Extended release metoprolol succinate: Initiate cautiously in patients with concomitant heart failure. Avoid in patients with decompensated heart failure; electrical cardioversion preferred. Oral immediate release [metoprolol tartrate]: Initiate only in stable patients or hospitalized patients after volume status has been optimized and IV diuretics, vasodilators, and inotropic agents have all been successfully discontinued.
Caution should be used when initiating in patients who required inotropes during their hospital course. Oral extended release [metoprolol succinate]: Oral metoprolol immediate release initiated within the first 24 hours is recommended in all other patients. Secondary prevention off-label use: Supraventricular tachycardia off-label use: Ventricular arrhythmias off-label use: When switching from immediate release metoprolol tartrate to extended release metoprolol succinate , the same total daily dose of metoprolol should be used.
Metoprolol tartrate is typically administered in 2 to 3 divided daily doses and metoprolol succinate is administered once daily.
When switching between oral and intravenous dosage forms, in most cases, equivalent beta-blocking effect is achieved when doses in a 2. IV ratio is used. However, in one bioavailability study including healthy volunteers, a range of Oral: IV conversion ratios was found to be approximately 2: Therefore, patient variability may exist and a specific ratio may not apply to all patients, especially if comorbid conditions are present.
For example, based on a range of 2. Recognizing that patients receiving larger chronic oral doses should not automatically be converted to a large IV dose, consideration should be given to further reducing the initial IV dose and basing subsequent doses on the clinical response Huckleberry Geriatric Refer to adult dosing. In the management of hypertension, consider lower initial doses and titrate to response Aronow Immediate-release tablet metoprolol tartrate: Adjust dose based on patient response; maximum daily dose: Extended-release tablet metoprolol succinate: Adjust dose based on patient response maximum: Renal Impairment No dosage adjustment necessary.
Hepatic Impairment There are no specific dosage adjustments provided in the manufacturer's labeling. Consider initiating with reduced doses and gradual dosage titration due to extensive hepatic metabolism. Crush twelve mg tablets in a mortar and reduce to a fine powder. Add 20 mL of the chosen vehicle and mix to a uniform paste; mix while adding the vehicle in incremental proportions to almost mL; transfer to a calibrated bottle, rinse mortar with vehicle, and add quantity of vehicle sufficient to make mL.
Label "shake well" and "protect from light". Stable for 60 days. Typically administered in 2 to 3 divided doses. Administer with or immediately following food Melander Administer once daily without regard to meals Tangeman ; van den Berg ; Wikstrand May divide tablets in half; do not crush or chew. When administered acutely for cardiac treatment, monitor ECG and blood pressure. Administer by IV bolus. Dietary Considerations Immediate-release tablets should be taken with or immediately following food Melander Do not freeze; protect from light.
Drug Interactions Abiraterone Acetate: Avoid concurrent use of abiraterone with CYP2D6 substrates that have a narrow therapeutic index whenever possible. Consider therapy modification Acetylcholinesterase Inhibitors: May enhance the bradycardic effect of Beta-Blockers.
May enhance the hypotensive effect of Blood Pressure Lowering Agents. Epinephrine used as a local anesthetic for dental procedures will not likely cause clinically relevant problems. Cardioselective beta-blockers and lower doses of epinephrine may confer a more limited risk.
Patients who may require acute subcutaneous epinephrine e. Consider therapy modification Alpha1-Blockers: Beta-Blockers may enhance the orthostatic hypotensive effect of Alpha1-Blockers. The risk associated with ophthalmic products is probably less than systemic products.
May enhance the AV-blocking effect of Beta-Blockers. Sinus node dysfunction may also be enhanced. Beta-Blockers may enhance the rebound hypertensive effect of Alpha2-Agonists.
This effect can occur when the Alpha2-Agonist is abruptly withdrawn. Closely monitor heart rate during treatment with a beta blocker and clonidine. Withdraw beta blockers several days before clonidine withdrawal when possible, and monitor blood pressure closely. Recommendations for other alpha2-agonists are unavailable.
Consider therapy modification Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. Consider therapy modification Aminoquinolines Antimalarial: May decrease the metabolism of Beta-Blockers.
Possibly to the point of cardiac arrest. Amiodarone may increase the serum concentration of Beta-Blockers. May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy Antipsychotic Agents Phenothiazines: May enhance the hypotensive effect of Beta-Blockers.
Beta-Blockers may decrease the metabolism of Antipsychotic Agents Phenothiazines. Antipsychotic Agents Phenothiazines may decrease the metabolism of Beta-Blockers. Consider therapy modification Barbiturates: May decrease the serum concentration of Beta-Blockers. Of particular concern with nonselective beta-blockers or higher doses of the beta1 selective beta-blockers. Monitor therapy Bradycardia-Causing Agents: May enhance the bradycardic effect of other Bradycardia-Causing Agents.
May enhance the bradycardic effect of Bradycardia-Causing Agents. The MHRA acknowledges that no product is completely risk free but takes into account research and evidence to ensure that any risks associated are minimal. The FDA has approved beta blockers for the treatment of cardiac arrhythmias, hypertension, migraines, and others. Prescribers may choose to prescribe beta blockers for other treatments if there is just cause even though it is not approved by the FDA. Drug manufacturers, however, are unable to advertise beta blockers for other purposes that have not been approved by the FDA.
Since the FDA does not regulate the practice of medicine after the drug has been approved, it is legal to prescribe beta blockers for other treatments such as performance anxiety.
Metoprolol tartrate is a generic version of Lopressor, which was licensed and authorised on June 6th to Novartis Pharmaceuticals. Beta blockers can be used to reduce heart rate and minimize tremors, which can enhance performance in sports such as archery. Furthermore, any form of beta blocker is banned within riflery competitions by the National Collegiate Athletic Association.
However, in modern times it is increasingly difficult to detect the presence of beta blockers used for sports doping purposes. The systemic availability and half-life of Lopressor in patients with renal failure do not differ to a clinically significant degree from those in normal subjects. Since the drug is primarily eliminated by hepatic metabolism, hepatic impairment may impact the pharmacokinetics of metoprolol.
The elimination half-life of metoprolol is considerably prolonged, depending on severity up to 7. In controlled, comparative, clinical studies, Lopressor has been shown to be as effective an antihypertensive agent as propranolol, methyldopa, and thiazide-type diuretics, to be equally effective in supine and standing positions. Angina Pectoris In controlled clinical trials, Lopressor, administered two or four times daily, has been shown to be an effective antianginal agent, reducing the number of angina attacks and increasing exercise tolerance.
The dosage used in these studies ranged from to mg daily. A controlled, comparative, clinical trial showed that Lopressor was indistinguishable from propranolol in the treatment of angina pectoris. Patients were randomized and treated as soon as possible after their arrival in the hospital, once their clinical condition had stabilized and their hemodynamic status had been carefully evaluated.
Initial treatment consisted of intravenous followed by oral administration of Lopressor or placebo, given in a coronary care or comparable unit. Significant reductions in the incidence of ventricular fibrillation and in chest pain following initial intravenous therapy were also observed with Lopressor and were independent of the interval between onset of symptoms and initiation of therapy.
In this study, patients treated with metoprolol received the drug both very early intra-venously and during a subsequent 3-month period, while placebo patients received no beta-blocker treatment for this period.
The study thus was able to show a benefit from the overall metoprolol regimen but cannot separate the benefit of very early intravenous treatment from the benefit of later beta-blocker therapy. Nonetheless, because the overall regimen showed a clear beneficial effect on survival without evidence of an early adverse effect on survival, one acceptable dosage regimen is the precise regimen used in the trial. Because the specific benefit of very early treatment remains to be defined however, it is also reasonable to administer the drug orally to patients at a later time as is recommended for certain other beta-blockers.
Indications and Usage for Lopressor Hypertension Lopressor tablets are indicated for the treatment of hypertension. They may be used alone or in combination with other antihypertensive agents. Angina Pectoris Lopressor is indicated in the long-term treatment of angina pectoris. Myocardial Infarction Lopressor tablets are indicated in the treatment of hemodynamically stable patients with definite or suspected acute myocardial infarction to reduce cardiovascular mortality when used alone or in conjunction with intravenous Lopressor.
Hypersensitivity to Lopressor and related derivatives, or to any of the excipients; hypersensitivity to other beta-blockers cross sensitivity between beta-blockers can occur. Severe peripheral arterial circulatory disorders. Warnings Heart Failure Beta-blockers, like Lopressor, can cause depression of myocardial contractility and may precipitate heart failure and cardiogenic shock.
If signs or symptoms of heart failure develop, treat the patient according to recommended guidelines. It may be necessary to lower the dose of Lopressor or to discontinue it.
Ischemic Heart Disease Do not abruptly discontinue Lopressor therapy in patients with coronary artery disease. Severe exacerbation of angina, myocardial infarction and ventricular arrhythmias have been reported in patients with coronary artery disease following the abrupt discontinuation of therapy with beta-blockers. When discontinuing chronically administered Lopressor, particularly in patients with coronary artery disease, the dosage should be gradually reduced over a period of 1 to 2 weeks and the patient should be carefully monitored.
If angina markedly worsens or acute coronary insufficiency develops, Lopressor administration should be reinstated promptly, at least temporarily, and other measures appropriate for the management of unstable angina should be taken.
Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue Lopressor therapy abruptly even in patients treated only for hypertension. Use During Major Surgery Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery; however, the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures.
Bradycardia Bradycardia, including sinus pause, heart block, and cardiac arrest have occurred with the use of Lopressor. Patients with first-degree atrioventricular block, sinus node dysfunction, or conduction disorders may be at increased risk. Monitor heart rate and rhythm in patients receiving Lopressor. If severe bradycardia develops, reduce or stop Lopressor. Because of its relative beta1 selectivity, however, Lopressor may be used in patients with bronchospastic disease who do not respond to, or cannot tolerate, other antihypertensive treatment.
Bronchodilators, including beta2 agonists, should be readily available or administered concomitantly. Diabetes and Hypoglycemia Beta-blockers may mask tachycardia occurring with hypoglycemia, but other manifestations such as dizziness and sweating may not be significantly affected.
Pheochromocytoma If Lopressor is used in the setting of pheochromocytoma, it should be given in combination with an alpha blocker, and only after the alpha blocker has been initiated. Administration of beta- blockers alone in the setting of pheochromocytoma has been associated with a paradoxical increase in blood pressure due to the attenuation of beta-mediated vasodilatation in skeletal muscle. Thyrotoxicosis Lopressor may mask certain clinical signs e. Avoid abrupt withdrawal of beta blockade, which might precipitate a thyroid storm.
Precautions Risk of Anaphylactic Reactions While taking beta-blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic.
Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reaction. Information for Patients Advise patients to take Lopressor regularly and continuously, as directed, with or immediately following meals. If a dose should be missed, the patient should take only the next scheduled dose without doubling it. Patients should not discontinue Lopressor without consulting the physician.
Drug Interactions Catecholamine-depleting drugs:
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