Pharmacology · A6
α2作動薬およびイミダゾリン受容体作用薬
A6: α2-agonists and drugs acting on the imidazoline receptors
💡 覚え方:A6の分類
🧠 共通点は 中枢の交感神経出力sympathetic outflow交感神経出力(sympathetic outflow)sympathetic outflow(交感神経出力)を下げる(→降圧antihypertensive (blood-pressure lowering)降圧(antihypertensive (blood-pressure lowering))antihypertensive (blood-pressure lowering)(降圧)・鎮静) こと。まず 受容体(α2作動とイミダゾリンimidazolineイミダゾリン(imidazoline)imidazoline(イミダゾリン)I1作動) で分け、α2群は 適応(降圧antihypertensive (blood-pressure lowering)降圧(antihypertensive (blood-pressure lowering))antihypertensive (blood-pressure lowering)(降圧)・鎮静・筋弛緩・眼) で枝分けするのがコツ。 語尾ヒント → イミダゾリンimidazolineイミダゾリン(imidazoline)imidazoline(イミダゾリン)I1系は -onidine(モキソニジンmoxonidineモキソニジン(moxonidine)moxonidine(モキソニジン)・リルメニジンrilmenidineリルメニジン(rilmenidine)rilmenidine(リルメニジン))で降圧antihypertensive (blood-pressure lowering)降圧(antihypertensive (blood-pressure lowering))antihypertensive (blood-pressure lowering)(降圧)専用。
1️⃣ 中枢性α2作動薬
■ 降圧antihypertensive (blood-pressure lowering)降圧(antihypertensive (blood-pressure lowering))antihypertensive (blood-pressure lowering)(降圧)
- メチルドパmethyldopaメチルドパ(methyldopa)methyldopa(メチルドパ) — 中枢α2作動(α-メチルノルアドレナリンalpha-methylnoradrenalineα-メチルノルアドレナリン(alpha-methylnoradrenaline)alpha-methylnoradrenaline(α-メチルノルアドレナリン)経由)|適応:高血圧(特に妊娠)
- クロニジンclonidineクロニジン(clonidine)clonidine(クロニジン) — 中枢α2作動|適応:高血圧・ADHD・オピオイド/アルコール離脱alcohol withdrawalアルコール離脱(alcohol withdrawal)alcohol withdrawal(アルコール離脱)症状
■ 鎮静
- デクスメデトミジンdexmedetomidineデクスメデトミジン(dexmedetomidine)dexmedetomidine(デクスメデトミジン) — 選択的中枢α2作動|適応:ICU鎮静・処置鎮静procedural sedation処置鎮静(procedural sedation)procedural sedation(処置鎮静)(呼吸駆動を保つ)
■ 筋弛緩
- チザニジンtizanidineチザニジン(tizanidine)tizanidine(チザニジン) — 中枢α2作動 → 運動ニューロンの興奮を抑制|適応:痙縮spasticity痙縮(spasticity)spasticity(痙縮)(MS・脊髄損傷spinal cord injury, SCI脊髄損傷(spinal cord injury, SCI)spinal cord injury, SCI(脊髄損傷))
■ 眼・局所
- ブリモニジンbrimonidineブリモニジン(brimonidine)brimonidine(ブリモニジン) — 選択的α2作動 → 房水産生aqueous humor production房水産生(aqueous humor production)aqueous humor production(房水産生)↓・ぶどう膜強膜流出uveoscleral outflowぶどう膜強膜流出(uveoscleral outflow)uveoscleral outflow(ぶどう膜強膜流出)↑|適応:開放隅角緑内障open-angle glaucoma開放隅角緑内障(open-angle glaucoma)open-angle glaucoma(開放隅角緑内障)・酒さrosacea酒さ(rosacea)rosacea(酒さ)の紅斑(外用)
2️⃣ イミダゾリンI1受容体作動薬
- モキソニジンmoxonidineモキソニジン(moxonidine)moxonidine(モキソニジン) — 中枢I1受容体作動 → 交感神経出力sympathetic outflow交感神経出力(sympathetic outflow)sympathetic outflow(交感神経出力)↓|適応:高血圧
- リルメニジンrilmenidineリルメニジン(rilmenidine)rilmenidine(リルメニジン) — 中枢I1受容体作動|適応:高血圧
🔁 1枚図でまとめ
flowchart TD
R["A6: 中枢の<span class='jp-term jp-term-diagram' title='sympathetic outflow'>交感神経出力</span>↓<br>(<span class='jp-term jp-term-diagram' title='antihypertensive (blood-pressure lowering)'>降圧</span>・鎮静)"]
R --> A2["中枢性α2作動"]
R --> I1["<span class='jp-term jp-term-diagram' title='imidazoline'>イミダゾリン</span>I1作動<br><span class='jp-term jp-term-diagram' title='moxonidine'>モキソニジン</span> / <span class='jp-term jp-term-diagram' title='rilmenidine'>リルメニジン</span><br>(<span class='jp-term jp-term-diagram' title='antihypertensive (blood-pressure lowering)'>降圧</span>専用)"]
A2 --> H["<span class='jp-term jp-term-diagram' title='antihypertensive (blood-pressure lowering)'>降圧</span><br><span class='jp-term jp-term-diagram' title='methyldopa'>メチルドパ</span>(妊娠)<br><span class='jp-term jp-term-diagram' title='clonidine'>クロニジン</span>(+ADHD/離脱)"]
A2 --> S["鎮静<br><span class='jp-term jp-term-diagram' title='ICU'>デクスメデトミジン</span>"]
A2 --> M["筋弛緩<br><span class='jp-term jp-term-diagram' title='tizanidine'>チザニジン</span>(<span class='jp-term jp-term-diagram' title='spasticity'>痙縮</span>)"]
A2 --> E["眼・局所<br><span class='jp-term jp-term-diagram' title='brimonidine'>ブリモニジン</span>(緑内障)"]
📋 まとめ表
| 薬剤 | 受容体 | 適応群Group適応群(Group)Group(適応群) | 適応 |
|---|---|---|---|
| メチルドパmethyldopaメチルドパ(methyldopa)methyldopa(メチルドパ) | 中枢α2 | 降圧antihypertensive (blood-pressure lowering)降圧(antihypertensive (blood-pressure lowering))antihypertensive (blood-pressure lowering)(降圧) | 高血圧(特に妊娠) |
| クロニジンclonidineクロニジン(clonidine)clonidine(クロニジン) | 中枢α2 | 降圧antihypertensive (blood-pressure lowering)降圧(antihypertensive (blood-pressure lowering))antihypertensive (blood-pressure lowering)(降圧) | 高血圧・ADHD・離脱症状withdrawal symptom離脱症状(withdrawal symptom)withdrawal symptom(離脱症状) |
| デクスメデトミジンdexmedetomidineデクスメデトミジン(dexmedetomidine)dexmedetomidine(デクスメデトミジン) | 選択的中枢α2 | 鎮静 | ICU・処置鎮静procedural sedation処置鎮静(procedural sedation)procedural sedation(処置鎮静) |
| チザニジンtizanidineチザニジン(tizanidine)tizanidine(チザニジン) | 中枢α2 | 筋弛緩 | 痙縮spasticity痙縮(spasticity)spasticity(痙縮)(MS・脊髄損傷spinal cord injury, SCI脊髄損傷(spinal cord injury, SCI)spinal cord injury, SCI(脊髄損傷)) |
| ブリモニジンbrimonidineブリモニジン(brimonidine)brimonidine(ブリモニジン) | 選択的α2 | 眼・局所 | 緑内障・酒さrosacea酒さ(rosacea)rosacea(酒さ)の紅斑 |
| モキソニジンmoxonidineモキソニジン(moxonidine)moxonidine(モキソニジン) | イミダゾリンimidazolineイミダゾリン(imidazoline)imidazoline(イミダゾリン)I1 | 降圧antihypertensive (blood-pressure lowering)降圧(antihypertensive (blood-pressure lowering))antihypertensive (blood-pressure lowering)(降圧) | 高血圧 |
| リルメニジンrilmenidineリルメニジン(rilmenidine)rilmenidine(リルメニジン) | イミダゾリンimidazolineイミダゾリン(imidazoline)imidazoline(イミダゾリン)I1 | 降圧antihypertensive (blood-pressure lowering)降圧(antihypertensive (blood-pressure lowering))antihypertensive (blood-pressure lowering)(降圧) | 高血圧 |