Metoprolol


Description

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.[

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Pharmacology

Indication

Metoprolol is indicated for the treatment of angina, heart failure, myocardial infarction, atrial fi... Read more

Pharmacodynamic

Administration of metoprolol in normal subjects is widely reported to produce a dose-dependent reduc... Read more

Mechanism of action

Metoprolol is a beta-1-adrenergic receptor inhibitor specific to cardiac cells with negligible effec... Read more

Absorption

When metoprolol is administered orally, it is almost completely absorbed in the gastrointestinal tra... Read more

Protein binding

Metoprolol is not highly bound to plasma proteins and only about 11% of the administered dose is fou... Read more

Volume of distribution

The reported volume of distribution of metoprolol is 4.2 L/kg.[ Read more

Clearance

The reported clearance rate on patients with normal kidney function is 0.8 L/min. In cirrhotic patie... Read more

Half life

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

Route of elimination

Metoprolol is mainly excreted via the kidneys. From the eliminated dose, less than 5% is recovered u... Read more

Toxicity

Oral administration of metoprolol to rats presents an LD50 in the range of 3090 to 4670 mg/kg. Cases... 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.

    Interactions

    Type in a drug name to check for interaction with Metoprolol

    The metabolism of (R)-warfarin can be decreased when combined with Metoprolol.
    The metabolism of (S)-Warfarin can be decreased when combined with Metoprolol.
    The metabolism of Metoprolol can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
    1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may decrease the antihypertensive activities of Metoprolol.
    1-benzylimidazole may decrease the antihypertensive activities of Metoprolol.
    1,10-Phenanthroline may increase the bradycardic activities of Metoprolol.
    The therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Metoprolol.
    The therapeutic efficacy of Metoprolol can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
    The therapeutic efficacy of Metoprolol can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The metabolism of Metoprolol can be increased when combined with 25-desacetylrifapentine.
    The risk or severity of adverse effects can be increased when Metoprolol is combined with 3-isobutyl-1-methyl-7H-xanthine.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Metoprolol.
    The therapeutic efficacy of Metoprolol can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
    The therapeutic efficacy of 4-Bromo-2,5-dimethoxyphenethylamine can be decreased when used in combination with Metoprolol.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Metoprolol.
    The metabolism of 4-Methoxyamphetamine can be decreased when combined with Metoprolol.
    The metabolism of 5-androstenedione can be decreased when combined with Metoprolol.
    The metabolism of Metoprolol can be decreased when combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of Metoprolol can be decreased when combined with 6-Deoxyerythronolide B.
    The risk or severity of adverse effects can be increased when Metoprolol is combined with 6-O-benzylguanine.

    References

    • 1 . Morris J, Dunham A: Metoprolol . [PubMed: 30422518]
    • 2 . Silberstein SD: Preventive Migraine Treatment. Continuum (Minneap Minn). 2015 Aug;21(4 Headache):973-89. doi: 10.1212/CON.0000000000000199. [PubMed: 26252585]
    • 3 . Bahar MA, Kamp J, Borgsteede SD, Hak E, Wilffert B: The impact of CYP2D6 mediated drug-drug interaction: a systematic review on a combination of metoprolol and paroxetine/fluoxetine. Br J Clin Pharmacol. 2018 Dec;84(12):2704-2715. doi: 10.1111/bcp.13741. Epub 2018 Sep 24. [PubMed: 30248178]
    • 4 . Regardh CG, Jordo L, Ervik M, Lundborg P, Olsson R, Ronn O: Pharmacokinetics of metoprolol in patients with hepatic cirrhosis. Clin Pharmacokinet. 1981 Sep-Oct;6(5):375-88. doi: 10.2165/00003088-198106050-00004. [PubMed: 7333059]
    • 5 . Frishman W., Cheng-Lai A. and Nawarskas J. (2005). Current cardiovascular drugs (4th ed.). Current medicine LLC.
    • 6 . Jones & Bartlett (2016). 2016 Nurse's drug handbook (15th ed.). Jones and Bartlett Publishers Inc..
    • 7 . Saeb-Parsy K., Assomull R., Khan F., Saeb-Parsy K. and Kelly A. (1990). Instant Pharmacology. Willey.
    • 8 . FDA approvals [Link]
    • 9 . Researchgate publications [Link]
    • 10 . Heart [Link]
    • 11 . FDA reports [Link]

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