Toprol-XL is used alone or together with other medicines to treat high blood pressure (hypertension). High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. A lower blood pressure can reduce the risk of strokes and heart attacks.
Toprol-XL is also used to treat severe chest pain (angina) and lowers the risk of repeated heart attacks. It is given to people who have already had a heart attack. In addition, Toprol-XL is used to treat patients with heart failure.
Toprol-XL is a beta-blocker. It works by affecting the response to nerve impulses in certain parts of the body, like the heart. As a result, the heart beats slower and decreases the blood pressure. When the blood pressure is lowered, the amount of blood and oxygen is increased to the heart.
Toprol-XL is available only with your doctor's prescription.
Toprol-XL indications
An indication is a term used for the list of condition or symptom or illness for which the medicine is prescribed or used by the patient. For example, acetaminophen or paracetamol is used for fever by the patient, or the doctor prescribes it for a headache or body pains. Now fever, headache and body pains are the indications of paracetamol. A patient should be aware of the indications of medications used for common conditions because they can be taken over the counter in the pharmacy meaning without prescription by the Physician.
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Hypertension
Toprol-XL tartrate tablets, USP are indicated for the treatment of hypertension. They may be used alone or in combination with other antihypertensive agents.
Angina Pectoris
Toprol-XL tartrate tablets, USP are indicated in the long-term treatment of angina pectoris.
Myocardial Infarction
Toprol-XL tartrate tablets, USP 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 Toprol-XL.
Oral Toprol-XL tartrate tablets, USP therapy can be initiated after intravenous Toprol-XL therapy or, alternatively, oral treatment can begin within 3 to 10 days of the acute event.
How should I use Toprol-XL?
Use Toprol-XL tartrate as directed by your doctor. Check the label on the medicine for exact dosing instructions.
Toprol-XL tartrate is usually given as an injection at your doctor's office, hospital, or clinic. If you will be using Toprol-XL tartrate at home, a health care provider will teach you how to use it. Be sure you understand how to use Toprol-XL tartrate. Follow the procedures you are taught when you use a dose. Contact your health care provider if you have any questions.
Do not use Toprol-XL tartrate if it contains particles, is cloudy or discolored, or if the vial is cracked or damaged.
Keep this product, as well as syringes and needles, out of the reach of children and pets. Do not reuse needles, syringes, or other materials. Ask your health care provider how to dispose of these materials after use. Follow all local rules for disposal.
If you miss a dose of Toprol-XL tartrate, use it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not use 2 doses at once.
Ask your health care provider any questions you may have about how to use Toprol-XL tartrate.
Uses of Toprol-XL in details
There are specific as well as general uses of a drug or medicine. A medicine can be used to prevent a disease, treat a disease over a period or cure a disease. It can also be used to treat the particular symptom of the disease. The drug use depends on the form the patient takes it. It may be more useful in injection form or sometimes in tablet form. The drug can be used for a single troubling symptom or a life-threatening condition. While some medications can be stopped after few days, some drugs need to be continued for prolonged period to get the benefit from it.
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Use: Labeled Indications
Angina: Long-term treatment of angina pectoris.
Heart failure with reduced ejection fraction (ER oral formulation): Treatment of stable, symptomatic (NYHA class II or III) heart failure of ischemic, hypertensive, or cardiomyopathic origin to reduce the rate of mortality plus hospitalization in patients already receiving angiotensin-converting enzyme inhibitors, diuretics, and/or digoxin.
Hypertension: Management of hypertension. Note: Beta-blockers are not recommended as first-line therapy (ACC/AHA [Whelton 2017]).
Myocardial infarction: Treatment of hemodynamically stable acute myocardial infarction to reduce cardiovascular mortality (injection to be used in combination with Toprol-XL oral maintenance therapy).
Off Label Uses
Atrial fibrillation/flutter
Based on the 2014 American Heart Association/American College of Cardiology/Heart Rhythm Society (AHA/ACC/HRS) guideline for the management of patients with atrial fibrillation (AF), the use of beta-blockers, including Toprol-XL, for ventricular rate control in patients with paroxysmal, persistent, or permanent AF is effective and recommended.
Atrial fibrillation prevention after cardiac surgery
Based on the American College of Cardiology Foundation/American Heart Association (ACCF/AHA) guideline for coronary artery bypass graft surgery, beta-blockers are recommended to help prevent postoperative atrial fibrillation.
Hypertrophic cardiomyopathy
Based on the American College of Cardiology Foundation/American Heart Association (ACCF/AHA) guideline for the diagnosis and treatment of hypertrophic cardiomyopathy, a beta blocker (eg, Toprol-XL) is an effective and recommended agent for the treatment of symptoms (eg, angina, dyspnea) in patients with obstructive or nonobstructive hypertrophic cardiomyopathy.
Marfan syndrome with aortic aneurysm
Based on the American College of Cardiology Foundation/American Heart Association/American Association for Thoracic Surgery (ACCF/AHA/AATS) guideline for the diagnosis and management of patients with thoracic aortic disease, a beta blocker (eg, Toprol-XL) is an effective and recommended agent to reduce the rate of aortic dilatation in patients with Marfan syndrome and aortic aneurysm, unless a contraindication exists.
Migraine prophylaxis
Data from small, randomized, active-controlled trials support the use of Toprol-XL for prevention of migraines.
Based on evidence-based guidelines for pharmacologic treatment for episodic migraine prevention in adults from the American Academy of Neurology and the American Headache Society, Toprol-XL is effective for migraine prevention in adults.
Based on the American College of Cardiology/American Heart Association/Heart Rhythm Society (ACC/AHA/HRS) guidelines for the management of adult patients with supraventricular tachycardia, the use of an oral or intravenous beta-blocker, including Toprol-XL, is effective and recommended for a variety of symptomatic supraventricular tachycardias (atrioventricular nodal reentrant tachycardia [AVNRT], atrioventricular reentrant tachycardia [AVRT], focal atrial tachycardia [AT], and multifocal atrial tachycardia [MAT]). In patients without pre-excitation, intravenous Toprol-XL is recommended for acute treatment in hemodynamically stable patients and oral Toprol-XL is recommended for ongoing management of symptomatic supraventricular tachycardias in patients who are not candidates for, or prefer not to undergo, catheter ablation.
Intravenous or oral Toprol-XL may be useful for rate control in the acute treatment or ongoing management of hemodynamically stable patients with atrial flutter.
Thyrotoxicosis
Based on the American Thyroid Association guidelines for diagnosis and management of hyperthyroidism and other causes of thyrotoxicosis, beta-blockers, including Toprol-XL, are effective and recommended in the treatment of symptomatic thyrotoxicosis. Beta-blockers should also be considered in asymptomatic patients who are at increased risk of complications due to worsening hyperthyroidism.
Ventricular arrhythmias
Based on the American Heart Association/American College of Cardiology/Heart Rhythm Society (AHA/ACC/HRS) guideline for management of patients with ventricular arrhythmias and prevention of sudden cardiac death, beta-blockers are effective for control of ventricular arrhythmias and ventricular premature beats.
Toprol-XL description
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Toprol-XL is a cardioselective β1-adrenergic blocking agent used for acute myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension. It may also be used for supraventricular and tachyarrhythmias and prophylaxis for migraine headaches. Toprol-XL is structurally similar to bisoprolol, acebutolol and atenolol in that it has two substituents in the para position of the benzene ring. The β1-selectivity of these agents is thought to be due in part to the large substituents in the para position. At low doses, Toprol-XL selectively blocks cardiac β1-adrenergic receptors with little activity against β2-adrenergic receptors of the lungs and vascular smooth muscle. Receptor selectivity decreases with higher doses. Unlike propranolol and pindolol, Toprol-XL does not exhibit membrane-stabilizing or intrinsic sympathomimetic activity. Membrane-stabilizing effects are only observed at doses much higher than those needed for β-adrenergic blocking activity. Toprol-XL possesses a single chiral centre and is administered as a racemic mixture.
Toprol-XL dosage
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Toprol-XL Dosage
Generic name: Toprol-XL
Dosage form: tablet, extended release
The information at Drugs.com is not a substitute for medical advice. Always consult your doctor or pharmacist.
TOPROL-XL is an extended-release tablet intended for once daily administration. For treatment of hypertension and angina, when switching from immediate-release Toprol-XL to TOPROL-XL, use the same total daily dose of TOPROL-XL. Individualize the dosage of TOPROL-XL. Titration may be needed in some patients.
TOPROL-XL tablets are scored and can be divided; however, do not crush or chew the whole or half tablet.
Hypertension
Adults: The usual initial dosage is 25 to 100 mg daily in a single dose. The dosage may be increased at weekly (or longer) intervals until optimum blood pressure reduction is achieved. In general, the maximum effect of any given dosage level will be apparent after 1 week of therapy. Dosages above 400 mg per day have not been studied.
Pediatric Hypertensive Patients ≥ 6 Years of age: A pediatric clinical hypertension study in patients 6 to 16 years of age did not meet its primary endpoint (dose response for reduction in SBP); however, some other endpoints demonstrated effectiveness. If selected for treatment, the recommended starting dose of TOPROL-XL is 1 mg/kg once daily, but the maximum initial dose should not exceed 50 mg once daily. Dosage should be adjusted according to blood pressure response. Doses above 2 mg/kg (or in excess of 200 mg) once daily have not been studied in pediatric patients.
TOPROL-XL is not recommended in pediatric patients < 6 years of age.
Angina Pectoris
Individualize the dosage of TOPROL-XL. The usual initial dosage is 100 mg daily, given in a single dose. Gradually increase the dosage at weekly intervals until optimum clinical response has been obtained or there is a pronounced slowing of the heart rate. Dosages above 400 mg per day have not been studied. If treatment is to be discontinued, reduce the dosage gradually over a period of 1 - 2 weeks.
Heart Failure
Dosage must be individualized and closely monitored during up-titration. Prior to initiation of TOPROL-XL, stabilize the dose of other heart failure drug therapy. The recommended starting dose of TOPROL-XL is 25 mg once daily for two weeks in patients with NYHA Class II heart failure and 12.5 mg once daily in patients with more severe heart failure. Double the dose every two weeks to the highest dosage level tolerated by the patient or up to 200 mg of TOPROL-XL. Initial difficulty with titration should not preclude later attempts to introduce TOPROL-XL. If patients experience symptomatic bradycardia, reduce the dose of TOPROL-XL. If transient worsening of heart failure occurs, consider treating with increased doses of diuretics, lowering the dose of TOPROL-XL or temporarily discontinuing it. The dose of TOPROL-XL should not be increased until symptoms of worsening heart failure have been stabilized.
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Toprol
Toprol-XL extended-release tablets
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Toprol-XL (Advanced Reading)
Other brands: Toprol-XL Tartrate, Toprol-XL ER, Lopressor
Catecholamine depleting drugs (e.g., reserpine, monoamine oxidase (MAO) inhibitors) may have an additive effect when given with beta-blocking agents. Observe patients treated with TOPROL-XL plus a catecholamine depletor for evidence of hypotension or marked bradycardia, which may produce vertigo, syncope, or postural hypotension.
CYP2D6 Inhibitors
Drugs that inhibit CYP2D6 such as quinidine, fluoxetine, paroxetine, and propafenone are likely to increase Toprol-XL concentration. In healthy subjects with CYP2D6 extensive metabolizer phenotype, coadministration of quinidine 100 mg and immediate-release Toprol-XL 200 mg tripled the concentration of S-Toprol-XL and doubled the Toprol-XL elimination half-life. In four patients with cardiovascular disease, coadministration of propafenone 150 mg t.i.d. with immediate-release Toprol-XL 50 mg t.i.d. resulted in two- to five-fold increases in the steady-state concentration of Toprol-XL. These increases in plasma concentration would decrease the cardioselectivity of Toprol-XL.
Digitalis, Clonidine, And Calcium Channel Blockers
Digitalis glycosides, clonidine, diltiazem and verapamil slow atrioventricular conduction and decrease heart rate. Concomitant use with beta blockers can increase the risk of bradycardia.
If clonidine and a beta blocker, such as Toprol-XL are coadministered, withdraw the beta-blocker several days before the gradual withdrawal of clonidine because beta-blockers may exacerbate the rebound hypertension that can follow the withdrawal of clonidine. If replacing clonidine by betablocker therapy, delay the introduction of beta-blockers for several days after clonidine administration has stopped.
The following adverse reactions are described elsewhere in labeling:
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Worsening angina or myocardial infarction.
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Worsening heart failure.
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Worsening AV block.
Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The adverse reaction information from clinical trials does, however, provide a basis for identifying the adverse events that appear to be related to drug use and for approximating rates.
Hypertension and Angina: Most adverse reactions have been mild and transient. The most common (>2%) adverse reactions are tiredness, dizziness, depression, diarrhea, shortness of breath, bradycardia, and rash.
Heart Failure: In the MERIT-HF study comparing Toprol-XL in daily doses up to 200 mg (mean dose 159 mg once-daily; n=1990) to placebo (n=2001), 10.3% of Toprol-XL patients discontinued for adverse events vs. 12.2% of placebo patients.
The table below lists adverse reactions in the MERIT-HF study that occurred at an incidence of ≥ 1% in the Toprol-XL group and greater than placebo by more than 0.5%, regardless of the assessment of causality.
Adverse Reactions Occurring in the MERIT-HF Study at an Incidence ≥ 1% in the Toprol-XL Group and Greater Than Placebo by More Than 0.5%
Toprol-XL
n = 1990 % of patients
Placebo
n = 2001 % of patients
Dizziness/vertigo
1.8
1
Bradycardia
1.5
0.4
Post-operative Adverse Events: In a randomized, double-blind, placebo-controlled trial of 8351 patients with or at risk for atherosclerotic disease undergoing non-vascular surgery and who were not taking beta–blocker therapy, Toprol-XL 100 mg was started 2 to 4 hours prior to surgery then continued for 30 days at 200 mg per day. Toprol-XL use was associated with a higher incidence of bradycardia (6.6% vs. 2.4%; HR, 2.74; 95% CI 2.19, 3.43), hypotension (15% vs. 9.7%; HR 1.55; 95% CI 1.37, 1.74), stroke (1% vs. 0.5%; HR 2.17; 95% CI 1.26, 3.74) and death (3.1% vs. 2.3%; HR 1.33; 95% CI 1.03, 1.74) compared to placebo.
Post-Marketing Experience
The following adverse reactions have been identified during post-approval use of extended-release Toprol-XL or immediate-release Toprol-XL. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Cardiovascular: Cold extremities, arterial insufficiency (usually of the Raynaud type), palpitations, peripheral edema, syncope, chest pain and hypotension.
Potential Adverse Reactions: In addition, there are adverse reactions not listed above that have been reported with other beta-adrenergic blocking agents and should be considered potential adverse reactions to Toprol-XL.
Central Nervous System: Reversible mental depression progressing to catatonia; an acute reversible syndrome characterized by disorientation for time and place, short-term memory loss, emotional lability, clouded sensorium, and decreased performance on neuropsychometrics.
You should not use this medication if you are allergic to Toprol-XL, or if you have a serious heart problem such as heart block, sick sinus syndrome, or slow heart rate.
Before taking Toprol-XL, tell your doctor if you have congestive heart failure, low blood pressure, circulation problems, pheochromocytoma, asthma or other breathing problems, diabetes, depression, liver or kidney disease, a thyroid disorder, or severe allergies.
Toprol-XL may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.
Drinking alcohol can increase certain side effects of Toprol-XL.
Do not stop taking Toprol-XL without first talking to your doctor. Stopping suddenly may make your condition worse.
If you need surgery, tell the surgeon ahead of time that you are using Toprol-XL.
Toprol-XL is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.
If you are being treated for high blood pressure, keep using this medication even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.
DailyMed. "METOPROLOL FUMARATE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
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