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

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-HT_1A, 5-HT_1B, and 5-HT_2Breceptors. The latter may be involved in the effectiveness of propranolol in the treatment of a migraine at high doses

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, 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.

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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

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.

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

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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

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.

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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).