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Medical English Amoxicillin 阿莫西林 Professor: Dr. Pat Chan Clinical specialist 1 Map of USA 2 Map of USA in Chinese 3 Minnesota 1. 2. 3. 4. 5. 6. 7. Lakes Healthy environment Education Good health care system Famous hospital Mayo Clinic, U of Minnesota Hospital… Family life Many famous companies ie 3M, Honeywell, General Mills, Cargill, Best buy, Seagate and many software companies 4 Expectations • Come to classes on time • Attendance is important. If you need to miss a • • class, you must be responsible for that missing lesson; send me an email why you miss the class [email protected] Class participation is part of the grading system I will email PPT to your class leader for future lectures 5 Examination • Will be held on September 26 • Learn pharmaceutical vocabularies • Write a short description of a drug which you • • • • have chosen 2 pages long in English Type your name and student numbers You can not copy from other materials. You can interpret the materials and use your own ideas and words Do not copy and paste 6 vocabulary • • • • • • • drug-resistant bacteria 细菌耐药性 effectiveness 成效 semisynthetic antibiotic半合成抗生素 Pharmacokinetics 药代动力学 drug-resistant bacteria 细菌耐药性 semisynthetic antibiotic半合成抗生素 broad spectrum of bactericidal activity 广谱抗菌 活性 7 vocabulary • gastric acid胃酸 • Stable稳定 • brain and spinal fluid 大脑 脊髓液 • meninges are inflamed 脑膜炎 • excreted unchanged in the urine 尿中排出 不变 • Half Life 半衰期 8 Vocabulary • Probenicid can delay amoxicillin’s excretion 丙 磺舒可延遲其排泄 • Average peak blood levels 平均血药浓程度 高峰 • excreted in the urine 在尿中排泄 • Pharmacology药理 • inhibition of biosynthesis of cell wall mucopeptide 抑制细菌细胞壁 的生物合成 • active multiplication 积极增殖 9 Medical terminology • Escherichia coli大肠埃希氏菌( b- lactamase negative only贝塔内酰胺酶 阴性株 ) • Haemophilus influenza( b-lactamase negative only)嗜血杆菌 • Neisseria gonorrhoeae淋球菌 • Proteus mirabilis变形杆菌 • Helicobacter pylori幽门螺杆菌 10 Medical terminology • Aerobic gram positive microorganism需氧革兰氏 • • • • • 阳性菌 Enterococcus faecalis 粪肠球菌 staphylococcus葡萄球菌(b-lactamase negative strain) (贝塔内酰胺酶阴性株 ) Streptococcus pneumoniae 肺炎链球菌 Streptococcus (b-lactamase negative) aerobic negative microorganism 好氧微生物负 11 Medical terminology • glomerular filtration rate腎小球濾過率 • B-lactamase B-内酰胺酶 • Susceptibility tests 药敏试验 • minimum inhibitory concentrations 最低抑 菌浓度 12 Amoxicillin in USA is prescription only • This is to reduce the development of drugresistant bacteria 细菌耐药性 • maintain the effectiveness 成效 of amoxicillin and other antibacterial drugs • amoxicillin should be used only to treat infections that are strongly suspected to be caused by bacteria • 强烈怀疑是由细菌引起的 13 Description Description: • Formulations of amoxicillin contain amoxicillin, a semisynthetic antibiotic半合成抗生素 • an analog 模拟 of ampicillin molecules • a broad spectrum of bactericidal activity广谱抗菌 活性 against many gram – positive and gramnegative microorganisms针对革兰氏阳性和革兰 氏阴性细菌 . 14 Clinical pharmacology & pharmacokinetics临 床药理学及药代动力学 • Amoxicillin is stable in the presence of gastric acid阿莫西林在胃酸是稳定的 • rapidly absorbed after oral administration. 口服后迅速吸收 • Amoxicillin diffuses readily into body tissues and fluids 扩散 人体组织和 体液 Except 除了 : 15 Pharmacokinetics of amoxicillin • Exception : of brain and spinal fluid 除了大脑 脊 • • • • 髓液 except when meninges are inflamed 脑膜炎 The half life of amoxicillin is 61.3 minutes Most of the amoxicillin is excreted unchanged in the urine 尿中排出不变 its excretion can be delayed by concurrent administration of probenecid 丙磺舒可延遲 amoxicillin排泄 16 Pharmacology药理 • Average peak blood levels平均 血药浓程度 高峰 1-2 hours after administration of 250 mg and 500 mg of amoxicillin capsules 17 Pharmacokinetics 药代动力学 • Detectable serum levels are observed up to 8 hours after an orally administered dose of amoxicillin. • 口服药剂后检出阿莫西林血清水平观察 长达到8 hours。 • Approximately 60% of an orally administrated dose of amoxicillin is excreted in the urine在尿中 排泄 within 6 to 8 hours 18 Microbiology • Amoxicillin is similar to ampicillin in its bactericidal action against susceptible organisms during the stage of active multiplication积极 增殖 . It acts through the inhibition of biosynthesis of cell wall mucopeptide 抑制细菌细胞壁 的生物合成 19 Medical terminology • Aerobic gram positive microorganism需氧革兰氏 • • • • • 阳性菌 Enterococcus faecalis 粪肠球菌 staphylococcus葡萄球菌(b-lactamase negative strain) (贝塔内酰胺酶阴性株 ) Streptococcus pneumoniae 肺炎链球菌 Streptococcus (b-lactamase negative) aerobic negative microorganism 好氧微生物负 20 Medical terminology • Escherichia coli大肠埃希氏菌( b- lactamase negative only贝塔内酰胺酶 阴性株 ) • Haemophilus influenza( b-lactamase negative only)嗜血杆菌 • Neisseria gonorrhoeae淋球菌 • Proteus mirabilis变形杆菌 • Helicobacter pylori幽门螺杆菌 21 Medical terminology • glomerular filtration rate腎小球濾過率 22 B-lactamase B-内酰胺酶 (an enzyme produced by some bacteria causes the antibiotic to become ineffective)一些细 菌所产生的酶,导致抗生素变得无 23 Amoxicillin has been shown to be active against most strains of the following microorganisms 24 Susceptibility tests 药敏试验 • The MIC ( minimum inhibitory concentrations)最低抑菌 • 浓度 provide estimates of the susceptibility of bacteria to antimicrobial compound The MIC should be determined using a standard procedure. Standardized procedures are based on diluted method稀释法 . 25 Minimum inhibitory concentration (MIC) Anti-infective agent dosing: 1. Need to be considered when administering antibiotics include absorption 2. 3. 4. 5. 6. 吸收 volume of distribution 分佈容積 代谢 Excretion 排泄. metabolism These factors determine the dose of each drug and the time interval of administration To effectively clear a bacterial infection, serum levels of the antibiotic need to be maintained above the minimum inhibitory concentration (MIC) for a significant perioid. 26 Indications and usage 使用指示 Amoxicillin is indicated in the treatment of infections due to susceptible (Only B-lactamas-negative) strains of bacteria. 1. Infections of the ear, nose, and throat—due Streptococcus spp. (alpha and beta hemolytic strains only), S. pneumoniae, Staphylococcus spps. Or H. influenzae 2. Infections of the genitourinary tract泌尿生殖系统—due to E. Coli, P. mirabils, or E. Faecalis 3. Infections of the skin and skin structure—due to Streptococcus spp. ( alpha and Beta hemolytic strains only), Staphlococcus spp., or E. Coli 27 Indication of use使用指示 4. Infections of the lower respiratory tract– due to Streptococcus spp. ( alpha and beta hemolytic strains only), S. pneumoniae, Staphylococcus spp., or H. influenzae 5. Gonorrhea, acute uncomplicated (ano-genital肛 生殖器 and urethral 尿道infections)—due to N. gonorrhoeae ( males and females) 6. H. pylori eradication消灭 to reduce the risk of duodenal ulcer十二指溃疡 recurrence 28 A word of warning: • To reduce the development of drug-resistant bacteria and maintain the effectiveness of amoxicillin and other antibacterial drugs, amoxicillin should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, the use of amoxicillin is based on practical experience or local epidemiology流行病学 29 Contraindication禁忌 • A history of allergic reaction to any of the penicillins is a contraindication 30 Warnings • Serious and occasionally fatal hypersensitivity (anaphylactic过敏的性 反应 ) reactions have been reported in patients on penicillin therapy. Although anaphylaxis is more frequent following parenteral therapy, it has occurred in patients on oral penicillins. These reactions are more likely to occur in individuals with a history of penicillin hypersensitivity. There have been reports of individuals with a history of hypersensitivity to penicillins who have experienced severe reaction to cephalosporins头孢菌素 (cefazolin头孢唑啉). Before initiating amoxicillin therapy, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins, or cephalosporins. 31 warnings • If an allergic reaction occurs, amoxicillin should • be discontinued Serious anaphylactic reactions require immediate emergency treatment with epinephrine肾上腺素, oxygen, intravenous steroids类固醇, and airway management, including intubation气管插管 should also be administered as indicated 32 Warnings • Pseudomembranous colitis 伪膜性结肠炎 can developed by using amoxicillin • Pseudomembranous colitis, also known as antibiotic- associated diarrhea (AAD), is an infection of the colon . It is often associated with Clostridium Difficile bacteria 难辨梭状芽孢杆菌 • Amoxicillin can cause the normal flora在in the bowel腸道正常菌群to change. This will result in more extensive growth of Clostridium difficile. In addition, C. Difficile can produce toxins 毒 and result in toxic megacolon 毒性巨結腸 . • . 33 Warnings • Pseudomembranous colitis is characterized by offensive-smelling diarrhea, fever, and abdominal pain. • In severe cases, life-threatening complications can develop, such as toxic megacolon 34 Picture of pseudomembranous colitis caused by Clostridium Difficile 35 Dosage and administration • Capsules, tablets and oral suspensions of amoxicillin may be given without regard to meals. The 400 mg suspension and the 875 mg tablet have been studies only when administered at the start of a light meal. However, food effect studies have not been performed with the 200mg and 500 mg formulations Neonates and infants aged < 12 weeks (<3 months) Due to incompletely developed renal function affecting elimination of amoxicilin in this age group, the rrecommended upper dose of amoxicillin is 30 mg/kg/day divided every 12 hours 36 37 Dosing and administration: • The children’s dosage is intended for individuals whose weight is less than 40 kg. Children weighing 40kg or more should be dosed according to the adult recommendations • After re-constitution 水来稀释 , the required amount of suspension should be placed directly on the child’s tongue for swallowing. Alternate means of administration are to add the required amount of suspension to formula, milk, fruit juice, water, ginger ale, or cold drinks. These preparations should then be taken immediately • All patients with gonorrhea 淋病 should be evaluated for syphilis 梅 毒 • Large doses may be required for stubborn or severe infections 38 Duration 为期 • In stubborn infections, therapy may be required for several weeks • In gonorrhea, treatment should be continued for a minimum of 48-72 hours beyond the time that the patient becomes asymptomatic or evidence of bacterial eradication has been obtained • It is recommended that at least 10 days treatment for any infection caused by streptococcus pyogenes 化膿性 鏈球菌 to prevent the occurrence of acute rheumatic fever 風濕熱 39 Dosing recommendations for adults with impaired renal function腎功能差 • Dosing with impaired renal function do not • • generally require a reduction in dose unless the impairment is severe. For patients with glomerular filtration rate腎小 球濾過率 of <30 ml/min should not receive 875 mg tablet (high dose) Patients with glomerular filtration rate of 10-30 ml/min should receive 500mg or 250mg every 12 hours, depending on the severity of the infection. 40 腎功能差 • Patients with less than 10 ml/min GFR should • • receive 500mg or 250mg every 24 hours, depending on the severity of the infection Hemodialysis洗血 patients should receive 500mg or 250mg q 24h, depending on the severity of the infection. They should receive an additional dose both during and at the end of dialysis There are no dosing recommendations for pediatric patients with impaired renal function. 41 Laboratory tests • As with any potent drug, periodic assessment of renal, hepatic, and blood tests should be made during prolonged therapy 评估肾脏,肝脏和血液测试 • • Patients with gonorrhea 淋病 should have a for syphilils 梅毒 serologic test 血清學檢測 • at the time of diagnosis 诊断 . Patients treated with amoxicillin should have a follow up serologic test for syphilis 梅毒 after 3 months 42 Carcinogenesis, mutagenesis, impariment of fertility 致癌,致基因突变 ,损害生育能力 • No carcinogenesis and mutagenesis have been reported or studied in human • In a multi-generation reproduction study 多代繁殖研究 in rats, no impairment of fertility or other adverse reproductive effects were seen at dose up to 500mg/kg ( approximately 3 times the human dose in mg/m2 43 Teratogenic effects 致畸胎 • Reproduction studies 繁殖研究 have been performed in mice and rats • no evidence 没有证据 of impaired fertility损害生育能力 or harm to the fetus due to amoxicillin 伤害到胎儿 • no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response • this drug should be used during pregnancy only if clearly needed 44 Nursing mother 哺乳的母亲 • Penicillins have been shown to excreted in human milk.在人乳分泌 • Amoxicillin use by nursing mother may lead to sensitization 促進 婴儿敏感 of infants . • Caution should be exercised when amoxicillin is administered to a nursing mother • 哺乳的母亲需要小心使用阿莫西林 45 Pediatric use • Because of the incompletely developed renal • function in neonates 新生儿 and young infants, the elimination of amoxicillin may be delayed. 阿莫西林消除可能会迟 Dosing of amoxicillin should be modified in pediatric patients 12 weeks or young • 12周或年轻的患者应修改阿莫西林的 剂量 46 Geriatric use 老人使用 amoxicillin • Clinical data have shown that there are no differences in response between elders and younger patients 47 老人使用 amoxicillin • Amoxicillin is excreted by the kidney, and the • • risk of toxic reaction to this drug may be greater in patients with impaired renal function Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection and it may useful to monitor renal function 由于老年患者可能有肾功能下降,应减少剂量, 和监测肾功能 48 Adverse reaction 不良反应 1. Gastrointestinal 胃肠道 : nausea, vomiting, 2. 3. diarrhea and hemorrhagic/ psuedomembranous colitis 恶心,呕吐,腹泻和出血性/伪膜性结肠炎 Hypersensitivity reactions: erythematous maculopapular rashes紅色斑丘疹, erythema multiforme 多形性紅斑,史蒂文斯約翰遜綜合徵 , Stevens-Johnson syndrome 49 Adverse reaction • Lymphatic systems淋巴系統 : Anemia, including hemolytic anemia溶血性貧血 • thrombocytopenia 血小板減少症, leukopenia白細胞減少症 • agranulocytosis 粒細胞缺乏症 have been reported 50 Adverse reactions • Central nervous system中枢神经系统 : agitation 躁動, anxiety, insomnia, confusion焦虑,失眠,精神错乱 • convulsion抽搐 and dizziness头晕 have been reported 51 Overdose: 过量用药 • Discontinuation of amoxicillin • If the overdose is recent, an attempt to emesis • 嘔吐 or other means of removing the drug from the stomach may be performed. 。 Overdosage of < 250mg/kg of amoxicillin are not associated with significant clinical symptoms and do not require gastric emptying 没有显着的临床症状 • • 没有必要清胃 。 52 Over dose • Crystalluria 結晶尿 from overdose of amoxicillin • • • • may lead to renal failure肾功能衰竭 . Adequate fluid intake 足够的液体 and diuresis 利尿 to reduce the risk of amoxicillin crystalluria. 以减少阿莫西林结晶风险 Amoxicillin may be removed by hemodialysis 血 液透析 阿莫西林可通过血液透析去除 53 Patient information • Amoxicillin may be taken every 8 hours or every • • 12 hours, depending on the strength of the product. 250 mg or 500mg may be given every 8 hours by mouth. Or 500mg to 875 mg twice a day or extended release tablets 缓释片 775 mg once daily. Amoxicillin does not treat virus infection病毒感染 ( common cold) only bacterial infections细菌感 染. 54 Patient information • The medication should be taken exactly as • • • • directed. 用药应采取的指示 Not completing the full course of therapy may: 未完成全程服药 1. decrease the effectiveness of the treatment 2. increase the chance of resistant to amoxicillin or other antibacterial drug in the future. 增加对阿莫西林耐药抗的机会 55 Patient information • Take amoxicillin with or without food. Take with food if it causes upset stomach 导致胃部不适 • Chewable tablet 咀嚼片 : chew or crush well. Mix crushed tablet with food. Do not swallow whole 不要吞下整个丸 • Extended release tablet 缓释片 : take with food. Swallow whole. Do not chew or break • Take a missed dose as soon as possible. If it is almost time for the next dose. Skip the missed dose and return to your regular schedule • Do not take a double dose or extra dose • 不要服用两个或额外的剂量 56 How should amoxicillin be stored应该如何储 存阿莫西林 • Store capsules or tablets at room temperature • Protect capsules and tablets from moisture 湿气 • • . Do not store in a bathroom or kitchen cabinet Store liquid suspension at room temperature or in a refrigerator冰箱 . Do not freeze. Throw away any unused portion after 2 weeks Talk with your physician or pharmacist if you are starting any new medicine, including over the counter supplements, medications, herbal or vitamins 补充剂,药物,草药或维生素 57 How does amoxicillin comes? • Capsule胶囊 , oral :250mg, 500mg • Powder oral粉剂 : 125mg/5ml (80ml, 100ml, • • • 150ml) 200mg/5ml (50ml, 75ml, 100ml, 150ml); 400mg/5ml (50ml, 75ml, 100ml) Tablet: oral 500mg or 875mg Tablet chewable, oral: 125mg, 200mg, 250mg, 400mg Tablet extended release, oral: 775 mg 58 Thank you! • I hope you have learnt many medical terminology and medical English from this presentation • This presentation is based on amoxicillin drug insert by Sandoz company 59