"Ebastine studies" about Ebastine Review Consensus 10 by CarPas (5225 pt) | 2022-Sep-09 11:50 |
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Compendium of the most significant studies with reference to properties, intake, effects.
Sastre J. Ebastine in allergic rhinitis and chronic idiopathic urticaria. Allergy. 2008 Dec;63 Suppl 89:1-20. doi: 10.1111/j.1398-9995.2008.01897.x.
Abstract. Histamine is a key mediator in the development of allergy symptoms, and oral H(1)-antihistamines are among the most widely used treatments for symptomatic relief in conditions such as allergic rhinitis and chronic urticaria. Ebastine is a second-generation antihistamine which has been shown to be an effective treatment for both seasonal and perennial allergic rhinitis. In controlled clinical trials in adult and adolescent patients with allergic rhinitis, ebastine 10 mg once-daily improved symptoms to a significantly greater extent than placebo and to a similar extent as loratadine 10 mg and cetirizine 10 mg (both once-daily), while ebastine 20 mg proved to be more effective than these two comparator antihistamines. In addition, ebastine was significantly more effective than placebo at relieving the symptoms of chronic idiopathic urticaria. Ebastine provides efficacy throughout the 24-h dosing interval with once-daily administration and clinical benefit is seen from the first day of treatment. Small studies have found beneficial effects for ebastine in patients with other disorders, including cold urticaria, dermographic urticaria, atopic asthma, mosquito bites and (in combination with pseudoephedrine) the common cold. In addition to the regular ebastine tablet, a fast-dissolving tablet (FDT) formulation, which disintegrates in the mouth without the aid of a drink, is also available. It has been shown to be bioequivalent to the regular tablet, and to be significantly more effective than desloratadine at reducing histamine-induced cutaneous wheals. A number of patient surveys demonstrated that the majority of individuals who tried the fast-dissolving formulation reported it to be convenient for use, fast-acting and preferred it to their previous antihistamine medication. Perhaps most importantly, a large proportion of patients indicated that they would prefer to use this new formulation in the future. Ebastine has a rapid onset of action and it can be administered once-daily, with or without food. Dose modifications are not needed in elderly patients, or in those with renal or mild to moderate hepatic impairment. Ebastine is generally well-tolerated, and clinical studies showed that at usual therapeutic doses of 10 and 20 mg once-daily, it had no clinically relevant adverse effects on cognitive function and psychomotor performance or on cardiovascular function. In conclusion, ebastine is an effective and generally well-tolerated treatment for allergic rhinitis and chronic idiopathic urticaria. In addition to the regular tablet formulation, ebastine is available as a FDT, providing a treatment option that is particularly convenient for patients.
Hurst M, Spencer CM. Ebastine: an update of its use in allergic disorders. Drugs. 2000 Apr;59(4):981-1006. doi: 10.2165/00003495-200059040-00018.
Abstract. ...Conclusions: Ebastine 10 mg daily is a well tolerated and effective treatment for allergic rhinitis and chronic idiopathic urticaria. At this dosage, it is as effective as the other second-generation antihistamines against which it has been compared. Ebastine 20 mg has similar tolerability to the 10 mg dose, and trends towards greater efficacy with the higher dose have been shown in some studies. Ebastine does not appear to be associated with any significant cardiac adverse events. Ebastine is a useful treatment option for patients with allergic rhinitis or chronic idiopathic urticaria.
Sastre J. Ebastine in the Treatment of Allergic Rhinitis and Urticaria: 30 Years of Clinical Studies and Real-World Experience. J Investig Allergol Clin Immunol. 2020;30(3):156-168. doi: 10.18176/jiaci.0401.
Abstract. Histamine, acting predominantly via the H1-receptor, is an important mediator of the symptoms of allergy. H1-antihistamines, which stabilize the receptor in its inactive form, are the treatment of choice for some chronic allergic conditions. Ebastine is a well-established secondgeneration oral H1-antihistamine that is administered once daily at a dose of 10-20 mg and is available both as a standard tablet and as a fast-dissolving tablet that disintegrates in the mouth. Ebastine has been shown to relieve symptoms in patients with allergic rhinitis or urticaria in multiple clinical trials. In addition to its antihistamine effects, the drug has modulating effects on the allergic inflammatory process, thus potentially explaining its beneficial effect on nasal obstruction in some patients. Ebastine is generally well tolerated at recommended doses and is one of the lowest-risk antihistamines with respect to adverse cognitive/psychomotor effects, as confirmed by decades of pharmacovigilance. New long-term data confirm its efficacy and tolerability during up to 1 year of treatment in patients with chronic urticaria.
Dhakal B, Thakur JK, Mahato RK, Rawat I, Rabin DC, Chhetri RR, Shah KP, Adhikari A, Pandey J. Formulation of Ebastine Fast-Disintegrating Tablet Using Coprocessed Superdisintegrants and Evaluation of Quality Control Parameters. ScientificWorldJournal. 2022 May 19;2022:9618344. doi: 10.1155/2022/9618344.
Abstract. ...This project was aimed to formulate and characterize orodispersible tablets of ebastine, utilizing different proportions of three disintegrants, namely crospovidone, sodium starch glycolate, and coprocessed superdisintegrant. ...Copyright © 2022 Bhawana Dhakal et al.
Frare RG, Singh AK. A Critical Review of Physicochemical Properties and Analytical Methods Applied to Quantitative Determination of Ebastine. Crit Rev Anal Chem. 2018 Mar 4;48(2):102-109. doi: 10.1080/10408347.2017.1412816.
Abstract. Allergic diseases are the most common conditions in children and the second most frequent in adults. Currently, there are two well-defined generations of antihistamines, those belonging to first generation, with inherent side effects such as drowsiness and anticholinergic effects. These side effects are often attributed to their high lipophilicity and high affinity for brain H1 receptors. The ebastine is a modern antihistaminic drug belongs to the second generation and has lower lipophilicity, which diminish the undesirable side effects. To ensure the quality, efficacy, safety, and effectiveness of ebastine drug products, efficient and reliable analytical methods are mandatory. Besides official compendial methods, alternative methods are often developed and used in quality control of pharmaceuticals as well as in pharmacokinetic studies. In this work, we present a critical review on characteristics, physicochemical properties, and analytical methods applied in the analysis of ebastine.
Goyal V, Gupta A, Gupta O, Lal D, Gill M. Comparative Efficacy and Safety of Ebastine 20 mg, Ebastine 10 mg and Levocetirizine 5 mg in Acute Urticaria. J Clin Diagn Res. 2017 Mar;11(3):WC06-WC09. doi: 10.7860/JCDR/2017/23961.9550.
Abstract. ...Aim: To compare the safety and efficacy of ebastine 20 mg, ebastine 10 mg and levocetirizine 5 mg in the patients of urticaria....Conclusion: Ebastine 20 mg is found to have superior efficacy for treatment of Urticaria as compared to ebastine 10 mg but with levocetirizine 5 mg the results were almost similar. Tolerability of ebastine 20 mg is similar to ebastine 10 mg but with levocetirizine 5 mg there were more side effects and less tolerability.
Schmidt AH, Molnár I. Using an innovative Quality-by-Design approach for development of a stability indicating UHPLC method for ebastine in the API and pharmaceutical formulations. J Pharm Biomed Anal. 2013 May 5;78-79:65-74. doi: 10.1016/j.jpba.2013.01.032.
Abstract. A stability-indicating ultra high performance liquid chromatographic (UHPLC) method has been developed for purity testing of ebastine and its pharmaceutical formulations. ...Copyright © 2013 Elsevier B.V.
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"Description" about Ebastine Review Consensus 10 by CarPas (5225 pt) | 2023-Oct-05 09:34 |
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Ebastine is a chemical compound consisting of 1-(4-(tert-butyl)phenyl)-4-(4-hydroxypiperidin-1-yl)butan-1-one (5.1.9) in a rather complex preliminary chemical process, which takes place in several steps and involves sodium bicarbonate, methyl isobutyl ketone and potassium iodide. Subsequently, benzhydryl bromide and sodium carbonate are used to obtain the finished product.
It appears as a white powder, insoluble in water, soluble in dichloromethane, slightly soluble in methanol, highly permeable in the lipid membrane.
What it is used for and where
Medical
Take only under medical supervision
Ebastine is a member of the class of drugs called selective non-sedating inhibitors of the histamine H1 receptor. Its action involves bronchi, blood capillaries and some smooth muscles, a receptor antagonist with an oxypiperidine structure, the active form of which is the metabolite carebastine.
Histamine is an important mediator of allergy symptoms that generally acts via the H1 receptor, is released during the initial phase of the immune response, and the treatment of choice for allergic conditions are H1 antihistamines, which tend to stabilise the H1 receptor in its inactive form. H1 antihistamines, which stabilise the receptor in its inactive form, are recognised as the primary treatment in international guidelines for treating urticaria and allergic rhinitis.
Among the second-generation H1-type antihistamines, Ebastine has been marketed worldwide since 1990 for the treatment of urticaria and allergic rhinitis, has no sedative activity, and is long-acting. It is also effective against motion sickness. The dosage form is generally the solid tablet in which flavourings may be present to improve the taste and 'superdisintegrants', e.g. Povidone, may be present to aid dissolution and increase water absorption.
In an in vitro study in nasal polyp cells, ebastine inhibited anti-IgE-induced release of leukotrienes C4/D4 and prostaglandin D2 (P<.05). It also inhibited tumour necrosis factor-α and interleukin 8 caused by the release of granulocyte-macrophage colony-stimulating factor (1). Among the various antihistamines on the market, it is also worth noting that ebastine showed superior effects to carebastine.
A recent study by researchers from University Centres in Huston, New York and Chicago, USA, based on the examination of Polycomb group proteins, chromatin and the transcriptional suppressor methylating H3, found that treatment with ebastine effectively reduced the progression and growth of breast cancer and improved progression-free survival. Thus, from these results, ebastine may prove to be a promising therapy for tumours with EZH mutations or overexpression carriers (2).
To summarise, ebastine can be useful in:
The most relevant studies on this chemical compound have been selected with a summary of their contents:
Appearance | White powder |
Boiling Point | 596.3±50.0°C at 760 mmHg |
Melting Point | 80-82°C |
Density | 1.1±0.1 g/cm3 |
Flash Point | 314.5±30.1°C |
Solubility | 1 mM 2.1292 mL 10.6460 mL 21.2920 mL 5 mM 0.4258 mL 2.1292 mL 4.2584 mL 10 mM 0.2129 mL 1.0646 mL 2.1292 mL |
PSA | 29.54000 |
LogP | 7.79 |
Refraction Index | 1.590 |
Vapor Pressure | 0.0±1.7 mmHg at 25°C |
Price
10 mg $236.00
50 mg $938.00
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Synonyms
References______________________________________________________________________
(1) Campbell A, Michel FB, Bremard-Oury C, Crampette L, Bousquet J. Overview of allergic mechanisms. Ebastine has more than an antihistamine effect. Drugs. 1996;52 Suppl 1:15-9. doi: 10.2165/00003495-199600521-00005.
(2) Li Q, Liu KY, Liu Q, Wang G, Jiang W, Meng Q, Yi Y, Yang Y, Wang R, Zhu S, Li C, Wu L, Zhao D, Yan L, Zhang L, Kim JS, Zu X, Kozielski AJ, Qian W, Chang JC, Patnaik A, Chen K, Cao Q. Antihistamine Drug Ebastine Inhibits Cancer Growth by Targeting Polycomb Group Protein EZH2. Mol Cancer Ther. 2020 Oct;19(10):2023-2033. doi: 10.1158/1535-7163.MCT-20-0250.
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"Nimesulide studies" about Nimesulide Review Consensus 10 by CarPas (5225 pt) | 2022-May-03 16:54 |
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Compendium of the most significant studies with reference to properties, intake, effects.
Senna GE, Passalacqua G, Andri G, Dama AR, Albano M, Fregonese L, Andri L. Nimesulide in the treatment of patients intolerant of aspirin and other NSAIDs. Drug Saf. 1996 Feb;14(2):94-103. doi: 10.2165/00002018-199614020-00004.
Abstract. Aspirin (acetylsalicylic acid) and other NSAIDs are responsible for many adverse effects. Among them, pseudo-allergic reactions (urticaria/angioedema, asthma, anaphylaxis) affect up to 9% of the population and up to 30% of asthmatic patients. The mechanisms provoking these reactions have not been fully elucidated, but it appears that inhibition of cyclo-oxygenase (COX) plays a central role. The anti-inflammatory action of nimesulide differs from that of other NSAIDs, possibly because of its chemical structure. In particular, nimesulide is selective for COX-2 and displays additional properties in terms of its effects on inflammatory mediator synthesis and release. For these reasons, nimesulide is generally well tolerated by NSAID-intolerant patients and patients with NSAID-induced asthma. The good tolerability of nimesulide as an alternative drug for use in patients with NSAID intolerance has been demonstrated in a large number of clinical studies.
Wei W, Evseenko VI, Khvostov MV, Borisov SA, Tolstikova TG, Polyakov NE, Dushkin AV, Xu W, Min L, Su W. Solubility, Permeability, Anti-Inflammatory Action and In Vivo Pharmacokinetic Properties of Several Mechanochemically Obtained Pharmaceutical Solid Dispersions of Nimesulide. Molecules. 2021 Mar 10;26(6):1513. doi: 10.3390/molecules26061513.
Abstract. The objective of the present study was to investigate the possibility of improving the solubility and the bioavailability of Nimesulide via complexation with polysaccharide arabinogalactan (AG), disodium salt of glycyrrhizic acid (Na2GA), hydroxypropyl-β-cyclodextrin (HP-β-CD) and MgCO3.
Ferreira RG, Narvaez LEM, Espíndola KMM, Rosario ACRS, Lima WGN, Monteiro MC. Can Nimesulide Nanoparticles Be a Therapeutic Strategy for the Inhibition of the KRAS/PTEN Signaling Pathway in Pancreatic Cancer? Front Oncol. 2021 Jul 20;11:594917. doi: 10.3389/fonc.2021.594917.
Abstract. ....However, there is a need to improve nimesulide through its encapsulation by solid lipid nanoparticles to overcome problems related to the hepatotoxicity and bioavailability of the drug.
Bernareggi A. Clinical pharmacokinetics of nimesulide. Clin Pharmacokinet. 1998 Oct;35(4):247-74. doi: 10.2165/00003088-199835040-00001.
Abstract. Nimesulide is a selective COX-2 inhibitor used in a variety of inflammatory, pain and fever states. After healthy volunteers received oral nimesulide 100 mg in tablet, granule or suspension form the drug was rapidly and extensively absorbed. Mean peak concentrations (Cmax) of 2.86 to 6.50 mg/L were achieved within 1.22 to 2.75 hours of administration. The presence of food did not reduce either the rate or extent of nimesulide absorption. When nimesulide was administered in the suppository form, the Cmax was lower and occurred later than after oral administration; the bioavailability of nimesulide via suppository ranged from 54 to 64%, relative to that of orally administered formulations.....
Kshirsagar NA, Bachhav SS. Nimesulide controversy: a comparison of EU and Indian scenario. Int J Risk Saf Med. 2013;25(4):239-46. doi: 10.3233/JRS-130602.
Abstract. To compare and evaluate, benefit and risk data for regulatory action, of nimesulide in India and EU.
Kasciuškevičiūtė S, Gumbrevičius G, Vendzelytė A, Ščiupokas A, Petrikonis K, Kaduševičius E. Impact of the World Health Organization Pain Treatment Guidelines and the European Medicines Agency Safety Recommendations on Nonsteroidal Anti-Inflammatory Drug Use in Lithuania: An Observational Study. Medicina (Kaunas). 2018 May 11;54(2):30. doi: 10.3390/medicina54020030.
Abstract. Background and objective: Irrational use of nonsteroidal anti-inflammatory drugs (NSAIDs) is the main cause of adverse effects-associated hospitalizations among all medication groups leading to extremely increased costs for health care.
Pulkkinen M. Nimesulide in dysmenorrhoea. Drugs. 1993;46 Suppl 1:129-33. doi: 10.2165/00003495-199300461-00028.
Abstract. Nimesulide does not affect active intrauterine pressure, as measured using microsensors, or the direction and velocity of the propagation of uterine activity, but nevertheless alleviates pain significantly by 30 minutes after oral administration. In dysmenorrhoeic patients, resting pressure is high only in the fundus.....
Raupp ÍN, Valério Filho A, Arim AL, Muniz ARC, da Rosa GS. Development and Characterization of Activated Carbon from Olive Pomace: Experimental Design, Kinetic and Equilibrium Studies in Nimesulide Adsorption. Materials (Basel). 2021 Nov 12;14(22):6820. doi: 10.3390/ma14226820.
Abstract. This work aims to develop and characterize an activated charcoal from olive pomace, which is an agro-industrial residue, for adsorption of Nimesulide in liquid effluent and to evaluate the adsorption kinetics and equilibrium using experimental design.
Santos BFE, Costa FO, Vasconcelos AMA, Cyrino RM, Cota LOM. Preemptive effects of ibuprofen and nimesulide on postoperative pain control after open flap periodontal surgeries: A randomized placebo-controlled split-mouth clinical trial. J Periodontol. 2022 Feb;93(2):298-307. doi: 10.1002/JPER.20-0887.
Abstract. The aim of this study was to evaluate and compare the analgesic effects of the preemptive administration of ibuprofen and nimesulide in open flap periodontal surgeries.
Bessone F, Hernandez N, Mendizabal M, Ridruejo E, Gualano G, Fassio E, Peralta M, Fainboim H, Anders M, Tanno H, Tanno F, Parana R, Medina-Caliz I, Robles-Diaz M, Alvarez-Alvarez I, Niu H, Stephens C, Colombato L, Arrese M, Reggiardo MV, Ono SK, Carrilho F, Lucena MI, Andrade RJ. Serious liver injury induced by Nimesulide: an international collaborative study. Arch Toxicol. 2021 Apr;95(4):1475-1487. doi: 10.1007/s00204-021-03000-8.
Abstract. We aim to analyze the clinical phenotype, outcome, and histological features of nimesulide-induced liver injury (nimesulide-DILI). We analyzed 57 cases recruited from the Spanish and Latin American DILI registries.
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"Descrizione" about Nimesulide Review Consensus 10 by CarPas (5225 pt) | 2023-Sep-11 11:01 |
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Nimesulide is a chemical compound, sulphonamide.
It occurs in the form of a yellow powder. Stable. Incompatible with strong oxidising agents.
What it is used for and where
Medicine
Take only under medical supervision
Non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties, launched in 1985 in Italy and marketed in more than 50 countries worldwide with relatively low risk of gastrointestinal side effects. Not available in the United States.
Brief history
Nimesulide was reported to be hepatotoxic in 1997 and its use was restricted or banned in 2002 first in Finland and then in Spain due to the high frequency of associated hepatotoxicity (1). However, several studies have downgraded the problem and the European Medicines Agency (2), after an extensive study, recognised its efficacy in
taking into account the risk/benefit ratio, only recommended a maximum daily dose for the 100mg dose. Stricter restrictions apply to the 200mg dose.
An important study from 2010 clarifies the risk/benefit ratio comprehensively: "Results suggest that implementation of regulatory actions regarding nimesulide may have prevented 79 admissions for liver damage, but increased admissions for UGIB by 859 cases."
Nimesulide as a preferential inhibitor of cyclooxygenase-2 could play a potential therapeutic role in the management of patients with cerebral ischaemia (4) and, together with silver complexes, a potential and safe agent for the topical treatment of skin cancer in humans (5).
Antidiabetic activity of Nimesulide has also been demonstrated (6).
However, recently, a study by Brazilian, Spanish and Argentinean researchers reiterated, this time negatively, the risk/benefit ratio of Nimesulide (7). Frankly, from the consumer's point of view, it is difficult to make a choice since the same doctors give opposite opinions.
Like all drugs it can cause side effects. Always ask the physician.
For more information: Nimesulide studies
Appearance | Yellow powder |
Boiling Point | 442.0±55.0 °C at 760 mmHg |
Melting Point | 140-146°C |
Flash Point | 221.1±31.5°C |
Density | 1.5±0.1 g/cm3 |
Vapour Pressure | 0.0±1.1 mmHg at 25°C |
Index of Refraction | 1.638 |
PSA | 109.60000 |
LogP | 3.79 |
Safety |
Synonyms
References_________________________________________________________________________
(1) Bessone, F., Fay, F., Fay, O., Vorobioff, J., Passamonti, M. E., Godoy, A., & Tanno, H. (1997, October). Nimesulide hepatotoxicity. In Hepatology (Vol. 26, No. 4, pp. 1417-1417). INDEPENDENCE SQUARE WEST CURTIS CENTER, STE 300, PHILADELPHIA, PA 19106-3399: WB SAUNDERS CO.
(2) epar.P.Nimesulide .EMEA-CPMP-1724-04-en-Final.doc (europa.eu)
(3) Venegoni M, Da Cas R, Menniti-Ippolito F, Traversa G. Effects of the European restrictive actions concerning nimesulide prescription: a simulation study on hepatopathies and gastrointestinal bleedings in Italy. Ann Ist Super Sanita. 2010;46(2):153-7. doi: 10.4415/ANN_10_02_08.
(4) Candelario-Jalil E. Nimesulide as a promising neuroprotectant in brain ischemia: new experimental evidences. Pharmacol Res. 2008 Apr;57(4):266-73. doi: 10.1016/j.phrs.2008.03.003.
(5) Candido TZ, de Paiva REF, Figueiredo MC, de Oliveira Coser L, Frajácomo SCL, Abbehausen C, Cardinalli IA, Lustri WR, Carvalho JE, Ruiz ALTG, Corbi PP, Lima CSP. Silver Nimesulide Complex in Bacterial Cellulose Membranes as an Innovative Therapeutic Method for Topical Treatment of Skin Squamous Cell Carcinoma. Pharmaceutics. 2022 Feb 21;14(2):462. doi: 10.3390/pharmaceutics14020462.
(6) Joharapurkar A, Kshirsagar S, Patel V, Patel M, Savsani H, Jain M. In vivo antidiabetic activity of nimesulide due to inhibition of amino acid transport. Basic Clin Pharmacol Toxicol. 2022 Jan;130(1):35-43. doi: 10.1111/bcpt.13670.
(7) Colombato L, Arrese M, Reggiardo MV, Ono SK, Carrilho F, Lucena MI, Andrade RJ. Serious liver injury induced by Nimesulide: an international collaborative study. Arch Toxicol. 2021 Apr;95(4):1475-1487. doi: 10.1007/s00204-021-03000-8.
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"Description" about A-DERMA EPITHELIALEA.H ULTRA 40ml by CarPas (5225 pt) | 2022-May-02 11:38 |
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