Пропранолол
Пропранолол Uses, Dosage, Side Effects, Food Interaction and all others data.
Пропранолол is a non-cardioselective β-blocker that competitively blocks β1- and β2-receptors resulting in decreased heart rate, myocardial contractility, BP and myocardial oxygen demand. It has membrane-stabilising properties.
Пропранолол is a beta-adrenergic receptor antagonist used to treat hypertension. Пропранолол has a long duration of action as it is given once or twice daily depending on the indication. When patients abruptly stop taking propranolol, they may experience exacerbations of angina and myocardial infarctions.
| Trade Name | Пропранолол |
| Availability | Prescription only |
| Generic | Propranolol |
| Propranolol Other Names | beta-Propranolol, Propanalol, Propanolol, Propranolol, Propranololo, Propranololum |
| Related Drugs | amlodipine, aspirin, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, Xarelto, clopidogrel |
| Type | |
| Formula | C16H21NO2 |
| Weight | Average: 259.3434 Monoisotopic: 259.157228921 |
| Protein binding | Approximately 90% of propranolol is protein bound in plasma. Other studies have reported ranges of 85-96%. |
| Groups | Approved, Investigational |
| Therapeutic Class | Beta-adrenoceptor blocking drugs, Beta-blockers |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Пропранолол is used for:
- essential and renal hypertension
- angina pectoris
- long term prophylaxis after recovery from acyte myocardial infarction
- cardiac dysrhythmia
- prophylaxis of migraine
- essential tremor
- anxiety and anxiety tachycardia
- adjunctive management of thyrotoxicosis and thyrotoxic crisis
- hypertrophic obstructive cardiomyopathy
- phaeochromocytoma (with α-blocker)
Пропранолол is also used to associated treatment for these conditions: Akathisia caused by antipsychotic use, Angina Pectoris, Atrial Fibrillation, Cardiovascular Mortality, Gastroesophageal variceal hemorrhage prophylaxis, Hemangiomas, High Blood Pressure (Hypertension), Migraine, Myocardial Infarction, Obstructive Hypertrophic Cardiomyopathy, Performance Anxiety, Pheochromocytomas, Proliferating Infantile Hemangioma, Supraventricular Arrhythmias, Tachyarrhythmia caused by Digitalis intoxication, Tachyarrhythmia caused by catecholamine excess, Thyroid Crisis, Thyrotoxicosis, Tremor caused by lithium, Tremor, Essential, Ventricular Tachycardia (VT)
How Пропранолол works
Пропранолол is a nonselective β-adrenergic receptor antagonist. Blocking of these receptors leads to vasoconstriction, inhibition of angiogenic factors like vascular endothelial growth factor (VEGF) and basic growth factor of fibroblasts (bFGF), induction of apoptosis of endothelial cells, as well as down regulation of the renin-angiotensin-aldosterone system.
Dosage
Пропранолол dosage
Tablet:
Adults:
- Hypertension: A starting dose of 80 mg twice a day may increased at weekly intervals according to response. The usual dose range is 160-320 mg per day. With concurrent diuretic or other antihypertensive drugs a further reduction of blood pressure is obtained.
- Angina, anxiety, migraine and essential tremor: A staring dose of 40 mg two or three times daily may be increased by the same amount at weekly intervals according to patients response. An adequate response in anxiety, migraine and essential tremor is usually seen in the range 80-160 mg/day and an angina in the range 120-240 mg/day.
- Situational and generalized anxiety: A dose of 40 mg daily may provide short term relief of acute situational anxiety. Generalized anxiety require long term therapy, usually responds adequately to 40 mg twice daily which ,which individual cases, may be increased to 40 mgthree times daily. Treatment should be continued according to responses. Patients should reviewed after 6 to 12 months treatment.
- Dysrhythmias, anxiety tachycardia, hypertrophic obstructive cardiomyopathy and thyrotoxicosis: A dosage range of 10-40 mg three or four times a day usually achieves the required response.
- Post myocardial infarction: Treatment should be started between days 5 and after 21 after myocardial infarction, with an initial dose of 40 mg four times a day for 2 or 3 days. In order to improve compliance the total daily doses three after be given as 80 mg twice a day. Phaeochromocytoma (Used only with an alpha receptor blocking drug).
- Pre-operative: 60 mg daily for three days.
- Non-operable malignant cases: 30 mg daily.
- Migraine: Under 12 years: 20 mg two or three times daily.Over 12 years : The adult dose.
Children:
- Sysrhythmias, Phaeochromocytoma, Thyrotoxicisis: Dosage should be individually determined and the following is only a guide 0.25-0.5 mg/kg three or four times daily as required.
Sustained Release Capsule:
Adult:
- Hypertension: The usual initial dose is 80mg Пропранолол SR once daily, whether used alone or added to a diuretic. The usual maintenance dosage is 120 to 160 mg once daily.
- Angina pectoris: Starting with 80mg Пропранолол SR once daily, dosage should be gradually increased three to seven day intervals until optimum response is obtained.
- Migraine: The initial oral dose is 80 mg Пропранолол SR once daily. T he usual effective dose range is 160 to 240 mg once daily. It may be advisable to withdraw the drug gradually over a period of several weeks.
- Hypertrophic subaortic stenosis: 80 mg Пропранолол SR once daily
Injection:
Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
The usual dose is 1 to 3 mg administered under careful monitoring, such as electrocardiography and central venous pressure. The rate of administration should not exceed 1 mg (1 mL) per minute to diminish the possibility of loweringblood pressureand causing cardiac standstill.
Sufficient time should be allowed for the drug to reach the site of action even when a slow circulation is present. If necessary, a second dose may be given after two minutes. Thereafter, additional drug should not be given in less than four hours. Additional propranolol hydrochloride should not be given when the desired alteration in rate or rhythm is achieved.
Transfer to oral therapy as soon as possible.
Side Effects
Пропранолол is usually well tolerated. Minor side effects such as cold extremities, nausea, diarrhea, sleep disturbances and lassitude are often transient. There have been reports of skin rashes and/or dry eyes associated with the use of beta-adrenergic blocking drugs.
Toxicity
Symptoms of overdose include hypotension, hypoglycemic seizure, restlessness, euphoria, insomnia. Patients with asthma may develop bronchospasm. In case of overdose, monitor vital signs, mental status, and blood glucose. Treat hypotension with intravenous fluids, bradycardia with atropine, and isoproterenol and aminophylline for bronchospasm. If patients do not respond to intravenous fluids, follow up with glucagon 50-150µg/kg intravenously, then 1-5mg/hour, followed by catecholamines. Dialysis will not be useful as propranolol is highly protein bound.
Precaution
Beta-adrenoceptor blocking drugs should be avoided in over heart failure. Пропранолол modifies the tachycardia of hypoglycaemic therapy in diabetic patients. Пропранолол may prolong the hypoglycaemic response to insulin.
Interaction
Beta-adrenoceptor blocking drugs interact with clonidine.If beta-adrenoceptor blocking drugs and clonidine are given concurrently, clonidine should be discontinued until several days after withdrawal of beta-adrenoceptor blocking drug. Care should be taken in prescribing a beta-adrenoceptor blocking drugs with class 1 antidysrhythmic agents (disopyramide).Beta-adrenoceptor blocking drugs should be used with caution in combination with verapamil in patients with impaired ventricular function.
Food Interaction
- Avoid alcohol. Alcohol increases propranolol plasma concentrations.
- Avoid natural licorice. Natural licorice inhibits the metabolism of propranolol, increasing drug exposure.
- Take with food.
[Moderate] ADJUST DOSING INTERVAL: The bioavailability of propranolol may be enhanced by food.
MANAGEMENT: Patients may be instructed to take propranolol at the same time each day, preferably with or immediately following meals.
Пропранолол Alcohol interaction
[Moderate]
Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.
Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.
Caution and close monitoring for development of hypotension is advised during coadministration of these agents.
Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.
Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.
Пропранолол Cholesterol interaction
[Moderate] Beta-adrenergic receptor blocking agents (aka beta-blockers) may alter serum lipid profiles.
Increases in serum VLDL and LDL cholesterol and triglycerides, as well as decreases in HDL cholesterol, have been reported with some beta-blockers.
Patients with preexisting hyperlipidemia may require closer monitoring during beta-blocker therapy, and adjustments made accordingly in their lipid-lowering regimen.
Пропранолол multivitamins interaction
[Moderate] ADJUST DOSING INTERVAL: Concurrent administration with calcium salts may decrease the oral bioavailability of atenolol and possibly other beta-blockers.
The exact mechanism of interaction is unknown.
In six healthy subjects, calcium 500 mg (as lactate, carbonate, and gluconate) reduced the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of atenolol (100 mg) by 51% and 32%, respectively.
The elimination half-life increased by 44%.
Twelve hours after the combination, beta-blocking activity (as indicated by inhibition of exercise tachycardia) was reduced compared to that with atenolol alone.
However, during a 4-week treatment in six hypertensive patients, there was no difference in blood pressure values between treatments.
The investigators suggest that prolongation of the elimination half-life induced by calcium coadministration may have led to atenolol cumulation during long-term dosing, which compensated for the reduced bioavailability.
It may help to separate the administration times of beta-blockers and calcium products by at least 2 hours.
Patients should be monitored for potentially diminished beta-blocking effects following the addition of calcium therapy.
Пропранолол Drug Interaction
Moderate: aripiprazole, diphenhydramine, duloxetine, clonazepam, fluoxetine, quetiapine, alprazolam, sertralineMinor: levothyroxine, ascorbic acidUnknown: amphetamine / dextroamphetamine, omega-3 polyunsaturated fatty acids, lamotrigine, escitalopram, pregabalin, topiramate, cyanocobalamin, cholecalciferol, lisdexamfetamine, cetirizine
Пропранолол Disease Interaction
Major: bradyarrhythmia/AV block, cardiogenic shock/hypotension, CHF, diabetes, hypersensitivity, ischemic heart disease, PVD, asthma/COPD, liver diseaseModerate: cerebrovascular insufficiency, glaucoma, hyperlipidemia, hyperthyroidism, hyperthyroidism PKs, myasthenia gravis, pheochromocytoma, psoriasis, tachycardia, Prinzmetal's variant angina, renal impairment
Volume of Distribution
The volume of distribution of propranolol is approximately 4L/kg or 320L.
Elimination Route
Patients taking doses of 40mg, 80mg, 160mg, and 320mg daily experienced Cmax values of 18±15ng/mL, 52±51ng/mL, 121±98ng/mL, and 245±110ng/mL respectively. Пропранолол has a Tmax of approximately 2 hours, though this can range from 1 to 4 hours in fasting patients. Taking propranolol with food does not increase Tmax but does increase bioavailability.
Half Life
The elimination half life of propranolol is approximately 8 hours. The plasma half life of propranolol is 3 to 6 hours.
Clearance
The clearance of propranolol is 2.7±0.03L/h/kg in infants 90 days. Пропранолол clearance increases linearly with hepatic blood flow. Propanolol has a clearance in hypertensive adults of 810mL/min.
Elimination Route
91% of an oral dose of propranolol is recovered as 12 metabolites in the urine.
Pregnancy & Breastfeeding use
There are no adequate and controlled studies in pregnant women. Пропранолол is excreted in human milk. Caution should be exercised when propranolol is administered to a nursing mother.
Contraindication
Пропранолол Hydrochloride is contraindicated in patients with known Hypersensitivity to any component of the formulation. If there is a history of bronchial asthma of bronchospasm.
Acute Overdose
The symptoms of over dosage may include bradycardia, hypotension, acute cardiac insufficiency and bronchospasm. Treatment of over dosage include close supervision, treatment in an intensive care ward, he use of gastric lavage, activated charcoal and a laxative to prevent absorption of any drug still present in the gastrointestinal tract, the use of plasma or plasma substitutes to treat hypotension and shock.
Storage Condition
Store in a cool dry place. Protect from light.
Innovators Monograph
You find simplified version here Пропранолол
Пропранолол contains Propranolol see full prescribing information from innovator Пропранолол Monograph, Пропранолол MSDS, Пропранолол FDA label
FAQ
What is Пропранолол usually prescribed for?
Пропранолол usually prescribed for high blood pressure and other heart problems, but it can also help with the physical signs of anxiety, like sweating and shaking.Пропранолол slows down your heart rate and makes it easier for your heart to pump blood around your body.
Is Пропранолол good for anxiety?
Пропранолол blocks the physical effects of anxiety, meaning you won't experience an increased heart rate, sweating and shakiness when you feel nervous. By blocking the physical symptoms of anxiety, propranolol can help you feel calmer, less nervous and more composed.
When should not I take Пропранолол?
You should not use Пропранолол if you are allergic to it, or if you have:
- asthma;
- very slow heart beats that have caused you to faint; or.
- a serious heart condition such as "sick sinus syndrome" or "AV block" (unless you have a pacemaker).
Can I take Пропранолол every day?
Пропранолол can be used daily for migraine prevention. It's only approved for prevention and shouldn't be used to stop a migraine that's already started. A common starting dose for migraine prevention is 80 mg per day, broken up into smaller, equal size doses throughout the day.
What time of day should I take Пропранолол?
Пропранолол extended release capsules should be taken at bedtime (10 pm). This medicine may be taken with or without food. However, you should take it the same way each time.
Does Пропранолол help me sleep?
Brand as well as other beta blockers, has been shown in some studies to reduce your body's secretion of melatonin an important hormone for optimal sleep. For a small percentage of propranolol users, this can lead to difficulties falling and staying asleep.
What are the worst side effects of Пропранолол?
Serious side effects of Пропранолол:
- Hallucinations.
- Cold hands or feet.
- Muscle weakness.
- Muscle cramps.
- Shortness of breath.
- Memory loss.
- Fluid retention.
- Blood sugar changes.
What can't I take with Пропранолол?
Some products that may interact with this drug include: alpha blockers (e.g., prazosin), aluminum hydroxide, anticholinergics (e.g., atropine, scopolamine), chlorpromazine, drugs affecting liver enzymes that remove Пропранолол from your body such as cimetidine, St.
What should be checked before giving Пропранолол?
Before administering Пропранолол, the nurse should always assess the patient's blood pressure and apical pulse.
Can Пропранолол harm for me?
Пропранолол may cause heart failure in some patients. Check with your doctor right away if you are having chest pain or discomfort, dilated neck veins, extreme fatigue, irregular breathing, an irregular heartbeat, swelling of the face, fingers, feet, or lower legs, or weight gain.
Can Пропранолол cause stroke?
Пропранолол will comes with serious risks if you don't take it as prescribed. If you don't take it at all: Your condition will get worse and you may be at risk of serious heart problems, such as heart attack or stroke.
Does Пропранолол affect breathing?
Пропранолол 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 people with pre-existing lung disease.
Does Пропранолол cause hair loss?
Пропранолол is one of several beta blockers that can cause hair loss. The hair loss from Пропранолол is not permanent and is typically a result of the medication causing some hair follicles to enter their shedding phase prematurely.
Can I drink alcohol with Пропранолол?
Mixing Пропранолол and alcohol is generally not advised by doctors or medical experts. This is because beta-blockers like Пропранолол lower your blood pressure by slowing your heart rate and reducing the force of each beat. Alcohol can also lower your blood pressure.
How many hours does Пропранолол last?
Пропранолол is usually taken once a day, and the effects last for 24 hours.
Is Пропранолол addictive?
Пропранолол is not a physically addictive, habit-forming medication.
What foods interact with Пропранолол?
Caffeine-containing food items and beverages when taken along with Пропранолол may decrease the effectiveness of the drug. It is better to avoid tea or coffee while taking Пропранолол.
How much does Пропранолол lower pulse?
The effects of oral Пропранолол were evaluated in 10 normal volunteers. The resting heart rate decreased from the mean control value of 68 plus or minus 3.3 (SE) to 56 plus or minus 2.8 beats per minute (bpm) on Пропранолол (p smaller than 0.001, paired test).
What is the antidote for Пропранолол?
Isoprenaline proved to be the best antidote for the treatment of Пропранолол intoxication antagonizing the bradycardia by 76% and the hypotension completely.
What is Пропранолол used for in mental health?
Пропранолол has been used for many years to treat high blood pressure and heart disease, and has been found useful in treating anxiety states such as social phobia and migraine.
Пропранолол for the Treatment of Acute Stress Disorder.
Can I Пропранолол if I have asthma?
Despite safety concerns, Пропранолол is still prescribed to some people with asthma and anxiety. Brand exposure is associated with an increased risk of asthma hospitalisation in susceptible people which appears to vary by dose and duration of exposure.
Can Пропранолол disturb sleep?
For a small percentage of Пропранолол users, this can lead to difficulties falling and staying asleep. Пропранолол is also linked to other sleep related issues, including nightmares and drowsiness. Like fatigue, sleep issues from Пропранолол are most common shortly after you start to use the medication.
Can Пропранолол cause permanent damage?
If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure.
Does Пропранолол affect appetite?
Пропранолол does effected depression,confusion, hallucinations; liver problems--nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
Can Пропранолол cause death?
We report on an 18-year-old man who ingested a massive dose of Пропранолол HCl in a suicide attempt. The patient was brought to the hospital in an unresponsive state within 30 minutes of ingestion. He was initially stabilized but subsequently died nine hours after the drug was ingested.
Can Пропранолол damage my heart?
Brand may cause heart failure in some patients. Check with your doctor right away if you are having chest pain or discomfort, dilated neck veins, extreme fatigue, irregular breathing, an irregular heartbeat, swelling of the face, fingers, feet, or lower legs, or weight gain.
Can Пропранолол affect my eyesight?
This Пропранолол can cause certain eye problems. If left untreated, this can lead to lasting eyesight loss. If eye problems happen, signs like change in eyesight or eye pain most often happen within hours to weeks of starting Пропранолол and hydrochlorothiazide. Call your doctor right away if you have these signs
What happens if I stop taking Пропранолол suddenly?
While stopping any beta-blocker may cause a mild response, abruptly stopping Пропранолол may lead to a withdrawal syndrome. Beta-blocker withdrawal can result in a rise in blood pressure, and in patients with heart disease, chest pain, heart attack, and even sudden death.
Is Пропранолол bad for my kidneys?
Пропранолол types of beta-blockers may reduce cardiac output and subsequently renal perfusion pressure, thereby exacerbating renal dysfunction.
Is Пропранолол safe during pregnancy?
Пропранолол 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. There are a number of abnormalities associated with the use of Пропранолол 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 Пропранолол include intrauterine growth retardation, small placentas, polycythemia, thrombocytopenia, and hypocalcemia.
Is Пропранолол to safe during breastfeeding?
Пропранолол is not recommended for mothers who are breastfeeding because it could potentially cause the baby's heart rate to slow down or its blood sugar to fall.
