Propranolol is a beta-blocker. Beta-blockers affect the heart and circulation (blood flow through arteries and veins).
Propranolol is used to treat tremors, angina (chest pain), hypertension (high blood pressure), heart rhythm disorders, and other heart or circulatory conditions. It is also used to treat or prevent heart attack, and to reduce the severity and frequency of migraine headaches.
(RS)-1-(1-methylethylamino)-3-(1-naphthyloxy)propan-2-ol
USES
For,
Hypertension
Angina pectoris
Tachyarrhythmias
Myocardial infarction
Control of tachycardia/tremor associated with anxiety, hyperthyroidism or lithium therapy.
Essential tremor
Migraine prophylaxis
Cluster headaches prophylaxis
Tension headache (Off label use)
Shaky hands
Hyperhidrosis
There has been some experimentation in psychiatric areas:
Treating the excessive drinking of fluids in psychogenic polydipsia,
Antipsychotic-induced akathisia,
Aggressive behavior of patients with brain injuries
Post-traumatic stress disorder
Calming down individuals with phobias via sedative effects
Performance anxiety
Glaucoma
Thyrotoxicosis via deiodinase inhibition
Primary exertional headache
While once first-line treatment for hypertension, the role for beta-blockers was downgraded in June 2006 in the United Kingdom to fourth-line as they perform less well than other drugs, particularly in the elderly, and evidence is increasing that the most frequently used beta-blockers at usual doses carry an unacceptable risk of provoking type 2 diabetes.
Propranolol is also used to lower portal vein pressure in portal hypertension and prevent esophageal variceal bleeding and ascites.
MECHANISM OF ACTION
Propranolol is a non-selective beta blocker, that is, it blocks the action of epinephrine and norepinephrine on both β1- and β2-adrenergic receptors. It has little intrinsic sympathomimetic activity (ISA) but has strong membrane stabilizing activity (only at high blood concentrations, e.g. overdosage). Research has also shown that propranolol has inhibitory effects on the norepinephrine transporter and/or stimulates norepinephrine release (present experiments have shown that the concentration of norepinephrine is increased in the synapse but do not have the ability to discern which effect is taking place).[31] Since propranolol blocks β-adrenoceptors, the increase in synaptic norepinephrine only results in α-adrenergic activation, with the α1-adrenoceptor being particularly important for effects observed in animal models. Therefore, some have suggested that it be looked upon as an indirect α1 agonist as well as a β antagonist. Probably owing to the effect at the α1-adrenoceptor, the racemic and the individual enantiomers of propranolol have been shown to substitute for cocaine in rats, with the most potent enantiomer being S-(–)-propranolol. In addition, some evidence suggests that propranolol may function as a partial agonist at one or more serotonin receptors (possibly 5-HT1B).
Both enantiomers of the drug have a local anesthetic (topical) effect, which is normally mediated by blockade of voltage-gated sodium channels. Few studies have demonstrated propranolol's ability to block cardiac, neuronal, and skeletal voltage-gated sodium channels, accounting for its known "membrane stabilizing effect" and anti-arrhythmic and other central nervous system effects.
Important information about propranolol :
You should not use this medication if you are allergic to propranolol, if you have asthma, a slow heart rate, or a serious heart condition such as "sick sinus syndrome" or "AV block" (unless you have a pacemaker). If you need surgery, tell the surgeon ahead of time that you are using propranolol. You may need to stop using the medicine for a short time. Do not skip doses or stop using propranolol without first talking to your doctor. You may need to use less and less before you stop the medication completely.
Avoid drinking alcohol. It may increase your blood levels of propranolol.
Propranolol is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.
If you are being treated for high blood pressure, keep using propranolol even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.
DOSAGES
Usual Adult Propranolol Dose for Hypertension:
Initial dose: 40 mg orally twice a day or 80 mg sustained release once a day, whether used alone or added to a diuretic. The dose should be administered at bedtime (approximately 10 PM).
Maintenance dose: 120 to 240 mg/day or 120 to 160 mg/day of sustained release
Maximum dose: 640 mg/day.
Usual Adult Propranolol Dose for Angina Pectoris:
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/day.
Usual Adult Propranolol Dose for Arrhythmias:
Oral: 10 to 30 mg 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, additional drug should not be given in less than 4 hours. Additional propranolol should not be given when the desired alteration in rate and/or rhythm is achieved.
Usual Adult Propranolol Dose for Myocardial Infarction:
180 to 240 mg/day in 3 to 4 divided doses.
Usual Adult Propranolol Dose for Migraine Prophylaxis:
Initial dose: 80 mg/day orally in divided doses.
Maintenance dose: 160 to 240 mg/day.
The dosage may be increased gradually to achieve optimum migraine prophylaxis. If a satisfactory response is not obtained within 4 to 6 weeks after reaching the maximum dose, propranolol therapy should be discontinued.
Sustained release: Initial dose: 80 mg orally once a day.
Maintenance dose: 160 to 240 mg once a day.
Usual Adult Propranolol Dose for Benign Essential Tremor:
Initial dose: 40 mg orally twice a day.
Maintenance dose: 120 to 320 mg/day.
Optimum reduction of essential tremor is usually achieved with a dose of 120 mg/day.
Occasionally, it may be necessary to administer 240 to 320 mg/day.
Usual Adult Propranolol Dose for Aortic Stenosis:
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.
Usual Adult Propranolol Dose for Pheochromocytoma:
Preoperatively: 60 mg/day orally in divided doses for 3 days prior to surgery, concomitantly with an alpha-adrenergic blocking agent.
Management of Inoperable Tumor: 30 mg/day orally in divided doses.
Usual Pediatric Propranolol 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).
Usual Pediatric Propranolol Dose for Hypertension:
Children:
Immediate release formulations:
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:
Immediate release formulations:
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).
Usual Pediatric Propranolol 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.
BRANDS
Beptazine Propranolol, Dihydralazine Sulphate M.M.LABS
Beptazine -H Propranolol, Dihydralazine Sulphate,Hydrochlorothiazide M.M LABS
Betaprp -DZ Propranolol, Diazepam Consern Pharma Pvt Ltd.
ciplar 10 proranolol cipla
inderal 10
Avlocardyl, Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilinum, Bedranol SR
Propranolol is used to treat tremors, angina (chest pain), hypertension (high blood pressure), heart rhythm disorders, and other heart or circulatory conditions. It is also used to treat or prevent heart attack, and to reduce the severity and frequency of migraine headaches.
(RS)-1-(1-methylethylamino)-3-(1-naphthyloxy)propan-2-ol
USES
For,
Hypertension
Angina pectoris
Tachyarrhythmias
Myocardial infarction
Control of tachycardia/tremor associated with anxiety, hyperthyroidism or lithium therapy.
Essential tremor
Migraine prophylaxis
Cluster headaches prophylaxis
Tension headache (Off label use)
Shaky hands
Hyperhidrosis
There has been some experimentation in psychiatric areas:
Treating the excessive drinking of fluids in psychogenic polydipsia,
Antipsychotic-induced akathisia,
Aggressive behavior of patients with brain injuries
Post-traumatic stress disorder
Calming down individuals with phobias via sedative effects
Performance anxiety
Glaucoma
Thyrotoxicosis via deiodinase inhibition
Primary exertional headache
While once first-line treatment for hypertension, the role for beta-blockers was downgraded in June 2006 in the United Kingdom to fourth-line as they perform less well than other drugs, particularly in the elderly, and evidence is increasing that the most frequently used beta-blockers at usual doses carry an unacceptable risk of provoking type 2 diabetes.
Propranolol is also used to lower portal vein pressure in portal hypertension and prevent esophageal variceal bleeding and ascites.
MECHANISM OF ACTION
Propranolol is a non-selective beta blocker, that is, it blocks the action of epinephrine and norepinephrine on both β1- and β2-adrenergic receptors. It has little intrinsic sympathomimetic activity (ISA) but has strong membrane stabilizing activity (only at high blood concentrations, e.g. overdosage). Research has also shown that propranolol has inhibitory effects on the norepinephrine transporter and/or stimulates norepinephrine release (present experiments have shown that the concentration of norepinephrine is increased in the synapse but do not have the ability to discern which effect is taking place).[31] Since propranolol blocks β-adrenoceptors, the increase in synaptic norepinephrine only results in α-adrenergic activation, with the α1-adrenoceptor being particularly important for effects observed in animal models. Therefore, some have suggested that it be looked upon as an indirect α1 agonist as well as a β antagonist. Probably owing to the effect at the α1-adrenoceptor, the racemic and the individual enantiomers of propranolol have been shown to substitute for cocaine in rats, with the most potent enantiomer being S-(–)-propranolol. In addition, some evidence suggests that propranolol may function as a partial agonist at one or more serotonin receptors (possibly 5-HT1B).
Both enantiomers of the drug have a local anesthetic (topical) effect, which is normally mediated by blockade of voltage-gated sodium channels. Few studies have demonstrated propranolol's ability to block cardiac, neuronal, and skeletal voltage-gated sodium channels, accounting for its known "membrane stabilizing effect" and anti-arrhythmic and other central nervous system effects.
Important information about propranolol :
You should not use this medication if you are allergic to propranolol, if you have asthma, a slow heart rate, or a serious heart condition such as "sick sinus syndrome" or "AV block" (unless you have a pacemaker). If you need surgery, tell the surgeon ahead of time that you are using propranolol. You may need to stop using the medicine for a short time. Do not skip doses or stop using propranolol without first talking to your doctor. You may need to use less and less before you stop the medication completely.
Avoid drinking alcohol. It may increase your blood levels of propranolol.
Propranolol is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.
If you are being treated for high blood pressure, keep using propranolol even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.
DOSAGES
Usual Adult Propranolol Dose for Hypertension:
Initial dose: 40 mg orally twice a day or 80 mg sustained release once a day, whether used alone or added to a diuretic. The dose should be administered at bedtime (approximately 10 PM).
Maintenance dose: 120 to 240 mg/day or 120 to 160 mg/day of sustained release
Maximum dose: 640 mg/day.
Usual Adult Propranolol Dose for Angina Pectoris:
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/day.
Usual Adult Propranolol Dose for Arrhythmias:
Oral: 10 to 30 mg 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, additional drug should not be given in less than 4 hours. Additional propranolol should not be given when the desired alteration in rate and/or rhythm is achieved.
Usual Adult Propranolol Dose for Myocardial Infarction:
180 to 240 mg/day in 3 to 4 divided doses.
Usual Adult Propranolol Dose for Migraine Prophylaxis:
Initial dose: 80 mg/day orally in divided doses.
Maintenance dose: 160 to 240 mg/day.
The dosage may be increased gradually to achieve optimum migraine prophylaxis. If a satisfactory response is not obtained within 4 to 6 weeks after reaching the maximum dose, propranolol therapy should be discontinued.
Sustained release: Initial dose: 80 mg orally once a day.
Maintenance dose: 160 to 240 mg once a day.
Usual Adult Propranolol Dose for Benign Essential Tremor:
Initial dose: 40 mg orally twice a day.
Maintenance dose: 120 to 320 mg/day.
Optimum reduction of essential tremor is usually achieved with a dose of 120 mg/day.
Occasionally, it may be necessary to administer 240 to 320 mg/day.
Usual Adult Propranolol Dose for Aortic Stenosis:
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.
Usual Adult Propranolol Dose for Pheochromocytoma:
Preoperatively: 60 mg/day orally in divided doses for 3 days prior to surgery, concomitantly with an alpha-adrenergic blocking agent.
Management of Inoperable Tumor: 30 mg/day orally in divided doses.
Usual Pediatric Propranolol 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).
Usual Pediatric Propranolol Dose for Hypertension:
Children:
Immediate release formulations:
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:
Immediate release formulations:
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).
Usual Pediatric Propranolol 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.
BRANDS
Beptazine Propranolol, Dihydralazine Sulphate M.M.LABS
Beptazine -H Propranolol, Dihydralazine Sulphate,Hydrochlorothiazide M.M LABS
Betaprp -DZ Propranolol, Diazepam Consern Pharma Pvt Ltd.
ciplar 10 proranolol cipla
inderal 10
Avlocardyl, Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilinum, Bedranol SR
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