Immune suppressing drugs Flashcards
TNF alpha
Tumor necrosis factor-alpha is a cytokine which mediates immune response by increasing the transport of white blood cells to sites of inflammation and through additional molecular mechanisms which initiate and amplify inflammation
Etanercept/ Enbrel
TNF alpha blocker
Class: DMARD, recombinant-DNA drug
• Indication: Moderate to severe rheumatoid
arthritis, moderate to severe polyarticular juvenile arthritis, psoriatic arthritis, ankylosing spondylitis and moderate to severe plaque psoriasis.
• MOA: Reduction of inflammatory response via anti-TNF alpha therapy.
• Char: SQ, dosed once or twice weekly. Supplied in powder or pre-mixed solution. injected subcutaneously, typically by the patient at home.
Etanercept/ Enbrel SE
- Side effects: Very broad side effect profile with notable decreased resistance to infection. Increasing number of reports of potential for increased risk for leukemia, lymphoma and solid tumors, as well as increasing number of reports of serious liver injury, congestive heart failure and demyelinating central nervous system disorders.
- Cost: $12,000 to 16,000+ per year
Infliximab/ Remicade

• Class: DMARD, recombinant-DNA drug • Indication: RA, Crohn’s disease, U.C. • MOA: According to product labeling, Infliximab neutralizes the biological activity of TNFα by binding with high affinity to the soluble (free floating in the blood) TNFα and the trans-membrane (located on the outer membranes of T cells and similar immune cells) forms of TNFα, thus preventing the effective binding of TNFα with its receptors. **Anti-TNF antibody! along with humira
Char: Infliximab is administered by intravenous infusion, typically at 6-8 week intervals. It cannot be administered orally, because the digestive system would destroy the drug.
infliximab treats:
psoriasis, Crohn’s disease, ankylosing spondylitis, psoriatic arthritis, rheumatoid arthritis and ulcerative colitis.
“mab” suffix =antibody, recombinant
Infliximab/ Remicade vs Etanercept/Enbrel MOA
- Infliximab causes programmed cell death of TNFα expressing activated T cells but Enbrel does not have this activity.
- It is generally assumed that the effect on activated T cells by Infliximab explains its efficacy in Crohn’s disease and U.C. whereas Etanercept has shown no efficacy in treating inflammatory bowel disease.
Hydroxychloroquine/ Plaquenil uses
- Hydroxychloroquine is a drug that was discussed in our review of anti-malarial agent.
- Hydroxychloroquine is also useful in treating rheumatoid arthritis, systemic lupus erythematosus and Sjögren’s Syndrome.
- Hydroxychloroquine is also widely used in the treatment of post-Lyme arthritis that can be induced by Lyme disease.
Hydroxychloroquine/ Plaqueni MO
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• While Hydroxychloroquine has been known for some time to increase lysosomal pH in antigen presenting cells, its mechanism of action in inflammatory conditions has been clarified further.
• It is now known that Hydroxychloroquine blocks the activation of toll-like receptors on plasmacytoid dendritic cells (PDCs).
• Toll-like receptor 9 (TLR 9), which recognizes DNA-containing immune complexes, leads to the production of interferon and causes the dendritic cells to mature and present antigen to T cells.
• By decreasing TLR 9 signaling, Hydroxy- chloroquine reduces the activation of dendritic cells which acts to limit the inflammatory process.

Hydroxychloroquine/ Plaquenil class/char/indications
• Class: Immunosuppressant and anti- malarial.
• Indication: RA, SLE, and Sjögren’s Syndrome as well as malaria in area of the world ion which there is low risk for hydroxychloroquine resistant malaria.
• MOA: As noted. The action of the drug may involve an anti-spirochete activity as well as an anti-inflammatory activity.
char: oral
Hydroxychloroquine/ Plaquenil and eyes
need to do frequent dilated eye exams! corneas can become opaque.
Because of the possibility of corneal and macular damage, yearly dilated eye exams are indicated for all patients on chronic therapy even when they have no vision or ocular symptoms.
Hydroxychloroquine/ Plaquenil sx of overdose
Symptoms of overdose can occur within a half-hour of taking the medication. Overdose symptoms include drowsiness, headache, vision problems, shortness of breath, and convulsions.
Children are more sensitive to hydroxychloroquine than adults are, and small doses can be potentially fatal.
Hydroxychloroquine/ Plaquenil SE
- Side effects: ** GI** and retina***Abdominal cramps, diarrhea, reduced appetite, headache, nausea and vomiting, vision difficulties, tinnitus, hearing loss diminished reflexes, hives, itching, rash, loss of hair, weakness and anemia.
- **Patients with G6PD enzyme deficiency who take Hydroxychloroquine can develop a severe anemia and should be closely monitored if the drug is not stopped.Lysis of RBCs.
Gold salts
• Gold salt compounds act to reduce inflammation, especially related to RA, inflammatory bowel disease, psoriatic arthritis, membranous nephritis, lupus erythematosus and infrequently, juvenile rheumatoid arthritis.
• Gold salts are sometimes used for children with progressive poly-arthritis who are unresponsive to NSAIDs, Methotrexate, and other medications such as DMARDs.

Gold Salts MOA
MOA: The mechanism by which gold drugs operate to treat arthritis is a matter of scientific debate.
• Of the various mechanisms that have been suggested, gold is proposed as having anti-mitochondrial activity as well as potentially inducing cell apoptosis.

Gold salts char
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• Gold drugs can be administered orally or by intramuscular injection, in which case it is administered weekly for ~three to five months before less-frequent doses begin.
• Auranofin (Ridaura) is the capsule form for oral administration that is marketed in the US.
• Orally administered gold has fewer side effects than intramuscular injections.
