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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/07/12 15:32:19」(JST)
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Acrivastine
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| Clinical data |
| AHFS/Drugs.com |
International Drug Names |
| MedlinePlus |
a682619 |
Pregnancy
category |
- US: B (No risk in non-human studies)
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Routes of
administration |
oral |
| ATC code |
|
| Legal status |
| Legal status |
- UK: General sales list (GSL, OTC)
- US: ℞-only
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| Pharmacokinetic data |
| Biological half-life |
1.5 hours |
| Excretion |
Renal |
| Identifiers |
IUPAC name
- (E)-3-{6-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-yl-
prop-1-enyl]pyridin-2-yl}prop-2-enoic acid
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| CAS Number |
|
| PubChem CID |
|
| ChemSpider |
|
| UNII |
|
| KEGG |
|
| ChEBI |
|
| ChEMBL |
|
| ECHA InfoCard |
100.110.306 |
| Chemical and physical data |
| Formula |
C22H24N2O2 |
| Molar mass |
348.438 g/mol |
| 3D model (Jmol) |
|
SMILES
-
O=C(O)\C=C\c3nc(\C(=C\CN1CCCC1)c2ccc(cc2)C)ccc3
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InChI
-
InChI=1S/C22H24N2O2/c1-17-7-9-18(10-8-17)20(13-16-24-14-2-3-15-24)21-6-4-5-19(23-21)11-12-22(25)26/h4-13H,2-3,14-16H2,1H3,(H,25,26)/b12-11+,20-13+ Y
-
Key:PWACSDKDOHSSQD-IUTFFREVSA-N Y
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| NY (what is this?) (verify) |
Acrivastine is a medication used for the treatment of allergies and hay fever. It is a second-generation H1-receptor antagonist antihistamine (like its base molecule triprolidine) and works by blocking histamine H1 receptors.
This non-sedating[verification needed] antihistamine is sold under the brand name Benadryl Allergy Relief in the United Kingdom by McNeil Laboratories. It should not be confused with Benadryl Once a Day which has cetirizine as the active ingredient and is also sold by McNeil in the UK. It is available as an over-the-counter medicine in the UK, and is available with or without pseudoephedrine under the Benadryl brand.
In the U.S., acrivastine is the active ingredient in the Semprex brand. Semprex-D also contains the decongestant pseudoephedrine. Semprex-D is marketed in the U.S. by Actient Pharmaceuticals.[1]
Comparisons with other popular antihistamines
Unlike cetirizine or loratadine, for which the standard dose is one tablet per day, a single acrivastine tablet may be taken up to three times a day.[2] It is not to be taken by over 65s, pregnant women, or people with compromised liver or kidney function.
References
- ^ SEMPREX-D - acrivastine and pseudoephedrine hydrochloride capsule U.S. National Library of Medicine, National Institutes of Health, May 2008
- ^ "Benadryl Allergy Relief". electronic Medicines Compendium (eMC). 2014. Retrieved 4 July 2014.
|
Antihistamines (R06)
|
| Aminoalkyl ethers |
- Bromazine (bromodiphenhydramine)
- Carbinoxamine
- Clemastine
- Chlorphenoxamine
- Diphenylpyraline
- Diphenhydramine
- Doxylamine
- Orphenadrine
- Phenyltoloxamine
|
| Substituted alkylamines |
- Brompheniramine
- Chlorphenamine
- Dexbrompheniramine (+pseudoephedrine)
- Dexchlorpheniramine (+betamethasone)
- Dimetindene
- Pheniramine
- Talastine
|
| Substituted ethylenediamines |
- Chloropyramine
- Histapyrrodine
- Mepyramine
- Methapyrilene
- Tripelennamine (pyribenzamine)
|
| Phenothiazine derivatives |
- Alimemazine
- Fenethazine
- Hydroxyethylpromethazine
- Isothipendyl
- Mequitazine
- Methdilazine
- Oxomemazine
- Promethazine
|
| Piperazine derivatives |
- Buclizine
- Cetirizine
- Chlorcyclizine
- Cinnarizine
- Cyclizine
- Hydroxyzine
- Meclizine
- Oxatomide
|
| Others for systemic use |
- Antazoline
- Azanator
- Azatadine
- Bamipine
- Cyproheptadine
- Deptropine
- Ebastine
- Emedastine
- Epinastine
- Ketotifen
- Latrepirdine
- Mebhydrolin
- Mizolastine
- Olopatadine
- Phenindamine
- Pimethixene
- Pyrrobutamine
- Quifenadine
- Rupatadine
- Triprolidine
- selective (Acrivastine
- Astemizole
- Azelastine
- Bilastine
- Desloratadine
- Fexofenadine
- Loratadine
- Terfenadine)
|
| For topical use |
- Bamipine
- Chloropyramine
- Chlorphenoxamine
- Clemastine
- Dimetindene
- Diphenhydramine
- Isothipendyl
- Mepyramine
- Promethazine
- Thenalidine
|
|
Histamine receptor modulators
|
| H1 |
- Agonists: 2-Pyridylethylamine
- Betahistine
- Histamine
- HTMT
- L-Histidine
- UR-AK49
- Antagonists: First-generation: 4-Methyldiphenhydramine
- Alimemazine
- Antazoline
- Azatadine
- Bamipine
- Benzatropine (benztropine)
- Bepotastine
- Bromazine
- Brompheniramine
- Buclizine
- Captodiame
- Carbinoxamine
- Chlorcyclizine
- Chloropyramine
- Chlorothen
- Chlorphenamine
- Chlorphenoxamine
- Cinnarizine
- Clemastine
- Clobenzepam
- Clocinizine
- Cloperastine
- Cyclizine
- Cyproheptadine
- Dacemazine
- Decloxizine
- Deptropine
- Dexbrompheniramine
- Dexchlorpheniramine
- Dimenhydrinate
- Dimetindene
- Diphenhydramine
- Diphenylpyraline
- Doxylamine
- Embramine
- Etodroxizine
- Etybenzatropine (ethylbenztropine)
- Etymemazine
- Fenethazine
- Flunarizine
- Histapyrrodine
- Homochlorcyclizine
- Hydroxyethylpromethazine
- Hydroxyzine
- Isopromethazine
- Isothipendyl
- Meclozine
- Medrylamine
- Mepyramine (pyrilamine)
- Mequitazine
- Methafurylene
- Methapyrilene
- Methdilazine
- Moxastine
- Orphenadrine
- Oxatomide
- Oxomemazine
- Phenindamine
- Pheniramine
- Phenyltoloxamine
- Pimethixene
- Piperoxan
- Pipoxizine
- Promethazine
- Propiomazine
- Pyrrobutamine
- Talastine
- Thenalidine
- Thenyldiamine
- Thiazinamium
- Thonzylamine
- Tolpropamine
- Tripelennamine
- Triprolidine
- Second/third-generation: Acrivastine
- Alinastine
- Astemizole
- Azelastine
- Bamirastine
- Barmastine
- Bepiastine
- Bepotastine
- Bilastine
- Cabastinen
- Carebastine
- Cetirizine
- Clemastine
- Clemizole
- Clobenztropine
- Desloratadine
- Dorastine
- Ebastine
- Efletirizine
- Emedastine
- Epinastine
- Fexofenadine
- Flezelastine
- Ketotifen
- Latrepirdine
- Levocabastine
- Levocetirizine
- Linetastine
- Loratadine
- Mapinastine
- Mebhydrolin
- Mizolastine
- Moxastine
- Noberastine
- Octastine
- Olopatadine
- Perastine
- Pibaxizine
- Piclopastine
- Quifenadine (phencarol)
- Rocastine
- Rupatadine
- Setastine
- Sequifenadine (bicarphen)
- Talastine
- Temelastine
- Terfenadine
- Vapitadine
- Zepastine
- Non-generational: Atypical antipsychotics (e.g., aripiprazole, asenapine, brexpiprazole, clozapine, iloperidone, olanzapine, paliperidone, quetiapine, risperidone, RP-5063, ziprasidone, zotepine)
- Tetracyclic antidepressants (e.g., amoxapine, loxapine, maprotiline, mianserin, mirtazapine, oxaprotiline)
- Tricyclic antidepressants (e.g., amitriptyline, butriptyline, clomipramine, desipramine, dosulepin (dothiepin), doxepin, imipramine, iprindole, lofepramine, nortriptyline, protriptyline, trimipramine)
- Typical antipsychotics (e.g., chlorpromazine, flupenthixol, fluphenazine, loxapine, perphenazine, prochlorperazine, thioridazine, thiothixene)
- Unknown/unsorted: Belarizine
- Elbanizine
- Flotrenizine
- Napactadine
- Tagorizine
- Trelnarizine
- Trenizine
|
| H2 |
- Agonists: Amthamine
- Betazole
- Dimaprit
- Histamine
- HTMT
- Impromidine
- L-Histidine
- UR-AK49
- Antagonists: Bisfentidine
- Burimamide
- Cimetidine
- Dalcotidine
- Donetidine
- Ebrotidine
- Etintidine
- Famotidine
- Isolamtidine
- Lafutidine
- Lamtidine
- Lavoltidine (loxtidine)
- Lupitidine
- Metiamide
- Mifentidine
- Niperotidine
- Nizatidine
- Osutidine
- Oxmetidine
- Pibutidine
- Quisultazine (quisultidine)
- Ramixotidine
- Ranitidine
- Roxatidine
- Sufotidine
- Tiotidine
- Tuvatidine
- Venritidine
- Xaltidine
- Zolantidine
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| H3 |
- Agonists: α-Methylhistamine
- Cipralisant
- Histamine
- Imetit
- Immepip
- Immethridine
- L-Histidine
- Methimepip
- Proxyfan
- Antagonists: A-349,821
- A-423,579
- ABT-239
- ABT-652
- AZD5213
- Betahistine
- Burimamide
- Ciproxifan
- Clobenpropit
- Conessine
- Enerisant
- GSK-189,254
- Impentamine
- Iodophenpropit
- Irdabisant
- JNJ-5207852
- MK-0249
- NNC 38-1049
- PF-03654746
- Pitolisant
- SCH-79687
- Thioperamide
- VUF-5681
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| H4 |
- Agonists: 4-Methylhistamine
- α-Methylhistamine
- Histamine
- L-Histidine
- OUP-16
- VUF-8430
- Antagonists: JNJ-7777120
- Mianserin
- Thioperamide
- Toreforant
- VUF-6002
|
|
See also: Receptor/signaling modulators • Monoamine metabolism modulators • Monoamine reuptake and release modulators
|
English Journal
- Development and validation of a rapid stability indicating HPLC-method using monolithic stationary phase and two spectrophotometric methods for determination of antihistaminic acrivastine in capsules.
- Gouda AA1, Hashem H2, Jira T3.
- Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy.Spectrochim Acta A Mol Biomol Spectrosc.2014 Sep 15;130:480-7. doi: 10.1016/j.saa.2014.04.015. Epub 2014 Apr 18.
- Simple, rapid and accurate high performance liquid chromatographic (HPLC) and spectrophotometric methods are described for determination of antihistaminic acrivastine in capsules. The first method (method A) is based on accurate, sensitive and stability indicating chromatographic separation method.
- PMID 24813276
- Computer-aided design, synthesis, and biological evaluation of 5- substituted aminomethylenepyrimidine-2,4,6-triones as H₁ antihistaminic agents (Part2).
- Elbayaa RY1.
- Medicinal chemistry (Shāriqah (United Arab Emirates)).Med Chem.2014;10(1):66-73.
- As a part of a research project pertaining to the synthesis of novel candidates as nonsedating, nonclassic H₁ histaminergic (H₁) blockers with low toxicity profiles, some new 5-substituted aminomethylenepyrimidine-2,4,6-triones were designed based on the H₁ histaminic receptor pharmacophore mo
- PMID 24016395
- Development and Validation of a Liquid Chromatography-tandem Mass Spectrometry Method for the Simultaneous Determination of Acrivastine and Pseudoephedrine in Human Plasma and its Application in Pharmacokinetics.
- He JC1, Feng EF, Liu M, Li HL, Tian M, Zhang Q, Dong LC, Xu GL.
- Arzneimittel-Forschung.Arzneimittelforschung.2012 Oct;62(10):e3. doi: 10.1055/s-0032-1329594. Epub 2012 Oct 9.
- PMID 23047471
Japanese Journal
- Effects of acrivastine, loratadine and cetirizine on histamine-induced wheal and flare responses
- A phase II study of vinblastine in combination with acrivastine in patients with advanced renal cell carcinoma.
- Terfenadine alter action potentials in isolated canine purkinje fibers more than acrivastine
Related Links
- Synopsis Acrivastine is a short acting histamine H 1-receptor antagonist with a rapid onset of action. Double-blind clinical trials have shown acrivastine (usually 8mg three times daily) to be an effective and well tolerated antihistamine ...
- Introduction Acrivastine is a second generation antihistamine that is used for the treatment of allergic rhinitis. Acrivastine has not been linked to instances of clinically apparent acute liver injury. Background ...
Related Pictures
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