Ra Drugs

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Nonsteroidal Antiinflammatory Drugs (NSAIDs)
Salicylates

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Magnesium Salicylate (Magan; Mobidin)

• Salsalate (Disalcid; generic)

• Difunisal (Dolobid; generic)

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Newer NSAIDs

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Ibuprofen (Motrin; Advil; Nuprin; etc.)
Naproxen (Naprosyn; Aleve)
Ketoprofen (Orudis; Oruvail)
Meclofenamate (Meclomen; generic)
Piroxicam (Feldene; generic)
Indomethacin (Indocin; generic)
Sulindac (Clinoril; generic)
Nabumetone (Relafen)
Diclofenac (Voltaren; generic)
Celecoxib (Celebrex)

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Disease – Modifying Antirheumetic Drugs(DMARD)

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Hydrochloroquine (Plaquenil)

Gold Compounds
-Aurothiglucose (Solganal)
-Auranofin (Ridaura) – oral

Immunosuppressive Agents:
-Methotrexate (Rheumatrex)
-Leflunomide (Arava)

Sulfasalazine (Azulfidine, generic)

Tumor necrosis factor (TNF) inhibitors;
-Infliximab (Remicade)
-Etanercept (Enbrel)

Interleukin–1 (IL-1) receptor antagonist:
-Anakinra (Kineret)

Coticosteroids; e.g., Prendisone

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drawbacks to salicylates for initial therapy

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requires frequent dosing & GI side effects

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alternative salicylates that have less GI irritation but are more expensive

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Salsalate (Disalcid; generic)
Diflunisal (Dolobid)- BID

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No NSAID is consistently more EFFECTIVE than any other in large-scale trials. T/F

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T

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___________ is associated with a high incidence of diarrhea.

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Meclofenamate (Meclomen)

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This prostaglandin analog may decrease GI toxicity caused by NSAIDs

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misoprostol (Cytotec)

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This can result from chronic use of high doses of NSAIDs in individuals at risk, e.g., elderly patients and pts with renal impairment, CHF, or volume depletion.

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Renal toxicity

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MOA of NSAID associated renal toxicity

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changes in renal haemodynamics (bloodflow), ordinarily mediated by prostaglandins, which are affected by NSAIDs.

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Indomethacin (Indocin)

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uses: moderate to severe RA,OA, & ankylosing sponylitis &
SE: high incidence
GI side effects
CNS: headache, dizziness, confusion
ductus arteriosus

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Sulindac (Clinoril):

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related to indomethacin
lower incidence of AEs but lower efficacy
Prodrug
1/2 life -12 hrs

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piroxicam (Feldene)—

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very long half life -- 50 hrs
severe GI side effects 20%
avoid in elderly

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Nabumetone (Relafen)

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prodrug
long-acting
less GI irritation & ulceration

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Celecoxib (Celebrex)MOA

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inhibits COX-2 only
PGs produced by cox 1 available to protect GI mucosa

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Celecoxib (Celebrex) effects

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1) anti-inflammatory, analgesic, & antipyretic effects
2) does not inhibit platelet aggregation and causes fewer GI ulcers
3) may be pro-thrombotic: Rofecoxib was withdrawn from markit in 2004 due to increase CV complications

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Celecoxib (Celebrex)clinical uses

side effects it does not have that COX 1 & 2 inhibitors have

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RA, OA, primary dysmenorrhea, dental, surgical pain

low risk of GI side effects, no edema or renal toxicity

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DISEASE-MODIFYING ANTIRHEUMATIC DRUGS (DMARDs): “Slow-Acting Antirheumatic Drugs (SAARDs):
What is their advantange?

How long do they take to start working (generally)?

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modify progression of disease

take a long time to start working (weeks to months)

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Hydroxychloroquine (Plaquenil)

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Antimalarial Drug

Use:
mild RA unresponsive to NSAIDS

Toxicity: Visual disturbances (retinopathy; corneal deposits);epigastric pain; skin rash; etc

Monitor closely for visual
changes--EVERY 6-12 MONTH

HEMOLYSIS IN PTS WITH G-6-PD DEFICIENCY

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Aurothioglucose (Solganal)

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Gold Compound
IM
Clinical uses: mild to moderate RA
May take 3-6 months to start working

Most common toxic effects:
• Pruritus, erythema, skin rash; stomatitis, glossitis--IM
• Exfoliative dermatitis – rare

b. Blood dyscrasias: Rare, but serious; can be lethal: thrombocytopenia, leukopenia, aplastic anemia
c. Proteinuria; metallic taste, skin pigmentation, enterocolitis.
CAUTION: monitor urine (UA) & blood (CBC)

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Auranofin (Ridaura)

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Gold Compound
oral-less effective, less AEs
Clinical uses: mild to moderate RA
May take 3-6 months to start working


•Diarrhea*
• Exfoliative dermatitis – rare

b. Blood dyscrasias: Rare, but serious; can be lethal: thrombocytopenia, leukopenia, aplastic anemia
c. Proteinuria; metallic taste, skin pigmentation, enterocolitis.
CAUTION: monitor urine (UA) & blood (CBC)

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Methotrexate (Rheumatrex)
what type of drug is it

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Immunosuppressive Agent(“Cytotoxic”)

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Methotrexate (Rheumatrex)
MOA

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MOA:Dihydrofolate reductase
inhibitor; FOLATE ANTAGONIST

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Methotrexate (Rheumatrex)
Clinical uses:

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Clinical uses: DOC for moderate to severe RA
-very effective
-well tolerated
-GI side effects

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Methotrexate (Rheumatrex)
AEs

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bone marrow depression (neutropenia, thrombocytopenia, anemia)

GI disturbances

Infection (due to decreased immune reactivity)

increased risk of teratogenesis

increased risk of malignancies

stomatitis, megaloblastic anemia, hepatitis/cirrhosis, pneumonitis

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Methotrexate (Rheumatrex)Contraindications

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•Pregnancy; children--Teratogenic

• Alcoholism; liver disease

• Blood dyscrasias

• Renal insufficiency/elderly

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Cyclosporine (Sandimmune)
category?
alone or used with?

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An immunosuppressant used in some patients with refactory RA. Used alone or with methotrexate.

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Cyclosporine (Sandimmune)
MOA

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Selectively supresses T-cell proliferation (B-cells also affected)

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Cyclosporine (Sandimmune)
AEs

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nephrotoxicity, hepatotoxicity
hypertension
hyperkalemia
drug interactions

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Leflunomide (Arava)
MOA

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A prodrug

inhibits dihydroorate dehydrogenase and DNA synthesis
Has antiproliferative effect on T-cell
anti-inflammatory effect.

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Leflunomide (Arava)
Uses

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for moderate to severe RA
alternative to methotrexate
PO, QD

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Leflunomide (Arava)
AEs

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COMMON:
diarrhea
elevation of liver enzymes

alopecia (reversable)
rash
anaphylaxis
teratogenic in animals

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Sulfasalazine (Azulfidine; generic)
Uses

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ulcerative colitis
mild to moderate RA

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Sulfasalazine (Azulfidine; generic)
MOA:

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Converts to sulfapyridine and 5-acetyl salicylate.

Sulfapyridine supresses lymphocyte and PMN function (helps with RA)
5-ASA --ANTIINFLAMMATORY

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Sulfasalazine (Azulfidine; generic)
Adverse reactions:

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Nausea, anorexia, dizziness;
skin rash.
Blood dyscrasias and hepatitis – rare.

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Infliximab (Remicade)

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Tumor necrosis factor (TNF) inhibitor

a chimeric human/mouse anti-TNF monoclonal antibody; IV

also used in crohns dz

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Etanercept (Enbrel)

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Tumor necrosis factor (TNF) inhibitor

a recombinant human TNF receptor; SC

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MOA of tumor necrosis factor inhibitors

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Binds to and blocks TNF, a cytokine and inhibits inflammation.

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Clinical Uses of tumor necrosis factor inhibitors

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RA refractive to methotrexate
can be used alone or w/ methotrexate
better than mtx in preventing jt distruction

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infliximab
Adverse reactions

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Headache, infection, infusion reaction (fever, urticaria, dyspenea, and hypotension)

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etanercept
Adverse reactions

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Erythema, local pain and itching at injection site

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Anakinra (Kineret)
type and MOA

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Interleukin-1 (IL-1) receptor antagonist:

Competitively block IL-1 R which decreases INFLAMMATION & JOINT DESTRUCTION

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Anakinra (Kineret)
Uses & route:

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Severe RA - - daily SC injection

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Anakinra (Kineret)
AEs

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Pruritus, rash, erythema and pain at injection site

• Neutropenia; severe infection – ↑ with etanercept (Enbrel).

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prednisone
MOA

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A CORTICOSTEROID

Anti-inflammatory action mediated by several possible mechanisms, including inhibition of phospholipase A2,selective inhibitition of COX immunosuppressive effects.???

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prednisone
uses in RA

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1) Adjunctive therapy (5-10
mg prednisone) for severe, rapidly progressing disease that does not respond or intolerant other DMARDs.

2) Low-dose prednisone may be especially useful in pregnant, elderly and younger pts to control active disease temporarily.

3) High-dose corticososteroids may be required to control severe, life- threatening situations– PERICARDITIS, VASCULITIS

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Prednisone
Intra-articular injections
what are the injectable forms and when should you use them?

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Use long-acting,microcrystal suspensions:

prednisolone tebutate (generic)
triamcinolone (generic; Kenalong; Aristocort)


Accepted adjunctive therapy when painful symptoms are confined to only one or two joints.

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prednisone
Adverse Reactions:

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Numerous and potentially serious, especially at high doses systemically and with chronic use.

Osteoporosis, poor wound healing, gastric ulcer, hypertension.

• Adrenal suppression, increased risk of infection, etc.