5/20 Sevikar 5/20mg film coated tablets

5/20 Sevikar 5/20mg film coated tablets

ፏဍ᛾ᒯԅ಑024929ဴ
2008ԑ6Т‫ڙ‬ॏ(಑1‫)ގ‬
๲૕ஶጰ՘ᒻ 5/20యպ
యպ
Sevikar® 5/20mg film coated tablets
ҏ᛾໸ҥᚂৱ೎П‫ٺ‬Ң
Sevikar® (amlodipineᇄolmesartan medoxomil)ᒻᏘ
ѹஏ‫ٺ‬Ң
ܻᛄѹ಑2‫ڷ‬಑3෈݈Ң‫ޢ‬௥հҢܻ๫શɯՖᆓԝᕻશ‫ف‬ಛ
‫ޟ‬᛾‫ސ‬Ȃџ૖༌৛ี‫ى‬ϛप‫ࣥڋ‬ՍഅԙԫιȄषี౪ᛄ
ѹȂᔖҳ։ୄҢSevikar®Ȧ୤َឌᇭЅ‫ݧ‬ཎ‫ٱ‬໶ (5.1)ȧȄ
1 ᎌᔖ੿ᇄҢഊ
൐Ιᕛ‫ݲ‬ฒ‫ݲ‬௡‫ޟڙ‬ଽՖᔆȂհ࣏಑ΠጣҢ᛾Ȅ
2 Ꮨ໔ᇄҢ‫ݲ‬
ΙૡՃኌ‫ٱ‬໶
Olmesartan medoxomil೽ல࡞Ѝ౰ҡ୙հҢȂи୙հҢᡗณ
ᇄᏘ໔ฒᜰȂծamlodipine‫ޟ‬୙հҢ(кौ࢐Ыရ)ࠌᇄᏘ໔
ԤᜰȄ
‫׽‬ᡐᏘ໔ࡣ2໊ϱџႀ‫ڗ‬ശσ६Ֆᔆਝ‫ݎ‬Ȅ
Sevikar®џས଩‫ܖ‬Ϛས଩ॵ‫݈ސ‬ҢȄ
Sevikar®џᇄ‫ڏ‬т६Ֆᔆ᛾‫ځސ‬ҢȄ
‫ٺ‬Ң2໊ࡣџቨёᏘ໔ȄSevikar®‫ޟ‬ശଽ࡚ដᏘ໔࢐10/40 mgȄ
෇ф‫ݽ‬ᕛ
Sevikar®џо‫ڥ‬ф‫ڏ‬এտ‫ޟ‬ԙӋȄ
‫ڥ‬фএտԙӋਢȂषՖᔆ௡‫ڙ‬ϫϚ౩དȂџඪଽ‫ڏ‬ϛΙᆍ
‫ڍܖ‬ᆍԙӋ‫ޟ‬Ꮨ໔Ȅ
࿋௉‫ޱ‬൐ᐿ‫ٺ‬ҢAmlodipine(‫ڏܖ‬тdihydropyridine໗ᚔυ೽
ၾߢᘞᏘ)‫ܖ‬൐ᐿ‫ٺ‬Ңolmesartan medoxomil(‫ڏܖ‬тՖᆓԝᕻ
શ‫ڧ‬ᡝߢᘞᏘ)ࡣՖᔆ௡‫ڙ‬Ϛ౩ད‫ޟ‬௉‫ޱ‬Ȃᙽ࣏Sevikar‫ݽ‬ᕛ
џඪ‫໌ټ‬Ι؏Ϟ६ᔆਝ‫ݎ‬Ȅ
3 Ꮨ࠮ᇄ֤໔
Sevikar®ᒻᏘ‫ޟ‬Ꮨ࠮࣏ο݈Ң᛾Ȃ֤໔ಢӫϷ࣏Ȉ
amlodipine ࣺ࿋ܻ (mg)
olmesartan medoxomil (mg)
5/20
5
20
4 ࿱‫੿נ‬
ฒȄ
5 ឌᇭЅ‫ݧ‬ཎ‫ٱ‬໶
Sevikar®‫ޟ‬Ϛ‫ي‬Іᔖ೽லᇄ‫ڏ‬এտԙӋԤᜰȄ
5.1 प‫ڋ‬ʝཱིҡ‫ڋ‬ᑯ੾ᇄԫι
Olmesartan medoxomilȄѹஏष݈Ң‫ޢ‬௥հҢܻ๫શɯՖ
ᆓԝᕻશ‫ف‬ಛ‫ޟ‬᛾‫ސ‬Ȃџ૖അԙप‫ཱིڷڋ‬ҡ‫ڋ‬ᑯ੾ᇄԫ
ιȄҬࠉжࣨМᝦϛϐԤኵΪӇ݈ҢՖᆓԝᕻશᙽ඲ ‫׻‬
‫ڙ‬Ꮨ௉‫ޟޱ‬ӱൢਰ‫ٽ‬Ȅषี౪ᛄѹȂᔖҳ։ୄҢSevikar®Ȅ
ӵᛄѹ಑2‫ڷ‬಑3෈ਢȂ೻᜸᛾‫ސ‬џ૖༌৛प‫ڋ‬Ȃѓࢂഅԙ
ճՖᔆȃཱིҡ‫ڋ‬ᢓ଼ี‫ى‬ϚӒȃฒ‫੿׍‬ȃџଛ‫ܖ‬Ϛџଛ‫ܒ‬
๫᠚૾ᆑЅԫιȄԪѴζෆีҡՀЫႆЍਰ‫ٽ‬Ȃᐃ௰ก࢐
ҥܻप‫ڋ‬๫ђ૖‫ܚཬڧ‬അԙȇषӰ೻ᆍӰશഅԙՀЫႆ
ЍȂџ૖Ᏺमप‫ڋ‬Ѳ޴ᠿᕻȃᢓ᚟࿌‫޲ڷל‬ഋี‫ى‬Ϛ‫ي‬Ȅ
ԪѴζෆีҡԞ౰ȃυ৞ϱҡߝᒶጥ‫ڷ‬໠ܹ‫ܒ‬ଢ଼૕Ᏺᆓ้
ਰ‫ٽ‬ȂծϚጂۡ೻‫֏࢐ݷޑٲ‬Ӱ݈ҢԪ᛾‫ܚ‬അԙȄ
ष༉ܻᛄѹ಑1෈ܻυ৞ϱ௥ញ᛾‫ސ‬ȂխнϚོ౰ҡΰक़
Ϛ‫ي‬ІᔖȄषѹஏ༉ܻᛄѹ಑1෈݈ҢՖᆓԝᕻશII‫ڧ‬ᡝ
ࡼ‫ת‬ᏘȂ‫ٺ‬तप‫ڷ‬प‫ڋ‬௥ញ၎᛾‫ސ‬Ȃᔖ֙‫ޣ‬ѹஏԪଉ਀Ȅ
ᏑᆓԃԪȂΙҍ௉‫ڧޱ‬ѹȂᚂৱᔖҳ։ᡱ௉‫ޱ‬ୄҢSevikar®Ȅ
ӵྃЍَ(џ૖ؐνӪѹஏϛϚ‫ڗ‬1‫ޟ)ٽ‬௑‫ݷ‬ϛȂџ૖‫ײ‬Ϛ
‫ڏڗ‬т᛾‫ڥސ‬фհҢܻ๫શɯՖᆓԝᕻશ‫ف‬ಛ‫ޟ‬᛾‫ސ‬Ȅӵ
೻ᆍ‫َق‬௑‫ݷ‬ϛȂᔖ֙‫ޣ‬ѹஏ‫ڏ‬प‫ڋ‬џ૖ᎏ‫ڧ‬Ӡ৛Ȃ‫໌ٮ‬
՗ӻԩ຺ॱ‫ݰ‬ᔮࢥоຟեՀጰϱᕗცȄ
षี౪ՀЫႆЍȂଶߨୄ᛾ོӠЅҔᡝ‫ڼܒ‬Ȃ֏ࠌᔖୄҢ
Sevikar®Ȅυ৞ԝᕻᔆΨกၐ(CST)ȃฒёᔆกၐ(NST)‫ܖ‬
प‫ڋ‬ҡ౩ࣀଢ଼ຟե(BPP)഍џ໌՗Ȃຜᛄѹ໊ኵՄۡȄณ
ՄȂ௉‫ڷޱ‬ᚂৱᔖᕣ၌Ȃџ૖ӵप‫ڋ‬ϐᎏ‫ڧ‬Ϛџଛ‫ܒ‬༌৛
ࡣȂϗю౪ՀЫႆЍ௑‫ל‬Ȅ
षᔉ‫ڋ‬ෆܻυ৞ϱ௥ញՖᆓԝᕻશII‫ڧ‬ᡝࡼ‫ת‬ᏘȂᔖ஝ϸ
ᢎᄆ࢐֏ԤճՖᔆȃЍ‫ڷ׍‬ଽՖ႕้౪ຫȄषีҡЍ‫׍‬Ȃ
ᔖ๿१ܻᆰࡻՖᔆᛧۡ‫ڷ‬๫᠚ៀࢺȂџ૖҆໸௴Ң඲Ֆ‫ܖ‬
ആ‫้ݙ‬П‫ݲ‬Ȃо‫׽‬๡ճՖᔆЅʝ‫ڥܖ‬ф౴ல๫ђ૖Ȅ
Olmesartan medoxomilоശଽ1000 mg/kg/dayο݈Ꮨ໔(о
mg/m2࣏அྥ඲ᆗȂࣺ࿋ܻΡᡝശଽ࡚ដᏘ໔[MRHD]‫ޟ‬
240ॻ)‫׹‬ϠᛄѹσჃȂ‫ܖ‬оശଽ1 mg/kg/dayο݈Ꮨ໔‫׹‬Ϡ
ᛄѹ‫ڊ‬υ(оmg/m2࣏அྥ඲ᆗȂࣺ࿋ܻMRHD‫ޟ‬Ιјȇҥ
ܻ‫؁‬ଽᏘ໔ོ߯Ᏺम‫ڊ‬υप‫ڋ‬ԫιȂӰԪฒ‫ݲ‬о‫؁‬ଽᏘ໔
ຟեᄇप‫ޟىีڋ‬ኇ៪)Ȃ‫ٮ‬Ґี౪म࿌पਝᔖȄӵσჃ
ϛȂᏘ໔1.6 mg/kg/dayਢȂ҂Ⴣюҡᡝ१‫ڷ‬ᡝ१ቨёൽ࡙
݂ᡗή६ȂᏘ໔8 mg/kg/dayਢȂ१ौี‫ٱى‬Ӈ‫۽‬ᒶ(ՆᄐϷ
Ⴄȃߝюήߞбȃю౪လЩȃ࿞βή६ЅಁᙂϷ໠้ี‫ى‬
֯‫۽‬ᒶ)Ȃи๫‫ޠ‬ᘗ஻ีҡ౥‫ޟ‬Ꮨ໔ࣺᜰ‫ܒ‬ЀଽȄσჃҐ
ю౪ี‫ޟܒࢳى‬ԤਝᏘ໔࢐0.3 mg/kg/dayȂघ࣏MRHD(։
40 mg/day)‫ޟ‬ΪϷϞΙȄ
ӵ‫ܚ‬Ԥ‫ݽ‬ᕛಢϞ໢ȂΙૡՄِτ‫ޟܒ‬Ыရีҡ౥ଽܻ‫ظ‬
‫ܒ‬Ȃᇄӑࠉ‫ޟ‬amlodipineၐᡛᢎᄆ๖‫ࣺݎ‬ӣȄ
ᚖ‫ี෈ޡ‬ҡ౥ၶճ‫ޟ‬Ϛ‫ي‬ІᔖȂӵSevikar® ‫ݽ‬ᕛಢ‫ีޟ‬
ҡШ౥ࣺ࿋ܻ‫ܖ‬ଽܻԊኑᏘಢȄ೻᜸୙հҢѓࢂճՖᔆȃ
࠼༖‫ܒ‬ճՖᔆȃҪ઄ȃཫᝨȃЖ௚ȃᓜ‫׍ۇڷ׍‬Ȅ
࣏෈44໊‫ޟ‬amlodipineӫ‫ځ‬olmesartan medoxomil໠ܹ኿Ұ
ፒП‫ݽ‬ᕛ‫ܚ‬ᡗҰ‫ޟ‬Ϛ‫ي‬ІᔖኵᐃȂᇄ8໊ᚖ‫ޡ‬ȃԊኑᏘᄇ
ྱ෈‫ޟ‬ኵᐃࣺխȄ
Amlodipine
छ୽‫ڏڷ‬т୽ড়‫ޟ‬ᖝ‫ח‬ၐᡛϐବᄇ຺ႆ11,000Ӫ௉‫ޱ‬ຟե
Amlodipine‫ޟ‬ԊӒ‫ܒ‬Ȅ௥‫ڧ‬amlodipine‫ݽ‬ᕛ෈໢ӱൢ‫ޟ‬Ϛ
‫ي‬Іᔖσӻ࣏ሆ࡙‫ܖ‬ϛ࡙Ȅӻ໶ᖝ‫ח‬ᄇྱၐᡛ‫ޢ‬௥Шၶശ
ଽᏘ໔ႀ10 mg‫ޟ‬amlodipine(N=1730) ᇄԊኑᏘ (N=1250)Ȃ
ี౪amlodipine‫ݽ‬ᕛಢѫԤघ1.5%‫ޟ‬௉‫ޱ‬ӰϚ‫ي‬ІᔖՄୄ
ҢamlodipineȂՄԊኑᏘಢࠌघ࣏1 %Ȅശலَ‫ޟ‬୙հҢ
࢐ᓞฮ‫ڷ‬ЫရȄᏘ໔ࣺᜰ‫ޟ‬୙հҢีҡ౥(%)ԃήȈ
୙հҢ
Ыရ
ᓞཷ
ዘऔ
Ж௚
ԊኑᏘ
N=520
0.6
1.5
0.0
0.6
2.5 mg
N=275
1.8
1.1
0.7
0.7
5.0 mg
N=296
3.0
3.4
1.4
1.4
10.0 mg
N=268
10.8
3.4
2.6
4.5
൷ኵᆍխнᇄ᛾‫ڷސ‬Ꮨ໔ࣺᜰ‫ޟ‬Ϛ‫ي‬ІᔖՄِȂτ‫ٺܒ‬
Ңamlodipine‫ݽޟ‬ᕛีҡ౥σܻ‫ܒظ‬Ȃԃήߒ‫ܚ‬ҰȈ
୙հҢ
Ыရ!
ዘऔ!
Ж௚
༞ᆃ
ԊኑᏘ
τ‫=ܒ‬%
‫=ܒظ‬%
(N=914) (N=336)
5.1
1.4
0.9
0.3
0.9
0.9
0.3
0.8
Amlodipine
τ‫=ܒ‬%
‫=ܒظ‬%
(N=1218) (N=512)
14.6
5.6
4.5
1.5
3.3
1.4
1.6
1.3
Olmesartan medoxomil
Ҭࠉϐବᄇ3825՝оΰ‫ޟ‬௉‫ޱ‬ʝ‫ڧ‬ၐ‫ޱ‬ຟեOlmesartan
medoxomil‫ޟ‬ԊӒ‫ܒ‬Ȃѓࢂᄇྱၐᡛϛ຺ႆ3275՝௥‫ڧ‬ଽ
Ֆᔆ‫ݽ‬ᕛ‫ޟ‬௉‫ޱ‬Ȅ‫ڏ‬ϛघ900Ρ௥‫ݽڧ‬ᕛՍЍ6এТȂ຺
ႆ525ΡՍЍ1ԑȄ‫ٺ‬Ңolmesartan medoxomil‫ݽ‬ᕛ‫ޟ‬ञ‫ڧ‬
‫يܒ‬ԁȂϚ‫ٱي‬Ӈีҡ౥ᇄԊኑᏘࣺխȂи೽ல࣏ሆ࡙ȃ
኷ਢ‫ܒ‬Ȃᇄolmesartan medoxomil‫ޟ‬Ꮨ໔ฒᜰȄ
Ϛ‫ٱي‬Ӈ‫ޟ‬ᐌᡝีҡᓜ౥ᇄᏘ໔ฒᜰȄਲ਼ᐃ‫ܒ‬տȃԑឭ
‫ڷ‬ᆍఊ‫ޟ‬Ϸ‫ݙ‬๖‫ݎ‬ᡗҰȂolmesartan medoxomil‫ݽ‬ᕛಢ‫ڷ‬
ԊኑᏘಢϞ໢‫ٮ‬ฒ৯౴Ȅӵ‫ܚ‬ԤବᄇଽՖᔆ௉‫໌ޱ‬՗‫ޟ‬
ၐᡛϛȂӰϚ‫ي‬Іᔖଝю‫ޟ‬Ш౥ӵolmesartan medoxomil
‫ݽ‬ᕛಢ࣏2.4%(79/3278)Ȃᄇྱಢࠌ࣏2.7%(32/1179)Ȅӵ
ԊኑᏘᄇྱၐᡛϛȂolmesartan medoxomil‫ݽ‬ᕛಢϛ୲Ι
ีҡܻ1%оΰ‫ޟ‬௉‫ޱ‬Ȃиีҡ౥ଽܻԊኑᏘಢ‫ޟ‬Ϛ‫ٱي‬
Ӈ࢐ᓞཷ(3%Ш1%)Ȅ
6.2 ΰѿࡣငᡛ
Sevikar®এտԙӋ೽ႆਯটࡣȂ‫ٺ‬Ңਢෆี౪оήϚ‫ي‬І
ᔖȄҥܻ೻‫ٲ‬Іᔖ֯ҥ௉‫ޱ‬Ռี‫ܒ‬ӱൢȂи௉‫ޱ‬ఊတσ
ωϚጂۡȂӰԪϚΙۡ૖ஊԤਝեᆗีҡ౥Ȃ‫ܖ‬ጂҳᇄ
Ϛ‫ي‬Іᔖᇄ᛾‫ސ‬໢‫ޟ‬Ӱ‫ݎ‬ᜰ߽Ȅ
AmlodipineȄΰѿࡣෆԤЍኵΡӱൢีҡ‫ܒظ‬τٰ੿Ȃ
ծӰ‫ݎ‬ᜰ߽ฒ‫ݲ‬ጂۡȄӵΰѿࡣငᡛϛȂෆԤ௉‫ޱ‬ӱൢ
‫ٺ‬Ңamlodipineբᓍีҡ༁આ‫مڷ‬᠚ሕશЀଽ(σӻᇄᖚ
Ҙ᢮ᑖ‫އمܖ‬Ιम)Ȃ࢚‫ᝒٽ੾ٲ‬१‫ڗ‬ሯौ՞଱Ȅ
Olmesartan medoxomilȄΰѿࡣငᡛϛෆൢ֙ีҡоή
Ϛ‫ي‬ІᔖȈ
Ӓ٘‫ܒ‬Ȉ૾৵ȃՖᆓ‫ܒ‬Ыရ
थဗȈმӥ
ՊՈ଼ᓫȈᐗ઴Պྙ၌
‫׍ݪ‬ҡ෥‫ف‬ಛȈࡨ‫ܒ‬๫૾ᆑ
ҪጳᇄߣӇȈ௬Ꮑȃཫᝨȃ⻼ബ઄
7 ᛾‫ސ‬ҺϣհҢ
7.1 ᇄSevikar®‫ޟ‬᛾‫ސ‬ҺϣհҢ
ӣਢࢊҢamlodipineᇄolmesartan medoxomilȂ᛾‫ސ‬ଢ଼ΨᏰ
‫ٮ‬Ґ‫׽‬ᡐȄ
Ҭࠉ‫ٮ‬ฒၐᡛຟեSevikar®‫ڏڷ‬т᛾‫ޟސ‬᛾‫ސ‬ҺϣհҢȂծ
ԃήМ‫ܚ‬क़ȂϐԤၐᡛं‫ـ‬Sevikar®‫ޟ‬এտԙӋamlodipine
‫ڷ‬olmesartan medoxomilȂၐᡛϛ‫ٮ‬Ґี౪ᡗ๿‫ޟ‬᛾‫ސ‬Һ
ϣհҢȄ
7.2 ᇄAmlodipine‫ޟ‬᛾‫ސ‬ҺϣհҢ
‫ޟ‬᛾‫ސ‬ҺϣհҢ
௉‫(ޱ‬Ў‫࢐ڏ‬१࡙ߢ༬‫ޑࠅܒ‬ଢ଼૕੽੾௉‫)ޱ‬໠ۖ௥‫ڧ‬໗ᚔ
υ೽ၾߢᘞᏘ‫ݽ‬ᕛ‫ܖ‬ඪଽᏘ໔ࡣȂЖ๕ฮ‫ܒࡨܖ‬ЖՊఠ༬
ีҡ‫ޟ‬ᓜ౥ȃࡻ៉ਢ໢‫ᝒܖ‬१‫ܒ‬џ૖ЀଽȄ೻ᆍਝᔖ‫ޟ‬ᐠ
‫ڙ‬Ҭࠉ‫ۦ‬ҐጂۡȄ
ᡝѴၐᡛኵᐃᡗҰȂamlodipine‫ٮ‬Ϛོኇ៪digoxinȃ
phenytoinȃwarfarin‫ڷ‬indomethacinᇄΡᡝՖዎೖҩ‫ޟ‬๖ӫȄ
‫ڏ‬т᛾‫ސ‬ᄇ
‫ڏ‬т᛾‫ސ‬ᄇAmlodipine‫ޟ‬ኇ៪
‫ޟ‬ኇ៪
CimetidineȈamlodipine‫ڷ‬cimetidine‫ځ‬ҢϚོ‫׽‬ᡐamlodipine
‫ޟ‬᛾‫ސ‬ଢ଼ΨᏰȄ
ိຉࢤҘȈ20՝୊ஶ‫ס‬᜹‫ޱ‬ӣਢ݈Ң240 mLိຉࢤҘ‫ڷ‬
10 mg൐ԩο݈Ꮨ໔‫ޟ‬amlodipineȂ‫ٮ‬Ґี౪amlodipine‫ޟ‬
᛾‫ސ‬ଢ଼ΨᏰ‫ڗڧ‬ᡗ๿ኇ៪Ȅ
Maalox®(‫ڙ‬ሖᏘ)Ȉӣਢ‫׹‬Ϡ‫ڙ‬ሖᏘMaalox®‫ڷ‬൐ԩᏘ໔‫ޟ‬
amlodipineȂᄇamlodipine‫ޟ‬᛾‫ސ‬ଢ଼ΨᏰ‫ؠ‬Ԥᡗ๿ኇ៪Ȅ
SildenafilȈনี‫ܒ‬ଽՖᔆ௉‫ٺޱ‬Ң൐ԩᏘ໔100 mg‫ޟ‬
sildenafilȂᄇamlodipine‫ޟ‬᛾‫ސ‬ଢ଼ΨᏰ୤ኵ‫ؠ‬Ԥኇ៪Ȅ
Amlodipine‫ڷ‬sildenafilоፒП‫ځ‬ҢਢȂ‫ڍ‬ᆍ᛾‫ސ‬Ϸտีථ
६Ֆᔆਝ‫ݎ‬Ȅ
Amlodipineᄇ‫ڏ‬т᛾‫ޟސ‬ኇ៪
ᄇ‫ڏ‬т᛾‫ޟސ‬ኇ៪
AtorvastatinȈ‫ځ‬Ңӻԩ10 mg‫ޟ‬amlodipine‫ڷ‬80 mg‫ޟ‬
atorvastatinȂี౪atorvastatin‫ޟ‬ᛧۡᄘ᛾ଢ଼୤ኵ‫ٮ‬ฒᡗ๿
ᡐϽȄ
DigoxinȈ୊ஶ‫ס‬᜹‫ޱ‬ӣਢ݈Ңamlodipine‫ڷ‬digoxinȂՖ఼
digoxinᐨ࡙‫ܖ‬digoxin๫᠚఼ଶ౥‫ٮ‬Ґ‫׽‬ᡐȄ
Κ᎕(ନᆠ)Ȉ൐ԩ‫ڷ‬ӻԩ10 mg‫ޟ‬amlodipineᄇΚ᎕‫ޟ‬᛾‫ސ‬
ଢ଼ΨᏰ‫ؠ‬Ԥᡗ๿ኇ៪Ȅ
WarfarinȈ‫ځ‬Ңamlodipine‫ڷ‬warfarin‫ٮ‬Ϛོ‫׽‬ᡐwarfarin‫ޟ‬
ᏗՖ নІᔖਢ໢Ȅ
ӵᖝ‫ח‬ၐᡛϛȂamlodipineෆᇄthiazideց‫׍‬ᏘȃΚ࠮Һཐ
ડငߢᘞᏘȃՖᆓԝᕻશᙽ඲ ‫ڙ׻‬Ꮨȃߝਝ࠮฼ሖᢄȃ
฼ሖҠ‫ݶ‬Տή֤аȃdigoxinȃwarfarinȃߨ᜸‫ھ‬᎕ੑ‫އ‬᛾ȃ
‫ת‬ҡશЅο݈६ՖᑥᏘԊӒӫ‫ٺځ‬ҢȄ
5.5 ᢮Ֆ‫ܒ‬Ж᠚૾ᆑ௉‫ޱ‬
7.3 ᇄOlmesartan Medoxomil‫ޟ‬᛾‫ސ‬ҺϣհҢ
‫ޟ‬᛾‫ސ‬ҺϣհҢ
AmlodipineȄΙૡՄِȂЖ᠚૾ᆑ௉‫ޱ‬ᔖᙱབ‫ٺ‬Ң໗ᚔυ
೽ၾߢᘞᏘȄΙ໶ԊኑᏘᄇྱၐᡛବᄇ1,153՝‫ٺ‬ҢᛧۡᏘ
໔‫ޟ‬ACE‫ڙ׻‬Ꮨȃdigoxin‫ڷ‬ց‫׍‬Ꮨ‫ޟ‬NYHA಑έ‫ܖ‬಑Ѳ઻
Ж᠚૾ᆑ௉‫ޱ‬Ȃं‫ـ‬Amlodipine(ؐЈ5-10 mg)‫ޟ‬ኇ៪Ȅଡ
ᙹਢ໢ՍЍ6এТȂҁ֯घ14এТȄ๖‫ݎ‬ᡗҰȂ၎᛾‫ސ‬ᄇ
Ԇࣀ౥‫ܖ‬Ж᠚ᑯ੾౥(ۡဎ࣏ӠЅҡ‫ޟڼ‬ЖࡡϚᐌȃࡨ‫ܒ‬
ЖՊఠ༬‫ܖ‬ӰЖ᠚૾ᆑ௑‫ݷ‬ඌϽՄ՞଱)‫ٮ‬ฒᐌᡝϚ‫ي‬ኇ
៪ȄԤѲএ࣏෈8Ս12໊‫ޟ‬ၐᡛШၶAmlodipine‫ڷ‬ԊኑᏘȂ
೻‫ٲ‬ၐᡛ‫ޟ‬ᄇຫ࣏NYHA಑Πȃέ઻Ж᠚૾ᆑ௉‫ޱ‬Ȃӓॎ
697ΡȄՄၐᡛϛਲ਼ᐃၼଢ଼ञΨ‫ޟ‬ก໔ȃNYHAϷ઻ȃ੿
‫ܖޑ‬LVEFȂҐี౪Ж᠚૾ᆑඌϽ‫ޟ‬ၬຫȄ
ӵ୊ஶ‫ס‬᜹‫ޱ‬оdigoxin‫ܖ‬warfarinӣਢ‫ځ‬Ңolmesartan
medoxomil‫ޟ‬ၐᡛϛȂҐӱൢю౪ᡗ๿‫ޟ‬᛾‫ސ‬ҺϣհҢȄ
Olmesartan medoxomilᇄ‫ڙ‬ሖᏘ[Al(OH)3/Mg(OH)2]‫ځ‬ҢਢȂ
ҡᡝџցҢ౥‫ٮ‬ฒᡗ๿‫׽‬ᡐȄ
Olmesartan medoxomilϚငҥಠफՓશP450‫ف‬ಛфᗂȂᄇ
P450ሕશζ‫ؠ‬Ԥኇ៪ȂӰԪȂႱ෈Ԫ᛾‫ސ‬Ϛོᇄ‫ڙ׻‬ȃᇶ
ี‫ܖ‬ҥ೻‫ٲ‬ሕશфᗂ‫ޟ‬᛾‫ސ‬౰ҡҺϣհҢȄ
5.2 ᡝశϚٗ‫ܖ‬ᢄӋϚٗ௉‫ีޱ‬ҡճՖᔆ
Olmesartan medoxomilȄ໠ۖ௥‫ڧ‬olmesartan medoxomil‫ݽ‬
ᕛࡣȂџ૖ีҡԤ੿‫ޟޑ‬ճՖᔆȄ๫શɯՖᆓԝᕻશ‫ف‬ಛ
ϐࣀϽ‫ޟ‬௉‫ޱ‬Ȃ‫ٽ‬ԃᡝశϚٗЅʝ‫ܖ‬ᢄӋϚٗ࠮௉‫ٽ(ޱ‬
ԃ௥‫ڧ‬ଽᏘ໔ց‫׍‬Ꮨ‫ݽ‬ᕛ‫)ޱ‬ȂЎ‫ڏ‬ৠܾีҡճՖᔆȄ೻
‫ٲ‬௉‫ޱ‬ᔖӵ஝ϸᚂᕛᅿ࿜ή໠ۖ௥‫ڧ‬Sevikar®‫ݽ‬ᕛȂषี
ҡճՖᔆȂᔖ߳ࡻӉ޼࠼༖Ȃ҆ौਢоᓗ૕ᒯశ๝Ϡҡ౩
ॵᢄЫȄ኷ਢ‫ܒ‬ճՖᔆІᔖ‫ߨٮ‬᝷៉‫ݽ‬ᕛ‫ޟ‬࿱‫੿נ‬Ȃ೽ல
ܻՖᔆᛧۡࡣ։џ᝷៉‫ݽ‬ᕛȄ
5.3 Ֆᆓᘗ஻
AmlodipineȄҥܻSevikar®ϛ‫ޟ‬amlodipineོംᅚᏲमՖᆓ
ᘗ஻ȂӰԪο݈ࡣྃЍีҡࡨ‫ܒ‬ճՖᔆȄᏑᆓԃԪȂԃӣ
‫ڏ‬т‫ں‬᜞Ֆᆓᘗ஻ᏘȂᔖᙱབ‫ٺ‬ҢSevikar®Ȃ१࡙кଢ଼૕
ᛞ੭બ௉‫ޱ‬Ў‫ڏ‬ᔖӻё‫ݧ‬ཎȄ
5.4 १࡙ߢ༬‫ޑࠅܒ‬ଢ଼૕੽੾௉‫ޱ‬
5.6 ๫ђ૖ϚӒ௉‫ޱ‬
Olmesartan medoxomilȄ௥‫ڧ‬olmesartan medoxomil‫ݽ‬ᕛ‫ޟ‬
ܾཐ‫੾ܒڧ‬௉Ȃҥܻ๫શɯՖᆓԝᕻશɯㄵ‫ھ‬⢄‫ف‬ಛ‫׻ڧ‬
‫ڙ‬Ȃџ૖ю౪๫ђ૖ᡐϽȄᄇܻ๫ђ૖џ૖‫ڧ‬๫શɯՖᆓ
ԝᕻશɯㄵ‫ھ‬⢄‫ف‬ಛࣀ‫ܒ‬ኇ៪‫ޟ‬௉‫(ޱ‬ԃ१࡙᢮Ֆ‫ܒ‬Ж᠚
૾ᆑ௉‫)ޱ‬Ȃ‫ٺ‬ҢՖᆓԝᕻશᙽ඲⋆‫ڙ׻‬Ꮨ‫ڷ‬Ֆᆓԝᕻશ
‫ڧ‬ᡝࡼ‫ת‬Ꮨ‫ݽ‬ᕛȂџ૖അԙЍ‫໌ܖ׍‬՗‫ܒ‬෨Ֆ੿ȂЅ(‫ق‬
َ)ࡨ‫ܒ‬๫૾ᆑЅʝ‫ܖ‬ԫιȄҥܻSevikar®֤Ԥolmesartan
medoxomilԙӋȂӰԪ௉‫݈ޱ‬ҢSevikar®ζџ૖ю౪᜸խІ
ᔖȦ୤َᖝ‫ח‬᛾౩Ᏸ (12.3)ȧȄ
ӵବᄇ൐୏‫ܖ‬ᚖ୏๫ଢ଼૕੭બ௉‫໌ܚޱ‬՗‫ޟ‬ACE‫ڙ׻‬Ꮨၐ
ᡛϛȂෆԤ௉‫ีޱ‬ҡՖ఼Պሖ⃝‫ܖ‬Ֆ‫׍‬શ෨(BUN)ΰЀ‫ޟ‬
௑‫ݷ‬ȄҬࠉ‫ٮ‬ฒၐᡛं‫ـ‬൐୏‫ܖ‬ᚖ୏๫ଢ଼૕੭બ௉‫෈ߝޱ‬
‫ٺ‬Ңolmesartan medoxomil‫ޟ‬ኇ៪ȂծҥܻSevikar®֤Ԥ
olmesartan medoxomilԙӋȂӰԪႱ෈ོ౰ҡ᜸խ‫ޟ‬ኇ៪Ȅ
8 ੫ۡఊတ‫ٺ‬Ң
8.1 ѹஏ
Olmesartan medoxomilȄᛄѹҢ᛾Ϸ઻C(಑1෈)‫ڷ‬D(಑
2ᇄ಑3෈)ȄȦ୤َឌᇭЅ‫ݧ‬ཎ‫ٱ‬໶ (5.1)ȧ
AmlodipineȄᛄѹσჃ‫ڊڷ‬υӵतपʝप‫ڋ‬кौᏢۢҡԙ
෈ငοៀॵശଽᏘ໔10 mg amlodipine/kg/day‫ޟ‬amlodipine
maleate(оmg/m2࣏அྥ඲ᆗȂϷտघ࣏amlodipineΡᡝശ
ଽ࡚ដᏘ໔10 mg‫ޟ‬10‫ڷ‬20ॻ)Ȃ‫ٮ‬ฒᜌᐃᡗҰԤम࿌प
‫ڏܖܒ‬тतपʝप‫ܒࢳڋ‬Ȅ(ΰक़ॎᆗ୅ۡ௉‫ޱ‬ᡝ१࣏60
ϴОȄ)ณՄȂσჃՌҺ଩ࠉ14Ј‫ڗ‬ᐌএҺ଩෈‫ׁڷ‬৒෈
௥‫ࣺڧ‬࿋ܻ10 mg amlodipine/kg/dayᏘ໔‫ޟ‬amlodipine maleateȂ
ี౪ؐᆐрपኵᡗ๿෵Ѝ(घ50%)Ȃиυ৞ϱԫιኵᡗ๿
ቨё(घ5ॻ)ȄᏘ໔10 mg‫ޟ‬amlodipine maleateȂོ‫ߝ۽‬σ
Ⴣ‫ׁޟ‬৒෈‫ڷ‬ҡ౰ਢ໢ȄҬࠉ‫ٮ‬Ґବᄇѹஏ໌՗ٗஊ‫يޟ‬
ԁᄇྱၐᡛȄѹஏषौ‫ٺ‬ҢamlodipineȂዖӵցઉ҆໸σ
ܻᄇप‫ޟڋ‬ዖӵॳᓎȄ
8.3 ঳ٰஏτ
AmlodipineȄҥܻamlodipineкौငҥ‫م‬᠚фᗂȂՄ१࡙
‫م‬ђ૖ϚӒ௉‫ޟޱ‬Ֆዎ఼ଶј૾෈(t1/2)࣏56ωਢȂӰԪ
ᄇ೻᜸௉‫ٺޱ‬ҢSevikar®ਢᔖᙱབȄ
Ҭࠉ‫ٮ‬ϚጂۡSevikar®‫ޟ‬amlodipine‫ܖ‬olmesartan medoxomil
ԙӋ࢐֏ོ໌ΣΡ᜸ٰҘȂծϐ‫ٰݪޣ‬σჃ‫ٰޟ‬Ҙϛོю
౪ճᐨ࡙olmesartanȄҥܻԪ᛾‫ސ‬џ૖Ᏺम௥‫ڧ‬঳ٰ‫ޟ‬ᔉ‫ڋ‬
౰ҡϚ‫ي‬ІᔖȂᔖՃኌ᛾‫ސ‬ᄇҔᒑ‫ޟ‬१ौ‫ܒ‬Ȃ‫֏࢐ؚۡ‬ୄ
Х঳ٰ‫ܖ‬ୄҢ᛾‫ސ‬Ȅ
5.8 ᚂᏰᔮᡛ
8.4 ‫ڋ‬ऋ௉‫ޱ‬
Sevikar®ȄҏፒП᛾ࠢ६ճՖऔશ‫ڷ‬Ֆ౨Шৠᑖ‫ޟ‬ਝ‫ݎ‬σ
ܻ‫ڏ‬এտԙӋȇ‫ڏ‬тᔮᡛ๖‫ݎ‬ᡐϽࠌ೽லџᘪӰܻ൐П
ԙӋȄ
AmlodipineȄӵΰѿࡣငᡛϛȂෆൢ֙ีҡ‫م‬᠚ሕશЀଽ
‫ޟ‬௑‫(ל‬6.2)Ȅ
Olmesartan medoxomilȄӵΰѿࡣငᡛϛȂෆൢ֙ีҡՖ
ϛՊሖ⃝঄ЀଽЅଽՖ႕௑‫ל‬Ȅ
Sevikar®ᄇ‫ڋ‬ऋ௉‫ޟޱ‬ԊӒ‫ڷܒ‬ਝ‫ۦݎ‬ҐጂҳȄ
AmlodipineȄAmlodipineᄇ6ྑоή௉‫ޱ‬Ֆᔆ‫ޟ‬ኇ៪Ϛ݂Ȅ
Olmesartan medoxomilȄOlmesartan medoxomilᄇ‫ڋ‬ऋ௉
‫ޟޱ‬ԊӒ‫ڷܒ‬ਝ‫ۦݎ‬ҐጂҳȄ
5.7 ‫م‬ђ૖ϚӒ௉‫ޱ‬
6 Ϛ‫ي‬Іᔖ
6.1 ᖝ‫ח‬ၐᡛငᡛ
ҥܻӨᖝ‫ח‬ၐᡛ‫ޟ‬धශ৯౴ྃσȂၐᡛுю‫࢚ޟ‬᛾‫ސ‬Ϛ‫ي‬
Іᔖีҡ౥ȂϚ૖‫ޢ‬௥‫ڷ‬ၐᡛϛѪΙᆍ᛾‫ސ‬Ϛ‫ي‬Іᔖีҡ
౥ࣺШၶȂՄиζϚΙۡІࢎᄂሬ௑‫ݷ‬Ȅ
Sevikar®
оήၥਟᡗҰԤ຺ႆ1600Ρෆ‫ٺ‬ҢSevikar®Ȃ‫ڏ‬ϛ1000Ρ
оΰ‫ٺ‬Ң၎᛾‫ސ‬ՍЍ6এТȂ700Ρоΰ௥ញ1ԑȄΙ໶Ԋ
ኑᏘᄇྱӰυၐᡛෆं‫ـ‬Sevikar®(୤َ14.1࿽)Ȃၐᡛఊ
တҁ֯ԑឭ54ྑȂघ55%࣏‫ܒظ‬Ȃ71%࣏ҩᆍΡȂ25%࢐
༃ΡȄ௉‫ޱ‬௥‫ޟڧ‬Ꮨ໔ጒ൜ҥ5/20 mg‫ڗ‬10/40 mgȂؐЈ
ο݈ΙԩȄ
‫ٺ‬ҢSevikar®‫ݽ‬ᕛ‫ޟ‬Ϛ‫ي‬Іᔖᐌᡝีҡ౥Ȃࣺ࿋ܻӣᏘ໔
Sevikar®এտԙӋЅԊኑᏘ‫ޟ‬Ϛ‫ي‬Іᔖีҡ౥Ȅ‫ܚ‬ӱൢ‫ޟ‬
Ϛ‫ي‬ІᔖΙૡ࣏֯ሆ࡙Ȃ࡞ЍᏲमୄХ‫ݽ‬ᕛ(Sevikar®ಢ
2.6%ȂԊኑᏘಢ6.8%)Ȅ
Ыရ
Ыရ࢐amlodipine‫ޟ‬ϐ‫ޣ‬୙հҢȂ‫ڎ‬Ꮨ໔ࣺᜰ‫ܒ‬Ȃծ‫ߨٮ‬
olmesartan medoxomil‫ޟ‬୙հҢȄ
ӵ8໊‫ޟ‬ᓍᐠȃᚖ‫ݽޡ‬ᕛ෈໢ȂԚଶԊኑᏘಢࡣȂо10 mg
‫ޟ‬amlodipine൐П‫ݽ‬ᕛ‫ޟ‬Ыရีҡ౥ശଽȄष஠20 mg‫ܖ‬
40 mg‫ޟ‬olmesartan medoxomilᇄ10 mg‫ޟ‬amlodipine‫ځ‬ҢȂ
ีҡ౥߯ᡗ๿६ճȄ
ᚖ‫ݽޡ‬ᕛ෈໢ԚଶԊኑᏘಢ‫ޟ‬Ыရีҡ౥
Amlodipine
ԊኑᏘ
5 mg
10 mg
*12.3%=ᄂሬԊኑᏘีҡ౥
Olmesartan Medoxomil
20 mg
ԊኑᏘ
40 mg
(-2.4%)
0%*
6.2%
5.7%
0.7%
6.2%
13.3%
24.5%
11.2%
8.5 Ղԑ௉‫ޱ‬
Sevikar®ᚖ‫ޡ‬ᖝ‫ח‬ၐᡛ‫ޟ‬ᖂ‫ڧ‬ၐΡኵϛȂԤ20% (384/1940)
ԑᅖ65ྑ‫ܖ‬оΰȂ3% (62/1940) ԑᅖ75ྑ‫ܖ‬оΰȄӵԑᅖ
65ྑᇄҐᅖ65ྑ‫ڧޟ‬ၐ‫ޱ‬໢Ȃ‫ٮ‬Ґี౪ԊӒ‫ܖܒ‬ਝ‫ݎ‬ΰ‫ޟ‬
ᐌᡝ৯౴Ȅ
AmlodipineȄӵᖝ‫ח‬ൢ֙‫ٱ‬ӇϛҐี౪Ղԑ‫ڷ‬ԑሆ௉‫ޱ‬ӵ
᛾‫ސ‬ІᔖΰԤ‫ܚ‬৯౴ȄΙૡՄِȂᔖᙱབ‫ؚۡ‬Ղԑ௉‫ޟޱ‬
Ꮨ໔ȂᠧܻԪఊတ௉‫ޱ‬ၶலีҡ‫م‬ȃ๫‫ܖ‬Ж᠚ђ૖६ճȂ
Ѕีҡ‫ܖ੿ีځ‬ӫ‫ڏځ‬т᛾‫ݽސ‬ᕛȂ೽ல௃Ꮨ໔ጒ൜ή३
໠ۖࢊҢȄՂԑ௉‫ޱ‬ᄇamlodipine‫఼ޟ‬ଶ౥ၶճȂᏲम
AUCቨёघ40%‫ڗ‬60%ȂӰԪଔۖᏘ໔џ૖҆໸ၶճȄ
Olmesartan medoxomilȄᖝ‫ח‬ၐᡛϛȂ݈Ңolmesartan
medoxomil‫ޟ‬ଽՖᔆ௉‫ޱ‬ᖂΡኵϛȂ20%оΰ‫ޟ‬௉‫ޱ‬ԑᅖ
65ྑ‫ܖ‬оΰȂՄ5%оΰԑᅖ75ྑ‫ܖ‬оΰȄՂԑ‫ڷ‬ԑሆ௉
‫ޱ‬໢‫ٮ‬Ґี౪ਝ‫ܖݎ‬ԊӒ‫ܒ‬ΰ‫ޟ‬ᐌᡝ৯౴Ȅӵ‫ڏ‬тᖝ‫ח‬
ൢ֙‫ٱ‬ӇϛζҐี౪Ղԑ‫ڷ‬ԑሆ௉‫ޱ‬ӵ᛾‫ސ‬ІᔖΰԤ৯
౴Ȃծฒ‫௶ݲ‬ଶഋϷՂԑΡఃཐ‫ܒ‬ၶଽȄ
8.6 ‫م‬ђ૖ϚӒ௉‫ޱ‬
Ҭࠉ‫ٮ‬ฒၐᡛं‫ـ‬Sevikar®ᄇ‫م‬ђ૖ϚӒ௉‫ޟޱ‬ኇ៪Ȃծ
ϐԤၥਟᡗҰȂamlodipine‫ڷ‬olmesartan medoxomilӵ‫م‬ђ
૖ϚӒ௉‫ޱ‬ϛᐨོ࡙ϛ࡙ቨёȂ१࡙‫م‬ђ૖ϚӒ௉‫ޱ‬໸
ωЖ‫ٺ‬ҢSevikar®Ȅ
8.7 ๫ђ૖ϚӒ௉‫ޱ‬
Ҭࠉ‫ٮ‬ฒၐᡛं‫ـ‬Sevikar®ᄇ๫ђ૖ϚӒ௉‫ޟޱ‬ኇ៪Ȅ
AmlodipineȄ๫ђ૖ϚӒ‫ٮ‬Ϛོᡗ๿ኇ៪amlodipine‫ޟ‬᛾
‫ސ‬ଢ଼ΨᏰȂӰԪ๫૾ᆑ௉‫ޱ‬џ௃ΙૡଔۖᏘ໔໠݈ۖҢȄ
Olmesartan medoxomilȄ๫ђ૖ϚӒ௉‫ޟޱ‬Ֆ఼olmesartan
ᐨ࡙Ш๫ђ૖ғல‫ޱ‬ଽȄ१᙭๝᛾ࡣȂ१࡙๫ђ૖ϚӒ
௉‫(ޱ‬Պሖ⃝఼ଶ౥ɴ20 mL/min)‫ޟ‬AUCघЀଽ3ॻȄᄇܻ
ϛ࡙Սᡗ๿๫ђ૖ϚӒ௉‫(ޱ‬Պሖ⃝఼ଶ౥ɴ40 mL/min)
࡚ដϚሯ፡ᐌଔۖᏘ໔Ȅ
8.8 ༃Ρ௉‫ޱ‬
ӵSevikar®ᚖ‫ޡ‬ᖝ‫ח‬ၐᡛ‫ޟ‬ᖂ‫ڧ‬ၐΡኵϛȂԤ25%(481/1940)
10 ᛾‫ސ‬ႆ໔
Ҭࠉ‫ٮ‬ฒᜰܻΡᡝ‫ٺ‬ҢSevikar®ႆ໔‫ޟ‬ၥଉȄ
AmlodipineȄωჃ‫ڷ‬σჃϷտ݈ҢᏘ໔ࣺ࿋ܻ40 mg
amlodipine/kgЅ100 mg amlodipine/kg‫ޟ‬൐ԩο݈amlodipine
maleateོमԫȄгହ݈Ңࣺ࿋ܻ4 mg amlodipine/kgоΰ
Ꮨ໔‫ޟ‬൐ԩο݈amlodipine maleate(оmg/m2࣏அྥ඲ᆗȂ
ࣺ࿋ܻΡᡝശଽ࡚ដᏘ໔‫ޟ‬11ॻоΰ)ȂོЕଔᡗ๿‫ںޟ‬
᜞Ֆᆓᘗ஻‫ڷ‬ճՖᔆȄ
᛾‫ސ‬ႆ໔џႱ෈ོЕଔ‫ں‬᜞Ֆᆓႆ࡙ᘗ஻բᓍᡗ๿ճՖ
ᔆȂ‫ٮ‬џ૖ԤІৢ‫ܒ‬ЖཀྵႆഀȄծΡ᜸‫ړ‬ཎႆ໔݈Ң
amlodipine‫ޟ‬ငᡛԤ३Ȅ
ԃ‫ݎ‬ႆ໔݈Ң᛾‫ސ‬ȂᔖᑖྃᅿกЖ᠚‫֜ڳڷ‬Ȃ‫ٮ‬໸ᓜᖅ
ก໔ՖᔆȄΙҍีҡճՖᔆȂᔖᄂࢊЖՖᆓЛࡻ‫ݽܒ‬ᕛȂ
ѓࢂܷଽѲ޴Ѕᎌ࿋ᒯశȄԃ‫ݎ‬೻᜸߳Ԉ‫ܒ‬௩ࢊϫฒ‫ݲ‬
‫׽‬๡ճՖᔆȂᔖՃኌ‫׹‬ϠЀᔆᏘ(ԃphenylephrine)Ȃ‫ݧٮ‬
ཎඉᕗৠᑖ‫׍ڷ‬ᒯю໔Ȅᓗ૕‫ိৢݧ‬ຉᑥሖ໗џଛᙽߢ
ᘞ໗ᚔυ໌Σ‫ޟ‬ਝᔖȄҥܻamlodipine‫ޟ‬ೖҩ፴ᗤ๖౥
ଽȂӰԪՖశആ‫ݙ‬ᔓօϚσȄ
Olmesartan medoxomilȄҬࠉᜰܻΡᡝ᛾‫ސ‬ႆ໔‫ޟ‬ၥਟ
Ԥ३Ȅ᛾‫ސ‬ႆ໔ശџ૖‫ޟ‬኉‫࢐ޑ‬ճՖᔆ‫ڷ‬Жཀྵႆഀȇԃ
‫ีݎ‬ҡ୙Һཐડင(ଜٖડင)‫ږ‬ᐭȂࠌџ૖ีҡЖཀྵႆ
ጥȄΙҍีҡԤ੿‫ޟޑ‬ճՖᔆȂᔖ໠ۖЛࡻ‫ݽܒ‬ᕛȄҬ
ࠉ‫ۦ‬ϚጂۡOlmesartan‫ޟ‬џആ‫ܒݙ‬Ȅ
11 ੫‫ܒ‬ᇳ݂
Sevikar®࢐໗ᚔυ೽ၾ‫ڧ‬ᡝߢᘞᏘ(CCB) amlodipine besylate
‫ڷ‬ՖᆓԝᕻશII‫ڧ‬ᡝߢᘞᏘ(ARB) olmesartan medoxomil‫ޟ‬ፒ
П᛾‫ސ‬Ȅ
Sevikar®ϛamlodipine besylateԙӋ‫ޟ‬ϽᏰԒ࣏3-ethyl-5-methyl
(±)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6methyl-3,5-pyridinedicarboxylate, monobenzenesulphonateȄ
ϷυԒ࣏C20H25ClN2O5ȆC6H6O3SȄ
Olmesartan medoxomil࢐Ιᆍࠉ៮᛾‫ސ‬Ȃӵဗथၾ֜ԝႆแ
ϛོЫ၌ԙolmesartanȄ
Sevikar®ϛolmesartan medoxomilԙӋ‫ޟ‬ϽᏰԒ࣏2,3-dihydroxy2-butenyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[p-( o-1 Htetrazol-5-ylphenyl) benzyl] imidazole-5-carboxylate, cyclic 2,3carbonateȄϷυԒ࣏C29H30N6O6Ȅ
amlodipine besylate‫ޟ‬๖ᄺԒ࣏Ȉ
olmesartan medoxomil‫ޟ‬๖ᄺԒ࣏Ȉ
Sevikar®ϛ֤Ԥamlodipine besylate(ҩ‫ܖ‬ԸҩՓ๖ව઱ґ)
Ѕolmesartan medoxomil(ҩՍష༁ҩՓ઱ґ‫ܖ‬๖ව઱ґ)Ȅ
Amlodipine besylate‫ڷ‬olmesartan medoxomil‫ޟ‬Ϸυ໔Ϸտ࢐
567.1‫ڷ‬558.59ȄAmlodipine besylateሆཌྙܻЫȂྃཌྙܻ
Κ᎕ȂՄOlmesartan medoxomilࠌඁнϚྙܻЫȂྃཌྙܻ
Ҧ᎕Ȅ
12 ᖝ‫ח‬᛾౩Ᏸ
12.1 հҢᐠ‫ڙ‬
Sevikar ® ȄSevikar ® ࢐‫ڍ‬ᆍ६Ֆᔆ᛾‫ޟސ‬ፒПȈΙᆍ࢐
dihydropyridine໗ࡼ‫ת‬Ꮨ(໗ᚔυࡼ‫ת‬Ꮨ‫ܖ‬ᄚഀ೽ၾߢᘞᏘ)
amlodipine besylateȂЅΙᆍ࢐ՖᆓԝᕻશII‫ڧ‬ᡝߢᘞᏘ
olmesartan medoxomilȄSevikar®‫ޟ‬amlodipineԙӋ‫ڙ׻‬໗ᚔ
υ ऎ ູ ಠ फ ጰ ໌ Σ Ֆ ᆓ ҁ ྤ Պ ‫ ڷ‬Ж Պ Ȃ Մ S e v i k a r ®‫ޟ‬
olmesartan medoxomilԙӋࠌߢᘞՖᆓԝᕻશII‫ޟ‬Ֆᆓԝᕻ
հҢȄ
AmlodipineȄᄂᡛኵᐃᡗҰamlodipineџᗤ๖ܻdihydropyridine
‫ߨڷ‬hydropyridine‫ޟ‬ᗤ๖՝ညȄЖՊ‫ڷ‬ՖᆓҁྤՊಠफѴ໗
ᚔυငҥ੫ۡᚔυ೽ၾಋΣ೻‫ٲ‬ಠफȂོኇ៪ЖՊ‫ڷ‬Ֆᆓ
ҁྤՊ‫ޟ‬ԝᕻႆแȄAmlodipineོᒵᐅ‫ڙ׻ܒ‬໗ᚔυऎູಠ
फጰȂᄇՖᆓҁྤՊಠफ‫ޟ‬հҢσܻЖՊಠफȄᡝѴၐᡛี
౪Ԫ᛾‫ސ‬џ૖෵৵Ж᠚ԝᕻ૖ΨȂծӵଢ଼‫ࣀސ‬ᡝ௥‫ڧ‬ᕛਝᏘ
໔‫ޟ‬ၐᡛϛࠌҐี౪ԪਝᔖȄAmlodipineϚኇ៪Ֆ఼໗ᐨ࡙Ȅ
ӵҡ౩pHጒ൜ϱȂamlodipine࣏ᚔυϽ‫ޟ‬Ͻӫ‫(ސ‬pKa=8.6)Ȃ
ᇄ໗೽ၾ‫ڧ‬ᡝ‫ޟ‬ଢ଼ΨҺϣհҢ੫‫ܒ‬Ȃӵܻᇄ‫ڧ‬ᡝᗤ๖ഋ՝ം
ᅚ๖ӫ‫ܖ‬၌ᚔȂоጥᄚีථ᛾ਝȄ
Amlodipine࢐‫ں‬᜞ଢ଼૕Ֆᆓᘗ஻ᏘȂ‫ޢ‬௥հҢܻՖᆓҁྤՊȂ
ོ६ճ‫ں‬᜞ՖᆓߢΨȂ௃Մ६ճՖᔆȄ
Olmesartan medoxomilȄՖᆓԝᕻશII࢐ҥՖᆓԝᕻશI‫ל‬
ԙȂԪІᔖҥՖᆓԝᕻશᙽ඲ (ACEȂkininase II)་ϽȄ
ՖᆓԝᕻશII࢐๫શɯՖᆓԝᕻશ‫ف‬ಛϛкौ‫ޟ‬ЀᔆᏘȂհ
ҢѓࢂՖᆓԝᕻȃ‫ږ‬ᐭㄵ‫ھ‬⢄ӫԙ‫ڷ‬ភܹȃ‫ږ‬ᐭЖ᠚ȂЅ
๫᠚ᄇ໘‫ޟ‬Ӕ֜ԝȄOlmesartanџᒵᐅ‫ߢܒ‬ᘞՖᆓԝᕻશII
ᗤ๖ܻՖᆓҁྤՊϛ‫ޟ‬AT1‫ڧ‬ᡝȂ௃Մߢᘞ‫ڏ‬Ֆᆓԝᕻհ
ҢȄӰԪȂԪ᛾‫ޟސ‬հҢϚ‫ڧ‬ՖᆓԝᕻશII‫ޟ‬ӫԙၯ৷‫ܚ‬ኇ
៪Ȅ
ӵ೨ӻಢᙑϛζџี౪AT2‫ڧ‬ᡝȂծҬࠉ‫ٮ‬ϚጂۡԪ‫ڧ‬ᡝ࢐
֏ᇄЖՖᆓ‫ޟ‬ᡝϱҁᒋԤᜰȄOlmesartanᄇAT1‫ڧ‬ᡝ‫ޟ‬ᒑ‫ڷ‬
Ψ࢐ᄇAT2‫ڧ‬ᡝ‫ޟ‬12,500ॻоΰȄ
оACE‫ڙ׻‬Ꮨߢᘞ๫શɯՖᆓԝᕻશ‫ف‬ಛȂ։‫ڙ׻‬ҥՖᆓԝ
ᕻશIӫԙՖᆓԝᕻશIIȂ࢐೨ӻ६Ֆᔆ᛾‫௴ܚސ‬Ң‫ޟ‬ᐠᙽȄ
ACE‫ڙ׻‬Ꮨζ‫ڙ׻‬bradykininϷ၌Ȃ೻໶Ϸ၌ІᔖһҥACE
་ϽȄҥܻolmesartanϚོ‫ڙ׻‬ACE(kininase II)ȂӰԪϚོ
ኇ៪ᄇbradykinin‫ޟ‬ІᔖȂϚႆҬࠉ‫ۦ‬Ϛጂۡ೻໶৯౴࢐֏
‫ڎ‬Ԥᖝ‫ח‬१ौ‫ܒ‬Ȅ
ߢᘞՖᆓԝᕻશII‫ڧ‬ᡝོ‫ڙ׻‬ՖᆓԝᕻશIIᄇ๫શϷ‫॒ޟݪ‬
өᆓ‫ڙ‬ӱ㔳Ȃ໌ՄᏲमՖዎ๫શࣀ‫ܒ‬ЅඉᕗՖᆓԝᕻશII
ᐨ࡙ΰЀȂϚႆ೻ᘈ‫ٮ‬Ϛኇ៪olmesartan௡‫ڙ‬Ֆᔆ‫ޟ‬ਝ‫ݎ‬Ȅ
12.2 ᛾ਝᏰ
AmlodipineȄଽՖᔆ௉‫ޱ‬௥‫ڧ‬ᕛਝᏘ໔‫ݽ‬ᕛࡣȂamlodipine
‫ޟ‬Ֆᆓᘗ஻ਝ‫ོݎ‬Ᏺम޼࠼‫ڷ‬મ࠼Ֆᔆή६Ȃծ೻ᘈ‫ٮ‬Ϛོ
അԙߝ෈Ң᛾ࡣЖ౥‫ܖ‬Ֆዎ‫ڋ‬૯⍇ᐨ࡙ю౪ᡗ๿ᡐϽȄ
ߝ෈ؐЈΙԩο݈Ң᛾Ȃ६Ֆᔆਝ‫ݎ‬џᆰࡻՍЍ24ωਢȄ
ӵԑሆ‫ڷ‬Ղԑ௉‫ޱ‬ϛȂՖዎᐨ࡙഍ོኇ៪᛾ਝȄAmlodipine
६Ֆᔆ‫ޟ‬ൽ࡙ζ‫ݽڷ‬ᕛࠉՖᔆЀଽแ࡙ԤᜰȇӰԪȂϛ࡙
ଽՖᔆ௉‫(ޱ‬๲஻ᔆ105-114 mmHg)‫ޟ‬ІᔖོШሆ࡙ଽՖᔆ
௉‫(ޱ‬๲஻ᔆ90-104 mmHg)ଽघ50%ȄՖᔆғல‫ڧޟ‬ၐ‫ٮޱ‬
Ґю౪ᖝ‫ח‬ΰᡗ๿‫ޟ‬ՖᔆᡐϽ(+1/-2 mmHg)Ȅ
ᄇܻ๫ђ૖ғல‫ޟ‬ଽՖᔆ௉‫ޱ‬Ȃamlodipine‫ޟ‬ᕛਝᏘ໔ོ
६ճ๫ՖᆓߢΨȂඪЀ๫๛౨ᘮႆ౥‫ڷ‬Ԥਝ๫Ֆዎࢺ໔Ȃ
ծϚོഅԙႆᘮϷ౥‫ܖ‬ೖҩ‫׍‬ᡐϽȄ
‫ ڏ ڷ‬т ໗ ೽ ၾ ߢ ᘞ ᏘΙኺȂЖࡉђ૖ғல‫ޟ‬௉‫ޱ‬௥‫ڧ‬
amlodipine‫ݽ‬ᕛࡣȂӄ਀‫ڷ‬ၼଢ଼(‫ܖ‬࿽ࡡ፡ᐌ)ਢЖ᠚ђ૖‫ޟ‬
Ֆశଢ଼Ψก໔঄ȂΙૡՄِӵЖࡾኵΰོю౪ཌൽΰЀȂ
ᄇܻdP/dt‫ܖ‬ѾЖࡉґ෈๲஻ᔆ‫ܖ‬ৠᑖࠌฒᡗ๿ኇ៪ȄӵՖ
శଢ଼ΨᏰं‫ـ‬ϛȂࣀᡝଢ଼‫ڷސ‬Ρᡝ௥‫ڧ‬ᕛਝᏘ໔ጒ൜ϱ‫ޟ‬
amlodipineȂ‫ٮ‬Ϛོ෵ճЖ᠚ԝᕻ૖ΨȂ։‫ٺ‬ӵΡᡝϱ‫ځ‬Ң
Κ࠮ҺཐડငߢᘞᏘȂζҐี౪ԪਝᔖȄณՄȂΙૡ‫ܖ‬ф
ᓻ‫ي‬ԁ‫ޟ‬Ж᠚૾ᆑ௉‫ٺޱ‬Ңџᡗ๿෵ճЖ᠚ԝᕻ૖Ψ‫ޟ‬᛾
‫ސ‬Ȃζෆю౪᜸խ௑‫ל‬Ȅ
AmlodipineϚོ‫׽‬ᡐࣀᡝଢ଼‫ܖސ‬Ρᡝ‫ޟ‬ᝮ‫ܘ‬๖ђ૖‫ࡉܘܖ‬
๖༈ᏲȄӵଽՖᔆ‫ܖ‬Ж๕ฮ௉‫ځޱ‬ҢAmlodipineᇄΚ࠮Һཐ
ડငߢᘞᏘ‫ޟ‬ᖝ‫ח‬ၐᡛϛȂҐี౪ᄇЖႫყ୤ኵ౰ҡϚ‫ي‬
ኇ៪Ȅ
Olmesartan medoxomilȄ2.5 mg‫ڗ‬40 mg‫ޟ‬olmesartan
medoxomilོ‫ڙ׻‬ՖᆓԝᕻશI‫ݧ‬Σࡣ‫ޟ‬Ѐᔆਝ‫ݎ‬Ȅ‫ڙ׻‬հҢ
‫៉ࡻޟ‬ਢ໢ᇄᏘ໔ԤᜰȂolmesartan medoxomilᏘ໔ɵ40 mgȂ
џӵ24ωਢีථɵ90%‫ڙ׻ޟ‬ਝ‫ݎ‬Ȅ
୊ ஶ ‫ ڧ‬ၐ ‫ ڷ ޱ‬ଽ Ֆ ᔆ௉‫ޱ‬൐ԩ‫ڷ‬१᙭݈Ң olmesartan
medoxomilࡣȂՖᆓԝᕻશI‫ڷ‬ՖᆓԝᕻશII‫ޟ‬Ֆዎᐨ࡙ЅՖ
ዎ๫શࣀ‫(ܒ‬PRA)ΰЀȄ१᙭݈Ңശଽ80 mg‫ޟ‬olmesartan
medoxomilȂᄇㄵ‫ھ‬⢄঄‫ޟ‬ኇ៪ྃωȂᄇՖ఼႕ࠌฒኇ៪Ȅ
12.3 ᛾‫ސ‬ଢ଼ΨᏰ
Sevikar®ϛamlodipine‫ڷ‬olmesartan medoxomil‫ޟ‬᛾‫ސ‬ଢ଼ΨᏰȂ
᜸խamlodipine‫ڷ‬olmesartan medoxomilϷ໠‫׹‬Ϡਢ‫ޟ‬᛾‫ސ‬ଢ଼
ΨᏰȄ‫ڍ‬ᆍԙӋ‫ޟ‬ҡᡝџҢ౥഍ሉճܻ100%Ȃծ‫ڍ‬ᆍԙӋ
֯Ϛ‫ސॵڧ‬ኇ៪ȄஅܻAmlodipine(45 ± 11ωਢ)‫ڷ‬olmesartan
(7 ± 1ωਢ)‫ޟ‬Ԥਝј૾෈ȂؐЈ݈᛾Ιԩamlodipineོಣᑖ
2‫ڗ‬3ॻȂՄolmesartan‫ޟ‬ಣᑖ໔ࠌџ‫܇‬౱Ȅ
AmlodipineȄο݈‫׹‬ϠamlodipineᕛਝᏘ໔ࡣȂငҥ֜ԝȂ
Ֆዎᐨ࡙৫঄ོю౪݈᛾ࡣ6Ս12ωਢ໢Ȅ๘ᄇҡᡝџҢ౥
եॎӵ64%‫ڗ‬90%Ϟ໢Ȅ
Olmesartan medoxomilȄOlmesartan medoxomilӵҥथဗ
ၾ֜ԝ‫ޟ‬ႆแϛȂོ‫פ‬ഀ⢅၌ԙolmesartanՄ‫ׇ‬ӒࣀϽȄ
Olmesartan medoxomil‫ޟ‬๘ᄇҡᡝցҢ౥घ࣏26%Ȅο݈‫׹‬
Ϡࡣܻ1‫ڗ‬2ωਢႀ‫ڗ‬olmesartanശσՖዎᐨ࡙(Cmax)Ȅॵ‫ސ‬
Ϛኇ៪olmesartan medoxomil‫ޟ‬ҡᡝџҢ౥Ȅ
Ϸշ
AmlodipineȄࣀᡝѴၐᡛᡗҰӵଽՖᔆ௉‫ޱ‬ᡝϱȂ໌Σඉ
ᕗ‫ޟ‬᛾‫ސ‬घԤ93%џᇄՖዎೖҩ፴ᗤ๖ȄؐЈΙԩ೿៉๝
᛾7Ս8ЈࡣȂџႀ‫ڗ‬amlodipine‫ޟ‬ᛧۡᄘՖዎᐨ࡙Ȅ
Olmesartan medoxomilȄOlmesartan‫ޟ‬Ϸշৠᑖघ࣏17 LȄ
OlmesartanџᇄՖዎೖҩ፴ଽ࡙ᗤ๖(99%) иϚऎആऔՖ౨Ȅ
ӵolmesartanՖዎᐨ࡙ሉଽܻ࡚ដᏘ໔ႀ‫ޟڗ‬ጒ൜ਢȂೖҩ
፴ᗤ๖౥ϫ߳ࡻ࡯ۡȄ
ӵσჃᡝϱȂolmesartanྃЍऎູՖသࡎራȂོ೽ႆपዺࡎ
ራ༈Սप‫ڋ‬ȂӵσჃٰҘϛζོю౪ճᐨ࡙olmesartanȄ
фᗂᇄ௶‫ݵ‬
AmlodipineȄAmlodipineкौ(घ90%)ငҥ‫م‬᠚фᗂᙽϽ࣏
ฒࣀ‫ܒ‬фᗂ‫ސ‬Ȅ௃Ֆዎϛ‫఼ޟ‬ଶ࣏ᚖࣺ‫ܒ‬Ȃശತ௶ଶј૾
෈घ࣏30‫ڗ‬50ωਢȄ10%‫ޟ‬ҔϽӫ‫ڷސ‬60%‫ޟ‬фᗂ‫ݵ௶ސ‬
ܻ‫׍‬శϛȄ
Olmesartan medoxomilȄOlmesartan medoxomilӵ֜ԝႆแ
ϛོ‫פ‬ഀ‫ׇ‬ӒᙽϽ࣏olmesartanȂՄolmesartanඁнϚོӔ
໌Ι؏фᗂȄOlmesartan‫ޟ‬Ֆዎᖂ఼ଶ౥࣏1.3 L/hȂ๫᠚఼
ଶ౥࣏0.6 L/hȄघ35%Ս50%‫֜ޟ‬ԝᏘ໔ོ໌Σ‫׍‬శȂ‫ڏ‬
ᎷࠌငҥᖚҘ௶‫ݵ‬Սᕶ߯ϛȄ
Olmesartanխн࢐оᚖࣺ‫ޟܒ‬ПԒ఼ଶȂശತ௶ଶј૾෈घ
࣏13ωਢȄ൐ԩο݈Ս320 mg‫ޟ‬olmesartan‫ڷ‬ӻԩο݈Ս
80 mg‫ޟ‬olmesartanࡣȂ᛾‫ސ‬ଢ଼ΨᏰ֕ጣ‫ܒ‬ȄؐЈΙԩ๝᛾
3Ս5ЈϱȂolmesartan߯џႀᛧۡᄘᐨ࡙ȂиؐЈΙԩ‫ޟ‬
Ꮨ໔ϚོഅԙՖዎϛ᛾‫ސ‬ಣᑖȄ
ՂԑΡ
Sevikar®ᄇՂԑΡ‫ޟ‬᛾‫ސ‬ଢ଼ΨᏰ੫‫ܒ‬ᇄএտԙӋ‫ޟ‬᛾‫ސ‬ଢ଼Ψ
ᏰࣺխȄ
AmlodipineȄՂԑ௉‫ޱ‬ᄇamlodipine‫఼ޟ‬ଶ౥ၶճȂᏲम
AUCቨёघ40%‫ڗ‬60%ȂӰԪଔۖᏘ໔҆໸ၶճȄ
Olmesartan medoxomilȄҬࠉϐԤၐᡛं‫ـ‬olmesartan
medoxomilӵՂԑΡ(65ྑоΰ)‫ޟ‬᛾‫ސ‬ଢ଼ΨᏰȄᐌᡝՄِȂ
ԑሆΡ‫ڷ‬ՂԑΡ‫ޟ‬olmesartanശσՖዎᐨ࡙ࣺխȄՂԑΡ१
᙭๝᛾ࡣю౪Ѝ೨‫ޟ‬olmesartanಣᑖȇՂԑ௉‫ ޟޱ‬AUCss,τ
Ѐଽ33%ȂՄCLRࠌघ६ճ30%Ȅ
‫็ڋ‬
AmlodipineȄ62՝6Ս17ྑ‫ޟ‬ଽՖᔆ௉‫ޱ‬௥‫ڧ‬1.25 mgՍ20
mg‫ޟ‬amlodipineȄਲ਼ᐃᡝ१፡ᐌࡣ‫఼ޟ‬ଶ౥ЅϷշᡝᑖᇄԙ
Ρ‫ޟ‬ኵ঄ࣺխȄ
Olmesartan medoxomilȄҬࠉ‫ٮ‬ฒၐᡛं‫ـ‬olmesartan
medoxomilӵҐᅖ18ྑ௉‫ޟޱ‬᛾‫ސ‬ଢ଼ΨᏰȄ
‫ܒ‬տ
တᡝ᛾‫ސ‬ଢ଼ΨᏰϷ‫ݙ‬ᡗҰȂτ‫ܒ‬௉‫ޟޱ‬olmesartan఼ଶ౥घ
Ш‫ܒظ‬ճ15%Ȅ‫ܒ‬տᄇamlodipine‫఼ޟ‬ଶ౥‫ؠ‬Ԥኇ៪Ȅ
Olmesartan medoxomilȄ‫ظ‬ȃτ௉‫ޟޱ‬olmesartan medoxomil
᛾ଢ଼ᏰѫԤ‫ٲ‬ཌ৯౴Ȅτ‫ޟܒ‬AUC‫ڷ‬CmaxШ‫ܒظ‬ଽ10%‫ڗ‬
15%Ȅ
๫ђ૖ϚӒ
AmlodipineȄ๫ђ૖ϚӒҐᡗ๿ኇ៪Amlodipine‫ޟ‬᛾‫ސ‬ଢ଼Ψ
ᏰȂӰԪ๫᠚૾ᆑ௉‫ޱ‬џ௥‫ڧ‬ΙૡଔۖᏘ໔Ȅ
Olmesartan medoxomilȄ๫ђ૖ϚӒ௉‫ޟޱ‬olmesartanՖ఼
ᐨ࡙Ȃଽܻ๫ђ૖ғல‫ޱ‬Ȅ१᙭๝᛾ࡣȂ१࡙๫ђ૖ϚӒ
௉‫(ޱ‬Պሖ⃝఼ଶ౥ɴ20 mL/min)‫ޟ‬AUCघЀଽ3ॻȄҬࠉ
‫ۦ‬ฒၐᡛं‫ـ‬Ֆశആ‫ݙ‬௉‫ޟޱ‬olmesartan medoxomil᛾‫ސ‬ଢ଼
ΨᏰȄ
‫م‬ђ૖ϚӒ
AmlodipineȄ‫م‬ђ૖ϚӒ௉‫ޟޱ‬amlodipine఼ଶ౥ή६ȂᏲ
मAUCቨёघ40%‫ڗ‬60%Ȅ
Olmesartan medoxomilȄࣺၶܻࣺᔖᄇྱಢȂϛ࡙‫م‬ђ૖
ϚӒ௉‫ޟޱ‬AUC0-∞‫ڷ‬CmaxΰЀȂAUCघቨё60%Ȅ
Ж᠚૾ᆑ
AmlodipineȄЖ᠚૾ᆑ௉‫ޟޱ‬amlodipine఼ଶ౥ή६ȂᏲम
AUCቨёघ40%‫ڗ‬60%Ȅ
13 ߨᖝ‫ސࢳח‬Ᏸ
13.1 मᕜ‫ܒ‬ȃमएᡐ‫ܒ‬ȃҡ‫ى‬Ψཬ༌
AmlodipineȄӵσჃᇄωჃ໽ॵϛёΣamlodipine maleate
ߝႀ2ԑȂᐨ࡙ငॎᆗࣺ࿋ܻؐР݈Ң0.5ȃ1.25‫ڷ‬2.5 mg/
kg/day‫ޟ‬amlodipineȂҐี౪Ԥ᛾‫ސ‬मᕜհҢȄᄇܻωჃȂ
оmg/m2࣏அྥ඲ᆗࡣȂശଽᏘ໔ࣺ࿋ܻamlodipine‫ޟ‬Ρᡝ
ശσ࡚ដᏘ໔(MRHD)10 mg/dayȄᄇܻσჃȂоmg/m2࣏
அྥ඲ᆗࡣȂശଽᏘ໔घ࣏MRHD‫ޟ‬2ॻјȄ(ΰक़ॎᆗ୅
ۡ௉‫ޱ‬ᡝ१࣏60ϴОȄ)
ବᄇamlodipine maleate‫ܚ‬ୈ‫ޟ‬मएᡐ‫ـंܒ‬ȂҐี౪அӰ
‫ࢗܖ‬ՓᡝԤ᛾‫ࣺސ‬ᜰኇ៪Ȅ
σჃоശଽ10 mg/kg/day‫ޟ‬amlodipine(оmg/m2࣏அྥ඲ᆗȂ
घ࣏MRHD 10 mg/day‫ޟ‬10ॻ)ៀॵamlodipine maleate(໰Ⴣ
ៀॵ64ЈȂርჃܻҺ଩ࠉៀॵ14Ј)Ȃ๖‫ݎ‬ᡗҰҡ‫ى‬ΨϚ‫ڧ‬
ኇ៪Ȅ
Olmesartan medoxomilȄငҥ໽ॵ஠olmesartan‫׹‬ϠσჃߝ
ႀ2ԑࡣȂҐี౪मᕜ‫ܒ‬Ȅกၐ‫ޟ‬ശଽᏘ໔(2000 mg/kg/day)
оmg/m 2࣏அྥ඲ᆗࡣȂघ࣏Ρᡝശσ࡚ដᏘ໔(MRHD)
40 mg/day‫ޟ‬480ॻȄବᄇωჃ໌՗‫ڍ‬໶मᕜ‫ܒ‬ၐᡛȂΙ໶ବ
ᄇϐণଶp53அӰ‫ޟ‬ωჃៀॵҏ᛾‫ސ‬6এТȂΙ໶࢐ବᄇ
Hras2அӰᙽ෥ωჃ‫ޟ‬6এТആႆ໽ॵ‫׹‬᛾ȂᏘ໔ശଽႀ
1000 mg/kg/day(घ࣏MRHD‫ޟ‬120ॻ)Ȃ๖‫ݎ‬Ґี౪olmesartan
ԤमᕜհҢȄOlmesartan medoxomil‫ڷ‬olmesartanӵၐᆓϱ
ఄց‫ٳ‬ঘჃतपಠफᙽϽᔮᡛϛ഍֕ഛ‫ܒ‬๖‫ݎ‬ȂиӵAmes
(ಠ຃मएᡐ‫)ܒ‬ᔮᡛϛҐᡗҰஅӰࢳ‫ܒ‬ȄณՄȂ‫ޱڍ‬഍ོ
അԙၐᆓϱஉᎴಠफ(ϛ୽ঘჃ޲᠚)ю౪ࢗՓᡝᡐ౴Ȃи
ωჃᡝϱాБዴ૓ဝ⣞ℐᐭ एᡐ‫ޟ‬ᔮᡛ๖‫֕֯ݎ‬໨‫ܒ‬Ȅ
оശଽႀ2000 mg/kg‫ޟ‬Ꮨ໔ο݈olmesartan medoxomilࡣȂ
MutaMouse‫ޟ‬ဗ‫ڷ‬๫᠚ࣀᡝϱएᡐᔮᡛЅωჃ଼ᡜࢗՓᡝ
ນ၌‫ܒ‬ᔮᡛ(ཌਯၐᡛ)‫ޟ‬๖‫࣏֯ݎ‬ഛ‫(ܒ‬Ґᔮᡛolmesartan)Ȅ
Ι໶ၐᡛܻҺ଩ࠉ2(ርჃ)‫ܖ‬9໊(໰Ⴣ)໠ۖ๝᛾Ȃоଽႀ
1000 mg/kg/day‫ޟ‬Ꮨ໔(MRHD‫ޟ‬240ॻ)‫׹‬ϠolmesartanȂ๖
‫ݎ‬ᡗҰσჃ‫ޟ‬ҡ‫ى‬ΨϚ‫ڧ‬ኇ៪Ȅ
14 ᖝ‫ח‬ၐᡛ
14.1 Sevikar®
Ι໶࣏෈8໊‫ޟ‬ӻϛЖȃᓍᐠȃᚖ‫ޡ‬ȃԊኑᏘᄇྱȃҁ՗Ϸ
ಢϞፒӰυၐᡛȂବᄇሆ࡙Ս१࡙ଽՖᔆ௉‫໌ޱ‬՗Ȃоր
ۡ‫ٺ‬ҢSevikar®‫ݽ‬ᕛࣺၶܻএտ൐Пᕛ‫ݲ‬Ȃ६Ֆᔆਝ‫֏࢐ݎ‬
‫ڎ‬ᖝ‫ח‬ᡗ๿‫ܒ‬Ȅၐᡛ஠1,940Ρᓍᐠҁ֯ϷՍоή12এ‫ݽ‬ᕛ
ಢȈԊኑᏘȂ௥‫ڧ‬5 mg‫ܖ‬10 mg‫ޟ‬amlodipine൐П‫ݽ‬ᕛȂ௥
‫ڧ‬10 mgȃ20 mg‫ܖ‬40 mg‫ޟ‬olmesartan medoxomil൐П‫ݽ‬ᕛȂ
‫ܖ‬௥‫ڧ‬5/10 mgȃ5/20 mgȃ5/40 mgȃ10/10 mgȃ10/20 mg‫ڷ‬
10/40 mg‫ޟ‬amlodipine/olmesartan medoxomilፒП‫ݽ‬ᕛȄ
ࣺၶܻএտ൐ПԙӋȂ௥‫ڧ‬Sevikar®‫ݽ‬ᕛࡣȂ๲஻‫ڷ‬ԝᕻᔆ
‫ޟ‬६ൽၶ࣏ᡗ๿Ȅ
ήߒᇳ݂௥‫ڧ‬Sevikar®‫ݽ‬ᕛ8໊ࡣȂֲ࠼ԝᕻ‫ڷ‬๲஻ᔆ‫ޟ‬ҁ
֯६ൽȄࣺၶܻஅጣȂ஠ԊኑᏘಢ፡ᐌࡣȂՖᔆ६ൽᓍ
Sevikar®‫ޟ‬amlodipine‫ڷ‬olmesartan medoxomil‫ڍ‬ᆍԙӋᏘ໔
ЀଽՄቨёȄ
ֲ࠼ԝᕻʝ๲஻ᔆ६ൽ
ֲ࠼ԝᕻʝ๲஻ᔆ६ൽ(mmHg)ȈፒПᕛ‫ࣺݲ‬ၶܻ൐ПԙӋ
ȈፒПᕛ‫ࣺݲ‬ၶܻ൐ПԙӋ
(ᚖ‫ݽޡ‬ᕛ෈
ᚖ‫ݽޡ‬ᕛ෈)
Amlodipine
࣏༃Ρ௉‫ޱ‬ȄSevikar®૖Ԥਝ‫ݽ‬ᕛ༃Ρ(೽ல࢐ճ๫શఊ
တ)Ȃи༃Ρ௉‫ޱ‬Ֆᔆή६ൽ࡙ᇄߨ༃Ρ௉‫ࣺޱ‬խȄ
Olmesartan Medoxomil
ԊኑᏘ 10 mg 20 mg 40 mg
(mmHg)
-12/-8 -14/-9 -16/-10
-5/-3
ҁ֯ᡐϽ
ԊኑᏘ ᄇྱԊኑᏘಢ
-8/-5
-10/-6 -13/-7
፡ᐌҁ֯ᡐϽ
-15/-9 -24/-14 -24/-14 -25/-16
ҁ֯ᡐϽ
5 mg ᄇྱԊኑᏘಢ
፡ᐌҁ֯ᡐϽ -12/-7 -20/-11 -20/-11 -22/-13
-20/-13 -25/-16 -29/-17 -30/-19
ҁ֯ᡐϽ
10 mg ᄇྱԊኑᏘಢ
፡ᐌҁ֯ᡐϽ -16/-10 -22/-13 -25/-14 -26/-16
ฒ፣௉‫ޱ‬ႆў࢐֏݈Ң६Ֆᔆ᛾‫ސ‬ȃԤฒᑥ‫੾׍‬ȃ࢐֏ϐ
ᅖ65ྑ‫ܒܖ‬տ࣏դȂ݈ҢSevikar®ࡣ‫ޟ‬६Ֆᔆਝ‫֯ݎ‬᜸խȄ
Sevikar®ᄇܻ༃Ρ௉‫(ޱ‬೽ல࢐ճ๫શఊတ)ζԤ‫ݽ‬ᕛਝ‫ݎ‬Ȃ
и༃Ρ௉‫ޟޱ‬Ֆᔆ६ൽᇄߨ༃Ρ௉‫ޟޱ‬६ൽࣺխȄӵ༃Ρ
௉‫ޱ‬ఊတϛȂ೻ᆍ६ᔆਝ‫ݎ‬ᇄACE‫ڙ׻‬ᏘȃՖᆓԝᕻશ‫ڧ‬
ᡝߢᘞᏘ‫ڷ‬Κ࠮ҺཐડငߢᘞᏘ᜸խȄ
ؐЈΙԩ݈ҢSevikar®Ȃ६Ֆᔆਝ‫ݎ‬џᆰࡻ24ωਢȂՄԝᕻ
ᔆ‫ڷ‬๲஻ᔆІᔖ‫ّޟ‬৫Шӵ71%‫ڗ‬82%Ϟ໢Ȅ
‫ׇ‬ԙ8໊ᚖ‫ޡ‬ȃԊኑᏘᄇྱၐᡛࡣȂ1684Ρ໌Σ44໊‫ޟ‬໠ܹ
‫۽ܒ‬ժၐᡛȂ௥‫ڧ‬5 mg‫ޟ‬amlodipineёΰ40 mg‫ޟ‬olmesartan
medoxomilፒП‫ݽ‬ᕛȄӵ໠ܹ‫۽ܒ‬ժၐᡛϛȂष௉‫ޱ‬௥‫ڧ‬
5/40 mg‫ޟ‬amlodipine/olmesartan medoxomil‫ݽ‬ᕛϫฒ‫ݲ‬шϷ
௡‫ڙ‬Ֆᔆ(։Ґႀ‫ڗ‬ɴ140/90 mmHgՖᔆҬ኿Ȃष࣏ᑥ‫੾׍‬
௉‫ޱ‬Ȃ։Ґႀɴ130/80 mmHgҬ኿঄)Ȃࠌ஠Ꮨ໔፡ЀՍ
10/40 mg‫ޟ‬amlodipine/olmesartan medoxomilȄषՖᔆ௡‫ڙ‬ϫ
Ϛ౩དȂࠌӔѪѴ‫׹‬Ϡ12.5 mg‫ޟ‬hydrochlorothiazideȂϞࡣ
ຜሯौଡё25 mgȂоႀ‫ڗ‬ՖᔆҬ኿঄Ȅ
14.2 Amlodipine
ҬࠉϐԤ15এᚖ‫ޡ‬ȃԊኑᏘᄇྱȃᓍᐠၐᡛᡗҰAmlodipine
‫ޟ‬६ՖᔆᕛਝȂ‫ڏ‬ϛ800Ρ௥‫ڧ‬amlodipine‫ݽ‬ᕛȂ538Ρ௥‫ڧ‬
ԊኑᏘȄሆ࡙Սϛ࡙ଽՖᔆ௉‫ؐޱ‬ЈΙԩ݈᛾ȂӵҢ᛾ࡣ
24ωਢȂࣺၶܻԊኑᏘಢȂ޼࠼‫ڷ‬મ࠼Ֆᔆ६ൽ֯‫ڎ‬Ԥಛ
ॎᡗ๿‫ܒ‬Ȃҁ֯મ࠼६ճघ12/6 mmHgȂ޼࠼६ճ13/7 mmHgȄ
ӵ24ωਢҢ᛾໢Ⴄϱџᆰࡻ६ᔆਝ‫ݎ‬Ȃଽȃճ঄໢‫ޟ‬৯౴
࡞ωȄ
14.3 Olmesartan medoxomil
ҬࠉϐԤ7এԊኑᏘᄇྱၐᡛᡗҰolmesartan medoxomil‫ޟ‬६
ᔆਝ‫ݎ‬ȂᏘ໔ጒ൜௃2.5 mg‫ڗ‬80 mgȂၐᡛ෈໢࣏6‫ڗ‬12໊Ȃ
ؐ໶ၐᡛ഍ᡗҰശଽ‫ڷ‬ശճՖᔆ֯Ԥಛॎΰᡗ๿६ൽȄӓ
2,693՝নี‫ܒ‬ଽՖᔆ௉‫ޱ‬୤ᇄၐᡛ(2,145Ρ௥‫ڧ‬olmesartan
medoxomilȇ548Ρ௥‫ڧ‬ԊኑᏘ)ȄؐЈΙԩ݈Ңolmesartan
medoxomilȂ६ᔆਝ‫ݎ‬џᆰࡻ24ωਢȂՄԝᕻᔆ‫ڷ‬๲஻ᔆІ
ᔖ‫ّޟ‬৫Шӵ60%‫ڗ‬80%Ϟ໢Ȅ
16 ѓ၆ȃᓽԆᇄ೎౩
Sevikar ®ᒻᏘ֤Ԥamlodipine besylate(Ꮨ໔ࣺ࿋ܻ5mg‫ޟ‬
amlodipine)Ѕolmesartan medoxomil 20mgȄ
Sevikar®ᒻᏘ࣏ο݈ҢȂ֤໔‫ڷ‬ѓ၆ೣਿԃήȈ
ᒻᏘ֤໔(amlodipine࿋໔ʝolmesartan
medoxomil)mg
ѓ၆ೣਿ
᛾ᒻΰ‫ړ‬౰ࠢጡဴ
᛾ᒻ᚟Փ
5/20 mg
14ᗻ᎟ᆙ2а၆
C73
ҩՓ
፜ᓽԆܻ25ʨ (77ʩ)оήȄ
17 ௉‫ޱ‬ᒚၚၥଉ
ᚂৱᔖ֙‫ىޣ‬ឭஏτȂܻ಑2‫ڷ‬಑3ׁ৒໦ࢲ௥ញհҢܻ๫
શɯՖᆓԝᕻશ‫ف‬ಛ‫ޟ‬᛾‫ސ‬Ȃџ૖അԙ঺‫ݎࡣٲ‬Ȃи೻‫ٲ‬
ࡣ‫ݎ‬խн‫ߨٮ‬Ӱᛄѹ಑Ι໦ࢲܻυ৞ϱ௥ញ᛾‫ܚސ‬അԙȄ
ᔖ֙‫ىޣ‬ឭஏτ௉‫ޱ‬ΙҍᛄѹȂሯҳ։೽‫ޣ‬ᚂৱȄȦ୤َ
ឌᇭЅ‫ݧ‬ཎ‫ٱ‬໶ (5.1)ȧ
Version: 6/2008
Copyright© Daiichi Sankyo, Inc. 2007. ‫ܚ᠌ގ‬ԤȄ
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