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Mebhydrolin/Methdilazine 585 Mebhydrolin/Methdilazine 585 Pharmacopoeias. In Chin. and Eur. (see p.vii). Mepyramine Hydrochloride (BANM, rINNM) Symptom Menstrual; Midol Pre-Menstrual Syndrome; Myci-Spray; MyHist- US specifies the monohydrate. DM; MyHist-PD; Nalex-A 12; ND-Gesic; P-Hist; P-Tanna; Pamprin; Poly- Hidrocloruro de mepiramina; Mépyramine, Chlorhydrate de; Histine†; Premsyn PMS; Pro-Red; Pyrlex CB; R-Tanna; R-Tannamine; R-Tan- Ph. Eur. 6.2 (Meclozine Hydrochloride). A yellow or yellowish- Mepyramini Hydrochloridum; Pyranisamine Hydrochloride; Py- nate; R-Tannic-S†; Rectagene Medicated Rectal Balm; Resperal; Rhinatate; white, crystalline powder. Slightly soluble in water; soluble in al- Robitussin Night Relief; Ryna-12; Soothaderm; Tanoral; Tri-Tannate; Tri- cohol and in dichloromethane. Store in airtight containers. rilamine Hydrochloride. codene Cough & Cold; Triotann; Triplex AD; Tritan; Tussi-12 D; Tussi-12D USP 31 (Meclizine Hydrochloride). The monohydrate is white or Мепирамина Гидрохлорид S; Tussplex; Viravan; Viravan-DM; Z-Xtra; Venez.: Fesanol†; Metilcodin†; Metilfedrin†; Pi-Fedrin; Pinazo. slightly yellowish crystalline powder that has a slight odour. C17H23N3O,HCl = 321.8. Practically insoluble in water and in ether; freely soluble in chlo- CAS — 6036-95-9. roform, in pyridine, and in acid-alcohol-water mixtures; slightly ATC — D04AA02; R06AC01. soluble in dilute acids and in alcohol. Store in airtight containers. ATC Vet — QD04AA02; QR06AC01. Mequitazine (BAN, rINN) LM-209; Mekitatsiini; Mekitazin; Mequitazina; Méquitazine; Adverse Effects and Precautions Mepyramine Maleate (BANM, rINNM) Mequitazinum. 10-(Quinuclidin-3-ylmethyl)phenothiazine. As for the sedating antihistamines in general, p.561. Maleato de mepiramina; Mepiramin Maleat; Mepiramin-maleát; Мехитазин For reports of the use of antihistamines, including Mepiramino maleatas; Mepyramiinimaleaatti; Mepyramin C20H22N2S = 322.5. meclozine, in pregnancy, see p.563. maleinát; Mépyramine, maléate de; Mepyramini maleas; CAS — 29216-28-2. Mepyraminmaleat; Pyranisamine Maleate; Pyrilamine Maleate. ATC — R06AD07. Interactions Mepyramine hydrogen maleate. ATC Vet — QR06AD07. As for the sedating antihistamines in general, p.563. Мепирамина Малеат C17H23N3O,C4H4O4 = 401.5. Uses and Administration CAS — 59-33-6. Meclozine hydrochloride, a piperazine derivative, is a ATC — D04AA02; R06AC01. N sedating antihistamine with antimuscarinic and moder- ATC Vet — QD04AA02; QR06AC01. ate sedative properties. It is mainly used for its an- Pharmacopoeias. In Eur. (see p.vii) and US. N tiemetic action, which may last for up to 24 hours. Ph. Eur. 6.2 (Mepyramine Maleate). A white or slightly yellow- ish, crystalline powder. Very soluble in water; freely soluble in Meclozine hydrochloride is used in the prevention and alcohol. M.p. 99° to 103°. A 2% solution in water has a pH of 4.9 treatment of nausea and vomiting associated with a va- to 5.2. Protect from light. S riety of conditions including motion sickness (p.564) USP 31 (Pyrilamine Maleate). A white crystalline powder usual- and for the symptomatic treatment of vertigo (p.565) ly having a faint odour. Soluble 1 in 0.5 of water, 1 in 3 of alco- Pharmacopoeias. In Jpn. caused by Ménière’s disease and other vestibular disor- hol, 1 in 15 of dehydrated alcohol, and 1 in 2 of chloroform; Adverse Effects and Precautions slightly soluble in ether and in benzene. Its solutions are acid to As for the sedating antihistamines in general, p.561. ders. Meclozine hydrochloride has also been used for litmus. Store in airtight containers. Protect from light. the symptomatic relief of hypersensitivity reactions Sedation. For discussion of the sedative effects of antihista- and pruritic skin disorders (p.565). Adverse Effects and Precautions mines, see p.562. When mequitazine is given in the recommend- ed dosage of 5 mg twice daily the incidence of sedation appears The usual oral dose of meclozine hydrochloride for As for the sedating antihistamines in general, p.561. comparable with that of terfenadine. Sedation has, however, oc- motion sickness is 25 to 50 mg taken about one hour curred after doses of 10 mg twice daily. before travelling and repeated every 24 hours if neces- Interactions Interactions sary; up to 100 mg daily in divided doses has been giv- As for the sedating antihistamines in general, p.563. As for the sedating antihistamines in general, p.563. en for the treatment of vertigo and vestibular disorders. Antibacterials. For a report of torsade de pointes in a patient In the prevention and treatment of motion sickness in Uses and Administration taking spiramycin and mequitazine, see Cytochrome P450 children aged 6 to 12 years, 12.5 mg is given once dai- Mepyramine, an ethylenediamine derivative, is a se- Isoenzymes under Interactions of Spiramycin, p.333. ly; for children aged 2 to 6 years the dose is 6.25 mg dating antihistamine with antimuscarinic and sedative Pharmacokinetics once daily. properties. Mepyramine maleate is used for the symp- After absorption from the gastrointestinal tract, mequitazine is Both meclozine hydrochloride and meclozine base tomatic relief of hypersensitivity reactions and in pru- metabolised. Unchanged drug and metabolites are excreted prin- cipally in the bile. have been given by the rectal route; doses are similar to ritic skin disorders (p.565). Mepyramine maleate is those given orally. also a common ingredient of compound preparations Uses and Administration for the symptomatic treatment of coughs and the com- Mequitazine, a phenothiazine derivative, is a sedating antihista- Preparations mon cold (p.564). mine with antimuscarinic and mild sedative properties. USP 31: Meclizine Hydrochloride Tablets. Mequitazine is used for the symptomatic relief of allergic condi- Mepyramine maleate has been given in an oral dose of tions including urticaria (p.565), rhinitis (p.565) and conjunctivi- Proprietary Preparations (details are given in Part 3) 50 mg at night as a hypnotic in the short-term manage- tis (p.564), and in pruritic skin disorders (p.565). It has been giv- Belg.: Agyrax; Postafene; Braz.: Meclin; Canad.: Bonamine; Chile: Bon- amina; Cz.: Postafen†; Denm.: Postafen; Fin.: Postafen; Fr.: Agyrax; Ger.: ment of insomnia (p.564). en in usual oral doses of 5 mg twice daily. Peremesin N†; Peremesin†; Postadoxin N; Postafen†; Gr.: Emetostop; Preparations Postafene†; Hong Kong: Postafene; Mex.: Chiclida; Marenin; Neth.: Su- A cream containing 2% mepyramine maleate is used primal; Norw.: Peremesin; Postafen; NZ: Sea-Legs; Philipp.: Bonamine; locally for insect bites or stings, and for hypersensitiv- Proprietary Preparations (details are given in Part 3) Postadoxine; Port.: Navicalm; Rus.: Bonine (Бонин); Spain: Chiclida; Arg.: Primalan; Chile: Mircol; Fr.: Primalan; Quitadrill; Ger.: Metaplexan; Dramine; Navicalm†; Swed.: Postafen; Switz.: Duremesan; Turk.: Posta- ity and pruritic skin conditions but, as with any antihis- Ital.: Primalan†; Mex.: Primalan; Philipp.: Primalan; Port.: Primalan; Rus.: doxine; UK: Sea-Legs; USA: Antivert; Antrizine; Bonine; Dizmiss; tamine, there is a risk of sensitisation. It has also been Primalan (Прималан); Spain: Mircol. Dramamine II; Meni-D; Vergon†. used in eye drops. Multi-ingredient: Austria: Contravert B ; Diligan; Ger.: Diligan†; Hong Kong: Navidoxine; India: Diligan; Pregnidoxin; Malaysia: Becoloxin†; In some countries mepyramine maleate is available for Navidoxine†; Mex.: Bonadoxina; Bonalen; Bonazin; Emediba; Liatriz; Mecl- Methdilazine (BAN, rINN) ifar; Meclison; Pidoxina; Vo-Remi; Neth.: Emesafene; Port.: Diligan†; parenteral use. Mepyramine hydrochloride has also S.Afr.: Geratar; Singapore: Navidoxine†; Switz.: Duremesan; Itinerol B ; been given parenterally or by the rectal route. Metdilatsiini; Metdilazin; Metdilazina; Methdilazinum; Metodilazi- UK: Traveleeze; Venez.: Bonadoxina; Etizil†; Mebax†. Mepyramine tannate and mepyramine acefyllinate na. 10-(1-Methylpyrrolidin-3-ylmethyl)phenothiazine. have been used orally. Метдилазин C18H20N2S = 296.4. Preparations CAS — 1982-37-2. Mepyramine (BAN, rINN) BP 2008: Mepyramine Tablets; ATC — R06AD04. Mepiramina; Mepyramiini; Mepyramin; Mépyramine; Mepyrami- USP 31: Pyrilamine Maleate Tablets. ATC Vet — QR06AD04. num; Pyranisamine; Pyrilamine. 2-(N-p-Anisyl-N-2-pyridylami- Proprietary Preparations (details are given in Part 3) no)ethyldimethylamine. Austral.: Relaxa-Tabs; Braz.: Alergitanil; Hong Kong: Anthisan; Irl.: An- thisan; NZ: Anthisan; S.Afr.: Anthisan; Antihist; Mepyraderm; Mepyrimal; Мепирамин Spain: Fluidasa; UK: Anthisan; USA: Pyrlex. N C H N O = 285.4. Multi-ingredient: Arg.: Bajumol†; Drynisan; Everfem; Fadanasal; Piracala- 17 23 3 CH3 CAS — 91-84-9. mina; Polipectol†; Rynatanic†; Austral.: Neo-Diophen†; Belg.: Nortussine; Braz.: Alergitrat†; Alergo Glucalbet†; Beclase; Benistina†; Benzomel†; Co- N ATC — D04AA02; R06AC01. nidrin; Expectussin†; Ginometrim Oral†; Gripanil†; Gripsay; Killgrip†; Narid- ATC Vet — QD04AA02; QR06AC01. rin; Nariflux; Nasogrip; Posdrink; Canad.: Extra Strength Multi-Symptom PMS Relief†; Hycomine; Jack and Jill; Midol Extra Strength; Midol PMS Extra Strength; Pamprin; Prefrin A; ratio-Theo-Bronc; Relievol PMS; Trendar S PMS†; Tylenol Menstrual; Chile: Alerzona; Kitadol Periodo Menstrual; Min- faden; Predual; Rinolergan; Tapsin Periodo Menstrual; Fr.: Nortussine; N Hong Kong: Easiko†; Israel: Aforinol; Alnase; Phenyphrine-Azol†; Ital.: Balsamina Kroner; Triaminic; Vasofen; Malaysia: Prefrin A†; Mex.: Femse- Methdilazine Hydrochloride (BANM, rINNM) din Kutz; Lentostamin; Pol.: Kato-Nasal; Pro-Miss;
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