PRODUCT MONOGRAPH IMITREX DF IMITREX ... - GlaxoSmithKline

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PART II: SCIENTIFIC INFORMATIONPHARMACEUTICAL INFORMATIONDrug SubstanceTablet/InjectionProper name:Chemical name:sumatriptan succinate (USAN, BAN and INN)3-[2-(dimethylamino)ethyl]-N-methyl-indole-5-methanesulphonamide succinate (1:1)Molecular formula : C 14 H 21 N 3 O 2 S•C 4 H 6 O 4Molecular mass: 413.5Structural formula:Physicochemical properties:Physical Characteristics: White to off-white powder with a melting point between164.6°C-165.5°C.Solubility:pH and pka:In water (4°C) = 54 mg/mLIn water (20°C) = 101 mg/mLIn saline (0.9% w/v, 4°C) = 62 mg/mLIn saline (0.9% w/v, 20°C) = 109 mg/mLThe pH of a 1% w/v solution of sumatriptan succinate in water isapproximately 4.9.pka 1 (succinic acid) = 4.21, 5.67pka 2 (3° amine group) = 9.63pka 3 (sulphonamide group) >12Partition Coefficient (between n-octanol and water): log P = 1.07 at a pH of 10.7October 21, 2014Page 24 of 58
Nasal SprayProper name:Chemical name:sumatriptan3-[2-(dimethylamino)ethyl]-N-methyl-1H-indole-5-methanesulphonamideMolecular formula : C 14 H 21 N 3 O 2 SMolecular mass: 295.4Structural formula:Physicochemical properties:Physical Characteristics: White to pale yellow powder with a melting point about176° C.Solubility:In water (4°C, 20°C) ≈ 1 mg/mLpka: pka 1 (3° amine group) = 9.63pka 2 (sulphonamide group) >12Partition Coefficient: log P = 1.06 (20° C)CLINICAL TRIALSMigraine:TabletsThe efficacy of <strong>IMITREX</strong> ® Tablets for the treatment of migraine was established in fourmulticentre, randomized, placebo-controlled studies. Patients enrolled and treated in thesestudies were primarily female (84%), Caucasian (98%) and with a mean age of 40 years(range of 18 to 65 years). Patients were instructed to treat a moderate to severe headache.In Study 2, up to three doses were permitted to treat a single attack within a 24-hourperiod, non-responders could take a second dose at two hours, while any recurrence ofmigraine could be treated with a third dose. Studies 1, 3 and 4 were designed to allow forthe treatment of up to three attacks.October 21, 2014Page 25 of 58
Page 3 and 4: IMITREX DF ®(sumatriptan succinate
Page 5 and 6: Ergot-containing drugs have been re
Page 7 and 8: The systematic approach described a
Page 9 and 10: three of the subjects (two of whom
Page 11 and 12: Special PopulationsPregnant Women:
Page 13 and 14: e intense. These may occur in any p
Page 15 and 16: Table 4Treatment-Emergent Adverse E
Page 17 and 18: unaltered when preceded by a single
Page 19 and 20: Clinical trials have shown that app
Page 21 and 22: ACTION AND CLINICAL PHARMACOLOGYMec
Page 23: STORAGE AND STABILITYIMITREX DF ®
Page 27 and 28: Table 7Percentage of Patients with
Page 29 and 30: Table 9Percentage of Patients with
Page 31 and 32: Sumatriptan (1-1000 μg/kg, iv) pro
Page 33 and 34: Metabolism of the methylaminosulpho
Page 35 and 36: Chronic toxicity studies were carri
Page 37 and 38: MutagenicitySumatriptan produced no
Page 39 and 40: In inhalation toxicity studies (dog
Page 41 and 42: 14. Heyck H. Pathogenesis of migrai
Page 43 and 44: IMPORTANT: PLEASE READPART III: CON
Page 45 and 46: IMPORTANT: PLEASE READOther side ef
Page 47 and 48: IMPORTANT: PLEASE READPART III: CON
Page 49 and 50: IMPORTANT: PLEASE READFigure 1• T
Page 51 and 52: IMPORTANT: PLEASE READFigure 12How
Page 53 and 54: IMPORTANT: PLEASE READSERIOUS SIDE
Page 55 and 56: IMPORTANT: PLEASE READ• you are t
Page 57 and 58: IMPORTANT: PLEASE READSIDE EFFECTS

PRODUCT MONOGRAPH IMITREX DF IMITREX ... - GlaxoSmithKline

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