

Allopurinol, Febuxostat- Drug Rxns

A

6-mercaptopurine and azathioprine (purine synthesis inhbitors)
Levels are increased- toxicity

66
Q

Pegloticase- Mech of Action

A

Porcine uricase= degrades uric acid

67
Q

Pegloticase- Absorption, Distribution

A

IV INFUSION EVERY 2 WKS

68
Q

Pegloticase- Clinical Use

A

Gout in frequent flares, topi, when other medications are contraindicated

69
Q

Pegloticase- Adverse Effects/Contraindications

A

Infusion rxn
increase in cardiovascular events
generation of anti-drug antibodies

REQUIRES NSAID/COLCHICINE PROPHYLAXIS