Hyoscyamine(BAN)

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Hyoscyamine(BAN) 1736 Gastrointestinal Drugs Espasmogress; Hiosinotil Compuesto†; Hiosultrina-F; Infafren Compuesto; ed by light. Soluble 1 in 0.5 of water and 1 in 5 of alcohol; prac- Ipomoea Resin Neo-Pasmonal; Ortran†; Pasmodil; Pirobutil; Precicol; Prestodol Compues- tically insoluble in ether. pH of a 1% solution in water is about Ipomoea, resina de; Mexican Scammony Resin; Scammony Resin. to; Retodol Compositum; Selpiran; Selpiran Compuesto; Serralpina Com- 5.3. puesta; Viladol Plus; Philipp.: Buscopan Plus; Pol.: Scopolan Compositum; CAS — 9000-34-4. Vegantalgin H; Port.: Buscopan Compositum N; S.Afr.: Buscopan Com- positum; Donnatal; Millerspas; Respinol; Respinol Compound; Scopex Co; Adverse Effects, Treatment, and Precau- Profile Virobis†; Spain: Buscapina Compositum; Midriati; Nolotil Compositum†; Ipomoea is the dried root of Ipomoea orizabensis (Convolvu- Oragalin Espasmolitico; Psico Blocan; Swed.: Spasmofen; Switz.: Nardyl; tions laceae). Ipomoea resin is a mixture of glycosidal resins obtained Thai.: Amcopan Plus; Buscopan Plus; Donnatal†; Pacopan; Spasgone; Uni- As for Atropine Sulfate, p.1219. gan; Turk.: Buscopan Compositum; Molit Plus; Skopolin; Spazmol Plus; from ipomoea and it has a drastic purgative and irritant action. It Tanko-Buskas; Tranko-Buskas; UK: Feminax; USA: Accuhist LA†; AeroHist has been superseded by less toxic laxatives. Plus; AeroKid; AH-chew; Alkabel; AllePak; AlleRx; Antispasmodic Elixir; Bar- Interactions bidonna†; Bellahist-D; Bellatal; Chlor-Mes; Chlor-Mes D; CPM PSE MSC; CPM/PE/MSC; DA Chewable; DA II; Dallergy; Dehistine; Dexphen M; Don- As for antimuscarinics in general (see Atropine Sul- natal; DriHist; Dura-Vent/DA; Durahist; Durahist D; Ex-Histine; Extendryl; fate, p.1220). Extendryl DM; Extendryl PEM; Hista-Vent DA; Histatab D; Histor-D Time- Irsogladine Maleate (rINNM) celles; Hyosophen; Mescolor†; Murocoll-2; Nacon; NoHist Plus; Norel DM; Irsogladine, Maléate d’; Irsogladini Maleas; Maleato de irsogladina; Omnihist LA; Pamine FQ Kit; Pannaz; PCM; Prehist D; PSE MSC; Ralix; Re- Uses and Administration dur-PCM; Relcof PSE; Rescon-MX; Ryneze; Stahist; Susano; Xiral†; Venez.: MN-1695. 2,4-Diamino-6-(2,5-dichlorophenyl)-S-triazine maleate. Brugesina; Buscapina Compositum; Buscapina Plus; Butilamina Compuesta; Hyoscyamine is a tertiary amine antimuscarinic with Ирсогладина Малеат Diezol Compuesto†; Fenopol†; Hioscinol Compuesto†; Sarifan Compues- the actions of atropine (which is racemic hyoscyamine, C H Cl N .C H O = 372.2. to†; Vuscobras. 9 7 2 5 4 4 4 see p.1219); hyoscyamine, the laevo-isomer, has about CAS — 57381-26-7 (irsogladine); 84504-69-8 (irsogla- twice the potency of atropine since the dextro-isomer dine maleate). has only very weak antimuscarinic activity. Hyo- (BAN) Hyoscyamine scyamine is used mainly in the relief of conditions as- Cl Hiosciamina; Hyoscyamin; (−)-Hyoscyamine; l-Hyoscyamine; Hy- sociated with visceral spasm. It has also been given for oscyaminum; Hyoskyamiini. (−)-(1R,3r,5S)-Tropan-3-yl (S)-tro- rhinitis and was formerly used in the treatment of par- N NH2 pate. kinsonism. Cl Гиосциамин Hyoscyamine is given in usual doses of 150 to N N C17H23NO3 = 289.4. 300 micrograms up to four times daily by mouth, but it CAS — 101-31-5. is more usually employed as the sulfate; the hydrobro- NH ATC — A03BA03. mide is also used. Suggested doses of hyoscyamine 2 ATC Vet — QA03BA03. sulfate are 125 to 250 micrograms orally or sublingual- (irsogladine) ly every four hours as needed, up to a maximum of 1.5 mg in 24 hours. Modified-release oral preparations Profile CH 3 of hyoscyamine sulfate are available in some coun- Irsogladine maleate is a cytoprotective drug that is used in the tries; dosage is specific to a particular formulation. Hy- treatment of peptic ulcer disease (p.1702) in a usual oral dose of N 4 mg daily. It has also been investigated for mucositis and mouth oscyamine sulfate has also been given by injection. ulceration. OH Preparations Mucositis. Irsogladine maleate 2 mg twice daily by mouth has 1 USP 31: Hyoscyamine Sulfate Elixir; Hyoscyamine Sulfate Injection; Hyo- been reported to reduce the incidence of aphthous stomatitis in O scyamine Sulfate Oral Solution; Hyoscyamine Sulfate Tablets; Hyoscyamine a small study in patients being treated with methotrexate for Ta bl e t s . rheumatoid arthritis. Proprietary Preparations (details are given in Part 3) 1. Yoshida T, Hirakata M. Therapeutic benefits of irsogladine O Canad.: Levsin†; Denm.: Egazil; Fin.: Egazil†; Fr.: Duboisine†; Hong maleate on aphthous stomatitis induced by methotrexate in rheu- Kong: Levsin; Norw.: Egazil; Swed.: Egazil; USA: A-Spas†; Anaspaz; Cyst- matoid arthritis. J Rheumatol 2003; 30: 2082–3. ospaz; Donnamar; ED-SPAZ; Gastrosed; IB-Stat; Levbid; Levsin; Levsinex; Preparations Description. Hyoscyamine is an alkaloid obtained from vari- Mar-Spas; Neosol; NuLev; Symax. ous solanaceous plants. It is the laevo-isomer of atropine into Multi-ingredient: Austral.: Donnagel; Donnalix; Donnatab; Braz.: Anal- Proprietary Preparations (details are given in Part 3) which it can be converted by heating or by the action of alkali. verin†; Neogrein; Ormigrein; Tropinal; Cz.: Solutan†; Indon.: Aludonna; Jpn: Gaslon N. Feminax; Ital.: Antispasmina Colica; S.Afr.: Donnatal; Millerspas; Switz.: Pharmacopoeias. In US. Nardyl; Thai.: Donnatal†; USA: Accuhist LA†; Alkabel; Antispasmodic Elix- USP 31 (Hyoscyamine). A white crystalline powder. M.p. 106° ir; Atrosept; Barbidonna†; Bellacane; Bellahist-D; Bellatal; Dolsed†; Donna- tal; Hyosophen; MHP-A; MSP-Blu; Phenazopyridine Plus; Prosed/DS; Pyrid- Isopropamide Iodide (BAN, rINN) to 109°. Slightly soluble in water and in benzene; freely soluble ium Plus; Stahist; Susano; Trac Tabs 2X†; Trellium Plus; UAA; Urelief Plus; in alcohol, in chloroform, and in dilute acids; sparingly soluble in Urelle; Uretron; Uridon Modified†; Urimar-T; Urimax; Urised; Uriseptic; Ioduro de isopropamida; Isopropamide, Iodure d’; Isopropamidi ether. Its solutions are alkaline to litmus. Store in airtight contain- UriSym†; Uritact; Uro Blue; Urogesic Blue; Utira. Iodidum. (3-Carbamoyl-3,3-diphenylpropyl)di-isopropylmethyl- ers. Protect from light. ammonium iodide. Изопропамида Йодид Hyoscyamine Hydrobromide (BANM) Indisetron Hydrochloride (rINNM) C23H33IN2O = 480.4. Bromidrato de Hiosciamina; Hiosciamina, hidrobromuro de; Hy- Hidrocloruro de indisetrón; Indisétron, Chlorhydrate d’; Indiset- CAS — 7492-32-2 (isopropamide); 71-81-8 (isopropa- oscyamine Bromhydrate. ron Dihydrochloride; Indisetroni Hydrochloridum; N-3389. N- mide iodide). ATC — A03AB09. endo H Гиосциамина Гидробромид (3,9-Dimethyl- -3,9-diazabicyclo[3.3.1]non-7-yl)-1 -inda- ATC Vet — QA03AB09. C17H23NO3,HBr = 370.3. zole-3-carboxamide dihydrochloride. CAS — 306-03-6. Индисетрона Гидрохлорид ATC — A03BA03. C17H23N5O,2HCl = 386.3. ATC Vet — QA03BA03. CAS — 141549-75-9 (indisetron); 160472-97-9 (indiset- H3C CH3 ron dihydrochloride). Pharmacopoeias. In US. H C USP 31 (Hyoscyamine Hydrobromide). White, odourless, crys- 3 N+ CH 3 − tals or crystalline powder. M.p. not less than 149°. Freely soluble I in water; soluble 1 in 2.5 of alcohol, 1 in 1.7 of chloroform, and H NH2 CH 1 in 2300 of ether. pH of a 5% solution in water is about 5.4. Store O 3 in airtight containers. Protect from light. H O N N CH3 NCH3 N Hyoscyamine Sulfate HN H Hiosciamina, sulfato de; Hiosciamino sulfatas; Hioscyjaminy siarc- Pharmacopoeias. In US. H . A white to pale yellow crystal- zan; Hioszciamin-szulfát; Hyoscyamin sulfát dihydrát; Hyo- USP 31 (Isopropamide Iodide) line powder. Soluble 1 in 50 of water, 1 in 10 of alcohol, and 1 in scyamine, sulfate d’; Hyoscyamine Sulphate (BANM); Hyoscyamini 5 of chloroform; very slightly soluble in ether and in benzene. sulfas; Hyoscyamini Sulfas Dihydricus; Hyoscyaminsulfat; Hyo- Protect from light. scyaminum Sulfuricum; Hyoskyamiinisulfaatti; Iosciamina Solfato. (indisetron) Profile Гиосциамина Сульфат Isopropamide iodide is a quaternary ammonium antimuscarinic (C17H23NO3)2,H2SO4,2H2O = 712.8. Profile with peripheral effects similar to those of atropine (p.1219). It CAS — 620-61-1 (anhydrous hyoscyamine sulfate); 6835- Indisetron is a 5-HT3-receptor antagonist with general properties has been used as an adjunct in the treatment of peptic ulcer dis- 16-1 (hyoscyamine sulfate dihydrate). similar to those of ondansetron (p.1756); it is also stated to be an ease, in the relief of gastrointestinal and urinary-tract disorders ATC — A03BA03. antagonist at 5-HT4 receptors. Indisetron hydrochloride is used associated with smooth muscle spasm, in rhinitis, and for the re- ATC Vet — QA03BA03. as an antiemetic in the management of nausea and vomiting as- lief of symptoms of colds. Pharmacopoeias. In Eur. (see p.vii) and US. sociated with chemotherapy. Isopropamide bromide has been used similarly. Ph. Eur. 6.2 (Hyoscyamine Sulphate). A white or almost white, Preparations crystalline powder or colourless needles. Very soluble in water; USP 31: Isopropamide Iodide Tablets. sparingly soluble or soluble in alcohol. A 2% solution in water Ipomoea has a pH of 4.5 to 6.2. Store in airtight containers. Protect from Proprietary Preparations (details are given in Part 3) light. Ipomoea Root; Mexican Scammony Root; Orizaba Jalap Root; Multi-ingredient: Arg.: Plidex†; Braz.: Ornatrol†; Canad.: Stelabid†; USP 31 (Hyoscyamine Sulfate). A white or almost white, crys- Scammony Root. Ital.: Raffreddoremed; Valtrax; Mex.: Stelabid. talline powder or colourless needles. It is deliquescent and affect- Ипомея.
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