scholarly journals Differential chemoreactome analysis of synergistic combinations of tolperisone and nonsteroidal anti-inflammatory drugs

2019 ◽  
Vol 11 (2) ◽  
pp. 78-85 ◽  
Author(s):  
I. Yu. Torshin ◽  
O. A. Gromova ◽  
L. V. Stakhovskaya ◽  
V. A. Semenov ◽  
A. N. Gromov
Keyword(s):  
Biological Activities ◽  
Muscle Relaxants ◽  
Antitumor Effects ◽  
Concurrent Use ◽  
Promising Treatment ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Muscle Hypertonia ◽  
Synergistic Combinations ◽  
Necrosis Factor

The concurrent use of muscle relaxants and nonsteroidal anti-inflammatory drugs (NSAIDs) is a promising treatment for painful muscle hypertonia and convulsive states.Objective: to identify the most effective and safe synergist combinations of tolperisone and NSAIDs.Material and methods. A differential chemoreactome analysis was employed to evaluate the effects of the muscle relaxant tolperisone and five NSAIDs (dexketoprofen, etoricoxib, meloxicam, naproxen, and diclofenac). The biological activities of the molecules under study were assessed in five sections: 1) inhibition of the proteins of prostaglandin and leukotriene metabolism; 2) inhibition of the effects of the transcription factor nuclear factor kappa, tumor necrosis factor-, and other anti-inflammatory mechanisms; 3) inhibition of excessive blood coagulation and platelet aggregation; 4) vasodynamic effects; 5) antitumor properties on cell lines in culture.Results and discussion. Based on the differences in the pharmacological activity profiles of tolperisone and NSAIDs under study, the investigators identified the most promising synergistic combinations, in which both active ingredients complemented each other as effectively and safely as possible. The obtained estimates of the degree of synergism of various combinations of tolperisone and NSAIDs hold that the most promising antithrombotic, and antitumor effects.Conclusion. The results of this study will help adequately choose combinations of muscle relaxants and NSAIDs in patients with muscle hypertonia, which will be able to improve the efficiency and safety of treatment.

scholarly journals Nonsteroidal anti-inflammatory drugs, muscle relaxants, and B-group vitamins in the treatment of lumbar ischialgia

2020 ◽  
Vol 12 (6) ◽  
pp. 71-76
Author(s):  
V. A. Shirokov ◽  
A. V. Potaturko ◽  
N. L. Terekhov
Keyword(s):  
Trigger Points ◽  
Pain Reduction ◽  
Muscle Relaxants ◽  
Mcgill Pain Questionnaire ◽  
Vitamin B ◽  
Patient Groups ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Group 2 ◽  
Group 1

Nonsteroidal anti-inflammatory drugs (NSAIDs) and muscle relaxants are used orally or intramuscularly (IM) to treat lumbar ischialgia caused by musculoskeletal disorders or radiculopathy. A comparative study has been conducted to investigate the efficacy and safety of the NSAID meloxicam (Amelotex®) injected intramuscularly and into the trigger points in combination with tolperisone and B-group vitamins for lumbar ischialgia.Patients and methods. The investigation enrolled 62 patients aged 30–60 years with lumbar ischialgia, who were randomized into three equal groups. Group 1 patients were injected with meloxicam 1.5 ml (15 mg of its active ingredient) into the trigger points daily for 3 days, followed by one 15-mg tablet daily for 14 days; Group 2 received IM meloxicam 15 mg daily for 3 days, followed by one 15-mg tablet daily for 14 days; Group 3 had IM meloxicam 15 mg daily for 3 days, followed by one 15-mg tablet daily for 14 days in combination with tolperisone (Calmirex®) as tablets: 150 mg (Day 1 of therapy), 300 mg (Day 2), and 450 mg daily (Day 3 until the end of therapy). All the patients received IM Vitamin B complex (Compligam B®) 2 ml for 5 days. The treatment efficiency was evaluated using the pain visual analogue scale (VAS), the Oswestry disability questionnaire, and the McGill pain questionnaire, the range of motion, and the severity of neurodystrophic syndrome.Results and discussion. All the patient groups showed a rapid and substantial pain reduction on the VAS and a functional activity improvement according to the Oswestry scale, which made it possible to complete the treatment within an average of 9.6 days. Groups 3 and 1 exhibited a faster improvement and, as a result, a shorter therapy duration on 8.6±1.2 and 9.2±0.9 days than did Group 2 (8.6±1.2 days). On day 2 of treatment, there was a more considerable pain reduction on the VAS in Group 1 that received meloxicam injections into the trigger zones. The administration of meloxicam intramuscularly and into the trigger zones in combination with tolperisone and vitamin B complex was noted to be safe and well tolerated.Conclusion. The injection of Amelotex into the trigger zones is highly effective and safe in treating lumbar ischialgia. An NSAID (meloxicam) in combination with a muscle relaxant (tolperisone) speeds up recovery and shortens the duration of NSAID intake.

scholarly journals Assessment of the Antiangiogenic and Anti-Inflammatory Properties of a Maslinic Acid Derivative and its Potentiation using Zinc Chloride

2019 ◽  
Vol 20 (11) ◽  
pp. 2828 ◽  
Author(s):  
Ioana Zinuca Pavel ◽  
Rene Csuk ◽  
Corina Danciu ◽  
Stefana Avram ◽  
Flavia Baderca ◽  
...  
Keyword(s):  
Zinc Chloride ◽  
Structural Changes ◽  
Biological Activities ◽  
Antitumor Effects ◽  
Pentacyclic Triterpene ◽  
Good Tolerability ◽  
Maslinic Acid ◽  
Dermal Thickness ◽  
Anti Inflammatory

Maslinic acid is a pentacyclic triterpene with a plethora of biological activities, including anti-inflammatory, antioxidant, antimicrobial, cardioprotective, and antitumor effects. New derivatives with improved properties and broad-spectrum activity can be obtained following structural changes of the compound. The present study was aimed to characterize a benzylamide derivative of maslinic acid—benzyl (2α, 3β) 2,3-diacetoxy-olean−12-en-28-amide (EM2)—with respect to the anti-angiogenic and anti-inflammatory effects in two in vivo experimental models. Consequently, the compound showed good tolerability and lack of irritation in the chorioallantoic membrane assay with no impairment of the normal angiogenic process during the tested stages of development. In the acute ear inflammation murine model, application of EM2 induced a mild anti-inflammatory effect that was potentiated by the association with zinc chloride (ZnCl2). A decrease in dermal thickness of mice ears was observed when EM2 and ZnCl2 were applied separately or in combination. Moreover, hyalinization of the dermis appeared only when EM2 was associated with ZnCl2, strongly suggesting the role of their combination in wound healing.

Synthesis and Anti-Inflammatory Activity of 3-Aryloxylindolizine Derivatives via Sonogashira Coupling/5-endo-trig Cycloisomerization Domino Strategy

2013 ◽  
Vol 781-784 ◽  
pp. 1093-1097 ◽  
Author(s):  
Yong Wei ◽  
Cheng Qiao Cao ◽  
Jian Feng Chen ◽  
Kun Zou ◽  
Zhang Shuang Deng ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Elemental Analysis ◽  
Biological Activities ◽  
Bacterial Lipopolysaccharide ◽  
Sonogashira Coupling ◽  
Propargyl Ether ◽  
Mouse Cells ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Stimulation Of

With the aim of obtaining potential IL-6 inhibitor for the treatment of rheumatoid arthritis, four 3-aryloxylindolizine derivatives were synthesized from the 2-bromopyridine and aryl propargyl ether through the Sonogashira coupling/5-endo-trigcycloisomerization domino strategy. These compounds were characterized by NMR, IR, EI-MS and elemental analysis. Their biological activities were evaluated by the bacterial lipopolysaccharide (LPS) stimulation of mouse cells on the RAW264.7 inflammation model. All the compounds revealed good anti-inflammatory activities with the inhibitions of 71~82% against IL-6 at 100 μM. The bioactive 3-aryloxylindolizines might be used as potential anti-inflammatory drugs.

scholarly journals Interaction of indomethacin with calf thymus DNA: a multi-spectroscopic, thermodynamic and molecular modelling approach

MedChemComm ◽  
2017 ◽  
Vol 8 (6) ◽  
pp. 1283-1296 ◽  
Author(s):  
Mohammed Amir Husain ◽  
Hassan Mubarak Ishqi ◽  
Tarique Sarwar ◽  
Sayeed Ur Rehman ◽  
Mohammad Tabish
Keyword(s):  
Acetic Acid ◽  
Acid Derivative ◽  
Molecular Modelling ◽  
Biological Activities ◽  
Calf Thymus Dna ◽  
Calf Thymus ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Modelling Approach

Indomethacin belongs to the acetic acid derivative class of non-steroidal anti-inflammatory drugs with diverse pharmacological and biological activities.

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