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1542 depends on the dissolution rates of the tablet formula- When given orally 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 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 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 (). 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 , 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 , such es are 5 to 25 mg of , 2 to 30 mg of Linoladiol-H N; NeyNormin N (Revitorgan-Dilutionen N Nr 65)†; NeyTu- as . 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 . 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 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 -; 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 . 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- is preferred. The more potent pituitary- facetamide Sodium, and Prednisolone Acetate Ophthalmic Ointment; suppressant properties of a 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. Prednisone/Tetracosactide 1543

Prednisone Acetate (BANM, rINNM) ⊗ Prolonged use of ophthalmic preparations containing corticoster- oids has caused raised intra-ocular pressure and reduced visual Acetato de prednisona; Prednisone, Acétate de; Prednisoni Ace- O function. tas; Prednizonu octan. Prednisone 21-acetate. Preparations Преднизона Ацетат CH3 O USP 31: Ophthalmic Suspension. C23H28O6 = 400.5. CAS — 125-10-0. O Proprietary Preparations (details are given in Part 3) CH3 Austria: Vexol; Belg.: Vexolon; Braz.: Vexol; Canad.: Vexol; Cz.: Vexol†; ATC — A07EA03; H02AB07. O H H3C CH Denm.: Vexol; Fin.: Vexol; Fr.: Vexol; Ger.: Rimexel; Vexol; Gr.: Vexol; ATC Vet — QA07EA03; QH02AB07. HO 3 Hong Kong: Vexol; Hung.: Vexol†; Irl.: Vexol; Ital.: Vexol; Mex.: Vexol; Neth.: Vexol; Norw.: Vexol; Port.: Vexol; Spain: Vexol; Swed.: Vexol; Pharmacopoeias. In Chin. and Pol. O H3C H Switz.: Vexol; Turk.: Vexol; UK: Vexol; USA: Vexol. Profile H F H Prednisone is a biologically inert corticosteroid that is Suprarenal Cortex ⊗ converted in the liver to the mainly glucocorticoid cor- O Corteza suprarrenal. ticosteroid prednisolone. It has the same chemical rela- HF Profile tionship to prednisolone as cortisone has to hydrocorti- Suprarenal cortex contains a number of compounds the sone. The indications and dosage of prednisone for oral Profile most active of which are , dehydrocorticosterone, use are exactly the same as those for prednisolone (see is a derivative of acetonide (p.1531) hydrocortisone, cortisone, and aldosterone. It has been prepared p.1542, and the chapter introduction, p.1495). that has been applied topically with and ciprocino- from the adrenal glands of oxen. Suprarenal cortex was formerly nide in the management of various skin disorders. used intramuscularly for the treatment of adrenocortical insuffi- In the UK prednisolone has historically been preferred ciency but it has been superseded by hydrocortisone and other to prednisone, on the grounds that it does not require corticosteroids (see p.1498). conversion to the active substance, but in practice this Suprarenal cortex is an ingredient of a wide range of prepara- is rarely significant (see Hepatic Impairment, under Resocortol Butyrate (USAN, rINNM) ⊗ tions, often with other organ extracts or vitamins, promoted for indications ranging from asthenia to liver disorders. Prednisolone, p.1541), and in some countries, such as ALO-2184; Butirato de resocortol; Org-7417; Résocortol, Bu- the USA, prednisone is the drug of choice for many of tyrate de; Resocortoli Butiras; Resocortoli Butyras; Resokortol- Preparations the conditions in which routine systemic corticosteroid butyrat; Resokortolibutyraatti. 11β,17α-Dihydroxy-17-propiony- Proprietary Preparations (details are given in Part 3) therapy is indicated. landrost-4-en-3-one 17-butyrate. Multi-ingredient: Austria: Mobilat; Belg.: Mobilat; Braz.: Broncopinol†; Mobilat; Suprasten†; Canad.: ratio-Heracline; Chile: Mobilat; Cz.: Mobilat; Preparations Резокортола Бутират Fin.: Mobilat; Ger.: Arthrodeformat P†; Mobilat†; Hong Kong: Mobilat†; Philipp.: Mobilat; Pol.: Mobilat; Singapore: Mobilat†; Spain: Neurocata- USP 31: Prednisone Oral Solution; Prednisone Tablets. C26H38O5 = 430.6. vin Dexa†; Pleocortex B6†; Rubrocortin†; Thai.: Mobilat. Proprietary Preparations (details are given in Part 3) CAS — 76675-97-3 (resocortol); 76738-96-0 (resocortol Arg.: Meticorten; Metilpres; Prednipirine; Prenisonal†; Austral.: Panafcort; butyrate). Predsone; Sone; Belg.: Prednicort†; Braz.: Artinizona; Becortem; Corti- ATC Vet — QD07AC90. corten; Meticorten; Metilen†; Precortil; Predicorten†; Predison; Prednax; (BAN, rINN) Predval; Canad.: Winpred; Chile: Bersen; Cortiprex; Meticorten; Procion; Tetracosactide ⊗ Cz.: Rectodelt; Fr.: Cortancyl; Ger.: Decortin; Predni Tablinen; Rectodelt; α1–24-Corticotrophin; β1–24-Corticotrophin; Cosyntropin (USAN); Hung.: Rectodelt; Indon.: Inflason; Ital.: Deltacortene; Mex.: Ednapron; Meprosona-F; Meticorten; Norapred; Nosipren†; Ofisolona†; Predicor†; CH3 Tetracosactida; Tétracosactide; Tetracosactido; Tetracosactidum; Prednidib; Premagnol†; Philipp.: Bioster; Oracort; Orasone; Pred; Prolix; Tetracosactrin; Tetrakosaktid; Tetrakosaktidi; Tetrakosaktrin; O Steerometz; Pol.: Encorton; Port.: Meticorten; S.Afr.: Meticorten; Panaf- Tetrakozaktidas. Corticotrophin-(1–24)-tetracosapeptide; Ser- cort; Predeltin; Pulmison; Spain: Dacortin; Swed.: Deltison; USA: Delta- H H C sone; Liquid Pred; Meticorten; Panasol-S; Sterapred; Venez.: Corticorp†; 3 OH Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys- Meticorten; Vitazon†. HO Arg-Arg-Pro-Val-Lys-Val-Tyr-Pro. Multi-ingredient: Arg.: Peganix; Austria: Fluorex Plus; Oleomycetin- H3C H Тетракозактид Prednison; Chile: Alerzona; Ger.: Oleomycetin-Prednison†; Mex.: Barige- sic; Pre Clor; Spain: Coliriocilina Prednisona; Fiacin; Kanafosal Predni; Pred- C136H210N40O31S = 2933.4. nisona Neomicina. H H CAS — 16960-16-0 (tetracosactide); 22633-88-1 (tetra- cosactide hexaacetate); 60189-34-6 (tetracosactide x ac- O etate). ATC — H01AA02. (BAN, rINN) ⊗ (resocortol) ATC Vet — QH01AA02. 16-Methyleneprednisolone; Prednilideeni; Prednilideno; Pred- Pharmacopoeias. In Eur. (see p.vii). nyliden; Prednylidène; Prednylidenum. 11β,17α,21-Trihydroxy- Profile 16-methylenepregna-1,4-diene-3,20-dione. Ph. Eur. 6.2 (Tetracosactide). A synthetic tetracosapeptide in Resocortol butyrate is a corticosteroid that is used topically in which the sequence of amino acids is the same as that of the first Преднилиден veterinary medicine. 24 residues of human corticotropin. It is available as an acetate C22H28O5 = 372.5. and contains water. It increases the rate at which corticoid hor- CAS — 599-33-7. mones are secreted by the adrenal gland. The potency is not less ATC — H02AB11. than 800 units/mg. A white or yellow, amorphous powder. Spar- ATC Vet — QH02AB11. Rimexolone (BAN, USAN, rINN) ⊗ ingly soluble in water. Store under nitrogen at a temperature of 2° to 8°. Protect from light. Org-6216; Rimeksolon; Rimeksoloni; Rimexolon; Rimexolona; OH Rimexolonum; Trimexolone. 11β-Hydroxy-16α,17α-dimethyl- 17β-propionylandrosta-1,4-dien-3-one. Adverse Effects, Withdrawal, and Precau- O tions Римексолон As for Corticotropin, p.1523. Although hypersensitivi- H H3C HO OH C24H34O3 = 370.5. ty reactions, including anaphylaxis, may occur with the CAS — 49697-38-3. use of tetracosactide, it is reported to be less immuno- H C H CH 3 2 ATC — H02AB12; S01BA13. genic than corticotropin; US licensed product informa- ATC Vet — QH02AB12; QS01BA13. tion suggests that patients with a history of hypersensi- H H tivity to corticotropin may tolerate tetracosactide. In O the UK, however, previous hypersensitivity to cortico- CH3 tropin or to tetracosactide is considered a contra-indi- Profile O cation to tetracosactide use. Tetracosactide is also con- Prednylidene is a corticosteroid that has been used for its gluco- tra-indicated in patients with a history of allergic corticoid activity similarly to prednisolone (see p.1540). It has H H3C HO CH3 been given orally as the free alcohol and by injection as the di- disorders such as asthma. ethylaminoacetate hydrochloride. H3C H CH3 Since hypersensitivity reactions may occur up to 1 Preparations hour after injection, sufficient time should be allowed Proprietary Preparations (details are given in Part 3) H H for recovery after use at the hospital or surgery. Self- Ger.: Decortilen†. administration is not recommended. O Interactions Pharmacopoeias. In US. As for Corticosteroids, p.1494. Procinonide (USAN, rINN) ⊗ USP 31 (Rimexolone). A white to off-white powder. Freely sol- Procinonida; Procinonidum; RS-2362. (6α,11β,16α)-6,9-Dif- uble in chloroform; sparingly soluble in methyl alcohol. luoro-11-hydroxy-16,17-[(1-methylethylidene)bis(oxy)]-21-(1- Pharmacokinetics oxopropoxy)-pregna-1,4-diene-3,20-dione. Profile On intravenous injection tetracosactide exhibits tripha- Rimexolone is a corticosteroid applied topically to the eye for its Процинонид glucocorticoid activity (see p.1490) in the treatment of inflam- sic pharmacokinetics. It is rapidly eliminated from C27H34F2O7 = 508.6. matory eye disorders including uveitis (p.1515) and postopera- plasma, mostly by distribution to the adrenal glands CAS — 58497-00-0. tive inflammation. It is used as a 1% suspension. and kidneys. It is metabolised by serum endopeptidases 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)