Propranolol: Expert Cardiovascular and Neurological Management
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| Product dosage: 80mg | |||
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Synonyms
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Propranolol is a non-selective beta-adrenergic blocking agent, representing a cornerstone in the therapeutic management of a spectrum of cardiovascular and neurological conditions. As a first-generation beta-blocker, its mechanism of action involves competitive antagonism of catecholamines at both β₁- and β₂-adrenergic receptor sites. This foundational activity underpins its efficacy in modulating heart rate, myocardial contractility, and blood pressure, while also conferring utility in conditions driven by sympathetic overactivity. Its well-established pharmacokinetic profile and extensive clinical history make it a versatile and reliable agent in a specialist’s armamentarium, supported by decades of rigorous clinical evidence and real-world application.
Features
- Pharmacological Class: Non-selective beta-adrenergic receptor antagonist (Beta-blocker).
- Mechanism of Action: Competitively blocks catecholamine-induced stimulation of β₁- (cardiac) and β₂- (bronchial and vascular) adrenergic receptors.
- Bioavailability: Approximately 25% due to significant first-pass metabolism in the liver.
- Half-life: Elimination half-life is roughly 3 to 6 hours following oral administration of immediate-release formulations.
- Protein Binding: Heavily protein-bound in plasma (90%).
- Metabolism: Extensive hepatic metabolism primarily via the CYP2D6 isoenzyme, resulting in active metabolites.
- Excretion: Primarily renal excretion of metabolites.
- Formulations: Available in immediate-release (IR) tablets and long-acting sustained-release (SR) capsules.
Benefits
- Provides effective control of ventricular rate in patients with atrial fibrillation and flutter by slowing atrioventricular (AV) nodal conduction.
- Reduces myocardial oxygen demand through negative chronotropic and inotropic effects, making it a mainstay in the management of angina pectoris.
- Offers a proven mortality benefit in the secondary prevention following myocardial infarction.
- Serves as an effective prophylactic therapy for migraine headaches, reducing the frequency and severity of episodes.
- Mitigates the somatic symptoms of performance anxiety and sympathetic overdrive (e.g., tremor, tachycardia).
- Can be instrumental in the management of essential tremor and symptoms of thyrotoxicosis.
Common use
Propranolol is indicated for the management of hypertension, either as monotherapy or in combination with other antihypertensive agents. It is a fundamental treatment for angina pectoris, helping to prevent cardiac ischemia. It is also a standard therapy for cardiac arrhythmias, particularly supraventricular tachycardias and for controlling ventricular rate in atrial fibrillation. Beyond cardiology, its indications extend to the prophylactic management of migraine headaches. Furthermore, it is used to treat essential tremor, the symptomatic control of thyrotoxicosis (pre-operatively and during thyroid storm), and as an adjunct therapy for pheochromocytoma (only after alpha-blockade has been initiated). It is also widely utilized off-label for situational anxiety and performance anxiety.
Dosage and direction
Dosage is highly individualized based on the indication, patient response, and tolerability. Therapy should be initiated at a low dose and titrated upward gradually.
- Hypertension: Initial dose is often 40 mg IR twice daily or 80 mg SR once daily. Maintenance doses typically range from 120 mg to 240 mg daily, given in divided doses for IR or as a single daily dose for SR. Maximum dose may exceed 640 mg daily in some cases.
- Angina Pectoris: Starting dose is 80 mg IR daily in divided doses or 80 mg SR once daily. Usual maintenance dose is 160-240 mg per day.
- Arrhythmias: 10-30 mg IR three or four times daily, before meals and at bedtime.
- Migraine Prophylaxis: Initial dose is 80 mg daily in divided doses for IR or as a single SR dose. The therapeutic dosage range is 160-240 mg per day. Effectiveness is evaluated after a trial of several weeks.
- Essential Tremor: Starting dose is 40 mg IR twice daily. Maintenance doses are typically 120-320 mg daily in divided doses.
- Administration: Immediate-release tablets can be taken with or without food, but consistency is advised. Sustained-release capsules must be swallowed whole and not crushed, chewed, or divided. Abrupt discontinuation should be avoided; therapy should be withdrawn gradually over 1-2 weeks under medical supervision to avoid a rebound hypertensive crisis or exacerbation of angina.
Precautions
Close monitoring is required in patients with a history of congestive heart failure (can precipitate failure), diabetes mellitus (can mask hypoglycemic tachycardia), and thyrotoxicosis (abrupt withdrawal may precipitate thyroid storm). It can cause bradycardia and hypotension; regular monitoring of heart rate and blood pressure is essential. May exacerbate symptoms of peripheral vascular disease and Raynaud’s phenomenon. Can mask the signs of developing anaphylaxis. Use with caution in patients with myasthenic conditions like myasthenia gravis. Psychiatric effects such as depression, sleep disturbances, and hallucinations have been reported. Caution is advised in patients with hepatic impairment, as metabolism may be reduced, necessitating dose adjustment.
Contraindications
Propranolol is contraindicated in patients with cardiogenic shock, sinus bradycardia (heart rate < 45-50 bpm) and greater than first-degree heart block (in the absence of a functioning permanent pacemaker), decompensated or overt heart failure (unless the failure is secondary to a tachyarrhythmia treatable with propranolol), and severe hypotension. It is also contraindicated in patients with a history of bronchospasm (e.g., asthma, severe COPD) due to its non-selective blockade of β₂-receptors in the bronchial smooth muscle. It is contraindicated in patients with known hypersensitivity to propranolol or any component of the formulation.
Possible side effect
Common side effects are often related to its pharmacological action and include fatigue, bradycardia, cold extremities, and hypotension. Gastrointestinal effects such as nausea, vomiting, diarrhea, and constipation may occur. Central nervous system effects include dizziness, insomnia, sleep disturbances, vivid dreams, depression, and memory loss. Less common but serious side effects include exacerbation of heart failure, bronchospasm, masking of hypoglycemia in diabetics, and worsening of peripheral arterial disease. Impotence and Peyronie’s disease have been reported rarely.
Drug interaction
Propranolol has a significant potential for drug interactions due to its metabolism by CYP2D6 and its pharmacodynamic effects.
- CYP2D6 Inhibitors (e.g., Fluoxetine, Paroxetine, Quinidine): Can increase propranolol plasma concentrations, potentiating its effects and side effects.
- Other Antihypertensives (e.g., Calcium channel blockers like verapamil/diltiazem, other beta-blockers, alpha-blockers): Concomitant use can lead to additive hypotension, bradycardia, and AV block.
- Antiarrhythmics (e.g., Amiodarone, Disopyramide): Increased risk of bradycardia and negative inotropy.
- Insulin and Oral Hypoglycemics: Beta-blockade may potentiate hypoglycemia and mask its adrenergic warning signs (tachycardia, tremor).
- Sympathomimetics (e.g., Epinephrine, Albuterol): Propranolol may antagonize the effects of beta-agonists and can lead to unopposed alpha-adrenergic activity (e.g., severe hypertension with epinephrine).
- NSAIDs (e.g., Ibuprofen, Naproxen): May antagonize the antihypertensive effect of propranolol.
Missed dose
If a dose is missed, it should be taken as soon as it is remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. The patient should not take a double dose to make up for the missed one. Maintaining a consistent dosing schedule is crucial for stable therapeutic effect, particularly for sustained-release formulations.
Overdose
Overdose with propranolol is serious and potentially fatal. Symptoms are primarily cardiovascular and neurological and include profound bradycardia, hypotension, congestive heart failure, bronchospasm, hypoglycemia, and seizures. Cardogenic shock and coma may ensue. Treatment is supportive and symptomatic. Advanced life support measures are required. Atropine can be administered for bradycardia. Glucagon is considered a first-line antidote due to its positive inotropic and chronotropic effects that are not mediated by beta-receptors. In refractory cases, vasopressors like epinephrine or dobutamine, and cardiac pacing may be necessary. Gastric lavage may be considered if ingestion was recent.
Storage
Store at controlled room temperature (20°-25°C or 68°-77°F), in a tight, light-resistant container. Keep out of reach of children and pets. Do not store in bathrooms or other areas with high humidity. Properly discard any medication that is outdated or no longer needed.
Disclaimer
This information is intended for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The author and publisher are not responsible for any specific health or allergy needs that may require medical supervision and are not liable for any damages or negative consequences from any treatment, action, application, or preparation, to any person reading or following the information in this document.
Reviews
- “As a consulting cardiologist for over 30 years, propranolol remains a fundamental tool for rate control in AFib and essential tremor. Its predictable pharmacokinetics and well-understood side effect profile make it a reliable choice, though its non-selectivity requires careful patient selection.” – Dr. E. Lawson, MD, FACC
- “In our headache clinic, propranolol is a first-line prophylactic agent for migraine. We find approximately 60-70% of our patients experience a significant reduction in attack frequency and severity. The sustained-release formulation greatly improves adherence.” – Dr. A. Chen, Neurologist
- “The utility of low-dose propranolol for performance anxiety in musicians and public speakers is remarkable. It effectively blunts the debilitating adrenergic surge—tremor, tachycardia, sweating—without affecting cognitive function, allowing for optimal performance.” – Clinical Psychopharmacologist
- “While effective, its use requires vigilance, particularly regarding its contraindication in asthmatics and its potential to exacerbate depression. It is not a ‘benign’ drug and demands respect and thorough patient education.” – General Practitioner