METOPROLOL SUCCINATE

Other

Brand names: Metoprolol Succinate

Oral

Mechanism of Action

12.1 Mechanism of Action Metoprolol is a beta 1 -selective (cardioselective) adrenergic receptor blocking agent. This preferential effect is not absolute, however, and at higher plasma concentrations, metoprolol also inhibits beta 2 -adrenoreceptors, chiefly located in the bronchial and vascular musculature. Metoprolol has no intrinsic sympathomimetic activity, and membrane-stabilizing activity is detectable only at plasma concentrations much greater than required for beta-blockade. Animal and human experiments indicate that metoprolol slows the sinus rate and decreases AV nodal conduction. The relative beta 1 -selectivity of metoprolol has been confirmed by the following: (1) In normal subjects, metoprolol is unable to reverse the beta 2 -mediated vasodilating effects of epinephrine. This contrasts with the effect of nonselective beta-blockers, which completely reverse the vasodilating effects of epinephrine. (2) In asthmatic patients, metoprolol reduces FEV1 and FVC significantly les

Indications

1 INDICATIONS AND USAGE Metoprolol succinate extended-release tablets are a beta-adrenergic blocker indicated for the treatment of: • Hypertension

to lower blood pressure. Lowering blood pressure reduces the risk of fatal and non-fatal cardiovascular events

primarily strokes and myocardial infarctions. (1.1) • Angina Pectoris (1.2) • Heart Failure

to lower blood pressure. Lowering blood pressure lowers the risk of fatal and non-fatal cardiovascular events

including

as appropriate

Contraindications

• 4 CONTRAINDICATIONS Metoprolol succinate extended-release tablets are contraindicated in severe bradycardia
• second or third degree heart block
• cardiogenic shock
• decompensated heart failure
• sick sinus syndrome (unless a permanent pacemaker is in place)

FDA Warnings

5 WARNINGS AND PRECAUTIONS • Abrupt cessation may exacerbate myocardial ischemia
3) • Concomitant use of glycosides, clonidine, diltiazem and verapamil with beta-blockers can increase the risk of bradycardia
1) • Hypoglycemia: May increase risk for hypoglycemia and mask early warning signs
3) ], may be at increased risk

Known Side Effects

11 documented side effects by frequency

Fatigue

>10%

Shortness of Breath

1-10%

Diarrhea

1-10%

Nausea

1-10%

Drug Not Working

1-10%

Dizziness

1-10%

Weakness

1-10%

Headache

1-10%

Falls

1-10%

Low Blood Pressure

0.1-1%

Vomiting

0.1-1%

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Formulations

Dosage Forms

Tablet

Route

Oral