2- DMARDs Flashcards
What is the MOA for gold salts?
Inhibit phagocytosis, prevent PG synthesis
What is the use for gold salts?
Supress cellular immunity
What are the SEs of gold salts?
BM damage, enterocolitis
What is the caution with use of Penicillamine?
HIGH incidence of SEs
(hematologic, renal, AI, ↑ risk > 65 yo)
What is the use for Penicillamine?
Wilson’s disease, RA
What type of properties does Hydroxychloroquine (Plaquenil) have?
Antihistaminic, anticholinesterase, antiprotease
(inhibits PG synthesis, stabilize lysosomes)
What are the SEs for Hydroxychloroquine (Plaquenil)?
Hemolysis (G6PD def), ototoxicity
What is the use for Sulfasalazine?
RA, better tolerated and less toxic
(but still not well tolerated)
What are general contraindications to use of DMARD agents?
Breastfeeding, children, renal disease +/- infections
What mediators of chronic inflammation are specifically identifed as DMARDs? (4)
Gold salts, Penicillamine, Hydroxychloroquine (Plaquenil), Sulfasalazine
What mediators of chronic inflammation are identifed as agents acting on TNF-alpha? (5)
Infliximab (Remicade)
Adalimumab (Humira)
Certolizumab Pegol (Cimiza)
Golimumab (Simponi)
Etanercept (Enbrel)
Which drug is a chimeric IgG1k monoclonal Ab targeting TNFa and is combined with Methotrexate?
Infliximab (Remicade)
What is the use for Infliximab (Remicade)?
(TNF-alpha agent)
RA, Crohn’s Disease
(given IV)
Which drug is a 100% HUMAN IgG1 monoclonal Ab targeting TNF-alpha?
Adalimumab (Humira)
(given subcutaneously)
What is the use for Adalimumab (Humira)?
RA (monotherapy)
Which drugs are humanized Abs targeting TNF-alpha?
Certolizumab Pegol (Cimiza)
Golimumab (Simponi)
What drug is considered a “fake TNFa receptor” and is a dimeric fusion protein?
Etanercept (Enbrel)
(given subcutaneously)
What are the contraindications to Etanercept (Enbrel)?
BM suppression, breastfeeding, children, DM, infection/ sepsis, live vaccines, current varicella infection
What are the SEs of Infliximab (Remicade)?
HA, infusion reactions
What are the SEs of Adalimumab (Humira)?
Rash, flu-like sxs, fatigue, HA
What is a SE of Etanercept (Enbrel) aside from injection site rxn and infections?
Increased incidence of antibody formation
What mediators of chronic inflammation are inhibitors of beta-cell differentiation and T-cell activation?
Rituximab
Abatacept
What mediators of chronic inflammation are inhibitors of nucleic acid synthesis?
Leflunomide
Micophenolate Mofetil
What mediators of chronic inflammation are interleukin receptor antagonists?
Anakinra
Tocilizumab
What mediators of chronic inflammation are JAK inhibitors?
Tofacitinib
Baricitinib
What drug is a genetically engineered chimeric antibody, specifically binds CD20 and is a B-lymphocyte differentiation antigen on B cells?
Rituximab (Rituxan)
(given IV)
What is the use for Rituximab (Rituxan)?
RA, relapsed/ refractory B-cell Non-Hodgkin Lymphoma (NHL)
What drug is a fully human recombinant fusion protein that blocks T cell activation to disturb key mechanisms of inflammation and progressive joint destruction?
Abatacept (Orencia)
(given IV, long half life)
What is the use for Abatacept (Orencia)?
RA
What drug inhibits DHODH and inhibits induction of COX-2?
Leflunomide (Arava)
(oral admin, long half life)
What are the SEs of Leflunomide (Arava)?
GI, immune suppression
What are the contraindications of Leflunomide (Arava)?
Pregnancy, breastfeeding, hepatic failure, renal failure
What drug inhibits lymphocyte purine synthesis and is a prodrug for the immunosuppressive agent MPA?
Mycophenolate Mofetil (Cellcept)
(given oral or IV)
Whare are the SEs of Mycophenolate Mofetil (Cellcept)?
Diarrhea, vomiting, GI bleeding
What are the contraindications to Mycophenolate Mofetil (Cellcept)?
Active GI disease, diarrhea, pregnancy, breast feeding, infections
What is the use for Mycophenolate Mofetil (Cellcept)?
RA, esp if resistant to Methotrexate
What drug is a human interleukin-1 receptor antagonist (IL-1Ra) and takes 4-13 weeks to have an effect?
Anakinra (Kineret)
(given subcutaneoulsy, eliminated renally)
What is the use for Anakinra (Kineret)?
RA- improve swollen/ painful joints
What drug is human interleukin-6 receptor antagonist (IL-6)?
Tocilizumab (Actemra)
What drug inhibits JAK1 and JAK 3 and is used in pts with mod-sev active RA who are intolerant to or have not had an adequate response to methotrexate?
Tofacitinib (Xeljanz)
(given orally)
What are the SEs of Tofacitinib (Xeljanz)?
Serious infections/ malignancy
What drug inhibits JAK1 and JAK2 and is used for the tx of mod-sev RA?
Baricitinib (Olumiant)
(mono or combo therapy)
What are the SEs of Baricitinib (Olumiant)?
Serious infection/ malignancy, thrombosis
