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
Leflunomide- Absorption, Distribution
1-2 months
27
Leflunomide- Clinical Use
alternative to Methotrexate for moderate/severe RA low cost oral alternative for TNF inhibitors
28
Leflunomide- Adverse Effects/Contraindications
CONTRAINDICATED IN PREGNANCY AND BREASTFEEDING AND LIVER DISEASE hypertension especially if used with NSAIDS diarrhea, nausea, rash, hepatotoxicity
29
Uncommon DMARDS- Available Drugs
``` Azathioprine D-penicillamine Gold salts Cyclosporin A Cyclophosphamide ```
30
Uncommon DMARDS- Clinical Use
RESERVED FOR REFRACTORY RA OR LIFE THREATENING SYMPTOMS SUCH AS VASCULITIS
31
Uncommon DMARDS- Adverse Effects/Contraindications
SIGNIFICANT TOXICITIES
32
Eternercept, Infliximab, Adalimumab- Mech of Action
Antibody-like structure that binds and interferes with TNF-a
33
Eternercept, Infliximab, Adalimumab- Absorption, Distribution
Sub-Q, IV | 1-4wks
34
Eternercept, Infliximab, Adalimumab- Clinical Use
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
Eternercept, Infliximab, Adalimumab- Adverse Effects/Contraindications
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
Abatacept- Mech of Action
T-cell inhibitor | Block CD80/86 on APC, blocking CD 28 co-stimulatory signal necessary for T-cell activation
37
Abatacept- Clinical Use
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
Abatacept- Adverse Effects/Contraindications
INCREASED RISK OF SERIOUS INFECTION, LATENT INFECTIONS (TB, HBV)
39
Abatacept- Drug Rxns
Do not give in combination with TNF-a inhibitor= shuts down the immune system
40
Rituximab- Mech of Action
B-cell inhibitor Binds CD20 on B cells Decreases antigen presentation to T-cells, decrease formation of autoantibodies
41
Rituximab- Clinical Use
reduce progression of RA, decrease signs and symptoms Effective in pts non-responsive to TNF-a inhibitors Screen for latent TB and HBV
42
Rituximab- Adverse Effects/Contraindications
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
Anakinra- Mech of Action
IL-1 receptor antagonist
44
Anakinra- Absorption, Distribution
Sub-Q
45
Anakinra- Elimination
Shorter half-life given daily
46
Anakinra- Clinical Use
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
Anakinra- Adverse Effects/Contraindications
SERIOUS INFECTION | neutropenia
48
Anakinra- Drug Rxns
more serious complications when given with TNF-a agents
49
Tocilizumab- Mech of Action
IL-6 receptor antagonist
50
Tocilizumab- Clinical Use
RA patients non-responsive to TNF-a inhibitors or used in combo w/ Methotrexate screen for latent TB and HBV
51
Tocilizumab- Adverse Effects/Contraindication
``` 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
Tocilizumab- Drug Rxns
do not combine with other BRMs/Biologics
53
Tofacitinib- Mech of Action
JAK tyrosine kinase inhibitor | blocks immune cell cytokine signaling
54
Tofacitinib- Clinical Use
RA Screen for latent TB and HBV
55
Tofacitinib- Adverse Effects/Contraindications
``` 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
Colchicine- Mech of Action
block leukocyte migration and phagocytosis can be used in prophylaxis with other anti-gout drugs
57
Colchicine- Clinical Use
Gout Anti-inflammatory NO ANALGESIA
58
Colchicine- Adverse Effects/Contraindications
diarrhea, nausea, vomiting
59
Probenecid- Mech of Action
Inhibits anion transporter in renal proximal tubule= decreased uric acid reabsorption= increased excretion
60
Probenecid- Clinical Use
gout in patients that undersecrete uric acid
61
Probenecid- Adverse Effects/Contraindications
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
Allopurinol, Febuxostat- Mech of Action
Inhibit Xanthine Oxidase= prevents production of uric acid
63
Allopurinol, Febuxostat- Clinical Use
Gout in patients that overproduce uric acid Uric acid kidney stones Tophi gout in renal insufficiency
64
Allopurinol, Febuxostat- Adverse Effects/Contraindications
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
Allopurinol, Febuxostat- Drug Rxns
6-mercaptopurine and azathioprine (purine synthesis inhbitors) Levels are increased- toxicity
66
Pegloticase- Mech of Action
Porcine uricase= degrades uric acid
67
Pegloticase- Absorption, Distribution
IV INFUSION EVERY 2 WKS
68
Pegloticase- Clinical Use
Gout in frequent flares, topi, when other medications are contraindicated
69
Pegloticase- Adverse Effects/Contraindications
Infusion rxn increase in cardiovascular events generation of anti-drug antibodies REQUIRES NSAID/COLCHICINE PROPHYLAXIS