Setastine

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Setastine
Systematic (IUPAC) name
File:Setastine.png
1-[2-[1-(4-chlorophenyl)-1-phenyl-ethoxy]ethyl]azepane
Identifiers
CAS Number	59767-13-4
PubChem	CID 43082
ChemSpider	39258
Chemical data
Formula	C₂₂H₂₈ClNO
Molar mass	357.92 g/mol
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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

Pharmacodynamics

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

Pharmacokinetics

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

References

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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

Phenylpropanolamine • Pseudoephedrine • Phenylephrine • Phenylpropylamine

M: RES

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

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

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

Histaminergics

Receptor
ligands

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 • Chlorpheniramine • Chlorphenoxamine • Cinnarizine • Clemastine • Clobenzepam • Clocinizine • Cyclizine • Cyproheptadine • Dacemazine • Deptropine • Dexbrompheniramine • Dexchlorpheniramine • Dimenhydrinate • Dimetindene • Diphenhydramine • Diphenylpyraline • Doxylamine • Embramine • Etybenzatropine (Ethylbenztropine) • Etymemazine • Histapyrrodine • Homochlorcyclizine • Hydroxyethylpromethazine • Hydroxyzine • Isopromethazine • Isothipendyl • Meclozine • Mepyramine (Pyrilamine) • Mequitazine • Methafurylene • Methapyrilene • Methdilazine • Moxastine • Niaprazine • Orphenadrine • Oxatomide • Oxomemazine • Phenindamine • Pheniramine • Phenyltoloxamine • Pimethixene • Piperoxan • Promethazine • Propiomazine • Pyrrobutamine • Talastine • Thenalidine • Thenyldiamine • Thiazinamium • Thonzylamine • Tolpropamine • Tripelennamine • Triprolidine; 2nd generation: Acrivastine • Astemizole • Azelastine • Cetirizine • Clemizole • Clobenztropine • Ebastine • Emedastine • Epinastine • Ketotifen • Latrepirdine • Levocabastine • Loratadine • Mebhydrolin • Mizolastine • Olopatadine • Rupatadine • Setastine • Terfenadine; 3rd generation: Desloratadine • Fexofenadine • Levocetirizine; Miscellaneous: Tricyclic Antidepressants (Amitriptyline, Doxepin, Trimipramine, etc) • Tetracyclic Antidepressants (Mianserin, Mirtazapine, etc) • Serotonin Antagonists and Reuptake Inhibitors (Trazodone, Nefazodone) • 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 • Quisultidine/Quisultazine • Ramixotidine • Ranitidine • Roxatidine • Sufotidine • Tiotidine • Tuvatidine • Venritidine • Zaltidine
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 • SCH-79,687 • Thioperamide • Tiprolisant • VUF-5,681
H₄	Agonists: 4-Methylhistamine • Histamine • VUF-8,430 Antagonists: JNJ-7,777,120 • Thioperamide • VUF-6,002

Reuptake
inhibitors

Vesicular

VMAT inhibitors	Ibogaine • Reserpine • Tetrabenazine

Enzyme
inhibitors

Anabolism

HDC inhibitors	α-FMH • Brocresine • Catechin • Cyanidanol-3 • McN-A-1293 • ME • Meciadanol • Naringenin • Thiazol-4-yimethoxyamine • Tritoqualine • Zy-15,029

Catabolism

HNMT inhibitors	Amodiaquine • BW-301U • Diphenhydramine • Harmaline • Metoprine • Quinacrine • SKF-91,488 • Tacrine
DAO inhibitors	1,4-Diamino-2-butyne • Aminoguanidine

Others

Precursors	L-Histidine
Cofactors	Vitamin B6 (pyridoxine, pyridoxamine, pyridoxal → Pyridoxal phosphate)

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↑ 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.
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Setastine

Contents

Pharmacology

Pharmacodynamics

Pharmacokinetics

See also

References

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