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tiemonium + noramidopyrine (Visceralgine Forte)

✓ Approved

Merck & Co. · CHRM1 · Small Molecule

What is tiemonium + noramidopyrine?

tiemonium + noramidopyrine is a small molecule developed by Merck & Co.. It is approved for therapeutic indications via injectable (others).

Drug Profile

Brand NamesVisceralgine Forte
CompanyMerck & Co.
Drug ClassSmall Molecule
Molecular TargetCHRM1, CHRM2, CHRM3, CHRM4, PTGS1, PTGS2
RouteInjectable (Others)
StatusApproved
Sources: ClinicalTrials.gov, Merck & Co.

Mechanism of Action

Molecular Targets

tiemonium + noramidopyrine acts on 6 molecular targets:

CHRM1cholinergic receptor muscarinic 1 (M1R, M1)
CHRM2cholinergic receptor muscarinic 2 (HM2)
CHRM3cholinergic receptor muscarinic 3 (EGBRS, m3AChR)
CHRM4cholinergic receptor muscarinic 4 (M4R, HM4)
PTGS1prostaglandin-endoperoxide synthase 1 (COX3, PCOX1)
PTGS2prostaglandin-endoperoxide synthase 2 (COX-2, COX2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

tiemonium + noramidopyrine is developed for 3 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
Gastrointestinal disordersAbdominal pain✓ Approved
Gastrointestinal disordersGastrointestinal disorder✓ Approved
Musculoskeletal and connective tissue disordersMuscle spasms✓ Approved

Related Research Articles

PubMedOpen veterinary journal2026-06-30

Chronic spasmodic colic management in a thoroughbred horse: A case report from Bangladesh.

Borsha Rupsana Perven RP, Hasan Maruf M, Zabbar Md Abdul MA

Equine colic refers to severe abdominal pain caused by gastrointestinal tract dysfunction. A clinical case of equine colic was reported from a riding school in the Chattogram coastal area of Bangladesh. The animal was a 10-year-old gelding thoroughbred horse with a body weight of 500 kg. Visible clinical signs included anorexia, bruxism, restlessness with rolling side to side and pawing by the front leg on both sand and hard surfaces, dehydration, looking at the flank, abdominal distension, and increased intestinal motility detected via rectal palpation. The case was treated using intravenous fluids to rehydrate the animal. Tiemonium methyl-sulphate was administered twice intravenously to mitigate the intestinal spasm. Flunixin meglumine was administered for pain relief. Omeprazole and 7.5% sodium-bi-carbonate was administered twice intravenously to reduce the gastric lesion during colic. Secnidazole was administered empirically due to concerns about bacterial overgrowth. Finally, the symptoms of the animal completely resolved within 12 hours of treatment initiation. The majority of colic cases can be effectively handled through proper management practices. This study has revealed that the affected horse started to respond to the treatment successfully after 12 hours. The major shortcomings of this study are the absence of radiography and ultrasound assessment due to resource constraints. Moreover, the case study was an in-depth analysis of a single case, and further studies are required to determine the possible interactions and outcomes of medication.

PMID 42376547
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PubMedPloS one2024-06-21

Influence of selected non-antibiotic pharmaceuticals on antibiotic resistance gene transfer in Escherichia coli.

Mohamed Doaa Safwat DS, Abd El-Baky Rehab Mahmoud RM, El-Mokhtar Mohamed Ahmed MA, Ghanem Sahar K SK et al.

Antibiotic resistance genes (ARGs) transfer rapidly among bacterial species all over the world contributing to the aggravation of antibiotic resistance crisis. Antibiotics at sub-inhibitory concentration induce horizontal gene transfer (HRT) between bacteria, especially through conjugation. The role of common non-antibiotic pharmaceuticals in the market in disseminating antibiotic resistance is not well studied. In this work, we indicated the effect of some commonly used non-antibiotic pharmaceuticals including antiemetic (metoclopramide HCl) and antispasmodics (hyoscine butyl bromide and tiemonium methyl sulfate) on the plasmid-mediated conjugal transfer of antibiotic resistance genes between pathogenic E. coli in the gastric intestinal tract (GIT). Broth microdilution assay was used to test the antibacterial activity of the tested non-antibiotic pharmaceuticals. A conjugation mating system was applied in presence of the studied non-antibiotic pharmaceuticals to test their effect on conjugal transfer frequency. Plasmid extraction and PCR were performed to confirm the conjugation process. Transmission electron microscopy (TEM) was used for imaging the effect of non-antibiotic pharmaceuticals on bacterial cells. No antibacterial activity was reported for the used non-antibiotic pharmaceuticals. Plasmid-mediated conjugal transfer between isolates was induced by metoclopramide HCl but suppressed by hyoscine butyl bromide. Tiemonium methylsulfate slightly promoted conjugal transfer. Aggregation between cells and periplasmic bridges was clear in the case of metoclopramide HCl while in presence of hyoscine butyl bromide little affinity was observed. This study indicates the contribution of non-antibiotic pharmaceuticals to the dissemination and evolution of antibiotic resistance at the community level. Metoclopramide HCl showed an important role in the spread of antibiotic resistance.

PMID 38905247
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PubMedForensic science international2020-06-01

Assessment of a portable quadrupole-based gas chromatography mass spectrometry for seized drug analysis.

Fiorentin Taís R TR, Logan Barry K BK, Martin David M DM, Browne Thom T et al.

The cutting agents, classified as diluents (pharmacologically inactive) or adulterants (pharmacologically active), are substances commonly used to cut drugs of abuse to increase profits. These substances are constantly changing over time, increasing the risks to the user's health caused by the compounds' potential individual toxicities as well as their drug-drug interactions. This work aimed to develop and validate a screening method using a portable quadrupole-based gas chromatography mass spectrometer (FLIR Griffin™ G510) to identify drugs of abuse and adulterants in seized material, and compare it with a well validated standard technology, gas chromatography mass spectrometry (GC-MS). The method was validated for the identification of alprazolam, amphetamine, aminopyrine, benzocaine, caffeine, cocaine, codeine, diltiazem, ephedrine, fentanyl, fenethylline, furanylfentanyl, heroin, hydroxyzine, levamisole, lidocaine, methamphetamine, morphine, noramidopyrine (a marker of metamizole), phencyclidine, phenacetin, procaine, strychnine and xylazine. The targeted substances were chosen based on current intelligence regarding prevalent adulterants observed in multiple jurisdictions. Interference, precision, robustness and carryover were evaluated. The method was successfully validated and proved to be suitable to detect and identify the 24 target compounds proposed. The reliability of the instrument for detecting the presence of targeted compounds was analyzed by using Receiver Operating Characteristic (ROC) analysis. The portable quadrupole-based gas chromatography mass spectrometer was considered suitable for use in forensic analysis as a screening method.

PMID 32474342
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PubMedJournal of receptor and signal transduction research2014-10-25

Controversial effect on Erk activation of some cytotoxic drugs in human LOVO colon cancer cells.

Jemel-Oualha Ikram I, Elloumi-Mseddi Jihene J, Beji Abdelhamid A, Hakim Bochra B et al.

The use of some classic antibiotics was recently shown to inhibit growth and to induce apoptosis in human LOVO colon cancer cells. In this study, we describe that ciprofloxacin (CI), trimebutine maleate (COL) and tiemonium methylsulfate (VIS) greatly inhibit cell proliferation in vitro. Proliferation inhibition reached its maximum at 10(-4 )M, 10(-3 )M and 10(-2 )M, respectively, for COL, CI and VIS. Moreover, phospho-extracellular-regulated kinase was totally abrogated in non-apoptotic cytotoxicity of VIS but decreases or increases in the apoptotic inhibition, respectively, of COL and CI treatments. CI: ciprofloxacin; COL: trimebutine maleate; VIS: tiemonium methylsulfate; MAPK/Erk: mitogen-activated protein kinases/extracellular-regulated kinase.

PMID 25343691
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PubMedForensic science international2011-11-01

General unknown screening in hair by liquid chromatography-hybrid quadrupole time-of-flight mass spectrometry (LC-QTOF-MS).

Broecker Sebastian S, Herre Sieglinde S, Pragst Fritz F

The retrospective investigation of the exposure to toxic substances by general unknown screening of hair is still a difficult task because of the large number of possible poisons, the low sample amount and the difficult sample matrix. In this study the use of liquid chromatography-hybrid quadrupole time-of-flight mass spectrometry (LC-QTOF-MS) was tested as a promising technique for this purpose. In the optimized procedure, 20mg hair were decontaminated with water and acetone and two times extracted by 18h incubation with 0.5ml of a mixture of methanol/acetonitrile/H(2)O/ammonium formate at 37°C. A mixture of deuterated standards from different drug groups was added for quantification and method control. The united extracts were evaporated to a residue of 0.5ml and 5μl were injected without clean-up for LC-QTOF-MS measurement (instrument Agilent 6530) with positive electrospray ionization and in data dependent acquisition mode. For peak identification the accurate mass data base and spectral library of the authors was used which contains accurate mass CID spectra of more than 2500 and theoretically calculated accurate mass data of more than 7500 toxicologically relevant substances. Validation at the example of 24 illegal drugs, their metabolites and benzodiazepines resulted in limits of detection of 0.003-0.015ng/mg, and limits of quantification of 0.006-0.021ng/mg with good accuracy and intra- and interday reproducibility. The matrix effect by ion suppression/enhancement was 72-107% for basic drugs and 42-75% for benzodiazepines. Yields of the hair extraction above 90% were determined for 59 drugs or metabolites. The method was applied to hair samples from 30 drug fatalities and from 60 death cases with known therapeutic drug intake at life time. Altogether 212 substances were identified with a frequency per drug of 1-40 (mean 4.2) and per case of 2-33 (mean 10.2), between them 35 illegal drug related substances and 154 therapeutic drugs. Comparison with the data known from case histories and from the analysis of blood, urine and gastric content showed only a low agreement, with many unexpected drugs detected and many reported drugs not detected in hair. Basic drugs and metabolites such as opioides, cocaine, amphetamines, several groups of antidepressants, neuroleptics, beta-blockers or the metamizole metabolite noramidopyrine were found with high frequency whereas acidic and several neutral drugs such as cannabinoids, salicylic acid, furosemide, barbiturates, phenprocoumone or cardiac glycosides could not be detected with sufficient sensitivity, mainly because of the low ion yield of positive ESI for these compounds. The advantage of a comprehensive acquisition of all substances is paid by a lower sensitivity in comparison to targeted screening LC-MS/MS procedures. In conclusion, the procedure of sample preparation and LC-QTOF-MS analysis proved to be a robust and sensitive routine method in which the qualitative screening for a wide variety of toxic substances in hair is combined with the quantitative determination of selected illegal drugs.

PMID 22036310
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PubMedOrganic letters2009-07-11

Direct asymmetric catalytic thienylaluminum addition to ketones: a concise approach to the synthesis of (S)-tiemonium iodide.

Biradar Deepak B DB, Zhou Shuangliu S, Gau Han-Mou HM

A direct asymmetric addition of a (2-thienyl)aluminum reagent to ketones catalyzed by a titanium catalyst of (S)-BINOL to afford chiral tertiary 2-thienyl alcohols is reported. The catalytic system works excellently for aromatic ketones and for 1-acetylcyclohexene, furnishing products in excellent enantioselectivities of up to 97% ee. However, the additions to dialkyl ketones afford products in low enantioselectivities of 8-17% ee. Importantly, a concise 3-step synthesis of (S)-tiemonium iodide with an 84% yield is demonstrated.

PMID 19588914
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