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RA (methotrexate, adalimumab (Humira), tofacitinib) - Coggle Diagram
RA
methotrexate
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MOA
folate antimetabolite that inhibits DNA synthesis, repair and cellular replication
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Monitoring
First 3 months
CBC with differential and platelets, serum creatinine, and LFTs Every 4-6 weeks
3-6months
CBC with differential and platelets, serum creatinine, and LFTs every 8-12 weeks
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adalimumab (Humira)
MOA
binds to TNF-alpha, interfering with TNFa receptor sites and cytokine driven inflammatory processes
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Monitoring
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TB, HepB, HepC, HIV screening
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CI/Warnings
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risk of deadly infections, TB and lymphoma and other cancers such as HSTCL
Counseling Points
give in fatty part of the skin on the top of the thigh or belly area,
allow to sit at room temp for 30 min before injection, store in fridge
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tofacitinib
Adverse
10% Infection and Nasopharyngitis
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Monitoring
TB screening, Hepatitis screening
Baseline neutrophil, lymphocyte, hemoglobin counts, HR, BP (then after 4-8 weeks of therapy, then every 3 months)
Signs/Symptoms of infection, periodic skin checks
MOA
Jak Inhibitor
Jaks active STATs which are responsible for regulating gene expression and intracellular activity. Blockage inhibits the cytokine or growth factor mediated gene expression
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Warnings :
Black Box Warnings:
- Risk of serious infections (TB, fungal infections, bacterial/viral infections)
- Thrombosis (PE, DVT, etc.) risk in patients with RA who have at least one other cardiovascular risk
- Higher risk of Lymphoma or other malignancies
Contraindicaitons
Non-Listed US label
Canada: Hypersensitivity to any parts of the formulation, severe hepatic impairment, pregnancy
Interactions
May increase the serum concentrations of CYP3A4 substrates, may enhance the effects of myelosuppressive agents and other immunosuppressive agents, can diminish effects of vaccines
Special Populations
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Reduce dose in Moderate to severe Renal impairment
End-stage: Administer after dialysis session on dialysis days if not given prior to dialysis
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PK
Protein binding ~40%
70% hepatic metabolism, through CYP3A4 and CYP2C19
Primarily renal excretion
Half-life: ~3 hours for IR formulation, ~ 6-8 hours for ER