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Toprol-XL (Metoprolol Succinate) - Summary


Boxed Warning section

Following abrupt cessation of therapy with certain beta-blocking agents, exacerbations of angina pectoris and, in some cases, myocardial infarction have occurred. When discontinuing chronically administered TOPROL-XL, particularly in patients with ischemic heart disease, the dosage should be gradually reduced over a period of 1 - 2 weeks and the patient should be carefully monitored. If angina markedly worsens or acute coronary insufficiency develops, TOPROL-XL administration should be reinstated promptly, at least temporarily, and other measures appropriate for the management of unstable angina should be taken. Warn patients against interruption or discontinuation of therapy without the physician’s advice. Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue TOPROL-XL therapy abruptly even in patients treated only for hypertension (5.1).




TOPROL-XL, metoprolol succinate, is a beta1-selective (cardioselective) adrenoceptor blocking agent, for oral administration, available as extended-release tablets. TOPROL-XL has been formulated to provide a controlled and predictable release of metoprolol for once-daily administration. The tablets comprise a multiple unit system containing metoprolol succinate in a multitude of controlled release pellets. Each pellet acts as a separate drug delivery unit and is designed to deliver metoprolol continuously over the dosage interval. The tablets contain 23.75, 47.5, 95 and 190 mg of metoprolol succinate equivalent to 25, 50, 100 and 200 mg of metoprolol tartrate, USP, respectively. Its chemical name is (±)1- (isopropylamino)-3-[p-(2-methoxyethyl) phenoxy]-2-propanol succinate (2:1) (salt).

TOPROL-XL, metoprolol succinate, is a beta1-selective adrenoceptor blocking agent.

TOPROL-XL is indicated for the treatment of:

•Hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions.


•Angina Pectoris.


•Heart Failure - for the treatment of stable, symptomatic (NYHA Class II or III) heart failure of ischemic, hypertensive, or cardiomyopathic origin.



TOPROL-XL is indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure lowers the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including metoprolol.

Control of high blood pressure should be part of comprehensive cardiovascular risk management, including, as appropriate, lipid control, diabetes management, antithrombotic therapy, smoking cessation, exercise, and limited sodium intake. Many patients will require more than 1 drug to achieve blood pressure goals. For specific advice on goals and management, see published guidelines, such as those of the National High Blood Pressure Education Program’s Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC).

Numerous antihypertensive drugs, from a variety of pharmacologic classes and with different mechanisms of action, have been shown in randomized controlled trials to reduce cardiovascular morbidity and mortality, and it can be concluded that it is blood pressure reduction, and not some other pharmacologic property of the drugs, that is largely responsible for those benefits. The largest and most consistent cardiovascular outcome benefit has been a reduction in the risk of stroke, but reductions in myocardial infarction and cardiovascular mortality also have been seen regularly.

Elevated systolic or diastolic pressure causes increased cardiovascular risk, and the absolute risk increase per mmHg is greater at higher blood pressures, so that even modest reductions of severe hypertension can provide substantial benefit. Relative risk reduction from blood pressure reduction is similar across populations with varying absolute risk, so the absolute benefit is greater in patients who are at higher risk independent of their hypertension (for example, patients with diabetes or hyperlipidemia), and such patients would be expected to benefit from more aggressive treatment to a lower blood pressure goal.

Some antihypertensive drugs have smaller blood pressure effects (as monotherapy) in black patients, and many antihypertensive drugs have additional approved indications and effects (eg, on angina, heart failure, or diabetic kidney disease). These considerations may guide selection of therapy.

TOPROL-XL may be administered with other antihypertensive agents.


TOPROL-XL is indicated in the long-term treatment of angina pectoris, to reduce angina attacks and to improve exercise tolerance.


TOPROL-XL is indicated for the treatment of stable, symptomatic (NYHA Class II or III) heart failure of ischemic, hypertensive, or cardiomyopathic origin. It was studied in patients already receiving ACE inhibitors, diuretics, and, in the majority of cases, digitalis. In this population, TOPROL-XL decreased the rate of mortality plus hospitalization, largely through a reduction in cardiovascular mortality and hospitalizations for heart failure.


See all Toprol-XL indications & dosage >>


Published Studies Related to Toprol-XL (Metoprolol)

Effect of fixed dose combinations of metoprolol and amlodipine in essential hypertension: MARS ? A randomized controlled trial. [2011.12]
Abstract Aim. To compare two strengths of a fixed drug combination (FDC) containing metoprolol XL and amlodipine (metoprolol/amlodipine 50/5; and metoprolol/amlodipine 25/2.5) with its components in hypertension...

Endothelial function is unaffected by changing between carvedilol and metoprolol in patients with heart failure-a randomized study. [2011.10.15]
ABSTRACT: BACKGROUND: Carvedilol has been shown to be superior to metoprolol tartrate to improve clinical outcomes in patients with heart failure (HF), yet the mechanisms responsible for these differences remain unclear. We examined if there were differences in endothelial function, insulin stimulated endothelial function, 24 hour ambulatory blood pressure and heart rate during treatment with carvedilol, metoprolol tartrate and metoprolol succinate in patients with HF... CONCLUSION: Endothelial function remained unchanged when switching the beta blocker treatment from carvedilol to either metoprolol tartrate or metoprolol succinate in this study, where blood pressure and heart rate also remained unchanged in patients with mild HF. TRIAL REGISTRATION: Current Controlled Trials NCT00497003.

beta-Blockers in patients with intermittent claudication and arterial hypertension: results from the nebivolol or metoprolol in arterial occlusive disease trial. [2011.08]
The use of beta-receptor blockers in peripheral arterial disease is controversial for their impact on vasomotor tone... In the direct comparison, there was no significant difference between nebivolol and metoprolol.

Differential effects of nebivolol and metoprolol on central aortic pressure and left ventricular wall thickness. [2011.06]
The aim of this study was to investigate the effects of the vasodilating beta-blocker nebivolol and the cardioselective beta-blocker metoprolol succinate on aortic blood pressure and left ventricular wall thickness... This proof-of-principle study provides evidence to suggest that beta-blockers with vasodilating properties may offer advantages over conventional beta-blockers in antihypertensive therapy; however, this remains to be tested in a larger trial.

The effect of nebivolol versus metoprolol succinate extended release on asymmetric dimethylarginine in hypertension. [2011.05]
This study sought to determine if metoprolol succinate ER (MET), and nebivolol (NEB), a beta1-AR with increased bioavailability of nitric oxide (NO), would have differing effects on plasma asymmetric dimethylarginine concentration in hypertensives. It was hypothesized that NEB, a beta1-AR antagonist and beta3-AR agonist with NO-releasing properties, and MET, only a beta1-AR antagonist, would have different effects on plasma asymmetric dimethylarginine (ADMA) concentration...

more studies >>

Clinical Trials Related to Toprol-XL (Metoprolol)

Nebivolol Versus Metoprolol: Comparative Effects on Fatigue and Quality of Life [Completed]
Beta-blockers are prescribed to millions of people for treatment of hypertension. Fatigue is a recognized and common side effect of beta-blockers that can have significant effects on quality of life. Worse, many people taking a beta-blocker for years are not even aware of the reduction of energy with which they are living. A new vasodilating beta-blocker, nebivolol, which is approved by the FDA for treatment of hypertension, appears to be far less associated with fatigue than are most currently available beta-blockers. The purpose of this study is to compare nebivolol with the current best-selling beta-blocker, metoprolol, and determine whether there is a significant difference in side effects including fatigue, reduced exertion tolerance, and reduced quality of life. In this study, 30 subjects will take each of the 2 study drugs for 8 weeks, consisting of 4 weeks at a lower dose, and 4 weeks ata higher dose. All dosages are FDA-approved for treatment of hypertension. Subjects and investigators will not know which drug is being administered until completion of the study. Subjects will undergo a treadmill stress test and will complete fatigue and quality of life questionnaires after each 4 weeks of treatment. An echocardiogram and non-invasive measurement of aortic blood pressure will be performed after 8 weeks on each drug. Also, blood will be drawn and stored for possible measurement of drug levels, after 4 and 8 weeks on each drug. Results on each drug will then be compared. If nebivolol is found to cause significantly less fatigue, it would be of substantial importance to the many millions of people who are on life-long beta-blocker therapy, and are living with reduced energy.

Open-Labeled PK-PD Studies of Metoprolol ER [Not yet recruiting]
Recently, the quality of generic metoprolol extended-release (ER) (Toprol XL, Activas,Wockhardt) products has been called into question with reports of inconsistent effects when switching from the brand name product to a generic formulation. Problems with how the body processes these drugs could have serious and widespread consequences given the high frequency of metoprolol ER use in the management of various cardiovascular disorders, including high blood pressure, coronary heart disease, heart failure, and cardiac arrhythmias. Investigators hypothesize that both product- and subject-specific factors lead to variability in the way the body breaks down the drug (pharmacokinetics) and clinical response to generic versus name brand metoprolol ER formulation. Investigators will study the brand name and generic metoprolol ER formulations in subjects with high blood pressure to compare the pharmacokinetics and cardiovascular responses among equivalent labeled doses of each product. The study objective is to provide information on how the body breaks down generic and brand name metoprolol ER products (pharmacokinetics) and how the body responds to generic and brand name metoprolol ER products (pharmacodynamics) to better understand if generic metoprolol ER products are as good as the brand name product.

Comparative Effects of Nebivolol and Metoprolol on Femal Sexual Function [Recruiting]
Beta-blockers (BB) are an important treatment for high blood pressure and heart disease. However beta-blockers can cause sexual dysfunction (SD) and this common side effect limits successful use of this class of medications. Sexual side effects often result in drug discontinuation, compromising therapy goals. The investigators are conducting the study to determine if nebivolol, a newer beta blocker that is selective for receptors in the heart and causes vasodilation in the body causes fewer sexual side effects, or even improves sexual function, compared with metoprolol succinate.

Factorial Study of Metoprolol Succinate TOPROL-XL (324A) [Completed]
The purpose of this research study is to determine if treatment with the combination of metoprolol succinate and hydrochlorothiazide is more effective at lowering blood pressure than treatment with either of the two drugs alone. The study will also determine which combined doses of metoprolol succinate and hydrochlorothiazide are most effective at lowering blood pressure (without unacceptable side effects), and whether it is possible to combine both drugs in a single tablet to simplify blood pressure treatment.

Bioequivalence Study of Metoprolol Succinate ER Tablets, 200 mg Under Fasting Conditions [Completed]

more trials >>

Reports of Suspected Toprol-XL (Metoprolol) Side Effects

Malaise (317)Drug Dose Omission (308)Hypertension (262)Myocardial Infarction (161)Drug Ineffective (139)Cerebrovascular Accident (138)Headache (121)Cardiac Disorder (113)Fall (109)Dizziness (109)more >>


Based on a total of 2 ratings/reviews, Toprol-XL has an overall score of 8. The effectiveness score is 7 and the side effect score is 10. The scores are on ten point scale: 10 - best, 1 - worst.

Toprol-XL review by 47 year old female patient

Overall rating:  
Effectiveness:   Considerably Effective
Side effects:   No Side Effects
Treatment Info
Condition / reason:   High Blood pressure
Dosage & duration:   50 mg. taken 1 daily for the period of 2 years
Other conditions:   breast cancer
Other drugs taken:   Dexameth 4mg., Vicodin 500mg., Compazine 10mg. Chemotherapy- Taxotere/Cytoxan 4tx., Neulasta
Reported Results
Benefits:   Vicodin 500mg- reduced bone pain caused by Neulasta shot. Dexameth 4mg.- reduced drug reactions caused by chemotherapy. Compazine 10mg.- reduced nausea caused by chemotherapy. Taxotere/Cytoxan- going thru tx. at this time. hope to be cancer free! Neulasta shot- increased whit blood count so we could continue with chemotherapy.
Side effects:   Vicodin 500mg.- some drowsiness Dexameth 4mg.- hot flashes, flushed face,insomnia Compazine 10mg.- none Taxotere- hairloss, very dry skin, some gum bleeding, tiredness, metalic taste in mouth, short term memory loss, confusion, liver toxin level increasing. Cytoxan- ? since I receive the Taxotere at the same time I'm not sure which side effects are which. Neulasta shot- extreme bone pain
Comments:   Vicodin 500mg- take as needed for bone pain caused by Neluasta shot. Dexameth 4mg.- Take 2 tablets night before chemo tx., 2 tablets morning of tx, tablets evening of tx., two tablets am after tx. Compazine 10mg.- take one tablet every six hours as needed for nasuea from chemo. Taxotere/Cytoxan- total of four treatments for IDC breast cancer, Grade 1, Stage 2, 0ne lymph node involved. Prior treatment completed- Dec.08 lumpectomy and sentiel node removal, Jan 09 full mastectomy with lypmh node dissection (removed 18), started chemotherapy Feb 22 09 once every three weeks, just had third tx on Mar 31 09. Neulasta shot- total of four treatments given 48 hours after chemotherapy tx. Shot is given in the stomach area to reduce the side effects.


Toprol-XL review by 45 year old female patient

Overall rating:  
Effectiveness:   Moderately Effective
Side effects:   No Side Effects
Treatment Info
Condition / reason:   high blood pressure and
Dosage & duration:   25mg taken once daily for the period of one year to date
Other conditions:   none
Other drugs taken:   tylenol and advil; ketorolac: frova
Reported Results
Benefits:   It seems to keep my blood pressure and headaches in check, especially during hormonal changes right before my period begins. I am also sleeping better at night (falling asleep and staying asleep; able to get back to sleep during the night), whereas before I was getting only a couple of hours of sleep a night.
Side effects:   none so far
Comments:   I had been dealing with more frequent "migraine" headaches (headaches unresponsive to OTC pain relievers)and began to notice a pattern that was related to my menstrual cycle. During treatment for the headaches with frova and ketorolac I had an episode where I had sudden and severe pain in my head and felt like my head was going to explode, which sent me to the emergency room. The cause was never really determined but in the process it was noticed that my blood pressure was elevated and remained elevated during following doctor visits. Since being on toprol, the headaches and blood pressure have remained managable throughout monthly hormonal changes.

See all Toprol-XL reviews / ratings >>

Page last updated: 2011-12-09

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