Description
Metoprolol succinate represents an entirely novel extended-release formulation of metoprolol, requiring administration only once daily to ensure constant metoprolol blood concentrations and sustained β1-adrenergic blocking effects throughout the 24-hour period. It offers numerous advantages in both pharmacology and clinical therapeutics. Clinically, it is primarily indicated for the management of hypertension,High blood pressure medication,angina pectoris, and stable chronic heart failure with left ventricular systolic dysfunction.
Administer orally once daily, preferably in the morning. Tablets may be divided but must not be chewed or crushed. Swallow with at least half a glass of liquid. Concomitant food intake does not affect bioavailability. Dosage should be individualised to avoid bradycardia. Effective dosing guidelines are as follows: Hypertension: 47.5–95 mg once daily. Patients unresponsive to 95 mg metoprolol succinate sustained-release tablets may combine with other antihypertensives, preferably diuretics and dihydropyridine calcium channel blockers, or increase dosage. Angina pectoris: 95–190 mg once daily. May be combined with nitrates or increased dosage as required.
Chemical Properties
White or almost white, crystalline powder.
History
Metoprolol Succinate, the world's first Beta-1 Selective Receptor blocker, was developed by AstraZeneca and first launched in 1992. It is commonly used in clinical practice to treat hypertension, angina pectoris, and stable chronic heart failure with impaired left ventricular systolic function.
Metoprolol was first developed in 1969 at Hassle Laboratories in Sweden. As a selective beta-1 adrenergic receptor blocker, it binds to beta-1 receptors to antagonize the effects of neurotransmitters and catecholamines on beta receptors. This action increases vascular smooth muscle sensitivity to vasoactive mediators and inhibits renin secretion. Clinically, it is used to treat hypertension, angina pectoris, and heart failure.
Uses
Metoprolol Succinate is used in the treatment of patients suffering from chronic heart failure, as well as to treat blood pressure from mild hypertension. β-adrenoceptor antagonist or β-blocker.
Uses
Anti - hypertensives
Definition
ChEBI: Metoprolol succinate is an alcohol and a member of phenols.
brand name
Toprol (AstraZeneca).
in vivo
Metoprolol (2.5 mg/kg/h; infusion; 11 weeks) reduces proinflammatory cytokines and atherosclerosis in ApoE/ Mice[1].
Metoprolol (15 mg/kg/q12h; i.g.; 5 days) shows anti-inflammation and anti-virus effects in murine model with coxsackievirus B3-induced viral myocarditis[2].
Metoprolol (2.5 mg/kg; i.v.; 3 bolus injections) significantly decreased activated caspase-9 protein expression and inhibits myocardial apoptosis in coronary microembolization (CME) rats[4].
| Animal Model: | Male ApoE/ mice[1] |
| Dosage: | 2.5mg/kg/h |
| Administration: | Via osmotic minipumps, 11 weeks |
| Result: | Significantly reduced atherosclerotic plaque area in thoracic aorta, reduced serum TNFα and the chemokine CXCL1 as well as decreasing the macrophage content in the plaques. |
| Animal Model: | Balb/c mice, coxsackievirus B3 (CVB3) induced viral myocarditis (VMC) model[2] |
| Dosage: | 15 mg/kg/q12h
|
| Administration: | Oral gavage, 5 consecutive days |
| Result: | Reduced pathological scores of VMC induced by CVB3 infection, protected the myocardium against viral damage by reducing serum cTn-I levels. Decreased the levels of myocardial pro-inflammatory cytokines and increase the expression of anti-inflammatory cytokine. Significantly decreased myocardial virus titers. |
