Fludrocortison-21-acetat

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H361：Kann vermutlich die Fruchtbarkeit beeinträchtigen oder das Kind im Mutterleib schädigen.

• Sicherheit

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

Fludrocortisone acetate Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R63:Kann das Kind im Mutterleib möglicherweise schädigen.

• S-Sätze Betriebsanweisung:

  S22:Staub nicht einatmen.
  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.

• Beschreibung

  Fludrocortisone acetate is the acetate form of the synthetic corticosteroid fludrocortisone, which is a mineralocorticoid receptor agonist. Fludrocortisone acetate (0.1-5 μg/animal) promotes sodium retention in rats in a dose-dependent manner with 37% of sodium excreted compared with control when used at a dose of 5 μg/animal. Formulations containing fludrocortisone acetate have been used in the treatment of Addison’s disease.

• Chemische Eigenschaften

  Crystalline Solid

• Originator

  Alflorone Acetate,MSD,US,1954

• Definition

  ChEBI: An acetate ester resulting from the formal condensation of the primary hydroxy group of fludrocortisone with acetic acid. A synthetic corticosteroid, it has glucocorticoid actions about 10 times as potent as hydrocortisone, while its mineralocorticoid acti ns are over 100 times as potent. It is used in partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's disease and for the treatment of salt-losing adrenal hyperplasia.

• Manufacturing Process

  Hydrocortisone acetate is first reacted with phosphorus oxychloride in pyridine to give the corresponding olefin. Then a sequence consisting of hypobromous acid addition, ring closure to the epoxide and ring opening with hydrogen fluoride gives fludrocortisone acetate. Preparation of a crystalline product is described then in US Patent 2,957,013.

• Trademarks

  Florinef (King).

• Therapeutic Function

  9-Fluoro-11β,17,21-trihydroxy-pregn-4-ene-3,20-dione acetate

• Allgemeine Beschreibung

  Fludrocortisone acetate,21-acetyloxy-9-fluoro-11β,17-dihydroxypregn-4-ene-3,20-dione, 9α-fluorohydrocortisone (Florinef Acetate), isused only for the treatment of Addison disease and for inhibitionof endogenous adrenocortical secretions. It has up to about 800 times the MC activity of hydrocortisone and about 11 times the GC activity. Its potent activity stimulated the synthesis and study of the many fluorinated steroids. Although its great salt-retaining activity limits its use to Addison disease, it has sufficient GC activity that in some cases of the disease, additional GCs need not be prescribed.

• Biochem/physiol Actions

  Fludrocortisone acetate is a synthetic corticosteroid with more mineralocorticoid than glucocorticoid activity.

• Clinical Use

  Fludrocortisone acetate is mineralocorticoid. It is used as a replacement therapy in adrenal insufficiency. Fludrocortisone acetate tablets USP, 0.1 mg are indicated as partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's disease and for the treatment of salt-losing adrenogenital syndrome. ludrocortisone is a man-made form of a natural substance (glucocorticoid) made by the body. It is used along with other medications (such as hydrocortisone) to treat low glucocorticoid levels caused by disease of the adrenal gland (such as Addison's disease, adrenocortical insufficiency, salt-losing adrenogenital syndrome). Glucocorticoids are needed in many ways for the body to function well. They are important for salt and water balance and keeping blood pressure normal. They are also needed to break down carbohydrates in your diet.

• Veterinary Drugs and Treatments

  Fludrocortisone is used in small animal medicine for the treatment of adrenocortical insufficiency (Addison’s disease). It can also be used as adjunctive therapy in hyperkalemia.
  Additionally, in humans, fludrocortisone has been used in saltlosing, congenital adrenogenital syndrome and in patients with severe postural hypotension.

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Aldesleukin: avoid concomitant use.
  Antibacterials: metabolism accelerated by rifamycins; metabolism possibly inhibited by erythromycin; possibly reduce isoniazid concentration.
  Anticoagulants: efficacy of coumarins and phenindione may be altered.
  Antiepileptics: metabolism accelerated by carbamazepine, fosphenytoin, phenobarbital, phenytoin and primidone.
  Antifungals: increased risk of hypokalaemia with amphotericin - avoid; metabolism possibly inhibited by itraconazole and ketoconazole.
  Antivirals: concentration possibly increased by ritonavir.
  Cobicistat: concentration of fludrocortisone increased.
  Vaccines: high dose corticosteroids can impair immune response to vaccines - avoid concomitant use with live vaccines

• Stoffwechsel

  Fludrocortisone is hydrolysed to produce the nonesterified alcohol. In human volunteers, excretion through urine was about 80%, and it was concluded that about 20% were excreted by a different route. It is likely that, as for the metabolism of other steroids, excretion into the bile is balanced by re-absorption in the intestine and some part is excreted with the faeces

Fludrocortisone acetate Upstream-Materialien And Downstream Produkte

Fludrocortison-21-acetat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(224)Suppliers

514-36-3, Fludrocortisone acetate Verwandte Suche: