High dose oral methylprednisolone in patients with rheumatoid arthritis: pharmacokinetics and clinical response

Abstract

A commercially available 1.0 g intravenous (i.v.) dosage formulation of methylprednisolone, as the sodium hemisuccinate salt (Solu Medrol, Upjohn) was administered both parenterally and orally (pulse steroid therapy) on separate occasions, to eight elderly (mean 65 y) patients with active rheumatoid arthritis. The relative oral bioavailability of the sterol was 69.2%. Elimination of methylprednisolone was prolonged when given orally; the mean residence times were 7.23 h and 3.94 h for oral and i.v. administrations, respectively. Clinical response to pulse steroid therapy was no different with respect to route of administration. There were no significant differences in standard clinical and laboratory assessments of disease activity when the two therapies were compared. Oral administration of methylprednisolone in patients requiring high-dose pulse steroid therapy is convenient and avoids the discomfort and inconvenience associated with i.v. administration.

Giant Cell Arteritis

“…15,70 Some authors have suggested better visual outcomes with IV corticosteroids; 32,71 and that IV therapy be used in patients with amaurosis fugax, marked loss of vision in 1 eye, or signs of fellow eye involvement, 15,70 because the IV route produces higher serum concentrations more rapidly than oral dosing. 72 However, there is no consensus regarding the use of IV corticosteroids, and several studies have demonstrated either no significant benefit, 71,73,74 or worse visual prognosis 70 with this mode of therapy.…”

Pulse steroid therapy

“…Studies show equivalent therapeutic responses in patients with multiple sclerosis and rheumatoid arthritis after oral and intravenous administration of the same high dose of pulsed methylprednisolone. [25][26] However, patients had nausea and malaise lasting several hours with oral prednisolone. [25][26] A comparison of pharmacokinetics of oral and intravenous high dose dexamethasone revealed a mean bioavailability of 63.4% for oral therapy.…”

“…[25][26] However, patients had nausea and malaise lasting several hours with oral prednisolone. [25][26] A comparison of pharmacokinetics of oral and intravenous high dose dexamethasone revealed a mean bioavailability of 63.4% for oral therapy. 27 However, bioavailability levels reported in the literature for oral low-dose dexamethasone show wide variation (53-100%).…”

Giant cell arteritis: managing the ophthalmic medical emergency

“…That is a lot of tablets to swallow. Furthermore, when compared with the oral administration of the same dose, the intravenous infusion results in a plasma concentration 4−5‐fold higher 15 . These calculations do not take into account other factors such as the variable absorption rate and time to achieve target serum concentrations, both of which affect the potency of oral corticosteroids 16 …”