Prednisolon

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Sicherheit

  P201：Vor Gebrauch besondere Anweisungen einholen.

  P202：Vor Gebrauch alle Sicherheitshinweise lesen und verstehen.

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

  P308+P313：BEI Exposition oder falls betroffen: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

  P405：Unter Verschluss aufbewahren.

  P501：Inhalt/Behälter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

Prednisolone Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R22:Gesundheitsschädlich beim Verschlucken.
  R34:Verursacht Verätzungen.
  R11:Leichtentzündlich.

• S-Sätze Betriebsanweisung:

  S22:Staub nicht einatmen.
  S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
  S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
  S16:Von Zündquellen fernhalten - Nicht rauchen.

• Beschreibung

  Prednisolone is the active metabolite of the synthetic corticosteroid prednisone , which is used in the suppression of inflammation and autoimmunity, as well as in other conditions. It alters gene expression through both the glucocorticoid and mineralocorticoid receptors.

• Chemische Eigenschaften

  Crystalline Solid. soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of prednisone in these solvents is approximately 3, 30, and 25 mg/ml, respectively.

• Originator

  Sterane, Pfizer ,US ,1955

• Verwenden

  Prednisolone is used for the same indications as all corticosteroids: rheumatism, polyarthritis, bronchial asthma, neurodermatitis, and eczema.

• Definition

  ChEBI: Prednisolone is a glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone. It has a role as an adrenergic agent, an anti-inflammatory drug, an antineoplastic agent, an immunosuppressive agent, a drug metabolite, an environmental contaminant and a xenobiotic. It is a glucocorticoid, an 11beta-hydroxy steroid, a 21-hydroxy steroid, a 17alpha-hydroxy steroid, a 20-oxo steroid, a 3-oxo-Delta(1),Delta(4)-steroid, a primary alpha-hydroxy ketone, a tertiary alpha-hydroxy ketone and a C21-steroid. It is functionally related to a Delta(1)-progesterone.

• Application

  Prednisolone is a synthetic corticosteroid with metabolically interconvertible with prednisone. It mediates its effect by acting on neurokinin 1 receptor. It is used to treat many conditions that cause inflammation, including inflammatory bowel disease (IBD).

• Trademarks

  Cortalone(Halsey); Delta-Cortef (Pharmacia & Upjohn); Fernisolone(Ferndale); Meti-Derm (Schering); Prelone (Muro); Prelone(Teva); Sterane (Pfizer).

• Therapeutic Function

  Glucocorticoid

• Allgemeine Beschreibung

  Prednisolone,Δ¹-hydrocortisone,11β,17,21-trihydroxypregna-1,4-diene-3,20-dione, hasless salt-retention activity than hydrocortisone, but some patients have more frequently experiencedcomplications such as gastric irritation and peptic ulcers.Because of low MC activity, it cannot be used alone for adrenalinsufficiency. Prednisolone is available in varioussalts and esters to maximize its therapeutic utility:
  Prednisolone acetate, USP (21-acetate)
  Prednisolone sodium phosphate, USP (21-sodiumphosphate)
  Prednisolone sodium succinate, USP (21-sodiumsuccinate)
  Prednisolone tebutate, USP (21-tebutate).

• Hazard

  Causes sodium retention; may have side effects similar to cortisone.

• Mechanism of action

  Prednisolone is hydrocortisone to which has been added a ?1 double bond. This places two double bonds in ring A, which flattens it and increases glucocorticoid action at the expense of mineralocorticoid activity. Prednisolone has fourfold the glucocorticoid activity of hydrocortisone while having approximately half its mineralocorticoid activity. In addition, prednisolone has an increased duration of action compared to hydrocortisone, because the extra double bond in ring A retards its metabolic reduction.

• Clinical Use

  Prednisolone can be used to treat severe asthmatic attacks that do not respond to conventional treatment, and it is available as the free alcohol for oral administration. The C-21 sodium phosphate (Hydeltrasol) ester is available for parenteral use.

• Nebenwirkungen

  A prodrug of prednisolone is prednisone. It is the 11-keto analogue of prednisolone and must be converted in vivo to the active 11β-hydroxy compound, which is necessary to hydrogen bond to Asn-564 in the glucocorticoid receptor. Prednisone should not be used in patients with hepatic dysfunction, because their ability to reduce the 11-keto group with 11β-hydroxysteroid dehydrogenase to the active metabolite may be impaired.
  Prednisolone is well tolerated by most people and can start to work very quickly. Side effects can be dependent on the dose and duration of treatment. Short courses of treatment often have fewer side effects than long term use. A Severe allergic reaction is a very rare side effect of prednisolone.

• Sicherheitsprofil

  A poison by intravenous and subcutaneous routes. Moderately toxic by ingestion and intraperitoneal routes. Human teratogenic effects by an unspecified route: developmental abnormalities of the central nervous system; effects on embryo or fetus: fetal death, extra embryonic structures. Human reproductive effects by an unspecified route: stdlbirth. An experimental teratogen. Experimental reproductive effects. Human mutation data reported. When heated to decomposition it emits acrid smoke and irritating fumes.

• Synthese

  Prednisolone is 11|?,17|á,21-trihydroxypregna-1,4-dien-3,20-dione (27.1.33). Structurally, prednisolone differs from prednisone in that the keto-group at C11 of prednisone is replaced by a hydroxyl group. Prednisolone is synthesized either by microbiological dehydrogenation of C1¨CC2 bond in hydrocortisone [16¨C19], or from 21-acetoxy- 11|?,17|á-dihydroxy-5|á-pregnan-3,20-dione, which undergoes dibromination by molecular bromine in acetic acid at positions C2 and C4, and then the resulting dibromide 27.1.32 is dehydrobrominated by heating it in collidine, which gives prednisolone as an acetate at position C21. Hydrolyzing this compound leads to formation of prednisolone (27.1.33).

  

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Aldesleukin: avoid concomitant use.
  Antibacterials: metabolism accelerated by rifamycins and rifampicin; metabolism possibly inhibited by erythromycin; concentration of isoniazid possibly reduced.
  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.
  Ciclosporin: rare reports of convulsions in patients on ciclosporin and high-dose corticosteroids; increased levels of prednisolone; increased ciclosporin levels reported with prednisolone.
  Cobicistat: concentration possibly increased by cobicistat - increased risk of adrenal suppression.
  Diuretics: enhanced hypokalaemic effects of acetazolamide, loop diuretics and thiazide diuretics.
  Vaccines: high-dose corticosteroids can impair immune response to vaccines - avoid with live vaccines.

• Stoffwechsel

  Prednisolone is hepatically metabolised and excreted in the urine as sulphate and glucuronide conjugates, with an appreciable proportion of unchanged prednisolone.

Prednisolone Upstream-Materialien And Downstream Produkte

Prednisolon Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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