Metilbetasone
Metilbetasone - General Information
A prednisolone derivative with similar anti-inflammatory action. [PubChem]
Pharmacology of Metilbetasone
Metilbetasone and its derivatives, methylprednisolone sodium succinate and methylprednisolone acetate, are synthetic glucocorticoids used as antiinflammatory or immunosuppressive agents.
Metilbetasone for patients
Persons who are on immunosuppressant doses of corticosteroids should be warned to avoid exposure to chicken pox or measles. Patients should also be advised that if they are exposed, medical advice should be sought without delay.
Metilbetasone Interactions
The pharmacokinetic interactions listed below are potentially clinically important. Mutual inhibition of metabolism occurs with concurrent use of cyclosporin and methylprednisolone; therefore, it is possible that adverse events associated with the individual use of either drug may be more apt to occur. convulsions have been reported with concurrent use of methylprednisolone and cyclosporin. Drugs that induce hepatic enzymes such as phenobarbital, phenytoin, and rifampin may increase the clearance of methylprednisolone and may require increased in methylprednisolone dose to achieve the desired response. Drugs such as troleandomycin and ketoconazole may inhibit the metabolism of methylprednisolone and thus decrease its clearance. Therefore, the dose of methylprednisolone should be titrated to avoid steroid toxicity.
Methylprednisolone may increase the clearance of chronic high dose aspirin. This could lead to decreased salicylate serum levels or increase the risk of salicylate toxicity when methylprednisolone is withdrawn. Aspirin should be used cautiously in conjunction with corticosteroids in patients suffering from hypoprothrombinemia.
The effect of methylprednisolone on oral anticoagulants is variable. There are reports of enhanced as well as diminished effects of anticoagulant when given concurrently with corticosteroids. Therefore, coagulation indices should be monitored to maintain the desired anticoagulant effect.
Metilbetasone Contraindications
Systemic fungal infections and known hypersensitivity to components.
Additional information about Metilbetasone
Metilbetasone Indication: Adjunctive therapy for short-term administration in rheumatoid arthritis.
Mechanism Of Action: Unbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Methylprednisolone
Synonyms: Methyleneprednisolone; Methylprednisolon; Methylprednisolonum [Inn-Latin]; Metilprednisolona [Inn-Spanish]; Metilprednisolone [Dcit]; 6alpha-Methylprednisolone
Drug Category: Neuroprotective Agents; Glucocorticoids; Antiemetics; Anti-inflammatory Agents; Adrenergic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Methylprednisolone: Artisone-Wyeth; Besonia; Dopomedrol; Esametone; Firmacort; Lemod; Medesone; Medixon; Medlone 21; Medrate; Medrol Adt Pak; Medrol Dosepak; Medrone; Mesopren; Metastab; Metilbetasone; Metrisone; Metrocort; Metysolon; Moderin; Nirypan; Noretona; Predni N Tablinen; Promacortine; Reactenol; Sieropresol; Solomet; Summicort; Suprametil; Urbason; Urbasone; Wyacort;
Absorption: Oral bioavailability 80-99%
Toxicity (Overdose): LD50=2000 mg/kg (orally in rat)
Protein Binding: 78%
Biotransformation: Hepatic
Half Life: 1-3 hours
Dosage Forms of Metilbetasone: Tablet Oral
Powder, for solution Intravenous
Powder Intramuscular
Powder Intravenous
Suspension Intramuscular
Chemical IUPAC Name: (6S,8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-6,10,13-trimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
Chemical Formula: C22H30O5
Methylprednisolone on Wikipedia: https://en.wikipedia.org/wiki/Methylprednisolone
Organisms Affected: Humans and other mammals