MSK Pharmacology Flashcards
Inhibitor of dihydrofolate reductase
Methotrexate
Methotrexate inhibits this
Dihydrofolate reductase
This drug is slow in onset of benefit (>6 weeks) but can be very effective for a long time
Methotrexate
Most commonly used DMARD, alone or in combination with biologics
Methotrexate
Methotrexate has bone marrow toxicity when coadministered with these
NSAIDs
Methotrexate is contraindicated in these 2 circumstances
Pregnancy and Renal failure
Methotrexate has drug interactions with these
Protein binding drugs
This DMARD has interactions with protein binding drugs
Methotrexate
This DMARD has bone marrow toxicity when coadministered with NSAIDs
Methotrexate
Drug that blocks pyrimidine synthesis by inhibiting dihydroorotate dehydrogenase
Leflunomide
Leflunomide blocks this by inhibiting dihydroorotate dehydrogenase
Pyrimidine synthesis
Leflunomide blocks pyrimidine synthesis by inhibiting this
Dihydroorotate dehydrogenase
Leflunomide has this black box warning
Hepatotoxicity
Leflunomide is contraindicated in this
Prengnancy (teratogenicity)
These two DMARDs together are super additive in benefit and toxicity (especially hepatotoxicity)
Methotrexate and Leflunomide
This may bind DNA and disrupt rheumatoid factor synthesis
Hydroxychloroquine
2 non-biologic DMARDs that can cause hemolysis in patients with deficiency in glucose-6-phosphate dehydrogenase
Hydroxychloroquine and Sulfasalazine
Hydroxychloroquine may bind DNA and disrupt synthesis of this
Rheumatoid factor
DMARD with unclear mechanism in Rheumatoid Arthritis, and hemolysis in patients with G6PD deficiency
Sulfasalazine
3 TNF inhibitors
Etanercept
Infliximab
Adalimumab
Recombinant human TNF receptor 2/IgG1 fusion protein (non-functional receptor fragment), acts as decoy receptor, captures TNF to block inflammation and decrease cytokine release
Etanercept
Biologic DMARD that acts as decoy receptor, captures TNF to block inflammation and decrease cytokine release
Etanercept
What is Etanercept?
Recombinant human TNF receptor 2/IgG1 fusion protein
Acts as a decoy receptor to capture TNF
Etanercept has increased risk of these 2 things
Malignancy and infections
DMARD that targets TNF alpha, suppresses cytokine synthesis and release
Infliximab
Drug with increased risk of infections and TB reactivation
Increased risk of lymphoma in children/adolescents
Infliximab
Infliximab has increased risk of infections, specifically reactivation of this
TB
Infliximab has increased risk of this in children/adolescents
Lymphoma
Recombinant human monoclonal antibody for TNF alpha, blocks interaction with receptor
Adalimumab
Oral Janus Kinase inhibitor (competitive)
Blocks intracellular Janus Kinase (JAK1 & JAK3) signal to disrupt activation of immune system
Tofacitinib
What does Tofacitinib do?
Blocks intracellular JAK signal to disrupt activation of immune system
(competitive oral janus kinase inhibitor)
Rheumatoid arthritis treatment usually begins with this monotherapy
Methotrexate