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Home , Formocortal, Hydrocortisone buteprate, Hydrocortisone phosphate

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Halcinonide (BAN, USAN, rINN) ⊗ Preparations (BANM, USAN, rINNM) ⊗ Alcinonide; Halcinonid; Halcinónida; Halcinonidum; Halsinonid; Proprietary Preparations (details are given in Part 3) Butirato de hidrocortisona; Butyrate; Hidrokortizon Halsinonidi; SQ-18566. 21-Chloro-9α-fluoro-11β-hydroxy- Austria: Sicorten; Belg.: Sicorten†; Ger.: Sicorten†; Hong Kong: Si- Bütirat; Hydrocortisone, Butyrate d’; Hydrocortisoni Butiras. Hy- corten; Neth.: Sicorten†; Port.: Sicorten†; Spain: Sicorten; Switz.: Si- 16α,17α-isopropylidenedioxypregn-4-ene-3,20-dione. corten; Turk.: Sicorten. drocortisone 17α-butyrate. Гальцинонид Multi-ingredient: Ger.: Sicorten Plus; Hong Kong: Sicorten Plus†; Isra- Гидрокортизона Бутират el: Sicorten Plus†; Port.: Sicorten Plus†; Spain: Sicorten Plus; Switz.: Si- C24H32ClFO5 = 455.0. corten Plus; Venez.: Sicorten Plus†. C25H36O6 = 432.5. CAS — 3093-35-4. CAS — 13609-67-1. ATC — D07AD02. ATC — D07AB02. ATC Vet — QD07AD02. ATC Vet — QD07AB02. Hydrocortisone (BAN, rINN) ⊗ Pharmacopoeias. In Chin., Jpn, and US. Anti-inflammatory Hormone; Compound F; Cortisol; Hidrocor- O CH3 USP 31 (Hydrocortisone Butyrate). A white to practically Cl tisona; Hidrokortizon; Hidrokortizonas; Hydrocortisonum; Hy- white, practically odourless crystalline powder. Practically insol- CH H3C O 3 drokortison; Hydrokortisoni; Hydrokortyzon; 17-Hydroxycorti- uble in water; soluble in alcohol, in acetone, and in methyl alco- HO O costerone; NSC-10483. 11β,17α,21-Trihydroxypregn-4-ene- hol; freely soluble in chloroform; slightly soluble in ether. 3,20-dione. H3CH Гидрокортизон Hydrocortisone Cipionate (BANM, rINNM) ⊗ C H O = 362.5. FH 21 30 5 Cipionato de hidrocortisona; Cortisol Cypionate; Hydrocorti- CAS — 50-23-7. O sone, Cipionate d’; Hydrocortisone Cyclopentylpropionate; Hy- ATC — A01AC03; A07EA02; C05AA01; D07AA02; drocortisone Cypionate; Hydrocortisoni Cipionas. Hydrocorti- H02AB09; S01BA02; S02BA01. sone 21-(3-cyclopentylpropionate). Pharmacopoeias. In Chin. and US. USP 31 (). A white to off-white, odourless, crystal- ATC Vet — QA01AC03; QA07EA02; QC05AA01; Гидрокортизона Ципионат line powder. Insoluble in water and in hexanes; slightly soluble QD07AA02; QD07XA01; QH02AB09; QS01BA02; C H O = 486.6. in alcohol and in ether; soluble in acetone and in chloroform. QS01CB03; QS02BA01. 29 42 6 CAS — 508-99-6. Profile ATC — A01AC03; A07EA02; C05AA01; D07AA02; Halcinonide is a used topically for its glucocorti- O H02AB09; S01BA02; S02BA01. coid activity (p.1490) in the treatment of various skin disorders. OH It is usually used as a 0.1% cream, lotion, or ointment. ATC Vet — QA01AC03; QA07EA02; QC05AA01; H3C OH QD07AA02; QH02AB09; QS01BA02; QS02BA01. When applied topically, particularly to large areas, when the skin HO is broken, or under occlusive dressings, may be H CH absorbed in sufficient amounts to cause systemic effects 3 Hydrocortisone Hydrogen Succinate (p.1490). The effects of topical corticosteroids on the skin are (BANM, rINNM) ⊗ described on p.1492. For recommendations concerning the cor- HH rect use of corticosteroids on the skin, and a rough guide to the Cortisol Hemisuccinate; Hidrogenosuccinato de hidrocortisona; clinical potencies of topical corticosteroids, see p.1497. O Hidrokortizon-hidrogén-szukcinát; Hidrokortizono hemisukcina- tas; Hydrocortisone Hemisuccinate; Hydrocortisone, Hémisuc- Preparations Pharmacopoeias. In Chin., Eur. (see p.vii), Int., Jpn, and US. cinate d’; Hydrocortisone, hydrogénosuccinate d’; Hydrocorti- USP 31: Halcinonide Cream; Halcinonide Ointment; Halcinonide Topical Ph. Eur. 6.2 (Hydrocortisone). A white or almost white, crys- sone Succinate; Hydrocortisoni Hemisuccinas; Hydrocortisoni Solution. talline powder. It shows polymorphism. Practically insoluble in hydrogenosuccinas; Hydrokortison-hydrogen-sukcinát; Hy- Proprietary Preparations (details are given in Part 3) water; sparingly soluble in alcohol and in acetone; slightly solu- drokortisonivetysuksinaatti; Hydrokortisonvätesuccinat. Hydro- Austria: Halog; Braz.: Halog; Canad.: Halog; Cz.: Betacorton; Ger.: Ha- ble in dichloromethane. Protect from light. 21-(hydrogen succinate). log†; Hong Kong: Halog; India: Cortilate; Indon.: Halog; Ital.: Halciderm; USP 31 (Hydrocortisone). A white to practically white, odour- Mex.: Dermalog; Spain: Halog; Switz.: Betacortone; Turk.: Volog; UK: less, crystalline powder. Very slightly soluble in water and in Гидрокортизона Гемисукцинат Halciderm†; USA: Halog; Venez.: Halog. ether; soluble 1 in 40 of alcohol and 1 in 80 of acetone; slightly C25H34O8 = 462.5. Multi-ingredient: Cz.: Betacorton S; Betacorton U; Ger.: Halog Tri†; soluble in chloroform. Store at a temperature of 25°, excursions CAS — 2203-97-6 (anhydrous hydrocortisone hydrogen India: Cobederm-H; Cortilate-S; Ital.: Anfocort; Halciderm; Halciderm permitted between 15° and 30°. Combi; Mex.: Dermalog-C; Switz.: Betacortone; Betacortone S; Turk.: succinate); 83784-20-7 (hydrocortisone hydrogen succi- Betacorton; Venez.: Halcicomb; Halog. nate monohydrate). (BANM, rINNM) ⊗ ATC — A01AC03; A07EA02; C05AA01; D07AA02; Acetato de hidrocortisona; Cortisol Acetate; Hidrokortizon H02AB09; S01BA02; S02BA01. ATC Vet — QA01AC03; QA07EA02; QC05AA01; (rINN) ⊗ Asetat; Hidrokortizon-acetát; Hidrokortizono acetatas; Hydro- cortisone, acétate d’; Hydrocortisoni acetas; Hydrokortisonace- QD07AA02; QH02AB09; QS01BA02; QS02BA01. C-48401-Ba; Halometason; Halometasona; Halométasone; tat; Hydrokortison-acetát; Hydrokortisoniasetaatti; Hydroko- Pharmacopoeias. In Eur. (see p.vii) and Jpn. US allows the Halometasoni; Halometasonum; Halometazon; Halomethasone. rtyzonu octan. Hydrocortisone 21-acetate. anhydrous form or the monohydrate. 2-Chloro-6α,9-difluoro-11β,17,21-trihydroxy-16α-methylpreg- Гидрокортизона Ацетат Ph. Eur. 6.2 (Hydrocortisone Hydrogen Succinate). A white or na-1,4-diene-3,20-dione. almost white, hygroscopic powder. Practically insoluble in wa- C H O = 404.5. Галометазон 23 32 6 ter; freely soluble in dehydrated alcohol and in acetone; dissolves CAS — 50-03-3. C H ClF O = 444.9. in dilute solutions of alkali carbonates and alkali hydroxides. 22 27 2 5 ATC — A01AC03; A07EA02; C05AA01; D07AA02; Store in airtight containers. Protect from light. CAS — 50629-82-8. H02AB09; S01BA02; S02BA01. USP 31 (Hydrocortisone Hemisuccinate). It contains one mole- ATC — D07AC12. ATC Vet — QA01AC03; QA07EA02; QC05AA01; cule of water of hydration or is anhydrous. Store in airtight con- ATC Vet — QD07AC12. QD07AA02; QH02AB09; QS01BA02; QS02BA01. tainers. NOTE. HCOR is a code approved by the BP 2008 for use on single unit doses of eye drops containing hydrocortisone acetate where Hydrocortisone Sodium Phosphate OH the individual container may be too small to bear all the appro- priate labelling information. (BANM, rINNM) ⊗ O Pharmacopoeias. In Chin., Eur. (see p.vii), Int., Jpn, US, and Cortisol Sodium Phosphate; Fosfato sódico de hidrocortisona; H H3C Hydrocortisone, Phosphate Sodique d’; Natrii Hydrocortisoni HO OH Viet. Ph. Eur. 6.2 (Hydrocortisone Acetate). A white or almost Phosphas. Hydrocortisone 21-(disodium orthophosphate). CH 3 white, crystalline powder. Practically insoluble in water; slightly H3C H Натрия Гидрокортизона Фосфат Cl H soluble in dehydrated alcohol and in dichloromethane. Protect from light. C H Na O P = 486.4. F H 21 29 2 8 USP 31 (Hydrocortisone Acetate). A white to practically white, CAS — 6000-74-4. O odourless, crystalline powder. Insoluble in water; soluble 1 in 230 of alcohol and 1 in 200 of chloroform. ATC — A01AC03; A07EA02; C05AA01; D07AA02; HF H02AB09; S01BA02; S02BA01. ATC Vet — QA01AC03; QA07EA02; QC05AA01; (BANM, rINNM) ⊗ Profile QD07AA02; QH02AB09; QS01BA02; QS02BA01. Halometasone is a corticosteroid used topically for its glucocor- Buteprato de hidrocortisona; Hydrocortisone, Butéprate d’; Hy- Pharmacopoeias. In Br., Jpn, and US. ticoid activity (p.1490) in the treatment of various skin disorders. drocortisone Butyrate Propionate; Hydrocortisone Probutate BP 2008 (Hydrocortisone Sodium Phosphate). A white or al- It is usually used as a cream containing 0.05% of halometasone (USAN); Hydrocortisoni Butepras; TS-408. Hydrocortisone 17- most white, hygroscopic powder. Freely soluble in water; practi- monohydrate. butyrate 21-propionate. cally insoluble in dehydrated alcohol and in chloroform. A 0.5% When applied topically, particularly to large areas, when the skin Гидрокортизона Бутепрат solution in water has a pH of 7.5 to 9.0. Protect from light. is broken, or under occlusive dressings, corticosteroids may be USP 31 (Hydrocortisone Sodium Phosphate). A white to light C H O = 488.6. absorbed in sufficient amounts to cause systemic effects 28 40 7 yellow, odourless or practically odourless, exceedingly hygro- (p.1490). The effects of topical corticosteroids on the skin are CAS — 72590-77-3. scopic, powder. Soluble 1 in 1.5 of water; slightly soluble in al- described on p.1492. For recommendations concerning the cor- ATC — D07AB11. cohol; practically insoluble in chloroform, in dioxan, and in rect use of corticosteroids on the skin, see p.1497. ATC Vet — QD07AB11. ether. Store in airtight containers. 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) 1536 Corticosteroids

Hydrocortisone Sodium Succinate um succinate esters is rapid, while absorption of ly to be less rapid than that observed after intravenous (BANM, rINNM) ⊗ hydrocortisone free alcohol and its lipid-soluble esters doses. Corticosteroids are considered to be of second- Cortisol Sodium Succinate; Hydrocortisone, Succinate Sodique is slower. Absorption of hydrocortisone acetate after ary value in anaphylactic shock because of their rela- d’; Hydrocortisoni Natrii Succinas; Hydrokortyzonu bursztynianu intra-articular or soft-tissue injection is also slow. Hy- tively slow onset of action, but intravenous hydrocorti- sól sodowa; Succinato sódico de hidrocortisona. Hydrocorti- drocortisone is absorbed through the skin, particularly sone may be a useful adjunct to adrenaline to prevent sone 21-(sodium succinate). in denuded areas. further deterioration in severely affected patients. Гидрокортизона Натрия Сукцинат Hydrocortisone is metabolised in the liver and most In patients with adrenal deficiency states supplementa- C25H33NaO8 = 484.5. CAS — 125-04-2. body tissues to hydrogenated and degraded forms such ry corticosteroid therapy may be necessary during ATC — A01AC03; A07EA02; C05AA01; D07AA02; as tetrahydrocortisone and tetrahydrocortisol. These some surgical operations and hydrocortisone sodium H02AB09; S01BA02; S02BA01. are excreted in the urine, mainly conjugated as glu- succinate or sodium phosphate may be given intramus- ATC Vet — QA01AC03; QA07EA02; QC05AA01; curonides, with a very small proportion of unchanged cularly or intravenously before surgery. Various regi- QD07AA02; QH02AB09; QS01BA02; QS02BA01. hydrocortisone. Hydrocortisone readily crosses the mens have been proposed (see also Surgery, p.1497). Pharmacopoeias. In Chin., Int., It., Jpn., Pol., and US. placenta. USP 31 (Hydrocortisone Sodium Succinate). A white or nearly In patients taking more than 10 mg of oral prednisolo- white, odourless, hygroscopic, amorphous solid. Very soluble in ne or its equivalent daily, the BNF recommends the fol- water and in alcohol; very slightly soluble in acetone; insoluble Uses and Administration lowing regimen: in chloroform. Store in airtight containers. Protect from light. Hydrocortisone is a corticosteroid with both glucocor- • minor surgery under general anaesthesia, either the ticoid and to a lesser extent mineralocorticoid activity usual oral corticosteroid dose on the morning of sur- (BANM, USAN, rINNM) ⊗ (p.1490). As cortisol it is the most important of the pre- gery or hydrocortisone 25 to 50 mg (usually as the Cortisol Valerate; Hydrocortisone, Valérate d’; Hydrocortisoni dominantly secreted by the ad- sodium succinate) intravenously at induction; the Valeras; Valerato de hidrocortisona. Hydrocortisone 17-valer- renal cortex. Hydrocortisone is used, usually with a usual oral corticosteroid dose is resumed after sur- ate. more potent mineralocorticoid, for replacement thera- gery Гидрокортизона Валерат py in adrenocortical insufficiency (p.1498). It may also • moderate or major surgery, the usual oral corticos- C26H38O6 = 446.6. be used for its glucocorticoid properties in other condi- CAS — 57524-89-7. teroid dose on the morning of surgery, plus hydro- ATC — A01AC03; A07EA02; C05AA01; D07AA02; tions for which corticosteroid therapy is indicated cortisone 25 to 50 mg intravenously at induction, H02AB09; S01BA02; S02BA01. (p.1495) but drugs with fewer mineralocorticoid ef- ATC Vet — QA01AC03; QA07EA02; QC05AA01; and followed by similar doses of hydrocortisone 3 fects tend to be preferred for the long-term systemic times daily, for 24 hours after moderate surgery and QD07AA02; QH02AB09; QS01BA02; QS02BA01. therapy of auto-immune and inflammatory disease. Pharmacopoeias. In US. 48 to 72 hours after major surgery; the usual corti- The dose may be expressed in terms of the base, and costeroid dose is resumed once hydrocortisone in- Adverse Effects, Treatment, Withdrawal, the following are each equivalent to about 100 mg of jections are stopped. hydrocortisone: and Precautions For local injection into soft tissues hydrocortisone is As for corticosteroids in general (see p.1490). • hydrocortisone acetate 112 mg usually used in the form of the sodium phosphate or When applied topically, particularly to large areas, • hydrocortisone buteprate 135 mg sodium succinate esters; doses in terms of hydrocorti- when the skin is broken, or under occlusive dressings, • hydrocortisone butyrate 119 mg sone are usually 100 to 200 mg. For intra-articular in- corticosteroids may be absorbed in sufficient amounts • hydrocortisone cipionate 134 mg jection hydrocortisone acetate is usually used in doses to cause systemic effects. Prolonged use of ophthalmic • hydrocortisone hydrogen succinate 128 mg of 5 to 50 mg depending upon the size of the joint. preparations containing corticosteroids has caused • hydrocortisone sodium phosphate 134 mg For topical application in the treatment of various raised intra-ocular pressure and reduced visual func- • hydrocortisone sodium succinate 134 mg skin disorders hydrocortisone and the acetate, bute- tion. prate, butyrate, and valerate esters are normally em- • hydrocortisone valerate 123 mg Effects on fluid and electrolyte balance. A report of ployed in creams, ointments, or lotions. Concentra- marked hypokalaemia and hypomagnesaemia associated with However, esterification generally alters potency and tions usually used have ranged from 0.1 to 2.5%. high-dose intravenous hydrocortisone therapy in an alcoholic pa- compounds with equivalent hydrocortisone content Although it is considered that hydrocortisone has few- 1 tient with suspected immune thrombocytopenia. Cardiac ar- may not have equivalent clinical effect. er adverse effects on the skin and is less liable to cause rhythmias developed, and prolonged infusion of magnesium and potassium was required to restore normal plasma concentrations. When given orally hydrocortisone free alcohol is usu- adrenal suppression than the more potent topical corti- 1. Ramsahoye BH, et al. The mineralocorticoid effects of high dose ally used; the cipionate ester is used in some formula- costeroids (see p.1497 for a rough guide to the clinical hydrocortisone. BMJ 1995; 310: 656–7. tions. For replacement therapy in acute or chronic potencies of topical corticosteroids), it should be borne Effects on the nervous system. For reports and comments adrenocortical insufficiency the normal requirement is in mind that this property may be considerably modi- on paraesthesia or perineal irritation associated with hydrocorti- 20 to 30 mg daily (usually taken in 2 doses, the larger fied both by the type of formulation or vehicle used and sone sodium phosphate given intravenously, see p.1492. in the morning and the smaller in the early evening, to by the type of esterification present; other factors that Hypersensitivity and anaphylaxis. References to hypersen- mimic the circadian rhythm of the body). Children may may also influence the degree of absorption include the sitivity reactions and anaphylaxis associated with the intrave- be given 400 to 800 micrograms/kg daily in 2 or 3 di- site of application, use of an occlusive dressing, the de- nous use of hydrocortisone;1-7 topical application can also result in hypersensitivity.8 vided doses, adjusted as needed. Additional sodium gree of skin damage, and the size of the area to which 1. Chan CS, et al. Hydrocortisone-induced anaphylaxis. Med J Aust chloride may be required if there is defective aldoster- the preparation is applied. 1984; 141: 444–6. one secretion, but mineralocorticoid activity is usually Hydrocortisone or its esters are also available in a vari- 2. Seale JP. Anaphylactoid reaction to hydrocortisone. Med J Aust 1984; 141: 446. supplemented by acetate orally. Simi- ety of other dosage forms including those for ophthal- 3. Corallo CE, Sosnin M. Bronchospasm, tachycardia following in- lar regimens have also been used to correct glucocorti- mic, aural, dental, and rectal application, for use in al- travenous hydrocortisone. Aust J Hosp Pharm 1985; 15: 103–4. coid deficiency in the salt-losing form of congenital ad- 4. Al Mahdy H, Hall M. Anaphylaxis and hydrocortisone. Ann In- lergic and inflammatory disorders. tern Med 1988; 108: 487–8. renal hyperplasia (p.1502). Other esters of hydrocortisone that have occasionally 5. Fulcher DA, Katelaris CH. Anaphylactoid reaction to intrave- Hydrocortisone may be given intravenously, by slow nous hydrocortisone sodium succinate: a case report and litera- been used include the aceponate, glycyrrhetinate, and ture review. Med J Aust 1991; 154: 210–14. injection or infusion, in the form of a water-soluble propionate. Esters such as the aceponate may show 6. Kawane H. Anaphylactoid reaction to intravenous hydrocorti- derivative such as hydrocortisone sodium succinate or sone sodium succinate. Med J Aust 1991; 154: 782. modified topical activity. 7. Currie GP, et al. An unexpected response to intravenous hydro- hydrocortisone sodium phosphate when a rapid effect cortisone succinate in an asthmatic patient. Br J Clin Pharmacol is required in emergencies: such conditions are acute Preparations 2005; 60: 342. adrenocortical insufficiency caused by Addisonian or BP 2008: Gentamicin and Hydrocortisone Acetate Ear Drops; Hydrocor- 8. Wilkinson SM, et al. Hydrocortisone: an important cutaneous al- tisone Acetate and Neomycin Ear Drops; Hydrocortisone Acetate and Ne- lergen. Lancet 1991; 337: 761–2. post-adrenalectomy crises, by the abrupt accidental omycin Eye Drops; Hydrocortisone Acetate and Neomycin Eye Ointment; withdrawal of therapy in corticosteroid-treated pa- Hydrocortisone Acetate Cream; Hydrocortisone Acetate Injection; Hydro- Ointment; Hydrocortisone and Clioquinol Cream; Hy- Interactions tients, or by the inability of the adrenal glands to cope drocortisone and Clioquinol Ointment; Hydrocortisone and Neomycin The interactions of corticosteroids in general are de- with increased stress in such patients; certain allergic Cream; Hydrocortisone Cream; Hydrocortisone Ointment; Hydrocorti- sone Oromucosal Tablets; Hydrocortisone Sodium Phosphate Injection; scribed on p.1494. emergencies such as anaphylaxis; acute severe asthma Hydrocortisone Sodium Succinate Injection; and Hydrocorti- (status asthmaticus—see also p.1108); and shock. The sone Acetate Cream; Miconazole and Hydrocortisone Cream; Miconazole and Hydrocortisone Ointment; Pharmacokinetics usual dose is the equivalent of 100 to 500 mg of hydro- USP 31: Chloramphenicol and Hydrocortisone Acetate for Ophthalmic For a brief account of the pharmacokinetics of corti- cortisone, repeated 3 or 4 times in 24 hours, according Suspension; Chloramphenicol, Polymyxin B Sulfate, and Hydrocortisone Acetate Ophthalmic Ointment; Clioquinol and Hydrocortisone Cream; costeroids, see p.1495. to the severity of the condition and the patient’s re- Clioquinol and Hydrocortisone Ointment; Colistin and Neomycin Sulfates Hydrocortisone is readily absorbed from the gastroin- sponse. Children up to 1 year of age may be given and Hydrocortisone Acetate Otic Suspension; Hydrocortisone Acetate Cream; Hydrocortisone Acetate Injectable Suspension; Hydrocortisone testinal tract and peak blood concentrations are at- 25 mg, those aged 1 to 5 years 50 mg, and those aged Acetate Lotion; Hydrocortisone Acetate Ointment; Hydrocortisone Ace- tained in about an hour. The plasma half-life is about 6 to 12 years 100 mg. Fluids and electrolytes should be tate Ophthalmic Ointment; Hydrocortisone Acetate Ophthalmic Suspen- sion; Hydrocortisone and Acetic Acid Otic Solution; Hydrocortisone Bu- 100 minutes. It is more than 90% bound to plasma pro- given as necessary to correct any associated metabolic tyrate Cream; Hydrocortisone Cream; Hydrocortisone Gel; teins. Following intramuscular injection, the absorp- disorder. Similar doses to those specified above may Hydrocortisone Injectable Suspension; Hydrocortisone Lotion; Hydrocor- tisone Ointment; Hydrocortisone Rectal Suspension; Hydrocortisone So- tion of the water-soluble sodium phosphate and sodi- also be given intramuscularly but the response is like- dium Phosphate Injection; Hydrocortisone Sodium Succinate for Injection;