methylprednisolone suleptanate profile

methylprednisolone suleptanate: prodrug of methylprednisolone [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

methylprednisolone suleptanate : An organic sodium salt that is the monosodium salt of methylprednisolone 21-suleptanic acid ester. It is a prodrug of methylprednisolone developed by Pharmacia Corp for the treatment of asthma. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID Source	ID
PubMed CID	23663977
CHEMBL ID	2106453
CHEBI ID	135864
SCHEMBL ID	43507
MeSH ID	M0148521

Synonyms (41)

Synonym
medrosol
methylprednisolone suleptanate
promedrol
u-67590a
sodium 2-[(8-{[(6alpha,11beta)-11,17-dihydroxy-6-methyl-3,20-dioxopregna-1,4-dien-21-yl]oxy}-8-oxooctanoyl)(methyl)amino]ethanesulfonate
90350-40-6
methylprednisolone suleptanate (usan/inn)
D05002
methylprednisolone suleptanate sodium salt
methylprednisolone suleptanate [usan:inn]
methylprednisolone 21-(8-(methyl-(2-sulfoethyl)amino)-1,8-dioxooctanoate)
suleptanato de methilprednisolona [spanish]
methylprednisoloni suleptanas [latin]
pnu 67590a
suleptanate de methylprednisolone [french]
u-67,590a
7-(methyl(2-sulfoethyl)carbamoyl)heptanoic acid, c-21-ester with 11beta,17,21-trihydroxy-6alpha-methylpregna-1,4-diene-3,20-dione, monosodium salt
u 67590a
pnu-67590a
pregna-1,4-diene-3,20-dione, 11,17-dihydroxy-6-methyl-21-((8-(methyl(2-sulfoethyl)amino)-1,8-dioxooctyl)oxy)-, monosodium salt, (6alpha,11beta)-
sodium 2-[{8-[(11beta,17-dihydroxy-6alpha-methyl-3,20-dioxopregna-1,4-dien-21-yl)oxy]-8-oxooctanoyl}(methyl)amino]ethanesulfonate
suleptanato de metilprednisolona
sodium 2-[{8-[(11beta,17-dihydroxy-6alpha-methyl-3,20-dioxopregna-1,4-dien-21-yl)oxy]-8-oxooctanoyl}(methyl)amino]ethane-1-sulfonate
methylprednisolone suleptanate sodium
CHEBI:135864
methylprednisoloni suleptanas
suleptanate de methylprednisolone
methylprednisolone suleptanate monosodium salt
g6cs53ncvs ,
suleptanato de methilprednisolona
unii-g6cs53ncvs
CHEMBL2106453
methylprednisolone suleptanate [inn]
methylprednisolone suleptanate [usan]
methylprednisolone suleptanate [who-dd]
pregna-1,4-diene-3,20-dione, 11,17-dihydroxy-6-methyl-21-((8-(methyl(2-sulfoethyl)amino)-1,8-dioxooctyl)oxy)-, monosodium salt, (6.alpha.,11.beta.)-
methylprednisolone suleptanate [jan]
SCHEMBL43507
DTXSID7023304
Q27278834
sodium;2-[[8-[2-[(6s,8s,9s,10r,11s,13s,14s,17r)-11,17-dihydroxy-6,10,13-trimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthren-17-yl]-2-oxoethoxy]-8-oxooctanoyl]-methylamino]ethanesulfonate

Research Excerpts

Overview

Methylprednisolone suleptanate (Promedrol) is being developed by Pharmacia Corp for the treatment of asthma.

Excerpt	Reference	Relevance
"Methylprednisolone suleptanate (Promedrol) is a prodrug of methylprednisolone being developed by Pharmacia Corp (formerly Pharmacia & Upjohn) for the treatment of asthma. "	( Methylprednisolone suleptanate Pharmacia Corp. Paggiaro, P, 2000)	3.19

Pharmacokinetics

Excerpt	Reference	Relevance
" No dependence on time was apparent for any prodrug pharmacokinetic parameter."	( Pilot study of the pharmacokinetics of methylprednisolone after single and multiple intravenous doses of methylprednisolone sodium succinate and methylprednisolone suleptanate to healthy volunteers. Della-Coletta, AA; Ferry, JJ; VanderLugt, JT; Weber, DJ, 1994)	0.49
"Ninety volunteers were included in the pharmacokinetic analysis."	( A comparative population pharmacokinetic analysis for methylprednisolone following multiple dosing of two prodrugs in patients with acute asthma. Daley-Yates, PT; Parker, TJ; Wood, SA, 1997)	0.3
" Based on individual Bayesian estimates, the exposure of patients to MP was marginally lower for MP suleptanate although the parameter estimates were not significantly different for half-life (2."	( A comparative population pharmacokinetic analysis for methylprednisolone following multiple dosing of two prodrugs in patients with acute asthma. Daley-Yates, PT; Parker, TJ; Wood, SA, 1997)	0.3
"The aim of this study was to establish whether pharmacokinetic differences between two pro-drugs of methylprednisolone (MP) are likely to be of clinical significance."	( Pharmacokinetic and pharmacodynamic assessment of bioavailability for two prodrugs of methylprednisolone. Brooks, CD; Daley-Yates, PT; Gregory, AJ, 1997)	0.3
" Bioequivalence was assessed by conventional pharmacokinetic analysis, by measuring pharmacodynamic responses plus a novel approach using pharmacokinetic/pharmacodynamic modeling."	( Pharmacokinetic and pharmacodynamic assessment of bioavailability for two prodrugs of methylprednisolone. Brooks, CD; Daley-Yates, PT; Gregory, AJ, 1997)	0.3
"The MP Cmax was less for MP suleptanate due to a longer absorption halflife of the prodrug from the intramuscular injection site."	( Pharmacokinetic and pharmacodynamic assessment of bioavailability for two prodrugs of methylprednisolone. Brooks, CD; Daley-Yates, PT; Gregory, AJ, 1997)	0.3
" The use of both pharmacokinetic and pharmacodynamic response data together gives greater confidence in the conclusions compared with those based only on conventional pharmacokinetic bioequivalence analysis."	( Pharmacokinetic and pharmacodynamic assessment of bioavailability for two prodrugs of methylprednisolone. Brooks, CD; Daley-Yates, PT; Gregory, AJ, 1997)	0.3

Bioavailability

Excerpt	Reference	Relevance
" In addition the differences in the pharmacokinetics for the prodrugs resulted in only a small difference in the relative bioavailability of MP for MP suleptanate (0."	( A comparative population pharmacokinetic analysis for methylprednisolone following multiple dosing of two prodrugs in patients with acute asthma. Daley-Yates, PT; Parker, TJ; Wood, SA, 1997)	0.3
" The bioavailability of MP was equivalent when based on AUC with a MP suleptanate median 108% of the MP succinate value (90% CI: 102-114%)."	( Pharmacokinetic and pharmacodynamic assessment of bioavailability for two prodrugs of methylprednisolone. Brooks, CD; Daley-Yates, PT; Gregory, AJ, 1997)	0.3

Dosage Studied

Excerpt	Relevance	Reference
"It was concluded that for the multiple dosage regimen used in patients with acute asthma the systemic exposure to MP following dosing with MP suleptanate is similar to that arising from MP succinate."	( A comparative population pharmacokinetic analysis for methylprednisolone following multiple dosing of two prodrugs in patients with acute asthma. Daley-Yates, PT; Parker, TJ; Wood, SA, 1997)	0.3

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Role	Description
anti-inflammatory agent	Any compound that has anti-inflammatory effects.
glucocorticoid receptor agonist	An agonist that selectively binds to and activates a glucocorticoid receptor.
prodrug	A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
anti-asthmatic drug	A drug used to treat asthma.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
organic sodium salt
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	3 (20.00)	18.7374
1990's	10 (66.67)	18.2507
2000's	2 (13.33)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	4 (26.67%)	5.53%
Reviews	1 (6.67%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	10 (66.67%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
histamine [no description available]	3.78	2	1	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
potassium chloride Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.. potassium chloride : A metal chloride salt with a K(+) counterion.	1.98	1	0	inorganic chloride; inorganic potassium salt; potassium salt	fertilizer
tetraethylammonium Tetraethylammonium: A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90)	1.97	1	0	quaternary ammonium ion
corticosterone [no description available]	1.98	1	0	11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone	human metabolite; mouse metabolite
edetic acid Edetic Acid: A chelating agent that sequesters a variety of polyvalent cations such as CALCIUM. It is used in pharmaceutical manufacturing and as a food additive.	1.97	1	0	ethylenediamine derivative; polyamino carboxylic acid; tetracarboxylic acid	anticoagulant; antidote; chelator; copper chelator; geroprotector
cycloheximide Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.. cycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus.	1.98	1	0	antibiotic fungicide; cyclic ketone; dicarboximide; piperidine antibiotic; piperidones; secondary alcohol	anticoronaviral agent; bacterial metabolite; ferroptosis inhibitor; neuroprotective agent; protein synthesis inhibitor
methylprednisolone Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone.	7.73	15	4	6-methylprednisolone; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antiemetic; environmental contaminant; neuroprotective agent; xenobiotic
dexamethasone 21-phosphate dexamethasone 21-phosphate: has anti-inflammatory activity. dexamethasone phosphate : A steroid phosphate that is the 21-O-phospho derivative of dexamethasone.	1.98	1	0	11beta-hydroxy steroid; 17-hydroxy steroid; 3-oxo-Delta(4) steroid; fluorinated steroid; steroid phosphate; tertiary alpha-hydroxy ketone	glucocorticoid receptor agonist
alpha-aminopyridine alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.	2.01	1	0
methylprednisolone hemisuccinate Methylprednisolone Hemisuccinate: A water-soluble ester of METHYLPREDNISOLONE used for cardiac, allergic, and hypoxic emergencies.	5.8	6	4	corticosteroid hormone; hemisuccinate
fpl 55712 FPL 55712: inhibitor of SRS-A and LTC4 and LTD4 receptors	1.98	1	0	aromatic ketone
bradykinin [no description available]	1.98	1	0	oligopeptide	human blood serum metabolite; vasodilator agent
ovalbumin Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.	1.98	1	0

Condition	Relationship Strength	Studies	Trials
Endotoxin Shock [description not available]	1.98	1	0
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	1.98	1	0
Shock, Septic Sepsis associated with HYPOTENSION or hypoperfusion despite adequate fluid resuscitation. Perfusion abnormalities may include but are not limited to LACTIC ACIDOSIS; OLIGURIA; or acute alteration in mental status.	1.98	1	0
Anaphylactic Reaction [description not available]	2.38	2	0
Anaphylaxis An acute hypersensitivity reaction due to exposure to a previously encountered ANTIGEN. The reaction may include rapidly progressing URTICARIA, respiratory distress, vascular collapse, systemic SHOCK, and death.	2.38	2	0
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	3.78	2	1
Bright Disease A historical classification which is no longer used. It described acute glomerulonephritis, acute nephritic syndrome, or acute nephritis. Named for Richard Bright.	1.98	1	0
Glomerulonephritis Inflammation of the renal glomeruli (KIDNEY GLOMERULUS) that can be classified by the type of glomerular injuries including antibody deposition, complement activation, cellular proliferation, and glomerulosclerosis. These structural and functional abnormalities usually lead to HEMATURIA; PROTEINURIA; HYPERTENSION; and RENAL INSUFFICIENCY.	1.98	1	0
Proteinuria The presence of proteins in the urine, an indicator of KIDNEY DISEASES.	1.98	1	0
Asthma, Bronchial [description not available]	5.77	4	2
Acute Disease Disease having a short and relatively severe course.	3.37	1	1
Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).	10.77	4	2
Injuries, Spinal Cord [description not available]	2.92	1	0
Spinal Cord Injuries Penetrating and non-penetrating injuries to the spinal cord resulting from traumatic external forces (e.g., WOUNDS, GUNSHOT; WHIPLASH INJURIES; etc.).	2.92	1	0
Constriction, Pathological [description not available]	1.98	1	0
Bronchial Diseases Diseases involving the BRONCHI.	1.98	1	0
Constriction, Pathologic The condition of an anatomical structure's being constricted beyond normal dimensions.	1.98	1	0
Cerebral Concussion [description not available]	1.97	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	1.97	1	0
Craniocerebral Injuries [description not available]	1.97	1	0
Brain Concussion A nonspecific term used to describe transient alterations or loss of consciousness following closed head injuries. The duration of UNCONSCIOUSNESS generally lasts a few seconds, but may persist for several hours. Concussions may be classified as mild, intermediate, and severe. Prolonged periods of unconsciousness (often defined as greater than 6 hours in duration) may be referred to as post-traumatic coma (COMA, POST-HEAD INJURY). (From Rowland, Merritt's Textbook of Neurology, 9th ed, p418)	1.97	1	0
Craniocerebral Trauma Traumatic injuries involving the cranium and intracranial structures (i.e., BRAIN; CRANIAL NERVES; MENINGES; and other structures). Injuries may be classified by whether or not the skull is penetrated (i.e., penetrating vs. nonpenetrating) or whether there is an associated hemorrhage.	1.97	1	0

methylprednisolone suleptanate

Description

Cross-References

Synonyms (41)

Research Excerpts

Overview

Pharmacokinetics

Bioavailability

Dosage Studied

Roles (4)

Drug Classes (1)

Research

Studies (15)

Market Indicators

Research Demand Index: 11.66

Study Types

methylprednisolone suleptanate

Description

Cross-References

Synonyms (41)

Research Excerpts

Overview

Pharmacokinetics

Bioavailability

Dosage Studied

Roles (4)

Drug Classes (1)

Research

Studies (15)

Market Indicators

Research Demand Index: 11.66

Study Types

Related Drugs (13)

Related Conditions (22)