Metoprolol
In medicine, metoprolol is a adrenergic beta-antagonist medication that is a "selective adrenergic beta-1-blocking agent with no stimulatory action. It's binding to plasma albumin is weaker than alprenolol and it may be useful in angina pectoris, hypertension, or cardiac arrhythmias." It is also used for heart failure.[1]
History
Metoprolol tartrate was developed by Novartis and received approval in the United States August 7, 1978.[2]
Toprol-XL brand of metoprolol succinate was developed by Astra Pharmaceuticals. Asta and Zeneca merged in 1999 to become AstraZeneca. Toprol's patent was filed on Sep 28, 1990 and approved on Jan 14, 1992 .[3] It received approval in the United States on January 10, 1992.[4] According to drugstore.com, 30 days of 100 mg pills costs $52.99 in January, 2009.
Generic metoprolol succinate was developed by Sandoz and received approval in the United States on July 31, 2006. According to drugstore.com, 30 days of 100 mg pills costs $25.99 in January, 2009.
Astrazenaca and the manufacturer of generic metoprolol succinate have engaged in a lawsuit.[5]
Chemistry
The IUPAC name of metroprolol is:
- (±)-1-(Isopropylamino)-3-[p-(2-methoxyethyl)phenoxy]-2-propanol (according to Dailymed)
- 1-[4-(2-methoxyethyl)phenoxy]-3-(propan-2-ylamino)propan-2-ol (according to DrugBank)[6]
Metabolism
It is metabolized by cytochrome P-450 2D6 allele and so may have drug interactions[7] and inherited variations in metabolism.[8]
Dosage
For healthy adults, the starting dose is 25 to 100 mg daily in single or divided doses and the maximum dose is 400 to 450 mg/day.
Efficacy
Metoprolol can benefit patients with heart failure.[9]
External links
The most up-to-date information about Metoprolol and other drugs can be found at the following sites.
- Metoprolol - FDA approved drug information (drug label) from DailyMed (U.S. National Library of Medicine).
- Metoprolol - Drug information for consumers from MedlinePlus (U.S. National Library of Medicine).
- Metoprolol - Detailed information from DrugBank.
References
- ↑ Anonymous (2024), Metoprolol (English). Medical Subject Headings. U.S. National Library of Medicine.
- ↑ Drugs@FDA. U S Food and Drug Administration
- ↑ Metroprolol succinate. Google Patents.
- ↑ Drugs@FDA. U S Food and Drug Administration
- ↑ [States Court of Appeals for the Federal Circuit] (July 23, 2007). United States Court of Appeals for the Federal Circuit. 2006-1254. IN RE METOPROLOL SUCCINATE PATENT LITIGATION (pdf). Retrieved on 2009-01-11.
- ↑ Showing Metoprolol (DB00264). DrugBank. Retrieved on 2009-06-20.
- ↑ Onalan O, Cumurcu BE, Bekar L (May 2008). "Complete atrioventricular block associated with concomitant use of metoprolol and paroxetine". Mayo Clin. Proc. 83 (5): 595–9. PMID 18452693. [e]
- ↑ Nozawa T, Taguchi M, Tahara K, et al (November 2005). "Influence of CYP2D6 genotype on metoprolol plasma concentration and beta-adrenergic inhibition during long-term treatment: a comparison with bisoprolol". J. Cardiovasc. Pharmacol. 46 (5): 713–20. PMID 16220080. [e]
- ↑ Waagstein F, Bristow MR, Swedberg K, et al (December 1993). "Beneficial effects of metoprolol in idiopathic dilated cardiomyopathy. Metoprolol in Dilated Cardiomyopathy (MDC) Trial Study Group". Lancet 342 (8885): 1441–6. PMID 7902479. [e]