Week 02 Adrenergic Agonists Flashcards
(26 cards)
Classification of Adrenergic Agonists (and definitions of each category)
- (1) Direct Acting adrenergic agonists
- act directly on a or b receptors, producing effects similar to those that occur following stimulation of Sympathetic nerves or release of the hormone EPINEPHRINE from the Adrenal Medulla - (2) Indirect Acting adrenergic agonists
- cause NOREPINEPHRINE release from Presynaptic Terminals, or Inhibit the uptake of Nor-epinephrine - (3) Mixed-Action adrenergic agonists
- induce the Release of NOREPINEPHRINE from Presynaptic Terminals
- directly stimulates Both a and b receptors on the Postsynaptic Membrane
Definition of Direct Acting adrenergic agonists
- 1 of the 3 categories of adrenergic agonists
- act directly on a or b receptors,
- producing effects similar to those that occur following stimulation of Sympathetic nerves or release of the hormone EPINEPHRINE from the Adrenal Medulla
Subcategories of Direct Acting adrenergic agonists
1) Catecholemines 儿茶酚胺
2) Noncatecholermines
Definition of Catecholemines
- in the category of Direct Acting adrenergic agonists
- 含有邻苯二酚(即儿茶酚)的胺类化合物，包括多巴胺、去甲肾上腺素和肾上腺素及它们的衍生物
- (off the notes–) catecholamines are hormones released by adrenal glands when a person is faced with any type of stress. This is a fight-or-flight response. The role is to increase breathing rate, heart rate, blood pressure, muscle strength and mental alertness
Name a few drugs of Catecholemines
- EPINEPHRINE (Adrenaline) a1, a2, b1, b2: for intense asthma, Anaphylactic shock (过敏) etc.
- Norepinephrine (Levophel) a1, a2, b1
- Isoproterenol (Isuprel) b1, b2
- DOBUTAMINE (Debutrex) b1: Drug of choice to Stimulate HT
- DOPAMINE (Intropin) a1, b1: used to treat shock
EPINEPHRINE (Adrenaline)
Catecholemines, Direct Acting adrenergic agonist. 肾上腺素
- a1, a2, b1, b2
- used for intense Asthma, Anaphylactic shock 过敏休克 etc.
Norepinephrine (Levophel)
Catecholemine, Direct Acting adrenergic agonist. a1, a2, b1
- 降肾上腺素／去甲肾上腺素
- 是一种肾上腺素受体激动药，有收缩血管、升高血压的作用
- treat low blood pressure and HT failure (from internet, not on class note)
Isoproterenol (Isuprel)
Catecholemines, Direct Acting adrenergic agonist. b1, b2.
- treats certain types of heart problems, also improves breathing while you are under anesthesia (not in class notes)
- 异丙（去甲）肾上腺素
- 临床上主要利用它的升压作用，静滴用于各种休克（但出血性休克禁用），以提高血压、保证对重要器官（如脑）的血液供应. 使用时间不宜过长，否则可引起血管持续强烈收缩.
- 可用于支气管哮喘，心脏聚停，房室传导阻滞。有抗休克的作用。
DOBUTAMINE (Debutrex)
Catecholemine, Direct Acting adrenergic agonist. b1
- Drug of choice to STIMULATE HT
- 多巴酚丁胺, 选择性心脏β1-受体兴奋剂
- 直接激动心脏β1受体以增强心肌收缩和增加搏出量，使心排血量增加
- 与多巴胺不同，多巴酚丁胺并不间接通过内源性去甲肾上腺素的释放，而是直接作用于心脏
- 口服无效，需静脉注射
DOPAMINE (Intropin)
Catecholemines, Direct Acting adrenergic agonist. a1, b1
- used to treat SHOCK
- 用于各种类型的休克，尤其适用于休克伴有心收缩力减弱，肾功能不全者
Definition of Noncatecholamines
- in the category of Direct Acting adrenergic agonists
off the notes: - are adrenergic drugs that are used to activate the alpha and beta preceptors. These drugs do not contain catechol in their nucleus
- used as treatment for various ailments such as against constriction of blood cells, for achieving muscle relaxation with ease, for nasal and eye decongestion and for dilatation of bronchi
Name a few drugs under the Noncatecholermines category
- PHENYLEPHRINE (Neo-Synephrine) a1: causes intense vasoconstriction
- TERBUTALINE (Brethine) b2: bronchodilator
- ALBUTEROL (Ventolin) b2: bronchodilator
- SALMETEROL (Serevent) b2: long acting bronchodilator
- Formoterol (Foradil) b2: long acting bronchodilator
PHENYLEPHRINE (Neo-synephrine)
Noncatecholermines, Direct Acting adrenergic agonist. a1
- 苯肾上腺素 “新福林”／”苯福林”（一种血管收缩剂）
- causes Intense Vasoconstriction
TERBUTALINE (Brethine)
Noncatecholermine, Direct Acting adrenergic agonist. b2
- “特必林” “特布他林” 气管扩张剂
- Bronchodilator
ALBUTEROL (Ventolin)
Noncatecholermines, Direct Acting adrenergic agonist. b2
- “舒喘灵”，沙丁胺醇(β-肾上腺素受体兴奋剂，用作治疗哮喘以及其它梗阻性肺病的支气管扩张剂)
- used as Bronchodilator
SALMETEROL (Serevent)
Noncatecholermines, Direct Acting adrenergic agonist. b2
- LONG Lasting bronchodilator
- “沙美特罗” (β2促效剂、扩张支气管)
- 新型选择性长效β2受体激动剂，一次剂量其支气管扩张作用可持续12小时。尚有强大的抑制肺肥大细胞释放过敏反应介质作用，可抑制吸入抗原诱发的早期和迟发相反应，降低气道高反应性。用于哮喘（包括夜间哮喘和运动性哮喘）、喘息性支气管炎和可逆性气道阻塞。
Formoterol (Foradil)
Noncatecholermines, Direct Acting adrenergic agonist. b2
- Long acting bronchodilator
- 福莫特罗（支气管扩张药）
- 是一种长效的选择性肾上腺素β2受体激动药，具有支气管扩张作用，且呈剂量依赖关系。能使第1秒用力呼气量(FEV1)、用力肺活量(FVC)和呼气峰流速(PER)增加。口服80mg本品，4小时后，扩张作用最强，其效应与口服4mg沙丁胺醇相当，但作用持久。本品还有抗组胺作用，能抑制肺肥大细胞释放组胺，其作用与组胺H1-受体拮抗药、肥大细胞稳定药酮替芬类似。
Definition of Indirect Acting adrenergic agonists
- 1 of 3 groups of Adrenergic Agonists
* cause Norepinephrine (降肾上腺素，去甲肾上腺素) release from Presynaptic Terminals or Inhibit the uptake of Nor-epinephrine
Name a few drugs under the category Indirect Acting Adrenergic Agonists
- AMPHETAMINE - has CNS stimulatory effects. used for Narcolepsy, ADHD, Appetite control (has bad reputation)
- METHYLPHENIDATE (Ritalin) - same
- Dextroamphetamine (Dexedrine) - same
- Tyramine - no clinical use, found in fermented food
AMPHETAMINE
Indirect Acting adrenergic agonist
- has CNS Stimulatory effects
- used for Narcolepsy 嗜睡症, ADHD, Appetite control
- has bad reputation (restricted drug, 可制成毒品)
- (off the notes–) could be extracted from 麻黄？
METHYLPHENIDATE (Ritalin)
Indirect Acting adrenergic agonists
- CNS stimulatory, for narcolepsy, ADHD, appetite control
- “利他灵”（一种中枢兴奋药）, 又称”聪明药”，但长期使用也容易上瘾
Dextroamphetamine (Dexedrine)
Indirect Acting adrenergic agonists
- CNS stimulatory, used for narcolepsy, ADHD, appetite control
- 甲基苯丙胺. 與苯丙胺的化學結構非常相似。甲基苯丙胺是由日本化學家長井長義於1893年自麻黃鹼成功合成
Tyramine
Indirect Acting adrenergic agonist
- no clinical use
- found in fermented food, e.g. ripe cheese, is oxidized by MAO (Manoamine Oxidase)
- if a patient taking MAO-inhibitors eat cheese, then the tyramine of cheese cannot be oxidized. Tyramine then enters nerve terminal, displaces stored Norepinephrine, causing HYPERTENSIVE CRISIS.
- such patient can take 1 or 2 25mg tablets of Chlorpromazine if symptoms occur, then rush to ER
Definition of Mixed-Action adrenergic agonists
- 1 of the 3 groups of Adrenergic Agonists
- induce the Release of Norepinephrine (降肾上腺素，去甲肾上腺素) from PRESYNAPTIC terminals
- Directly Stimulates BOTH a and b receptors on POSTSYNAPTIC Membrane
