cholinergic antagonists-1509
孕妇禁服的药物（Drugsforpregnantwomen）
孕妇禁服的药物（Drugs for pregnant women）There are many taboos in pregnant women medication. Because some drugs are more harmful to the fetus, and even lead to fetal malformations. There are many kinds of teratogenic agents, usually with the following drugs:1. Antibiotics. Such as tetracycline, oxytetracycline, streptomycin, gentamicin, neomycin and so on. Tetracycline, oxytetracycline may cause fetal short limb malformations, congenital cataract, fontanelle bulge, late pregnancy taking can cause childhood enamel hypoplasia; streptomycin, gentamicin drugs can damage the fetus eighth of the brain, resulting in congenital deafness, also can damage the kidney function; neomycin can make fetal bone dysplasia, parallel to kidney, pulmonary artery stenosis, congenital cataract, intellectual disability.2. Antimalarial drugs. Such as quinine, chloroquine, pyrimidine, can cause multiple malformations of the fetus. Such as deafness, limb defect, hydrocephalus and so on.3, the treatment of diabetes drugs. Such as chlorine sulfur C, McCann, urine sugar, equal, can cause limb malformation, cleft lip, stillbirth etc..4. Barbiturates and other sedative hypnotic drugs. Such as phenytoin, primidone, stability, limb, facial deformity and can cause brain development.5. Anticancer drugs. Such as actinomycin D, cyclophosphamide, 5 - fluorine Wo pyrimidine, thiotepa, can cause anencephaly,hydrocephalus, cleft palate, cleft lip, kidney and ureter defect, deformity of limbs and eyes.6. Hormone drugs. Such as diethylstilbestrol, progesterone, androgen, cortisone. Oral contraceptives cause malformations of fetal genital organs. Such as female fetal masculine, Yang pedicle hypertrophy, labia fusion, male fetal urethral following abnormalities.7. Anticoagulant drugs. Such as heparin, coumarin, aspirin, salicylic acid, etc. can also teratogenic, and can induce hemorrhagic diseases. In short, pregnancy should pay attention to avoid drug abuse, but in case of emergency situations endanger the safety of pregnant women, to medication, should be to save the life of the pregnant woman, when emergency situations in the past, should prompt a reduction or withdrawal. The idea that the fetus was refused medication was wrong. If the pregnant woman had a dangerous life, the fetus would talk about He Anquan. Therefore, in pregnant women medication problems, should distinguish between the primary and secondary contradictions, comprehensive consideration.1. penicillin: safer, including broad-spectrum penicillins, such as piperacillin. Oral, intramuscular, intravenous drip can be used for pregnant women. Warning: according to the recommended dosage, can not be excessive.2.: the same medicine and bacteria to erythromycin and roxithromycin, yarn, high molecular weight, is not easy to reach the fetus through the placenta, penicillin allergy can use the drug of choice for chlamydia and Mycoplasma infection.3. cephalosporin: there is no teratogenic effect at present.Tips: dangerous antibiotics ReportSome antibiotics can not be used by pregnant women because of their different side effects:Tetracycline: can cause yellow brown pigmentation of teeth, or storage in the fetal skeleton, but also can cause acute fatty liver and renal insufficiency in pregnant women.Gentamicin: kanamycin, and so on can cause damage to the fetal auditory nerve and kidney.Chloramphenicol: cause grey baby syndrome.Conclusion compound sulfamethoxazole and sulfamethoxazole tablets can cause neonatal jaundice, and can also antagonize folic acid.Furan gall bites: women suffering from urinary tract infection often choose, because it can cause hemolysis, should be used with caution.There is no report on the vancomycin: Although fetal risk, but renal toxicity to pregnant women, ototoxicity.The ciprofloxacin, norfloxacin, ofloxacin, irreversible arthritis occurred in the dog experiment.The anti tuberculosis drug use: when considering the pros and cons according to their size please ask the doctor.9 antifungal drugs: clotrimazole, nystatin, griseofulvin, pregnant women are not the best.The antiviral: do not advocate for pregnant women.4. metronidazole: insecticide, the treatment of Trichomonas infection, advocated early pregnancy does not use.5.: the treatment of Toxoplasma gondii infection, no adverse effects on the fetus.6. anthelmintic: animals have teratogenic effect, should be used with caution.7. digoxin: cardiac drug,It is easy to pass through the placenta and has no obvious adverse effect on the fetus, and the pregnant women with heart failure can be used.8. beta blockers: a report of fetal retardation.9. antihypertensive drugs: definite teratogenic effects of pregnant women is angiotensin converting enzyme inhibitors, such as Kato Pury, angiotensin II receptor antagonists such as losartan, other types of drugs such as calcium antagonists (on behalf of the heart medicine education, cause uterine blood flow can be reduced, diuretic administration can reduce thenear term should be used with caution, the cause of neonatal platelet work experiment acetazolamide limb deformity, pregnant women do not use.10. drugs for the treatment of asthma: such as tea, epinephrine, sodium citrate, prednisone, no teratogenic effect.11. anticonvulsant drugs: the incidence of fetal congenital malformations was 2-3 times higher than that of women who took anticonvulsant drugs during pregnancy. Commonly used phenytoin sodium, C Masi Bing, trimethyl ketone, valproic acid and so on.12. antipsychotic drugs have teratogenic effects.13.: sedative drugs such as diazepam, estazolam, individual teratogenic effect.14. analgesic: acetaminophen can produce hepatotoxicity. Aspirin may be accompanied by oligohydramnios and premature closure of fetal ductus arteriosus. Bloven, Nai Pusheng, indomethacin can cause fetal arterial contraction leads to pulmonary hypertension and oligohydramnios, after 34 weeks of pregnancy should not use indomethacin, can cause fetal intraventricular hemorrhage, bronchopulmonary dysplasia and adverse effects of necrotizing enterocolitis.15. antiemetic drugs: no deformity and increasing the service road.16. antitumor drugs: a clear teratogenic effect.17.: immunosuppressant azathioprine, cyclosporine has obvious toxicity on mother and infant.18. vitamin A: a large number of use can cause birth defects, the smallest human teratogenic quantity is 25000-50000iuld.19. vitamin A isomer: the treatment of skin diseases, retinoic acid in the embryonic phase of medication can produce a variety of malformations.20. acitretin (aromatic retinoic acid): for the treatment of psoriasis, half-life is very long, withdrawal of drugs in >2 years, there are still drug testing, so at least 2 years of drug withdrawal can be conceived.The 21. hormone class: albendazole, diethylstilbestrol, should not be used for pregnant women, oral contraceptive sand dune degree has a positive teratogenic effect.The standard of risk for pregnancy was issued by the American drug and Food Administration (FDA) during pregnancy:Type A: control studies showed no harm. It has been proved that this kind of medicine has no adverse effects on human fetus, and is the safest.Class B: no evidence of harm to human beings. Animal experiments are harmful to fetal animals, but have not been proven to be harmful to the fetus or animal experiments are harmless to the fetus, but there is no adequate study in humans.Class C: non exception hazards. Animal experiments may be harmful or lack of research on fetal animals, but lack of relevant studies in humans, but the benefits for pregnant women are greater than the harm to the fetus.Class D: harm to the fetus. Market research or research confirms that it is harmful to the fetus, but the benefits for pregnant women outweigh the risks to the fetus.Class X: forbidden during pregnancy. In human or animal studies, or market research shows that the harm to the fetus more than the benefit of pregnant women, pregnancy prohibited drugs.Grade standard of commonly used drugs:Antihistamines:Chlorpheniramine (B), Simiti Martin (B), diphenhydramine (B) and promethazine (C)Two. Anti infective drugs:1. anthelmintic: gentian violet (C)2. antimalarial drug: chloroquine (D)3. Trichomonas agents: metronidazole (B)4. antibiotics: amikacin (C), gentamicin (C), kanamycin (D), neomycin (D),Cephalosporins (B), streptomycin (D), penicillins (B), tetracycline (D) and oxytetracycline (D),Chlortetracycline (D) and Bacillus peptide (C), chloramphenicol (C), erythromycin (B), Lincomycin (B) and stickyActinomycin B (B) and vancomycin (C)5. other antibiotics: SMZ-TMP (B/C) and trimethoprim (C), furazolidone, nitrofurantoin (C)Cause (B)6. anti tuberculosis drugs: ethambutol (B), isoniazid (C), Li Fuping (C), and salicylic acid (C)7. antifungal agents: clotrimazole (C), miconazole (C), nystatin (B)8. antiviral agents: amantadine (C), adenosine arabinoside (C), ribavirin (X), C, and noneCyclic guanosine (C)Three. Antineoplastic agents:Bleomycin (D), cyclophosphamide (D), D, cisplatin (D), cytarabine (D), and moreLincomycin (D), thiotepa (D) and daunorubicin (D), adriamycin(D) and 5-fluorouracil (D), nitrogenMustard (D), Ma Falan (D), methotrexate (D), vincristine (D)Four. Autonomic nervous system drugs:1. cholinergic drugs: acetylcholine (C) and neostigmine (C)2. anticholinergic drugs: atropine, belladonna (C) (C), Proulx Bernd Sin (C)3. adrenergic drugs: epinephrine (C), norepinephrine (D), ephedrine (C), and isoproterenolC, D, Dobaamine (C), dobutamine (C), B, and hydroxyEphedrine (B)Five. Central nervous system drugs:1. central stimulant: caffeine (B)2. antipyretic analgesics: acetylsalicylic acid (C/D), Fi Bernard Shiden (B), sodium salicylate (C/D)3. non steroidal anti-inflammatory drugs: indomethacin (B/D)4.: analgesic codeine, morphine (B/D) (B/D), opioid (B/D) and pethidine (B/D), narloKetone (C)5. sedative, hypnotic: amobarbital (C), Babito (C), Bernd Bobby Toy (B), chloral hydrate (C), ethanol (D/X), diazepam (D) and nitro (C)6. diazepam: droperidol (C) and chlorpromazine (C)7. antidepressants: doxepin (C)Six. Cardiovascular drugs:1.: digitalis cardiac glycosides (B) (B), digoxin, digitoxin(B), quinidine (C)2. antihypertensive drugs: clonidine (C), Ca Guido Ba (C), B,D and prazosin(C)3. vasodilator drugs: C, Pan Shengding (C), two isosorbide dinitrate (C),Result (C)Seven. DiureticsHydrochlorothiazide (D) and ethacrynic acid (D) and furosemide (C), Gan Luchun (C), triamterene (D)Eight. Digestive system drugs:Compound Camphor Tincture (B/D)Nine. Hormones:1. adrenal cortex hormone: cortisone (D), Batamison (C), dexamethasone (C), hydrocortisone (prednisone)B)2. estrogen: diethylstilbestrol (X), estradiol (D), oral contraceptive pill (D)3. progesterone: progesterone (D)4. hypoglycemic drugs: insulin (B), sulfonylurea (D), methyl sulfonyl Ding Niao (D)5.: antithyroid drug propylthiouracil (D) and methimazole (D)This paper is reproduced from QQ spacePenicillin: can destroy fetal red blood cell, cause serious jaundice, cause fetal death. Yangzhou First People's Hospital gynecology YulinStreptomycin: congenital deafness, skeletal deformity.Tetracycline induced amelogenesis imperfecta, skeletal and heart malformations, congenital cataract, short limb or defect (e.g. four fingers), neonatal jaundice, the most serious personcan appear kernicterus and even death.Oxytetracycline and doxycycline: make fetal short limb deformity.Chloramphenicol induced blood circulation disorders, respiratory insufficiency, cyanosis, neonatal abdominal distension (i.e. "gray baby syndrome"). If used in the end of pregnancy, it can cause neonatal thrombocytopenia, aplastic anemia or fetal death.Cara: deafness.Erythromycin: congenital cataract, limb deformities and so on.Gentamicin: fetal ear damage, and even lead to congenital gastric vascular malformation and polycystic kidney.Sulfa drugs (mainly based on long-acting sulfonamides and antibacterial synergist): hyperbilirubinemia, brain nuclear jaundice, deformity.Heroin: respiratory depression and death in the fetus.Pethidine: caused by neonatal asphyxia.Morphine: the inhibition of neonatal respiration and the withdrawal of the newborn like withdrawal, such as taking a week before delivery, can cause neonatal spasms, excitement and shrill cry.Aspirin: cause fetal small, malformation, cause neonatal prothrombin reduction group and bleeding and liver detoxification dysfunction.Finasteride and paracetamol: neonatal hypercholesterolemia.Indomethacin: cause jaundice and aplastic anemia.Barbiturate induced fetal heart: congenital malformation, facial and hand retardation, cleft lip and cleft palate.Primidone: fetal finger and toe deformities, late pregnancy can cause fetal asphyxia, taking hemorrhage and brain injury.Sleeping pills: malformations.Valium, tranquility, insomnia, and sleep induction can cause fetal abnormalities and become pregnant women.Activin induced cleft palate.Insulin: causes miscarriage, premature birth, stillbirth, and other congenital malformations.Progesterone: masculine female fetus.Cortisone and prednisone: fetal cleft lip and cleft palate. Cortisone can also cause fetal absence, premature delivery, premature death.Progesterone and testosterone: abnormalities of fetal externalgenital organs.Vitamin D: large doses, can cause fetal hypercalcemia and mental retardation.Vitamin K: a large number of taking, can cause hyperbilirubinemia, nuclear jaundice.Vitamin B6: a large number of taking, can cause neonatal vitamin B6 dependence, convulsions. Vitamin B6 derivatives naofuxin, caused by cleft lip in animal experiments, should be used with caution.Vitamins: if taken during pregnancy in the first three months of the risk of neurological deficiency in infants go through thick and thin together up to 60%.Promethazine hydrochloride: fetal limb deformities.Antimalarial drugs quinine, chloride, and pyrimidine: can cause hydrocephalus, bulging, cleft palate, renal arrest, development or malformation, retinal damage.Chlorpheniramine, Meclozine, An Qimin, and other anti allergy medicine diphenhydramine Dramamine: in addition to potentially induced cleft palate, cleft lip, short limb function, can also cause liver poisoning and brain injury, neonatal respiratory inhibition.Fluorouracil, cyclophosphamide, can cause fetal limb, nose, palate, urinary tract deformity and death.Methotrexate: no fetal brain, hydrocephalus, encephalocele, cleft lip, cleft palate, or limb deformities.Hydroxyurea and busulfan induced multiple malformations.Bai Ning: caused by the injury of central nervous system and brain.6- purine, testosterone propionate and L- L-asparaginase: fetal malformations.It can cause kidney and ureter defect.Fetal death caused by pethidine, 5-, fluorouracil, mitomycin C and colchicine. It is safer to use these antineoplastic agents after sixteenth weeks of pregnancy.Coumarin drugs: can cause fetal skin bleeding spots, brain disorders, placental abruption, bone and facial deformity, mental retardation or fetal death.Warfarin: nasal dysplasia, malformations.D860, a kind of sulfonylurea, can induce abortion and premature delivery, and has the effect of promoting distortion.MTU, propylthiouracil, methimazole, jiakangping, potassium iodide: induced hypothyroidism, cretinism, delayed ossification and hypospadias.Hydrochlorothiazide or cyclopenthiazide: can cause neonatal thrombocytopenia.Reserpine: cause neonatal poisoning, nasal congestion, respiratory obstruction, and even death due to lack of oxygen.Caffeine causes cleft lip and palate.Ether: a large number of continuous use, can cause fetal death.All arsenic containing drugs: all cause fetal death.Polymyxin E, B and vancomycin: taking too much time, so that pregnant women suffered from acute renal failure, the children are susceptible to neuromuscular blockade, ataxia, vertigo, seizures and mouth week after birth 3 years paresthesia. Vancomycin can also cause temporary or permanent hearing loss in infants.Rifampicin: fetal malformation.Anti fungal drugs griseofulvin, amphotericin B, nystatin, clotrimazole: serious adverse reactions of pregnant women's nervous system, hematopoietic system, liver and kidney function. Griseofulvin also led to abortion and teratism.Triamterene (three methotrexate): liver damage, change of maternal blood.Hydrochlorothiazide: adverse effects on the fetus.Furosemide: nausea and vomiting, diarrhea, drug rash, itching, blurred vision, postural hypotension and even water and electrolyte disorders in pregnant women and parturient.Diuretics: can cause transient hearing loss and sometimes develop permanent hearing loss.Other: alcoholism pregnant women newborns showed withdrawal like inhibitory state; multiple abnormalities can cause fetal alcohol. The contraceptive pill should be pregnant after six months of complete withdrawal of the drug, so as to avoid the birth of malformation or dementia caused by improper medication。
胆碱能药物
第八页，编辑于星期日：十八点 十四分。
M受体激动剂的临床应用
M样作用：引起心肌收缩力减弱，心率减慢；消化
道、呼吸道及其他脏器平滑肌收缩；动脉血管平滑 肌松弛，血管舒张，但大剂量又可使静脉血管收缩； 腺体分泌增加。 M受体激动剂属于直接作用于胆碱受体的拟胆碱药。 M受体激动剂主要用于手术后腹气涨、尿潴留；降 低眼内压，治疗青光眼；治疗阿尔茨海默症；大部 分胆碱受体激动剂还具有吗啡样镇痛作用，可用于 止痛。
Bethanechol的手性
CH3
H O
CH2N+(CH3)3
H
H3C O
CH2N+(CH3)3
O
NH2
O
NH2
S-(+)-Bethanechol
R-(-)-Bethanechol
S-异构体的活性大大高于R-异构体
第十四页，编辑于星期日：十八点 十四分。
生物碱类M受体激动剂
HO
H3C O
H3C
N+(CH3)3 O
乙酰胆碱酯酶单体为椭球型分子，其分子结构最显著 的特点是在表面有一向内凹陷的深而窄的峡谷。
其催化三联体的构成（Ser-His-Glu）与通常丝氨酸 蛋白酶（Ser-His-Asp）有所不同。
AChE活性中心位于谷底，由三个主要区域组成：
酯解部位 阴离子部位
疏水性区域
第二十四页，编辑于星期日：十八点 十四分。
H3C
O
N+(CH3)3
Muscarine
N CH3 N
Nicotine
M受体：M1，M2，M3，M4，M5 N受体：N1，N2
第四页，编辑于星期日：十八点 十四分。
文档：拟胆碱药和抗胆碱药
拟胆碱药和抗胆碱药(Cholinergic and Anticholinergic Drugs)一、单项选择题1．下列药物中哪一个属于M胆碱受体激动剂A．Physostigmine B．Galantamine C．Scopolamine D．Pilocarpine2．下列哪种叙述与胆碱受体激动剂不符A．乙酰胆碱的乙酰基部分为芳环或较大分子量的基团时，转变为胆碱受体拮抗剂B．乙酰胆碱亚乙基桥上β位甲基取代，由于M样作用大大增强，故成为选择性M受体激动剂C．Bethanechol Chloride作用较乙酰胆碱强而持久D．中枢M胆碱受体激动剂是潜在的抗老年痴呆药物3．Neostigmine Bromide的化学名是A．氯化2-[(氨基甲酰)氧基]-N,N,N-三甲基-1-丙铵B．溴化3-[[(二甲氨基)甲酰]氧基]-N,N,N-三甲基苯铵C．N-甲基-N-(1-甲基乙基)-N-[2-[(9H-呫吨-9-甲酰)氧基]乙基]-2-丙胺溴化物D．1,1'-[(2β,3α,5α,16β,17β)-3,17-双-(乙酰氧基)雄甾烷-2,16-二基]双[1-甲基哌啶鎓]二溴化物4．下列有关乙酰胆碱酯酶抑制剂的叙述不正确的是A．Neostigmine Bromide是可逆性乙酰胆碱酯酶抑制剂，其与AChE结合后形成的二甲氨基甲酰化酶，水解释出原酶需要几分钟B．Neostigmine Bromide结构中N, N-二甲氨基甲酸酯较Physostigmine结构中N-甲基氨基甲酸酯稳定C．中枢乙酰胆碱酯酶抑制剂可用于抗老年痴呆D．有机磷毒剂也是可逆性乙酰胆碱酯酶抑制剂5．下列哪个与Atropine Sulfate不符A．化学结构为二环氨基醇酯类B．具有左旋光性C．显托烷生物碱类鉴别反应D．碱性条件下易被水解6．Atropine 的水解产物是A．山莨菪醇和托品酸B．托品（莨菪醇）和左旋托品酸C．托品和消旋托品酸D．莨菪品和左旋托品酸7．以下叙述哪个不正确A．托品（莨菪醇）结构中C1、、C3、C5为手性碳原子，具旋光性B．托品酸结构中有一个手性碳原子，具旋光性C．山莨菪醇结构中C1、C3、C5、C6为手性碳原子，具旋光性D．莨菪品（东莨菪醇）结构中有三个手性碳原子，由于内消旋无旋光性8．下列合成的M胆碱受体拮抗剂分子中，具有9-呫吨甲酰基结构的是A．格隆溴铵B．盐酸苯海索C．溴丙胺太林D．甲溴贝那替嗪9． Pancuronium Bromide 与下列哪个药物的用途相似A ．甲睾酮B ．奥美溴铵C ．苯丙酸诺龙D ．维库溴铵 10． 下列哪项不符合氯琥珀胆碱的性质A ．为酯类化合物，难溶于水B ．为季铵盐类化合物，极易溶于水C ．在血浆中极易被酯酶水解，作用时间短D ．为去极化型肌松药 11． 下列有关M 胆碱受体的描述哪个不正确A ．蕈毒碱是M 受体激动剂B ．M 受体属于G 蛋白偶联受体家族C ．当乙酰胆碱与M 受体结合时，心收缩力减弱，心率减慢；腺体分泌增强D ．M 受体激动时，动脉血管收缩 12． 下列有关N 胆碱受体的描述哪个不正确A ．烟碱是N 受体激动剂B ．外周N 受体属于配体门控受体家族，本身既是受体，又是离子通道C ．乙酰胆碱与N 1受体结合可使自主神经节兴奋，血压降低D ．乙酰胆碱与N 2受体结合可使骨骼肌收缩 13． 下列生物碱何者为蕈毒碱A ．B ．C ．D ．H 3+(CH 3)3NNCH 3NNOH 3CCH 3ONNCH 3CH 3OOHNH 3C CH 314． 下列生物碱何者为烟碱A ．B ．C ．D ．CH 33H 3NNCH3H 3+(CH 3)315． 下列哪个是氯贝胆碱A ．B ．C ．D ．NNH 2H 2N OOCH 3N +(CH 3)3 Cl - H 3C OOCH 3N +(CH 3)3 Cl -N ON(CH 3)2CH 3O+Br -16． 下列结构中哪个是 AnisodamineA ．B ．C ．D ．NO OHOCH 3NCH 3NCH 3OOHONCH 317． 哌仑西平的结构是A ．B ．C ．D ．H NNN OON N CH 3H NNOON NCH 3S CH 3 H NNOONNCH 3CH 3Br -N O SS CH 3O H 3C OH +二、填空题1． 乙酰胆碱的生物合成在 内完成，由丝氨酸脱羧酶将 脱羧，再经胆碱N-甲基转移酶催化 生成胆碱，然后由胆碱乙酰基转移酶催化，将乙酰基由乙酰辅酶A 转移至胆碱，从而合成乙酰胆碱。
药理学中英文对照表
Aacetaminophen 对乙酰氨基酚acetylcholine (Ach) 乙酰胆碱acetylsalicylic acid 乙酰水杨酸adrenaline/epinephrine (Adr) 肾上腺素amantadine 金刚烷胺amobarbital 异戊巴比妥anisodamine 山莨菪碱arecoline 槟榔碱aspirin 阿斯匹林atropine 阿托品Bbarbiturates 巴比妥类benzodiazepines (BDZ) 苯二氮卓类bromocriptine 溴隐亭buspirone 丁螺环酮（布司匹隆）Ccarbachol 卡巴胆碱carbamazepine 卡马西平（酰胺咪嗪）carbidopa 卡比多巴chlorpromazine (wintermin) 氯丙嗪（冬眠灵）chloral hydrate 水合氯醛codeine 可待因Ddiazepam 地西泮dobutamine 多巴酚丁胺dolantin 度冷丁dopamine (DA) 多巴胺Eephedrine 麻黄碱estazolam 艾司唑仑（舒乐安定）ethosuximide 乙琥胺Fflurazepam 氟西泮Ggalanthamine 加兰他敏Iibuprofen 布洛芬imipramine 丙咪嗪indomethacin 吲哚美辛isoprenaline 异丙肾上腺素Llamotrigine 拉莫三嗪levodopa 左旋多巴lithium carbonate 碳酸锂Mmagnesium sulfate 硫酸镁mecamylamine 美卡拉明（美加明）metaraminol (aramine) 间羟胺（阿拉明）methaone 美沙酮morphine 吗啡muscarine 毒蕈碱Nnaloxone 纳洛酮neostigmine 新斯的明nimesulide 尼美舒利nitrazepam 硝西泮noradrenaline (NA) 去甲肾上腺素Oorganophosphates 有机磷酸酯类oxyphenbutazone 羟布宗PPAM-I 派姆paracetamol 扑热息痛pentazocin 喷他佐辛pethidine 派替啶phenbarbital 苯巴比妥phenobarbital 苯巴比妥phenoxybenzamine 酚苄明phentolamine 酚妥拉明phenylbutazone 保泰松phenytoin sodium (dilantin) 苯妥英钠（大仑丁）physostigmine (eserin) 毒扁豆碱（依色体）pilocarpine 毛果芸香碱（匹鲁卡品）pralidoximen chloride 氯解磷定pralidoximen iodide 碘解磷定primidone 扑米酮propranolol 普萘洛尔Ssalbutamol 沙丁胺醇scoline 司可林scopolamine/hyoscine 东莨菪碱secobarbital 司可巴比妥selegiline 司来吉兰sodium valprate 丙戊酸钠succinylcholine/suxamethonium 琥珀胆碱Tterbutaline 特布他林thiopental 硫喷妥trihexyphenidyl (antane) 苯海索（安坦）tubocurarine 筒箭毒碱Vvalium 安定venlafaxine 文拉法新Zzolpidem 唑吡坦zopiclone (imovane) 佐匹克隆（依梦返）药理学英文药名总结Cholinergic Drugsacetylcholine (Ach) 乙酰胆碱carbachol 卡巴胆碱pilocarpine 毛果芸香碱（匹鲁卡品）muscarine 毒蕈碱arecoline 槟榔碱neostigmine 新斯的明physostigmine（eserin）毒扁豆碱（依色体）galanthamine 加兰他敏Organophosphates Poisoning and Cholinesterase Reactivators organophosphates 有机磷酸酯类pralidoximen iodide 碘解磷定PAM－I 派姆pralidoximen chloride 氯解磷定Muscarinic Antagonistsatropine 阿托品anisodamine 654 山莨菪碱scopolamine，hyoscine 东莨菪碱Nicotinic Antagonists mecamylamine 美卡拉明，美加明succinylcholine，suxamethonium 琥珀胆碱scoline 司可林tubocurarine 筒箭毒碱Adrenergic Drugsadrenaline，epinephrine，Adr 肾上腺素dopamine，DA 多巴胺ephedrine 麻黄碱noradrenaline，NA 去甲肾上腺素metaraminol（aramine）间羟胺（阿拉明）isoprenaline 异丙肾上腺素dobutamine 多巴酚丁胺salbutamol 沙丁胺醇terbutaline 特布他林Antiadrenergic Drugsphentolamine 酚妥拉明phenoxybenzamine 酚苄明propranolol 普萘洛尔Anixiolytic and Hypnotics benzodiazepines BDZ 苯二氮卓类diazepam 地西泮valium 安定flurazepam 氟西泮nitrazepam 硝西泮estazolam 艾司唑仑，舒乐安定buspirone 丁螺环酮，布司匹隆zopiclone（imovane）佐匹克隆（依梦返）zolpidem 唑吡坦barbiturates 巴比妥类phenbarbital 苯巴比妥amobarbital 异戊巴比妥secobarbital 司可巴比妥thiopental 硫喷妥chloral hydrate 水合氯醛Antiepileptic and Anticonvulsive drugs phenytoin sodium（dilantin）苯妥英钠（大仑丁）carbamazepine 卡马西平，酰胺咪嗪lamotrigine 拉莫三嗪phenobarbital 苯巴比妥primidone 扑米酮ethosuximide 乙琥胺sodium valprate 丙戊酸钠magnesium sulfate 硫酸镁Drug Treatment of Psychosis chlopromazine（wintermin）氯丙嗪（冬眠灵）imipramine 丙咪嗪venlafaxine 文拉法新lithium carbonate 碳酸锂Antiparkinsonism Drugslevodopa 左旋多巴carbidopa 卡比多巴selegiline 司来吉兰bromocriptine 溴隐亭amantadine 金刚烷胺trihexyphenidyl（antane）苯海索（安坦）Antipyretic-Analgesic and Antiinflammatory Drugs acetylsalicylic acid 乙酰水杨酸aspirin 阿斯匹林acetaminophen 对乙酰氨基酚paracetamol 扑热息痛phenylbutazone 保泰松oxyphenbutazone 羟布宗indomethacin 吲哚美辛ibuprofen 布洛芬nimesulide 尼美舒利Analgesics morphine 吗啡codeine 可待因pethidine 派替啶dolantin 度冷丁methaone 美沙酮pentazocin 喷他佐辛naloxone 纳洛酮。
吉大生科院的药物化学名词解释
吉大名词解释第二章1、巴比妥类药物（barbiturates agents）：具有5，5二取代基的环丙酰脲结构的一类镇静催眠药。
20世纪初问市的一类药物，主要由于5，5取代基的不同，有数十个各具药效学和药动学特色的药物供使用。
因毒副反应较大，其应用已逐渐减少。
2、内酰胺-内酰亚胺醇互变异构（lactam-lactimtautomerism）：类似酮-烯醇式互变异构，酰胺存在酰胺-酰亚胺醇互变异构。
即酰胺羰基的双键转位，羰基成为醇羟基，酰胺的碳氮单键成为亚胺双键，两个异构体间互变共存。
这种结构中的亚胺醇的羟基具有酸性，可成钠盐。
3、锥体外系反应（effects of extrapyramidalsystem，EPS）：锥体外系指在中枢锥体系以外的连接大脑皮层、基底神经节、丘脑、小脑网状结构及神经元的神经束和传导系统。
是一套复杂的神经环路。
锥体外系的反应指震颤麻痹，静坐不能、急性张力障碍和迟发性运动障碍等神经系统锥体外系的症状，常是抗精神病药物的副反应。
?4、非经典的抗精神病药物（atypical antipsychotic agents）：近年来问世的一些抗精神病药物。
和传统的吩噻嗪类和氟哌啶醇药物不同，其拮抗多巴胺受体的作用较弱，可能是产生多巴胺和5-羟色胺受体的双相调节作用，其锥体外系的副反应较少，具有明显治疗精神病阳性和阴性症状的作用。
代表药物如氯氮平。
?5、构效关系（structure-activity relationship，SAR）：在同一基本结构的一系列药物中，药物结构的变化，引起药物活性的变化的规律称该类药物的构效关系。
其研究对揭示该类药物的作用机制、寻找新药等有重要意义。
6、选择性5-羟色胺再摄取抑制剂（selective serotonin-reuptake inhibitors，SSRIS）：通过选择性的阻碍突触间隙中的神经递质5-羟色胺的再摄取，提高5-羟色胺的浓度，产生抗抑郁作用的一类药物。
药理学名词解释 三理一免
absorption药物的吸收:药物从用药部位向血液循环中的转运Adrenoceptor agonists肾上腺素受体激动药:一类化学结构与药理作用和肾上腺素`去甲肾上腺素相似作用的药物,与肾上腺素受体结合后可激动受体,产生肾上腺素样的作用adverse reaction不良反应:凡不符合用药目的,并为病人带来不适或痛苦的有害反应afterdepolarization后除极:在一个动作电位中继0相除极后所发生的除极,其频率较快,振幅较小,呈振荡性波动,膜电位不稳定,容易引起异常冲动发放,引起触发活动.根据发生时间的不同,可分为早后除极和晚后除极agonist激动药:既有亲和力又有内在活性的药物,它们能与受体结合并激动受体而产生效应analgesics镇痛药:作用于CNS,能缓解疼痛,用于剧痛的药物Antidepressant drugs抗抑郁症药:用于治疗情绪低落`抑郁消极,使抑郁症状得到缓解的药物Antimanic drugs抗燥狂症药:使躁狂症状得到缓解的药物Antipsychotic drugs抗精神病药:临床上主要用于治疗精神分裂症,对精神失常的躁狂症状也有效的一类药物aspirin asthma阿司匹林哮喘:某些哮喘患者服用阿司匹林或其它解热镇痛药后可诱发哮喘bioavaiabiity生物利用度:药物制剂给药后其中能被吸收进入体循环的相对数量及速度calcium antagonists钙拮抗药:是一类能阻滞钙离子经细胞膜上电压依赖性钙通道进入细胞内`减少细胞内钙离子浓度,从而影响细胞功能的药物,又称钙通道阻滞剂cholinergic risk胆碱能危象:抗胆碱酯酶药如新斯的明治疗重症肌无力,因应用过量可使骨骼肌运动中伴有过多乙酰胆碱堆积,导致持久去极化,加重神经肌肉传递功能障碍,使肌无力症状加重,为胆碱能危象competitive α-receptor blocker竞争性α受体阻断药:酚妥拉明等药物与α受体结合后可拮抗肾上腺素的α型作用,但结合较疏松易于解离,故能竞争性阻断α受体Css稳态血药浓度:按照一级动力学规律消除的药物,其体内药物总量随着不断给药而逐步增多,直至从体内消除的药物量和进入体内的药物量相等时,体内药物总量不再增加而达到稳定状态,此时的血浆药物浓度depolarizing muscular relaxants除极化性肌松药:药物可与运动终板膜上N2胆碱受体结合,产生与乙酰胆碱相似但较持久的除极化,使终板不能对乙酰胆碱起反应而使骨骼肌松弛,此类药物称为dose-effect relationship量效关系:药理效应与剂量一定范围内成比例drngresistance耐药性:指病原体或肿瘤细胞对反复应用的化学治疗药物的敏感性降低,也称抗药性ED50半数有效量:能引起50%实验动物出现阳性反应时的药物剂量elimination药物的消除:药物因分布`代谢`排泄而自血液或机体的清除excitation兴奋: 机体器官原有功能水平的提高exocytosis胞裂外排:当神经冲动到达神经末稍时,钙离子进入神经末稍,促进囊泡膜与突触前膜融合,形成裂孔,通过裂孔将囊泡内容物一并排出至突触间隙,其中递质NA和Ach可与其各自受体结合,产生效应first order elimination一级消除动力学:体内药物在单位时间内消除的药物百分率不变,即单位时间内消除的药物量与血浆药物浓度成正比first pass effect首关效应:药物经肝脏时被肝脏代谢,进入体循环的药量减少GF生长比率:增殖细胞群在肿瘤全细胞群中的比率hepato-enteric circulation肝肠循环:自胆汁排进十二指肠的结合型药物在肠中经水解后再吸收,形成循环idiosyncrasy特异质反应:少数特异质病人对某些药物反应特别敏感,反应性质也可能与常人不同,但与药物固有药理作用基本一致inhibition抑制:机体器官原有功能水平的降低ion channels离子通道:细胞膜中的跨膜蛋白质分子,对某些离子能选择通透,其功能是细胞生物电活动的基础k消除速率常数:体内瞬间消除的百分率LD50半数致死量:能引起50%的实验动物死亡时的药物剂量loading dose负荷剂量:为了使血药浓度迅速达到所需的水平,在常规给药前应用的一次剂量maximum efficacy效能:随着剂量或浓度的增加,效应也增加,当效应增加到一定程度后,若继续增加药物浓度或剂量而其效应不再继续增强,这一药理效应的极限称为最大效应.MBC最低杀菌浓度:体外试验中,药物能够杀灭培养基内细菌生长的最低浓度membrane responsiveness膜反应性:指膜电位水平与其所激发的0相最大上升速率之间的关系.一般膜电位高,0相上升速率快,动作电位振幅大,传导速度快.反之,则传导减慢MIC最低抑菌浓度:体外试验中,药物能够抑制培养基内细菌生长的最低浓度Nervous transmitter神经递质:神经元与下一级神经元或效应期之间通过释放传递信息的化学物质neuromodulator神经调质:由神经组织或非神经组织生成的化学物质,其本质不具有递质活性,不直接引起突触后生物学效应,但能调制神经递质在突触前的释放及突触后细胞的兴奋性,调制突触后细胞对递质的反应noncompetitive α-receptor blocker非竞争性α受体阻断药:酚苄明等药物与α受体结合后形成牢固的共价键,长时间占据受体,可拮抗肾上腺素的α型作用,且该作用是非竞争性的nondepolarizing muscular relaxants非除极化性肌松药:药物可与运动终板膜上N2胆碱受体结合,竞争性阻断乙酰胆碱除极化使骨骼肌松弛,此类药物on-off response开关反应:患者服用左旋多巴后突然出现多动不安,而后又出现全身性或肌强直性运动不能,严重妨碍病人的正常活动,称为PAE抗菌后效应:将细菌暴露于浓度高于MIC的某种抗菌药物后,再去除培养基中的抗菌药,去除抗菌药的一定时间内细菌繁殖不能恢复正常的现象PBPs青霉素结合蛋白:细菌细胞壁粘肽合成酶,即是位于细菌胞浆膜上的特殊蛋白,也是β-内酰胺类抗生素的结合靶点pharmacodynamics药物效应动力学:研究药物对机体的作用及作用原理pharmacokinetics药物代谢动力学:研究药物的体内过程及体内药物浓度随时间变化的规律pharmacology药理学:研究药物与机体作用规律及原理的科学,为临床合理用药防治疾病提供理论基础placebo安慰剂:不具药理活性的剂型potency效价强度:指能引起等效反应（一般采用50%效应量）的相对浓度或剂量,其值越小则强度越大.receptor受体:构成细胞的物质成分,具有严格的立体专一性,能与药物相互作用引起细胞效应reentry折返激动:指一个冲动沿着曲折的环形通路返回到其起源的部位,并可再次激动而继续向前传播的现象.单次折返可引起早搏,连续折返可引起阵发性心动过速.regulative paralysis调节麻痹: 抗胆碱药如阿托品,可阻断眼睫状肌M受体,使睫状肌松弛,悬韧带拉紧,晶状体处于扁平状态,屈光度变小,故不能将近处物体成像在视网膜上,视近物模糊,适于视远物的现象.regulative spasm调节痉挛:抗胆碱药如毛果芸香碱,可激动眼睫状肌M受体,使睫状肌收缩,悬韧带松弛,晶状体变凸,屈光度增加,故不能将远处物体成像在视网膜上,视远物模糊,适于视近物的现象.residual effect后遗效应:指停药后血药浓度已降至阈浓度以下时残存的药理效应.Reye syndrome瑞夷综合症:病毒感染伴有发热的儿童或青年服用阿司匹林后出现一系列反应,有严重肝功能不良合并脑病side reaction副反应:当药物的某一效应用作治疗目的时,其他效应就成为~T1/2半衰期:血浆药物浓度下降一半所需的时间Tachyphylaxis快速耐受性:有些药物,如麻黄碱,短期内反复给药,作用可逐渐减弱therapeutic index治疗指数:药物的LD50/ED50的比值time-concentration时-量曲线:药物在血浆的浓度随时间的推移而发生变化所作的曲线tolerance耐受性:机体在连续多次用药后反应性降低,要达到原来反应必须增加剂量.toxic reaction毒性反应:指在剂量过大或药物在体内蓄积过多时发生的危害性反应Uptake1摄取1:神经摄取,去甲肾上腺素的失活主要依赖于神经末稍的摄取use dependence频率依赖性:指通道开放的频率与药物的阻滞作用呈正相关.即通道开放的频率越频繁,药物的阻滞作用越强.维拉帕米`地尔硫卓有明显频率依赖性,而硝苯地平则无Vd表观分布容积:当血浆或组织内药物分布达到平衡后,体内药物按此时的血浆药物浓度在体内分布时所需体液容积withdrawal reaction停药反应:指突然停药后原有疾病加剧,又称回跃反应.zero order elimination零级消除动力学:药物在体内以恒定的速率消除,即不论血浆药物浓度高低,单位时间而你消除的药物量不变β-内酰胺类抗生素:指化学结构中具有一个β-内酰胺环的一类抗生素.包括青霉素类`头孢菌素类`非典型β-内酰胺类和β-内酰胺酶抑制剂等化疗药物:化疗过程中所用的药物,包括抗微生物药`抗寄生虫药和抗肿瘤药化疗指数: 是衡量化疗药物临床应用和安全性评价的重要参数,一般可用实验动物LD50/ED50表示化学治疗:应用药物对病原体所致疾病进行预防或治疗称为化学治疗学:研究药物`病原体和宿主之间相互作用`作用机制和作用规律的学科戒断症状:反复使用阿片类药物的患者,一旦停药则可出现兴奋`失眠`流泪`出汗震颤`呕吐`腹泻甚至虚脱,意识丧失等抗菌活性: 抗菌药物抑制或杀灭病原菌的能力,可用体外和体内两种试验方法测定抗菌谱:抗菌药物抑制或杀灭病原微生物的范围抗菌药:指能抑制或杀灭细菌,用于预防和治疗细菌性感染的药物,包括人工合成抗菌药和抗生素:微生物的代谢产物,分子量较低,低浓度时能杀灭或抑制其他病原微生物抗生素:是微生物的代谢产物,分子量较低,低浓度时能杀灭或抑制其他病原微生物.包括天然的和人工半合成的抗生素杀菌药:不仅能抑制病原菌的生长繁殖而且具有杀灭作用的药物肾毒性:指药物引起肾脏的中毒表现,可出现蛋白尿`管型尿,严重发生氮质血症及无尿首剂现象:首次应用哌唑嗪后出现低血压`晕厥`心悸等反应细菌的耐药性:指长期或反复用药过程中,特别是滥用药物后,细菌对药物的敏感性下降甚至消失,造成抗菌药物对耐药菌感染的疗效降低或无效心肌肥厚与重构:各种充血性心力衰竭发病过程中,心脏形态结构多种病理变化的总和,其最终发展为心力衰竭药物耳毒性:药物引起的前庭功能和耳蜗神经的损伤,前庭功能的损伤表现为眩晕恶心呕吐`平衡障碍;耳蜗神经损害表现为听力减退或耳聋抑菌药:仅能抑制病原菌的生长繁殖而无杀灭作用的药物正性肌力作用:即加强心肌收缩性,表现为心肌收缩时最高张力和最大缩短速率的提高,使心肌收缩有力敏捷,增加心输出量。
拟副交感神经药课件
• 2.眼科用药 –虹膜睫状体炎
• 松弛,充分休息 • 与缩瞳药交替使用,防粘连 –验光配镜
• 睫状肌充分松弛,晶状体固 定,屈光度测量准确
3.平滑肌痉挛性疼痛
–各种内脏绞痛
–对胃肠绞痛，膀胱刺激症状 效果好，但对胆绞痛、肾绞 痛和输尿管绞痛效果差
• 缓慢性心律失常 –心动过缓、窦房阻滞、房室传 导阻滞
–抑制中枢AChE活性，治疗阿尔 茨海默病
难逆性胆碱酯酶抑制药
• 有机磷酸酯类：与AChE难逆性结 合,Ach大量堆积
• 应用
–杀虫剂 果
敌百虫,敌敌畏,乐
–战争毒气 沙林,塔崩
中毒机制:
与AChE难逆性结合 磷酰化AChE AChE失活 Ach大量堆积
“老化”
• 若不及时解救, 磷酰化AChE可生 成更稳定的化合物
–汗腺分泌减少,机体散热减少
• 扩瞳 • 眼内压升高 • 调节麻痹
睫状肌松弛,退向外缘,悬韧 带拉紧,晶状体变扁平,看近物 模糊,看远物清楚
• 松弛多种内脏平滑肌,尤其对过 度活动和痉挛者更显著
• 缓解胃肠绞痛 • 降低尿道和膀胱逼尿肌张力和收
缩幅度 • 对胆管、输尿管和支气管解痉作
用弱
• 心率加快 –解除迷走神经(胆碱能神经) 对心脏的抑制作用
复） •阿托品: 阿托品化 •胆碱酯酶复活药
胆碱酯酶复活药——解磷定
• 恢复被有机磷酸酯类抑制的AChE活性 磷酰化胆碱酯酶－解磷定复合物
磷酰化解磷定 随尿排出
AChE 被解救出来
• 与体内游离的有机磷酸酯直接 结合
• 迅速控制肌肉震颤，并缓解中 枢作用
• 不能直接对抗积聚的ACh，临 床上与阿托品联用
外周神经系统药物
Choline receptor
毒蕈碱型受体：副交感神经的节后纤维的胆 碱受体对毒蕈碱较为敏感，故称为M-胆碱受体 烟碱型受体：位于神经节细胞和骨骼肌膜上 的胆碱受体，对尼古丁比较敏ห้องสมุดไป่ตู้，故称为N-胆 碱受体
受体 M M1 分布 大脑皮质、海马、 大脑皮质、海马、纹状体 、周围神经节和分泌腺体 生理功能 与传递神经元的兴奋冲 动有关、调节大脑的各 动有关、 种功能， 种功能，并调节汗腺和 消化腺体的分泌 引起心肌收缩力减弱、 引起心肌收缩力减弱、 心率降低、 心率降低、传导减慢 激动剂药物作用 治疗早老性痴呆 拮抗剂药物作用 治疗消化道溃疡
槟榔碱： 槟榔碱：A cycle “reverse ester” ” 反向酯 of acetylcholine Act at both N- and M-receptor,Partial agonist at M1 and M2 used as animal drug
占诺美林
promising for AD
M2 M3
中枢神经系统较低脑区和 心脏等周围效应器组织 腺体和平滑肌
有可能用于治疗冠 有可能用于治疗冠 心病和心动过速
治疗心动徐缓性心 治疗心动徐缓性心 率失常
血管平滑肌舒张、 治疗痉挛性血管病 治疗慢性阻塞性呼 痉挛性血管病、 血管平滑肌舒张、胃肠 治疗痉挛性血管病、 治疗慢性阻塞性呼 吸道疾病、 道和膀胱平滑肌收缩、 手术后腹气胀、 道和膀胱平滑肌收缩、 手术后腹气胀、尿 吸道疾病、尿失禁 括约肌松弛、瞳孔缩小、 潴溜 括约肌松弛、瞳孔缩小、 腺体分泌增加 抑制钙离子通道 孤儿受体 释放乙酰胆碱 缺乏特异性配基 缺乏特异性配基 治疗早老性痴呆 治疗高血压 松弛骨骼肌
((3s-cis)-3-ethyl-dihydro-4-[(1-methyl-1Himidazol-5-yl) methyl]-2(3H)-furanone Reduction of intraocular pressure in some types of glaucoma
- 1、下载文档前请自行甄别文档内容的完整性，平台不提供额外的编辑、内容补充、找答案等附加服务。
- 2、"仅部分预览"的文档,不可在线预览部分如存在完整性等问题,可反馈申请退款(可完整预览的文档不适用该条件!)。
- 3、如文档侵犯您的权益，请联系客服反馈,我们会尽快为您处理(人工客服工作时间：9:00-18:30)。
1. 阐述阿托品的作用、机理、用途、 不良反应、禁忌证；
2. 比较山莨菪碱和东莨菪碱的作用 特点及用途；
3. 列举阿托品的合成代用品； 4. 列举肌松药的分类、代表药、主要
特点。
1
1．新斯的明一般不被用于 A. 重症肌无力 B．机械性肠及泌尿道梗
阻 C．肌松药过量中毒 D．手术后腹气胀和尿潴留 E．支气管哮喘
15
【Clinical Uses 】
antispasmodic drug(解痉药） 1. visceral colic pain（内脏绞痛 ）
胃肠绞痛 (gastric and intestinal colic pain )
膀胱刺激症状 (bladder irritating
symptoms )
合用哌替啶
14
6. CNS
larger dose：excitation depression
不安、幻觉、谵妄、惊厥 循环抑制、呼吸抑制
restlessness(不安) , hallucination ( 幻觉),
delirium (谵妄) and convulsion (惊厥) circulatory (-) respiratory (-)
7
1． glands（腺体）
the secretion↓
sweat gland，salivary gland> lachrymal
> gastric parietal cells
（汗腺、唾液腺> 泪腺、呼吸道腺体Biblioteka >胃壁细胞 ）8
2. eye
Please compare atropine with pilocarpine
Attention: too large dose → HR↑，耗氧量↑，可致
室颤
19
暴发性流脑
5. Antishock（抗休克）
中毒性菌痢
中毒性肺炎
infectious shock (感染性休
克) 大剂量→解除血管痉挛，改善微循环
（large dose → abolish the vessel
spasm and improve microcirculation） Note: 休克伴发热及心动过速者禁用
（Atropine can not be used to the shock
patient accompany with fever and
tachycardia. ）
20
6. Organophosphate intoxication (有机磷酸酯中毒)
5. Vessels＆ blood pressure (血管与 血压 )
Therapeutic dose ---no significant effect
原因：多数血管缺乏胆碱能神经支配 Larger dose--- 皮肤、内脏血管扩张 面
The mechan色is潮m 红is，n解ot除k小no血wn管. 痉挛
Chapter 8
胆碱受体阻断剂
(cholinoceptor blocking drugs)
------------ M-R blocking drugs
5
§1 Atropine ＆ atropine-like alkaloid
（阿托品和阿托品类生物碱）
阿托品 Atropine
[ætrə'pɪn]
1) mydriasis（扩瞳）
atropine (-) 瞳孔括约肌M-R
开大肌功能占优势 瞳孔扩大
9
2) intraocular pressure↑ (升高眼内压)
Atropine → 扩瞳→ 虹
膜退向四周边缘→根
部变厚→前房角间隙 ↓
→房水回流↓ →眼
内
10
3）调节麻痹
睫状肌M-R
Atropine (-) 睫状肌M－R → 睫状肌松驰 →悬韧带拉紧→晶状体扁平→视远物清 楚，近物模糊。
17
3. 眼科(ophthalmologic disorders)
1) 虹膜睫状体炎 (Iridocyclitis)
⑴ 虹膜括约肌和睫状肌休息充分， 有助于炎症消退。
⑵与缩瞳药交替使用，防止粘连
2) 验光配镜、检查眼底 （Optical examination）
作用持续时间长
儿童用
18
4. 缓慢型心律失常 迷走N过度兴奋所致： 窦性心动过缓、窦房阻滞、房室传导阻滞
12
4. Heart 1）HR
therapeutic dose HR （部分病人） larger dose HR↑
Mechanism: （-）窦房结M2-R →解除迷走神经
对心脏的抑制 （迷走张力高者作用显著）
13
2） A – V conduction（房室传导）
Atropine facilitates AV conduction. （阿托品促进房室传导）
11
3. smooth muscle
relaxes
Characteristics ： 1) 作用强度与平滑肌的功能状态有 关 2) 作用强度顺序：
gastrointestinal tract >urinary bladder
> Biliary tract, uterus 胃肠道 > 膀胱 > 胆管、子宫
胆绞痛 (gallbladder colic pain )
肾绞痛 (renal colic pain )
16
2. Inhibition of the secretion of the glands
抑制腺体分泌 1) premedication（麻醉前给药） 2) severe night sweat（盗汗） 3）salivation (流涎)
2
2. 新斯的明对下列哪一效应器
兴奋作用最强?( )
A. 心脏
B. 腺
体
C. 眼
D.骨
骼肌
E . 心脏
3
Q＆A
某工地部分工人午饭后出现头晕、恶心 症状，其中两名工人瞳孔缩小、大汗淋漓、呼 吸困难、肌肉震颤。试分析
⑴ 此可能为哪类毒物中毒？为什么？简述 中毒机理。
⑵ 应为两名工人选用什么抢救药物？简述 选药理由及用药原则。
颠茄
曼陀罗
莨菪
6
【 Mechanism of action】 1.（-）M-R 2. large dose: CNS （+）
【 PharNmNa-cRological actions 】 gland > eye>heart > smooth muscle >CNS （腺体>眼>心>平滑肌>CNS ）