Description

Simple

A medication used to treat high blood pressure, chest pain or pressure, and to decrease the risk of death from a heart attack.

Clinical

A beta-blocker used in the treatment of hypertension and angina, and used to reduce mortality due to myocardial infarction.

Overview

Metoprolol is a selective beta-1 blocker commonly employed as the succinate and tartrate derivatives depending if the formulation is designed to be of immediate release or extended release.[2, 9] The possibility of the generation of these formulations comes from the lower systemic bioavailability of the succinate derivative.[5] To this date, it is one of the preferred beta-blockers in general clinical guidelines and it is widely prescribed in the Netherlands, New Zealand, and the US.[3] Metoprolol was developed since 1969 by US Pharmaceutical Holdings I and FDA approved in 1978.[8]

Pharmacology

Indication

Metoprolol is indicated for the treatment of angina, heart failure, myocardial infarction, atrial fibrillation, atrial flutter and hypertension.[1]

Some off-label uses of metoprolol include supraventri... Read more

Pharmacodynamic

Administration of metoprolol in normal subjects is widely reported to produce a dose-dependent reduction on heart rate and cardiac output.[1] This effect is generated due to a decreased cardiac excitabili... Read more

Mechanism of action

Metoprolol is a beta-1-adrenergic receptor inhibitor specific to cardiac cells with negligible effect on beta-2 receptors. This inhibition decreases cardiac output by producing negative chronotropic and inotropic effects without presenting activity towards membrane stabilization nor intrinsic sympat... Read more

Absorption

When metoprolol is administered orally, it is almost completely absorbed in the gastrointestinal tract.[1] The maximum serum concentration is achieved 20 min after intravenous administration and 1-2 hours... Read more

Protein binding

Metoprolol is not highly bound to plasma proteins and only about 11% of the administered dose is found bound. It is mainly bound to serum albumin.[1]

Volume of distribution

The reported volume of distribution of metoprolol is 4.2 L/kg.[5] Due to the characteristics of metoprolol, this molecule is ab... Read more

Clearance

The reported clearance rate on patients with normal kidney function is 0.8 L/min. In cirrhotic patients, the clearance rate changes to 0.61 L/min.[ Read more

Half life

The immediate release formulations of metoprolol present a half-life of about 3-7 hours.[1]

Route of elimination

Metoprolol is mainly excreted via the kidneys. From the eliminated dose, less than 5% is recovered unchanged.[1]

Toxicity

Oral administration of metoprolol to rats presents an LD50 in the range of 3090 to 4670 mg/kg. Cases of overdose have reported bradycardia, hypotension, bronchospasm, and cardiac failure. In the case of an overdose, gastric lavage is recommended followed by specific treatment according to symptoms.[... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Heart Failure US
  • Kind: experimental
    • Percent: 28%
  • Kind: placebo
    • Percent: 30%
  • Clinical Trial
    Hypotension US
  • Kind: experimental
    • Percent: 27%
  • Kind: placebo
    • Percent: 23%
  • Clinical Trial
    Bradycardia US
  • Kind: experimental
    • Percent: 16%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    Tiredness US
  • Kind: experimental
    • Percent: 10%
  • Clinical Trial
    First-degree heart block US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Second- or third-degree heart block US
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 5%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 5%
  • Clinical Trial
    Pruritus US
  • Kind: experimental
    • Percent: 5%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: 5%
  • Clinical Trial
    Shortness of Breath US
  • Kind: experimental
    • Percent: 3%
  • Clinical Trial
    Bradycardia US
  • Kind: experimental
    • Percent: 3%
  • Clinical Trial
    Bradycardia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Chest Pain US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Syncope US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Dyspnea aggravated US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Ventricular Tachycardia US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Coronary artery disorder US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Hypotension US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Arrhythmia aggravated US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Peyronie's Disease US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Myocardial Infarction US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Accident or injury US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Cerebrovascular Disorder US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Pneumonia US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial
    Hypotension US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Bronchospasm US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Gastric pain US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Digestive tract disorders US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Heartburn US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Cold extremities US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Arterial Insufficiency US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Palpitations US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Congestive Heart Failure US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Syncope US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Chest Pain US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Tiredness US
  • Kind: experimental
    • Percent: 1%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: >1%
  • Kind: placebo
    • Percent: ≤0.5%
  • Clinical Trial

    Contraindications

    • Hypersensitivity:
      • Beta-blockers
    • Regions: US
    • Hypersensitivity:
      • true
    • Regions: US
    • Regions: US
    • Patient Conditions:
        • Name: Heart block greater than first degree
        • Drugbank Id: DBCOND0107492
    • Regions: US
    • Patient Conditions:
        • Name: Cardiogenic Shock
        • Drugbank Id: DBCOND0030788
    • Regions: US
    • Patient Conditions:
        • Name: Decompensated cardiac failure
        • Drugbank Id: DBCOND0107538
    • Regions: US
    • Patient Conditions:
        • Name: Sick Sinus Syndrome
        • Drugbank Id: DBCOND0000493
    • Regions: US
    • Patient Conditions:
        • Name: Severe bradycardia
        • Drugbank Id: DBCOND0097899
        • Modification Of:
          • Base:
            • Name: Bradycardia
            • Drugbank Id: DBCOND0000504
          • Severity:
            • Includes:
              • severe

    Food Interactions

    Avoid alcohol.

    Avoid natural licorice.

    Take with food.