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Prednisone is a prodrug and must be converted to prednisolone by the liver before it becomes active. [6] [7] Prednisolone then binds to glucocorticoid receptors, activating them and triggering changes in gene expression. [4] Prednisone was patented in 1954 and approved for medical use in the United States in 1955.
Large dosage variations in the patient's medication (including a self-increased dosage from 10 mg/day to as much as 100 mg/day for at least 3 months) produced extreme behavioral changes, from missed appointments to physical altercations, and eventually admission to a psychiatric ward and later to a locked Alzheimer facility.
[7] [8] [6] It differs from the similarly named prednisone in having a hydroxyl at the 11th carbon instead of a ketone. Common side effects with short-term use include nausea, difficulty concentrating, insomnia, increased appetite, and fatigue. [5] More severe side effects include psychiatric problems, which may occur in about 5% of people. [9]
Ocular effects: Topical steroid drops are frequently used after eye surgery but can also raise intraocular pressure (IOP) and increase the risk of glaucoma, cataract, retinopathy as well as systemic adverse effects. [14] Tachyphylaxis: The acute development of tolerance to the action of a drug after repeated doses. [15]
Then change to oral hydrocortisone or cortisone as a single morning dose, and gradually decrease by 2.5 mg each week. When the morning dose is less than replacement, the return of normal basal adrenal function may be documented by checking 0800 cortisol levels prior to the morning dose; stop drugs when 0800 cortisol is 10 μg/dl.
[6] [7] [8] Applying once daily is enough as it is as effective as twice or more daily application. [13] Strong steroids should be avoided on sensitive sites such as the face, groin and armpits. Even the application of weaker or safer steroids should be limited to less than two weeks on those sites.
The neuropsychiatric effects are partly mediated by sensitization of the body to the actions of adrenaline. Therapeutically, the bulk of corticosteroid dose is given in the morning to mimic the body's diurnal rhythm; if given at night, the feeling of being energized will interfere with sleep. An extensive review is provided by Flores and Gumina ...
The combination is then referred to as COP (cyclophosphamide, Oncovin, and prednisone or prednisolone) or CVP (cyclophosphamide, vincristine, and prednisone or prednisolone). As elderly patients have a greater risk of toxicity from the drugs, an option is to use an attenuated drug regimen, called miniCHOP.