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Ebastina
Pro:
Antiallergico (1) Antistaminico (1)Contro:
Assumere solo sotto controllo medico (1)10 pt da CarPas
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"Descrizione" su Ebastina Consenso relazione 10 di CarPas (5225 pt) | 11-set-2023 10:12 |
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Ebastina è un composto chimico formato da 1-(4-(tert-butyl)phenyl)-4-(4-hydroxypiperidin-1-yl)butan-1-one (5.1.9) in un procedimento chimico preliminare piuttosto complesso, che si svolge in diverse fasi e che coinvolge sodio bicarbonato, methyl isobutyl ketone e ioduro di potassio. Successivamente, per ottenere il prodotto finito, sono utilizzati bromuro di benzidrile e carbonato di sodio.
Si presenta in forma di polvere bianca, insolubile in acqua., solubile in diclorometano, leggermente solubile in metanolo, altamente permeabile nella membrana lipidica.
A cosa serve e dove si usa
Assumere solo sotto controllo medico
Medicina
Ebastina è un membro della classe di farmaci chiamati inibitori selettivi non sedativi del recettore H1 dell'istamina. La sua azione coinvolge bronchi, capillari sanguigni ed alcuni muscoli lisci, antagonista del recettore con struttura a base di ossipiperidina, la cui forma attiva è il metabolita carebastina.
L'istamina è un importante mediatore dei sintomi dell'allergia che agisce generalmente tramite il recettore H1, viene rilasciata durante la fase iniziale della risposta immunitaria e il trattamento di scelta per le patologie allergiche sono gli antistaminici H1 che tendono a stabilizzare il recettore H1 nella sua forma inattiva. Gli antistaminici H1, che stabilizzano il recettore nella sua forma inattiva, sono riconosciuti come trattamento primario nelle linee guida internazionali per cura dell'orticaria e della rinite allergica.
Tra gli antistaminici di seconda generazione tipo H1, Ebastina è stato commercializzato in tutto il mondo dal 1990 per il trattamento dell'orticaria e della rinite allergica, non ha attività sedante, possiede una lunga durata di azione. E' anche efficace contro la cinetosi. La forma di dosaggio è generalmente la compressa solida nella quale possono essere presenti aromi per migliorarne il gusto e "superdisintegranti", ad esempio il Povidone, per favorirne lo scioglimento ed aumentare l'assorbimento dell'acqua.
L'ebastina, in uno studio in vitro nelle cellule del polipo nasale, ha inibito il rilascio di leucotrieni C4/D4 e prostaglandina D2 indotto da anti-IgE (P<.05). Inoltre, ha inibito fattore di necrosi tumorale-α e interleuchina 8 causato dal rilascio di fattore stimolante le colonie di granulociti-macrofagi (1). Tra i vari antistaminici presenti sul mercato è anche da notare come l'ebastina abbia mostrato effetti superiori alla carebastina.
Un recente studio di ricercatori di Centri universitari di Huston, New York e Chicago, USA, partendo dall'esame delle proteine del gruppo Polycomb, dalla cromatina e dal soppressore trascrizionale metilandolo H3, ha scoperto che un trattamento con ebastina ha ridotto efficacemente la progressione e la crescita del carcinoma mammario e ne ha migliorato la sopravvivenza libera da progressione. Quindi, da questi risultati, l'ebastina potrebbe rivelarsi una terapia promettente per i tumori con mutazioni EZH o portatori di sovraespressione (2).
Per riassumere, l'ebastina può essere utile in:
Come tutti i farmaci può causare effetti collaterali. Consultare sempre il medico.
Per questo composto chimico sono stati selezionati gli studi più rilevanti con una sintesi dei loro contenuti:
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 |
Prezzo
10 mg $236.00
50 mg $938.00
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Sinonimi
Bibliografia______________________________________________________________________
(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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"Ebastina studi" su Ebastina Consenso relazione 10 di CarPas (5225 pt) | 09-set-2022 11:49 |
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Compendio degli studi più significativi con riferimento a proprietà, assunzione, effetti.
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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Tipologia:   Chemical Principali sostanze contenute:   Ultimo aggiornamento:   2022-09-09 10:35:12 | Rischio chimico:   |