Precautions
Propranolol, sold under the brand name Inderal among others, is a medication of the beta blocker class. It is used to treat high blood pressure , a number of types of irregular heart rate , thyrotoxicosis , capillary hemangiomas , performance anxiety , and essential tremors , [1] [2] [3] as well to prevent migraine headaches , and to prevent further heart problems in those with angina or previous heart attacks . [1]
What group of drugs does propranolol belong to?
Typical starting dosage: 40 mg taken twice per day. Dosage increases: You may need to take a total dosage of 120 mg per day. In some cases, it may be necessary to take 240–320 mg per day.
What is a normal dose of propranolol?
Propranolol calms you down, improves your blood flow, and regularizes your cardiac rhythm. Propranolol comes in tablet form, as an extended-release oral capsule, and as a solution. All forms of propranolol are generally safe to take, but you should consult your doctor before taking propranolol.
Is propranolol a safe drug?
propranolol: What's the difference?
- Metoprolol and propranolol are beta-blockers used to treat high blood pressure ( hypertension ), heart pain ( angina ), abnormal heart rhythms, and some neurologic conditions.
- Metoprolol is also used to treat congestive heart failure and hyperthyroidism, and to prevent migraine headaches.
- Brand names for metoprolol include Lopressor and Toprol XL.
What is the difference between metoprolol and propranolol?
Is propranolol a Class C drug?
US FDA pregnancy category C: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant.
What drugs are classified beta blockers?
Examples of beta blockers Acebutolol. Atenolol (Tenormin) Bisoprolol (Zebeta) Metoprolol (Lopressor, Toprol XL)
Is propranolol a SSRI?
First off, it's important to understand that propranolol technically isn't an anti-anxiety medication like Xanax (alprazolam, a benzodiazepine) or Zoloft (sertraline, an SSRI). These drugs work by targeting specific parts of your brain and central nervous system, causing you to feel relaxed and calm.
Is propranolol addictive drug?
Propranolol is not a physically addictive, habit-forming medication. However, when propranolol is used to treat anxiety, it's possible to become used to the feeling of relaxation that it provides, especially if you often experience performance or social anxiety.
What does propranolol do to the brain?
Propranolol is one of several protein synthesis inhibitors that have been used in animal studies to reduce the saliency of emotional memories. A recent neuroimaging study revealed altered amygdala and hippocampus activity associated with propranolol-induced emotional memory impairment in healthy individuals.
What is the safest beta blocker?
Based on research studies, there are three beta blockers that are best for heart failure: carvedilol, metoprolol succinate (the long-acting form of metoprolol), and bisoprolol. These beta blockers have been shown to lower your risk of dying from heart failure complications.
Is propranolol good for mental anxiety?
Propranolol belongs to a group of medicines called beta blockers. It's used to treat heart problems, help with anxiety and prevent migraines.
Is propranolol good for depression?
Propranolol was found to cause depression as a side effect with a statistically greater frequency than the control medications used in these trials.
Does propranolol cause weight gain?
Secondly, Propranolol causes your body to retain more fluid than normal, leading to an increase in your body weight. This weight gain isn't usually noticeable (around a few pounds is average), and it is also far less likely at the dose used for anxiety treatment (the 10mg tablets).
Does propranolol clear your mind?
Scientists at the University of Amsterdam have discovered that the drug propranolol, a beta-blocker, prevents the return of unpleasant memories. The finding could lead to a new realm of treatments for patients with posttraumatic stress and other emotional disorders.
What are three complications of propranolol?
The more common side effects of propranolol can include:slower heart rate.diarrhea.dry eyes.hair loss.nausea.weakness or tiredness.
Is propranolol high risk?
Long-term use of beta-blockers may cause common side effects to worsen. It can also mask symptoms of low blood sugar in people with diabetes, which could potentially become life-threatening. High doses of propranolol that are taken long-term can even make heart problems worse and cause irregular heart rates.
Is Xanax a beta-blocker?
Xanax, a benzodiazepine, minimizes stress by targeting the central nervous system. Propranolol, a beta-blocker, reduces anxious symptoms through beta-receptors.
What is the most popular beta-blocker?
What is the most prescribed beta blocker? The most prescribed beta-blocker medication in 2021 was metoprolol succinate with more than 18 million prescriptions. The drug is an extended-release medication that can be taken once a day. Metoprolol tartrate has the second most prescriptions at around 11 million.
What brand name drug is classified as a beta-blocker to treat hypertension?
Beta blockers [acebutolol hydrochloride (Sectral), atenolol (Tenormin), betaxolol hydrochloride (Kerlone), carteolol hydrochloride (Cartrol), esmolol hydrochloride (Brevibloc), metoprolol (Lopressor, Toprol XL), nadolol (Corgard), penbutolol sulfate (Levatol), pindolol (Visken), propranolol (Inderal, InnoPran), and ...
Are statins beta-blockers?
Statins are typically prescribed to reduce cholesterol, one of the warning signs for heart disease. Beta-blockers are given to patients with high blood pressure, another warning sign for heart disease.
How long does propranolol take to absorb?
Propranolol is rapidly and completely absorbed, with peak plasma levels achieved about 1–3 hours after ingestion. More than 90% of the drug is found bound to plasma protein in the blood. Coadministration with food appears to enhance bioavailability. Despite complete absorption, propranolol has a variable bioavailability due to extensive first-pass metabolism. Hepatic impairment therefore increases its bioavailability. The main metabolite 4-hydroxypropranolol, with a longer half-life (5.2–7.5 hours) than the parent compound (3–4 hours), is also pharmacologically active. Most of the metabolites are excreted in the urine.
Why is propranolol used in sports?
Propranolol is used by musicians, actors, and public speakers for its ability to treat anxiety symptoms activated by the sympathetic nervous system. It has also been used as a performance-enhancing drug in sports where high accuracy is required, including archery, shooting, golf, and snooker.
How long does it take for propranolol to work?
Propranolol appears in the blood after 30 minutes and has a maximum effect between 60 and 90 minutes when taken by mouth. Common side effects include nausea, abdominal pain, and constipation. It should not be used in those with an already slow heart rate and most of those with heart failure.
What is propranolol antagonist?
Propranolol is a non-selective beta receptor antagonist . It competes with sympathomimetic neurotransmitters for binding to receptors, which inhibits sympathetic stimulation of the heart. Blockage of neurotransmitter binding to beta 1 receptors on cardiac myocytes inhibits activation of adenylate cyclase, which in turn inhibits cAMP synthesis leading to reduced PKA activation. This results in less calcium influx to cardiac myocytes through voltage gated L-type calcium channels meaning there is a decreased sympathetic effect on cardiac cells, resulting in antihypertensive effects including reduced heart rate and lower arterial blood pressure.
Why do people use propranolol?
Propranolol is used by musicians, actors, and public speakers for its ability to treat anxiety symptoms activated by the sympathetic nervous system. It has also been used as a performance-enhancing drug in sports where high accuracy is required, including archery, shooting, golf, and snooker. In the 2008 Summer Olympics, 50-metre pistol silver medalist and 10-metre air pistol bronze medalist Kim Jong-su tested positive for propranolol and was stripped of his medals.
When was propranolol first used?
Propranolol was patented in 1962 and approved for medical use in 1964. It is on the World Health Organization's List of Essential Medicines. Propranolol is available as a generic medication. In 2018, it was the 53rd most commonly prescribed medication in the United States, with more than 14 million prescriptions.
Is propranolol safe for hyperthyroidism?
Propranolol should be used with caution in people with: Diabetes mellitus or hyperthyroidism, since signs and symptoms of hypoglycaemia may be masked. Peripheral artery disease and Raynaud's syndrome, which may be exacerbated. Phaeochromocytoma, as hypertension may be aggravated without prior alpha blocker therapy.
What is propranolol bound to?
Approximately 90% of circulating Propranolol is bound to plasma proteins (albumin and alpha-1-acid glycoprotein). The binding is enantiomer-selective. The S (-)-enantiomer is preferentially bound to alpha-1-glycoprotein and the R (+)-enantiomer is preferentially bound to albumin.
How long does propranolol hydrochloride last?
In dietary administration studies in which mice and rats were treated with Propranolol hydrochloride for up to 18 months at doses of up to 150 mg/kg/day, there was no evidence of drug-related tumorigenesis. On a body surface area basis, this dose in the mouse and rat is, respectively, about equal to and about twice the maximum recommended human oral daily dose (MRHD) of 640 mg Propranolol hydrochloride. In a study in which both male and female rats were exposed to Propranolol hydrochloride in their diets at concentrations of up to 0.05% (about 50 mg/kg body weight and less than the MRHD), from 60 days prior to mating and throughout pregnancy and lactation for two generations, there were no effects on fertility. Based on differing results from Ames Tests performed by different laboratories, there is equivocal evidence for a genotoxic effect of Propranolol in bacteria ( S. typhimurium strain TA 1538).
How much propranolol reaches the systemic circulation?
However, it undergoes high first pass metabolism by the liver and on average, only about 25% of Propranolol reaches the systemic circulation. Propranolol hydrochloride extended-release capsules (60, 80, 120, and 160 mg) release Propranolol HCl at a controlled and predictable rate.
How long is propranolol used for stenosis?
In an uncontrolled series of 13 patients with New York Heart Association (NYHA) class 2 or 3 symptoms and hypertrophic subaortic stenosis diagnosed at cardiac catheterization, oral Propranolol 40 to 80 mg t.i.d. was administered and patients were followed for up to 17 months. Propranolol was associated with improved NYHA class for most patients.
How is propranolol metabolized?
Propranolol is metabolized through three primary routes: aromatic hydroxylation (mainly 4-hydroxylation), N-dealkylation followed by further side-chain oxidation, and direct glucuronidation. It has been estimated that the percentage contributions of these routes to total metabolism are 42%, 41% and 17%, respectively, but with considerable variability between individuals. The four major metabolites are Propranolol glucuronide, naphthyloxylactic acid and glucuronic acid, and sulfate conjugates of 4-hydroxy Propranolol.
What are the substrates of CYP2D6?
Blood levels and/or toxicity of Propranolol may be increased by co-administration with substrates or inhibitors of CYP2D6, such as amiodarone, cimetidine, delavudin, fluoxetine, paroxetine, quinidine, and ritonavir.
Is there any data on drug interactions with propranolol?
All drug interaction studies were conducted with Propranolol. There are no data on drug interactions with Propranolol hydrochloride extended-release capsules.
How does propranolol work?
Propranolol is a medicine that may be used to treat certain heart conditions, reduce essential tremor, or prevent migraine. It works by blocking beta-receptors. There are two types of beta receptors, beta-1 receptors (located in the heart) and beta-2 receptors (located in the bronchioles of the lungs and the arteries of skeletal muscle).
What is propranolol used for?
2. Upsides. May be used to treat high blood pressure (hypertension), either alone or in combination with thiazide diuretics or other medicines for hypertension.
What medications interact with propranolol?
Common medications that may interact with propranolol include: Some heart medications, such as amiodarone, clonidine, digoxin, diltiazem, propafenone, quinidine, and verapamil. NSAIDs, such as diclofenac, ibuprofen, and indomethacin, may decrease the blood pressure-lowering capabilities of propranolol.
What are some heart medications?
Some heart medications, such as amiodarone, clonidine, digoxin, diltiazem, propafenone, quinidine, and verapamil. Other medications including celecoxib, hydralazine, and rifampicin. NSAIDs, such as diclofenac, ibuprofen, and indomethacin, may decrease the blood pressure-lowering capabilities of propranolol.
What to do if your toes are numb?
Talk to your doctor as soon as possible if any new numbness, pain, skin color changes, or sensitivity occurs in fingers or toes. Call your doctor immediately if you develop a severe skin rash or painful blisters anywhere on your body.
Does propranolol cause nightmares?
Propranolol is mainly used for blood pressure and angina control; however, it also has a role in migraine prevention and the treatment of essential tremor. Propranolol may cause vivid dreams and is not usually recommended for people with pre-existing breathing difficulties. 5. Tips.
Can propranolol cause dreams?
Propranolol is more likely than some other beta-blockers (such as atenolol) to cause vivid or unusual dreams. Abrupt discontinuation has been associated with exacerbation of angina, and rarely, heart attacks. Only discontinue on a doctor's advice and reduce dosage gradually over a few weeks.
What is propranolol used for?
Propranolol can be used to ameliorate the sympathetic response in angina, tachyarrhythmias, prevention of acute ischemic attacks , migraine prophylaxis, and restless leg syndrome. Propranolol can be used in almost all cases if the desired result is to slow contractility and decrease a patient’s heart rate. Propranolol is also used off-label in a variety of other cases, for instance, in performance anxiety, which is a subset of social phobia, a psychiatric condition whose symptoms also include tachycardia, sweating, and flushing secondary to the activation of the sympathetic nervous system. This activity examines the indications, dosing, contraindications, mechanism, and management of propranolol therapy by the interprofessional healthcare team.
What is interprofessional care?
The interprofessional healthcare team includes the patient, the physician, the nurse, certified nurse's aid, and the pharmacist, all working in concert to optimize the patient's health. Therefore, all team members must remain up to date with literature on medication and potential side effects. Furthermore, they must utilize excellent communication skills between the different disciplines to ensure the desired outcome for their patient. A proper history and continuous physical assessments will need to be performed by the health care team to ensure that propranolol is used correctly, with appropriate precautions maintained in at-risk populations to minimize adverse outcomes. Nurses can offer counsel to the patients on their dosing regimen. The pharmacist can check for potential interactions, reinforce the nurse's counsel, answer patient questions, and report any concerns to the prescriber. This interprofessional approach will yield better therapeutic outcomes when using propranolol. [Level 5]
How long does propranolol stay in your system?
Furthermore, like most ingested medications, propranolol is predominantly cleared by the renal system, with a half-life of about 3 to 6 hours in patients with healthy renal systems. [10]
What happens when beta-1 receptors are activated?
When there is an activation of these receptors, there is an increase in cyclic AMP, which leads to increased intracellular calcium. This process leads to increased contractility of muscle fibers. When there is a blockage of beta-adrenergic receptors, this results in an overall decreased workload of the heart, which leads to subsequent reduced oxygen demand and myocardial remodeling. [8]
Is propranolol metabolized by enzymes?
Since propranolol is metabolized by hepatic enzymes and excreted through the renal system, prescribers should proceed with caution when prescribing it to a patient with known hepatic or renal impairments. Furthermore, dosages may need to be adjusted to avoid toxicity resulting from the inability to metabolize or clear the medication from the body properly.
What is the Creative Commons 4.0 license?
This book is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits use, duplication, adaptation, distribution, and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, a link is provided to the Creative Commons license, and any changes made are indicated.
Is propranolol good for tremors?
Propranolol not only has extensive use in cardiovascular disease, but it also has several implications in the treatment of noncardiovascular disease processes. It is used as a means of migraine prophylaxis, treatment of restless leg syndrome, essential tremors, and has even been of great success in treating infantile hemangioma. [5]
How long after propranolol is milk fed?
While no adverse effects in the nursing infant have been reported, experts advise monitoring the infant for signs and symptoms of beta-blockade and to schedule feedings at least three hours after maternal propranolol administration.
What does TGA stand for?
TGA. Therapeutic Goods Administration. Australian Drug Evaluation Committee "Prescribing medicines in pregnancy: an Australian categorisation of risk of drug use in pregancy. Available from: URL: http://www.tga.gov.au/docs/pdf/medpreg.pdf." ( [1999]):
Can you excrete propranolol into human milk?
Use is not recommended. Excreted into human milk: Yes. Comments: Propranolol levels in breast milk are low and would not be expected to cause any adverse effects in breastfed infants. See references.
Can propranolol cause respiratory depression?
There are a number of abnormalities associated with the use of propranolol during pregnancy, but many of these may be attributable to underlying diseases. These abnormalities include some signs of beta-blockade, such as bradycardia, hypoglycemia, and respiratory depression. Other abnormalities that may be due to propranolol include intrauterine ...
Is propranolol safe for pregnancy?
Propranolol Pregnancy Warnings. This drug is only recommended for use during pregnancy when there are no alternatives and the benefit outweighs the risk. Beta blockers may cause decreased placental perfusion, fetal and neonatal bradycardia, and hypoglycemia.
Can beta blockers cause hypoglycemia?
Beta blockers may cause decreased placental perfusion, fetal and neonatal bradycardia, and hypoglycemia. Propranolol has been used safely to treat a variety of conditions during pregnancy, including hypertension and pheochromocytoma in the mother, and tachyarrhythmias in both the mother and fetus.
Is there a pregnancy category C?
US FDA pregnancy category C: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant.
How long does propranolol stay in your system?
91% of an oral dose of propranolol is recovered as 12 metabolites in the urine. 6. Half-life. The elimination half life of propranolol is approximately 8 hours. 9 The plasma half life of propranolol is 3 to 6 hours. 7, 8.
How many metabolites of propranolol are recovered?
91% of an oral dose of propranolol is recovered as 12 metabolites in the urine. 6
How much propranolol is in plasma?
Approximately 90% of propranolol is protein bound in plasma. 7, 8, 9 Other studies have reported ranges of 85-96%. 5
What is DB00571 used for?
Propranolol is a racemic mixture of 2 enantiomers where the S (-)-enantiomer has approximately 100 times the binding affinity for beta adrenergic receptors. 8 Propranolol is used to treat a number of conditions but most commonly is used for hypertension. 7, 8, 9.
What are the symptoms of overdose?
Symptoms of overdose include hypotension, hypoglycemic seizure, restlessness, euphoria, insomnia. 7 Patients with asthma may develop bronchospasm. 7 In case of overdose, monitor vital signs, mental status, and blood glucose. 7 Treat hypotension with intravenous fluids, bradycardia with atropine, and isoproterenol and aminophylline for bronchospasm. 7 If patients do not respond to intravenous fluids, follow up with glucagon 50-150µg/kg intravenously, then 1-5mg/hour, followed by catecholamines. 7, 8, 9 Dialysis will not be useful as propranolol is highly protein bound. 7, 8, 9
What is the function of steroid hydroxylase?
Steroid hydroxylase activity. Specific Function. Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im... Gene Name.
What is the G-protein coupled receptor for?
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Usual Adult Dose for Hypertension
Initial dose: Immediate-release: 40 mg orally 2 times a day Sustained-release: 80 mg orally once a day XL sustained-release: 80 mg orally once a day at bedtime Maintenance dose: Immediate-release: 120 to 240 mg orally per day Sustained-release: 120 to 160 mg orally per day XL sustained-release: 80 to 120 mg orally once a day at bedtime Maximum dose: IR/SR: 640 mg orally per day XR: 120 mg orally per day Comments: -The XL sustained-release formulation should be administered once daily at bedtime (approximately 10 PM) and should be taken consistently either on an empty stomach or with food. -Dose titration should be done gradually until adequate blood pressure control is achieved. -The recommended dosing is the same whether used alone or added to a diuretic. -The time needed for full hypertensive response to a given dosage is variable and may range from a few days to several weeks. -While twice daily dosing of the immediate release formulation is effective and can maintain a reduction in blood pressure throughout the day, some patients, especially when lower doses are used, may experience a modest rise in blood pressure toward the end of the 12 hour dosing interval.
Usual Adult Dose for Angina Pectoris
Immediate-release: Total daily doses of 80 to 320 mg orally 2 to 4 times a day have been shown to increase exercise tolerance and to reduce ischemic changes in the ECG. Sustained-release: Initial dose: 80 mg orally once a day. Dosage should be gradually increased at 3 to 7 day intervals.
Usual Adult Dose for Arrhythmias
Immediate-release: 10 to 30 mg orally 3 to 4 times a day, before meals and at bedtime IV: 1 to 3 mg at a rate not exceeding 1 mg/min. Sufficient time should be allowed for the drug to reach the site of action even when a slow circulation is present. A second dose may be given after 2 minutes.
Usual Adult Dose for Myocardial Infarction
Immediate-release: Initial dose: 40 mg orally 3 times a day for 1 month, then increase to 60 to 80 mg orally 3 times a day as tolerated. Maintenance dose: 180 mg to 240 mg orally per day in divided doses (2 to 4 times daily) Maximum dose: 240 mg orally per day
Usual Adult Dose for Migraine Prophylaxis
Immediate-release: Initial dose: 80 mg orally per day in divided doses Maintenance dose: 160 to 240 mg orally per day in divided doses Sustained-release: Initial dose: 80 mg orally once a day Maintenance dose: 160 to 240 mg once a day Comments: -The dosage should be increased gradually to achieve optimum migraine prophylaxis.
Usual Adult Dose for Benign Essential Tremor
Immediate-release: Initial dose: 40 mg orally 2 times a day Maintenance dose: 120 to 320 mg orally per day Comments: -Optimum reduction of essential tremor is usually achieved with a dose of 120 mg orally per day. -Occasionally, it may be necessary to administer 240 to 320 mg orally per day.
Usual Adult Dose for Aortic Stenosis
Immediate-release: 20 to 40 mg orally 3 to 4 times a day, before meals and at bedtime Sustained-release: 80 to 160 mg orally once a day Use: Hypertrophic Subaortic Stenosis
Overview
This medication is a beta blocker used to treat high blood pressure, irregular heartbeats, shaking (tremors), and other conditions. It is used after a heart attack to improve the chance of survival. It is also used to prevent migraine headaches and chest pain (angina).
May Treat: Hypertension · Angina · Essential tremor · Hypertrophic cardiomyopathy · Pheochromocytoma adjunct therapy and more
Brand Names: Inderal · Inderal LA · InnoPran XL · Hemangeol · Inderal XL and more
Drug Class: Beta Blockers Non-Cardiac Selective
Availability: Prescription Required
Pregnancy: Do not use. This medication may be harmful to an unborn child.
May Treat: Hypertension · Angina · Essential tremor · Hypertrophic cardiomyopathy · Pheochromocytoma adjunct therapy and more
Brand Names: Inderal · Inderal LA · InnoPran XL · Hemangeol · Inderal XL and more
Drug Class: Beta Blockers Non-Cardiac Selective
Availability: Prescription Required
Pregnancy: Do not use. This medication may be harmful to an unborn child.
Lactation: Consult a doctor before using
Driving: May cause drowsiness or dizziness. Use caution
Adverse effects
Medical uses
Contraindications
Overdose
Interactions
Propranolol should be used with caution in people with:
• Diabetes mellitus or hyperthyroidism, since signs and symptoms of hypoglycaemia may be masked
• Peripheral artery disease and Raynaud's syndrome, which may be exacerbated
• Phaeochromocytoma, as hypertension may be aggravated without prior alpha blocker therapy
Pharmacology
Propranolol is used for treating various conditions, including:
• Hypertension
• Angina pectoris (with the exception of variant angina)
• Myocardial infarction
• Tachycardia (and other sympathetic nervous system symptoms, such as muscle tremor) associated with various conditions, including anxiety, panic
Propranolol is used for treating various conditions, including:
• Hypertension
• Angina pectoris (with the exception of variant angina)
• Myocardial infarction
• Tachycardia (and other sympathetic nervous system symptoms, such as muscle tremor) associated with various conditions, including anxiety, panic, hyperthyroidism, and lithium therapy
History
Propranolol may be contraindicated in people with:
• Reversible airway diseases, particularly asthma or chronic obstructive pulmonary disease (COPD)
• Slow heart rate (bradycardia) (<60 beats/minute)
• Sick sinus syndrome
Description
In overdose propranolol is associated with seizures. Cardiac arrest may occur in propranolol overdose due to sudden ventricular arrhythmias, or cardiogenic shock which may ultimately culminate in bradycardic PEA.
Clinical Pharmacology
Since beta blockers are known to relax the cardiac muscle and to constrict the smooth muscle, beta-adrenergic antagonists, including propranolol, have an additive effect with other drugs which decrease blood pressure, or which decrease cardiac contractility or conductivity. Clinically significant interactions particularly occur with:
• Verapamil
Pharmacokinetics and Drug Metabolism
Propranolol is classified as a competitive non-cardioselective sympatholytic beta blocker that crosses the blood–brain barrier. It is lipid soluble and also has sodium channel blocking effects. Propranolol is a non-selective β-adrenergic receptor antagonist, or beta blocker; that is, it blocks the action of epinephrine (adrenaline) and norepinephrine (noradrenaline) at both β1- and β2-adrenergic receptors. It has little intrinsic sympathomimetic activity, but has strong membrane stabilizing ac…
Pharmacodynamics and Clinical Effects
Scottish scientist James W. Black developed propranolol in the 1960s. It was the first beta-blocker effectively used in the treatment of coronary artery disease and hypertension. In 1988, Black was awarded the Nobel Prize in Medicine for this discovery. Propranolol was inspired by the early β-adrenergic antagonists dichloroisoprenaline and pronethalol. The key difference, which was carried through to essentially all subsequent beta blockers, was the inclusion of an oxymethylene grou…
Indications and Usage
Contraindications
- General
Propranolol is a nonselective, beta-adrenergic receptor-blocking agent possessing no other autonomic nervous system activity. It specifically competes with beta-adrenergic receptor-stimulating agents for available receptor sites. When access to beta-receptor sites is blocked b… - Mechanism of Action
The mechanism of the antihypertensive effect of Propranolol has not been established. Among the factors that may be involved in contributing to the antihypertensive action include: (1) decreased cardiac output, (2) inhibition of renin release by the kidneys, and (3) diminution of ton…
Warnings
- Absorption
Propranolol is highly lipophilic and almost completely absorbed after oral administration. However, it undergoes high first pass metabolism by the liver and on average, only about 25% of Propranolol reaches the systemic circulation. Propranolol hydrochloride extended-release capsu… - Distribution
Approximately 90% of circulating Propranolol is bound to plasma proteins (albumin and alpha-1-acid glycoprotein). The binding is enantiomer-selective. The S(-)-enantiomer is preferentially bound to alpha-1-glycoprotein and the R(+)-enantiomer is preferentially bound to albumin. The v…
Precautions
- Hypertension
In a retrospective, uncontrolled study, 107 patients with diastolic blood pressure 110 to 150 mmHg received Propranolol 120 mg t.i.d. for at least 6 months, in addition to diuretics and potassium, but with no other hypertensive agent. Propranolol contributed to control of diastolic … - Angina Pectoris
In a double-blind, placebo-controlled study of 32 patients of both sexes, aged 32 to 69 years, with stable angina, Propranolol 100 mg t.i.d. was administered for 4 weeks and shown to be more effective than placebo in reducing the rate of angina episodes and in prolonging total exercise ti…
Adverse Reactions
- Hypertension
Propranolol Hydrochloride Extended-Release Capsules are indicated in the management of hypertension. It may be used alone or used in combination with other antihypertensive agents, particularly a thiazide diuretic. Propranolol Hydrochloride Extended-Release Capsules are not in… - Angina Pectoris Due to Coronary Atherosclerosis
Propranolol Hydrochloride Extended-Release Capsules are indicated to decrease angina frequency and increase exercise tolerance in patients with angina pectoris.
Overdosage
- Propranolol is contraindicated in 1) cardiogenic shock; 2) sinus bradycardia and greater than first-degree block; 3) bronchial asthma; and 4) in patients with known hypersensitivity to Propranolol hydrochloride.
How It Works
- Angina Pectoris
There have been reports of exacerbation of angina and, in some cases, myocardial infarction, following abrupt discontinuance of Propranolol therapy. Therefore, when discontinuance of Propranolol is planned, the dosage should be gradually reduced over at least a few weeks, and t… - Hypersensitivity and Skin Reactions
Hypersensitivity reactions, including anaphylactic/anaphylactoid reactions, have been associated with the administration of Propranolol (see ADVERSE REACTIONS). Cutaneous reactions, including Stevens-Johnson Syndrome, toxic epidermal necrolysis, exfoliative dermatitis, erythem…
Upsides
- General
Propranolol should be used with caution in patients with impaired hepatic or renal function. Propranolol hydrochloride extended-release capsules are not indicated for the treatment of hypertensive emergencies. Beta-adrenergic receptor blockade can cause reduction of intraocula… - Clinical Laboratory Tests
In patients with hypertension, use of Propranolol has been associated with elevated levels of serum potassium, serum transaminases, and alkaline phosphatase. In severe heart failure, the use of Propranolol has been associated with increases in Blood Urea Nitrogen.
Downsides
- The following adverse events were observed and have been reported in patients using Propranolol. Cardiovascular:Bradycardia; congestive heart failure; intensification of AV block; hypotension; paresthesia of hands; thrombocytopenic purpura; arterial insufficiency, usually of the Raynaud type. Central Nervous System:Light-headedness; mental depression manifested by ins…
Bottom Line
- Propranolol is not significantly dialyzable. In the event of overdosage or exaggerated response, the following measures should be employed: General:If ingestion is or may have been recent, evacuate gastric contents, taking care to prevent pulmonary aspiration. Supportive Therapy:Hypotension and bradycardia have been reported following Propranolol overdose and s…
Tips
- Propranolol is a medicine that may be used to treat certain heart conditions, reduce essential tremor, or prevent migraine. It works by blocking beta-receptors. There are two types of beta receptor...
- Propranolol blocks beta-1 receptors in the heart which slows the heart rate and decreases how hard the heart has to work to pump blood around the body, decreasing blood pressure.
- Propranolol is a medicine that may be used to treat certain heart conditions, reduce essential tremor, or prevent migraine. It works by blocking beta-receptors. There are two types of beta receptor...
- Propranolol blocks beta-1 receptors in the heart which slows the heart rate and decreases how hard the heart has to work to pump blood around the body, decreasing blood pressure.
- Propranolol has a "nonselective" action. This means that it also blocks beta-2 receptors in the bronchioles, which can cause a narrowing of the bronchioles which may cause breathing difficulties in...
- Propranolol also has a membrane-stabilizing effect at higher dosages which can affect the electrical impulses of the heart, although is not thought to contribute much to its antiarrhyth…
Response and Effectiveness
- May be used to treat high blood pressure (hypertension), either alone or in combination with thiazide diuretics or other medicines for hypertension.
- May improve the symptoms of angina and increase a person with angina's capacity to exercise.
- May be used in the prevention of migraine headaches.
- May be used to treat high blood pressure (hypertension), either alone or in combination with thiazide diuretics or other medicines for hypertension.
- May improve the symptoms of angina and increase a person with angina's capacity to exercise.
- May be used in the prevention of migraine headaches.
- May improve symptoms of hypertrophic subaortic stenosis; however, will not change the course of the disease.
Interactions
- If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include: 1. Low blood pressure (which may be felt as dizziness upon standing); cold extremities or Raynaud's phenomenon (characterized by numbness and cold in the fingers and toes in response to cold temperatures o…
Further Information
- Propranolol is mainly used for blood pressure and angina control; however, it also has a role in migraine prevention and the treatment of essential tremor. Propranolol may cause vivid dreams and is not usually recommended for people with pre-existing breathing difficulties.