药品详细
Pindolol(吲哚洛尔)
化学结构式图
中文名
吲哚洛尔
英文名
Pindolol
分子式
C14H20N2O2
化学名
[2-hydroxy-3-(1H-indol-4-yloxy)propyl](propan-2-yl)amine
分子量
Average: 248.3208
Monoisotopic: 248.152477894
Monoisotopic: 248.152477894
CAS号
13523-86-9
ATC分类
C07A 未知;C07A 未知;C07A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A moderately lipophilic beta blocker (adrenergic beta-antagonists). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
生产厂家
- Genpharm pharmaceuticals inc
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Mutual pharmaceutical co inc
- Mylan pharmaceuticals inc
- Nostrum laboratories inc
- Novartis pharmaceuticals corp
- Purepac pharmaceutical co
- Sandoz inc
- Teva pharmaceuticals usa inc
- Watson laboratories inc
封装厂家
- Advanced Pharmaceutical Services Inc.
- Ivax Pharmaceuticals
- Major Pharmaceuticals
- Merckle GmbH
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Novartis AG
- Novopharm Ltd.
- Pharmaceutical Utilization Management Program VA Inc.
- Physicians Total Care Inc.
- Qualitest
- Sandhills Packaging Inc.
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | For the management of hypertension, edema, ventricular tachycardias, and atrial fibrillation. | ||||||
| Pharmacodynamics | Pindolol is a non-selective beta-adrenergic antagonist (beta-blocker) which possesses intrinsic sympathomimetic activity (ISA) in therapeutic dosage ranges but does not possess quinidine-like membrane stabilizing activity. Pindolol impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Pindolol is nonpolar and hydrophobic, with low to moderate lipid solubility. Pindolol has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, pindolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action. | ||||||
| Mechanism of action | Pindolol non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. By binding beta-2 receptors in the juxtaglomerular apparatus, Pindolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively. | ||||||
| Absorption | Rapidly and reproducibly absorbed (bioavailability greater than 95%). | ||||||
| Volume of distribution |
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| Protein binding | 40% | ||||||
| Metabolism |
Hepatic. In man, 35% to 40% is excreted unchanged in the urine and 60% to 65% is metabolized primarily to hydroxy-metabolites which are excreted as glucuronides and ethereal sulfates.
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| Route of elimination | Pindolol undergoes extensive metabolism in animals and man. In man, 35% to 40% is excreted unchanged in the urine and 60% to 65% is metabolized primarily to hydroxy-metabolites which are excreted as glucuronides and ethereal sulfates. About 6% to 9% of an administered intravenous dose is excreted by the bile into the feces. | ||||||
| Half life | 3 to 4 hours | ||||||
| Clearance |
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| Toxicity | LD50=263 mg/kg (orally in rats). Signs of overdose include excessive bradycardia, cardiac failure, hypotension, and bronchospasm. | ||||||
| Affected organisms |
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| Pathways |
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理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Acetohexamide | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Aminophylline | Antagonism of action and increased effect of theophylline |
| Chlorpromazine | Increased effect of both drugs |
| Chlorpropamide | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Clonidine | Increased hypertension when clonidine stopped |
| Dihydroergotamine | Ischemia with risk of gangrene |
| Dihydroergotoxine | Ischemia with risk of gangrene |
| Diltiazem | Increased risk of bradycardia |
| Disopyramide | The beta-blocker, pindolol, may increase the toxicity of disopyramide. |
| Dyphylline | Antagonism of action and increased effect of theophylline |
| Epinephrine | Hypertension, then bradycardia |
| Ergonovine | Ischemia with risk of gangrene |
| Ergotamine | Ischemia with risk of gangrene |
| Fenoterol | Antagonism |
| Formoterol | Antagonism |
| Gliclazide | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Glipizide | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Glisoxepide | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Glyburide | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Glycodiazine | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Ibuprofen | Risk of inhibition of renal prostaglandins |
| Indomethacin | Risk of inhibition of renal prostaglandins |
| Insulin Glargine | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Isoproterenol | Antagonism |
| Lidocaine | The beta-blocker increases the effect and toxicity of lidocaine |
| Mesoridazine | Increased risk of cardiotoxicity and arrhythmias |
| Methyldopa | Possible hypertensive crisis |
| Methysergide | Ischemia with risk of gangrene |
| Orciprenaline | Antagonism |
| Oxtriphylline | Antagonism of action and increased effect of theophylline |
| Pipobroman | Antagonism |
| Pirbuterol | Antagonism |
| Piroxicam | Risk of inhibition of renal prostaglandins |
| Prazosin | Risk of hypotension at the beginning of therapy |
| Procaterol | Antagonism |
| Repaglinide | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Salbutamol | Antagonism |
| Salmeterol | Antagonism |
| Terazosin | Increased risk of hypotension. Initiate concomitant therapy cautiously. |
| Terbutaline | Antagonism |
| Theophylline | Antagonism of action and increased effect of theophylline |
| Thioridazine | Increased risk of cardiotoxicity and arrhythmias |
| Tolazamide | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Tolbutamide | The beta-blocker, pindolol, may decrease symptoms of hypoglycemia. |
| Treprostinil | Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. |
| Verapamil | Increased effect of both drugs |
食物相互作用
- Magnesium, potassium and zinc needs increased.
- Take without regard to meals. Avoid alcohol.
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