| 药品名称 | Isoprenaline |
|---|---|
| 分子靶点 | Beta-1 adrenergic receptor;Beta-2 adrenergic receptor;Beta-3 adrenergic receptor;Mitogen-activated protein kinase 1;Phosphatidylinositol 3-kinase regulatory subunit alpha;Phosphatidylinositol 3-kinase regulatory subunit beta;Phosphatidylinositol 3-kinase |
| 酶 | Cytochrome P450 1A1 |
| 药物类型 | Small Molecule |
| 研发阶段 | Approved, Investigational |
| 药物描述 | Isopropyl analog of epinephrine; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant. |
| 结构式 |
 |
| 药物别名 | (±)-isoprenaline;(±)-isoproterenol;1-(3,4-dihydroxyphenyl)-2-(isopropylamino)ethanol;1-(3,4-dihydroxyphenyl)-2-isopropylaminoethanol;3,4-dihydroxy-α-[(isopropylamino)methyl]benzyl alcohol;Isoprenalina;Isoprenaline;Isoprénaline;Isoprenalinum;Isopropyl noradrenaline;Isoproterenol;N-isopropyl-β-dihydroxyphenyl-β-hydroxyethylamine;N-Isopropylnoradrenaline;N-Isopropylnorepinephrine;α-(isopropylaminomethyl)protocatechuyl alcohol |
| 治疗类别 | Adrenergic Agents;Adrenergic Agonists;Adrenergic and Dopaminergic Agents;Adrenergic beta-2 Receptor Agonists;Adrenergic beta-Agonists;Adrenergics for Systemic Use;Adrenergics, Inhalants;Agents producing tachycardia;Agents that produce hypertension;Alcohols;Amines;Amino Alcohols;Anti-Asthmatic Agents;Autonomic Agents;Biogenic Amines;Biogenic Monoamines;Bronchodilator Agents;Cardiac Stimulants Excl. Cardiac Glycosides;Cardiac Therapy;Cardiotonic Agents;Cardiovascular Agents;Catecholamines;Drugs for Obstructive Airway Diseases;Ethanolamines;Neurotransmitter Agents;Non-selective Beta-adrenergic Agonists;Peripheral Nervous System Agents;Protective Agents;Respiratory System Agents;Sympathomimetics |
| UNII号 | L628TT009W |
| CAS号 | 7683-59-2 |
| 分子量 | 211.2576 |
| 分子式 | C11H17NO3 |
| 适应症 | For the treatment of mild or transient episodes of heart block that do not require electric shock or pacemaker therapy also used in management of asthma and chronic bronchitis |
| 药效学 | Isoprenaline is a non-selective beta adrenergic receptor agonist used in a number of indications for the heart, as well as bronchospasm in anesthesia. Isoprenaline has a short duration of action as it is rapidly cleared, and a wide therapeutic index. Patients should be counselled regarding the risks of isoprenaline in the treatment of cardiogenic shock following myocardial infarction, paradoxical worsening of heart block, or precipitation of Adams-Stokes attacks. |
| 作用机制 | Isoprenaline is a non-selective beta adrenergic receptor agonist. Agonism of beta-1 and beta-2 adrenergic receptors causes the alpha subunit of G-protein coupled receptors to exchange GMP for GTP, activating them, and allowing the alpha subunit to dissociate from the beta and gamma subunits. Dissociation of the alpha subunit activates adenylate cyclase, converting ATP to cyclic AMP. Cyclic AMP activates protein kinase A (PKA), which phosphorylates cardiac L-type calcium channels such as Ca1.2. These channels depolarize cells by inward active transport of calcium ions.Agonism of beta-1 adrenergic receptors lead to increased strength of contractility, conduction of nerve impulses, speed of relaxation, and rate in the heart. Agonism of beta-2 adrenergic receptors leads to glycogenolysis in the liver, glucagon release from the pancreas, and activation of the renin-angiotensin-aldosterone system.In the alveoli, agonism of beta-2 adrenergic receptors, activates similar pathways to the heart, however the end result is regulation of sodium channels, the cystic fibrosis transmembrane conductance regulator (CFTR), and sodium potassium ATPase. PKA phosphorylates scaffolding proteins and sodium channels, increasing the number of sodium channels on the apical side of alveolar cells and increasing active transport of sodium ions into cells. Agonism of beta-2 adrenergic receptors can also increase chloride ion transport across CFTR. Together, these actions lead to passive transport of water out of the alveoli, and the clearance of alveolar fluid. |
| 吸收 | Data regarding absorption kinetics of isoprenaline are not readily available. |
| 分布量 | In pediatric patients, the volume of distribution was 216 ± 57 mL/kg. |
| 蛋白结合 | Isoprenaline is 68.8 ± 1.2% protein bound in plasma, mainly to serum albumin. |
| 代谢 | Isoprenaline is predominantly metabolized to glucuronide conjugates. Isoprenaline can also be O-methylated by catechol O-methyltransferase to the metabolite 3-O-methylisoprenaline, which can also be further glucuronidated. |
| 排泄 | Isoprenaline is 12.2-27.0% recovered in the feces and 59.1-106.8% recovered in the urine after 48 hours. The majority of the recovered dose in the urine is conjugated isoprenaline, with 6.5-16.2% free isoprenaline, and 2.6-11.4% 3-O-methylisoprenaline and conjugates. |
| 半衰期 | The half life of intravenous isoprenaline is 2.5-5 minutes. Oral isoprenaline has a half life of 40 minutes. |
| 清除 | In pediatric patients, the clearance of isoprenaline was 42.5 ± 5.0 mL/kg/min. |
| 毒理 | Patients experiencing an overdose may present with tachycardia, arrhythmias, palpitations, angina, hypotension, or hypertension. Overdose should be treated by reducing or stopping administration of isoprenaline and monitoring blood pressure, pulse, respiration, and ECG.In rats, the LD is 2221 mg/kg orally, 128 mg/kg intraperitoneally, and 600 mg/kg subcutaneously. In mice, the LD is 1260 orally and 450 mg/kg intraperitoneally. |
| ATC代码 | C01CA02 |
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