Toprol-xl

— THERAPEUTIC CATEGORIES —
  • Angina
  • CHF and arrhythmias
  • Hypertension
PAGE CONTENTS
  • Jump to Section
  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Toprol-xl Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Metoprolol succinate 25mg, 50mg, 100mg, 200mg; scored ext-rel tabs.

    Pharmacological Class

    Beta-blocker.

    How Supplied

    Tabs—100, 1000

    How Supplied

    Toprol-XL Tablets are supplied in 100- and 1000-count bottles in the following strengths:

    • 25 mg: white, biconvex, film-coated, oval, scored tablets engraved with “A/β”

    • 50 mg: white, biconvex, film-coated, round, scored tablets engraved with “A/mo”

    • 100 mg: white, biconvex, film-coated, round, scored tablets engraved with “A/ms”

    • 200 mg: white, biconvex, film-coated, oval, scored tablets engraved with “A/mY”

    Storage

    • Store at 25°C (77°F). Excursions permitted to 15-30°C (59-86°F).

    Manufacturer

    Melinta Therapeutics

    Generic Availability

    YES

    Mechanism of Action

    Metoprolol is a β1-selective (cardioselective) adrenergic receptor blocking agent that slows the sinus rate and decreases AV nodal conduction. The β-blocking activity of metoprolol has been shown by reduction in heart rate and cardiac output at rest and upon exercise, reduction of systolic blood pressure upon exercise, inhibition of isoproterenol-induced tachycardia, and reduction of reflex orthostatic tachycardia.

    Toprol-xl Indications

    Indications

    Angina pectoris.

    Toprol-xl Dosage and Administration

    Adult

    Initially 100mg once daily. May increase at 1-week intervals; max 400mg/day.

    Children

    Not established.

    Toprol-xl Contraindications

    Contraindications

    Severe bradycardia. 2nd- or 3rd-degree heart block. Cardiogenic shock. Decompensated heart failure. Sick sinus syndrome (unless paced).

    Toprol-xl Boxed Warnings

    Not Applicable

    Toprol-xl Warnings/Precautions

    Warnings/Precautions

    Mild or compensated heart failure. Ischemic heart or peripheral vascular disease. 1st-degree AV block. Sinus node dysfunction. Conduction disorders (eg, Wolff-Parkinson-White). Monitor HR during therapy. Bronchospastic disease. Pheochromocytoma. Surgery. Diabetes. May mask signs and increase risk for hypoglycemia. Hyperthyroidism. Avoid abrupt cessation. Hepatic impairment. Elderly. Neonates. Pregnancy. Nursing mothers: monitor infants.

    Warnings/Precautions

    Abrupt Cessation of Therapy

    • Avoid abruptly discontinuing Toprol-XL in patients treated only for hypertension.

    • When discontinuing chronically administered Toprol-XL especially in patients with ischemic heart disease, gradually reduce the dose of Toprol-XL over a period of 1 to 2 weeks and monitor the patient.

    • Immediately reinstate Toprol-XL if angina worsens or acute coronary ischemia develops, and appropriately manage unstable angina. Advise patients not to interrupt therapy without consulting a physician.

    Heart Failure 

    • While up-titration, worsening cardiac failure may occur. If these symptoms occur, then increase diuretics and restore clinical stability prior to advancing the dose of Toprol-XL.

    • Consider lowering the dose of Toprol-XL or temporarily discontinuing it.

    Bronchospastic Disease 

    • In general, do not give beta-blockers to patients with bronchospastic disease.

    • Toprol-XL may be used in patients with bronchospastic disease who do not respond to, or cannot tolerate, other antihypertensive treatment. Use the lowest possible dose of Toprol-XL.

    • Have bronchodilators, including beta2-agonists, readily available or administered concomitantly.

    Bradycardia

    • Bradycardia, including sinus pause, heart block, and cardiac arrest have occurred with the use of Toprol-XL. 

    • Increased risk for bradycardia in patients with first-degree AV block, sinus node dysfunction, conduction disorders (including Wolff-Parkinson-White) or on concomitant drugs.

    • Monitor heart rate. Discontinue or reduce dose of Toprol-XL if severe bradycardia occurs.

    Pheochromocytoma

    • Administer with an alpha-blocker and only after the alpha-blocker has been initiated if Toprol-XL is used in the setting of pheochromocytoma.

    • Administration of beta-blockers alone in the setting of pheochromocytoma may cause a paradoxical increase in BP.

    Major Surgery

    • Avoid initiating a high-dose regimen of metoprolol extended-release in patients undergoing non-cardiac surgery, since such use in patients with cardiovascular risk factors has been associated with bradycardia, hypotension, stroke, and death. 

    • Do not routinely withdraw chronically administered beta-blocking therapy prior to major surgery.

    Hypoglycemia

    • May prevent early warning signs of hypoglycemia (eg, tachycardia) and increased risk for severe or prolonged hypoglycemia especially in patients with diabetes mellitus or children who are fasting.

    • Seek emergency treatment if severe hypoglycemia occurs.

    Thyrotoxicosis

    • May mask certain clinical signs of hyperthyroidism, (eg, tachycardia). Abrupt withdrawal may precipitate a thyroid storm.

    Peripheral Vascular Disease 

    • May worsen symptoms of arterial insufficiency in patients with peripheral vascular disease.

    Anaphylactic Reaction 

    • While taking beta-blockers, patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated challenge and may be unresponsive to the usual doses of epinephrine used to treat an allergic reaction. 

    Pregnancy Considerations

    Risk Summary

    • Untreated hypertension and heart failure during pregnancy can lead to adverse outcomes for the mother and the fetus.

    • Available data from published observational studies have not demonstrated a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes with metoprolol use during pregnancy.

    Clinical Consideration

    • Fetal/Neonatal adverse reactions: Metoprolol crosses the placenta. Neonates born to mothers who are receiving metoprolol during pregnancy, may be at risk for hypotension, hypoglycemia, bradycardia, and respiratory depression. Observe neonates and manage accordingly.

    Nursing Mother Considerations

    Risk Summary

    • Limited available data from published literature report that metoprolol is present in human milk.

    • No adverse reactions of metoprolol on the breastfed infant have been identified. There is no information regarding the effects of metoprolol on milk production.  

    Clinical Consideration

    • Monitor the breastfed infant for bradycardia and other symptoms of beta-blockade such as listlessness. 

    Pediatric Considerations

    • Safety and effectiveness of ToproL-XL have not been established in patients < 6 years of age. 

    Geriatric Considerations

    • There were no notable differences in efficacy or the rate of adverse reactions between older and younger patients. 

    • In general, use a low initial starting dose in elderly patients given their greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.  

    Hepatic Impairment Considerations

    • No studies have been performed with Toprol-XL in patients with hepatic impairment.

    • Poor hepatic function is most likely to increase blood levels of metoprolol. In patients with impaired hepatic function, initiate Toprol-XL at doses lower than recommended and gradually increase the dose.

    Other Considerations for Specific Populations

    Females and Males of Reproductive Potential

    • Risk Summary: Beta-blockers (including metoprolol) may cause erectile dysfunction and inhibit sperm motility.

    Toprol-xl Pharmacokinetics

    Absorption

    • Average bioavailability at steady-state: 77%.

    Distribution

    • Plasma protein bound: ~12%.

    Metabolism

    • Hepatic (CYP2D6).

    Elimination

    • Renal. Half-life: 3–7hrs.

    Toprol-xl Interactions

    Interactions

    May potentiate hypotension or marked bradycardia with catecholamine depleting drugs (eg, reserpine, MAOIs). Potentiated by strong CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone); monitor if unavoidable. Increased risk of bradycardia with glycosides, clonidine, diltiazem, verapamil. May block epinephrine.

    Toprol-xl Adverse Reactions

    Adverse Reactions

    Fatigue, dizziness, depression, diarrhea, dyspnea, bradycardia, rash; heart block, MI, angina.

    Toprol-xl Clinical Trials

    Clinical Trials

    Angina Pectoris

    • Controlled clinical studies have shown that the immediate-release formulation of metoprolol at dosages of 100 to 400 mg once daily was effective as an antianginal agent, reducing the number of angina attacks and increasing exercise tolerance.

    Toprol-xl Note

    Not Applicable

    Toprol-xl Patient Counseling

    See Literature

    Toprol-xl Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Metoprolol succinate 25mg, 50mg, 100mg, 200mg; scored ext-rel tabs.

    Pharmacological Class

    Beta-blocker.

    How Supplied

    Tabs—100, 1000

    How Supplied

    Toprol-XL Tablets are supplied in 100- and 1000-count bottles in the following strengths:

    • 25 mg: white, biconvex, film-coated, oval, scored tablets engraved with “A/β”

    • 50 mg: white, biconvex, film-coated, round, scored tablets engraved with “A/mo”

    • 100 mg: white, biconvex, film-coated, round, scored tablets engraved with “A/ms”

    • 200 mg: white, biconvex, film-coated, oval, scored tablets engraved with “A/mY”

    Storage

    • Store at 25°C (77°F). Excursions permitted to 15-30°C (59-86°F).

    Manufacturer

    Melinta Therapeutics

    Generic Availability

    YES

    Mechanism of Action

    Metoprolol is a β1-selective (cardioselective) adrenergic receptor blocking agent that slows the sinus rate and decreases AV nodal conduction. The β-blocking activity of metoprolol has been shown by reduction in heart rate and cardiac output at rest and upon exercise, reduction of systolic blood pressure upon exercise, inhibition of isoproterenol-induced tachycardia, and reduction of reflex orthostatic tachycardia.

    Toprol-xl Indications

    Indications

    Heart failure, to reduce the risk of cardiovascular mortality and heart failure hospitalizations in patients with heart failure.

    Toprol-xl Dosage and Administration

    Adult

    Class II: initially 25mg once daily; more severe: 12.5mg once daily. May double dose as tolerated every 2 weeks; reduce if symptomatic bradycardia occurs; max 200mg/day.

    Children

    Not established.

    Toprol-xl Contraindications

    Contraindications

    Severe bradycardia. 2nd- or 3rd-degree heart block. Cardiogenic shock. Decompensated heart failure. Sick sinus syndrome (unless paced).

    Toprol-xl Boxed Warnings

    Not Applicable

    Toprol-xl Warnings/Precautions

    Warnings/Precautions

    Mild or compensated heart failure. Ischemic heart or peripheral vascular disease. 1st-degree AV block. Sinus node dysfunction. Conduction disorders (eg, Wolff-Parkinson-White). Monitor HR during therapy. Bronchospastic disease. Pheochromocytoma. Surgery. Diabetes. May mask signs and increase risk for hypoglycemia. Hyperthyroidism. Avoid abrupt cessation. Hepatic impairment. Elderly. Neonates. Pregnancy. Nursing mothers: monitor infants.

    Warnings/Precautions

    Abrupt Cessation of Therapy

    • Avoid abruptly discontinuing Toprol-XL in patients treated only for hypertension.

    • When discontinuing chronically administered Toprol-XL especially in patients with ischemic heart disease, gradually reduce the dose of Toprol-XL over a period of 1 to 2 weeks and monitor the patient.

    • Immediately reinstate Toprol-XL if angina worsens or acute coronary ischemia develops, and appropriately manage unstable angina. Advise patients not to interrupt therapy without consulting a physician.

    Heart Failure 

    • While up-titration, worsening cardiac failure may occur. If these symptoms occur, then increase diuretics and restore clinical stability prior to advancing the dose of Toprol-XL.

    • Consider lowering the dose of Toprol-XL or temporarily discontinuing it.

    Bronchospastic Disease 

    • In general, do not give beta-blockers to patients with bronchospastic disease.

    • Toprol-XL may be used in patients with bronchospastic disease who do not respond to, or cannot tolerate, other antihypertensive treatment. Use the lowest possible dose of Toprol-XL.

    • Have bronchodilators, including beta2-agonists, readily available or administered concomitantly.

    Bradycardia

    • Bradycardia, including sinus pause, heart block, and cardiac arrest have occurred with the use of Toprol-XL. 

    • Increased risk for bradycardia in patients with first-degree AV block, sinus node dysfunction, conduction disorders (including Wolff-Parkinson-White) or on concomitant drugs.

    • Monitor heart rate. Discontinue or reduce dose of Toprol-XL if severe bradycardia occurs.

    Pheochromocytoma

    • Administer with an alpha-blocker and only after the alpha-blocker has been initiated if Toprol-XL is used in the setting of pheochromocytoma.

    • Administration of beta-blockers alone in the setting of pheochromocytoma may cause a paradoxical increase in BP.

    Major Surgery

    • Avoid initiating a high-dose regimen of metoprolol extended-release in patients undergoing non-cardiac surgery, since such use in patients with cardiovascular risk factors has been associated with bradycardia, hypotension, stroke, and death. 

    • Do not routinely withdraw chronically administered beta-blocking therapy prior to major surgery.

    Hypoglycemia

    • May prevent early warning signs of hypoglycemia (eg, tachycardia) and increased risk for severe or prolonged hypoglycemia especially in patients with diabetes mellitus or children who are fasting.

    • Seek emergency treatment if severe hypoglycemia occurs.

    Thyrotoxicosis

    • May mask certain clinical signs of hyperthyroidism, (eg, tachycardia). Abrupt withdrawal may precipitate a thyroid storm.

    Peripheral Vascular Disease 

    • May worsen symptoms of arterial insufficiency in patients with peripheral vascular disease.

    Anaphylactic Reaction 

    • While taking beta-blockers, patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated challenge and may be unresponsive to the usual doses of epinephrine used to treat an allergic reaction. 

    Pregnancy Considerations

    Risk Summary

    • Untreated hypertension and heart failure during pregnancy can lead to adverse outcomes for the mother and the fetus.

    • Available data from published observational studies have not demonstrated a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes with metoprolol use during pregnancy.

    Clinical Consideration

    • Fetal/Neonatal adverse reactions: Metoprolol crosses the placenta. Neonates born to mothers who are receiving metoprolol during pregnancy, may be at risk for hypotension, hypoglycemia, bradycardia, and respiratory depression. Observe neonates and manage accordingly.

    Nursing Mother Considerations

    Risk Summary

    • Limited available data from published literature report that metoprolol is present in human milk.

    • No adverse reactions of metoprolol on the breastfed infant have been identified. There is no information regarding the effects of metoprolol on milk production.  

    Clinical Consideration

    • Monitor the breastfed infant for bradycardia and other symptoms of beta-blockade such as listlessness. 

    Pediatric Considerations

    • Safety and effectiveness of ToproL-XL have not been established in patients < 6 years of age. 

    Geriatric Considerations

    • There were no notable differences in efficacy or the rate of adverse reactions between older and younger patients. 

    • In general, use a low initial starting dose in elderly patients given their greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.  

    Hepatic Impairment Considerations

    • No studies have been performed with Toprol-XL in patients with hepatic impairment.

    • Poor hepatic function is most likely to increase blood levels of metoprolol. In patients with impaired hepatic function, initiate Toprol-XL at doses lower than recommended and gradually increase the dose.

    Other Considerations for Specific Populations

    Females and Males of Reproductive Potential

    • Risk Summary: Beta-blockers (including metoprolol) may cause erectile dysfunction and inhibit sperm motility.

    Toprol-xl Pharmacokinetics

    Absorption

    • Average bioavailability at steady-state: 77%.

    Distribution

    • Plasma protein bound: ~12%.

    Metabolism

    • Hepatic (CYP2D6).

    Elimination

    • Renal. Half-life: 3–7hrs.

    Toprol-xl Interactions

    Interactions

    May potentiate hypotension or marked bradycardia with catecholamine depleting drugs (eg, reserpine, MAOIs). Potentiated by strong CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone); monitor if unavoidable. Increased risk of bradycardia with glycosides, clonidine, diltiazem, verapamil. May block epinephrine.

    Toprol-xl Adverse Reactions

    Adverse Reactions

    Fatigue, dizziness, depression, diarrhea, dyspnea, bradycardia, rash; heart block, MI, angina.

    Toprol-xl Clinical Trials

    Clinical Trials

    Heart Failure

    • The randomized, double-blind, placebo-controlled MERIT-HF study evaluated the efficacy of Toprol-XL in 3991 patients with ejection fraction ≤0.40 and NYHA Class II-IV heart failure attributable to ischemia, hypertension, or cardiomyopathy. Patients were randomly assigned 1:1 to receive Toprol-XL or placebo. The primary endpoints of the trial were (1) all-cause mortality plus all-cause hospitalization (time to first event) and (2) all-cause mortality.

    • The trial was terminated early for a statistically significant reduction in all-cause mortality (34%, nominal P =.00009). 

    • The risk of all-cause mortality plus all-cause hospitalization was reduced by 19% (P =.00012). The trial also showed improvements in heart failure-related mortality and heart failure-related hospitalizations, and NYHA functional class. 

    Toprol-xl Note

    Not Applicable

    Toprol-xl Patient Counseling

    See Literature

    Toprol-xl Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Metoprolol succinate 25mg, 50mg, 100mg, 200mg; scored ext-rel tabs.

    Pharmacological Class

    Cardioselective beta-blocker.

    How Supplied

    Tabs—100, 1000

    How Supplied

    Toprol-XL Tablets are supplied in 100- and 1000-count bottles in the following strengths:

    • 25 mg: white, biconvex, film-coated, oval, scored tablets engraved with “A/β”

    • 50 mg: white, biconvex, film-coated, round, scored tablets engraved with “A/mo”

    • 100 mg: white, biconvex, film-coated, round, scored tablets engraved with “A/ms”

    • 200 mg: white, biconvex, film-coated, oval, scored tablets engraved with “A/mY”

    Storage

    • Store at 25°C (77°F). Excursions permitted to 15-30°C (59-86°F).

    Manufacturer

    Melinta Therapeutics

    Generic Availability

    YES

    Mechanism of Action

    Metoprolol is a β1-selective (cardioselective) adrenergic receptor blocking agent that slows the sinus rate and decreases AV nodal conduction. The β-blocking activity of metoprolol has been shown by reduction in heart rate and cardiac output at rest and upon exercise, reduction of systolic blood pressure upon exercise, inhibition of isoproterenol-induced tachycardia, and reduction of reflex orthostatic tachycardia.

    Toprol-xl Indications

    Indications

    Hypertension.

    Toprol-xl Dosage and Administration

    Adult

    Initially 25–100mg once daily, alone or with a diuretic. May increase at 1-week intervals; max 400mg/day.

    Children

    <6yrs: not established. ≥6yrs: initially 1mg/kg once daily; max 50mg/day. Adjust based on response. Max 2mg/kg (200mg) daily.

    Toprol-xl Contraindications

    Contraindications

    Severe bradycardia. 2nd- or 3rd-degree heart block. Cardiogenic shock. Decompensated heart failure. Sick sinus syndrome (unless paced).

    Toprol-xl Boxed Warnings

    Not Applicable

    Toprol-xl Warnings/Precautions

    Warnings/Precautions

    Mild or compensated heart failure. Ischemic heart or peripheral vascular disease. 1st-degree AV block. Sinus node dysfunction. Conduction disorders (eg, Wolff-Parkinson-White). Monitor HR during therapy. Bronchospastic disease. Pheochromocytoma. Surgery. Diabetes. May mask signs and increase risk for hypoglycemia. Hyperthyroidism. Avoid abrupt cessation. Hepatic impairment. Elderly. Neonates. Pregnancy. Nursing mothers: monitor infants.

    Warnings/Precautions

    Abrupt Cessation of Therapy

    • Avoid abruptly discontinuing Toprol-XL in patients treated only for hypertension.

    • When discontinuing chronically administered Toprol-XL especially in patients with ischemic heart disease, gradually reduce the dose of Toprol-XL over a period of 1 to 2 weeks and monitor the patient.

    • Immediately reinstate Toprol-XL if angina worsens or acute coronary ischemia develops, and appropriately manage unstable angina. Advise patients not to interrupt therapy without consulting a physician.

    Heart Failure 

    • While up-titration, worsening cardiac failure may occur. If these symptoms occur, then increase diuretics and restore clinical stability prior to advancing the dose of Toprol-XL.

    • Consider lowering the dose of Toprol-XL or temporarily discontinuing it.

    Bronchospastic Disease 

    • In general, do not give beta-blockers to patients with bronchospastic disease.

    • Toprol-XL may be used in patients with bronchospastic disease who do not respond to, or cannot tolerate, other antihypertensive treatment. Use the lowest possible dose of Toprol-XL.

    • Have bronchodilators, including beta2-agonists, readily available or administered concomitantly.

    Bradycardia

    • Bradycardia, including sinus pause, heart block, and cardiac arrest have occurred with the use of Toprol-XL. 

    • Increased risk for bradycardia in patients with first-degree AV block, sinus node dysfunction, conduction disorders (including Wolff-Parkinson-White) or on concomitant drugs.

    • Monitor heart rate. Discontinue or reduce dose of Toprol-XL if severe bradycardia occurs.

    Pheochromocytoma

    • Administer with an alpha-blocker and only after the alpha-blocker has been initiated if Toprol-XL is used in the setting of pheochromocytoma.

    • Administration of beta-blockers alone in the setting of pheochromocytoma may cause a paradoxical increase in BP.

    Major Surgery

    • Avoid initiating a high-dose regimen of metoprolol extended-release in patients undergoing non-cardiac surgery, since such use in patients with cardiovascular risk factors has been associated with bradycardia, hypotension, stroke, and death. 

    • Do not routinely withdraw chronically administered beta-blocking therapy prior to major surgery.

    Hypoglycemia

    • May prevent early warning signs of hypoglycemia (eg, tachycardia) and increased risk for severe or prolonged hypoglycemia especially in patients with diabetes mellitus or children who are fasting.

    • Seek emergency treatment if severe hypoglycemia occurs.

    Thyrotoxicosis

    • May mask certain clinical signs of hyperthyroidism, (eg, tachycardia). Abrupt withdrawal may precipitate a thyroid storm.

    Peripheral Vascular Disease 

    • May worsen symptoms of arterial insufficiency in patients with peripheral vascular disease.

    Anaphylactic Reaction 

    • While taking beta-blockers, patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated challenge and may be unresponsive to the usual doses of epinephrine used to treat an allergic reaction. 

    Pregnancy Considerations

    Risk Summary

    • Untreated hypertension and heart failure during pregnancy can lead to adverse outcomes for the mother and the fetus.

    • Available data from published observational studies have not demonstrated a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes with metoprolol use during pregnancy.

    Clinical Consideration

    • Fetal/Neonatal adverse reactions: Metoprolol crosses the placenta. Neonates born to mothers who are receiving metoprolol during pregnancy, may be at risk for hypotension, hypoglycemia, bradycardia, and respiratory depression. Observe neonates and manage accordingly.

    Nursing Mother Considerations

    Risk Summary

    • Limited available data from published literature report that metoprolol is present in human milk.

    • No adverse reactions of metoprolol on the breastfed infant have been identified. There is no information regarding the effects of metoprolol on milk production.  

    Clinical Consideration

    • Monitor the breastfed infant for bradycardia and other symptoms of beta-blockade such as listlessness. 

    Pediatric Considerations

    • Safety and effectiveness of ToproL-XL have not been established in patients < 6 years of age. 

    Geriatric Considerations

    • There were no notable differences in efficacy or the rate of adverse reactions between older and younger patients. 

    • In general, use a low initial starting dose in elderly patients given their greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.  

    Hepatic Impairment Considerations

    • No studies have been performed with Toprol-XL in patients with hepatic impairment.

    • Poor hepatic function is most likely to increase blood levels of metoprolol. In patients with impaired hepatic function, initiate Toprol-XL at doses lower than recommended and gradually increase the dose.

    Other Considerations for Specific Populations

    Females and Males of Reproductive Potential

    • Risk Summary: Beta-blockers (including metoprolol) may cause erectile dysfunction and inhibit sperm motility.

    Toprol-xl Pharmacokinetics

    Absorption

    • Average bioavailability at steady-state: 77%.

    Distribution

    • Plasma protein bound: ~12%.

    Metabolism

    • Hepatic (CYP2D6).

    Elimination

    • Renal. Half-life: 3–7hrs.

    Toprol-xl Interactions

    Interactions

    May potentiate hypotension or marked bradycardia with catecholamine depleting drugs (eg, reserpine, MAOIs). Potentiated by strong CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone); monitor if unavoidable. Increased risk of bradycardia with glycosides, clonidine, diltiazem, verapamil. May block epinephrine.

    Toprol-xl Adverse Reactions

    Adverse Reactions

    Fatigue, dizziness, depression, diarrhea, dyspnea, bradycardia, rash; heart block, MI, angina.

    Toprol-xl Clinical Trials

    Clinical Trials

    Hypertension

    • A double-blind study evaluated the efficacy of Toprol-XL in 1092 patients with mild to moderate hypertension. Patients were randomly assigned to receive once daily Toprol-XL (25, 100, or 400 mg), Plendil (felodipine extended-release tablets), the combination, or placebo. Results showed that treatment with Toprol-XL alone decreased sitting BP by 6–8/4–7 mmHg (placebo-corrected change from baseline) at 24 hours post-dose after 9 weeks. The combination of Toprol-XL and Plendil had greater effects on BP.

    • In controlled clinical studies, an immediate-release dosage form of metoprolol (100–450 mg daily) achieved effective antihypertensive effects when used alone or as concomitantly with thiazide-type diuretics. Toprol-XL at dosages of 100–400 mg once daily had similar results as conventional metoprolol tablets administered 2 to 4 times daily. Moreover, Toprol-XL 50 mg once daily lowered blood pressure 24 hours post-dosing in placebo-controlled studies.

    • In controlled, comparative clinical studies, immediate-release dosage form of metoprolol was observed to be comparable to propranolol, methyldopa, and thiazide-type diuretics, and affected both supine and standing BP.

    Toprol-xl Note

    Not Applicable

    Toprol-xl Patient Counseling

    See Literature

    • Latest News Your top articles for Wednesday

    • Haymarket Medical NetworkTop Picks

    • Loading...

      Continuing Medical Education (CME/CE) Courses

      Show More