Atenolol

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Atenolol.jpg

[edit] MECHANISM OF ACTION

Atenolol is a β1 selective adrenergic antagonist;

β1 receptors are predominantly located in the heart. The blockade of these receptors reduces the ability of the sympathetic nervous system to increase the myocardial contractile force and rate and the result is a decrease in heart rate and blood pressure

β1 receptors are also located in the juxtaglomerular apparatus of the kidney. The blockade of these receptors inhibits the release of renin from the kidney. Decreased circulating plasma renin leads to a decrease in angiotensin II and aldosterone production, causing a decrease in vasoconstriction and a decrease in water retention.

Atenolol has the lowest lipid solubility of this drug class and it does not have intrinsic sympathomimetic properties or membrane-stabilizing activity.

[edit] INDICATIONS

  • Hypertension (lowering blood pressure lowers the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions.
  • Angina pectoris due to coronary atherosclerosis
  • Management of hemodynamically stable patients with definite or suspected acute myocardial infarction to reduce cardiovascular mortality. Treatment can be initiated as soon as the patient's clinical condition allows

[edit] DOSAGE

  • Hypertension: initial dose is 50 mg/day either alone or added to diuretic therapy. The full effect of this dose will usually be seen within one to two weeks. If an optimal response is not achieved, the dosage should be increased to 100 mg/day.
  • Angina Pectoris: The initial dose is 50 mg/day. If an optimal response is not achieved within one week, the dosage should be increased to 100 mg/day. Some patients may require a dosage of 200 mg once a day for optimal effect.
  • Acute Myocardial Infarction: In patients with definite or suspected acute myocardial infarction, treatment with Atenolol I.V. Injection should be initiated as soon as possible after the patient's arrival in the hospital and after eligibility is established. Treatment should begin with 5 mg of Atenolol over 5 minutes followed by another 5 mg intravenous injection 10 minutes later.

    In patients who tolerate the full intravenous dose (10 mg), Atenolol Tablets 50 mg should be initiated 10 minutes after the last intravenous dose followed by another 50 mg oral dose 12 hours later. Thereafter, Atenolol can be given orally either 100 mg once daily or 50 mg twice a day for a further 6-9 days or until discharge from the hospital. If bradycardia or hypotension requiring treatment or any other untoward effects occur, Atenolol should be discontinued.

    Data from other beta blocker trials suggest that if there is any question concerning the use of IV beta blocker or clinical estimate that there is a contraindication, the IV beta blocker may be eliminated and patients fulfilling the safety criteria may be given Atenolol Tablets 50 mg twice daily or 100 mg once a day for at least seven days.
    Although the demonstration of efficacy of Atenolol is based entirely on data from the first seven postinfarction days, data from other beta blocker trials suggest that treatment with beta blockers that are effective in the postinfarction setting may be continued for one to three years if there are no contraindications.

    Atenolol is an additional treatment to standard coronary care unit therapy.

[edit] CONTRAINDICATIONS

  • Second- or third-degree AV block
  • Sinus bradycardia (resting heart rate of 60 beats per minute or less)
  • Patients in cardiogenic shock or decompensated heart failure
  • History of hypersensitivity to Atenolol

[edit] WARNINGS AND PRECAUTIONS

  • Acute exacerbation of coronary artery disease upon cessation of therapy: Severe exacerbation of angina and the occurrence of myocardial infarction and ventricular arrhythmias have been reported in angina patients following the abrupt discontinuation of therapy with beta blockers. Do not abruptly discontinue.
  • Bradycardia, hypotension, worsening heart failure/fluid retention may occur. Reduce the dose as needed.
  • Patients with bronchospastic disease (e.g., chronic bronchitis and emphysema): Avoid β-blockers. However, if deemed necessary (patients who do not respond to, or cannot tolerate, other antihypertensive treatment), use with caution and at lowest effective dose.
  • Diabetes and Hypoglycemia: Beta blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia. Nonselective beta blockers may potentiate insulin-induced hypoglycemia and delay recovery of serum glucose levels. Because of its beta1-selectivity, this is less likely with Atenolol. However, patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents, should be cautioned about these possibilities and Atenolol should be used with caution

[edit] INTERACTIONS

  • Concomitant Use of Verapamil or diltiazem type calcium channel blockers: Bradycardia and heart block can occur and the left ventricular end diastolic pressure can rise when beta-blockers are administered with verapamil or diltiazem. Patients with pre­existing conduction abnormalities or left ventricular dysfunction are particularly susceptible
  • Hypotensive agents (e.g., reserpine, MAO inhibitors, clonidine) may increase the risk of hypotension and/or severe bradycardia.
  • Disopyramide is a Type I antiarrhythmic drug with potent negative inotropic and chronotropic effects. Disopyramide has been associated with severe bradycardia, asystole and heart failure when administered with beta blockers.
  • Amiodarone is an antiarrhythmic agent with negative chronotropic properties that may be additive to those seen with beta blockers.
  • Both digitalis glycosides and beta blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase the risk of bradycardia.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category D (US)
  • Nursing Mothers: Atenolol is excreted in human breast milk at a ratio of 1.5 to 6.8 when compared to the concentration in plasma. Caution should be exercised when Atenolol is administered to a nursing woman. Clinically significant bradycardia has been reported in breast-fed infants. Premature infants, or infants with impaired renal function, may be more likely to develop adverse effects.

[edit] SIDE EFFECTS

Possible adverse effects include: Bradycardia, Dizziness, Drowsiness, Fatigue and Nausea.

[edit] BIBLIOGRAPHY

[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)