Documenti di Didattica
Documenti di Professioni
Documenti di Cultura
Adverse drug reactions (ADRs) associated with the use of beta blockers include: nausea, diarrhoea, bronchospasm, dyspnea, cold extremities, exacerbation of Raynaud's syndrome, bradycardia, hypotension, heart failure, heart block, fatigue, dizziness, abnormal vision, decreased concentration, hallucinations, insomnia, nightmares, clinical depression, sexual dysfunction, erectile dysfunction and/or alteration of glucose and lipid metabolism. Mixed 1/-antagonist therapy is also commonly associated with orthostatic hypotension. Carvedilol therapy is commonly associated with edema. Clinical guidelines in Great Britain, but not in the United States, call for avoiding diuretics and beta-blockers as first-line treatment of hypertension due to the risk of diabetes. Beta blockers must not be used in the treatment of cocaine, amphetamine, or other alpha adrenergic stimulant overdose. The blockade of only beta receptors increases hypertension, reduces coronary blood flow, left ventricular function, and cardiac output and tissue perfusion by means of leaving the alpha adrenergic system stimulation unopposed. The appropriate antihypertensive drugs to administer during hypertensive crisis resulting from stimulant abuse are vasodilators like nitroglycerin, diuretics like furosemide and alpha blockers like phentolamine.
Apa itu beta blokers
Beta blockers (sometimes written as -blocker) is a class of drugs used for various indications, but particularly for the management of cardiac arrhythmias, cardioprotection after myocardial infarction (heart attack), and hypertension. As beta adrenergic receptor antagonists, they diminish the effects of epinephrine (adrenaline) and other stress hormones. Invented by Sir James W. Black in the late 1950s, Propranolol was the first clinically useful beta blocker; it revolutionized the medical management of angina pectoris and is considered to be one of the most important contributions to clinical medicine and pharmacology of the 20th century. Beta blockers may also be referred to as beta-adrenergic blocking agents, beta-adrenergic antagonists, or beta antagonists. Examples of beta-blockers include: acebutolol, betaxolol, bisoprolol, esmolol, propranolol, atenolol, labetalol, carvedilol, metoprolol, and nebivolol.
-Receptor antagonism
Stimulation of 1 receptors by epinephrine induces a positive chronotropic and inotropic effect on the heart and increases cardiac conduction velocity and automaticity. Stimulation of 1 receptors on the kidney causes renin release. Stimulation of 2 receptors induces smooth muscle relaxation, induces tremor in skeletal muscle, and increases glycogenolysis in the liver and skeletal muscle. Stimulation of 3 receptors induces lipolysis. Beta blockers inhibit these normal epinephrine-mediated sympathetic actions, but have minimal effect on resting subjects. That is, they reduce the effect of excitement/physical exertion on heart rate and force of contraction, dilation of blood vessels and opening of bronchi, and also reduce tremor and breakdown of glycogen. It is therefore expected that non-selective beta blockers have an antihypertensive effect. The antihypertensive mechanism appears to involve reduction in cardiac output (due to negative chronotropic and inotropic effects), reduction in renin release from the kidneys, and a central nervous system effect to reduce sympathetic activity (for those -blockers that do cross the blood-brain barrier, e.g. Propranolol). Antianginal effects result from negative chronotropic and inotropic effects, which decrease cardiac workload and oxygen demand. Negative chronotropic properties of beta blockers allow the lifesaving property of heart rate control. Beta blockers are readily titrated to optimal rate control in many pathologic states. The antiarrhythmic effects of beta blockers arise from sympathetic nervous system blockade resulting in depression of sinus node function and atrioventricular node conduction, and prolonged atrial refractory periods. Sotalol, in particular, has additional antiarrhythmic properties and prolongs action potential duration through potassium channel blockade. Blockade of the sympathetic nervous system on renin release leads to reduced aldosterone via the renin angiotensin aldosterone system with a resultant decrease in blood pressure due to decreased sodium and water retention.
Agents with ISA are not used in post-myocardial infarction as they have not been demonstrated to be beneficial. They may also be less effective than other beta blockers in the management of angina and tachyarrhythmia.
1-Receptor antagonism
Some beta blockers (e.g. labetalol and carvedilol) exhibit mixed antagonism of both - and 1adrenergic receptors, which provides additional arteriolar vasodilating action.
Other effects
Beta blockers decrease nocturnal melatonin release, perhaps partly accounting for sleep disturbance caused by some agents. Beta blockers protect against social anxiety: "Improvement of physical symptoms has been demonstrated with beta-blockers such as propranolol; however, these effects are limited to the social anxiety experienced in performance situations." (example: an inexperienced symphony soloist) Beta blockers can impair the relaxation of bronchial muscle (mediated by beta-2) and so should be avoided by asthmatics. They can also be used to treat glaucoma because they decrease intraocular pressure by lowering aqueous humor secretion.
Digunakan untuk
Large differences exist in the pharmacology of agents within the class, thus not all beta blockers are used for all indications listed below. Indications for beta blockers include:
Hypertension Angina Mitral valve prolapse Cardiac arrhythmia Atrial fibrillation Congestive heart failure Myocardial infarction Glaucoma Migraine prophylaxis Symptomatic control (tachycardia, tremor) in anxiety and hyperthyroidism Essential tremor Phaeochromocytoma, in conjunction with -blocker
Hypertrophic obstructive cardiomyopathy Acute dissecting aortic aneurysm Marfan syndrome (treatment with propranolol slows progression of aortic dilation and its complications) Prevention of variceal bleeding in portal hypertension Possible mitigation of hyperhidrosis Social anxiety disorder and other anxiety disorders
Officially, beta blockers are not approved for anxiolytic use by the U.S. Food and Drug Administration. Since they lower heart rate and reduce tremor, beta blockers have been used by some Olympic marksmen to enhance performance, though beta blockers are banned by the International Olympic Committee (IOC). Although they have no recognisable benefit to most sports, it is acknowledged that they are beneficial to sports such as archery and shooting. A recent, high-profile transgression took place in the 2008 Summer Olympics, where 50 metre pistol silver medallist and 10 metre air pistol bronze medallist Kim Jong-su tested positive for propranolol and was stripped of his medal.
Preventing PTSD
Post Traumatic Stress Disorder is theorized to be the result of neurological patterns caused by adrenaline and fear in the brain. By administering beta blockers immediately following a traumatic event, as well as over the next couple weeks, the formation of PTSD has been reduced in clinical studies.
Obat beta blokers
Non-selective agents
Alprenolol Bucindolol Carteolol Carvedilol (has additional -blocking activity) Labetalol (has additional -blocking activity) Nadolol Penbutolol (has intrinsic sympathomimetic activity) Pindolol (has intrinsic sympathomimetic activity) Propranolol Timolol
1-Selective agents
Acebutolol (has intrinsic sympathomimetic activity) Atenolol Betaxolol Bisoprolol Celiprolol Esmolol Metoprolol Nebivolol
2-Selective agents
Butaxamine (weak -adrenergic agonist activity) - No common clinical applications, but used in experiments. ICI-118 Highly selective 2-adrenergic receptor antagonist - No known clinical applications, but used in experiments due to its strong receptor specificity.
Comparative Information
Pharmacological differences
Agents with intrinsic sympathomimetic action (ISA) o Acebutolol, carteolol, celiprolol, mepindolol, oxprenolol, pindolol o Agents with greater aqueous solubility , celiprolol, nadolol, sotalol Agents with membrane stabilizing effect Acebutolol, betaxolol, pindolol, propranolol Agents with antioxidant effect Carvedilol Nebivolol
Indication differences
Agents specifically indicated for cardiac arrhythmia o Esmolol, sotalol, landiolol o Agents specifically indicated for congestive heart failure Bisoprolol, carvedilol, sustained-release metoprolol, nebivolol Agents specifically indicated for glaucoma Betaxolol, carteolol, levobunolol, metipranolol, timolol Agents specifically indicated for myocardial infarction Atenolol, metoprolol, propranolol Agents specifically indicated for migraine prophylaxis Timolol, propranolol
Propranolol is the only agent indicated for control of tremor, portal hypertension and esophageal variceal bleeding, and used in conjunction with -blocker therapy in phaeochromocytoma.