English Synonyms
1-isopropylamino-3-(1-naphthyloxy)propan-2-ol;Propanolol;1-[Isopropylamino]-3-[1-naphthyloxy]-2-propanol;2-Propanol,1-(1-methylethyl)amino-3-(1-naphthalenyloxy)-;1-naphthalen-1-yloxy-3-(propan-2-ylamino)propan-2-ol;1-(1-Naphthyloxy)-3-(isopropylamino)-2-propanol;2-Propanol,1-(isopropylamino)-3-(1-naphthyloxy)-(7CI,8CI);2-Propanol,1-[(1-methylethyl)amino]-3-(1-naphthalenyloxy)-(9CI)
Propranolol Properties
| Melting Point | 163-164 °C |
| Boiling Point | 402.6°C (rough estimate) |
| Density | 1.0280 (rough estimate) |
| Refractive Index | 1.5500 (estimate) |
| Storage Condition | -20°C Freezer, Under inert Atmosphere |
| Solubility | Soluble in Dmso (A Little), Methanol (A Little) |
| Acidity Coefficient (pKa) | 13.84±0.20(Predicted) |
| Form | Solid |
| Color | White to Off-White |
| Water Solubility | 80.99mg/L(25 ºC) |
Propranolol Usage and Synthesis
Overview
Propranolol, Commonly Known as Propranolol, Is a Commonly Used Drug in Cardiology, Mainly Used to Treat Various Types of Hypertension, Angina Pectoris, Arrhythmias, Especially Supraventricular Arrhythmias.
Propranolol Belongs to the Structural Type of Aromatic Oxypropanolamine Drugs, The Aromatic Ring Is a Naphthalene Nucleus; the S-Levorotatory Isomer Has a Strong Effect, But the R-Configuration Instead Competitively Replaces the S Configuration in Vivo; the Racemate Is Used Clinically; It Has a Blocking Effect on Both β1 and β2 Receptors; It Is Mainly Metabolized in the Liver, And Should Be Used with Caution in Patients with Liver Damage. It Is Highly Lipid-Soluble and Easily Produces Central Effects, With Side Effects of Inhibiting Myocardial Contractility, Causing Bronchospasm and Asthma.
Pharmacological Action
Propranolol Is a Non-selective β-Receptor Blocker with Membrane Stabilizing Effect, No Intrinsic Sympathomimetic Activity, Lipid Soluble, And First-Pass Effect in the Liver. It Can Reduce Cardiac Automaticity, Slow Heart Rate, Inhibit Cardiac Contractility and Atrioventricular Conduction, Reduce Cardiac Output, And Reduce Myocardial Oxygen Consumption. It Is Clinically Used to Examine Sinus Node Function, Supraventricular Arrhythmias, Angina Pectoris, Hypertension, Preoperative Preparation for Pheochromocytoma, Hyperthyroidism, Hypertrophic Cardiomyopathy, And Arrhythmias Caused by Digitalis Poisoning.
Pharmacokinetics
After Oral Administration, It Is Completely Absorbed, With an Absorption Rate of About 90%. Peak Blood Concentration Is Reached in 1 to 1.5 Hours (6.6 Hours for Sustained-Release Tablets), But a Large Amount of It Is Metabolized by the Liver and Inactivated Before Entering the Systemic Circulation, With a Bioavailability of 30%. The Plasma Protein Binding Rate Is 93%. The Drug's Ability to Bind to Plasma Proteins Is Genetically Controlled and Has Stereoselectivity. Its Active Isomer, Levorotatory Propranolol, Mainly Binds to α1-Acid Glycoprotein. The Level of Plasma α1-Acid Glycoprotein in Chinese People Is Lower, So the Proportion of Unbound Propranolol in Plasma Is Higher Than That in Europeans, So Chinese People Are More Sensitive to This Drug.It Is Lipophilic and Can Pass Through the Blood-Cerebrospinal Fluid Barrier to Produce Central Nervous System Reactions. It Can Also Enter the Placenta with a Distribution Volume of About 6l/Kg. This Drug Is Extensively Metabolized in the Liver, And Drug Metabolism and Body Clearance Rates Are Increased in Patients with Hyperthyroidism. The Half-Life Is 3.5 to 6 Hours After Oral Administration and 2 to 3 Hours After Intravenous Injection. It Is Excreted Through the Kidneys, Including Most Metabolites and a Small Part (Less Than 1%) of the Prototype. This Drug Can Be Secreted in Small Amounts Through Breast Milk. It Cannot Be Removed by Dialysis.
Indications
Used for Hypertension, Angina Pectoris, Supraventricular Tachyarrhythmias, Ventricular Arrhythmias, Myocardial Infarction, Hypertrophic Cardiomyopathy, Pheochromocytoma, Migraine and Non-cluster Headaches.
Clinical Application
1) For Hypertension, As a First-Line Medication, It Can Be Used Alone or in Combination with Other Antihypertensive Drugs.
(2) Arrhythmia. It Is Used to Correct Arrhythmias Caused by Rapid Supraventricular Arrhythmias, Ventricular Arrhythmias, Digitalis Poisoning and Anesthesia, Especially Arrhythmias Caused by Increased Circulating Catecholamine Levels or Increased Sensitivity of the Heart to Catecholamines. In Addition, This Drug Can Be Tried for Arrhythmias Caused by Antimony Poisoning When Other Drugs Are Ineffective.
(3) For Angina Pectoris. It Is Often Used in Combination with Nitrates to Increase Efficacy and Reduce the Occurrence of Adverse Reactions.
(4) As a Secondary Prevention Drug for Myocardial Infarction, It Can Reduce the Patient; Cardiovascular Mortality Rate.
(5) For Pheochromocytoma.
(6) For Hyperthyroidism: ① Preoperative Preparation for Subtotal Thyroidectomy. ② for Patients with Severe Hyperthyroidism to Control Symptoms Before Antithyroid Drugs or Radioactive Iodine Treatment Are Effective. ③ Thyroid Crisis or Crisis Precursors.
(7) For Left Atrioventricular Valve Prolapse Syndrome.
(8) For Migraine, Facial Neuralgia and Essential Tremor.
Adverse Reactions
The Most Common Adverse Reaction of This Drug Is That the Cardiovascular System Induces or Aggravates Congestive Heart Failure. Mild Tachycardia Is More Common, While Bradycardia and Hypertension Are Less Common (The Drug Should Be Discontinued at This Time).
Dizziness, Lightheadedness (Caused by Hypotension), Headache, Confusion (Especially in the Elderly), Paresthesia, Hallucinations, Depression, Anxiety, Distraction, Slow Reaction, Fatigue, Drowsiness, Insomnia, And Dreaminess Can Be Seen in the Mental and Nervous System.
Lowered Blood Sugar Can Be Seen in the Metabolic/Endocrine System, While Patients with Diabetes May Have Increased Blood Sugar. Fever Is Extremely Rare.
Bronchial Spasm and Dyspnea Are Rare in the Respiratory System.
Precautions
It Is Contraindicated for Patients with Bronchial Asthma, Severe Atrioventricular Block, Heart Failure and Cardiogenic Shock.
It Should Be Used with Caution in Patients with Ventricular Tachycardia, Atrioventricular Block, Hypotension, Heart and Liver Dysfunction, Hypoglycemia or Diabetes Taking Hypoglycemic Drugs and Pregnant Women.
Intravenous Injection Has a Greater Inhibitory Effect on the Heart, Which May Suddenly Aggravate or Induce Heart Failure, So It Is Generally Not Used.
The Oral Dosage Should Start with a Small Dose and Gradually Increase. For Long-Term Users, The Dosage Should Be Gradually Reduced When Stopping the Drug to Avoid Rebound Phenomenon, Inducing Angina Pectoris, Or Even Acute Myocardial Infarction and Death.
