CAS Number: 80274-67-5

Lopresor OROS / Metoprolol Fumarate | 80274-67-5

Metoprolol Fumarate is the fumarate salt form of metoprolol, a cardioselective competitive beta-1 adrenergic receptor antagonist that lacks intrinsic sympathomimetic activity and possesses antihypertensive properties. It exerts its effects by antagonizing beta-1 adrenergic receptors in the myocardium, thereby reducing the rate and force of myocardial contraction and decreasing cardiac output. Additionally, metoprolol fumarate may lower renin secretion, leading to reduced levels of angiotensin II, which helps prevent vasoconstriction and aldosterone secretion. It is commonly used in the management of cardiovascular conditions such as hypertension, angina, heart failure, and arrhythmias, and is available in immediate- or extended-release formulations. Common side effects include fatigue, dizziness, bradycardia, and hypotension, and it should be withdrawn gradually to avoid rebound effects. The typical starting dose is 25–50 mg daily, with a maximum of up to 200–400 mg daily in divided doses, depending on patient tolerance and clinical response.

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References

  • Comparison of the pharmacodynamic and pharmacokinetic profiles of single and multiple doses of a commercial slow-release metoprolol formulation with a new Oros delivery system.
    A new osmotic pressure mediated delivery system for metoprolol (Lopresor Oros) has been evaluated by measuring the haemodynamic effects and pharmacokinetics after single and multiple oral dosing in young healthy volunteers. 2 Similar studies have been carried out in the same group using equivalent single and multiple oral doses of the commercial slow-release preparation (Slow Lopresor). 3 The new osmotic delivery system produces a more uniform haemodynamic response: a plateau metoprolol concentration in plasma is reached about 6 h after dosing and is maintained for 10 h.
    DOI: 10.1111/j.1365-2125.1982.tb01391.x
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