Prednisolon 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.
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).
Allgemeine Beschreibung
Prednisolone,Δ
1-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.
Prednisolon Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte