Propranolol; Uses, Dosage, Side Effects, Interactions, Pregnancy

Propranolol, Propranolol; Uses, Dosage, Side Effects, Interactions, Pregnancy, Rx Harun
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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, hyperthyroidism, 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 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.

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Indications of Propranolol

Cardiovascular

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

Others

  • Essential tremor. Evidence for use for akathisia, however, is insufficient
  • Migraine and cluster headache prevention and in primary exertional 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

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.
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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

Common

Rare

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Drug Interactions of Propranolol

Propranolol may interact with following drugs, supplements, & may change the efficacy of drugs

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

Pregnancy
Propranolol is a category C pregnancy drug. That means

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

Propranolol, Propranolol; Uses, Dosage, Side Effects, Interactions, Pregnancy, Rx Harun

Propranolol, Propranolol; Uses, Dosage, Side Effects, Interactions, Pregnancy, Rx Harun

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