Anti Rheumatic Drugs

Question 1

Gold Salts

Answer 1

1. Anti rheumatic- DMARD
2. Inhibit the immune system (various aspects)
3. Toxicity: bone marrow suppression, dermatitis, jaundice, peripheral neuropathy

Question 2

Penicillamine

Answer 2

1. Anti rheumatic- DMARD
3. Toxicity:
   - pruritis, rash, alteration in taste
   - thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia
   - lupus like disease, Good pastures syndrome, myasthenia gravis, polymyotisi
   - pts. over 65 have a high risk

Question 3

Hydroxychloroquine

Answer 3

1. Anti rheumatic, DMARD
2. Inhibits various aspects of the immune system
3. Toxicity:
   - pruritis, hemolysis (G6PD deficiey), ototoxicity, retinopathy, peripheral neuropathy

Question 4

Sulfasalazine

Answer 4

1. Anti Rheumatic, DMARD
3. Toxicities:
   - GI disturbances, rash, hepatitis, blood dyscrasia, monitor blood and hepatic function for first 3 months

Question 5

Infliximab

Answer 5

1. Antirheumatic, and for crohns disease, TNFa
2. MAB with human constant region and murine variable region- antibody that targets TNFa, substantially improves clinical symptoms
   - administered IV, predominately distributed within the vascular compartment, long half life
3. Toxicities
   a) infusion
   b) systemic- inc infections, inc cancer, headache nausea back pain, depression, etc.
   c) hypersensitivity rxns to murine component
5. CI in pregnancy, breast feeding, infections, children

Question 6

Adalimumab

Answer 6

1. anti rheumatic, monotherapy for RA
2. MAB, IgG, fully human, specific for TNFa, SQ administration, half life 8-10 days
3. Toxicities
   a) rash- infusion rxn
   b) infections- systemic, fatigue, headach, pruritis, nausea and vomiting

Question 7

Certrolizumab

Answer 7

1. Anti-Rheumatic, potent neutralized of TNFa
2. Toxicity: adverse effects are similar to those of other TNFa binders
   - humanized

Question 8

Golimumab

Answer 8

1. Anti-Rheumatic, TNFa binder
2. human derived monoclonal antibody with constant regions TNF
   - human derived

Question 9

Etanercept

Answer 9

1. Anti rheumatic, TNF
2. Not a monoclonal antibody, it is a protein with a ligand for TNF and a Fc portion of the human IgG, it will bind to and inactivate TNFa but it does not affect TNF production or serum levels, human and murine components - hypersensitivity
   - administered SQ
3. Toxicities
   a) injection site reaction
   b) infections
   c) inc. incidence of antibody formation
4. CI: bone marrow suppression, breast feeding, children, infections, DM, sepsis, vaccinations, varicella

Question 10

Rituximab

Answer 10

1. Anti rheumatic, inhibitor of B and T cells activation
2. Genetically engineered monoclonal antibody- Human constant and murine variable, specifically binds CD20 (on pre B cells, and mature B lymphocytes)
3. Toxicities
   a) infusion related reactions
   b) hypersensitivity rxns, fever, chilles, rigors, nausea, vomiting, asthenia, pruritis, etc. angioedema
4. CI in abciximad hypersensitivity, murine protein hypersensitivity

Question 11

Abetacept

Answer 11

1. Anti rheumatic
2. Fully human, blocks T cell activation (key mechanism in inflammatory response and joint destruction), IV administration, 13 day half life
3. affects host defenses against infections and malignancies

Question 12

Leflunomide

Answer 12

1. Anti rheumatic, inhibits nucleic acid synthesis
2. inhibits DHODH enzyme for de novo pyrimidine synthesis, secondary action is inhibition of cytokine and GF receptor associated with TK acticity, inhibits COX-2
   - oral administration, 16 hours half life
3. Toxicity
   - diarrhea, dyspepsia, nausea, vomiting, abdominal pain, back pain, weight loss, anorexia, oral ulceration, and elevated hepatic enzymes
   CI in pregnacy, breast feeding, hepatic, and renal failure

Question 13

Mycophenolate Mofetil (cellcept)

Answer 13

1. Anti rheumatic, inhibits nucleic acid synthesis
2. inhibits de novo lymphocyte purine synthesis , and non competitively inhibits the IMPDH enzyme, oral administration then metabolized into free form MPA- (active component), conjugated in the liver to form inactive glucoronide
3. Toxicity
   - diarrhea, vomiting, nausea, inc plasma concentration in pts with renal insufficiency
   4 . CI in pts with active GI disease, pregnancy, breast feeding, and infections
4. useful in pts with RA that are resistant to methotrexate

Question 14

Anakinra

Answer 14

1. Anti RA, interleukin receptor antagonist
2. recombinant non glycoslyated for of human IL-1 receptor antagonist (IL-1Ra), sq administration
4. improves swollen joints and reduces pain

Question 15

Tocilizumab

Answer 15

1. Anti RA

2. Humanized IL-6 receptor inhibitor MAB (competes with IL-6 for binding)

Question 16

Tofacitinib

Answer 16

1. Anti RA, JAKs inhibitor
   2, primarily inhibits JAK1 and JAK3, and to a less extent JAX2
2. Toxicities
   - serious infections and malignancies are precipitates
3. For adults with moderate to severe active RA who cannot tolerate Methotrexate or do no respond to it