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Propranolol is a synthetic, nonselective beta-adrenergic receptor blocker with antianginal, antiarrhythmic, antihypertensive properties. Propranololcompetitively antagonizes beta-adrenergic receptors, thereby causing negative chronotropic and inotropic effects leading to a reduction in cardiac output.
Propranolol is used in the treatment or prevention of many disorders including acute myocardial infarction, arrhythmias, angina pectoris, hypertension, hypertensive emergencies, thyroid gland makes too much hormone. সহজ বাংলা: থাইরয়েড হরমোন বেশি।" data-rx-term="hyperthyroidism" data-rx-definition="Hyperthyroidism means the thyroid gland makes too much hormone. সহজ বাংলা: থাইরয়েড হরমোন বেশি।">hyperthyroidism, pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।" data-rx-term="migraine" data-rx-definition="Migraine is a recurring headache disorder often with throbbing pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।">migraine, pheochromocytoma, menopause, and anxiety. Due to the high penetration across the blood-brain barrier, lipophilic beta blockers such as propranolol and metoprolol are more likely than other less lipophilic beta blockers to cause sleep disturbances such as insomnia and vivid dreams, and nightmares. Dreaming (rapid eye movement sleep, REM) was reduced and increased awakening.
Mechanism of Action of Propranolol
Propranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.
Propranolol is classified as a 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 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 activity (only at high blood concentrations, e.g. overdose). Propranolol is able to cross the blood-brain barrier and exert effects in the central nervous system in addition to its peripheral activity.
In addition to blockade of adrenergic receptors, propranolol has very weak inhibitory effects on the norepinephrine transporter and/or weakly stimulates norepinephrine release (i.e., the concentration of norepinephrine is increased in the synapse). Since propranolol blocks β-adrenoceptors, the increase in synaptic norepinephrine only results in α-adrenoceptor activation, with the α1-adrenoceptor being particularly important for effects observed in animal models. Therefore, it can be looked upon as a weak indirect α1-adrenoceptor agonist in addition to the potent β-adrenoceptor antagonist. In addition to its effects on the adrenergic system, there is evidence that indicates that propranolol may act as a weak antagonist of certain serotonin receptors, namely the 5-HT1A, 5-HT1B, and 5-HT2Breceptors. The latter may be involved in the effectiveness of propranolol in the treatment of a pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।" data-rx-term="migraine" data-rx-definition="Migraine is a recurring headache disorder often with throbbing pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।">migraine at high doses
or
Propranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.
Indications of Propranolol
Cardiovascular
- Hypertension
- Angina pectoris (with the exception of variant angina)
- Arrhythmia
- Aortic Stenosis
- Atrial Fibrillation
- Tachyarrhythmia
- Myocardial infarction
- Tachycardia (and other sympathetic nervous system symptoms, such as muscle tremor) associated with various conditions, including anxiety, panic, thyroid gland makes too much hormone. সহজ বাংলা: থাইরয়েড হরমোন বেশি।" data-rx-term="hyperthyroidism" data-rx-definition="Hyperthyroidism means the thyroid gland makes too much hormone. সহজ বাংলা: থাইরয়েড হরমোন বেশি।">hyperthyroidism, and lithium therapy
- Portal hypertension, to lower portal vein pressure
- Prevention of esophageal variceal bleeding and ascites
- Anxiety
- Hypertrophic cardiomyopathy
- Hemangioma
- Intermittent Explosive Disorder
- Mitral Valve Prolapse
- Panic Disorder
- Pheochromocytoma
- Portal Hypertension
- Tardive Dyskinesia
- Thyrotoxicosis
Psychiatric
Propranolol is occasionally used to treat performance anxiety. Evidence to support its use in other anxiety disorders is poor. Some experimentation has been conducted in other psychiatric areas
- Post-traumatic stress disorder (PTSD) and specific phobias
- Aggressive behavior of patients with brain injuries
- Treating the excessive drinking of fluids in psychogenic polydipsia
- Treatment of specific phobias, such as arachnophobia, dental fear, and social phobia.
Others
- Essential tremor. Evidence for use for akathisia, however, is insufficient
- Migraine and cluster headache prevention and in primary exertional pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">headache
- Hyperhidrosis (excessive sweating)
- Proliferating infantile hemangioma
- Glaucoma
- Thyrotoxicosis by deiodinase inhibition
- Akathisia caused by the antipsychotic use
- Angina Pectoris
- Cardiovascular Mortality
- Gastroesophageal variceal hemorrhage prophylaxis
- Hemangiomas
- High Blood Pressure (Hypertension)
- Idiopathic hypertrophic subaortic stenosis
- Migraines
- Nonvalvular Atrial Fibrillation
- Obstructive Hypertrophic Cardiomyopathy
- Performance Anxiety
- Pheochromocytomas
- Supraventricular Arrhythmias
- Tachyarrhythmia caused by Digitalis intoxication
- Tachyarrhythmia caused by catecholamine excess
- Thyroid Crisis
- Thyrotoxicosis
- The tremor caused by lithium
- Tremor, Essential
- Ventricular Tachycardia
Contra-Indications of Propranolol
Propranolol may be contraindicated in people with
- Reversible airways diseases, particularly asthma or chronic obstructive pulmonary disease (COPD)
- Bradycardia (<60 beats/minute)
- Sick sinus syndrome
- Atrioventricular block (second- or third-degree)
- Shock
- Severe hypotension
- Cocaine toxicity
Dosage of Propranolol
Strengths: 10 mg; 20 mg; 40 mg; 60 mg; 80 mg; 120 mg; 160 mg; & 1 mg/mL; 20 mg/5 mL; 80 mg/mL; 40 mg/5 mL; 4.28 mg/mL
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
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. The average optimal dosage appears to be 160 mg once a day.
- Maximum dose: 320 mg per day
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
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. Thereafter, the additional drug should not be given in less than 4 hours.
pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।" data-rx-term="migraine" data-rx-definition="Migraine is a recurring headache disorder often with throbbing pain, nausea, or light sensitivity. সহজ বাংলা: বারবার হওয়া বিশেষ ধরনের মাথাব্যথা।">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
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
Benign Essential Tremor
Immediate-release
- Initial dose: 40 mg orally 2 times a day
- Maintenance dose: 120 to 320 mg orally per day
Adult Dose for Atrial Fibrillation
Immediate-release
- 10 mg to 30 mg orally 3 or 4 times a day before meals and at bedtime
Pediatric Dose for Arrhythmias
- Oral: Children: Initial: 0.5 to 1 mg/kg/day in divided doses every 6 to 8 hours; titrate dosage upward every 3 to 5 days;
- usual dose: 2 to 4 mg/kg/day; higher doses may be needed; do not exceed 16 mg/kg/day
- IV: Children: 0.01 to 0.1 mg/kg slow IV over 10 minutes; maximum dose: 1 mg (infants); 3 mg (children)
Pediatric Dose for Hypertension
- Children:Initial: 0.5 to 1 mg/kg/day in divided doses every 6 to 12 hours; increase gradually every 5 to 7 days
- Usual dose: 1 to 5 mg/kg/day
- Maximum dose: 8 mg/kg/day
Children and Adolescents 1 to 17 years
- Initial: 1 to 2 mg/kg/day divided in 2 to 3 doses/day; titrate dose to effect
- Maximum dose: 4 mg/kg/day up to 640 mg/day;
- Sustained release formulation may be dosed once daily (National High Blood Pressure Education Program Working Group on High Blood Pressure in Children and Adolescents).
Pediatric Dose for Thyrotoxicosis
- Neonates: Oral: 2 mg/kg/day in divided doses every 6 to 12 hours; occasionally higher doses may be required
- Adolescents: Oral: 10 to 40 mg/dose every 6 hours
Side Effects of Propranolol
The most common
- A dry cough
- Depression
- Dizziness and light-headedness due to low blood pressure
- Fatigue, especially in the early stages
- Mouth dryness in the early stages
- The most common (a burning feeling in the chest, behind the breastbone or gullet)
- Abdominal or stomach pain
- Constipation
- High blood pressure
- Nausea, vomiting,
- painful or swollen gums
- numbness or heavy feeling in the jaw
- dull, aching pain in the hip, groin, or thigh
- stomach pain,
- a headache,
- reversible hair loss or thinning, and
- fever.
Common
- chills or fever
- a headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- excessive sweating
- sudden drowsiness or need to sleep
- coughing up blood
- liver problems–nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes)
- decreased amount of urine
Rare
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- hallucinations
- headache
- irritability
- lightheadedness
- cold and clammy skin
- fast and shallow breathing
- swelling of your feet, legs, or hands purple spot on your skin caused by internal bleeding
- fast or abnormal heart rate or palpitations
- loss of appetite
- lower back, side, or stomach pain
- mental depression
- muscle pain or cramps
Drug Interactions of Propranolol
Propranolol may interact with following drugs, supplements, & may change the efficacy of drugs
- aminophylline
- asthma medications (e.g., theophylline)
- diabetes medications (e.g., glyburide)
- calcium channel blocker medicines (e.g., diltiazem, nifedipine, verapamil)
- diltiazem
- medications for abnormal heart rhythms (e.g., disopyramide)
- nitroglycerin
- nonsteroidal anti-inflammatory medications (NSAIDs; e.g., indomethacin, naproxen)
- oral diabetes medications (e.g., metformin, pioglitazone)
- pentoxifylline
- monoamine oxidase (MAO) inhibitors (e.g., phenelzine, selegiline, )
- other beta-blockers (e.g., propranolol, metoprolol)
- oxtriphylline
- verapamil
- SSRI antidepressants including fluoxetine, paroxetine, fluvoxamine,
- Other drugs to treat high blood pressure (e.g., clonidine, hydralazine, methyldopa, , haloperidol,)
- other heart medications (e.g. , quinidine), theophylline, thioridazine, thyroid hormones (e.g., levothyroxine),
- warfarin.
This medication may interfere with certain laboratory tests (including glaucoma screening test, cardiovascular stress testing using arbutamine), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.
Pregnancy & Lactation of Propranolol
FDA pregnancy catagory C
Research in animals has shown adverse effects to the fetus when the mother takes the drug.There haven’t been enough studies done in humans to be certain how the drug might affect the fetus.
Tell your doctor if you’re pregnant or plan to become pregnant. Propranolol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Lactation
Propranolol is passed through breast milk. The drug may be used while you’re breastfeeding, but your baby should be monitored. In your baby, propranolol may cause lower heart rate, low blood sugar, and decreased oxygen in the blood that can cause blue color in your baby’s skin, lips, or nails (cyanosis).
References
