Methylprednisolone topical

Patients with severe UC symptoms require hospitalization for management of their disease. If the patient is unresponsive to oral or topical mesalamine and oral corticosteroids, then a course of intravenous corticosteroids should be initiated.1 Hydrocortisone 300 mg/day given in three divided doses or methylprednisolone 60 mg daily for 7 to 10 days are the preferred therapies. 

Hydrocortisone, Topical Systemic (Cortef, Solu-Cortef) Methylprednisolone (Solu-Medrol)... 

Examples of group I, i.e. weak or low efficacy topical steroids, are hydrocortisone acetate in various concentrations, methylprednisolone 1.0% and prednisolone 0.5%. Group II, the moderately potent steroids, includes alclometasone dipropionate 0.05%, hydrocortisone butyrate 0.1%, triamcinolone acetonide 0.025% and fluocinolone ace-tonide 0.01%. Group III, the potent steroids, contains among others betamethasone valerate 0.1%, betamethasone dipropionate 0.05%, budesonide 0.025%, desoximetasone 0.05%, fluticasone propionate 0.05%, amcinonide 0.1%, fluocinonide 0.05% and mometasone furoate 0.1%. Group IV comprises the very potent agents such as clobetasol propionate 0.05% and halobetasol propionate 0.05%. 

Synthetic glucocorticoids are prednisolone, prednisone, methylprednisolone, dexamethasone, betamethasone and triamcinolone (Table 13.2). Hydrocortisone is available as either succinate or phosphate salts for oral and intravenous administration. It is the drug of choice when a rapid effect is required, e.g. acute adrenal insufficiency, or as peri-operative replacement therapy. Prednisolone can also be given intravenously. It has about 0.8 of the mineralocorticoid activity of hydrocortisone. Prednisone is a prodrug that is converted to prednisolone in the body. For chronic therapy, synthetic steroids without mineralocorticoid activity are preferred, such as dexamethasone, betamethasone or triamcinalone. Beclo-metasone passes membranes poorly and is more active topically than when given orally. It is used as an aerosol for chronic rhinitis and asthma, and topically in severe eczema. Fludrocortisone is a synthetic halogenated derivate of cortisol that is used for its mineralocorticoid effect. 

Chronic lichenified eczema has been attributed to prolonged use of topical methylprednisolone aceponate and budesonide (strength and duration of therapy not stated) in a 26-year-old woman (425). Patch tests were positive for methylprednisolone aceponate and budesonide cream, but negative for all other topical glucocorticoids. 

Generic Name Methylprednisolone Name(s) Medrol, others Systemic X Topical Inhalation Ophthalmic Otic Nasal... 

A 75-year-old woman was given hydroxychloroquine 400 mg/day for erosive lichen planus in conjunction with topical glucocorticoids and a short course of oral methylprednisolone 0.5 mg/kg/day. After 10 days she became disoriented in time and place, followed by feelings of depersonalization and kinesthetic hallucinations, preceded by nightmares. She stopped taking hydroxychloroquine 1 week later and the hallucinations progressively disappeared. She recovered her normal mental state within 1 month and had not relapsed 2 years later. 

An 11-year-old boy with iridocyclitis developed Cushing s syndrome, a posterior subcapsular cataract, and increased intraocular pressure in both eyes after the topical administration of prednisolone acetate 1 % eye-drops bilaterally for 6 months. The Cushing s syndrome was aggravated when periocular methylprednisolone acetate was started while bilateral posterior subtenon injections of 80 mg of suspension were continued every 6 weeks for 6 months. He had not used systemic glucocorticoids before. 

The prodrug approach described above also can be used to alter the solubility characteristics, which, in turn, can increase the flexibility in formulating dosage forms. The solubility of methylprcdnisolonc can be altered from essentially water-insoluble methylpredni.solone acetate to slightly water-insoluble methylprednisolone to water-soluble meth-ylprednisolone. sodium succinate. The water-soluble sodium hemisuccinate salt is used in oral, intravenous, and intramuscular dosage forms. Methylprednisolone itself is normally found in tablels. The acetate ester is found in topical ointments and sterile aqueous suspensions for intramuscular injection. Both the succinate and acetate esters are hydrolyzed to the active methylprednisolone by the patient s own systemic hydrolytic enzymes (esterases). 

Steroids snch as beclamethasone dipropionate, budes-onide, triamcinolone acetonide, and flunisolide are active when given topically and can control asthma without causing systemic effects or adrenal suppression. However, orally administered steroids such as prednisone, prednisolone, or methylprednisolone are still needed by some patients. 

Topical glucocorticoids can aid in alleviating dermatitis (see Table 20-2). These include dexamethasone (Decadron) cream, hydrocortisone ointment or cream, methylprednisolone acetate (Medrol) ointment, triamcinolone acetonide (Aristocort), and flurandrenolide (Cordran). 

UVB-induced erythema, a model for sunburned skin, did not enhance penetration of topical methylprednisolone, perhaps addressing concerns of toxicity when treating sunburns with topical corticosteroids (Table 4.8) [96],... 

Gunther G, Kecskes A, Staks T, Tauber U. Percutaneous absorption of methylprednisolone ace-ponate following topical application of Advantan lotion on intact, inflamed and stripped skin of male volunteers. Skin Pharmacol Appl Skin Physiol. 1998 11 35-42. 

A 23-year-old man with ulcerative proctitis was treated successfully with topical mesalazine and beclometasone dipropionate [94 ]. After 1 month the treatment was stopped, but 5 years later, a relapse was treated with topical mesalazine and then oral mesalazine 2.4 g/day. After 3 days the patient developed pleuritic chest pain, exertional dyspnea, fever (38°C), and arthralgias, in particular in the shoulders and spine. Chest X-ray showed a right-sided basal pleural effusion. He was given intramuscular ceftriaxone 1 g/day and oral methylprednisolone 16 mg/day and after 11 days the chest symptoms resolv 1 month later mesalazine and glucocorticoid treatment were withdrawn, but 1 month later a relapse was treated again with oral mesalazine 2.4 g/ day. After 3 days the same pleuritic symptoms occurred and disappeared promptly on withdrawal of mesalazine. 

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