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

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
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
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
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may decrease the antihypertensive activities of Metoprolol.
1-benzylimidazole
1-benzylimidazole may decrease the antihypertensive activities of Metoprolol.
1,10-Phenanthroline
1,10-Phenanthroline may increase the bradycardic activities of Metoprolol.
2,4-thiazolidinedione
The therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Metoprolol.
2,5-Dimethoxy-4-ethylamphetamine
The therapeutic efficacy of Metoprolol can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The therapeutic efficacy of Metoprolol can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
25-desacetylrifapentine
The metabolism of Metoprolol can be increased when combined with 25-desacetylrifapentine.
3-isobutyl-1-methyl-7H-xanthine
The risk or severity of adverse effects can be increased when Metoprolol is combined with 3-isobutyl-1-methyl-7H-xanthine.
4-Bromo-2,5-dimethoxyamphetamine
The therapeutic efficacy of Metoprolol can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
4-Bromo-2,5-dimethoxyphenethylamine
The therapeutic efficacy of 4-Bromo-2,5-dimethoxyphenethylamine can be decreased when used in combination with Metoprolol.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be decreased when combined with Metoprolol.
4-Methoxyamphetamine
The metabolism of 4-Methoxyamphetamine can be decreased when combined with Metoprolol.
5-methoxy-N,N-dimethyltryptamine
The metabolism of Metoprolol can be decreased when combined with 5-methoxy-N,N-dimethyltryptamine.
6-Deoxyerythronolide B
The metabolism of Metoprolol can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanine
The risk or severity of adverse effects can be increased when Metoprolol is combined with 6-O-benzylguanine.
7-Deazaguanine
The risk or severity of adverse effects can be increased when Metoprolol is combined with 7-Deazaguanine.
7-ethyl-10-hydroxycamptothecin
The metabolism of Metoprolol can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Metoprolol.
7,9-Dimethylguanine
The risk or severity of adverse effects can be increased when Metoprolol is combined with 7,9-Dimethylguanine.
11 References
  1. 1 . Morris J, Dunham A: Metoprolol .PubMed: 30422518
  2. 2 . Silberstein SD: Preventive Migraine Treatment. Continuum (Minneap Minn). 2015 Aug;21(4 Headache):973-89. doi: 10.1212/CON.0000000000000199.PubMed: 26252585
  3. 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. 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. 5 . Frishman W., Cheng-Lai A. and Nawarskas J. (2005). Current cardiovascular drugs (4th ed.). Current medicine LLC.
  6. 6 . Jones & Bartlett (2016). 2016 Nurse's drug handbook (15th ed.). Jones and Bartlett Publishers Inc..
  7. 7 . Saeb-Parsy K., Assomull R., Khan F., Saeb-Parsy K. and Kelly A. (1990). Instant Pharmacology. Willey.
  8. 8 . FDA approvals Link
  9. 9 . Researchgate publications Link
  10. 10 . Heart Link
  11. 11 . FDA reports Link