Pulse glucocorticoids Many clinicians use IV pulse GCs as the initial treatment of severe life-threatening or organ-threatening presentations of rheumatic diseases. This is typically methylprednisolone given in doses of 1 g/day for 3 to 5 consecutive days. Many physicians split the dose (500 mg IV q12 hours or 250 mg IV q6 hours) on inpatients …
What are JAK inhibitors (Jakinibs)? JAKs are intracellular proteins that associate with and transduce signals from a number of cytokine and growth factor receptors. There are four JAKs (JAK1, JAK2, JAK3, and tyrosine kinase 2 [TYK2]) that form various homodimers and heterodimers with different pairings being associated with different cell surface receptors. When a specific …
How is apremilast supplied and used in the treatment of rheumatic diseases? • FDA-approved indications: psoriasis and PsA. Also effective for Behçet’s disease (oral and genital ulcers). • Available formulation: starter therapy pack (10-, 20-, 30-mg tablets); 30-mg tablets. • Dosage: use starter pack to start with 10 mg one per day (QD) and escalate up to 30 …
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major toxicities of cyclosporine and tacrolimus? • Decreased renal function (usually reversible with discontinuation of drug). • Hypertension (treat with nifedipine or labetalol). • Anemia (note that does not decrease WBC count). • Malignancies (lymphomas and skin cancers): lymphoma (EBV-related) may regress with stopping drug. • Hyperuricemia and gout (switch to tacrolimus which causes less hyperuricemia). • Bone pain (treat with …
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What rheumatic syndromes have been treated with cyclosporine? • RA (especially when combined with MTX). • Polymyositis/dermatomyositis (especially with ILD): tacrolimus may be a better drug. • PsA and psoriasis. • SLE (especially membranous glomerulonephritis due to its effect on podocytes). • Uveitis. • Others: Behçet’s, macrophage-activation syndrome (Still’s disease, SLE), pyoderma gangrenosum, Sjogren’s dry eyes (ophthalmic emulsion).
What are tacrolimus and sirolimus? Tacrolimus is a macrolide produced by a fungus (actinomycete). It has immunosuppressive effects similar to cyclosporine but at a dose 10 to 100 times lower (0.1–0.25 mg/kg per day; usual dose 2–5 mg BID). Tacrolimus, like cyclosporine, is a potent inhibitor of T-cell activation and inhibits transcription of early T-cell …
How is cyclosporine microemulsion used in the treatment of rheumatic diseases? • Available formulations: 25- and 100-mg capsule; oral solution 100 mg/mL; IV solution 50 mg/mL. • Dosage: 2.5 to 4 mg/kg ideal body weight for most rheumatic diseases. Start low in divided doses, and increase 0.5 mg/kg per day every 4 to 8 weeks. • Cost (200 …
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