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Pharmacy - sem2 > NM blocker > Flashcards

NM blocker Flashcards

1
Q

Hemicholinium

A

抑制choline uptake into neuron

Ach合成減少

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2
Q

Triethylcholine

A

Ach合成減少

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3
Q

vesamicol

A

transporter負責將Ach放進儲存泡裡，

這時vesamicol可以抑制transporter ，進而抑制Ach進入儲存泡。

inhibitory to N-M conduction

（作用似reserpine）

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4
Q

Botulinum toxin

A

Release of Ach from vesicle is blocked

due to action potential

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5
Q

spider venom

A

causes release of Ach out of neuron

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6
Q

Tetrodotoxin河豚毒素

A

抑制Na+通道（毒素主要在卵巢，肝，皮膚）

inhibit muscle activity

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7
Q

Saxitoxin

A

inhibit sodium ion channel

inhibit muscle activity

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8
Q

Local anesthetic

A

Local anesthetic：抑制Na+, K+通道，無動作電位 à 無訊息傳導 à 無ACh釋放

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9
Q

effect of muscle by Mg2+

A
  1. ACh釋放需要Ca2+，而Mg2+會與Ca2+競爭，所以太多的Mg2+會減少Ca2+，造成ACh釋放減少

inhibitory to muscle

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10
Q

Aminoglycoside

A
  1. 減低Ca2+存在
  2. 降低receptor對ACh的sensitivity

inhibit muscle activity

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11
Q

tetracycline

A

會造成肌肉鬆弛的抗生素：tetracycline（因喜歡和二價離子結合）, polymyxin, lincomycin（後二機制不明)

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12
Q

Physostigmine

A
  • Since it can increases the concentration of Ach, it could reverse the effect caused by competitive Ach blocker, such as d-tubercurarine, 肌肉張力回升
  • 阻止AChE 分解ACh，使副交感興奮
  • 三級胺，可穿過 BBB， 作用在中樞
  • When Overdose…
  • 2. 骨骼肌過度極化： weakness, fasciculation，再 paralysis
    3. CNS effect: nausea
    1. Excess bronchiolar secretion
      5. Death could occur
    1. 以前被當作裁判豆 (犯罪、緊張的人 因交感興奮而吸收 佳，導致毒性高)
      7. Atropine as 解藥
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13
Q

Neostigmine

A

Since it can increases the concentration of Ach, it could reverse the effect caused by competitive Ach blocker, such as d-tubercurarine

阻止AChE 分解ACh，使副交感興奮 (reversible)

no CNS effect, quaternary amine

是一種Mixedtype，可以抑制 酶，也可自行刺 激受體（作用類 似交感的那三個 mixed-type）
2. More active at nicotinic receptor
 多用於治療如 myasthenia gravis 等肌肉無力 症狀; overdose also cause 過度極 化
3. Little CNS effect

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14
Q

Edrophonium

A

reversible AchE inhibitor, no CNS effect

Nm and Nn receptors being activated at the same time

very short duration

Curare antagonist (curare is muscle relaxant)

mostly used for diagnosis prodcedures

IV injection improve muscle function, such as myashtenia gravis

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15
Q

去極化性depolarizing agents of muscle relaxant

describe the stage, characteristics

A

低劑量à造成去極化，與Ach類似

  1. 高劑量à造成抑制效果
  2. 例如；Succinylcholine、decamethonium （這兩個藥是去極性的代表藥品）
  3. 剛開始會與ACh有類似效果à暫時性的造成抽蓄（twitch）、肌束搐動（fasciculation）
    * 造成twitch原因：因為一開始低劑量造成結後收縮，會形成「逆向衝動」，衝動會往回走到比較大的神經，整條被這條神經所innervate的肌肉就會收縮

à fasciculation （術後可能造成肌肉痠痛，甚至橫紋肌溶解）

  1. 長時間持續刺激會造成無力肢體麻痺（flaccid paralysis）
  • 造成flaccid paralysis原因：使用depolarizing藥物時，細胞膜依舊對於鈉離子是有通透性的，造成持續性的去極化，使得再極化（repolarizing）不完全，所以最後傳導被阻斷
  • Succinylcholine不會被AChE水解，需要從N-M junction擴散到血液中才會被pseudocholine esterase分解，因此接上ion channel的時間較長，ion channel長時間打開，造成再極化不完全
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16
Q

Phase of depolarizing agent

A

(1) Phase I：去極化藥品所造成的阻斷（以上所說的）
(2) Phase II：

  1. 發生在長時間，高劑量下
  2. 類似競爭性的效果，對去極化藥品不會有反應
  3. 光光註釋：其實並不會是變成競爭性拮抗，只是長期之用去極化藥品會使Receptor失去敏感性（desensitization），是快速耐受性（tachyphylaxis）造成的結果。看起來像競爭性的作用但機制是完全不同的。

(一) Mixed block

Phase I 和 Phase II合併使用

(二) Dual block 雙重阻斷

過量去極化藥物造成的Phase II block

17
Q

Atracurium

A

是類似競爭性藥物，phase II block看似競爭性但實際上不是

no effect on autonomic ganglia and cardiac M2 receptor

sligh effect on histamine release (blood pressure falls)

18
Q

Succinylcholine

A
  • 去極化性depolarizing agents
  • 1/1000 of Ach potency
  • 剛開始會與ACh有類似效果à暫時性的造成抽蓄（twitch）、肌束搐動（fasciculation）
  • 長時間持續刺激會造成無力肢體麻痺（flaccid paralysis）
  • Neostigmine acclerates the paralysis
  • Succinylcholine不會被AChE水解，需要從N-M junction擴散到血液中才會被pseudocholine esterase分解，因此接上ion channel的時間較長，ion channel長時間打開，造成再極化不完全
  • 肌肉張力回升快慢與Pseudo-ChE的量有關。
  • Autonomic ganglia stimulation: vasoconstriction, blood pressure rises
  • cardiac M2 receptors stimulation: M2 decreases heart rate
  • slight effect on histamine release : reduction on blood pressure
19
Q

decamethonium

A
  • 去極化性depolarizing agents
  • 剛開始會與ACh有類似效果à暫時性的造成抽蓄（twitch）、肌束搐動（fasciculation）
  • 長時間持續刺激會造成無力肢體麻痺（flaccid paralysis）
  • Neostigmine acclerates the paralysis
  • 不會被AChE水解，需要從N-M junction擴散到血液中才會被pseudocholine esterase分解，因此接上ion channel的時間較長，ion channel長時間打開，造成再極化不完全
  • vs Succinylcholine: decamethonium對pseudoChE具more resistance，半衰期比較長。
  • 肌肉張力回升快慢與Pseudo-ChE的量有關。
20
Q

d-tubocurarine

A
  • Autonomic effect

d-tubocurarine會阻斷神經節（交感&副交感）& 造成histamine release→血壓下降。

原因：交感在血管優勢，阻斷交感會導致vasodilation。而且histamine會擴張小血管。（histamine個人資訊：上升心跳、增加血管通透性、擴張小血管、收縮大血管，整體來說會降低周邊血壓）

  • 在快速IV時會造成histamine釋放造成低血量，心跳上升，CO上升，分泌上升，氣管收縮等，類似過敏反應
  • （succinylcholine, d-tubocurarine, pancuronium）對心臟及histamine release影響較明顯，新合成的藥對心臟及Histamine release影響較少
21
Q

histamine release ?

A

（succinylcholine, d-tubocurarine, pancuronium）對心臟及histamine release影響較明顯，新合成的藥對心臟及Histamine release影響較少

在快速IV時會造成histamine釋放造成低血量，心跳上升，CO上升，分泌上升，氣管收縮等，類似過敏反應

22
Q

tubocurarine

A
23
Q

mivacurium

A

competitve non-depolarizing NM blocker

no effect on autonomic ganglia and M2 receptor

slight effect on histamine release

Pharmacy - sem2 (14 decks)

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