Propranolol

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Propranolol.jpg

[edit] MECHANISM OF ACTION

Propranolol is a lipophilic non-selective beta-adrenoceptor blocker, it blocks both β1 and β2 adrenergic receptors, reducing ability of the sympathetic nervous system to increase the myocardial contractile force and rate.

Propranolol also inhibit the release of renin by the kidneys (the release of renin from the kidney is regulated by the β1-adrenoceptors). Decreasing circulating plasma renin leads to a decrease in angiotensin II (a potent vasoconstrictor)

[edit] INDICATIONS

  • Hypertension
  • Angina prophylaxis
  • Arrhythmia prophylaxis after MI
  • Supraventricular tachycardia
  • Hypertrophic cardiomyopathy
  • Migraine
  • Tremor
  • Thyrotoxicosis [Propranolol reduces some of the peripheral manifestations (e.g.,tachycardia, sweating, severe tremor , nervousness) of hyperthyroidism]. In addition to providing symptomatic relief, propranolol inhibits the peripheral conversion of T4 to T3.

[edit] DOSAGE

Hypertension
Dosage must be individualized. The usual initial dosage is 40 mg twice daily, whether used alone or added to a diuretic. Dosage may be increased gradually until adequate blood pressure is achieved. The usual dosage is 160-480 mg/day. In some instances, a dosage of 640 mg/day may be required.

Angina Pectoris
Dosage must be individualized. Starting with 10-20 mg 3-4 times daily before meals and at bedtime, dosage should be gradually increased at 3-7 day intervals until optimum response is obtained. If treatment is to be discontinued, the dosage should be reduced gradually over a period of several weeks.

Arrhythmias
10-30 mg 3-4 times daily, before meals and at bedtime.

Migraine
Dosage must be individualized. The initial oral dose is 80 mg daily, in divided doses. The usual effective dose range is 160-240 mg/day. The dosage may be increased gradually to achieve optimum migraine prophylaxis.

Hypertrophic Subaortic Stenosis
20-40 mg 3-4 times daily, before meals and at bedtime.

Pheochromocytoma
Preoperatively
60 mg daily in divided doses for 3 days prior to surgery, concomitantly with an alpha-adrenergic blocking agent.

Management of Inoperable Tumor
30 mg daily, in divided doses.

Myocardial Infarction
The recommended dosage is 180-240 mg/day, in divided doses. The effectiveness and safety of daily dosages greater than 240 mg for the prevention of cardiac mortality has not been established.

[edit] CONTRAINDICATIONS

  • Propranolol is contraindicated in patients with asthma or a history of bronchospasm
  • Known hypersensitivity to the drug.
  • Sinus bradycardia and greater than first degree heart block, cardiogenic shock, right ventricular failure secondary to pulmonary hypertension, congestive heart failure unless secondary to a tachyarrhythmia treatable with Beta blockers.

[edit] WARNINGS AND PRECAUTIONS

Cardiac Failure
Sympathetic stimulation may be a vital component supporting circulatory function in congestive heart failure, and ß-blockade always carries the potential hazard of further depressing myocardial contractility and precipitating cardiac failure.

In hypertensive and angina pectoris patients, presenting with congestive heart failure controlled by digitalis and diuretics, special caution should be exercised when administering the ß-blocker, since both digitalis and the beta blocker depress AV conduction.

In patients without a history of cardiac failure, continued depression of the myocardium by ß-blockers over a period of time can, in some cases, lead to cardiac failure. Therefore, at the first sign or symptom of impending cardiac failure, patients should be fully digitalized and/or given a diuretic. The response should be observed closely. If cardiac failure continues, despite adequate digitalization and diuretic therapy, ß-blocker therapy should be gradually withdrawn.

Discontinuation of Therapy
Ischemic Heart Disease
Severe exacerbation of angina and the occurrence of myocardial infarction and ventricular arrhythmia have been reported in angina patients following the abrupt discontinuation of therapy with ß-blockers. Because of the problems encountered with ß-blockers, when discontinuation of therapy is planned, patients should be carefully observed and advised to limit physical activity to a minimum.

If the angina worsens or acute coronary insufficiency develops, it is recommended that therapy be promptly reinstituted, at least temporarily.

Thyrotoxicosis
Beta Adrenergic blockade may mask certain clinical signs of hyperthyroidism (e.g. tachycardia). Abrupt withdrawal may be followed by an exacerbation of the symptoms of hyperthyroidism, including thyroid storm.

Hypotension during Anaesthesia
Some patients receiving ß-adrenergic blocking agents have been subject to protracted severe hypotension during anesthesia. Therefore, in elective surgery, ß-blockers should be withdrawn gradually. Clinical evidence suggests that the effect of ß-blockade is no longer present 48 hours after withdrawal of the drug. In emergency surgery, since ß-blockers are competitive inhibitors of ß-adrenergic receptor agonists, their effects on the heart can be reversed by the administration of such agents (e.g, dobutamine or isoproterenol) with caution. Manifestations of vagal tone (e.g. profound bradycardia or hypotension) may be corrected by the I.V. administration of atropine 1-2 mg.

If Beta-blockade is continued during surgery, care should be taken when using anesthetic agents, which depress the myocardium (e.g. ether, cyclopropane, tetrachloroethylene).

Propranolol is not to be used in the treatment of migraine after an attack has begun.

[edit] INTERACTIONS

[edit] PHARMACOKINETICS

Propranolol is completely absorbed after oral administration and peak plasma concentrations occur 1 to 2 hours after dosing in fasting patients. The liver removes up to 90% of an oral dose with an elimination half-life of 3 to 6 hours. Propranolol is widely and rapidly distributed throughout the body with highest levels occurring in the lungs, liver, kidney, brain, and heart. Propranolol is highly protein bound (80 to 95%).
Since the half-life may be increased in patients with significant hepatic or renal impairment, care should be taken when starting treatment and selecting the initial dose.

[edit] PREGNANCY AND LACTATION

Pregnancy Category C (US): The drug should be used only if clearly needed. Neonatal bradycardia, hypoglycemia and respiratory depression have been associated with both cardioselective and non-cardioselective Beta blocker therapy during pregnancy.

Nursing Mothers: Beta blockers appear in breast milk. Patients using this drug should stop nursing.

[edit] SIDE EFFECTS

  • Centrally-mediated side effects (because of its lipid solubility), such as sleep disturbances (Insomnia), vivid dreams, nightmares and, rarely, hallucinations
  • Sexual dysfunction
  • Bradycardia
  • Asthma (bronchoconstriction)

[edit] RELATED LINKS

[edit] REFERENCES

Antihypertensives
ACE inhibitors Benazepril (Lotensin)   Captopril (Capoten)   Cilazapril   Delapril   Enalapril (Renitec, Vasotec)   Fosinopril (Monopril)  Lisinopril (Prinivil, Zestril)   Moexipril (Univasc)  Perindopril (Aceon)  Quinapril (Accupril)  Ramipril (Altace, Triatec)   Trandolapril (Mavik)  Zofenopril (Bifril, Zopranol)
Angiotensin II receptor antagonist Azilsartan (Edarbi)   Candesartan (Atacand)   Eprosartan (Teveten)   Irbesartan (Aprovel, Avapro, Karvea)   Losartan (Cozaar)   Olmesartan (Benicar, Olmetec)   Telmisartan (Micadis)   Valsartan (Diovan, Tareg)
Renin inhibitors Aliskiren (Rasilez, Tekturna)
Alpha-1 blockers Doxazosin (Cardura)   Prazosin (Minipress)   Terazosin (Hytrin)
Alpha-2 agonists (centrally acting) Clonidine (Oral route)   Clonidine (Transdermal) (Catapresan)   Guanfacine (Tenex)   Methyldopa (Aldomet)
Calcium channel blockers Dihydropyridines‎ Amlodipine (Norvasc)   Barnidipine (Vasexten)   Felodipine (Plendil)   Isradipine (Dynacirc)   Lacidipine (Lacipil, Motens)   Lercanidipine (Zanidip)   Manidipine   Nicardipine   Nifedipine (Adalat)   Nisoldipine   Nitrendipine
Benzothiazepine‎ Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)
Phenylalkylamine‎ Gallopamil   Verapamil (Calan)
Beta blockers Beta1 selective (cardioselective) Acebutolol (Sectral)   Atenolol (Tenormin)   Betaxolol (Kerlon)   Bisoprolol (Concor)   Celiprolol (Cordiax)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Nebivolol (Bystolic, Lobivon, Nebilox)
Nonselective (Beta1 and Beta2 blockers) Oxprenolol (Trasitensin)   Propranolol (Inderal)   Timolol (Blocadren)
Nonselective (Beta1, Beta2 and Alpha1 blockers) Carvedilol (Dilatrend)   Labetalol (Trandate)
Beta blocker with intrinsic sympathomimetic activity (ISA) Acebutolol (Sectral)   Celiprolol (Cordiax)
Lipophilic Beta blockers Propranolol (Inderal)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Oxprenolol (Trasitensin)
Diuretics Carbonic anhydrase inhibitors Acetazolamide (Diamox)
Loop diuretics Bumetanide   Etacrynic acid   Furosemide (Lasix)   Piretanide   Torasemide (Demadex)
Thiazide diuretics Chlorothiazide (Diuril)   Hydrochlorothiazide (Esidrex)
Thiazide-like diuretics Chlortalidone (Hygroton)   Indapamide (Lozol, Lozide)   Metolazone
Potassium-sparing diuretics Epithelial sodium channel blockers: Amiloride (Midamor)   Triamterene (Dyrenium)
Aldosterone receptor antagonists: Potassium canrenoate   Eplerenone (Inspra)   Spironolactone (Aldactone)
Osmotic diuretics Mannitol
Combination therapy Amiloride/Hydrochlorothiazide (Moduretic)   Spironolactone/Hydrochlorothiazide (Aldactazide)
Antimigraine preparations
5 HT1 agonists (Triptans) Almotriptan (Almogran, Axert)   Eletriptan (Relpax)   Frovatriptan (Frova, Migard, Menatriptan)   Rizatriptan (Maxalt)   Sumatriptan (Imigran)   Zolmitriptan (Zomig)
Ergot alkaloids Dihydroergotamine   Ergotamine
NSAIDs/ Analgesics Indometacin   Acetylsalicylic acid (Aspirin)   Diclofenac (Voltaren)   Ibuprofen (Advil, Brufen, Dolgit, Nurofen)   Ketorolac (Toradol)   Naproxen (Naprosyn, Aleve)   Nimesulide   Paracetamol (Efferalgan, Panadol...)
Prophylaxis Cinnarizine (Stugeron, Stugeron forte)   Flunarizine (Sibelium)   Nifedipine (Adalat)   Pizotifen   Propranolol (Inderal)   Topiramate (Topamax)