Metoprolol succinate is a beta-adrenergic blocker with selective activity on beta-1 adrenoreceptors located mainly in cardiac muscles. At higher doses, metoprolol also inhibits beta-2 adrenoreceptors of bronchial and vascular smooth muscles. Possible mechanisms of antihypertensive effects of metoprolol include: competitive antagonism of catecholamines at peripheral and cardiac adrenergic receptors (resulting in decreased cardiac output), a central effect leading to reduced sympathetic outflow, and suppression of renin activity. The exact mechanism for the beneficial effects of metoprolol in heart failure is unknown
藥動學
Absorption:
Bioavailability, oral, extended-release tablet: 77% relative to immediate-release oral formulation
Distribution:
Vd: 5.6 L/kg
Metabolism:
Liver: main route via CYP2D6
Excretion:
Renal, oral: less than 5% unchanged
Elimination Half Life:
3 to 7 hours
禁忌症
Cardiogenic shock
Decompensated cardiac failure
Hypersensitivity to metoprolol succinate or any component of the product
Second- or third-degree heart block
Severe bradycardia
Sick sinus syndrome (without a functional permanent pacemaker)
懷孕分類
C (FDA) (AUS)
哺乳分類
Maternal medication usually compatible with breastfeeding.(AAP)
Infant risk is minimal.(MDX)
Acute myocardial infarction:
Initial dose: Metoprolol tartrate orally 25 to 50 mg every 6 to 12 hours, then transition in 2 to 3 days to metoprolol succinate and titrate to 200 mg once daily as tolerated.
Angina pectoris:
Initial, 100 mg orally once daily; increase dose gradually at weekly intervals based on clinical response and tolerability; dosages above 400 mg daily have not been studied .
Discontinuing therapy, gradually reduce dosage over 1 to 2 weeks .
Switching from immediate-release metoprolol to metoprolol succinate, use the same total daily dose of metoprolol succinate .
Congestive heart failure:
Prior to initiation, stabilize dosage of other heart failure medication(s)
(NYHA class II) Initial, 25 mg orally once daily for 2 weeks
(NYHA class III) Initial, 12.5 mg orally once daily for 2 weeks
Dosage titration, double every 2 weeks to highest tolerated dose or up to 200 mg daily. Reduce dose if symptomatic bradycardia occurs. Consider reducing dose, temporary discontinuation, or increasing diuretic doses if transient worsening of heart failure occurs; do not increase dosage until symptoms of worsening heart failure have stabilized.
Hypertension:
Initial, 25 to 100 mg orally once daily
Dosage titration, increase dosage at weekly or longer intervals to achieve optimum antihypertensive effect; dosages above 400 mg daily have not been studied
When switching from immediate-release metoprolol to metoprolol succinate, use the same total daily dose of metoprolol succinate .
小兒調整劑量
(6 years or older) Initial, 1 mg/kg orally once daily; MAX 50 mg once daily; adjust dosage based on clinical response.
Dosages above 2 mg/kg or 200 mg once daily have not been studied
腎功能調整劑量
Adjustment not necessary?.
肝功能調整劑量
Initiate therapy at lower dose based on indication and increase dosage gradually.