Metoprolol Tartrate

Metoprolol

[met-oh-proh-lawl, -lol]
Metoprolol is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension. It is marketed under the brand name Lopressor or Lopresor, respectively, by Novartis, and Toprol-XL (in the USA); Selokeen (in Nederlands); as Minax by Alphapharm (in Australia), Metrol by Arrow Pharmaceuticals (in Australia), as Betaloc by AstraZeneca, as Neobloc by Unipharm (in Israel) and as Corvitol by Berlin-Chemie AG. A number of generic products are available as well. The active substance metoprolol is employed either as metoprolol succinate or metoprolol tartrate (whereas 100 mg metoprolol tartrate corresponds to 95 mg metoprolol succinate), respectively as prolonged-release or conventional-release formulation.

Physical properties

Metoprolol is very low melting. Its melting point is around 45 degrees Celsius (as determined by Differential scanning calorimetry). For this reason metoprolol is always manufactured in salt form, as drugs with melting points below 100 degrees Celsius are difficult to work with in a manufacturing environment. The free base exists as a waxy white solid, where the tartrate salt is finer crystalline material.

Pharmacology

  • Selective
  • Moderately Lipophilic
  • Without intrinsic sympathomimetic activity (ISA)
  • With weak membrane stabilizing activity
  • Short half-life, therefore must be taken at least twice daily or as a Slow-release preparation.
  • Decreases Heart Rate, Contractility and Cardiac Output, therefore decreasing blood pressure

Indications

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