Setastine

Setastine

Systematic (IUPAC) name
1-[2-[1-(4-chlorophenyl)-1-phenyl-ethoxy]ethyl]azepane
Clinical data
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	59767-13-4
ATC code	?
PubChem	CID 43082
ChemSpider	39258
UNII	6G3OCF528J^Y
Chemical data
Formula	C₂₂H₂₈ClNO
Mol. mass	357.92 g/mol
SMILES CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCN3CCCCCC3

Setastine (Loderix) is an antihistamine used to treat allergies and rhinitis.^[1]^[2]

1 Pharmacology
- 1.1 Pharmacodynamics
- 1.2 Pharmacokinetics
2 See also
3 References

Pharmacology [edit]

Pharmacodynamics [edit]

Setastine acts as a highly selective H₁ receptor antagonist.^[3] It has no anticholinergic, antiadrenergic, or antiserotonergic effects.

Pharmacokinetics [edit]

Setastine penetrates the blood-brain-barrier only weakly, hence, it is not sedating or is only mildly so.^[3]

References [edit]

^ Lantos A, Tóth A, Zsiray M (1991). "Loderix (setastine) tablets in the treatment of allergic rhinoconjunctivitis". Therapia Hungarica (English Edition) 39 (1): 22–4. PMID 1677500.
^ Hirschberg A, Ribári O, Krasznai M (1989). "Results obtained with Loderix tablet in chronic rhinitis patients". Therapia Hungarica (English Edition) 37 (4): 202–4. PMID 2576575.
^ ^a ^b Porszász J, Varga F, Porszász KG, et al. (December 1990). "Pharmacology of the new H1-receptor antagonist setastine hydrochloride". Arzneimittel-Forschung 40 (12): 1340–5. PMID 1982751.

Decongestants and other nasal preparations (R01)

Topical

Sympathomimetics, plain	Cyclopentamine Ephedrine Phenylephrine Oxymetazoline Tetryzoline Xylometazoline Naphazoline Tramazoline Metizoline Tuaminoheptane Fenoxazoline Tymazoline Epinephrine

Antiallergic agents, excluding corticosteroids	Spaglumic acid histamine antagonists (Levocabastine Antazoline Thonzylamine) mast cell stabilizer (some are also antihistamines) (Cromoglicic acid Nedocromil Azelastine Olopatadine Lodoxamide)

Corticosteroids	Beclometasone Prednisolone Dexamethasone Flunisolide Budesonide Betamethasone Tixocortol Fluticasone Mometasone furoate Triamcinolone Ciclesonide

Other nasal preparations	Cafaminol Calcium hexamine thiocyanate Retinol Ipratropium bromide Ritiometan Mupirocin Hexamidine Framycetin Hyaluronic acid Eucalyptus oil

Systemic use:
Sympathomimetics

M: RES

anat (n, x, l, c)/phys/devp

noco (c, p)/cong/tumr, sysi/epon, injr

proc, drug (R1/2/3/5/6/7)

Histaminergics

Receptor

H₁	Agonists: 2-Pyridylethylamine Betahistine Histamine HTMT UR-AK49 Antagonists: 1st generation: 4-Methyldiphenhydramine Alimemazine Antazoline Azatadine Bamipine Benzatropine/Benztropine Bepotastine Bromazine Brompheniramine Buclizine Captodiame Carbinoxamine Chlorcyclizine Chloropyramine Chlorothen Chlorphenamine Chlorphenoxamine Cinnarizine Clemastine Clobenzepam Clocinizine Cyclizine Cyproheptadine Dacemazine Deptropine Dexbrompheniramine Dexchlorpheniramine Dimenhydrinate Dimetindene Diphenhydramine Diphenylpyraline Doxylamine Embramine Etodroxizine Etybenzatropine/Ethylbenztropine Etymemazine Flunarizine Histapyrrodine Homochlorcyclizine Hydroxyethylpromethazine Hydroxyzine Isopromethazine Isothipendyl Meclozine Mepyramine/Pyrilamine Mequitazine Methafurylene Methapyrilene Methdilazine Moxastine Niaprazine Orphenadrine Oxatomide Oxomemazine Phenindamine Pheniramine Phenyltoloxamine Pimethixene Piperoxan Pipoxizine Promethazine Propiomazine Pyrrobutamine Talastine Thenalidine Thenyldiamine Thiazinamium Thonzylamine Tolpropamine Tripelennamine Triprolidine 2nd generation: Acrivastine Alinastine Astemizole Azelastine Bamirastine Barmastine Bepiastine Bepotastine Bilastine Cabastinen Carebastine Cetirizine Clemastine Clemizole Clobenztropine Dorastine Ebastine Emedastine Epinastine Flezelastine Ketotifen Latrepirdine Levocabastine Linetastine Loratadine Mapinastine Mebhydrolin Mizolastine Moxastine Noberastine Octastine Olopatadine Perastine Piclopastine Rocastine Rupatadine Setastine Talastine Temelastine Terfenadine Zepastine 3rd generation: Desloratadine Fexofenadine Levocetirizine Ungrouped: Belarizine Efletirizine Elbanizine Flotrenizine Medrylamine Napactadine Pibaxizine Tagorizine Trelnarizine Trenizine Vapitadine Miscellaneous: Tricyclic antidepressants (amitriptyline, doxepin, trimipramine, etc) Tetracyclic antidepressants (mianserin, mirtazapine, etc) Typical antipsychotics (chlorpromazine, thioridazine, etc) Atypical antipsychotics (clozapine, olanzapine, quetiapine, etc)

H₂	Agonists: Amthamine Betazole Dimaprit Histamine HTMT Impromidine UR-AK49 Antagonists: Bisfentidine Burimamide Cimetidine Dalcotidine Donetidine Ebrotidine Etintidine Famotidine Lafutidine Lamtidine Lavoltidine/Loxtidine Lupitidine Metiamide Mifentidine Niperotidine Nizatidine Osutidine Oxmetidine Pibutidine Quisultazine/Quisultidine Ramixotidine Ranitidine Roxatidine Sufotidine Tiotidine Tuvatidine Venritidine Xaltidine

H₃	Agonists: α-Methylhistamine Cipralisant Histamine Imetit Immepip Immethridine Methimepip Proxyfan Antagonists: A-349,821 A-423,579 ABT-239 Betahistine Burimamide Ciproxifan Clobenpropit Conessine GSK-189,254 Impentamine Iodophenpropit JNJ-5,207,852 MK-0249 NNC-38-1,049 PF-03654746 Pitolisant SCH-79,687 Thioperamide VUF-5,681

H₄	Agonists: 4-Methylhistamine Histamine VUF-8,430 Antagonists: JNJ-7,777,120 Thioperamide VUF-6,002

Transporter

VMAT	Inhibitors: Ibogaine Reserpine Tetrabenazine

Enzyme

HDC	Inhibitors: Catechin Meciadanol Naringenin Tritoqualine

DAO	Inhibitors: Aminoguanidine

Others

Endogenous	Histamine; Precursors: L-Histidine; Cofactors: Vitamin B6

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Contents

Pharmacology [edit]

Pharmacodynamics [edit]

Pharmacokinetics [edit]

See also [edit]

References [edit]