DMARDs Flashcards
Clinical signs of RA
Stiffness/ pain lasting 1 hours+ in bouts
- becomes progressively worse
- symmetrical pain
- NSAIDs are no longer working
Corticosteroid side effects
Numerous
- can inhibit hypothalamic-pituitary adrenal system by mimicking cortisol
( cant stop cold turkey) - can increases osteoporosis
(must prescribe Vit. D and calcium vitamins with use) - can cause Cushing disease
Which DMARDs are teratogens?
Methotrexate and Lefulnomide
-Methotrexate disables dihydrofolate reductase enzymes which are used to make both cytokines and purines/thymine residues
What DMARDs can also be used as a cancer treatment?
Methotrexate
Azothioprine
Leflunomide
What is the first line traditional DMARD?
Methotrexate
if patient cant handle it or is pregnant, then usually Tolcilizumab is first line
What DMARD is the prodrug to 6-mercaptopurine (6-MP) and is also used to prevent transplant rejection?
Azothioprine
- 6-MP produces PPRP amidotransferase which inhibits purine synthesis and disables antibodies
What DMARD is associated with malignancies and raises sensitivity to the sun?
Azothioprine
What traditional DMARDs are completely safe for pregnant patients?
Hydroxychoroquine
Sulfasalazine
What biological DMARDs are The most safe for pregnant patients?
Anakinra (BEST CHOICE)
All TNF-a inhibitors (“MABs” and etanercept)
What DMARD is a prodrug for 5-aminosalicylate and is cleaved in small intestines to produce drug?
Sulfasalazine
- helps to treat IBDs
- makes urine hello-orange and is contraindicated in patients with sulfa allergies
What DMARD is contraindicated for sulfa-allergic patients and also may present yellow-orange urine/skin?
Sulfasalazine
What DMARD is a pyrimidine synthase inhibitor and is the only DMARD to require a loading dose?
Leflunomide
- contraindicated in liver disease patients due to build up of liver enzymes
What DMARD is a purine synthase inhibitor?
Methotrexate
What DMARD can produce Stevens-Johnson syndrome
Leflunomide
What DMARDs inhibit the JAK/STAT pathway?
Tofacitinib
Tocilizumab
What DMARDs do you have to monitor cholesterol with?
Tofacitinib and tocilizumab
- contraindicated in patients with high cholesterol
What TNF-a inhibitor also inhibits TNF-b?
Etanercept
- super high half life at 102 hrs
What DMARD inhibts IL-1 receptors?
Anakinra
What DMARD is an IL-6 inhibitor?
Tocilizumab
- competitive inhibition of both membrane bound and free soluble IL-6 receptors
What DMARD can produce false glucose readings and also can worsen COPD symptoms?
Abatacept
Pharmacological targets of DMARDs
Inhibt gene expression
Inhibit intracellular signaling
Decrease T-cell stimulation by down regulating stoking receptors and neutralizing cytokines
Deplete naive and active T-cell levels
Inhibit APCs
What two DMARDs can also be used to treat lupus?
Azothioprine and aminoquinoline
What is the receptor on T-cells that binds usually to CD80/86 receptors on APCs?
CD28
What NSAID is given often times with methotrexate to alleviate pain?
Naproxen
