part 10. local anesthetics (局部麻醉药)
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Part 10. Local anesthetics (局部麻醉药). Peripheral mechanisms of pain. 1. Pharmacological effects: (1)Local anesthetic effects: local analgesia( 局部痛觉消失 ) ① Characteristics of effects: ▲ non-specific. ▲ reversibility. ② Mechanism of effects: - PowerPoint PPT PresentationTRANSCRIPT
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Part 10.Local anesthetics
( 局部麻醉药 )
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Peripheral mechanisms of pain2
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1. Pharmacological effects: (1)Local anesthetic effects: local analgesia( 局部痛觉消失 ) ① Characteristics of effects: ▲ non-specific. ▲ reversibility. ② Mechanism of effects: by blocking sodium influx of neural
cell membrane.
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Mechanism of effects:
by blocking sodium influx of neural cell membrane.
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(2)Systemic effects( 全身作用 ) (absorptive effects, 吸收作用 ): ①CNS effects: Initial time, exciting: vertigo( 眩晕 ), dysphoria( 烦躁 ), anxi-ety( 焦虑 ), muscular tremor( 肌肉震颤 ), Later mental confusion( 精神错乱 ), convulsion( 惊厥 ), Last coma( 昏迷 ), respiratory para-lysis( 呼吸麻痹 ) dead. ②Cardiovascular effects heart inhibited, vasodilation, BP .
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2. Main methods of local anes-thesia( 主要的局麻方法 ):
(1)Surface anesthesia( 表面麻醉 ) (2)Infiltration anesthesia( 浸润麻醉 ) (3)Conduction anesthesia( 传导麻醉 ) (4)Epidural ansthesia( 硬膜外麻醉 ) (5)Subarachoid anesthesia( 蛛网膜下腔
麻醉 ) or Spinal anesthesia( 脊髓麻醉或腰麻 ).
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Peripheral mechanisms of pain
①
② ③④⑤
(1)Surface anesthesia( 表面麻醉 ) (2)Infiltration anesthesia( 浸润麻
醉 ) (3)Conduction anesthesia( 传导麻
醉 ) (4)Epidural ansthesia( 硬膜外麻醉 ) (5)Subarachoid anesthesia( 蛛网膜
下腔麻醉 ) or Spinal anesthesia( 脊髓麻醉或腰麻 ).
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3. Local anesthetics most in use:
COCH2CH2N
OC2H5
H2N
C2H5
NHCCH2N
OC2H5
C2H5
CH3
CH3
COCH2CH2N
OCH3
CH3
HN
H9C4
普鲁卡因
procaine
利多卡因
lidocaine
丁 卡 因tetracaine
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3. Local anesthetics most in use: Procaine( 普鲁卡因 ): weak, lipid solubility small, toxicity small, safety. 30’ ~45’ 1 ○②③④⑤ Lidocaine( 利多卡因 ): stronger, toxicity small, lipid solubility large, safety. 90’ 2 ①②③④⑤ Tetracaine( 丁卡因 ): strongest, toxicity high, lipid solubility large, 120’ 10 ①○③④⑤ Bupivacaine( 布比卡因 ): 3 ~ 4 times stronger than Lidocaine. 120’ 6.5 ○②③④○ (1)Surface anesthesia( 表面麻醉 )
(2)Infiltration anesthesia( 浸润麻醉 ) (3)Conduction anesthesia( 传导麻
醉 ) (4)Epidural ansthesia( 硬膜外麻醉 ) (5)Subarachoid anesthesia( 蛛网膜下
腔麻醉 ) or Spinal anesthesia( 脊髓麻醉或腰麻 ).
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4. Influencing factors of anesthe- tic effect: (1)Size of nerves & nerve fibers; (2)pH of body fluid;
(3)Medicated with vasoconstrictors: ▲ prolong duration of action; ▲ decrease systemic absorption; ▲ decrease operative bleeding.
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5. Adverse reactions: (1)Toxic reaction: ①CNS effects; ②Cardiovascular effects: Preventive measures: ▲ separate administration; ▲ put a little adrenaline into local anesthetics solution: 1/250,000 ~ 1/500,000. (2)Anaphylaxis( 过敏反应 ): Preventive measures: ▲ skin test; ▲ small dose begin; Emergency treatment.
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Part 11. Antipyretic, analgesic, andanti-inflammatory drugs ( 解热镇痛抗炎药 ) —— Non-steroid anti-inflammatory
drugs (NSAIDs, 非甾体抗炎药 )
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1.General pharmacological properties(1)Inhibition of PG biosynthesis:
Phospholipids of cell menbrane Phospholipase A2 (PLA2, 磷脂酶 A2) Arachidonic acid ( 花生四烯酸 ) Cyclooxygenase Lipoxygenenase (Cox, 环氧酶 ) ( 脂氧酶 ) PGG2 5-HPETE
Prostaglandins(PGs) Leukotriene(LTs) ( 前列腺素 ) ( 白三烯 )
NSAIDs (-)
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(2)Products of Cyclooxygenase(COX)
Arachidonic acid ( 花生四烯酸 ) COX PGG2
合成酶 PGI2synthetase TXA2synthetase PGH2 Isomerase Reductase 异构酶 还原酶
PGI2 PGE2 PGF2 TXA2
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Effects of products of COX:
PGE2 : inducing inflammation, fever,algogenic ( 致痛 ) effect, uterine constriction ( 子宫收缩 ); PGF2: bronchoconstriction, vaso-constriction; PGI2 : platelet depolymerization ( 血小板解聚 ); vasodilation,
TXA2 : platelet aggregation ( 血小板聚集 ), vasoconstriction. 17
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(3)Cyclooxygenase(COX, 环氧酶 ) It can be divided into two kinds of isoforms( 同功酶 ): COX-1, COX-2. COX-1 is a constitutive isoform found in blood vessel, stomach, and kidney, it regulates vessel constriction and relaxation, secretion of gastric acid, and renal blood flow. COX-2 is a induced isoform that can be induced by cytokines and inflammatory mediators in settings of inflammation, to promote inflammation.
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Most antipyretic ( 解热 ) and analgesic ( 镇痛 ) drugs are non-selective inhibitors to COX-1 and COX-2, but some
new drugs(such as celecoxib, 塞来昔布 ) are selective inhibitors to COX-2, the latter’s ADR is less.
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2. Classification of antipyretic, anal- gesic and anti-inflammatory drugs according to chemical structure: (A)Salicylates: Aspirin( 阿司匹林 ) (B)Aminobenzene derivatives: Paracetamol( 对乙酰氨基酚 ) (C)Indole derivatives: Indomethacin( 吲哚美辛 ) (D)Propionic acid derivatives: Ibuprofen( 布洛芬 ) (E)Selective COX-2 inhibitor: Celecoxib( 塞来昔布 ) (F)Others: Phenylbutazone( 保泰松 )
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(A)Salicylates:
Acetylsalicylic acid( 乙酰水杨酸 ,Aspirin, 阿司匹林 )
1. Pharmacological effects and clinical uses: Aspirin can inhibit COX-1 and COX-
2, there are antipyretic, analgesic, anti-inflammatory and anti-rheumatic effects, etc.
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(1)Antipyretic effect: Endogenous pyrogen( 内源性致热原 , interleukin-1, 白介素 -1, IL-1) can stimulated synthesis of PGs (especially PGE2 ) in hypothalamus ( 下丘脑 ). PGs can act on heat-regulating center, to ↑ body temperature. Aspirin can inhibit the synthesis of PGs in hypothalamus, to treat fever.
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(2)Analgesic effect Aspirin inhibits COX-2, decrease
synthesis of PGE2 in the regions of pain. PG is an algogenic ( 致痛 ) substance and hyperalgic substance. (Bradykinin ( 缓激肽 ) is a main algogenic substance)
Aspirin can be used to treat pain of low-to-moderate intensity, such as headache, toothache, dysmenorrhea ( 痛经 ), muscular pain, neuralgia ( 神经痛 ), etc.
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(3)Anti-inflammation and anti-rheumatism:
Aspirin inhibit COX-2 and synthesis of PG in the inflammatory region, to
alleviate inflammation and symptoms. PG is an inflammatory substance.
Aspirin can be used ① to treat acute rheumatic fever( 急性风湿热 ), ② to abate pain and symptoms of rheumatic & rheumatoid arthritis ( 风湿性和类风湿性关节炎 ).
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(4)Inhibition of platelet aggregation:
COX-1 and TXA2 ( 血栓素 ) synthetase in platelet catalyze TXA2 synthesis, to promote platelet aggregation.
COX-1 and PGI2 synthetase in intima( 内膜 ) of blood vessel catalyze PGI2 synthesis, promote vasodilation and platelet depolymerization ( 血小板解聚 ).
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Small dose(40mg/day) of Aspirin can inhibit COX-1 in platelet, TXA2 synthesis , inhibit platelet aggregation. Large dose of Aspirin can inhibit COX-1 in in intima of blood vessel, PGI2 synthesis , promote platelet aggregation.
Therefore, small dose Aspirin can be used to prevent coronary artery thrombosis ( 血栓形成 ), to treat ischemic ( 缺血 ) heart disease, and reduce the mortality of myocardiac infarction ( 心肌梗死 ), and prevent cerebral thrombosis ( 脑血栓 ) too. 26
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(5)Other clinical uses: ▲ Senile dementia( 老年性痴呆 ).
▲ Hypertension of pregnancy and preeclampsia( 先兆子痫 )
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2. Pharmacokinatics: (1)Absorption: It is absorbed fast in stomach by po.; (2)Biotransformation: Aspirin is transformed to salicylic acid ( 水
杨酸 ) form in the body;(3)Plasma protein binding rate: 80%-90%;(4) Metabolism: in liver by conjugation with glycine ( 甘氨酸 ) and glucuronic acid ( 葡糖醛酸 );
(5) Elimination: When the dose > 1g, Nonlinear
elimination kinetics (zero-order kinetics 零级动力学 ). 28
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3. Adverse reaction:(1)Gastrointestinal reactions: irritation and hemorrhea ( 大出血 ).(2)Prolongation of bleeding time: inhibit platelet aggregation and synthesis of thrombogen( 凝血酶原 ). Contraindications: One week prior to surgery; Severe hepatic damage, Vitamin K deficiency, Prothrombinopenia( 凝血酶原减少症 ).(3)Allergy: urticaria( 荨麻疹 ), angioneurotic edema ( 血管神经性水肿 ), aspirin-induced asthma.
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Aspirin-induced asthma: Phospholipids of cell menbrane
Aspirin PLA2
(-) Arachidonic acid
Cyclooxygenase Lipoxygenenase ( 环氧酶 ) ( 脂氧酶 ) PGG2 5-HPETE
白三烯 Prostaglandin(PGs)
Leukotriene(LTs)
attack of asthma30
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(4)Salicylism ( 水杨酸反应 ): dose > 5g/d: CNS symptoms, even mental disorder; hyperventilation ( 换气过度 ).
iv NaHCO3 can promote the excretion of Aspirin.
(5)Hepatic damage: Overdose hepatic damage; Reye’s syndrome( 瑞夷综合征 ): in children, severe hepatic damage( 严重的肝损害 ) and encephalopathy( 脑病 )
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(B)Aminobenzene derivatives:Acetaminophen( 对乙酰氨基酚 ,
Paracetamol, 扑热息痛 ) It is the metabolite of phenacetin( 非那西
丁 ) in the body. Its antipyretic and analgesic effects are mild and lasting, but anti-inflammatory effects is less.
It is a higher selectivity to COX in the central nervous system.
Common mainly used in cold, fever, and headache, etc.
Overdose can damage liver & kidney.32
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(C)Indole derivatives:Indomethacin( 吲哚美辛 )
1. Potent anti-inflammatory agent It is a non-selective inhibitor to COX. Its
antipyretic, analgesic, and anti-inflammatory effects are very strong.
2. Clinical uses: Rheumatic and rheumatoid arthritis; Ankylosing spondylitis( 强直性脊髓炎 ); Osteoarthritis( 骨关节炎 ); Some types of fever.
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3. Adverse reaction: more and serious. GI reaction; CNS symptoms (headache, vertigo); hematological reactions (WBC↓, platelet↓); allergy(skin rash, asthma).
Sulindac( 苏林酸 ) It is a prodrug and appears inactive in vitro, but its metabolite in vivo is very active and as an strong inhibitor of COX.
Its GI reaction is very mild.
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(D)Propionic acid derivatives: There are Naproxen( 萘普生 ), Ibuprofen( 布洛芬 ), etc.
Naproxen( 萘普生 ) 1. Anti-inflammatory effect: A potent anti-inflammatory agent, the
potency is stronger than Aspirin 20 times; 2. Clinical uses: Used for rheumatic and rheumatoid
arthritis, t ½ 14 hr, bid. 3. Adverse reaction: less, blurred vision
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Ibuprofen( 布洛芬 )1. A potent anti-inflammatory agent, the anti-inflammatory effect is the same as Aspirin;
2. Used for rheumatic & rheumatoid arthritis, etc.
3. Adverse reaction: less. blurred vision, toxic amblyopia( 中毒性弱视 ).
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(E)Selective COX-2 inhibitor:
Celecoxib( 塞来昔布 ) 1. Pharmacological effects: Selectively inhibiting COX-2. 2. Clinical uses: to treat rheumatic and rheumatoid arthritis, t½=11.2 hr, 100 mg, bid.
3. Adverse reaction: less, mainly GI stimulation.
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(F)Others:Oxyphenbutazone( 羟基保泰松 )
1. Potent anti-rheumatic agent;2. Clinical uses: Rheumatic & rheumatoid arthritis;3. Adverse reaction: GI reaction; retention of water and sodium ( 水钠潴留 ); Allergy; lever & kidney damage; thyroid enlargement ( 甲状腺肿大 ) and mucous edema ( 黏液水肿 ), etc. 4. Drug interaction: Plasma protein binding rate: 98%.38
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Diclofenac( 双氯芬酸 )1. Effects: Belong to fenamates( 灭酸类 ), the potency inhibiting COX is stronger than indomethacin ( 吲哚美辛 ).
2. Clinical Uses: Used for rheumatic & rheumatoid arthritis, etc.
3. Adverse reaction: More.
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Part 12.CNS stimulatants
( 中枢兴奋药 )
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CNS stimulatants can be divided into 3 kinds:
(1)Drugs that mainly stimulating cerebral cortex ( 大脑皮层 ):
Caffeine ( 咖啡因 ) (2)Drugs that mainly stimulating
medulla oblongata ( 延髓 ) respiratory center:
Nikethamide ( 尼可刹米 ) (3)Drugs stimulating spinal cord ( 脊
髓 ):Strychnine ( 士的宁 )41
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Ⅰ. Drugs that mainly stimulating cerebral cortex:
Caffeine ( 咖啡因 )1. Pharmacological effects: (1)Small dose: ① stimulating cerebral cortex, in high spirits, eliminating tire, promoting work efficiency; ② can contract cerebral vessel, bring down the intracranial pressure ( 颅内压 ); ③ can strengthen the effects of antipyretic-analgesics( 解热镇痛药 ).
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(2)Larger dose: To excite respiratory center and vasomotor ( 血管舒缩 ) center of medulla oblongata ( 延髓 ) directly,
to make respiration deep and fast, myocardial contractive force, heart rate, cardiac output, Bp.
lead to insomnia.
(3)Overdose: lead to convulsion ( 抽搐 ), especially in children.
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2. Clinical uses: (1)As a composition of drinks: to recover from fatigue ( 疲劳 ) and sleepy; (2)Compatibility( 配伍 ) with other drugs: Compatibility with antipyretic analge-sics( 解热镇痛药 ), can increase the latter’s analgesic effects, to treat common cold and headache; Compatibility with Ergotamine( 麦角胺 ) can be used to treat migraine( 偏头痛 ). (3)Emergency treatment of respiratory and circulatory failure ( 呼吸循环衰竭 ): The preparation is caffeine sodium benzoate(CSB, 苯甲酸钠咖啡因 ), sc or im.
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3. Adverse reaction: Insomnia( 失眠 ); Convulsion/overdose, especially children in fever. But, the children in fever should not take the drug contained caffeine, such as APC(复方阿司匹林 ), to avoid leading to cause convulsion.
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Methylphenidate(哌甲酯 , Ritalin, 利他林 )
1. Pharmacological effect: a milder central stimulants. (1)Stimulating mental activity: more potent, can excite spirit & eliminate depressant symptoms; (2)Stimulating respiratory center: but weaker; (3)Overdose: lead to Bp , headache, even convulsion.
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2. Clinical Uses: (1)Child enuresis( 小儿遗尿症 ): lightly stimulating cerebral cortex, easy to wake up by urinary feeling at night. (2)Central respiratory failure: such as severe infection disease, overdose of central inhibitor, etc. 呼吸三联针 : Ritalin ( 利他林 ) 20 mg, Lobeline ( 洛贝林 )12 mg, Demifline (回苏灵 )16 mg, in 10% glucose 250~500ml, iv. gtt.
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(3)Child hyperactive syndrome: (儿童多动综合征 )
The patients of child hyperactive syndrome lack one of the neurotran-smitters of NA, DA, 5-HT in brain.
Ritalin can promote those neuro-transmitters release from the ending of
CNS, to control child hyperactive syndrome.
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Ⅱ. Drugs that mainly stimulatingrespiratory center:
Nikethamide( 尼可刹米 , Coramine, 可拉明 )
(1)Direct action: stimulating respiratory center of medulla oblongata;
(2)Indirect action: stimulating chemoreceptor of carotid sinus (颈动脉窦 )& aortic sinus ( 主动脉窦 ), reflexly stimulating respiratory center.
The effect is shorter(5’~10’) and milder.
Convulsion/overdose.49
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Demifline(二甲弗林 , 回苏灵 ) Directly stimulating respiratory center of medulla oblongata;
The potency of Demifline is 100 times of Nikethamide ( 尼可刹米 ).
Used to central respiratory inhibition. im. or iv.
Characteristics : to take effect fast, the curative effect well, and the rate of resuscitation high.
Convulsion/overdose. if iv, should inject slowly after dilution. 50
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Lobeline (山梗菜碱 , 洛贝林 )
Only indirect action: to stimulate chemoreceptor of carotid sinus (颈动脉窦 ) and aortic sinus( 主动脉窦 ), reflex stimulating respiratory center. Effect of stimulating respiration is milder and shorter, the margin of safety
is large, adverse reaction less, suitable to child. 51