36 Drugs 36.1 Introduction 36.2 Development of Aspirin and cis-Platin

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36 Drugs 36.1 Introduction 36.2 Development of Aspirin and cis-Platin 36.3 Key Stages of Drug Development 36.4 Over-the-Counter Drugs and Prescription Drugs 36.5 Narcotics and their Adverse Effects 36.6 Stimulants and their Adverse Effects

36.1 Introduction 簡介

Medicines and Drugs 藥與藥物 36.1 Introduction (SB p.190) Medicines and Drugs 藥與藥物 Medicines藥  used to cure and prevent diseases  用來醫治和防禦疾病的物質 Drugs藥物  alter the way that our body functions  一種能夠改變身體功能的物質

Medicines and Drugs Most medicines contain drugs 大部分藥都含有藥物 36.1 Introduction (SB p.190) Medicines and Drugs Most medicines contain drugs 大部分藥都含有藥物  but some drugs are not medicines  但有些藥物並不是藥

Alcohol and nicotine are not medicines but they are drugs 36.1 Introduction (SB p.190) Example:例如: Alcohol and nicotine are not medicines but they are drugs 酒精和尼古丁屬於藥物,但並不是藥 Some drugs may or may not be medicines depending on one’s state of health 一些藥物則需視乎服用者的健康狀況,以斷定它是否藥

Drugs Derived from Folk Remedies 36.1 Introduction (SB p.190) Drugs Derived from Folk Remedies 源自民間療法的藥物 Since ancient times 自古以來,  man has used natural materials to relieve pains, heal injuries and cure diseases 人類已運用天然物料去舒緩痛楚、癒合傷口和醫治疾病

Many of these folk remedies have been shown to be very effective 36.1 Introduction (SB p.190) Many of these folk remedies have been shown to be very effective 這些民間療法大多證實功效顯著

With latest scientific and technological advancement 隨近代科技的發展 36.1 Introduction (SB p.190) With latest scientific and technological advancement 隨近代科技的發展  active ingredients of folk remedies have been isolated from the natural medicines  人們可以從天然物質中分離有效成分  their structures are identified  並鑑定其結構

Morphine – extracted from the poppy Papaver somniferum 36.1 Introduction (SB p.190) Example: Morphine – extracted from the poppy Papaver somniferum  嗎啡 – 由罌粟(學名為 Papaver somniferum)提鍊而成

 unless used carefully, morphine can be harmful to our bodies 36.1 Introduction (SB p.190) Morphine 嗎啡  powerful painkiller  一種有效的止痛劑  unless used carefully, morphine can be harmful to our bodies  如果不謹慎使用,嗎啡會對人體有害

Salicylic acid – isolated from willow bark  水楊酸 – 由柳樹的樹皮分離出來 36.1 Introduction (SB p.190) Example: Salicylic acid – isolated from willow bark  水楊酸 – 由柳樹的樹皮分離出來 Salicylic acid水楊酸  the precursor of aspirin  阿士匹靈的前體

Development of Aspirin and cis-Platin 36.2 Development of Aspirin and cis-Platin 阿士匹靈和 順鉑的發展

Aspirin阿士匹靈 For a long time, the bark of the willow tree (salix alba) 36.2 Development of Aspirin and cis-Platin (SB p.191) Aspirin阿士匹靈 For a long time, the bark of the willow tree (salix alba) 長久以來,柳樹(楊柳科植物)的樹皮  used as a traditional medicine  用作民間傳統的藥物  relieve the symptom of fever  以舒緩發燒的症狀

Aspirin In the 1860s, chemists showed 1860 年代,化學家證實柳樹的樹皮 36.2 Development of Aspirin and cis-Platin (SB p.191) Aspirin In the 1860s, chemists showed 1860 年代,化學家證實柳樹的樹皮  salicylic acid (2-hydroxybenzoic acid) in willow bark  含有水楊酸(2-羥基苯酸)  as active ingredient  作為有效成分

Aspirin By 1870, salicylic acid was widely used as 直至 1870 年,水楊酸被廣泛用作 36.2 Development of Aspirin and cis-Platin (SB p.191) Aspirin By 1870, salicylic acid was widely used as 直至 1870 年,水楊酸被廣泛用作  painkiller (analgesic)  止痛劑  fever depressant (antipyretic)  退熱劑

Aspirin Salicylic acid has the undesirable side effects 水楊酸會產生不良的副作用 36.2 Development of Aspirin and cis-Platin (SB p.191) Aspirin Salicylic acid has the undesirable side effects 水楊酸會產生不良的副作用  irritating and damaging the lining of the mouth and stomach  刺激和損害口腔和胃部內壁

Aspirin Molecular modification is necessary 透過改造分子的結構 36.2 Development of Aspirin and cis-Platin (SB p.191) Aspirin Molecular modification is necessary 透過改造分子的結構  give a derivative whicheffective as salicylic acid but has less undesirable side effects  製造出一種和水楊酸具有相同效能但產生較少不良副作用的衍生物

1897 年,菲利克斯‧霍夫曼開設的拜爾製藥公司,成功把水楊酸乙化 36.2 Development of Aspirin and cis-Platin (SB p.191) In 1897, Felix Hoffmann of the Bayer pharmaceutical company succeeded in the acetylation of salicylic acid 1897 年,菲利克斯‧霍夫曼開設的拜爾製藥公司,成功把水楊酸乙化  produce acetylsalicylic acid  製成乙水楊酸  later named as aspirin  其後命名為阿士匹靈

Structures of (a) salicylic acid; (b) aspirin 36.2 Development of Aspirin and cis-Platin (SB p.191) Aspirin (a) (b) Structures of (a) salicylic acid; (b) aspirin

Acetylation of salicylic acid to produce aspirin 36.2 Development of Aspirin and cis-Platin (SB p.191) Aspirin Acetylation of salicylic acid to produce aspirin

36.2 Development of Aspirin and cis-Platin (SB p.191) Let's Think 1

Aspirin At present, aspirin is still widely used in the world 36.2 Development of Aspirin and cis-Platin (SB p.192) Aspirin At present, aspirin is still widely used in the world 現時,世界各地仍廣泛使用阿士匹靈

最近多項研究已證實,每天服用少量阿士匹靈能有助預防疾病 36.2 Development of Aspirin and cis-Platin (SB p.192) Recent researches have shown that small daily doses of aspirin may help prevent diseases 最近多項研究已證實,每天服用少量阿士匹靈能有助預防疾病  such as heart attack, stroke, and the blindness and kidney damage suffered by many patients with diabetes  例如心臟病、中風、失明和大部分糖 尿病患者患上的腎衰竭

36.2 Development of Aspirin and cis-Platin (SB p.192) Check Point 36-2

36.2 Development of Aspirin and cis-Platin (SB p.193) In 1964, the biophysicist, Barnett Rosenberg and his research group were studying the effect of an electric field on the growth of bacteria 1964 年,生物物理學家巴涅特‧羅森伯格和其研究小組鑽研電場對細菌生長的影響

36.2 Development of Aspirin and cis-Platin (SB p.193)  A platinum-containing substance extracted from the bacterial culture inhibited cell division  由細菌培養液中抽取含鉑的物質能夠 阻止細胞分裂

cis-Platin Further studies showed that 其後的研究更顯示 36.2 Development of Aspirin and cis-Platin (SB p.193) cis-Platin Further studies showed that 其後的研究更顯示  cis-diamminedichloroplatinum(II) [Pt(NH3)2Cl2], also called cis-platin was effective at inhibiting cell division  順-二氨二氯合鉑(II)([Pt(NH3)2Cl2]),亦稱為順-鉑,也能有效阻止細胞分裂

cis-platin alters the DNA of the cancer cell 順鉑能改變癌細胞的脫氧核糖核酸 36.2 Development of Aspirin and cis-Platin (SB p.193) cis-platin alters the DNA of the cancer cell 順鉑能改變癌細胞的脫氧核糖核酸  when the cell tries to replicate, its DNA cannot be copied correctly  細胞複製時,其脫氧核糖核酸無法 正常複製  the cell dies  以致細胞死亡

The geometry of cis-platin is important to its action 36.2 Development of Aspirin and cis-Platin (SB p.193) The geometry of cis-platin is important to its action 順鉑的幾何構型對它的反應亦是重要的

The geometrical isomer of cis-platin, trans-platin, was ineffective in treating cancer 順鉑的幾何異構體,即反鉑,對治療癌症是無效的

研究人員嘗試探究這化合物怎樣影響哺乳動物的細胞分裂 36.2 Development of Aspirin and cis-Platin (SB p.193) Researchers investigate how this compound affects cell division in mammalian cells 研究人員嘗試探究這化合物怎樣影響哺乳動物的細胞分裂  they treated two mice having cancer with cis-platin  他們給兩隻患癌症的老鼠服用順鉑

cis-Platin Results: 結果:  the size of tumours was reduced  老鼠的腫瘤縮小 36.2 Development of Aspirin and cis-Platin (SB p.193) cis-Platin Results: 結果:  the size of tumours was reduced  老鼠的腫瘤縮小  the mice were subsequently cured  並且痊癒

More animal studies were conducted 隨後,人們利用狗隻和猴子進行多項動物測試 36.2 Development of Aspirin and cis-Platin (SB p.193) More animal studies were conducted 隨後,人們利用狗隻和猴子進行多項動物測試  determine the toxic side effects of different dose levels of cis-platin  以斷定不同劑量的順鉑產生具有的 毒性副作用 Dogs and monkeys were used as the test subjects

The most severe side effects: 最嚴重的副作用:  nausea作嘔  vomiting嘔吐 36.2 Development of Aspirin and cis-Platin (SB p.193) The most severe side effects: 最嚴重的副作用:  nausea作嘔  vomiting嘔吐  toxicity to the kidney對腎產生毒性  toxicity to the bone marrow  對骨髓產生毒性

順鉑成功治療老鼠的腫瘤,加上在狗隻和猴子的毒性測試獲得的資料 36.2 Development of Aspirin and cis-Platin (SB p.193) The success of cis-platin in curing tumours in mice, together with the toxicity information gained from studies on dogs and monkeys 順鉑成功治療老鼠的腫瘤,加上在狗隻和猴子的毒性測試獲得的資料  this compound might be effective as an anticancer agent in humans with cancer  研究人員便認為這化合物可能有助治 療癌症病人

The use of cis-platin as an anticancer agent 36.2 Development of Aspirin and cis-Platin (SB p.193) cis-Platin The use of cis-platin as an anticancer agent

Key Stages of Drug Development 36.3 Key Stages of Drug Development 藥物發展的 主要階段

Key Stages of Drug Development 藥物的發展的主要階段 36.3 Key Stages of Drug Development (SB p.194) Key Stages of Drug Development 藥物的發展的主要階段 1. Lead compound discovery導引化合物的發現 2. Molecular modification分子結構的修訂 3. Formulation development配方的發展 4. Safety tests and human trials安全測試驗和臨床試驗 5. Approval for marketing獲准公開發售途

36.3 Key Stages of Drug Development (SB p.197) Check Point 36-3

Over-the-Counter Drugs and Prescription Drugs 36.4 Over-the-Counter Drugs and Prescription Drugs 非處方藥物和 處方藥物

Over-the-Counter Drugs and Prescription Drugs非處方藥物和處方藥物 36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.197) Over-the-Counter Drugs and Prescription Drugs非處方藥物和處方藥物 Drugs can be divided into two categories based on how they can be bought 藥物可以根據購買途徑分為兩類:  Over-the-counter (non-prescription) drugs非處方藥物(無須醫生處方)  Prescription drugs處方藥物

Structure and uses of some common over-the-counter drugs 36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.197) Structure and uses of some common over-the-counter drugs Name Structure Uses Aspirin 阿士匹靈 As analgesics and antipyretics 作為止痛劑和退熱劑 Acetaminophen 醋氨酚

Structure and uses of some common over-the-counter drugs 36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.197) Structure and uses of some common over-the-counter drugs Name Structure Uses Vitamin C 維生素 C Helps maintain elasticity of the skin, aids the absorption of iron and improves resistance to infection •幫助保持皮膚彈性,有助吸收鐵質和增強預防傳染病的抵抗力

Structure and uses of some common over-the-counter drugs 36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.197) Structure and uses of some common over-the-counter drugs Name Structure Uses Vitamin C 維生素 C • Essential for the formation of collagen and intercellular material, bone and teeth and for healing of wounds 作幫助形成膠原蛋白、胞間物質、骨骼和牙齒,並有助癒合傷

Structure and uses of some common prescription drugs 36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.198) Structure and uses of some common prescription drugs Name Structure Uses Albuterol 沙丁胺醇 • For treating asthma, emphysema and chronic bronchitis • 治療哮喘、肺氣腫和慢性支氣管炎 • Dilates the bronchial airways by relaxing the surrounding muscles • 鬆馳四周的肌肉,以擴大支氣管氣道 Amoldipine 氨氯地平 As an anti-hypertensive 作為抗血壓藥

Structure and uses of some common prescription drugs 36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.198) Structure and uses of some common prescription drugs Name Structure Uses Loratadine 氯雷他定 Relieves nasal and non-nasal symptoms of seasonal allergies 舒緩季節性敏感引起的鼻腔和非鼻腔症狀 • As an antihistamine • 作為抗組胺劑

Structure and uses of some common prescription drugs 36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.198) Structure and uses of some common prescription drugs Name Structure Uses Amoxicillin 安莫西林 As an antibiotic used to treat bacterial infections 作為治療細菌感染的抗生素

Structure and uses of some common prescription drugs 36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.198) Structure and uses of some common prescription drugs Name Structure Uses Omeprazole 奧美拉唑 • Suppresses secretion of gastric acid • 抑制胃酸分泌 • Used for the treatment of duodenal and gastric ulcers and gastroesophageal reflux disease • 治療十二指腸潰瘍、胃潰瘍和胃酸倒流

36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.199) Check Point 36-4

Narcotics and their Adverse Effects 36.5 Narcotics and their Adverse Effects 麻醉劑和它們的 不良效應

Morphine and Heroin as Narcotic Drugs嗎啡和海洛因作為麻醉劑 36.5 Narcotics and their Adverse (SB p.199) Morphine and Heroin as Narcotic Drugs嗎啡和海洛因作為麻醉劑 About 5000 years ago, the Babylonians used crude opium to relieve pains 約五千年前,巴比倫人使用天然鴉片舒緩痛楚

Morphine and Heroin as Narcotic Drugs 36.5 Narcotics and their Adverse (SB p.199) Morphine and Heroin as Narcotic Drugs The alkaloid morphine was first isolated from the opium poppy (Papaver somniferum) in 1803 1803 年,生物鹼嗎啡首次由鴉片(罌粟,學名為 Papaver somniferum)分離出來 Its addictive properties were known from early times 嗎啡使服用者上癮的性質在早期已被發現

Morphine and Heroin as Narcotic Drugs 36.5 Narcotics and their Adverse (SB p.199) Morphine and Heroin as Narcotic Drugs In 1898, morphine was acetylated to produce diacetylmorphine, or heroin 1898 年,人們進行嗎啡的乙化作用,生成二乙嗎啡(亦稱為海洛因)  quickly realized to be even more addictive than morphine  隨即發現它比嗎啡更易令人上癮

Morphine and Heroin as Narcotic Drugs 36.5 Narcotics and their Adverse (SB p.199) Morphine and Heroin as Narcotic Drugs Morphine Heroin

 a wonderful painkiller  強效的止痛劑 36.5 Narcotics and their Adverse (SB p.199) Morphine嗎啡  a wonderful painkiller  強效的止痛劑  used in cases of radical surgery and on the battlefield  在基本手術和戰場上使用  50 times as potent as aspirin  它的止痛效能比阿士匹靈強 50 倍

 painkillers (or analgesics)  一種止痛劑 36.5 Narcotics and their Adverse (SB p.199) Narcotics麻醉劑  painkillers (or analgesics)  一種止痛劑  produce euphoria, a feeling of peace and tranquility  它能產生興奮、平靜和安寧的感覺  addictive  會令人上癮

 more dangerous than morphine  比嗎啡更危險  causes rapid addiction 36.5 Narcotics and their Adverse (SB p.199) Heroin海洛因  more dangerous than morphine  比嗎啡更危險  causes rapid addiction  它令人很快上癮

Heroin and morphine海洛因和嗎啡  narcotics麻醉劑  generally called opiates 36.5 Narcotics and their Adverse (SB p.199) Heroin and morphine海洛因和嗎啡  narcotics麻醉劑  generally called opiates  一般稱為鴉片劑  obtained from opium  都是由鴉片提煉出來  obtained by evaporating the sap of the opium poppy  鴉片是罌粟汁液蒸發後的殘餘物

Examples of narcotic drugs: morphine 36.5 Narcotics and their Adverse (SB p.199) Morphine and Heroin as Narcotic Drugs Examples of narcotic drugs: morphine

Examples of narcotic drugs: heroin 36.5 Narcotics and their Adverse (SB p.199) Morphine and Heroin as Narcotic Drugs Examples of narcotic drugs: heroin

Adverse Effects of Use of Morphine and Heroin濫用嗎啡和海洛因的害處 36.5 Narcotics and their Adverse (SB p.200) Adverse Effects of Use of Morphine and Heroin濫用嗎啡和海洛因的害處 Opiates鴉片劑  pain relief and a general feeling of well-being  舒緩痛楚和產生愉快的感覺

Adverse Effects of Use of Morphine and Heroin濫用嗎啡和海洛因的害處 36.5 Narcotics and their Adverse (SB p.200) Adverse Effects of Use of Morphine and Heroin濫用嗎啡和海洛因的害處 Opiates鴉片劑  produce drowsiness that leads to sleep  使人疲倦,令人昏昏欲睡

Used non-medically, morphine 嗎啡用於非醫學用途上: 36.5 Narcotics and their Adverse (SB p.200) Used non-medically, morphine 嗎啡用於非醫學用途上:  produces a typical “high”, a feeling of extreme well-being, and then drowsiness  令人產生一種「快感」–— 一種極 興奮,繼而昏昏欲睡的感覺

 tolerance and physical dependence develop rapidly among users 36.5 Narcotics and their Adverse (SB p.200)  tolerance and physical dependence develop rapidly among users  產生耐藥性和生理依藥性

Used non-medically, heroin 海洛因用於非醫學用途上: 36.5 Narcotics and their Adverse (SB p.200) Used non-medically, heroin 海洛因用於非醫學用途上:  inducing an intense brief period of euphoria, known as the “rush”  引致劇烈和短暫的興奮  stop diarrhoea, slow breathing, and cause nausea and vomiting  可以止腹瀉、減慢呼吸,使濫藥者作嘔和嘔吐

Morphine and heroin are addictive 嗎啡和海洛因都會令人上癮 36.5 Narcotics and their Adverse (SB p.200) Morphine and heroin are addictive 嗎啡和海洛因都會令人上癮 Their heavy use or even occasional use over a long period will likely result in opiate abuse and dependence 過量服用,甚至長期非經常服用,都可能導致藥物濫用和依藥性

Characteristics of dependence: 上癮的徵狀包括:  daily use每日服用 36.5 Narcotics and their Adverse (SB p.200) Characteristics of dependence: 上癮的徵狀包括:  daily use每日服用  inability to stop usage無法停服  constant or repeated intoxication with a narcotic drug  因麻醉劑而持續或重複的中毒

 withdrawal symptoms戒斷症狀 36.5 Narcotics and their Adverse (SB p.200)  overdoses服用過量  tolerance耐藥性  withdrawal symptoms戒斷症狀

濫用嗎啡和海後,通常也不會對腦部、肝臟或心臟造成生理損害 36.5 Narcotics and their Adverse (SB p.200) Morphine and heroin usually do not cause physical damage to the brain, liver, or heart 濫用嗎啡和海後,通常也不會對腦部、肝臟或心臟造成生理損害 They do not induce psychotic experiences or increase susceptibility to seizures 它們不會引致精神錯亂或影響情緒

The problems frequently associated with the abuse of narcotics 36.5 Narcotics and their Adverse (SB p.200) The problems frequently associated with the abuse of narcotics 濫用麻醉劑的常見問題  typically related to the neglect of personal health and safety  一般與忽略個人健康和安全有關

Heroin abusers are prone to numerous life-endangering conditions 36.5 Narcotics and their Adverse (SB p.200) Heroin abusers are prone to numerous life-endangering conditions 濫用海洛因的人容易構成生命危險  tend to neglect their health  他們大多忽略健康

 fail to detect common signs of illness  無法察覺患病的徵狀 36.5 Narcotics and their Adverse (SB p.200)  fail to detect common signs of illness  無法察覺患病的徵狀  frequently resort to intravenous injection of opiates with shared needles  經常共用針筒,把鴉片劑注射進靜脈

Commonly observed problems: 常見的問題包括: 36.5 Narcotics and their Adverse (SB p.200) Commonly observed problems: 常見的問題包括:  the transmission of HIV, AIDS, viral hepatitis (hepatitis B virus)  人類免疫力缺乏病毒、愛滋病病毒、 乙型肝炎病毒的傳播  inflammation of the heart’s lining  引致心內膜發炎

 tetanus, malaria, syphilis  破傷風、瘧疾、梅毒 36.5 Narcotics and their Adverse (SB p.200)  blood poisoning  血中毒  tetanus, malaria, syphilis  破傷風、瘧疾、梅毒

 blood vessel inflammation血管發炎  heart valve infection心瓣膜感染 36.5 Narcotics and their Adverse (SB p.200)  blood vessel inflammation血管發炎  heart valve infection心瓣膜感染  malnutrition營養不良

 festering sores on the arms and legs  手臂和大腿潰瘍 36.5 Narcotics and their Adverse (SB p.200)  festering sores on the arms and legs  手臂和大腿潰瘍  the toxic effects of overdose  由於服食過量而引致的中毒

Government posters on campaign against drug abuse 36.5 Narcotics and their Adverse (SB p.200) Government posters on campaign against drug abuse

Stimulants and their Adverse Effects 36.6 Stimulants and their Adverse Effects 興奮劑和它們的 不良效應

Introduction簡介 Stimulant興奮劑 36.6 Stimulants and their Adverse Effects (SB p.200) Introduction簡介 Stimulant興奮劑  a drug that increases the activity of various parts of our nervous system  刺激中樞神經的藥物,具有短暫的提 神作用

 作為增加耐力和生產力,並抑制食慾 的藥物 36.6 Stimulants and their Adverse Effects (SB p.200)  can be used to boost endurance and productivity as well as to suppress appetite  作為增加耐力和生產力,並抑制食慾 的藥物

36.6 Stimulants and their Adverse Effects (SB p.200) Ketamine氯胺酮 Belongs to a class of drugs called “dissociative anaesthetics” 屬於一系列「分離麻醉劑」

越戰時,一個美國士兵首次使用氯胺酮,但現時已避免使用 36.6 Stimulants and their Adverse Effects (SB p.200) First used on American soldiers during the Vietnam War, but it is often avoided now 越戰時,一個美國士兵首次使用氯胺酮,但現時已避免使用  it can cause unpleasant out-of-body experiences它會產生「靈魂出竅」的不息感覺 Still used widely in veterinary medicines, and for certain human applications 除了應用於人類的特殊用途外,氯胺酮常被獸醫廣泛採用,作為麻醉的用途

36.6 Stimulants and their Adverse Effects (SB p.201) Become popular among teenagers and young adults at disco and rave parties 在的士高和狂野派對深受青少年人的歡迎 When used recreationally, ketamine can be known as K, Ket, special K, or Kitty 俗稱為「K 仔」、「茄仔」或「特別 K」

當濫藥者吸入氯胺酮粉末後瞬間湧現強烈的幻覺 36.6 Stimulants and their Adverse Effects (SB p.201) Some people describe a speedy rush within a few minutes of sniffing the ketamine powder 當濫藥者吸入氯胺酮粉末後瞬間湧現強烈的幻覺

36.6 Stimulants and their Adverse Effects (SB p.201)  leading to powerful hallucinations and even out-of-body experiences, along with physical incapacitation  甚至有「靈魂出竅」的感覺

Adverse Effects of Use of Ketamine 濫用氯胺酮的害處 36.6 Stimulants and their Adverse Effects (SB p.201) Adverse Effects of Use of Ketamine 濫用氯胺酮的害處 At low doses服用少量氯胺酮  causes an increase in heart rate  令濫藥者的心跳加速  gives a mild, dreamy feeling and drowsiness  產生一種做夢的狀態,令人昏昏欲睡

At higher doses服用大量氯胺酮  produce a hallucinogenic effect 36.6 Stimulants and their Adverse Effects (SB p.201) At higher doses服用大量氯胺酮  produce a hallucinogenic effect  令濫藥者產生幻覺

 may cause the users to feel very far away from their body 36.6 Stimulants and their Adverse Effects (SB p.201)  may cause the users to feel very far away from their body  甚至有離開軀體的感覺,

 俗稱「K 洞」。濫藥者可從遠處看到自己的身體,或者處在臨死或重生的狀態 36.6 Stimulants and their Adverse Effects (SB p.201)  this effect is referred to as entering a “K-Hole”, and has been compared to a near death experience with sensations of rising above one’s body  俗稱「K 洞」。濫藥者可從遠處看到自己的身體,或者處在臨死或重生的狀態

Frequent intake of ketamine can cause 經常濫用氯胺酮會出現  depression抑鬱 36.6 Stimulants and their Adverse Effects (SB p.201) Frequent intake of ketamine can cause 經常濫用氯胺酮會出現  depression抑鬱  nausea嘔吐

 impaired long-term memory and cognitive difficulties  記憶力衰退及認知困難 36.6 Stimulants and their Adverse Effects (SB p.201)  impaired long-term memory and cognitive difficulties  記憶力衰退及認知困難

 impaired motor function, respiratory and heart problems 36.6 Stimulants and their Adverse Effects (SB p.201)  impaired motor function, respiratory and heart problems  行動機能受損,呼吸和心臟機能受損

Frequent intake of ketamine can cause 濫用氯胺酮 36.6 Stimulants and their Adverse Effects (SB p.201) Frequent intake of ketamine can cause 濫用氯胺酮  a tremendous physiological /psychological dependence  引致嚴重的生理和心理依藥性  addiction上癮 Example 36-6

Phenylethanamine and Substituted Phenylethanamines 苯基乙胺和取代的苯基乙胺 36.6 Stimulants and their Adverse Effects (SB p.202) Phenylethanamine and Substituted Phenylethanamines 苯基乙胺和取代的苯基乙胺 Phenylethanamine (or 2-phenylethan-1-amine) is an alkaloid and monoamine 苯基乙胺(或 2-苯基乙-1-胺)是生物鹼,並屬於單一胺

Phenylethanamine苯基乙胺 36.6 Stimulants and their Adverse Effects (SB p.202) Phenylethanamine苯基乙胺  believed to function as a neurotransmitter in the human brain  作為人類腦部的神經遞質  found in many foods like chocolate  它亦可以在很多食物中找到 (例如巧克力)

 當進食足夠分量含有苯基乙胺的食物後可能會對心理或精神有顯著的影響 36.6 Stimulants and their Adverse Effects (SB p.202)  may have psychoactive effects in sufficient quantities, but quickly metabolized in our body  當進食足夠分量含有苯基乙胺的食物後可能會對心理或精神有顯著的影響  prevent significant concentrations from reaching the brain  它會瞬間在人體內代謝,避免大量 苯基乙胺進入腦部

Substituted Phenylethanamine 取代的苯基乙胺 36.6 Stimulants and their Adverse Effects (SB p.202) Substituted Phenylethanamine 取代的苯基乙胺  a broad and diverse class of compounds  屬於一系列廣泛和具有不同分類的 化學物  include hormones, stimulants, hallucinogens and antidepressants  包括荷爾蒙、興奮劑、迷幻劑、抗 抑鬱劑

Amphetamine安非他命(俗稱「冰」)  a homologue of phenylethanamine  苯基乙胺的同系列 36.6 Stimulants and their Adverse Effects (SB p.202) Amphetamine安非他命(俗稱「冰」)  a homologue of phenylethanamine  苯基乙胺的同系列  carrying an  methyl group  含有一個α-甲基團

 用作抑制食慾、控制體重、治療嗜眠病和注意力不足過動障礙 36.6 Stimulants and their Adverse Effects (SB p.202)  synthetic stimulant  合成的興奮劑  used to suppress the appetite, control weight and treat disorders including narcolepsy and attention- deficit hyperactivity disorder  用作抑制食慾、控制體重、治療嗜眠病和注意力不足過動障礙

 used recreationally and for performance enhancement 36.6 Stimulants and their Adverse Effects (SB p.202)  used recreationally and for performance enhancement  服用安非他明可以增加運動員的表現  these uses are illegal in most countries  很多國家都禁止使用

36.6 Stimulants and their Adverse Effects (SB p.202) Check Point 36-6

Adverse Effects of Use of Amphetamine 濫用安非他明的害處 36.6 Stimulants and their Adverse Effects (SB p.203) Adverse Effects of Use of Amphetamine 濫用安非他明的害處 The side effects: 副作用包括:  insomnia失眠  Irritability過度活躍

Adverse Effects of Use of Amphetamine 36.6 Stimulants and their Adverse Effects (SB p.203) Adverse Effects of Use of Amphetamine  loss of appetite食慾不振

Adverse Effects of Use of Amphetamine 36.6 Stimulants and their Adverse Effects (SB p.203) Adverse Effects of Use of Amphetamine  hallucination產生幻覺

Adverse Effects of Use of Amphetamine 36.6 Stimulants and their Adverse Effects (SB p.203) Adverse Effects of Use of Amphetamine  increased likelihood of heart attack and stroke增加心臟病和中風的可能性

Adverse Effects of Use of Amphetamine 36.6 Stimulants and their Adverse Effects (SB p.203) Adverse Effects of Use of Amphetamine Regular use of amphetamines: 經常濫用安非他明  induces tolerance引致耐藥性  leads to taking of higher to higher dosage to produce the same effects  每次需要服食更多的劑量,才能產生 相同的效果

Adverse Effects of Use of Amphetamine 36.6 Stimulants and their Adverse Effects (SB p.203) Adverse Effects of Use of Amphetamine Chronic users of amphetamines: 長期濫用者  psychologically dependent on amphetamines  產生心理依藥性

 chronic heavy users generally fail to eat properly長期濫用者一般都是食慾不振 36.6 Stimulants and their Adverse Effects (SB p.203)  chronic heavy users generally fail to eat properly長期濫用者一般都是食慾不振  develop various illnesses related to vitamin deficiencies and malnutrition  他們都會患上有關缺乏維他命的疾病 和營養失調

Users may also be more prone to illness 濫用者一般較容易生病 36.6 Stimulants and their Adverse Effects (SB p.203) Users may also be more prone to illness 濫用者一般較容易生病  they are generally run down他們較疲倦

 live in an unhealthy environment 生活習慣不健康 36.6 Stimulants and their Adverse Effects (SB p.203)  lack sleep缺乏睡眠  live in an unhealthy environment 生活習慣不健康

Chronic heavy users may also develop mental disturbance 嚴重濫用者可能引致思覺失調 36.6 Stimulants and their Adverse Effects (SB p.203) Chronic heavy users may also develop mental disturbance 嚴重濫用者可能引致思覺失調  known as amphetamine psychosis  亦稱為安非他命精神病

The END

36.2 Development of Aspirin and cis-Platin (SB p.191) Let's Think 1 We do not want to rely on the natural products (like willow trees) as medicines (like salicylic acid). Why? Answer Medicines which are “natural products” (e.g. those which come directly from plants) may be difficult to obtain when needed. The supply may be seasonal, may depend on weather conditions and may be liable to contamination. Collecting plants from their natural habitat may cause harms to the environment. Back

36.2 Development of Aspirin and cis-Platin (SB p.192) Example 36-2 At the end of the 19th century, the compound phenol was already well-known in the pharmaceutical industry. Phenol has germicidal properties. It was also readily available and its molecular structure differs from that of 2-hydroxybenzoic acid by only one functional group. Phenol 2-Hydroxybenzoic acid

36.2 Development of Aspirin and cis-Platin (SB p.192) Example 36-2 (a) What extra atoms have to be added to phenol to give 2-hydroxybenzoic acid? Answer (a) 1 carbon atom and 2 oxygen atoms

36.2 Development of Aspirin and cis-Platin (SB p.192) Back Example 36-2 (b) Suggest reagents and conditions necessary to bring about the change from phenol to 2-hydroxybenzoic acid. Answer (b) Carbon dioxide can be combined directly with phenol to give 2-hydroxybenzoic acid by careful control of the conditions. In an alkaline medium, phenol is heated with carbon dioxide at 130°C and under a pressure of 5 – 7 atm. Subsequent acid hydrolysis yields salicylic acid. The reaction is known as the Kolbe-Schmitt synthesis.

36.2 Development of Aspirin and cis-Platin (SB p.192) Check Point 36-2 Aspirin belongs to a class of organic compounds known as esters. Esterification of salicylic acid with a reagent is used to produce aspirin. (a) Suggest reagents for converting salicylic acid to aspirin in the esterification. Answer (a) Ethanoyl chloride and ethanoic anhydride may be used.

36.2 Development of Aspirin and cis-Platin (SB p.192) Check Point 36-2 Aspirin belongs to a class of organic compounds known as esters. Esterification of salicylic acid with a reagent is used to produce aspirin. (b) Write a chemical equation for the reaction involved. Answer

Check Point 36-2 36.2 Development of Aspirin and cis-Platin (SB p.192)

36.2 Development of Aspirin and cis-Platin (SB p.192) Back Check Point 36-2 (b)

Check Point 36-3 Answer (a) What is the lead compound of aspirin? 36.3 Key Stages of Drug Development (SB p.197) Check Point 36-3 (a) What is the lead compound of aspirin? Answer (a) 2-Hydroxybenzoic acid (or salicylic acid)

36.3 Key Stages of Drug Development (SB p.197) Check Point 36-3 (b) Why is molecular modification of the lead compound of aspirin necessary? Answer (b) It is because the lead compound of aspirin has many undesirable effects. It irritates and damages the lining of the mouth and stomach. Back

Check Point 36-4 Answer cis-Platin is a prescription drug. 36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.199) Check Point 36-4 cis-Platin is a prescription drug. (a) What is the meaning of a prescription drug? (a) A prescription drug means that the use of the drug must be prescribed by a medical doctor. Answer

Check Point 36-4 Answer cis-Platin is a prescription drug. 36.4 Over-the-Counter Drugs and Prescription Drugs (SB p.199) Check Point 36-4 cis-Platin is a prescription drug. (b) Why is cis-platin regarded as a prescription drug? (b) cis-Platin is a prescription drug because it has numerous side effects on our health. A professional decision from the medical doctor is necessary for its adminstration. Answer Back

36.6 Stimulants and their Adverse Effects (SB p.201) Example 36-6 Based on the structural formula of ketamine shown above, answer the following questions: (a) Give the molecular formula of ketamine. Answer (a) C13H16ClNO

36.6 Stimulants and their Adverse Effects (SB p.201) Example 36-6 Based on the structural formula of ketamine shown above, answer the following questions: (b) Name all the functional groups of ketamine. Answer (b) Amine (secondary), ketone, halobenzene, benzene ring

36.6 Stimulants and their Adverse Effects (SB p.201) Example 36-6 Based on the structural formula of ketamine shown above, answer the following questions: (c) Mark the chiral centre of ketamine in its structural formula. (c) Answer Back

36.6 Stimulants and their Adverse Effects (SB p.202) Check Point 36-6 (a) Is amphetamine a primary, secondary or tertiary amine? (a) A primary amine Answer

36.6 Stimulants and their Adverse Effects (SB p.202) Check Point 36-6 (b) Mark the chiral centre of the molecule of amphetamine in its structural formula. (b) (*chiral centre) Amphetamine Answer Back