Fludrocortisone 21-acetate

Chemical Name 9-fluoro-11/3,17,21-trihydroxy-pregn-4-ene-3,20-dione acetate Common Name — 

Trade Name Manufacturer Country Year Introduced 

Hydrocortisone acetate is first reacted with phosphorus oxychloride in pyridine to give the 

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Amphotericin B. Amphotericin B (3), an important polyene antibiotic, is administered almost exclusively via the intravenous route and is therefore discussed in more detail under the systemic antimycotics. The vaginal tablets contain 50 mg amphotericin B, and 100 mg tetracycline base per tablet (see also Antibiotics, tetracyclines). The tablets for oral use contain 50 mg amphotericin B, 250 mg tetracycline base, and 125 mg sodium hexametaphosphate. A combination ointment contains 1 mg fludrocortisone acetate, 2.5 mg neomycin, 0.25 mg gramicidin, and 1 g plastibase in addition to 30 mg amphotericin B (see also Antibiotics, peptides). 

Hyperkalemia Restrict dietary intake dialysis May be exacerbated by CSA or TAC or ACEIs, acidosis, or Rl fludrocortisone acetate 0.1 mg orally every day twice daily for refractory hyperkalemia... 

Fludrocortisone acetate 0.05 to 0.2 mg orally once daily can be used to replace mineral ocorticoid loss. If parenteral therapy is needed, 2 to 5 mg of... 

If hyperkalemia is present after the hydrocortisone maintenance phase, additional mineralocorticoid usually is required. Fludrocortisone acetate 0.1 mg orally once daily is the agent of choice. 

Diphenhydramine hydrochloride, 3,173 Diphenoxylate hydrochloride, 7,149 Disulflram, 4, 168 Dobutamine hydrochloride, 8,139 Droperidol, 7,171 Echothiophate iodide, 3,233 Epinephrine, 7, 193 Ergotamine tartrate, 6,113 Erythromycin, 8,139 Erythromycin estolate, 1, 101 2, 573 Estradiol valerate, 4,192 Ethambutol hydrochloride, 7,231 Ethynodiol diacetate, 3,253 Fenoprofen calcium, 6,161 Flucytosine, 5,115 Fludrocortisone acetate, 3, 281 Fluorouracil, 2,221 Fluoxymesterone, 7,251 Fluphenazine enanthate, 2, 245 4,523 Fluphenazine hydrochloride, 2,263 4,518 Gluthethimide,5,139 Gramicidin, 8,179 Griseofulvin, 8,219 Halcinonide, 8,251 Halothane, 1, 119 2,573 Hexetidine, 7,277 Hydralazine hydrochloride, 8,283 Hydroflumethiazide, 7,297 Hydroxyprogesterone caproate, 4,209 Hydroxyzine dihydrochloride, 7,319 Iodipamide, 3,333 Isocarboxazid, 2, 295... 

The natural glucocorticoid is hydrocortisone (cortisol). Semi-synthetic 9a-bromohydrocortisone 21-acetate was found to be less active as an anti-inflammatory agent than hydrocortisone 21-acetate by a factor of three, and 9a-iodohydrocortisone 21-acetate was also less active by a factor of 10. However, 9a-fluorohydrocortisone 21-acetate (fludrocortisone acetate) was discovered to be about 11 times more active than hydrocortisone acetate. Although the bromination sequence shown is equally applicable to chlorine and iodine compounds, fluorine must be introduced indirectly by the P-epoxide formed by base treatment of the 9a-bromo-lip-hydroxy analogue. 

The introduction of a 9a-fluoro substituent increases anti-inflammatory activity, but it increases mineralocor-ticoid activity even more (300x). Fludrocortisone acetate is of little value as an anti-inflammatory, but it is employed as a mineralocorticoid. On the other hand, additional modifications may be employed. Introduction of a 1,2-double bond increases glucocorticoid activity over mineralocorticoid activity, and a 16-methyl group reduces mineralocorticoid activity without affecting glucocorticoid activity. A combination of these three structural modifications gives valuable anti-inflammatory drugs, e.g. betamethasone, with hardly any mineralocorticoid activity. ... 

Flucinolone Acetonide Fludrocortisone Acetate Fludroxycortide Flumethasone Fluocortolone Fluorometholone 9a-Fluoroprednisolone Acetate... 

Fludrocortisone acetate Synthetic corticosteroid with some glucocorticoid and potent mineralocorticoid activity Administered orally to treat primary adrenal insufficiency... 

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