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Adrenoceptor Antagonist Drugs 肾上腺素受体阻断药 11 Antagonist of α Antagonist of β Antagonist of αβ 第1节 α肾上腺素受体阻断药 αAntagonist Drugs Non-selective α Antagonist: 1. Short: Phentolamine Tolazoline 2. Long: Phenoxybenzamine I. Non-selective α Antagonist Phentolamine, Inj. Tolazoline, Tab., Inj. Effect: Phentolamine Tolazoline Reversible 1. Heart—Stimulation? 2. Blood Vessel—Dilation 3. Others: cholinoceptor agonist effect? [INDICATIONS] 1. Peripheral Vascular Disease 2. Local Vasoconstrictor Excess 3. Pheochromocytoma? 4. Shock? 5. Hypertension induced by agents [Side Effects] 1. Dizziness or drowsiness(Low BP)2. Fast heartbeat3. Prolonged painful erection of the penis4. Vomiting? 5. Facial flushing6. Nasal stuffiness?7. Nausea Slow Injection or Infusion Phenoxybenzamine 酚苄明 Noncompetitive alpha-R antagonist? Inhibition of Up-take 1 and Up-take 2 2. Onset: 1h. Duration: 3-4 days. [ADME] A prodrug and Stored in fat tissues and thus it has a long duration(3-4d). Onset: 1h. [ACTION] It has no effect on the parasympathetic system? Somewhat selective for alpha 1. [INDICATIONS] 1. Peripheral Vascular Disease 2. Shock 3. Pheochromocytoma 4. Prostatic Hyperplasia SIDE EFFECTS: Stomach upset ? Nasal congestion,weakness? Constricted pupils? Postural hypotention? Cardiac arrhythmia? II. α1 Antagonist Prazosin 哌唑嗪 α1>>α2 Less effects on heart PNS? Usage: hypertension 特拉唑嗪 Terazosin 坦洛新 Tamsulosin, alpha 1A Prostatic Hyperplasia II. α2 Antagonist Yohimbine 育亨宾 1. Alpha adrenoceptor COVALENT blocker: ??A.propranolol B.phenoxybenzamine ?? C.phentolamine D.pilocarpine 2. Pressor effects of epinephrine are blocked by this drug (epinephrine reversal) A.??propranolol (Inderal) B.??phentolamine (Regitine) C.??phenylephrine (Neo-Synephrine) D.??metoprolol (Lopressor) 3. Therapeutic use of esmolol (Brevibloc): A.??bronchial asthma B.??ant
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