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Pharmacy - sem2 > cholinergic > Flashcards

cholinergic Flashcards

1
Q

Comparing methacoline, carbachol and bethanecol in

  1. cardovascular system
  2. GI system
  3. other smooth muscle inculding urinary, uterus, bronchio
  4. sweat glands
  5. skeletal muscle
A
  1. 對心血管影響：均是負向

• methacholine > carbachol> bethanechol

  1. 消化道影響：均是興奮

• carbachol＆bethanechol > methacholine

  1. 其他平滑肌：
  • 尿道：排尿；carbachol＆bethanechol > methacholine
  • 子宮肌肉：收縮；pregnancy v.s. after parturition
  • 氣管：收縮（氣管阻塞、肺部疾病不能用）
  1. 汗腺：carbachol會造成馬流汗
  2. 骨骼肌：劑量太多會paralysis；only carbacol is effective (N agonist property)
  3. 其他：carbachol產生diffusional sympathomimetic effects (因為會作用於N receptor)
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2
Q

Methacholine

A

synthetic choline esters

Chemical property:

  • methyl group on beta carbon ：nicotinic agonist mainly

route of aministration: 吸入性投

interaction:

在人醫：

  1. 治療血管痙攣，使血管舒張
  2. 治療supraventricular tachycardia

在獸醫：(rarely used in vet med)

  1. 用來診斷，診斷氣管是否會過敏

Pharmacokinetics:

  1. 因為有四級胺，口服吸收很差
  2. 主要抗pseudocholinesterase (plasma中的酶)
  3. 次要抗AChE
  4. More active on cardiovascular system than on GI/Urinary

心血管抑制

Larger dose can cause atrial fibrillation as side effect

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3
Q

Carbacol

A

synthetic choline esters

Chemical property: very potent!, can act on both N and M receptors (so may cause diffusional sympathomimetic effects !)

route of aministration:

局部、SC：平滑肌收縮

（四級胺口服不佳）

IM, IV：吸收太快，有副作用；use SC instead

interaction:

  1. 縮瞳，下降眼壓(IOP)
  2. 消化道作用上升，主要用在單純食物遲滯，促進蠕動

(用在治療肌肉無力，但不可治器官扭轉哦!)

  1. 生產時/後給予，促胎兒排出，也促進胎盤排出

Pharmacokinetics: 因為會作用在N receptor，會部分刺激交感活化，因此會有肌肉顫抖，馬流汗（beta 2 adrenergic）

side effect:

  1. 若非用在單純食物遲滯時，會造成腸套疊，器官爆裂
    （對單胃動物影響大，反芻還好）
  2. 若是懷孕後期使用，會造成流產
  3. Severe slivation, vomiting, diarrhea and frequent urination
  4. Potent, so be careful of over-dose! No IV/IM ；骨骼肌：劑量太多會paralysis
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4
Q

Bethanecol

A

synthetic choline esters

Chemical property:

  1. beta-carbon methylation: muscarinic agonist
  2. carbamy group: not easily decomposed by esterase

route of aministration: PO/SC

interaction:

  1. 治療遺尿、頻尿者：因為可以促進排尿
  2. Treat urinary agony after incidence of urolithiasis
  3. 治療單純食物遲滯
  4. 可用兩種藥物代替：

Examples

  • neostigmine：抑制AChE，使副交作用上升
  • metoclopramide：使ACh釋出量增加
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5
Q

Pilocarpine

A

the only clinically in-use naturally occurring cholinomimetic alkaloid毛果芸香鹼

  • tertiary amine alkaloid acting on muscarinic receptors mainly

Pharmacologic effects:

  1. 有三級胺，可以穿過BBB，造成中樞的作用。can applied topically
  2. 作用會類似carbachol

Pharmacokinetics and adverse effect

  1. Local irritation and inflammation、inflammation of oveal tract (葡萄膜炎) (此藥物較少用於治療青光眼)
  2. 曾經有人拿來促貓咪的嘔吐，但是效果不好（貓的催吐會用alpha 2 agonist的 Xylazine）
  3. 大量分泌液體 (saliva, digestive juice)
  4. 嘔吐 vomitting
  5. Bronchioconstricting、阻塞，造成呼吸不順(dyspnea)
  6. 急性腹痛（疝痛colic）
  7. 腹瀉diarrhea
  8. Pupil constrictor effect (縮瞳)

Clinical use

  1. 口服（三級胺口服優）：使分泌增加，用於口水的收集、乾燥症的治療，或用於化療後口水分泌下降的人
  2. 治療Glaucoma (青光眼)，降低眼壓，瞳孔收縮 (miosis) by IV or applying topically
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6
Q

Arecoline

comparing with pilocarpine, which one is more potent?

A

naturally occurring cholinomimetic alkaloid 檳榔鹼 mainly targeting muscarinic receptors

比pilocarpine強

Use

  • Tenicacide殺絛蟲藥（用於狗）

Side effect

  1. 大量分泌液體 (saliva, digestive juice)
  2. 嘔吐 vomitting
  3. Bronchioconstricting、阻塞，造成呼吸不順(dyspnea)
  4. 急性腹痛（疝痛colic）
  5. 腹瀉diarrhea
  6. Pupil constrictor effect (縮瞳)
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7
Q

Muscarine

A

naturally occurring cholinomimetic alkaloid 檳榔鹼 mainly targeting muscarinic receptors

expensive, only use in experiement

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8
Q

Physostigmine

A

阻止AChE分解ACh，使副交感興奮; reversible AChE inhibitor

tertiary amine group, so can pass through BBB

Interaction with Esterase

  1. 會被血漿中的酶水解 (Non-regenerable)
  2. 速度是ACh水解的1/106倍
  3. Toxicity

· 犬、牛血中的esterase比較少，故容易中毒

· 馬的esterase比較多，比較不容易中毒

Characteristics

  1. 作用時間較長，可達3-~6小時

When Overdose…

  1. 骨骼肌過度極化：weakness, fasciculation，再paralysis
  2. CNS effect: nausea
  3. Excess bronchiolar secretion
  4. Death could occur
  5. 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)
  6. Atropine as 解藥

Effect

  1. 增加消化道活性
  2. 分泌增加
  3. 對眼睛：縮瞳，睫狀肌(ciliary muscle)收縮，lens變圓，適合看近的
  4. 骨骼肌：會和NM junction blocker去競爭，使肌肉不會鬆弛
    （d-tubocurarine antagonist）（d-tubocurarine is a non-depolarizing neuromuscular blocking agent）
  5. Bronchoconstriction
  6. Smooth muscle of urinary bladder contraction
  7. In higher dose (physostigmine and neostigmine mainly): 副交感過度興奮hypotension and tachycardia à 心律不整Arrhythmia心血管過度放鬆
  8. 氣管收縮, leading to excessive bronchiolar secretion
  9. 分泌增加

＝>用_atropine_或其他antimuscarinic drugs當解藥

Clinical use

  1. 治療青光眼(glaucoma)：使前房液流出，降低眼壓
  2. 增加瘤胃(rumen)活動性via SC

· 阻塞性obstructive agony不能用: violent peristalsis causes rupture or intussusception of the gut!!!

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9
Q

Neostigmine

A

阻止AChE分解ACh，使副交感興奮; reversible AChE inhibitor

四級amine group, so can’t pass through BBB

Interaction with Esterase

  1. 四級胺端(alcholic portion)會和酶的anion端接在一起
  2. Carbamyl group端會和酶的serine OH端接在一起
  3. Alcoholic portion first breaks, followed by hydrolysis of carbamylated enzyme
  4. 速度是ACh水解的1/106倍
  5. Non-regenerable

Characteristics

  1. 是一種Mixed-type，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

Effect

  1. 增加消化道活性
  2. 分泌增加
  3. 對眼睛：縮瞳，睫狀肌(ciliary muscle)收縮，lens變圓，適合看近的
  4. 骨骼肌：會和NM junction blocker去競爭，使肌肉不會鬆弛
    （d-tubocurarine antagonist）（d-tubocurarine is a non-depolarizing neuromuscular blocking agent）
  5. Bronchoconstriction
  6. Smooth muscle of urinary bladder contraction
  7. higher dose: hypotension and tachycardia à 心律不整Arrhythmia

Clinical use

治療肌肉無力myasthenia gravis

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10
Q

Organophosphate

A

阻止AChE分解ACh，使副交感興奮; irreversible AChE inhibitor (causing phosphorylation on the esteratic site of the esterase)

can pass through BBB

Interaction with Esterase

  1. 會被血漿中的酶水解 (Non-regenerable)
  2. 速度是ACh水解的1/106倍
  3. Toxicity

· 犬、牛血中的esterase比較少，故容易中毒

· 馬的esterase比較多，比較不容易中毒

Characteristics

  1. Variable forms
  2. Irreversibly phosphorylate the esteratic site
  3. Leading to excessive preservation and accumulation of endogenous Ach
  4. Poisioning: cholinomimetic effect (including skeletal muscle fasciculation, twitching, muscle paralysis subsequently), and death!

Effect

Clinical use

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11
Q

Edrophonium

A

阻止AChE分解ACh，使副交感興奮; reversible AChE inhibitor

四級amine group, so cant pass through BBB

Interaction with Esterase

  1. 四級胺端會和酶的anion端接在一起
  2. Carbamyl group端會和酶的Histamine N端接在一起
  3. 速度是ACh水解速度的1/105倍
  4. Could be regenerated, no hydrolysis is involved

Characteristics

  1. Duration of action非常短10~15 min
  2. Curare (筒箭毒類藥物) antagonist

Little CNS effect

Effect

  1. 增加消化道活性
  2. 分泌增加
  3. 對眼睛：縮瞳，睫狀肌(ciliary muscle)收縮，lens變圓，適合看近的
  4. 骨骼肌：會和NM junction blocker去競爭，使肌肉不會鬆弛
    （d-tubocurarine antagonist）（d-tubocurarine is a non-depolarizing neuromuscular blocking agent）
  5. Bronchoconstriction
  6. Smooth muscle of urinary bladder contraction

Clinical use

  1. 多用於診斷: if IV injection of this agent improves muscle function, myasthenia gravis is indicated and dose of AchE inhibitor should be increased
  2. Anticurare agent抗筒箭毒（d-tubocurarine antagonist）：和NM junction blocker競爭
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12
Q

Pyridostigmine

A

作用 Reversible

化學性

四級化合物 (so can’t pass through BBB)

給藥 Parenteral

作用： 4~6小時（長效）

可用於治療肌無力症

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13
Q

demecarium

A

作用 Reversible

化學性

四級化合物 (so can’t pass through BBB)

給藥 topical

作用： 4~6小時（長效）

可用於治療青光眼

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14
Q

carbaryl

A

作用 Reversible

化學性

四級化合物 (so can’t pass through BBB)

給藥 外用

作用：

和propoxur均可殺外寄生蟲，使蟲副交感過度興奮

（做成頸圈、粉狀、洗髮精）

和有機磷中毒Organophosphate一樣

（中毒不可用COMT解毒，而是要用atropine，因為是 reversible類的）

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15
Q

Hemicholinium：

A

阻止 chilone 入突觸，減 少合成

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16
Q

Vesamicol：

A

減少ACh 進入儲存泡，也 減少釋出

17
Q

cholinergic receptor for

  1. heart
  2. glands
  3. 血管内皮
A
    1. M2 (Gi) : in low dose being activated, so reducing heart rate
    1. M3 (Gq)

Glands: M1/M3 (both positive response)

but note equine’s sweat gland is b2 (adrenergic)

  1. endothelium : M3. release NO to dilate causing vasodilation in presence of Ach
18
Q

Arecoline Muscarine Pilocarpine

what are them

compare the CNS effect

A

Muscarinic agonist (due to blockage of nicotinic 特性）

only muscarine is 4級amine, so cant cross BBB

Pilocarpine毛果芸香：類似carbachol

19
Q

which AchE inhibitor is can affect CNS

A

Physostigmine: 三級amine

有機磷：本來就是脂溶性

neostigmine, endrophonium cant

20
Q

toxicity to physostigmine

A

 犬、牛血中的 esterase 比較少， 故容易中毒
 馬的 esterase 比較 多，比較不容易中 毒

21
Q

which AchE inhibitor is mix typed

A

neostigmine

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）

22
Q

which AchE inhibitor has very short duration of acting

A

endrophonium (IV only)

23
Q

和 propoxur 均可殺外寄 生蟲，使蟲副交感過度興 奮
（做成頸圈、粉狀、洗髮 精）

A

carbaryl

Pharmacy - sem2 (14 decks)

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