| 词条 | Ebastine |
| 释义 |
| verifiedrevid = 439227374 | IUPAC_name = 4-(4-benzhydryloxy-1-piperidyl)-1-(4-tert-butylphenyl)butan-1-one | image = Ebastine.svg | tradename = | Drugs.com = {{drugs.com|international|ebastine}} | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = Oral | bioavailability = | protein_bound = Greater than 95% | metabolism = Hepatic (CYP3A4-mediated), to carebastine | elimination_half-life = 15 to 19 hours (carebastine) | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 90729-43-4 | ATC_prefix = R06 | ATC_suffix = AX22 | PubChem = 3191 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 3079 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = TQD7Q784P1 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 305660 | C=32 | H=39 | N=1 | O=2 | molecular_weight = 469.658 g/mol | smiles = O=C(c1ccc(cc1)C(C)(C)C)CCCN4CCC(OC(c2ccccc2)c3ccccc3)CC4 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C32H39NO2/c1-32(2,3)28-18-16-25(17-19-28)30(34)15-10-22-33-23-20-29(21-24-33)35-31(26-11-6-4-7-12-26)27-13-8-5-9-14-27/h4-9,11-14,16-19,29,31H,10,15,20-24H2,1-3H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = MJJALKDDGIKVBE-UHFFFAOYSA-N }} Ebastine is a H1 antihistamine with low potential for causing drowsiness. It does not penetrate the blood–brain barrier to a significant amount and thus combines an effective block of the H1 receptor in peripheral tissue with a low incidence of central side effects, i.e. seldom causing sedation or drowsiness.[1][2][3] It was patented in 1983 and came into medical use in 1990.[1] The substance is often provided in micronised form due to poor water solubility. UsesEbastine is a second-generation H1 receptor antagonist that is indicated mainly for allergic rhinitis and chronic idiopathic urticaria.[5] It is available in 10 and 20 mg tablets[6] and as fast-dissolving tablets,[7] as well as in pediatric syrup. It has a recommended flexible daily dose of 10 or 20 mg, depending on disease severity. Data from over 8,000 patients in more than 40 clinical trials{{failed verification|date=March 2014}} and studies[3][5][6][11][12] suggest efficacy of ebastine in the treatment of intermittent allergic rhinitis, persistent allergic rhinitis and other indications. SafetyEbastine has shown overall safety and tolerability profile with no cognitive/psychomotor impairment[6] and no sedation[6] worse than placebo,[2] and cardiac safety, that is, no QT prolongation.[6] The incidence of most commonly reported adverse events was comparable between the ebastine and placebo groups, which confirms that ebastine has a favourable safety profile. While experiments in pregnant animals showed no risk for the unborn, no such data are available in humans. It is not known whether ebastine passes into the breast milk. Pharmacokinetic profileAfter oral administration, ebastine undergoes extensive first-pass metabolism by hepatic cytochrome P450 3A4 into its active carboxylic acid metabolite, carebastine. This conversion is practically complete. {{clear left}}Brand namesEbasten - ACI Pharmaceuticals, Bangladesh .[2] Ebamont (ebastine+montelukast), mankind pharma India Atmos - Scotmann Pharmaceuticals, Pakistan . Ebastine is available in different formulations (tablets, fast dissolving tablets and syrup) and commercialized under different brand names around the world, Ebatrol, Atmos, Ebet, Ebastel FLAS, Kestine, KestineLIO, KestinLYO, EstivanLYO, Evastel Z, Ebasten (ACI), etc. References1. ^{{cite book |last1=Fischer |first1=Jnos |last2=Ganellin |first2=C. Robin |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=549 |url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA549 |language=en}} [2][3][4][5][6][7][8]2. ^1 2 {{cite journal|last=Bousquet |first=J |last2=Gaudaño |first2=EM |last3=Palama Carlos |first3=AG |title=A 12-week, placebo-controlled study of the efficacy and safety of ebastine, 10 and 20 mg once daily, in the treatment of perennial allergic rhinitis |journal=Allergy |year=1999 |volume=54 |issue=6 |pages=562–568 |pmid=10435469 |doi=10.1034/j.1398-9995.1999.00984.x}} 3. ^1 {{cite journal|last=Tagawa |first=M |last2=Kano |first2=M |last3=Okamura |first3=N |title=Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-clorphrniramine, a classical antihistamine |journal=Br J Clin Pharmacol |year=2001 |volume=52 |issue=5 |pages=501–509 |pmc=2014616 |pmid=11736858 |doi=10.1046/j.1365-2125.2001.01471.x}} {{open access}} 4. ^1 2 {{cite journal|last=Van Cauwenberge |first=P |last2=de Belder |first2=T |last3=Sys |first3=L |title=A review of the second-generation antihistamine ebastine for the treatment of allergic disorders |journal=Exp Rew Pharmacother |year=2004 |volume=5 |issue=8 |pages=1807–13 |pmid=15264995 |doi=10.1517/14656566.5.8.1807}} 5. ^1 {{cite journal|last=Ratner |first=P |last2=Falqués |first2=M |last3=Chuecos |first3=F |title=Meta-analysis of the efficacy of ebastine 20 mg compared to loratadine 10 mg and placebo in the symptomatic treatment of seasonal allergic rhinitis |journal=Int Arch Allergy Immunol |year=2005 |volume=138 |issue=4 |pages=312–8 |pmid=16224195 |doi=10.1159/000088869}} 6. ^1 {{cite journal|last=Antonijoan |first=RM |last2=García-Gea |first2=C |last3=Puntes |first3=M |title=A comparison of ebastine 10 mg fast-dissolving tablet with oral desloratadine and placebo in inhibiting the cutaneous reaction to histamine in healthy adults |journal=Clin Drug Invest |year=2007 |volume=27 |issue=7 |pages=453–61 |pmid=17563125 |doi=10.2165/00044011-200727070-00002}} 7. ^1 {{cite journal|last=Antonijoan |first=R |last2=García-Gea |first2=C |last3=Puntes |first3=M |title=Comparison of inhibition of cutaneous histamine reaction of ebastine fast-dissolving tablet (20 mg) versus desloratadine capsules (5 mg): a randomized, double-blind, double-dummy, placebo-controlled, three period crossover study in healthy, nonatopic adults |journal=Clin Ther |year=2007 |volume=29 |issue=5 |pages=814–22 |pmid=17697901 |doi=10.1016/j.clinthera.2007.05.001}} 8. ^1 2 3 4 5 {{cite journal|last=Sastre |first=J |title=Ebastine in allergic rhinitis and chronic idiopathic urticaria |journal=Allergy |year=2008 |volume=63 |issue=Suppl 89 |pages=1–20 |doi=10.1111/j.1398-9995.2008.01897.x |pmid=19032340}} 9. ^1 2 3 {{cite book|title=Arzneistoff-Profile|editor1=Dinnendahl, V |editor2=Fricke, U |publisher=Govi Pharmazeutischer Verlag|location=Eschborn, Germany|year=2010|edition=23|volume=4|isbn=978-3-7741-98-46-3|language=German}} [9]}} Aims Pharmaceuticals,Pakistan External links
5 : H1 receptor antagonists|Ethers|Piperidines|Aromatic ketones|Peripherally selective drugs |
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