安徽医科大学：《药理学》课程教学资源（PPT课件讲稿）M受体阻断药——阿托品

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MUSCARINIC ANTAGONIST ATROPINE 阿托品 Teacher. Lanlan zhou 周兰 Department: Pharmacology 药理

ATROPINE 阿托品 Teacher: Lanlan Zhou 周 兰 兰 Department: Pharmacology 药 理 MUSCARINIC ANTAGONIST

Atropine, block muscarinic receptors, causing inhibition of all muscarinic functions Source and chemistry: alkaloid 生物碱 Stramonium曼陀罗 Belladonna颠茄 thron apple(曼陀罗)

Atropine, block muscarinic receptors, causing inhibition of all muscarinic functions. thron apple (曼陀罗) 【Source and chemistry】 : alkaloid 生 物 碱 Stramonium 曼陀罗 Belladonna 颠茄

Mechanism: block muscarenic receptors Atropine has a high affinity for muscarinic receptors Atropine is both a central and peripheral muscarinic blocker Atropin 可● Acetyicholine Muscarine Competition of atropine with acetycholine for the Mr

【 Mechanism 】: block muscarenic receptors Atropine has a high affinity for muscarinic receptors. Atropine is both a central and peripheral muscarinic blocker. Competition of atropine with acetycholine for the MR

( Pharmacokinetics 药动学 Absorption: readily Distribution: blood brain barrier Metabolism: partially by the liver 4 Elimination: primarily in the urine 今Half-life:4 hours Its general actions last about 4 hours except when placed topically in the eye, where the action may last for days

药动学 ❖ Absorption: readily ❖ Distribution: blood brain barrier ❖ Metabolism: partially by the liver ❖ Elimination: primarily in the urine ❖ Half-life : 4 hours Its general actions last about 4 hours except when placed topically in the eye, where the action may last for days. 【 Pharmacokinetics 】

I Drug Actions I earn by heart. MYDR LASIS 1. Eye: mydriasis散瞳 unresponsiveness to light cycloplegia调节麻痹 Eye treated intraocular pressure with atropine 2. Gastrointestinal(G1):胃肠道 Reduce activity of the gl tract -antispasmodic Hydrochloric acid production is not affected

1.Eye: ❖ mydriasis 散瞳 ❖ unresponsiveness to light ❖ cycloplegia 调节麻痹 ❖ intraocular pressure 2. Gastrointestinal (Gl ): 胃肠道 ❖ Reduce activity of the Gl tract —antispasmodic Hydrochloric acid production is not affected MYDRIASIS Eye treated with atropine 【 Drug Actions 】

3. Cardiovascular: divergent effects depending on 心血管 the e dose ow doses> Cardiac rate(Bradycardia) → blockade of the m1(位于突触前膜)→ACH higher doses-Cardiac rate( Tachycardia → blocked the mr(位于突触后膜) at toxic levels- Arterial blood pressure is affected dilate the cutaneous vasculature

3.Cardiovascular: divergent effects depending on 心血管 the dose ❖ Low doses →Cardiac rate (Bradycardia) → blockade of the M1（位于突触前膜）→ACH ❖ higher doses → Cardiac rate ( Tachycardia ) →blocked the MR（位于突触后膜） ❖ at toxic levels→Arterial blood pressure is affected → dilate the cutaneous vasculature

4. Urinary systen:泌尿系统 Reduce hypermotility states of the urinary bladder 5. Secretions:腺体分泌 Locks the salivary glands on the oral mucous membranes-> xerostomia Sweat - elevated body temperature f Lacrimal gl glands→ xeropl ophthalmia

4.Urinary system: 泌尿系统 Reduce hypermotility states of the urinary bladder 5.Secretions: 腺体分泌 ❖ Rlocks the salivary glands on the oral mucous membranes → xerostomia ❖ Sweat →elevated body temperature ❖ Lacrimal glands →xerophthalmia

Therapeutic uses 临床应用 1. Ophthalmic:眼 Measurement of refractive errors s Induce an attack to narrow angle glaucoma 2. Antispasmodic agent:解痉剂 Atropine is used as an antispasmodic agent to relax the gastrointestinal tract and bladder Enuresis->among children

1.Ophthalmic: 眼 ❖ Measurement of refractive errors ❖ Induce an attack to narrow angle glaucoma. 2.Antispasmodic agent: 解痉剂 ❖ Atropine is used as an antispasmodic agent to relax the gastrointestinal tract and bladder. ❖ Enuresis → among children 【 Therapeutic uses 】 临床应用

3. As antidote for cholinergic agonists:解毒剂 ☆ Organophosphate有机磷中毒 Mushroom poisoning蘑菇中毒 Amanita muscaria 毒蝇鹅膏菌:有毒,含毒蝇碱 4. Antisecretory agent:抗分泌剂 Block secretions in the upper and lower respiratory tracts prior to surgery

3.As antidote for cholinergic agonists:解毒剂 ❖ Organophosphate 有机磷中毒 ❖ Mushroom poisoning 蘑菇中毒 4. Antisecretory agent : 抗分泌剂 Block secretions in the upper and lower respiratory tracts prior to surgery. Amonita muscaria 毒蝇鹅膏菌:有毒,含毒蝇碱