Effects of tolmetin: A Synthesis of Findings from 28 Studies

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Original Abstract of the Article

Major Research Findings

Tolmetin is a nonsteroidal anti-inflammatory drug (NSAID) that has been shown to have a variety of effects. 15 found that tolmetin hydrazide-hydrazones, a novel series of compounds, demonstrated anti-cancer activity by inducing apoptosis in colon cancer cells, specifically targeting caspase-8 and caspase-9. 4 investigated the efficacy of tolmetin in protecting the stomach and duodenum from injury. The study found that misoprostol was significantly more effective than cimetidine in protecting the gastric mucosa from tolmetin-induced injury. 20 explored the gastroprotective effect of amtolmetin guacyl (AMG), a prodrug of tolmetin, in mice. 8 and 17 delve into the effects of amtolmetin guacyl on lipid peroxidation and antioxidant systems in different models of gastrointestinal injury. 14 discusses the role of NSAIDs in osteoarthritis and categorizes them based on their effect on glycosaminoglycan synthesis. Tolmetin is categorized as stimulatory. 1 investigates the gastroprotective effects of amtolmetin guacyl in rats and suggests that the gastro-sparing effect is due to the production of nitric oxide. 18 shows that tolmetin binds to human serum albumin (HSA). 21 , 7 , 2 , 27 , and 12 demonstrate that tolmetin is metabolized to reactive metabolites. 9 , 26 , 11 , 25 , and 23 show that tolmetin can have developmental toxicity in animals. 28 explores the relationship between the pharmacokinetics and antinociceptive effect of tolmetin in rats. 19 demonstrates that ketorolac, another NSAID, is effective in controlling postoperative pain in pediatric orthopedic patients. 5 explores the molecular characteristics of the inhibition of human neutrophil elastase by NSAIDs. 16 proposes a new classification of NSAIDs based on their reactivity with peroxidase. 10 investigates the scavenging activity of tolmetin for reactive oxygen species (ROS) and reactive nitrogen species (RNS) using in vitro systems.

Benefits and Risks

Benefit Summary

Tolmetin has been shown to be effective in treating inflammation, pain, and osteoarthritis. It also has gastroprotective effects and can be used to treat postoperative pain in children. Tolmetin has the potential to scavenge reactive oxygen species (ROS) and reactive nitrogen species (RNS).

Risk Summary

Tolmetin can cause gastrointestinal issues, such as ulcers, and may have developmental toxicity in animals.

Comparison of Studies

Commonalities Among Studies

Many studies confirm that tolmetin has anti-inflammatory and analgesic properties. Additionally, the studies indicate that tolmetin can be beneficial in protecting the stomach lining.

Differences Among Studies

There is variation in the specific effects and mechanisms of action of tolmetin. Some studies show that tolmetin has anti-cancer effects, while others focus on its gastroprotective properties. Some studies explore the role of metabolites and their potential toxicity, while others examine the influence of tolmetin on development. The specific effects of tolmetin may depend on the form of the drug (e.g. prodrug), the dosage, and the duration of treatment.

Consistency and Contradictions of Results

While consistent evidence supports the anti-inflammatory and analgesic properties of tolmetin, its potential for gastrointestinal side effects and developmental toxicity in animals requires further investigation. The specific mechanisms of action and the impact of metabolites on the body are not fully understood. The data suggests that the effects of tolmetin can vary depending on factors such as dosage, duration of treatment, and individual variations. Further research is needed to fully elucidate the effects of tolmetin.

Considerations for Real-Life Application

It is important to use tolmetin according to a doctor's instructions. To minimize potential gastrointestinal side effects, it is best to avoid taking tolmetin on an empty stomach or when experiencing an upset stomach. Tolmetin is not recommended for use during pregnancy or breastfeeding. Tolmetin can interact with other medications, so it is essential to consult with a doctor or pharmacist before taking it.

Current Limitations of Research

More research is necessary to comprehensively understand the effects and potential risks of tolmetin. This includes investigating the specific roles of metabolites, their effects on the body, and the impact of tolmetin on development, particularly in humans. Further research is also required to explore the optimal dosage and duration of treatment for various conditions, considering individual variations and potential interactions with other medications.

Directions for Future Research

Future research should focus on characterizing the specific metabolites of tolmetin and their effects on the body. This includes investigating the mechanisms of their action and their potential for toxicity. Additionally, more research is needed to understand the developmental effects of tolmetin, particularly in human populations. Studies investigating the long-term effects of tolmetin, including its impact on various organs and systems, are essential. Finally, research should aim to develop safer and more effective formulations of tolmetin to minimize potential side effects and maximize therapeutic benefits.

Conclusion

Tolmetin is an NSAID with a variety of effects, including anti-inflammatory and analgesic properties. It has also shown gastroprotective effects and potential to scavenge ROS and RNS. However, potential risks include gastrointestinal side effects and developmental toxicity in animals. More research is needed to fully understand the effects and risks of tolmetin. Remember to consult with a healthcare professional before using tolmetin to ensure its safe and effective use.

Literature analysis of 28 papers
Positive Content
19
Neutral Content
4
Negative Content
5
Article Type
2
0
0
2
28
2.

Limitations of hepatocytes and liver homogenates in modelling in vivo formation of acyl glucuronide-derived drug-protein adducts.

Author: BaileyM J, DickinsonR G

Drug toxicity

The patterns of covalent binding of zomepirac (ZP) to proteins in the livers of intact rats, isolated rat hepatocytes, and in rat liver homogenates were compared.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

3.

Effect of beta-cyclodextrin complexation on the photochemical and photosensitizing properties of tolmetin: a steady-state and time-resolved study.

Author: SortinoS, ScaianoJ C, De GuidiG, MontiS

Protection against damage
Reduced photodecomposition
None mentioned

Beta-cyclodextrin complexation was found to reduce the photochemical and photosensitizing properties of tolmetin. This complexation protected against the drug-induced damage on biological substrates.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

4.

Double-blind, placebo-controlled endoscopic comparison of the mucosal protective effects of misoprostol versus cimetidine on tolmetin-induced mucosal injury to the stomach and duodenum.

Author: LanzaF L, AspinallR L, SwabbE A, DavisR E, RackM F, RubinA

Duodenal mucosal protection
Gastric mucosal protection

Misoprostol was more effective than cimetidine in protecting the gastric mucosa from tolmetin-induced injury in 90 volunteers. Both drugs were highly protective in the duodenum.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Controlled Clinical TrialA clinical trial that evaluates the effectiveness of a treatment by comparing a group that receives the intervention with a group that receives a placebo or standard treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.

Language : English

5.

Molecular characteristics of the inhibition of human neutrophil elastase by nonsteroidal antiinflammatory drugs.

Author: KangK, BaeS J, KimW M, LeeD H, ChoU, LeeM H, LeeM S, NamS, KuettnerK E, SchwartzD E

Anti-inflammatory effect

This study investigated the inhibition of human neutrophil elastase (HNElastase) by various nonsteroidal anti-inflammatory drugs (NSAIDs). Phenylbutazone showed strong inhibition, suggesting a potential mechanism of action for NSAIDs beyond cyclooxygenase inhibition.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
Research Support, U.S. Gov't, P.H.S.Research funding provided by the Public Health Service (PHS).

Language : English

6.

Lipid-drug interaction: biophysical effects of tolmetin on membrane mimetic systems of different dimensionality.

Author: NunesCláudia, BrezesinskiGerald, LopesDaniela, LimaJosé L F C, ReisSalette, LúcioMarlene

Gastrointestinal toxicity

Tolmetin, a nonsteroidal anti-inflammatory drug (NSAID), interacts with lipid membranes, and its interaction is strongly dependent on the degree of drug ionization and the lipid phase state.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

8.

In vivo effects of amtolmetin guacyl on lipid peroxidation and antioxidant defence systems. Comparison with non-selective and COX-2 selective NSAIDs.

Author: KirkovaM, AlexandovaA, KesiovaM, TodorovS

Gastric tolerability

This study compared the in vivo effects of amtolmetin guacyl, a pro-drug of the NSAID tolmetin, with other NSAIDs on lipid peroxidation, glutathione levels, and antioxidant enzyme activity in rat tissues. Amtolmetin guacyl showed no pro-oxidant effects, suggesting improved gastric tolerability.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

9.

Treatment of congenital nephrogenic diabetes insipidus by hydrochlorothiazide and cyclooxygenase-2 inhibitor.

Author: PattaragarnAnirut, AlonUri S

Treatment of cNDI

This study describes a case of congenital nephrogenic diabetes insipidus (cNDI) in a 1-month-old infant successfully treated with a combination of hydrochlorothiazide (HCTZ) and rofecoxib. This combination was effective in decreasing urinary free water losses and had no side effects.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

10.

In vitro scavenging activity for reactive oxygen and nitrogen species by nonsteroidal anti-inflammatory indole, pyrrole, and oxazole derivative drugs.

Author: FernandesEduarda, CostaDavid, TosteSofia A, LimaJosé L F C, ReisSalette

Anti-inflammatory effect
RNS scavenging
ROS scavenging

Certain nonsteroidal anti-inflammatory drugs (NSAIDs) were found to have scavenging activity against reactive oxygen species (ROS) and reactive nitrogen species (RNS), potentially contributing to their anti-inflammatory effects.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

11.

Skeletal developmental effects of selective and nonselective cyclooxygenase-2 inhibitors administered through organogenesis and fetogenesis in Wistar CRL:(WI)WUBR rats.

Author: BurdanFranciszek, SzumiloJustyna, MarzecBarbara, KlepaczRobert, DudkaJaroslaw

Femoral epiphyses safety
Joint formation safety
Skeletal variations

This study evaluated the prenatal skeletal effects of selective and nonselective COX-2 inhibitors in pregnant rats. While nonselective inhibitors showed skeletal variations at high doses, neither selective nor nonselective COX-2 inhibitors disturbed joint formation or morphology of femoral epiphyses.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

12.

Evidence for the bioactivation of zomepirac and tolmetin by an oxidative pathway: identification of glutathione adducts in vitro in human liver microsomes and in vivo in rats.

Author: ChenQing, DossGeorge A, TungElaine C, LiuWensheng, TangYui S, BraunMatthew P, DidolkarVarsha, StraussJohn R, WangRegina W, StearnsRalph A, EvansDavid C, BaillieThomas A, TangWei

Anaphylactic reactions

Zomepirac (ZP) and tolmetin (TM) induce anaphylactic reactions and form reactive acyl glucuronides.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

14.

The influence of tissue cross-talking on OA progression: role of nonsteroidal antiinflammatory drugs.

Author: PelletierJ P

Osteoarthritis treatment

Osteoarthritis is a complex illness involving bone, synovial tissue, and cartilage. Nonsteroidal antiinflammatory drugs can be categorized into three classes based on their effects on glycosaminoglycan synthesis in chondrocytes.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

15.

Synthesis of Tolmetin Hydrazide-Hydrazones and Discovery of a Potent Apoptosis Inducer in Colon Cancer Cells.

Author: KüçükgüzelŞ Güniz, KoçDerya, Çıkla-SüzgünPelin, ÖzsavcıDerya, Bingöl-ÖzakpınarÖzlem, Mega-TiberPınar, OrunOya, ErzincanPınar, Sağ-ErdemSafiye, ŞahinFikrettin

Anti-cancer activity
Apoptotic pathway activation
Cytotoxicity

A novel tolmetin hydrazide-hydrazone (4g) exhibited anti-cancer activity against colon cancer cell lines HT-29 and did not display cytotoxicity towards control NIH3T3 cells. This anti-cancer activity was attributed to the activation of caspase-8 and caspase-9 involved in the apoptotic pathway.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

16.

[Direction of strategic use: a new classification of non-steroidal anti-inflammatory drugs based on reactivity with peroxidase].

Author: MiuraToshiaki

Anti-inflammatory effects
Side effects

A new classification of non-steroidal anti-inflammatory drugs (NSAIDs) has been proposed based on their reactivity to peroxidase. The best drug for each inflammatory disease should be selected for therapy.

English AbstractA summary of a research paper/publication written in English for a wider audience.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : Japanese

17.

In vivo effects of amtolmetin guacyl on lipid peroxidation and antioxidant defence systems in different models of gastrointestinal injury.

Author: KirkovaM, KesiovaM, KonstantinovaS, AlexandrovaA, PetrovL, TsvetanovaE, TodorovS

Antioxidant activity
NSAID-induced damage prevention

Amtolmetin guacyl (AMG), a non-steroid anti-inflammatory drug (NSAID), was shown to possess antioxidant activity and limited the adverse actions of other NSAIDs, ethanol, and 2,4,6-trinitrobenzenesulfonic acid (TNBS) in various experimental models of free radical-induced damage.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

21.

In vitro reactivity of carboxylic acid-CoA thioesters with glutathione.

Author: SideniusUlrik, SkonbergChristian, OlsenJørgen, HansenSteen Honoré

Adverse Effects

This study investigated the reactivity of acyl-CoA thioesters toward the tripeptide, glutathione. The results suggest that the reactivity of acyl-CoAs with glutathione is dependent on the structure of the acyl-CoA.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

22.

Morphological features of rat gastric mucosa after acute and chronic treatment with amtolmetin guacyl: comparison with non-selective and COX-2-selective NSAIDs.

Author: MoriniGiuseppina, GuaitaElena, LazzarettiMirka, GrandiDaniela, CoruzziGabriella

Lower ulcerogenicity

Amtolmetin guacyl (AMG) is a non-selective non-steroidal anti-inflammatory drug (NSAID) with lower ulcerogenicity compared to traditional NSAIDs. This is due to its unique mechanism of action, which involves increasing the endogenous production of gastric nitric oxide.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.

Language : English

23.

Maternal toxicity of nonsteroidal anti-inflammatory drugs as an important factor affecting prenatal development.

Author: BurdanFranciszek, SzumiloJustyna, KlepaczRobert

Developmental abnormalities

This study aimed to assess maternal effects of non-selective cyclooxygenase (COX) inhibitors on developmental abnormalities in rats. While previous studies showed toxicities associated with these drugs, this study focused on specific developmental abnormalities.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

24.

Developmental outcome after exposure to cyclooxygenase inhibitors during pregnancy and lactation.

Author: BurdanFranciszek, Pliszczynska-SteudenMalgorzata, Rozylo-KalinowskaIngrid, ChalasAnna, RozyloT Katarzyna, StaroslawskaElzbieta, KlepaczRobert, SzumiloJustyna

Bone problems

Ibuprofen, piroxicam, and tolmetin, non-selective cyclooxygenase inhibitors, did not cause any teratogenic effects in rats, but they affected pup growth and the mineralization of the lumbar vertebrae.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

25.

Developmental toxicity evaluation of ibuprofen and tolmetin administered in triple daily doses to Wistar CRL:(WI)WUBR rats.

Author: BurdanFranciszek

Prenatal effects

Ibuprofen and tolmetin are commonly used non-steroidal anti-inflammatory drugs. Previous studies showed that these drugs are safe for pregnant animals when given in single doses. However, this study found that triple daily doses of these drugs had developmental effects on offspring in pregnant animals.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

26.

Cyclooxygenase inhibitors affect bone mineralization in rat fetuses.

Author: BurdanFranciszek, Rozylo-KalinowskaIngrid, SzumiloJustyna, DudkaJaroslaw, KlepaczRobert

Fetal bone mineralization decrease
Intrauterine growth retardation

Nonselective COX inhibitors (ibuprofen, piroxicam, tolmetin) were found to decrease fetal bone mineralization in rats, unlike the selective COX-2 inhibitor DFU.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

27.

Studies on the metabolism of tolmetin to the chemically reactive acyl-coenzyme A thioester intermediate in rats.

Author: OlsenJørgen, LiChunze, SkonbergChristian, BjørnsdottirInga, SideniusUlrik, BenetLeslie Z, HansenSteen Honoré

Covalent binding
Tolmetin metabolism
Clofibric acid treatment
Reactive metabolites

Tolmetin, a carboxylic acid, is metabolized to reactive metabolites in rats, including tolmetin acyl-CoA (Tol-CoA), which can bind covalently to liver proteins. Clofibric acid pretreatment significantly increases Tol-CoA levels and covalent binding to liver proteins, suggesting a potential role for Tol-CoA in drug-induced liver toxicity.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

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