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1542 Corticosteroids

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1542 Corticosteroids 1542 Corticosteroids depends on the dissolution rates of the tablet formula- When given orally prednisolone is usually used al- Irl.: Deltacortril; Pred Forte†; Pred Mild; Predenema; Predfoam; Prednesol; Predsol; Israel: Pred Forte; Prelone†; Ultracortenol; Ital.: Meticortelone†; tions. As discussed under Hepatic Impairment, above, though prednisolone sodium phosphate or prednisolo- Soludacortin†; Jpn: Farnerate; Farnezone; Lidomex; Livimex; Malaysia: reduced corticosteroid concentrations when giving ne steaglate are also given; the usual dose, expressed in Dhasolone; Pred Forte; Pred Mild; Predon; Setsolone†; Sterosone†; Mex.: Cetapred; Delta-Diona; Fisopred; Meticortelone; Pred; Pred-NF; Prednefrin prednisone to patients with liver disease do not seem to terms of prednisolone, is about 2.5 to 60 mg daily in SF; Sophipren; Neth.: Di-Adreson-F; Pred Forte; Ultracortenol; Norw.: be a problem in practice. After intramuscular doses the divided doses, as a single daily dose after breakfast, or Pred-Clysma; Ultracortenol; NZ: Pred Forte; Pred Mild; Redipred; Philipp.: Histacort; Inflastat; Liquipred; Optipred; Pred Forte; Predisyr; sodium phosphate ester of prednisolone is rapidly ab- as a double dose on alternate days. Alternate-day early- Prednecort; Syrupred; Pol.: Encortolon; Fenicort; Mecortolon; Port.: sorbed whereas the acetate, in the suspension form, is morning dosage regimens produce less suppression of Frisolona; Lepicortinolo; Predniocil; Sintisone†; Solu-Dacortina; Rus.: Me- dopred (Медопред); S.Afr.: Capsoid; Lenisolone; Meticortelone†; Pred only slowly absorbed. the hypothalamic-pituitary axis but may not always Mild; Predsol†; Preflam; Prelone; Singapore: Dhasolone; Econopred; Pred; provide adequate control. Enteric-coated tablets of Walesolone; Xepasone†; Spain: Dacortin H†; Estilsona; Pred Forte; Peak plasma concentrations of prednisolone are ob- Swed.: Precortalon aquosum; Pred-Clysma; Ultracortenol; Switz.: Corti- tained 1 or 2 hours after an oral dose, and it has a usual prednisolone are also available (for the view that these Clyss†; Hexacortone; Pred Forte; Pred Mild; Solu-Dacortine†; Spiricort; Ul- should not be used in patients with inflammatory bow- tracortene H†; Ultracortenol; Thai.: Di-Adreson-F; Inf-Oph; Opredsone; plasma half-life of 2 to 4 hours. Its initial absorption, Polypred; Pred Forte; Pred Mild; Predisole†; Prednersone; Prednisil; Turk.: but not its overall bioavailability, is affected by food. el disease, see above). Codelsol; Codelton; Deltacortril; Hexacorton; Neocorten; Norsol; Pred Forte; Prednol; UAE: Gupisone; UK: Deltacortril; Deltastab; Precortisyl; Prednisolone is extensively bound to plasma proteins, For parenteral use the sodium phosphate ester is nor- Pred Forte; Predenema; Predfoam; Predsol; USA: Ak-Pred†; Delta-Cor- tef†; Econopred†; Flo-Pred; Hydeltrasol†; Inflamase†; Key-Pred-SP; Key- although less so than hydrocortisone (cortisol). The mally given, either intravenously by injection or infu- Pred†; Millipred; Orapred; Pediapred; Pred; Pred Forte; Pred Mild; Pred- volume of distribution, and also the clearance are re- sion or intramuscularly by injection; doses appear to Phosphate; Predalone†; Predcor; Prednisol; Prelone; Venez.: Meticorte- ported to increase with an increase from low to moder- have been variously expressed in terms of prednisolo- lone; Ocupred; Prednefrin†; Sintisone; Sophipren. ate doses; at very high doses, clearance appears to be- ne, prednisolone phosphate, or prednisolone sodium Multi-ingredient: Arg.: Bactio Rhin Prednisolona; Blefamide; Cortizul; Delta Tomanil B12; Deltar; Efecoryl Forte; Esodar; Fenipred; Itro†; Neocor- come saturated. phosphate but are generally within the range of 4 to tizul; Oftalmoflogol†; Otidrops; Prednefrin; Prednifarma; Procto Venart; 60 mg daily. An aqueous suspension of prednisolone Relefrina; Rucaten Prednisolona; Scheriproct; Solupred; Austral.: Predne- Prednisolone is excreted in the urine as free and conju- frin; Scheriproct; Austria: Alpicort; Delta-Hadensa; Phoscortil; Scheriproct; gated metabolites, with an appreciable proportion of acetate is also used intramuscularly for a prolonged ef- Belg.: Hemosedan; Predmycin P; Scheriproct; Sofrasolone; Braz.: Colu- fect, in doses of 25 to 100 mg once or twice weekly. toide; Fonergin; Isopto Cetapred; Polipred; Predmicin; Reumazine†; Rifo- unchanged prednisolone. Prednisolone is largely inac- cort; Rinisone; Canad.: Blephamide; Dioptimyd†; Vasocidin†; Chile: Ban- tivated as it crosses the placenta; small amounts are ex- The sodium succinate ester has also been given edif Oftalmico con Prednisolona; Blefamide; Deltamid; Gemitin con parenterally. Prednisolona; Pred G†; Scheriproct; Sintoftona; Cz.: Alpicort; Alpicort F; creted in breast milk. Imacort; Isopto Cetapred†; Linola-H-compositum N†; Linoladiol-H N†; Prednisolon J†; Fin.: Scheriproct; Septison; Fr.: Cortisal; Deliproct; Derinox; Prednisolone has a biological half-life lasting several For intra-articular injection the acetate, sodium Deturgylone; Ger.: Alferm†; Alpicort; Alpicort F; Anumedin†; Aquapred; hours, intermediate between those of hydrocortisone phosphate, and tebutate esters are used. Suggested dos- Berlicetin; Bismolan H Corti; Blephamide; Corti-Dynexan†; Dexa-Phlogont L†; Imazol comp; Inflanegent; Leioderm P; Linola-H-compositum N†; (cortisol) and the longer-acting glucocorticoids, such es are 5 to 25 mg of prednisolone acetate, 2 to 30 mg of Linoladiol-H N; NeyNormin N (Revitorgan-Dilutionen N Nr 65)†; NeyTu- as dexamethasone. It is this intermediate duration of prednisolone phosphate (for the sodium phosphate es- morin N (Revitorgan-Dilutionen N Nr 66)†; Scheriproct†; Ultra-Demo- plas†; Virunguent P†; Gr.: Blephamide†; Dermol; Isopto Cetapred; Precor- action that makes it suitable for the alternate-day dos- ter), and 4 to 40 mg of prednisolone tebutate. The sodi- tivit†; Scheriproct Neo; Hong Kong: Blephamide; Chlomy-P†; Pilelife; age regimens which have been found to reduce the risk um phosphate and tebutate esters are also given by in- Prednitracin†; Hung.: Alpicort; Alpicort F; Aurobin; Linoladiol-H N†; Pred- nisolon J; Rheosolon; India: Atrisolon; Otek-AC†; Perfocyn; Polyderm†; In- of adrenocortical insufficiency, yet provide adequate tralesional injection and by injection into soft tissue. don.: Borraginol-S; Chloramphecort-H; Klorfeson; Irl.: Scheriproct; Israel: corticosteroid coverage in some disorders. Aflumycin; Blephamide; Threolone; Ital.: Bio-Delta Cortilen; Deltamidrina; Prednisolone acetate and prednisolone sodium phos- Solprene; Malaysia: Blephamide†; Mex.: Artrilan; Blefamide; Blefamide-F; ◊ General reviews of the pharmacokinetics of prednisolone1,2 phate are also used in the topical treatment of allergic Dartrizon; Deltamid; Deltron; Isopto Cetapred; Metimyd†; Obrypre; Otal- 3 and some references to its pharmacokinetics in healthy subjects and inflammatory conditions of the eyes or ears, usual- gan; Premid; Scheriproct; Norw.: Scheriproct; NZ: Blephamide; Philipp.: and in various disease states.4-8 Cetapred; Histacort; Isopto Cetapred; Predmycin-P; Pol.: Alpicort; Alpi- ly as drops containing 0.5 or 1%. Prednisolone has also cort E; Mecortolon N; Port.: Anacal; Ciclobiotico†; Conjunctilone-S; 1. Begg EJ, et al. The pharmacokinetics of corticosteroid agents. Flogiftalmina†; Meocil; Neo-Davisolona; Predniderma†; Predniftalmina; Med J Aust 1987; 146: 37–41. been used topically as the free alcohol and as the hemi- Scheriproct; Vitasma†; Rus.: Aurobin (Ауробин); Dermosolon 2. Frey BM, Frey FJ. Clinical pharmacokinetics of prednisone and succinate, pivalate, and metasulfobenzoate sodium es- (Дермозолон); Hepatrombin H (Гепатромбин Г); Tergynan (Тержинан); prednisolone. Clin Pharmacokinet 1990; 19: 126–46. ters. S.Afr.: Scheriproct; Singapore: Blephamide; Predmycin-P†; Spain: Alergi- 3. Rohatagi S, et al. Pharmacokinetics of methylprednisolone and cal; Antigrietun; Kanapomada; Nasopomada; Otonina†; Poly Pred; Predni prednisolone after single and multiple oral administration. J Clin Azuleno; Proctium; Rinobanedif; Rinovel; Ruscus; Scheriproct; Teolixir Com- Pharmacol 1997; 37: 916–25. For rectal use prednisolone metasulfobenzoate sodi- positum; Swed.: Scheriproct N; Switz.: Alpicort F; Blephamide; Calpred; Imacort; Locaseptil-Neo; Mycinopred; Nystacortone†; Prednitracin†; Pre- 4. Berghouse LM, et al. Plasma prednisolone levels during intrave- um or prednisolone sodium phosphate are often given. mandol; Scheriproct; Thai.: Denson; Farakil; Levoptin; Mysolone-N; Neo- nous therapy in acute colitis. Gut 1982; 23: 980–3. Retention enemas containing the equivalent of 20 mg pred†; Neozolone; Pred Oph; Predex†; Predmycin†; Prednisil-N; Prednisil†; 5. Shaffer JA, et al. Absorption of prednisolone in patients with Scheriproct†; Unipred; Turk.: Blephamid; Otimisin; Prednol-A; Suprenil; Crohn’s disease. Gut 1983; 24: 182–6. of prednisolone per 100 mL, rectal foam containing the UK: Predsol-N; Scheriproct; USA: Blephamide; Metimyd; Poly-Pred; Pred 6. Reece PA, et al. Prednisolone protein binding in renal transplant equivalent of 20 mg of prednisolone per dose, or sup- G; Sulfamide; Vasocidin; Vasocine; Venez.: Clorasona; Permucal; patients. Br J Clin Pharmacol 1985; 20: 159–62. positories containing the equivalent of 5 mg of pred- Scheriproct; Sulfacort. 7. Frey FJ, et al. Altered metabolism and decreased efficacy of prednisolone and prednisone in patients with hyperthyroidism. nisolone are available. Prednisolone has also been used Clin Pharmacol Ther 1988; 44: 510–21. rectally as the free alcohol and
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