DMARDs (Lauren🌭)

Question 1

Are DMARDs analgesics?

Answer 1

No

Question 2

Do DMARDs have any immediate effects?

Answer 2

No. Used to slow the progression of the disease.

Question 3

What is the main effect of Gold Salts?

Answer 3

Suppress cellular immunity

Question 4

What are the main toxicities of Gold Salts?

Answer 4

Bone marrow damage

Enterocolitis

PRETTY TOXIC

NOT USED MUCH

Question 5

What kind of drug is Penicillamine (Cuprimine)

Answer 5

A chelating drug that works for RA and Wilson’s disease

Question 6

What are the toxicities of Penicillamine (Cuprimine)

Answer 6

It fucks up everything

Question 7

What are the main toxicities of Hydroxychloroquine (Plaquenil)?

Answer 7

Hemolysis (G6PD deficient)

Ototoxicity

Retinopathy

Peripheral neuropathy

Pruritus

Methemoglobinemia

Question 8

Sulfasalazine (Azulfidine) is a prodrug that is metabolized into _________ and ________

Answer 8

Sulfonamide

Salicylate

Question 9

The adverse effects of sulfasalazine are related to it being metabolized into (sulfonamide/salicylate/both)

Answer 9

Both

Question 10

What DMARDs act on TNFα?

Answer 10

Infliximab (Remicade) 👩🏻‍🦲🐁

Adalimumab (Humira)👩🏻‍🦲

Cetrolizumab (Cimiza)

Golimumab (Simponi)

Etanercept (Enbrel)

Question 11

What are the old school DMARDs that aren’t used much

Answer 11

Gold Salts

Penicillamine (Cuprimine)

Hydroxychloroquine (Plaquenil)

Sulfasalazine (Azulfidine)

Question 12

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?

Answer 12

Basically anything that comes along with a decreased immune system:

Increased risk of infection

TB

Valley fever

Development of cancer

Etc

Question 13

Infliximab (Remicade) and Adalimumab (Humira) are both what kind of drugs?

Answer 13

Monoclonal antibodies against TNFα

Question 14

Infliximab (Remicade) and Adalimumab (Humira) are both monoclonal antibodies against TNFα. What is the main difference between them?

Answer 14

Infliximab (Remicade) is chimeric. (Mix of human and murine regions) 👩🏻‍🦲🐁

Adalimumab (Humira) is fully human 👩🏻‍🦲👩🏻‍🦲

Question 15

What does chimeric mean?

Answer 15

Mix of animals

Question 16

What is the benefit of Adalimumab (Humira) being 100% human peptide sequences?

Answer 16

Decreased risk of sensitivity reactions

Question 17

What are the 2 “Me-too” drugs that are pretty much the same thing as adalimumab (Humira)? 🤑

Answer 17

Certrolizumab (Cimiza)

Golimumab (Simponi)

Question 18

How does Etanercept (Enbrel) target TNFα?

Answer 18

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’)

Question 19

Which DMARD inhibits B cell differentiation by binding to CD20?

Answer 19

Rituximab (Rituxan)

Question 20

Which DMARD inhibits T cell activation?

Answer 20

Abatacept (Orencia)

Question 21

All of the drubs that are monoclonal antibodies end in “___”

Answer 21

“mab”

Infliximab

Adalimumab

Certrolizumab

Golimumab

Rituximab

Question 22

All of the drugs that are fusion proteins end in “_____”

Answer 22

“cept”

Etanercept

Abatacept

Question 23

Which two drugs inhibit the synthesis of nucleic acid in WBCs?

Answer 23

Leflunomide (Arava)

Mycophenolate mofetil (Cellcept)

Question 24

Leflunomide (Arava) inhibits nucleic acid synthesis by inhibiting the enzyme that does de novo (purine/pyramidine) synthesis

Answer 24

Pyrimidine

Question 25

Mycophenolate mofetil (Cellcept) inhibits nucleic acid synthesis by inhibiting the enzyme that makes (purines/pyrimidines)

Answer 25

Purines

Question 26

If Leflunomide (Arava) and Mycophenolate mofetil (Cellcept) are preventing the production of purines and pyrimidines, why doesn’t it kill us?

Answer 26

Because they SPECIFICALLY affect the pathways in WBCs and nowhere else. (the “de novo” pathways are the ones used by WBCs)

Question 27

Other than inhibiting the production of de novo pyrimidine synthesis, Leflunomide has 2 other MOAs. What are those?

Answer 27

Inhibits induction of COX-2 = antiinflammatory effect Inhibits tyrosine kinase (not important)

Question 28

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)

Answer 28

A “very nice rash”

Question 29

WHat are the two DMARDs that are Interleukin receptor antagonists?

Answer 29

Anakinra (Kineret) IL-1 Tocilizumab (Actemra) IL-6

Question 30

Which DMARD drug will block IL-1?

Answer 30

Anakinra (Kineret)

Question 31

Which DMARD drug will block IL-6?

Answer 31

Tocilizumab (Actemra)

Question 32

Interleukins are (strong/weak) promoters of the immune response

Answer 32

Strong

Question 33

Almost all DMARD drugs are combined with _________

Answer 33

Methotrexate

Question 34

If someone is intolerant to Methotrexate, but they need a DMARD, which drug can be used all by itself without methotrexate?

Answer 34

Tofacitinib (Xeljanz) (Baricitinib (Olumiant) can also be used as monotherapy, but he barely talked about it and it was not mentioned in the review)

Question 35

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

Answer 35

Tofacitinib (Xeljanz)

Question 36

Which two DMARD drugs are Janus Kinase (JAKs) inhibitors?

Answer 36

Tofacitinib (Xeljanz) Baricitinib (Olumiant)

Question 37

What is the MOA of sulfasalazine?

Answer 37

Inhibits dihydrofolate (DHF) synthesis

Question 38

Which drug primarily inhibits JAK1 and JAK3?

Answer 38

Tofacitinib (Xeljanz)

Question 39

Which drug is a fully human TNFα blocker?

Answer 39

Adalimumab (Humira)

Question 40

Which DMARD will increase your risk of TB?

Answer 40

ALL OF THEM

Question 41

Which drug is a chimeric monoclonal antibody that binds CD20?

Answer 41

Rituxumab (Rituxan)🐀

Question 42

What are the two chimeric drugs that use mouse parts

Answer 42

Infliximab (Remicade) Rituximab (Rituxan)

Question 43

Which DMARDs pride themselves on containing 100% human parts

Answer 43

Adalimumab (Humira) Certrolizumab (Cimiza) Golimumab (Simponi) Abatacept (Orencia)