setastine

{{Short description|Chemical compound}}

{{Drugbox

| IUPAC_name = 1-[2-[1-(4-chlorophenyl)-1-phenyl-ethoxy]ethyl]azepane

| image = Setastine.png

| image2 = Setastine-3D-balls.png

| tradename =

| pregnancy_category =

| legal_status =

| routes_of_administration =

| bioavailability =

| protein_bound =

| metabolism =

| elimination_half-life =

| excretion =

| index2_label = HCl

| CAS_number2_Ref = {{cascite|correct|CAS}}

| CAS_number2 = 59767-13-4

| UNII2_Ref = {{fdacite|correct|FDA}}

| UNII2 = T2MB6P84ON

| CAS_number = 64294-95-7

| ATC_prefix =

| ATC_suffix =

| PubChem = 43082

| ChemSpiderID = 39258

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = 6G3OCF528J

| C=22 | H=28 | Cl=1 | N=1 | O=1

| smiles = CC(C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCCN3CCCCCC3

}}

Setastine (Loderix) is an antihistamine used to treat allergies and rhinitis.{{cite journal | vauthors = Lantos A, Tóth A, Zsiray M | title = Loderix (setastine) tablets in the treatment of allergic rhinoconjunctivitis | journal = Therapia Hungarica | volume = 39 | issue = 1 | pages = 22–24 | year = 1991 | pmid = 1677500 }}{{cite journal | vauthors = Hirschberg A, Ribári O, Krasznai M | title = Results obtained with Loderix tablet in chronic rhinitis patients | journal = Therapia Hungarica | volume = 37 | issue = 4 | pages = 202–204 | year = 1989 | pmid = 2576575 }}

Pharmacology

= Pharmacodynamics =

Setastine acts as a highly selective H1 receptor antagonist.{{cite journal | vauthors = Porszász J, Varga F, Porszász KG, Szolscányi J, Barthó L, Petöcz L, Kápolnai L | title = Pharmacology of the new H1-receptor antagonist setastine hydrochloride | journal = Arzneimittel-Forschung | volume = 40 | issue = 12 | pages = 1340–1345 | date = December 1990 | pmid = 1982751 }} It has no anticholinergic, antiadrenergic, or antiserotonergic effects.

= Pharmacokinetics =

Setastine penetrates the blood-brain-barrier poorly so it is only mildly sedating compared to related molecules like diphenhydramine.

See also

References