DMARDs (Lauren🌭) Flashcards
Are DMARDs analgesics?
No
Do DMARDs have any immediate effects?
No. Used to slow the progression of the disease.
What is the main effect of Gold Salts?
Suppress cellular immunity
What are the main toxicities of Gold Salts?
Bone marrow damage
Enterocolitis
PRETTY TOXIC
NOT USED MUCH
What kind of drug is Penicillamine (Cuprimine)
A chelating drug that works for RA and Wilson’s disease
What are the toxicities of Penicillamine (Cuprimine)
It fucks up everything
What are the main toxicities of Hydroxychloroquine (Plaquenil)?
Hemolysis (G6PD deficient)
Ototoxicity
Retinopathy
Peripheral neuropathy
Pruritus
Methemoglobinemia
Sulfasalazine (Azulfidine) is a prodrug that is metabolized into _________ and ________
Sulfonamide
Salicylate
The adverse effects of sulfasalazine are related to it being metabolized into (sulfonamide/salicylate/both)
Both
What DMARDs act on TNFα?
Infliximab (Remicade) 👩🏻🦲🐁
Adalimumab (Humira)👩🏻🦲
Cetrolizumab (Cimiza)
Golimumab (Simponi)
Etanercept (Enbrel)
What are the old school DMARDs that aren’t used much
Gold Salts
Penicillamine (Cuprimine)
Hydroxychloroquine (Plaquenil)
Sulfasalazine (Azulfidine)
Every drug in this lecture has pretty much the same set of adverse effects since they all inhibit some part of the immune system.
What are those side effects?
Basically anything that comes along with a decreased immune system:
Increased risk of infection
TB
Valley fever
Development of cancer
Etc
Infliximab (Remicade) and Adalimumab (Humira) are both what kind of drugs?
Monoclonal antibodies against TNFα
Infliximab (Remicade) and Adalimumab (Humira) are both monoclonal antibodies against TNFα. What is the main difference between them?
Infliximab (Remicade) is chimeric. (Mix of human and murine regions) 👩🏻🦲🐁
Adalimumab (Humira) is fully human 👩🏻🦲👩🏻🦲
What does chimeric mean?
Mix of animals
What is the benefit of Adalimumab (Humira) being 100% human peptide sequences?
Decreased risk of sensitivity reactions
What are the 2 “Me-too” drugs that are pretty much the same thing as adalimumab (Humira)? 🤑
Certrolizumab (Cimiza)
Golimumab (Simponi)
How does Etanercept (Enbrel) target TNFα?
It is a fusion protein that is a FAKE TNFα receptor.
Uses up all the TNFα so it cant bind to the real receptor
(EtanerCEPT= looks like “receptor’)
Which DMARD inhibits B cell differentiation by binding to CD20?
Rituximab (Rituxan)
Which DMARD inhibits T cell activation?
Abatacept (Orencia)
All of the drubs that are monoclonal antibodies end in “___”
“mab”
Infliximab
Adalimumab
Certrolizumab
Golimumab
Rituximab
All of the drugs that are fusion proteins end in “_____”
“cept”
Etanercept
Abatacept
Which two drugs inhibit the synthesis of nucleic acid in WBCs?
Leflunomide (Arava)
Mycophenolate mofetil (Cellcept)
Leflunomide (Arava) inhibits nucleic acid synthesis by inhibiting the enzyme that does de novo (purine/pyramidine) synthesis
Pyrimidine
Mycophenolate mofetil (Cellcept) inhibits nucleic acid synthesis by inhibiting the enzyme that makes (purines/pyrimidines)
Purines
If Leflunomide (Arava) and Mycophenolate mofetil (Cellcept) are preventing the production of purines and pyrimidines, why doesn’t it kill us?
Because they SPECIFICALLY affect the pathways in WBCs and nowhere else. (the “de novo” pathways are the ones used by WBCs)
Other than inhibiting the production of de novo pyrimidine synthesis, Leflunomide has 2 other MOAs. What are those?
Inhibits induction of COX-2 = antiinflammatory effect
Inhibits tyrosine kinase (not important)
What is the unique adverse effect of mycophenolate mofetil (Cellcept) that Dr Kerecsen mentioned in the review (but nowhere else in his lectures or handouts lol)
A “very nice rash”
WHat are the two DMARDs that are Interleukin receptor antagonists?
Anakinra (Kineret) IL-1
Tocilizumab (Actemra) IL-6
Which DMARD drug will block IL-1?
Anakinra (Kineret)
Which DMARD drug will block IL-6?
Tocilizumab (Actemra)
Interleukins are (strong/weak) promoters of the immune response
Strong
Almost all DMARD drugs are combined with _________
Methotrexate
If someone is intolerant to Methotrexate, but they need a DMARD, which drug can be used all by itself without methotrexate?
Tofacitinib (Xeljanz)
(Baricitinib (Olumiant) can also be used as monotherapy, but he barely talked about it and it was not mentioned in the review)
All DMARD drugs open you up to higher risks for infection and malignancy, but which drug has the WORST risk for this?
SERIOUS!!!
HUGE
REALLY BAD INFECTIONS AND CANCERS
Tofacitinib (Xeljanz)
Which two DMARD drugs are Janus Kinase (JAKs) inhibitors?
Tofacitinib (Xeljanz)
Baricitinib (Olumiant)
What is the MOA of sulfasalazine?
Inhibits dihydrofolate (DHF) synthesis
Which drug primarily inhibits JAK1 and JAK3?
Tofacitinib (Xeljanz)
Which drug is a fully human TNFα blocker?
Adalimumab (Humira)
Which DMARD will increase your risk of TB?
ALL OF THEM
Which drug is a chimeric monoclonal antibody that binds CD20?
Rituxumab (Rituxan)🐀
What are the two chimeric drugs that use mouse parts
Infliximab (Remicade)
Rituximab (Rituxan)
Which DMARDs pride themselves on containing 100% human parts
Adalimumab (Humira)
Certrolizumab (Cimiza)
Golimumab (Simponi)
Abatacept (Orencia)
