Toprol-XL


Also found in: Dictionary, Thesaurus, Wikipedia.
Related to Toprol-XL: metoprolol, Metoprolol succinate

metoprolol succinate

Toprol-XL

metoprolol tartrate

Apo-Metoprolol (CA), Betaloc (CA) (UK), Betaloc Durules (CA), Dom-Metoprolol (CA), Gen-Metoprolol (CA), Lopresor (UK), Lopresor SR (CA), Lopressor, Novo-Metoprol (CA), Nu-Metop (CA), PHL-Metoprolol, PMS-Metoprolol-L (CA), Sandoz Metoprolol (CA)

Pharmacologic class: Beta-adrenergic blocker (selective)

Therapeutic class: Antihypertensive, antianginal

Pregnancy risk category C

FDA Box Warning

• Exacerbations of angina pectoris and myocardial infarction (MI) may follow abrupt withdrawal of some beta blockers. When discontinuing long-term therapy, particularly in patients with ischemic heart disease, reduce dosage gradually over 1 to 2 weeks and monitor patient carefully. If angina worsens markedly or acute coronary insufficiency develops, reinstate drug promptly (at least temporarily) and take other appropriate measures to manage unstable angina. Caution patient not to interrupt or discontinue therapy without prescriber's advice. Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue drug abruptly even in patients treated only for hypertension.

Action

Blocks stimulation of beta1 (myocardial) adrenergic receptors, usually without affecting beta2 (pulmonary, vascular, uterine) adrenergic receptor sites

Availability

Injection (tartrate): 1 mg/ml

Tablets: 50 mg, 100 mg

Tablets (extended-release, succinate): 25 mg, 50 mg, 100 mg, 200 mg

Indications and dosages

Hypertension

Adults: 50 to 100 mg P.O. daily as a single dose or in two divided doses (conventional tablets) or once daily (extended-release tablets). May be increased q 7 days as needed, up to 450 mg/day (tartrate) or 400 mg (succinate extended-release).

Angina pectoris

Adults: 100 mg P.O. daily as a single dose or in two divided doses (conventional tablets) or once daily (extended-release tablets). May be increased q 7 days as needed, up to 400 mg.

MI

Adults: Three bolus injections of 5 mg I.V. given at 2-minute intervals. If patient tolerates I.V. dose, give 50 mg P.O. 15 minutes after last I.V. dose, and continue P.O. doses q 6 hours for 48 hours. For maintenance, 100 mg P.O. b.i.d. If patient doesn't tolerate full I.V. dose, give 25 to 50 mg P.O. (depending on degree of intolerance), starting 15 minutes after last I.V. dose or when clinical condition allows; discontinue drug if patient shows severe intolerance. As late treatment, 100 mg P.O. b.i.d. when clinical condition allows, continued for at least 3 months.

Symptomatic heart failure

Adults: 25 mg P.O. daily (extended-release tablets) in patients with NYHA Class II heart failure. Dosage may be doubled q 2 weeks, up to 200 mg/day or until highest tolerated dosage is reached. For more severe heart failure, start with 12.5 mg P.O. daily.

Off-label uses

• Ventricular arrhythmias, tachycardia

• Tremors

• Anxiety

Contraindications

• Sinus bradycardia, heart block greater than first degree, cardiogenic shock, overt cardiac failure (with Lopressor used for hypertension or angina)

• Heart rate below 45 beats/minute, second- or third-degree heart block, significant first-degree heart block; systolic pressure below 100 mm Hg; or moderate-to-severe cardiac failure (when Lopressor is used for MI)

• Hypersensitivity to drug or its components, severe bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome (unless permanent pacemaker is in place) (with Toprol-XL)

Precautions

Use cautiously in:

• renal or hepatic impairment, pulmonary disease, diabetes mellitus, thyrotoxicosis

• MAO inhibitor use within past 14 days

• pregnant or breastfeeding patients

• children (safety not established).

Administration

• Give metoprolol tartrate with or immediately after meals, because food enhances its absorption.

• Know that succinate extended-release tablets are scored and can be divided. However, tablet or half-tablet should be swallowed whole and not crushed or chewed.

• For I.V. administration, give each dose undiluted by direct injection over at least 1 minute.

Adverse reactions

CNS: fatigue, weakness, anxiety, depression, dizziness, drowsiness, insomnia, memory loss, mental status changes, nervousness, nightmares

CV: orthostatic hypotension, peripheral vasoconstriction, bradycardia, heart failure, pulmonary edema

EENT: blurred vision, stuffy nose

GI: nausea, vomiting, constipation, diarrhea, flatulence, gastric pain, heartburn, dry mouth

GU: urinary frequency, erectile dysfunction, decreased libido

Hepatic: hepatitis

Metabolic: hyperglycemia, hypoglycemia

Respiratory: wheezing, bronchospasm

Musculoskeletal: back pain, joint pain

Skin: rash

Other: drug-induced lupus syndrome

Interactions

Drug-drug. Amphetamines, ephedrine, epinephrine, norepinephrine, phenylephrine, pseudoephedrine: unopposed alpha-adrenergic stimulation (excessive hypertension, bradycardia)

Antihypertensives, nitrates: additive hypotension

Digoxin: additive bradycardia

Dobutamine, dopamine: reduced cardiovascular benefits of these drugs

General anesthestics, phenytoin (I.V.), verapamil: additive myocardial depression

Insulin, oral hypoglycemics: altered efficacy of these drugs

MAO inhibitors: hypertension

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, blood urea nitrogen, glucose, lactate dehydrogenase, lipoproteins, potassium, triglycerides, uric acid: increased levels

Drug-food. Any food: enhanced drug absorption

Drug-behaviors. Acute alcohol ingestion: additive hypotension

Cocaine use: unopposed alpha-adrenergic stimulation (excessive hypertension, bradycardia)

Patient monitoring

• Measure blood pressure closely when starting therapy and titrating dosage. Once patient stabilizes, measure blood pressure every 3 to 6 months.

• Monitor blood pressure and pulse before I.V. administration. If patient is hypotensive or has bradycardia, consult prescriber before giving dose.

• Watch for orthostatic hypotension in at-risk patients, particularly the elderly.

• Assess glucose levels in diabetic patient. Be aware that drug may mask signs and symptoms of hypoglycemia.

• Monitor for signs and symptoms of hyperthyroidism. Know that drug may mask these. Reduce dosage gradually in hyperthyroid patients.

When discontinuing drug, reduce dosage gradually over 1 to 2 weeks.

Patient teaching

• Advise patient to take with or immediately after meals.

• Tell patient that extended-release tablets are scored and can be divided, but that he should swallow tablets or half-tablets whole and not crush or chew them.

Advise patient with heart failure to report signs or symptoms of worsening condition, including weight gain and increasing shortness of breath.

• Caution patient to avoid driving and other hazardous activities until drug effects are known.

• Instruct patient to notify health care providers (including dentists) that he is taking drug before having surgery.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and behaviors mentioned above.

metoprolol

(me-toe-proe-lole) ,

Betaloc IV

(trade name),

Lopresor

(trade name),

Lopresor SR

(trade name),

Lopressor

(trade name),

Toprol-XL

(trade name)

Classification

Therapeutic: antianginals
Pharmacologic: beta blockers
Pregnancy Category: C

Indications

Hypertension.Angina pectoris.Prevention of MI and decreased mortality in patients with recent MI.Management of stable, symptomatic (class II or III) heart failure due to ischemic, hypertensive or cardiomyopathc origin (may be used with ACE inhibitors, diuretics and/or digoxin; Toprol XL only).Ventricular arrhythmias/tachycardia.Migraine prophylaxis.Tremors.Aggressive behavior.Drug-induced akathisia.Anxiety.

Action

Blocks stimulation of beta1(myocardial)-adrenergic receptors. Does not usually affect beta2(pulmonary, vascular, uterine)-adrenergic receptor sites.

Therapeutic effects

Decreased BP and heart rate.
Decreased frequency of attacks of angina pectoris.
Decreased rate of cardiovascular mortality and hospitalization in patients with heart failure.

Pharmacokinetics

Absorption: Well absorbed after oral administration.
Distribution: Crosses the blood-brain barrier, crosses the placenta; small amounts enter breast milk.
Metabolism and Excretion: Mostly metabolized by the liver (primarily by CYP2D6; the CYP2D6 enzyme system exhibits genetic polymorphism); genetic implication ∼7% of population may be poor metabolizers and may have significantly ↑ metoprolol concentrations and an ↑ risk of adverse effects.
Half-life: 3–7 hr.

Time/action profile (cardiovascular effects)

ROUTEONSETPEAKDURATION
PO†15 minunknown6–12 hr
PO–ERunknown6–12 hr24 hr
IVimmediate20 min5–8 hr
†Maximal effects on BP (chronic therapy) may not occur for 1 wk. Hypotensive effects may persist for up to 4 wk after discontinuation

Contraindications/Precautions

Contraindicated in: Uncompensated HF;Pulmonary edema;Cardiogenic shock;Bradycardia, heart block, or sick sinus syndrome (in absence of a pacemaker).
Use Cautiously in: Renal impairment;Hepatic impairment; Geriatric: ↑ sensitivity to beta blockers; initial dose reduction recommended;Pulmonary disease (including asthma; beta1 selectivity may be lost at higher doses);Diabetes mellitus (may mask signs of hypoglycemia);Thyrotoxicosis (may mask symptoms);Patients with a history of severe allergic reactions (intensity of reactions may be increased);Untreated pheochromocytoma (initiate only after alpha blocker therapy started); Obstetric / Lactation / Pediatric: Safety not established; all agents cross the placenta and may cause fetal/neonatal bradycardia, hypotension, hypoglycemia, or respiratory depression.

Adverse Reactions/Side Effects

Central nervous system

  • fatigue (most frequent)
  • weakness (most frequent)
  • anxiety
  • depression
  • dizziness
  • drowsiness
  • insomnia
  • memory loss
  • mental status changes
  • nervousness
  • nightmares

Ear, Eye, Nose, Throat

  • blurred vision
  • stuffy nose

Respiratory

  • bronchospasm
  • wheezing

Cardiovascular

  • bradycardia (life-threatening)
  • HF (life-threatening)
  • pulmonary edema (life-threatening)
  • hypotension
  • peripheral vasoconstriction

Gastrointestinal

  • constipation
  • diarrhea
  • drug-induced hepatitis
  • dry mouth
  • flatulence
  • gastric pain
  • heartburn
  • ↑ liver enzymes
  • nausea
  • vomiting

Genitourinary

  • erectile dysfunction (most frequent)
  • ↓ libido
  • urinary frequency

Dermatologic

  • rashes

Endocrinologic

  • hyperglycemia
  • hypoglycemia

Musculoskeletal

  • arthralgia
  • back pain
  • joint pain

Miscellaneous

  • drug-induced lupus syndrome

Interactions

Drug-Drug interaction

General anesthesia, IVphenytoin, and verapamil may cause ↑ myocardial depression.↑ risk of bradycardia when used with digoxin, verapamil, diltiazem, or clonidine.↑ hypotension may occur with other antihypertensives, acute ingestion of alcohol, or nitrates.Concurrent use with amphetamines, cocaine, ephedrine, epinephrine, norepinephrine, phenylephrine, or pseudoephedrine may result in unopposed alpha-adrenergic stimulation (excessive hypertension, bradycardia).Concurrent administration of thyroid administration may ↓ effectiveness.May alter the effectiveness of insulins or oral hypoglycemic agents (dose adjustments may be necessary).May ↓ the effectiveness of theophylline.May ↓ the beneficial beta1-cardiovascular effects of dopamine or dobutamine.Use cautiously within 14 days of MAO inhibitor therapy (may result in hypertension).

Route/Dosage

When switching from immediate-release to extended-release product, the same total daily dose can be used

Oral (Adults) Antihypertensive/antianginal—25–100 mg/day as a single dose initially or 2 divided doses; may be ↑ q 7 days as needed up to 450 mg/day (immediate-release) or 400 mg/day (extended-release) (for angina, give in divided doses). Extended-release products are given once daily. MI—25–50 mg (starting 15 min after last IV dose) q 6 hr for 48 hr, then 100 mg twice daily. Heart failure—12.5–25 mg once daily (of extended-release), can be doubled every 2 wk up to 200 mg/day. Migraine prevention—50–100 mg 2–4 times daily (unlabeled).
Intravenous (Adults) MI—5 mg q 2 min for 3 doses, followed by oral dosing.

Availability (generic available)

Tablets (tartrate): 25 mg, 50 mg, 100 mg Cost: Generic — All strengths $7.18 / 100
Extended-release tablets (succinate; Toprol XL): 25 mg, 50 mg, 100 mg, 200 mg Cost: Generic — 25 mg $35.68 / 100, 50 mg $41.93 / 100, 100 mg $53.95 / 100, 200 mg $84.54 / 100
Injection: 1 mg/mL
In combination with: hydrochlorothiazide (Lopressor HCT). See combination drugs.

Nursing implications

Nursing assessment

  • Monitor BP, ECG, and pulse frequently during dose adjustment and periodically during therapy.
  • Monitor frequency of prescription refills to determine compliance.
  • Monitor vital signs and ECG every 5–15 min during and for several hours after parenteral administration. If heart rate <40 bpm, especially if cardiac output is also decreased, administer atropine 0.25–0.5 mg IV.
  • Monitor intake and output ratios and daily weights. Assess routinely for signs and symptoms of HF (dyspnea, rales/crackles, weight gain, peripheral edema, jugular venous distention).
  • Angina: Assess frequency and characteristics of anginal attacks periodically during therapy.
  • Lab Test Considerations: May cause ↑ BUN, serum lipoprotein, potassium, triglyceride, and uric acid levels.
    • May cause ↑ ANA titers.
    • May cause ↑ in blood glucose levels.
    • May cause ↑ serum alkaline phosphatase, LDH, AST, and ALT levels.

Potential Nursing Diagnoses

Decreased cardiac output (Side Effects)
Noncompliance (Patient/Family Teaching)

Implementation

  • high alert: IV vasoactive medications are inherently dangerous. Before administering intravenously, have second practitioner independently check original order and dose calculations.
  • high alert: Do not confuse Toprol-XL (metoprolol) with Topamax (topiramate). Do not confuse Lopressor with Lyrica. Do not confuse metoprolol tartrate with metoprolol succinate.
  • Oral: Take apical pulse before administering. If <50 bpm or if arrhythmia occurs, withhold medication and notify health care professional.
    • Administer metoprolol with meals or directly after eating.
    • Extended-release tablets should be swallowed whole; do not break, crush, or chew.
  • Intravenous Administration
  • Diluent: Administer undiluted.Concentration: 1 mg/mL.
  • Rate: Administer over 1 min.
  • Y-Site Compatibility: acyclovir, alemtuzumab, alfentanil, alteplase, amikacin, aminocaproic acid, aminophylline, amiodarone, amphotericin B liposome, anidulafungin, argatroban, ascorbic acid, atropine, azathioprine, aztreonam, benztropine, bivalirudin, bleomycin, bumetanide, buprenorphine, butorphanol, calcium chloride, calcium gluconate, carboplatin, carmustine, caspofungin, cefazolin, cefonocid, cefoperazone, cefotaxime, cefotetan, cefoxitin, ceftaroline, ceftazidime, ceftriaxone, cefuroxime, chloramphenicol, chlorpromazine, cisplatin, clindamycin, cyanocobalamin, cyclophosphamide, cyclosporine, cytarabine, dactinomycin, daptomycin, dexamethasone, dexmedetomidine, digoxin, diltiazem, diphenhydramine, dobutamine, docetaxel, dopamine, doxorubicin, doxycycline, enalaprilat, ephedrine, epinephrine, epirubicin, epoetin alfa, eptifibatide, esmolol, etoposide, etoposide phosphate, famotidine, fenoldopam, fentanyl, fluconazole, fludarabine, fluorouracil, folic acid, furosemide, ganciclovir, gemcitabine, gentamicin, glycopyrrolate, granisetron, heparin, hetastarch, hydrocortisone, hydromorphone, idarubicin, ifosfamide, imipenem/cilastatin, indomethacin, insulin, irinotecan, isoproterenol, ketorolac, labetalol, linezolid, lorazepam, magnesium sulfate, mannitol, mechlorethamine, meperidine, methotrexate, methoxamine, methyldopate, methylprednisolone, metoclopramide, metronidazole, midazolam, milrinone, mitoxantrone, morphine, multivitamins, mycophenolate, nafcillin, nalbuphine, naloxone, nitroprusside, norepinephrine, octreotide, ondansetron, oxacillin, oxaliplatin, oxytocin, paclitaxel, palonosetron, pamidronate, pancuronium, papaverine, pemetrexed, penicillin G, pentamidine, pentazocine, pentobarbital, phenobarbital, phentolamine, phenylephrine, phytonadione, piperacillin/tazobactam, potassium acetate, potassium chloride, procainamide, prochlorperazine, promethazine, propranolol, protamine, pyridoxime, quinupristin/dalfopristin, ranitidine, rocuronium, sodium bicarbonate, streptokinase, succinylcholine, sufentanil, tacrolimus, teniposide, theophylline, thiamine, thiotepa, ticarcillin/clavulanate, tigecycline, tirofiban, tobramycin, tolazoline, trimetaphan, vancomycin, vasopressin, vecuronium, verapamil, vincristine, vinorelbine, voriconazole, zoledronic acid
  • Y-Site Incompatibility: allopruinol, amphotericin B cholesteryl, amphotericin B colloidal, amphotericin B lipid complex, dantrolene, diazepam, diazoxide, pantoprazole, phenytoin, trimethoprim/sulfamethoxazole

Patient/Family Teaching

  • Instruct patient to take medication as directed, at the same time each day, even if feeling well; do not skip or double up on missed doses. Take missed doses as soon as possible up to 8 hr before next dose. Abrupt withdrawal may precipitate life-threatening arrhythmias, hypertension, or myocardial ischemia.
  • Teach patient and family how to check pulse daily and BP biweekly and to report significant changes to health care professional.
  • May cause drowsiness. Caution patient to avoid driving or other activities that require alertness until response to the drug is known.
  • Advise patient to change positions slowly to minimize orthostatic hypotension.
  • Caution patient that this medication may increase sensitivity to cold.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any Rx, OTC, or herbal products, especially cold preparations, concurrently with this medication. Patients on antihypertensive therapy should also avoid excessive amounts of coffee, tea, and cola.
  • Diabetics should closely monitor blood glucose, especially if weakness, malaise, irritability, or fatigue occurs. Medication does not block sweating as a sign of hypoglycemia.
  • Advise patient to notify health care professional if slow pulse, difficulty breathing, wheezing, cold hands and feet, dizziness, light-headedness, confusion, depression, rash, fever, sore throat, unusual bleeding, or bruising occurs.
  • Instruct patient to inform health care professional of medication regimen before treatment or surgery.
  • Advise patient to carry identification describing disease process and medication regimen at all times.
  • Hypertension: Reinforce the need to continue additional therapies for hypertension (weight loss, sodium restriction, stress reduction, regular exercise, moderation of alcohol consumption, and smoking cessation). Medication controls but does not cure hypertension.

Evaluation/Desired Outcomes

  • Decrease in BP.
  • Reduction in frequency of anginal attacks.
    • Increase in activity tolerance.
  • Prevention of MI.

Toprol-XL

(tŏp′rôl′, -rŏl′)
A trademark for an extended-release formulation of the succinate salt of metoprolol.

metoprolol

A beta-blocker used for hypertension and angina.
 
Adverse effects
Headache, fatigue, dizziness, dry cough, angiooedema.
 
Contraindications
Sinus bradycardia, cardiogenic shock, heart failure, heart block > 1st degree.
References in periodicals archive ?
Under the terms of the agreement, Aralez, an Irish company, is provided with the exclusive distributor rights to Lannett's Toprol-XL (Metoprolol Succinate) Extended Release Tablets in 25 mg, 50 mg, 100 mg and 200mg in the US.
The deal will see Aralez paying AstraZeneca $175 million to buy the rights to Toprol-XL tablets in the US, and the authorised generic drug marketed by Par Pharmaceuticals.
The basis for AstraZeneca's complaint is that the action taken by Eon infringes AstraZeneca's patents covering TOPROL-XL.
Ireland-based Aralez Pharmaceuticals Trading DAC (Aralez Ireland) has acquired the United States rights to English-Swedish-based AstraZeneca's generic high blood pressure drug, Toprol-XL, it was reported yesterday.
Under the terms of the agreement, Aralez will pay AstraZeneca $175 million to acquire the rights to Toprol-XL tablets in the US, and the authorised generic medicine marketed by Par Pharmaceuticals.
A federal judge in Delaware has refused to dismiss a lawsuit accusing AstraZeneca of anticompetitive practices involving the heart drug Toprol-XL.
has announced approval of the 50-mg strength of a generic version of Toprol-XL (AstraZeneca PLC).
But other Astra products under pressure from generic copies included angina drug Toprol-XL, where sales slumped 60% to pounds 96.
Sales of Toprol-XL, a treatment for angina, heart failure and high blood pressure, dived by 43% in the quarter, after generic competition launched in August.
Reports of mixups between Topamax and Toprol-XL (AstraZeneca) have been submitted to the Food and Drug Administration, the World Health Organization, and the U.
Competitively priced with the generics of TOPROL-XL and hydrochlorothiazide tablets, regardless of insurance coverage3
AstraZeneca has also agreed to sell the US rights to its generic high blood pressure drug, Toprol-XL, to Aralez Pharmaceuticals Trading DAC for an initial payment of USD175m.