Page last updated: 2024-11-10

rioprostil

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Rioprostil: A synthetic methylprostaglandin E1 analog that reduces gastric acid secretion and enhances the gastric mucus-bicarbonate barrier. It is effective in the therapy of gastric ulcers and gives significant protection against NSAID-induced gastric mucosal damage. The drug also prevents cyclosporin A-induced damage to endocrine and exocrine pancreatic secretions. It shows a low order of acute toxicity and there is no evidence of embryotoxicity, fetotoxicity, teratogenicity, or mutagenicity in animal studies. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311413
CHEMBL ID3301679
CHEBI ID135498
SCHEMBL ID693575
SCHEMBL ID186845
MeSH IDM0025346

Synonyms (35)

Synonym
orf-15927
tr-4698
D05732
77287-05-9
rioprostil (usan/inn)
rioprostil
(2r,3r,4r)-4-hydroxy-2-(7-hydroxyheptyl)-3-((e)-(4rs)-(4-hydroxy-4-methyl-1-octenyl))cyclopentanone
prost-13-en-9-one, 1,11,16-trihydroxy-16-methyl-, (11alpha,13e)-
(13e)-11alpha,16-dihydroxy-16-methyl-9-oxo-13-prostenol
rioprostilo [spanish]
rwj-15927
rioprostilum [latin]
rwj 15927
orf 15927
CHEBI:135498
(2r,3r,4r)-4-hydroxy-2-(7-hydroxyheptyl)-3-[(e)-4-hydroxy-4-methyloct-1-enyl]cyclopentan-1-one
7jl402pvqr ,
rioprostil [usan:inn:ban]
unii-7jl402pvqr
rioprostilum
rioprostilo
rioprostil [mi]
(2r,3r,4r)-4-hydroxy-2-(7-hydroxyheptyl)-3-[(e)-(4rs)-(4-hydroxy-4-methyl-1-octenyl)]cyclopentanone
rioprostil [inn]
prost-13-en-9-one, 1,11,16-trihydroxy-16-methyl-, (11.alpha.,13e)-
rioprostil [usan]
rioprostil [mart.]
CHEMBL3301679
SCHEMBL693575
SCHEMBL186845
AC-31146
(2r,3r,4r)-4-hydroxy-3-((e)-4-hydroxy-4-methyloct-1-en-1-yl)-2-(7-hydroxyheptyl)cyclopentan-1-one
Q27268415
DTXSID701021622
AKOS040747394

Research Excerpts

Overview

Rioprostil is a 16-methyl-16-hydroxy alcohol analogue of prostaglandin E1 with anti-secretory activity. It is currently under study for peptic ulcer healing.

ExcerptReferenceRelevance
"Rioprostil is a synthetic prostaglandin E1 analogue currently under study for peptic ulcer healing. "( Rioprostil, a new prostaglandin E1 analogue does not affect glucose homeostasis in healthy volunteers.
Businger, JA; Eichler, HG; Korn, A; Waldhäusl, WK,
)
3.02
"Rioprostil is a 16-methyl-16-hydroxy alcohol analogue of prostaglandin E1 with anti-secretory activity. "( The effects of rioprostil on gastric emptying and intragastric acidity.
Johnston, DA; Penston, JG; Wormsley, KG, 1986
)
2.07
"Rioprostil is a new prostaglandin E1 analogue."( Prostaglandins and peptic ulcer disease: nocturnal administration of rioprostil vs ranitidine in duodenal ulcer healing.
Dammann, HG; Müller, P; Simon, B, 1986
)
1.23

Treatment

Rioprostil, 7 days pretreatment, did not affect control parameters of blood coagulation activity. Treatment with rioprostill remained without effect on mixed meal-induced changes in plasma glucose levels.

ExcerptReferenceRelevance
"Rioprostil, 7 days pretreatment, did not affect control parameters of blood coagulation activity."( The interaction of the prostaglandin E derivative rioprostil with oral anticoagulant agents.
Hamulyàk, K; Thijssen, HH, 1989
)
1.25
"Treatment with rioprostil remained without effect on mixed meal-induced changes in plasma glucose levels and concomitant increases in insulin, pancreatic polypeptide, and somatostatin levels."( Effect of rioprostil, a methylprostaglandin E1 analog, on basal and stimulated plasma pancreatic hormone levels in man.
Segers, O; Somers, G, 1990
)
1.02

Toxicity

ExcerptReferenceRelevance
", is a safe and effective treatment for gastric ulcer disease."( Efficacy and safety of rioprostil, 300 micrograms b.d., in the treatment of gastric ulcer: a comparison vs. ranitidine, 150 mg b.d., in a randomized multicentre study.
Barbier, P; Businger, JA; Demol, P; Rutgeerts, P; Simon, B; Vantrappen, G, 1989
)
0.59
" Diarrhoea is the main adverse event, but is generally mild and self-limiting."( Efficacy and safety of rioprostil, 300 micrograms b.d., in the treatment of duodenal ulcer: a double-blind, controlled multicentre clinical study vs. ranitidine.
Businger, JA; Coremans, G; Demol, P; Vantrappen, G, 1989
)
0.59
" Patients who dropped out of the studies and those with adverse drug reactions are classified and compared within different subgroups."( Drug safety of rioprostil in patients with active gastric or duodenal ulcer.
Corsing, C; Demol, P, 1989
)
0.63

Pharmacokinetics

ExcerptReferenceRelevance
" Blood samples are taken on days 4 and 5 to check steady-state plasma levels of theophylline and on days 6 and 7 to determine the main pharmacokinetic parameters."( Pharmacokinetic interactions between theophylline and rioprostil.
d'Athis, P; de Lauture, D; Olive, G; Paccaly, D; Prunieras, F; Rey, E; Richard, MO; Strauch, G, 1989
)
0.53

Compound-Compound Interactions

ExcerptReferenceRelevance
" The antiulcer effect of the drug combination was additive, suggesting that each compound acts independently to prevent gastric bleeding."( Antiulcer effect of rioprostil, a prostaglandin E1 analog, in combination with antacid.
Genna, T; Katz, LB; Shriver, DA, 1986
)
0.59

Bioavailability

ExcerptReferenceRelevance
" The bioavailability of indomethacin in the three groups does not differ significantly."( Protective effect of rioprostil on indomethacin-induced lesions of gastric and duodenal mucosa in healthy volunteers.
Gerova, Z; Kirkov, V; Popov, P; Vlahov, V, 1989
)
0.6
" A systemic bioavailability of 2%, in spite of a rapid and nearly complete absorption (fa = 90%), indicates an extended first-pass effect."( Pharmacokinetics of rioprostil in rats.
Petersen-von Gehr, JK; Siefert, HM; Steinke, W, 1989
)
0.6

Dosage Studied

Daily oral dosing of rioprostil (50 micrograms/kg BID for 15 days) did not influence the course of the adjuvant disease in rats or alter the antiinflammatory or analgesic effect.

ExcerptRelevanceReference
" The most effective inhibitory dosage with maximal carbachol (10(-5) M; 30."( Prostaglandin E analogue inhibition of pancreatic enzyme secretion.
Adrian, TE; Bilchik, AJ; Modlin, IM; Zucker, KA, 1989
)
0.28
" Daily oral dosing of rioprostil (50 micrograms/kg BID for 15 days) did not influence the course of the adjuvant disease in rats or alter the antiinflammatory or analgesic effect of the NSAID."( Rioprostil prevents gastric bleeding induced by nonsteroidal antiinflammatory drugs in dogs and arthritic rats.
Abrutyn, D; Argentieri, DC; Capetola, RJ; Genna, T; Hartnagel, RE; Jasty, V; Katz, LB; Moore, LE; Porter, MC; Shriver, DA, 1986
)
2.03
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aliphatic alcoholAn alcohol derived from an aliphatic compound.
[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]

Bioassays (19)

Assay IDTitleYearJournalArticle
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (91)

TimeframeStudies, This Drug (%)All Drugs %
pre-199082 (90.11)18.7374
1990's9 (9.89)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 26.48

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index26.48 (24.57)
Research Supply Index4.98 (2.92)
Research Growth Index4.28 (4.65)
Search Engine Demand Index34.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (26.48)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials51 (54.26%)5.53%
Reviews5 (5.32%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other38 (40.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]