1. ȯڿ
2. ̻
1) 12 ̻ ӻ迡 1 50mg(1 1ȸ) Ǵ 1 100mg(1 1ȸ 100mg Ǵ 1 2ȸ 50mg) 뷮 ٱ۸ƾ 3,784κ ڷḦ Ͽ. ȯڵ ߿ 2,264 ٱ۸ƾ ܵ Ұ, 1,520 ٸ Բ Ҵ. 2,682 ȯڵ ٱ۸ƾ 1 100mg(1 1ȸ 100mg Ǵ 1 2ȸ 50mg) Ұ, 1,102 1 1ȸ 50mg Ҵ.
2) ӻ迡 Ÿ ̻ κ Ͻ̾, ߴ ʿ䰡 . ̻ , , Ⱓ Ǵ 뷮 ߰ߵ ʾҴ.
3) ̻ 幰 Ǿ. Ϲ ӻ ̾, ߴ Ŀ ȸǾ. 24 ܵ ӻ , ALT Ǵ AST ġ(ULN) 3 ̻ Ÿ ٱ۸ƾ 50mg 1 1ȸ, ٱ۸ƾ 50mg 1 2ȸ 鿡 0.2%, 0.3%, 0.2% Ÿ. Ʈƹ̳ ġ Ϲ ̰ -̸, ü Ȳް .
4) ٱ۸ƾ 幰 Ǿ, ACE Ͽ Ҵ. ̻ κ ̾ ٱ۸ƾ ذǾ.
5) ܵ ߸Ͱ ȯڿ ̻ MedDRA Ͽ. 賻 ̻ Ͽ.( ϰ ̻ ó ) ɰ ϴ ̻ Ͽ. ̻ ش з : ſ ϰ(1/10) ; ϰ(1/100, 1/10) ; ʰ(1/1,000, 1/100) ; 幰(1/10,000, 1/1,000) ; ſ 幰(1/10,000) ; Ҹ( )
(1) Ʈΰ
- 1 100mg Ʈ ӻ迡, ̻ ߴ Ʈ Ǵ Ʈ ο ʾҴ.
- ӻ迡 1 100mg Ʈ 1% ϰ, Ʈ 0.4% ʰ Ÿ. ʾҴ.
- ӻ迡 Ʈο 1 100mg Ͽ +0.2kg, -1.0kg ü ȭ .
[ǥ1] Ͱ ӻ(208) Ʈΰ 1 ٱ۸ƾ 100mg ȯڿ ̻
- 2 ̻ Ⱓ ӻ迡 Ʈο ٱ۸ƾ ߰ Ͽ , ߰ ȣ Ǵ ߴ ʾҴ.
- 索 ȯڿ ٱ۸ƾ Ʈ ӻ迡 ߰ ȣ Ǵ ߴ ʾҴ.
(2) ҿ췹ƿ
- 50mg ҿ췹 ӻ迡, ̻ ߴܷ ҿ췹 0.6%, ҿ췹 0%̾.
- ӻ迡 ۸Ǹ忡 1 1ȸ 50mg ߰ Ͽ 1.2%̾ ۸Ǹ 0.6%̾. ʾҴ.
- ӻ迡, ۸Ǹ忡 1 50mg ߰ Ͽ -0.1kg, -0.4kg ü ȭ .
[ǥ2] Ͱ ӻ(170) ҿ췹ƿ 1 ٱ۸ƾ 50mg ȯڿ ̻
(infections and infestations)
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ſ 幰
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εο
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Ű ̻
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ϰ
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ϰ
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ϰ
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ϰ
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̻
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ʰ
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̻
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ϰ
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(3) ġ°
- 1 100mg ǿ۸Ÿ ӻ迡, ̻ ߴ ǿ۸Ÿ ǿ۸Ÿ ο ʾҴ.
- ӻ迡 ٱ۸ƾ ǿ۸Ÿ ȯ(0.6%) ʾ, ǿ۸Ÿ ȯ(1.9%) Ͽ. ʾҴ.
- ǿ۸Ÿ ӻ迡 1 100mg ü 1.4kg 2.7kg̾.
- 1 100mg ǿ۸Ÿ(1 45mg) ִ 뷮 ߰ Ǿ 7.0%̾, ǿ۸Ÿ ܵ ÿ 2.5%̾.
[ǥ3] Ͱ ӻ(158) ġ° 1 ٱ۸ƾ 100mg ȯڿ ̻
(4) ٱ۸ƾ ܵ
- ܵ ӻ迡, ̻ ߴܷ (0.6%) Ǵ Ȱ(0.5%) ٱ۸ƾ (0.3%) ʾҴ.
- ܵ ӻ迡, Ȱ Ǵ (0.2%, 1,082 2) ٱ۸ƾ 1 100mg (0.4%, 1,855 7) ʰ Ǿ. ߴ Ǵ ̻ ʾҴ.
- ӻ迡, ٱ۸ƾ -0.3kg, -1.3kg ٱ۸ƾ 1 100mg ܵν Ǿ ü ȭ .
Ű ̻
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ϰ
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ʰ
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̻
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ʰ
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ٰݰ ̻
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ʰ
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̻
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ʰ
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(infections and infestations)
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ſ 幰
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ſ 幰
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εο
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̻
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ʰ
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[ǥ4] Ͱ ӻ(1,855) ܵ ٱ۸ƾ 1 100mg ȯڿ ̻
- 2 ̻ Ⱓ ӻ迡 ٱ۸ƾ ܵ ߰ ȣ Ǵ ߴ ʾҴ.
(5) ν
- ν Ǵ ν Ʈΰ ٱ۸ƾ 50mg 1 2ȸ ߰ ӻ迡 ̻ ߴܷ ٱ۸ƾ 0.3%, ౺ ش 찡 ʾҴ.
- ٱ۸ƾ(14.0%) ౺(16.4%) Ͽ. ٱ۸ƾ 2 Ǿ, ౺ 6 Ǿ.
- ü߿ ġ ̹Ͽ. [ٱ۸ƾ(ġκ +0.6kg)/ ౺(0kg)]
[ǥ5] ν Ǵ ν Ʈΰ ٱ۸ƾ 1 100mg ӻ(371) ̻
Ű ̻
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ϰ
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̻
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ϰ
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ϰ
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ĵ
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ʰ
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ʰ
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â
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̻
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ϰ
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˻(Investigations) ġ
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ϰ
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(6) Ʈ ҿ췹ƿ
- ٱ۸ƾ+Ʈ+۸Ǹ 뱺( ٱ۸ƾ) ̻ ߴ ʾҰ, +Ʈ+۸Ǹ 뱺( ౺) ߴܷ 0.6%̾.
- ٱ۸ƾ(5.1%) ౺(1.9%) ϰ Ͽ. ٱ۸ƾ 1 Ǿ.
- ü߿ ġ ̹Ͽ.ٱ۸ƾ(+0.6kg) ౺(-0.1kg)
[ǥ6] Ʈ ҿ췹ƿ ٱ۸ƾ 1 100mg ӻ(157) ̻
(7)
ڹߺ ʸ κ ̻ Ǿ. ̷ ̻ Һи ũ αܿ ڹ μ ŷڼ ִ Ʊ зϿ.
- 忰
- ( ߴ )
- ε巯, Ż Ǻκ( õâ )
- ָ ϴ
6)
ɻ縦 Ͽ 6 3,080 ǽ , ػ ΰ 2.05%(63/3,080, 86) Ǿ.
ߴ ػ 0.32%(10/3,080, 16) ɱٰ 0.06%(2/3,080, 2), ơ, 㳶, 䡯, 㼮, , ʵȯ, ɽǼơ, ɺ, ˾硯, ϡ, INR , ⿰, , ơ 0.03%(1/3,080, 1), ΰ踦 ߴ ػʴ .
ػ ΰ 1.36%(42/3,080, 55) Ǿ, ػʴ κ 0.16%(5/3,080, 5), ȣ 0.13%(4/3,080, 4), ɱٰ, ħ, ȭҷ, , ơ 0.06%(2/3,080, 2) Ǿ. ΰ踦 ػ 0.32%(10/3,080, 10) , , 䡯, Ҹ, ȭҷ, ֡, Լ, , κ, ⡯ 0.03%(1/3,080, 1) Ǿ.
ɻ ػ ڹ ۿ ڷḦ 㰡 Ǿǰ ػ ڷ ɻ , ٸ Ǿǰ ػʿ ϰ ػ Ȯε ͵ . ٸ, ش缺а ػʰ ΰ谡 ǹϴ ƴϴ.
. ʽŰ : , ô߰
. : , ȭҷ, 忰, , ˾, Ʈ, ⿰
. 㵵 ȯ : 氣, 㳶
. ȯ : Į,
. Ϲ ȯ : ɺ,
. ɱ, ɳ, ɸ, Ǹ ȯ :
. ڵ :
. ȯ : ų
. Ż :
. ȯ : ٸ, Cܹ
3. Ϲ
1) ν ʿ䰡 ʿ ȯڿ ν ü ʴ´. 1 索 ȯ Ǵ 索 ȯڿ ؼ ȴ.
2) : ϴ (ESRD)ȯڿ ̹Ƿ, ̵ ȯڿ Ͽ Ѵ.
3) : ̻ 幰 Ǿ. Ϲ ӻ ̾, ߴ Ŀ ȸǾ. ϱ (ȯ ˱ ) ϴ ˻縦 ǽϿ Ͽ Ѵ. ˻縦 ǽϴ 쿡 ó 1 3, Ŀ ǽϴ ٶϴ.
Ʈƹ̳ ġ µ ȯڴ Ǿ ϰ, ȸ Ǿ Ѵ. ġ(ULN) 3 ̻ AST Ǵ ALT ӵǸ ǰѴ. Ȳ Ǵ ٸ ̻ Ÿ ĸ ȯڴ ߴϿ Ѵ.
ߴϰ ˻簡 ȸ Ŀ 簳 ʾƾ Ѵ.
4) ɺ : New York Heart Association (NYHA) functional class I-III ȯڸ ӻ迡 Ͽ , ½ɽ ȭ Ǵ ɺ ȭʹ õ . NYHA class III ȯ ӻ ̾ ϱ ƴ.
NYHA class IV ȯڿ ӻ ʴ´.
5) Ǻ̻ : ˾ Ǻ ܺο Ǿ(9. Ÿ ). ӻ迡 Ǻ ʾ, 索 Ǻ պ ִ ȯڿ . 迡 Ż Ǻκ Ǿ. Ƿ Ǵ ˾ Ǻ ְ Ÿ Ͽ 索 ȯڸ Ѵ.
6) 忰 :
ٱ۸ƾ 忰 ߺ ִ. ϴ ȯڿ 忰 Ư¡ ˷־ Ѵ. 忰 ǽɵ ٱ۸ƾ ߴؾ ϸ, 忰 Ȯ 쿡 ٽ ؼ ȵȴ. 忰 ִ ȯڿ ؼ Ͽ Ѵ.
7) Ű ˷ ϴ ȯ : ҿ췹 迭 ν к ִ. ҿ췹ƿ Ǿ ִ. Ͽ ּȭŰ Ͽ 뷮 ν к ʿ ִ.
8) ۿ ġ ʾ ̻ ִ ȯڴ Ǵ ؾ Ѵ.
9) ָ ϴ
DPP-4 ȯ 翡 ָ ϴ Ǿ. ñ 1 ĺ ı پϿ. ÿ ȭǾ. Ϻ ȯڿ Ǵ ٸ DPP-4 ٽ ÿ Ÿ. DPP-4 Ͽ Ѵ.
10) õâ
DPP-4 ȯ 翡 Կ ʿ ϴ õâ Ǿ. ȯڵ Ϲ DPP-4 Ǵ 鿪 ġ ȸǾ. ȯڵ鿡 ϴ Ǵ ϸ ǻ翡 ϵ ˷ Ѵ. , õâ ǽɵǴ , ߴϰ ġḦ Ǻΰ ǿ ؾ Ѵ.
4. ȣۿ
5. Ӻ, , Ҿƿ
6. óġ
7. ǻ
8. Ǿǰ
9. Ÿ
1) 峻 Ǿ(ؿ뷮 15mg/kg [Cmax 7]).
2) 带 26 ݺ 콺 13 ݺ迡, 콺 ļ Ǿ. 忡 ؿ뷮 25mg/kg (AUC 5)̰, 콺 750mg/kg (AUC 142)̾.
52 ݺ迡 , Ư , , , 뷮 Ǿ, ؿ뷮 Ȯ ʾҴ.
3) 迡 ٱ۸ƾ in vitro in vivo 迡 ̸ Ÿ ʾҴ.
4) 忡 ´ ʱ , ٱ۸ƾ ´, ķ ʱ ̻ ٰŰ Ÿ ʾҴ. 䳢 Ǿ. 忡 ü ü ҿ õ Ļ Ͽ, ؿ뷮 75mg/kg( 10)̾. 䳢 Ÿ ¾ ü ü Ÿ Ǿ, ؿ뷮 50mg/kg( 9)̾. 䳢 ٱ۸ƾ 750 150mg/kg 뷮 , ֱ Ÿ ʾҴ. 忡 , 150mg/kg ̻ 뷮 ü õ Ұ߸ Ǿ, 1 ڼտ ɷ ҿ Ͻ ü Ұ Ÿ.
5) 忡 900mg/kg( ִ 뷮 ⷮ 200) 汸뷮 ߾ϼ 2 ǽõǾ. ٱ۸ƾ ʾҴ. 콺 1,000mg/kg 汸 뷮 ߾ϼ 2 Ǿ. Ǿ, ؿ뷮 500mg/kg( 59) 100mg/kg( 16)̾. 콺 ̷ ٱ۸ƾ ֿ ü Ÿ ʰ ְ Ÿ , Ѵٰ ʴ´.
6) ̸ 13 ݺ 迡, Ǻ 5mg/kg/day ̻ 뷮 Ÿ. ̴ ܺ(, , , ) ϰǰ Ÿ. 5mg/kg/day (100mg 뷮 AUC 뷫 ) 뷮 Ǿ, ұϰ ̾ ̻ . ȭ ִ Ǻ, Ǻιڸ, , 20mg/kg/day(100mg 뷮 AUC 3) ̻ 뷮 Ǿ. 缺 80mg/kg/day ̻ 뷮 Ǿ. 160mg/kg/day ̿ Ǻ 4 ȸ Ⱓ ʾҴ.
8. Ǿǰ 1
. (ٱ۸ƾ)[ѱƼ] 꽺50и(ٱ۸ƾ)[ѱƼ] 22 1 ǰ ο ȸ 汸Ͽ 28 ٱ۸ƾ , ġ(AUCt, Cmax) αȯϿ óϿ , ġ 90% ŷڱ log 0.8 log 1.25 ̳μ Ͽ.