2015年第11章传出神经药物.pptVIP

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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 heartbeat 3. Prolonged painful erection of the penis 4. Vomiting? 5. Facial flushing 6. 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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