Paramethasone Acetate/Prednisolone 1541

Prednisolone Acetate (BANM, rINNM) ⊗ Pharmacopoeias. In Eur. (see p.vii). Owing to its less pronounced mineralocorticoid activi- Ph. Eur. 6.2 (Prednisolone Pivalate). A white, or almost white, ty prednisolone is less likely than cortisone or hydro- Acetato de prednisolona; Prednisolonacetat; Prednisolon-acetát; crystalline powder. Practically insoluble in water; slightly solu- Prednisolone, acétate de; Prednisoloni acetas; Prednisolonia- ble in alcohol; soluble in dichloromethane. Protect from light. cortisone to cause sodium retention, electrolyte imbal- setaatti; Prednizolon Asetat; Prednizolon-acetát; Prednizolono ance, and oedema. Prolonged use of ophthalmic acetatas; Prednizolonu octan. Prednisolone 21-acetate. Prednisolone Sodium Phosphate (BANM, rINNM) ⊗ preparations containing corticosteroids has caused Преднизолона Ацетат Fosfato sódico de prednisolona; Natrii Prednisoloni Phosphas; raised intra-ocular pressure and reduced visual func- C23H30O6 = 402.5. Prednisolone, phosphate sodique de; Prednisolonfosfát sodná tion. CAS — 52-21-1. sůl; Prednisoloni natrii phosphas; Prednisoloninatriumfosfaatti; Breast feeding. Concentrations of prednisone and prednisolo- ATC — A07EA01; C05AA04; D07AA03; H02AB06; Prednisolonnatriumfosfat; Prednizolon Sodyum Fosfat; Prednizo- ne in breast milk from one woman 120 minutes after prednisone R01AD02; S01BA04; S02BA03; S03BA02. lon-nárium-foszfát; Prednizolono natrio fosfatas. Prednisolone 10 mg by mouth were found to be 26.7 nanograms and ATC Vet — QA07EA01; QC05AA04; QD07AA03; 21-(disodium orthophosphate). 1.6 nanograms/mL respectively.1 In 7 similar women given a QH02AB06; QR01AD02; QS01BA04; QS02BA03; Натрия Преднизолона Фосфат single 5-mg oral dose of tritium-labelled prednisolone, a mean of QS03BA02. 0.14% of the radioactivity from the dose was recovered per litre C21H27Na2O8P = 484.4. 2 Pharmacopoeias. In Chin., Eur. (see p.vii), Int., Jpn, and US. CAS — 125-02-0. of milk in the following 48 to 61 hours. In a study of 3 women, ATC — A07EA01; C05AA04; D07AA03; H02AB06; only about 0.025% of a single intravenous dose of prednisolone Ph. Eur. 6.2 (Prednisolone Acetate). A white or almost white, 3 crystalline powder. Practically insoluble in water; slightly solu- R01AD02; S01BA04; S02BA03; S03BA02. phosphate 50 mg was recovered in breast milk over 6 hours. ble in alcohol and in dichloromethane. Protect from light. ATC Vet — QA07EA01; QC05AA04; QD07AA03; During maintenance therapy with prednisolone in daily doses of USP 31 (Prednisolone Acetate). A white to practically white, QH02AB06; QR01AD02; QS01BA04; QS02BA03; 10 to 80 mg in 6 women, the milk to serum concentration ratio of odourless, crystalline powder. Practically insoluble in water; sol- QS03BA02. prednisolone ranged from 0.2, for doses of 30 mg or more, to 0.1 for lower doses.4 The authors estimated that the breast-fed infant uble 1 in 120 of alcohol; slightly soluble in acetone and in chlo- NOTE. PRED is a code approved by the BP 2008 for use on single would receive less than 0.1% of the maternal dose of prednisolo- roform. Store at a temperature of 25°, excursions permitted be- unit doses of eye drops containing prednisolone sodium phos- ne, and that this would be a negligible addition to the infant’s tween 15° and 30°. phate where the individual container may be too small to bear all the appropriate labelling information. endogenous cortisol production. They also concluded that expo- sure could be minimised by breast feeding at least 4 hours after Pharmacopoeias. In Eur. (see p.vii), Int., and US. Prednisolone Caproate (rINNM) ⊗ the dose. Ph. Eur. 6.2 (Prednisolone Sodium Phosphate). A white or al- 5 Caproato de prednisolona; Prednisolone, Caproate de; Pred- most white, hygroscopic, crystalline powder. Freely soluble in A review by the UK CSM remarked that prednisolone was dis- nisolone Hexanoate (BANM); Prednisoloni Caproas. Prednisolone water; very slightly soluble in alcohol. A 5% solution in water tributed into breast milk in small amounts and recommended that 21-hexanoate. has a pH of 7.5 to 9.0. Protect from light. infants of mothers receiving 40 mg or more daily should be mon- . A white or slightly itored for signs of adrenal suppression. The American Academy Преднизолона Капроат USP 31 (Prednisolone Sodium Phosphate) 6 yellow friable granules or powder. Is odourless or has a slight of Pediatrics considers that the use of prednisone or prednisolo- ne is usually compatible with breast feeding. C27H38O6 = 458.6. odour. Is slightly hygroscopic. Soluble 1 in 4 of water and 1 in 13 ATC — A07EA01; C05AA04; D07AA03; H02AB06; of methyl alcohol; slightly soluble in alcohol and in chloroform; 1. Katz FH, Duncan BE. Entry of prednisone into human milk. N R01AD02; S01BA04; S02BA03; S03BA02. Engl J Med 1975; 293: 1154. very slightly soluble in acetone and in dioxan. pH of a 1% solu- 2. McKenzie SA, et al. Secretion of prednisolone into breast milk. ATC Vet — QA07EA01; QC05AA04; QD07AA03; tion in water is between 7.5 and 10.5. Store in airtight containers. Arch Dis Child 1975; 50: 894–6. QH02AB06; QR01AD02; QS01BA04; QS02BA03; 3. Greenberger PA, et al. Pharmacokinetics of prednisolone trans- QS03BA02. fer to breast milk. Clin Pharmacol Ther 1993; 53: 324–8. Prednisolone Sodium Succinate (BANM, rINNM) ⊗ 4. Öst L, et al. Prednisolone excretion in human milk. J Pediatr Prednisolone Sodium Hemisuccinate; Prednisolone, Succinate 1985; 106: 1008–11. Prednisolone Hydrogen Succinate Sodique de; Prednisoloni Natrii Succinas; Succinato sódico de 5. CSM/MCA. Systemic corticosteroids in pregnancy and lacta- (BANM, rINNM) ⊗ tion. Current Problems 1998; 24: 9. Also available at: prednisolona. 11β,17α,21-Trihydroxypregna-1,4-diene-3,20-di- http://www.mhra.gov.uk/home/idcplg?IdcService=GET_FILE& Hidrogenosuccinato de prednisolona; Prednisolone Hemisucci- one 21-(sodium succinate). dDocName=CON2023392&RevisionSelectionMethod= nate; Prednisolone, Hémisuccinate de; Prednisoloni Hemisucci- Преднизолона Натрия Сукцинат LatestReleased (accessed 20/06/06) 6. American Academy of Pediatrics. The transfer of drugs and oth- nas. Prednisolone 21-(hydrogen succinate). C25H31NaO8 = 482.5. er chemicals into human milk. Pediatrics 2001; 108: 776–89. CAS — 1715-33-9. Преднизолона Гемисукцинат Correction. ibid.; 1029. Also available at: ATC — A07EA01; C05AA04; D07AA03; H02AB06; http://aappolicy.aappublications.org/cgi/content/full/ C25H32O8 = 460.5. R01AD02; S01BA04; S02BA03; S03BA02. pediatrics%3b108/3/776 (accessed 27/04/04) CAS — 2920-86-7. ATC Vet — QA07EA01; QC05AA04; QD07AA03; Hepatic impairment. Conversion of prednisone to pred- ATC — A07EA01; C05AA04; D07AA03; H02AB06; QH02AB06; QR01AD02; QS01BA04; QS02BA03; nisolone has been reported to be impaired in chronic active liver QS03BA02. R01AD02; S01BA04; S02BA03; S03BA02. disease.1,2 However, although plasma-prednisolone concentra- ATC Vet — QA07EA01; QC05AA04; QD07AA03; Pharmacopoeias. US includes Prednisolone Sodium Succi- tions were found to be more predictable after prednisolone than QH02AB06; QR01AD02; QS01BA04; QS02BA03; nate for Injection. prednisone in a group of healthy subjects,3 no difference was not- QS03BA02. USP 31 (Prednisolone Sodium Succinate for Injection). A creamy ed in patients with chronic active hepatitis, in whom impaired white powder with friable lumps, having a slight odour. Pharmacopoeias. In Jpn and US. elimination of prednisolone compensated for any impaired con- version of prednisone. A review of the pharmacokinetics of pred- USP 31 (Prednisolone Hemisuccinate). A fine, creamy-white, 4 practically odourless, powder with friable lumps. Soluble 1 in Prednisolone Steaglate (BAN, rINN) ⊗ nisone and prednisolone concluded that fear of inadequate con- 4170 of water, 1 in 6.3 of alcohol, 1 in 1064 of chloroform, and Esteaglato de prednisolona; Prednisolone, Stéaglate de; Pred- version of prednisone into prednisolone was not justified. 1 in 248 of ether; soluble in acetone. Store in airtight containers. nisoloni Steaglas. Prednisolone 21-stearoylglycolate. 1. Powell LW, Axelsen E. Corticosteroids in liver disease: studies on the biological conversion of prednisone to prednisolone and Преднизолона Стеаглат plasma protein binding. Gut 1972; 13: 690–6. Prednisolone Metasulfobenzoate Sodium C41H64O8 = 684.9. 2. Madsbad S, et al. Impaired conversion of prednisone to pred- CAS — 5060-55-9. nisolone in patients with liver cirrhosis. Gut 1980; 21: 52–6. (rINNM) ⊗ ATC — A07EA01; C05AA04; D07AA03; H02AB06; 3. Davis M, et al. Prednisone or prednisolone for the treatment of chronic active hepatitis? A comparison of plasma availability. Br Metasulfobenzoato sódico de prednisolona; Natrii Prednisoloni R01AD02; S01BA04; S02BA03; S03BA02. J Clin Pharmacol 1978; 5: 501–5. Metasulfobenzoas; Prednisolone Métasulfobenzoate Sodique; ATC Vet — QA07EA01; QC05AA04; QD07AA03; 4. Frey BM, Frey FJ. Clinical pharmacokinetics of prednisone and Prednisolone Metasulphobenzoate Sodium (BANM); Prednisolo- QH02AB06; QR01AD02; QS01BA04; QS02BA03; prednisolone. Clin Pharmacokinet 1990; 19: 126–46. QS03BA02. ne Sodium Metasulphobenzoate; R-812. Prednisolone 21-(sodi- Inflammatory bowel disease. Symptoms recurred in a pa- um m-sulphobenzoate). tient with Crohn’s disease on changing from conventional to en- Prednisolone Tebutate (BANM, rINNM) ⊗ 1 Натрий Метасульфобензоат Преднизолон teric-coated tablets of prednisolone. This was not an isolated oc- Prednisolone Butylacetate; Prednisolone 21-tert-Butylacetate; currence in the authors’ unit, and it was advocated that only non- C28H31NaO9S = 566.6. Prednisolone, Tébutate de; Prednisolone Tertiary-butylacetate; enteric-coated prednisolone tablets should be used in Crohn’s CAS — 630-67-1. Prednisoloni Tebutas; Tebutato de prednisolona. Prednisolone disease, and that the enteric-coated form be used with caution in ATC — A07EA01; C05AA04; D07AA03; H02AB06; 21-(3,3-dimethylbutyrate). any condition characterised by diarrhoea or a rapid transit time. R01AD02; S01BA04; S02BA03; S03BA02. Преднизолона Тебутат 1. Beattie RM, Walker-Smith JA. Use of enteric coated prednisolo- ATC Vet — QA07EA01; QC05AA04; QD07AA03; ne in Crohn’s disease. Arch Dis Child 1994; 71: 282. C27H38O6,H2O = 476.6. QH02AB06; QR01AD02; QS01BA04; QS02BA03; CAS — 7681-14-3 (anhydrous prednisolone tebutate). QS03BA02. ATC — A07EA01; C05AA04; D07AA03; H02AB06; Interactions R01AD02; S01BA04; S02BA03; S03BA02. The interactions of corticosteroids in general are de- Prednisolone Pivalate (BANM, rINNM) ⊗ ATC Vet — QA07EA01; QC05AA04; QD07AA03; scribed on p.1494. QH02AB06; QR01AD02; QS01BA04; QS02BA03; Pivalato de prednisolona; Prednisolone, pivalate de; Prednisolone QS03BA02. Trimethylacetate; Prednisoloni pivalas; Prednisolonipivalaatti; Pharmacokinetics Pharmacopoeias. In US. Prednisolonpivalat; Prednisolon-pivalát; Prednizolono pivalatas; USP 31 (Prednisolone Tebutate). A white to slightly yellow, hy- For a brief outline of the pharmacokinetics of cortico- Prednizolon-pivalát; Prednizolonu piwalan. Prednisolone 21- groscopic, free-flowing powder, which may show some soft steroids, see p.1495. pivalate. lumps. Is odourless or has not more than a moderate characteris- Prednisolone and prednisone are both readily absorbed Преднизолона Пивалат tic odour. Very slightly soluble in water; sparingly soluble in al- from the gastrointestinal tract, but whereas prednisolo- C H O = 444.6. cohol and in methyl alcohol; soluble in acetone; freely soluble in 26 36 6 chloroform and in dioxan. Store in airtight containers sealed un- ne already exists in a metabolically active form, pred- CAS — 1107-99-9. der nitrogen at a temperature not exceeding 8°. nisone must be converted in the liver to its active me- ATC — A07EA01; C05AA04; D07AA03; H02AB06; tabolite, prednisolone. In general, this conversion is R01AD02; S01BA04; S02BA03; S03BA02. Adverse Effects, Treatment, Withdrawal, rapid so this difference is of little consequence when ATC Vet — QA07EA01; QC05AA04; QD07AA03; QH02AB06; QR01AD02; QS01BA04; QS02BA03; and Precautions seen in the light of intersubject variation in the pharma- QS03BA02. As for corticosteroids in general (see p.1490). cokinetics of prednisolone itself; bioavailability also The symbol † denotes a preparation no longer actively marketed The symbol ⊗ denotes a substance whose use may be restricted in certain sports (see p.vii) 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 as the acetate and 8. Miller PFW, et al. Pharmacokinetics of prednisolone in children caproate esters. with nephrosis. Arch Dis Child 1990; 65: 196–200. Prednisone (BAN, rINN) ⊗

Other esters of prednisolone that have occasionally 1 Uses and Administration Δ -Cortisone; 1,2-Dehydrocortisone; Deltacortisone; Deltade- been used include the farnesil, palmitate, sodium tetra- hydrocortisone; Metacortandracin; NSC-10023; Prednison; Prednisolone is a corticosteroid with mainly glucocor- hydrophthalate, and valeroacetate. Prednisona; Prednisoni; Prednisonum; Prednizon; Prednizonas. ticoid activity (p.1490); 5 mg of prednisolone is equiv- 17α,21-Dihydroxypregna-1,4-diene-3,11,20-trione. alent in anti-inflammatory activity to about 25 mg of Preparations Преднизон cortisone acetate. In general, prednisolone, either in the BP 2008: Gastro-resistant Prednisolone Tablets; Prednisolone Enema; form of the free alcohol or in one of the esterified Prednisolone Sodium Phosphate Eye Drops; Prednisolone Tablets; C21H26O5 = 358.4. USP 31: Chloramphenicol and Prednisolone Ophthalmic Ointment; Gen- forms, is the drug of choice in the UK for conditions in tamicin and Prednisolone Acetate Ophthalmic Ointment; Neomycin and CAS — 53-03-2. which routine systemic corticosteroid therapy is indi- Polymyxin B Sulfates and Prednisolone Acetate Ophthalmic Suspension; ATC — A07EA03; H02AB07. Neomycin Sulfate and Prednisolone Acetate Ointment; Neomycin Sulfate cated (see p.1495), except adrenocortical-deficiency and Prednisolone Acetate Ophthalmic Ointment; Neomycin Sulfate and ATC Vet — QA07EA03; QH02AB07. states for which hydrocortisone with supplementary Prednisolone Acetate Ophthalmic Suspension; Neomycin Sulfate and Pred- nisolone Sodium Phosphate Ophthalmic Ointment; Neomycin Sulfate, Sul- fludrocortisone is preferred. The more potent pituitary- facetamide Sodium, and Prednisolone Acetate Ophthalmic Ointment; suppressant properties of a glucocorticoid such as dex- Prednisolone Acetate Injectable Suspension; Prednisolone Acetate Oph- O amethasone may, however, be required for the diagno- thalmic Suspension; Prednisolone Cream; Prednisolone Sodium Phosphate OH Injection; Prednisolone Sodium Phosphate Ophthalmic Solution; Pred- H C OH sis and management of conditions associated with ad- nisolone Sodium Succinate for Injection; Prednisolone Syrup; Prednisolone 3 Tablets; Prednisolone Tebutate Injectable Suspension; Sulfacetamide Sodi- O renal hyperplasia. um and Prednisolone Acetate Ophthalmic Ointment; Sulfacetamide Sodi- H C H The dose may be expressed in terms of the base, and um and Prednisolone Acetate Ophthalmic Suspension. 3 the following are each equivalent to about 100 mg of Proprietary Preparations (details are given in Part 3) HH prednisolone: Arg.: Cortizul; Ultracortenol; Austral.: Panafcortelone; Predmix; Predsol; Predsolone; Redipred; Solone; Sterofrin; Austria: Aprednislon; Kuhlpred- O • prednisolone acetate 110 mg non; Prednihexal; Rectopred; Solu-Dacortin; Ultracortenol; Belg.: Delta- cortril†; Pred Forte; Prednicortelone†; Solu-Dacortine†; Ultracortenol; • prednisolone caproate 127 mg Braz.: Oftpred; Pred Fort; Pred Mild; Predsim; Prelone; Canad.: Ak-Tate; Pharmacopoeias. In Eur. (see p.vii). US allows the anhydrous Diopred†; Inflamase†; Ophtho-Tate†; Pediapred; Pred Forte; Pred Mild; • prednisolone hydrogen succinate 128 mg SAB-Prednase†; Chile: Pred Forte; Pred Mild†; Predsolets; Preventan†; form or the monohydrate. • prednisolone metasulfobenzoate sodium 157 mg Cz.: Inflanefran†; Linola-H N†; Linola-H-Fett N; Predni-POS; Solu-Decortin Ph. Eur. 6.2 (Prednisone). A white or almost white, crystalline H†; Ultracortenol; Denm.: Pred-Clysma; Ultracortenol; Fin.: Di-Adreson- powder. It shows polymorphism. Practically insoluble in water; • prednisolone pivalate 123 mg F; Pred Forte; Ultracortenol; Fr.: Hydrocortancyl; Solupred; Ger.: Decortin slightly soluble in alcohol and in dichloromethane. Protect from H; Dermosolon; Dontisolon D; duraprednisolon; hefasolon; Infectocor- • prednisolone sodium phosphate 135 mg tikrupp; Inflanefran; Klismacort; Linola-H N; Linola-H-Fett N; Lygal Kopftink- light. tur N; Prectal†; Prednabene; Predni; Predni H; Predni-Ophtal; Predni-POS; USP 31 (Prednisone). It contains one molecule of water of hy- • prednisolone sodium succinate 134 mg Prednigalen; Prednihexal; Prednisolut; Solu-Decortin H; Ultracortenol; Gr.: dration or is anhydrous. A white to practically white, odourless, Adelcort; Adelone; Deltacortril; Prezolon; Hong Kong: Dhasolone; Di- crystalline powder. Very slightly soluble in water; soluble 1 in • prednisolone steaglate 190 mg Adreson-F; Panafcortelone; Pred Forte; Pred Mild; Predenema; Predfoam; Prelone†; Redipred; Ultracortenol; Hung.: Di-Adreson-F; Klismacort†; 150 of alcohol and 1 in 200 of chloroform; slightly soluble in di- • prednisolone tebutate 132 mg Linola-H N; Linola-H-Fett N; Ultracortenol; India: Predone; Wysolone; oxan and in methyl alcohol.