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QuickView for Methylprednisolone (compound)

Summary
General Info

PubChem

PubChem Compound 11869640

PubChem Compound 11869640

Name:	Methylprednisolone
PubChem Compound ID:	11869640
Description:	A PREDNISOLONE derivative with similar anti-inflammatory action.
Molecular formula:	C₂₂H₃₀O₅
Molecular weight:	374.471 g/mol
Synonyms:	ZINC03881944

DrugBank

Identification

Name:	Methylprednisolone
Name (isomeric):	DB00959
Drug Type:	small molecule
Description:	A PREDNISOLONE derivative with similar anti-inflammatory action.
Synonyms:	Methylprednisolon; Metilprednisolone [Dcit]; Metilprednisolona [INN-Spanish]; Methyleneprednisolone; Methylprednisolonum [INN-Latin]; 6alpha-Methylprednisolone
Brand:	Medrol Dosepak, Wyacort, Metysolon, Suprametil, Medixon, Reactenol, Lemod, Mesopren, Moderin, Esametone, Promacortine, Besonia, Firmacort, Solomet, Dopomedrol, Predni N Tablinen, Nirypan, Artisone-Wyeth, Medesone, Urbasone, Urbason, Medrate, Medlone 21, Metilbetasone, Medrone, Medrol Adt Pak, Metastab, Metrocort, Metrisone, Summicort, Sieropresol, Noretona
Brand name mixture:	Neo-Medrol(Methylprednisolone Acetate + Neomycin Sulfate), Methylprednisolone Sodium Succinate for Injection(Methylprednisolone + Water), Depo-Medrol with Lidocaine(Lidocaine Hydrochloride + Methylprednisolone Acetate), Medrol Acne Lotion(Aluminum Chlorohydrate + Methylprednisolone Acetate + Sulfur), Neo-Medrol Acne Lotion(Aluminum Chlorohydrate... show more » Neo-Medrol(Methylprednisolone Acetate + Neomycin Sulfate), Methylprednisolone Sodium Succinate for Injection(Methylprednisolone + Water), Depo-Medrol with Lidocaine(Lidocaine Hydrochloride + Methylprednisolone Acetate), Medrol Acne Lotion(Aluminum Chlorohydrate + Methylprednisolone Acetate + Sulfur), Neo-Medrol Acne Lotion(Aluminum Chlorohydrate + Methylprednisolone Acetate + Neomycin Sulfate + Sulfur) show less «
Category:	Adrenergic Agents, Antiemetics, Glucocorticoids, Neuroprotective Agents, Anti-inflammatory Agents
CAS number:	83-43-2

Pharmacology

Indication:	Adjunctive therapy for short-term administration in rheumatoid arthritis.
Pharmacology:	Methylprednisolone and its derivatives, methylprednisolone sodium succinate and methylprednisolone acetate, are synthetic glucocorticoids used as antiinflammatory or immunosuppressive agents.
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 an... show more » 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. show less «
Absorption:	Oral bioavailability 80-99%
Protein binding:	78%
Biotransformation:	Hepatic
Half Life:	1-3 hours
Toxicity:	LD₅₀=2000 mg/kg (orally in rat)
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Itraconazole	The imidazole, itraconazole, may increase the effect and toxicity of the corticosteroid, methylprednisolone.
Trastuzumab	Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Aprepitant	Increases the effect and toxicity of methylprednisolone
Ketoconazole	The imidazole, ketoconazole, may increase the effect and toxicity of the corticosteroid, methylprednisolone.
Rifampin	The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, methylprednisolone.

Itraconazole	The imidazole, itraconazole, may increase the effect and toxicity of the corticosteroid, methylprednisolone.
Trastuzumab	Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Aprepitant	Increases the effect and toxicity of methylprednisolone
Ketoconazole	The imidazole, ketoconazole, may increase the effect and toxicity of the corticosteroid, methylprednisolone.
Rifampin	The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, methylprednisolone.
Conivaptan	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Methylprednisolone. Consider methylprednisolone dose titration and/or adjustments in patients receiving strong CYP3A4 inhibitors (eg, azole antifungals, protease inhibitors) and monitor for increased steroid related adverse effects.
Phenobarbital	The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, methylprednisolone.
Quinupristin	This combination presents an increased risk of toxicity
Clarithromycin	The macrolide, clarithromycin, may increase the effect of corticosteroid, methylprednisolone.
Erythromycin	The macrolide, erythromycin, may increase the effect of corticosteroid, methylprednisolone.
Acetylsalicylic acid	The corticosteroid, methylprednisolone, may decrease the effect of the salicylate, acetylsalicylic acid.
Vecuronium	Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Methylprednisolone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
Tacrolimus	Methylprednisone may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Methylprednisone therapy is initiated, discontinued or altered.
Midodrine	Increased arterial pressure
Fosphenytoin	The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, methylprednisolone.
Pyridostigmine	The corticosteroid, methylprednisolone, may decrease the effect of the anticholinesterase, pyridostigmine.
Tacrine	Tacrine and Methylprednisolone may independently exacerbate muscle weakness in myasthenia gravis patients. Monitor for additive muscle weakness effects.
Phenytoin	The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, methylprednisolone.
Primidone	The barbiturate, primidone, may decrease the effect of the corticosteroid, methylprednisolone.

Targets

Glucocorticoid receptor

Enzymes

Cytochrome P450 3A4

Transporters

Multidrug resistance protein 1