Page last updated: 2024-12-05

methantheline

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

Description

Methantheline is a synthetic anticholinergic drug that was once widely used to treat a variety of gastrointestinal disorders. It is a quaternary ammonium compound that acts by competitively blocking acetylcholine receptors at the muscarinic receptors in the parasympathetic nervous system. This leads to a reduction in the activity of the gastrointestinal tract, including decreased motility, reduced gastric acid secretion, and decreased saliva production. Methantheline is no longer widely used due to the availability of more effective and safer anticholinergic drugs. It was synthesized in the mid-20th century and studied extensively for its potential to treat conditions such as peptic ulcer disease, irritable bowel syndrome, and urinary incontinence. Methantheline is not used in the treatment of these conditions today because its effects are relatively short-lived and it can cause a variety of side effects, including dry mouth, blurred vision, constipation, and urinary retention.'

Methantheline: A quaternary ammonium compound that acts as an antimuscarinic agent. It has been used in the treatment of PEPTIC ULCER, in gastrointestinal disorders associated with smooth muscle spasm, and in the management of urinary incontinence, and may also be used for the treatment of HYPERHIDROSIS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4097
CHEMBL ID1201264
CHEBI ID6817
SCHEMBL ID77917
MeSH IDM0224681

Synonyms (39)

Synonym
BRD-K09859624-004-03-9
banthine bromide
methanthine bromide
PRESTWICK3_001066
NCGC00016239-01
cas-53-46-3
PRESTWICK2_001066
BSPBIO_001052
AB00514028
5818-17-7
C07849
methantheline
methanthelinium
methantheline cation
DB00940
methantheline ion
methanthelinum
n,n-diethyl-n-methyl-2-[(9h-xanthen-9-ylcarbonyl)oxy]ethanaminium
BPBIO1_001158
PRESTWICK1_001066
SPBIO_002966
PRESTWICK0_001066
L000712
diethyl-methyl-[2-(9h-xanthene-9-carbonyloxy)ethyl]azanium
CHEMBL1201264
chebi:6817 ,
NCGC00016239-02
36ei79tx7i ,
ethanaminium, n,n-diethyl-n-methyl-2-((9h-xanthen-9-ylcarbonyl)oxy)-
unii-36ei79tx7i
methanthelinium [who-dd]
ethanaminium, n,n-diethyl-n-methyl-2-((9h-xanthen-9-ylcarbonyl)oxy)
diethyl(2-hydroxyethyl)methylammonium xanthene-9-carboxylate
methantheline [vandf]
SCHEMBL77917
DTXSID7046964
diethyl(methyl){2-[(9h-xanthen-9-yl)carbonyloxy]ethyl}azanium
ethanaminium,n,n-diethyl-n-methyl-2-[(9h-xanthen-9-ylcarbonyl)oxy]-
Q6823610

Research Excerpts

Overview

Methantheline is a strong muscarinic receptor blocking drug used in the treatment of overactive bladder syndrome, hypersalivation and hyperhidrosis.

ExcerptReferenceRelevance
"Methantheline is a strong muscarinic receptor blocking drug used in the treatment of overactive bladder syndrome, hypersalivation and hyperhidrosis. "( Relative bioavailability and pharmacodynamic effects of methantheline compared with atropine in healthy subjects.
Franke, G; Giessmann, T; Lötsch, J; Müller, C; Siegmund, W; Walter, R; Zschiesche, M, 2012
)
2.07

Toxicity

ExcerptReferenceRelevance
" No serious adverse events were reported."( [Randomized, placebo-controlled, double blind clinical trial for the evaluation of the efficacy and safety of oral methantheliniumbromide (Vagantin) in the treatment of focal hyperhidrosis].
Hund, M; Rzany, B; Sinkgraven, R, 2004
)
0.32
" The most frequent adverse event was dry mouth."( Efficacy and safety of methantheline bromide (Vagantin(®) ) in axillary and palmar hyperhidrosis: results from a multicenter, randomized, placebo-controlled trial.
Berensmeier, A; Dirschka, T; Fischer, T; Hamm, H; Müller, C; Reich, K; Rzany, B, 2013
)
0.7
"Fifty milligrams methantheline bromide three times a day is an effective and safe treatment of axillary hyperhidrosis."( Efficacy and safety of methantheline bromide (Vagantin(®) ) in axillary and palmar hyperhidrosis: results from a multicenter, randomized, placebo-controlled trial.
Berensmeier, A; Dirschka, T; Fischer, T; Hamm, H; Müller, C; Reich, K; Rzany, B, 2013
)
1.04

Pharmacokinetics

ExcerptReferenceRelevance
" To provide basic information on the pharmacokinetics, magnitude of pharmacodynamic (PD) effects and their correlations with plasma concentrations, we performed a clinical study in 12 healthy subjects receiving methantheline as immediate-release coated tablets (IR) or in watery solution (SOL) in comparison with atropine and placebo tablets."( Relative bioavailability and pharmacodynamic effects of methantheline compared with atropine in healthy subjects.
Franke, G; Giessmann, T; Lötsch, J; Müller, C; Siegmund, W; Walter, R; Zschiesche, M, 2012
)
0.81

Dosage Studied

ExcerptRelevanceReference
" In some instances, patients who did not have good response at first were relieved later when the size of doses and the dosage schedule were adjusted to fit their particular needs."( The use of banthine in the treatment of digestive disturbances.
ASHER, LM, 1952
)
0.23
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
xanthenes
[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]

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency3.98110.00207.533739.8107AID891
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency56.23410.010323.856763.0957AID2662
gemininHomo sapiens (human)Potency0.01880.004611.374133.4983AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.00910.005612.367736.1254AID624032
lamin isoform A-delta10Homo sapiens (human)Potency3.98110.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (335)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990320 (95.52)18.7374
1990's1 (0.30)18.2507
2000's2 (0.60)29.6817
2010's11 (3.28)24.3611
2020's1 (0.30)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.66

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index39.66 (24.57)
Research Supply Index5.87 (2.92)
Research Growth Index5.29 (4.65)
Search Engine Demand Index52.87 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (39.66)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (0.85%)5.53%
Reviews3 (0.85%)6.00%
Case Studies1 (0.28%)4.05%
Observational0 (0.00%)0.25%
Other344 (98.01%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
[NCT01429090]Phase 112 participants (Actual)Interventional1999-10-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]