Metoprolol

Metoprolol Brand Names

First-Metoprolol | KAPSPARGO | Lopressor | Toprol XL

What is Metoprolol

Metoprolol is a competitive, beta-1 selective (cardioselective) adrenergic antagonist, which is most similar to atenolol.

It has moderate lipid solubility, lacks intrinsic sympathomimetic activity (ISA), and has weak membrane stabilizing activity (MSA).

Metoprolol is more lipid soluble than atenolol, but less than propranolol and betaxolol. The degree of lipid solubility affects metoprolol’s route of elimination (extensively metabolized) and, theoretically, it’s potential for CNS side effects.

Metoprolol has a relatively short elimination half-life compared to other cardioselective beta-blockers.

It is used for the treatment of hypertension, myocardial infarction, angina, atrial fibrillation or flutter, tremor, migraine, and heart failure.

Cardioselective beta blockers are also utilized in the management of heart failure. The COMET trial evaluated carvedilol vs. metoprolol in patients with chronic heart failure (NYHA Class II—IV), and demonstrated a significantly lower all-cause mortality for carvedilol (34% vs. 40% for metoprolol).

The COMET study has been criticized for utilizing the immediate-release form of metoprolol (tartrate) vs. the extended-release formulation (succinate), which has been FDA-approved for heart failure based on the favorable findings of the MERIT-HF trial.

In the MERIT-HF trial, extended-release metoprolol significantly reduced the incidence of sudden death and mortality due to progressive heart failure in patients receiving conventional therapy (e.g., ACE inhibitors, diuretics, and, in most cases, digitalis).

The COMET trial has also been criticized for evaluating a substantially lower metoprolol target dosage (50 mg PO twice daily) than the FDA-approved target dosage for heart failure (200 mg PO once daily) supported by the MERIT-HF trial.

Authors of the statement also provide recommendations for drug therapy, according to CAD status. In keeping with recent European guidelines, beta-blockers are no longer recommended for blood pressure control in the primary prevention group.

The 2007 AHA guidelines for the management of hypertension state beta-blockers should not be used as first-line therapy for the treatment of hypertension, as several comparative clinical trials have shown beta blockers to be inferior to ACE inhibitors, angiotensin-receptor blockers, or calcium channel blockers for preventing both stroke and coronary artery disease complications.

These guidelines do, however, recommend the use of beta-blockers for the treatment of hypertension in patients with angina, prior myocardial infarction, or heart failure.

The perioperative use of beta blockers to prevent cardiac complications has become somewhat controversial.

In the POISE trial, published online in Lancet in May 2008, 8351 patients with or at risk for atherosclerotic disease were randomized to receive placebo or extended release metoprolol 100 mg 2—4 hours before surgery followed by a daily dose of 200 mg for 30 days following non-cardiac surgery.

Results from this trial show that fewer patients in the extended release metoprolol group had a myocardial infarction compared to the placebo group.

However, the results also indicated that 3.1% of the patients in the extended release metoprolol group died compared with 2.3% in the placebo group, and 1% of patients in the metoprolol group had a stroke compared with 0.5% of those administered placebo.

Metoprolol was initially approved by the FDA in 1978. In February 2001 Toprol-XL™ was approved for the treatment of stable, symptomatic (NYHA Class II—III) heart failure of ischemic, hypertensive, or cardiomyopathic origin, largely based on the MERIT-HF study findings.

Indications

1. acute myocardial infarction, STEMI
2. angina
3. atrial fibrillation
4. atrial flutter
5. cardiomyopathy
6. heart failure
7. hypertension
8. migraine prophylaxis
9. reduction of cardiovascular mortality
10. tremor
11. unstable angina

Side Effects

1. abdominal pain
2. agranulocytosis
3. alopecia
4. amnesia
5. anxiety
6. arthralgia
7. AV block
8. blurred vision
9. bradycardia
10. bronchospasm
11. chest pain (unspecified)
12. confusion
13. constipation
14. depression
15. diabetes mellitus
16. diaphoresis
17. diarrhea
18. dizziness
19. drowsiness
20. dysgeusia
21. dyspnea
22. elevated hepatic enzymes
23. fatigue
24. flatulence
25. hallucinations
26. headache
27. heart failure
28. hepatitis
29. hyperglycemia
30. hyperhidrosis
31. hypertension
32. hypertriglyceridemia
33. hypoglycemia
34. hypotension
35. impotence (erectile dysfunction)
36. insomnia
37. jaundice
38. laryngospasm
39. libido decrease
40. lupus-like symptoms
41. musculoskeletal pain
42. nausea
43. nightmares
44. palpitations
45. paresthesias
46. penile fibrosis
47. peripheral edema
48. peripheral vasoconstriction
49. photosensitivity
50. pruritus
51. psoriasis
52. purpura
53. pyrosis (heartburn)
54. rash
55. retroperitoneal fibrosis
56. rhinitis
57. sinus tachycardia
58. stroke
59. syncope
60. thrombocytopenia
61. thrombotic thrombocytopenic purpura (TTP)
62. tinnitus
63. tissue necrosis
64. tremor
65. vertigo
66. visual impairment
67. vomiting
68. weight gain
69. wheezing
70. withdrawal
71. xerophthalmia
72. xerosis
73. xerostomia

Monitoring Parameters

• blood pressure
• heart rate

Contraindications

• abrupt discontinuation
• acute bronchospasm
• acute heart failure
• asthma
• AV block
• beta-blocker hypersensitivity
• bradycardia
• breast-feeding
• bronchitis
• cardiogenic shock
• cerebrovascular disease
• chronic obstructive pulmonary disease (COPD)
• depression
• diabetes mellitus
• driving or operating machinery
• emphysema
• geriatric
• hepatic disease
• hyperthyroidism
• hypotension
• myasthenia gravis
• peripheral vascular disease
• pheochromocytoma
• pregnancy
• psoriasis
• pulmonary disease
• pulmonary edema
• Raynaud’s phenomenon
• sick sinus syndrome
• surgery
• thyroid disease
• thyrotoxicosis
• vasospastic angina
• ventricular dysfunction

Interactions

• Abiraterone
• Acetaminophen; Aspirin, ASA; Caffeine
• Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
• Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
• Acetaminophen; Diphenhydramine
• Acetaminophen; Propoxyphene
• Adenosine
• Albiglutide
• Aldesleukin, IL-2
• Alemtuzumab
• Alfentanil
• Alfuzosin
• Aliskiren; Amlodipine
• Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
• Alogliptin; Metformin
• Alpha-blockers
• Alpha-glucosidase Inhibitors
• Alprostadil
• Amifostine
• Amiodarone
• Amlodipine
• Amlodipine; Atorvastatin
• Amlodipine; Benazepril
• Amlodipine; Celecoxib
• Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
• Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
• Amlodipine; Olmesartan
• Amlodipine; Telmisartan
• Amlodipine; Valsartan
• Amobarbital
• Amyl Nitrite
• Antithyroid agents
• Apomorphine
• Apraclonidine
• Aripiprazole
• Artemether; Lumefantrine
• Articaine; Epinephrine
• Asenapine
• Aspirin, ASA
• Aspirin, ASA; Butalbital; Caffeine
• Aspirin, ASA; Butalbital; Caffeine; Codeine
• Aspirin, ASA; Caffeine; Dihydrocodeine
• Aspirin, ASA; Caffeine; Orphenadrine
• Aspirin, ASA; Carisoprodol
• Aspirin, ASA; Carisoprodol; Codeine
• Aspirin, ASA; Citric Acid; Sodium Bicarbonate
• Aspirin, ASA; Dipyridamole
• Aspirin, ASA; Omeprazole
• Aspirin, ASA; Oxycodone
• Aspirin, ASA; Pravastatin
• Atazanavir
• Atazanavir; Cobicistat
• Baclofen
• Belladonna Alkaloids; Ergotamine; Phenobarbital
• Beta-agonists
• Bismuth Subsalicylate
• Bismuth Subsalicylate; Metronidazole; Tetracycline
• Bosentan
• Bretylium
• Brexpiprazole
• Bupivacaine
• Bupivacaine Liposomal
• Bupivacaine; Lidocaine
• Bupropion
• Bupropion; Naltrexone
• Cabergoline
• Caffeine; Ergotamine
• Canagliflozin; Metformin
• Carbetapentane; Diphenhydramine; Phenylephrine
• Carbidopa; Levodopa
• Carbidopa; Levodopa; Entacapone
• Cariprazine
• Ceritinib
• Cevimeline
• Chloroprocaine
• Chlorthalidone; Clonidine
• Choline Salicylate; Magnesium Salicylate
• Cimetidine
• Cinacalcet
• Citalopram
• Clevidipine
• Clonidine
• Clozapine
• Co-Enzyme Q10, Ubiquinone
• Cobicistat
• Cocaine
• Conivaptan
• Crizotinib
• Dacomitinib
• Dapagliflozin; Metformin
• Darunavir
• Darunavir; Cobicistat
• Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
• Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
• Desflurane
• Desvenlafaxine
• Dexmedetomidine
• Dextromethorphan; Diphenhydramine; Phenylephrine
• Dextromethorphan; Quinidine
• Diazoxide
• Digoxin
• Dihydroergotamine
• Diltiazem
• Dipeptidyl Peptidase-4 Inhibitors
• Diphenhydramine
• Diphenhydramine; Hydrocodone; Phenylephrine
• Diphenhydramine; Ibuprofen
• Diphenhydramine; Naproxen
• Diphenhydramine; Phenylephrine
• Dipyridamole
• Disopyramide
• Donepezil
• Donepezil; Memantine
• Doxazosin
• Dronedarone
• Dulaglutide
• Duloxetine
• Dutasteride; Tamsulosin
• Eliglustat
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
• Empagliflozin; Linagliptin; Metformin
• Empagliflozin; Metformin
• Enalapril; Felodipine
• Encainide
• Enflurane
• Epoprostenol
• Ergonovine
• Ergotamine
• Ertugliflozin; Metformin
• Escitalopram
• Estradiol
• Estradiol Cypionate; Medroxyprogesterone
• Ethanol
• Etomidate
• Exenatide
• Fedratinib
• Felodipine
• Fenoldopam
• Fingolimod
• Fish Oil, Omega-3 Fatty Acids (Dietary Supplements)
• Flecainide
• Fluorescein
• Fluoxetine
• Fluoxetine; Olanzapine
• Fluvoxamine
• food
• Fospropofol
• Galantamine
• General anesthetics
• Ginger, Zingiber officinale
• Glipizide; Metformin
• Glucagon
• Glyburide; Metformin
• Guanabenz
• Guanfacine
• Haloperidol
• Halothane
• Hydralazine; Isosorbide Dinitrate, ISDN
• Icosapent ethyl
• Iloperidone
• Iloprost
• Imatinib
• Incretin Mimetics
• Insulin Degludec; Liraglutide
• Insulin Glargine; Lixisenatide
• Insulins
• Intravenous Lipid Emulsions
• Isocarboxazid
• Isoflurane
• Isoniazid, INH; Pyrazinamide, PZA; Rifampin
• Isoniazid, INH; Rifampin
• Isosorbide Dinitrate, ISDN
• Isosorbide Mononitrate
• Isradipine
• Ivabradine
• Ketamine
• Lacosamide
• Lanreotide
• Lasmiditan
• Levobupivacaine
• Levodopa
• Levothyroxine
• Levothyroxine; Liothyronine (Porcine)
• Levothyroxine; Liothyronine (Synthetic)
• Lidocaine
• Lidocaine; Prilocaine
• Linagliptin; Metformin
• Linezolid
• Liothyronine
• Liraglutide
• Lithium
• Lixisenatide
• Lofexidine
• Lopinavir; Ritonavir
• Lovastatin; Niacin
• Lurasidone
• Magnesium Salicylate
• Mefloquine
• Meglitinides
• Mephobarbital
• Mepivacaine
• Mepivacaine; Levonordefrin
• Mestranol; Norethindrone
• Metformin
• Metformin; Pioglitazone
• Metformin; Repaglinide
• Metformin; Rosiglitazone
• Metformin; Saxagliptin
• Metformin; Sitagliptin
• Methacholine
• Methohexital
• Methylergonovine
• Methysergide
• Milrinone
• Mirabegron
• Nefazodone
• Nesiritide, BNP
• Neuromuscular blockers
• Niacin, Niacinamide
• Niacin; Simvastatin
• Nicardipine
• Nifedipine
• Nimodipine
• Nisoldipine
• Nitrates
• Nitroglycerin
• Nitroprusside
• Non-Ionic Contrast Media
• Nonsteroidal antiinflammatory drugs
• Octreotide
• Olanzapine
• Ombitasvir; Paritaprevir; Ritonavir
• Omeprazole; Amoxicillin; Rifabutin
• Oritavancin
• Oxymetazoline
• Paliperidone
• Panobinostat
• Paroxetine
• Pasireotide
• Pentoxifylline
• Perindopril; Amlodipine
• Phenelzine
• Phenothiazines
• Phenoxybenzamine
• Phentolamine
• Pilocarpine
• Pramlintide
• Prazosin
• Prilocaine
• Prilocaine; Epinephrine
• Primidone
• Procainamide
• Procaine
• Propafenone
• Propofol
• Propoxyphene
• Quinidine
• Quinine
• Ranolazine
• Rasagiline
• Remifentanil
• Reserpine
• Rifabutin
• Rifampin
• Rifamycins
• Rifapentine
• Risperidone
• Ritonavir
• Rivastigmine
• Rolapitant
• Ropivacaine
• Salsalate
• Selegiline
• Semaglutide
• Sevoflurane
• SGLT2 Inhibitors
• Silodosin
• Siponimod
• Sufentanil
• Sulfonylureas
• Sympathomimetics
• Tacrine
• Tamsulosin
• Tasimelteon
• Telithromycin
• Terazosin
• Terbinafine
• Tetrabenazine
• Tetracaine
• Thalidomide
• Thiazolidinediones
• Thiopental
• Thiothixene
• Thyroid hormones
• Tipranavir
• Tizanidine
• Trandolapril; Verapamil
• Tranylcypromine
• Trazodone
• Vemurafenib
• Venlafaxine
• Verapamil
• Yohimbine
• Ziprasidone