Kapspargo Sprinkle

— THERAPEUTIC CATEGORIES —
  • Angina
  • CHF and arrhythmias
  • Hypertension

Kapspargo Sprinkle Generic Name & Formulations

General Description

Metoprolol succinate 25mg, 50mg, 100mg, 200mg; ext-rel caps.

Pharmacological Class

Beta-blocker.

How Supplied

Ext-rel caps—30

Generic Availability

NO

Mechanism of Action

Metoprolol is a beta1-selective (cardioselective) adrenergic receptor blocking agent. This preferential effect is not absolute, however, and at higher plasma concentrations, metoprolol also inhibits beta2-adrenoreceptors, chiefly located in the bronchial and vascular musculature. By blocking catecholamine-induced increases in heart rate, in velocity and extent of myocardial contraction, and in blood pressure, metoprolol reduces the oxygen requirements of the heart at any given level of effort, thus making it useful in the long-term management of angina pectoris.

Kapspargo Sprinkle Indications

Indications

Long-term management of angina pectoris.

Kapspargo Sprinkle Dosage and Administration

Adult

Swallow whole. If difficulty swallowing cap, may open and sprinkle contents over a teaspoonful of soft food (eg, applesauce, yogurt, pudding) and consume mixture within 60mins; or, can give via NG tube (mix contents with 15mL of water first). Individualize. Initially 100mg once daily. May increase at 1-week intervals; max 400mg/day. Reduce dose gradually over 1–2 weeks.

Children

Not established.

Kapspargo Sprinkle Contraindications

Contraindications

Severe bradycardia. 2nd or 3rd degree heart block. Cardiogenic shock. Decompensated heart failure. Sick sinus syndrome (unless paced).

Kapspargo Sprinkle Boxed Warnings

Not Applicable

Kapspargo Sprinkle Warnings/Precautions

Warnings/Precautions

Worsening heart failure; increase diuretic and stabilize before up-titration; reduce or discontinue dose if necessary. Ischemic heart or peripheral vascular disease. 1st-degree AV block. Sinus node dysfunction. Conduction disorders (eg, Wolff-Parkinson-White). Monitor HR during therapy. Discontinue or reduce dose if severe bradycardia develops. Bronchospastic disease. Pheochromocytoma (initiate with an alpha-blocker first). Surgery. May mask signs and increased risk for hypoglycemia. Hyperthyroidism. History of severe anaphylactic reactions to allergens. Avoid abrupt cessation. Hepatic impairment. Elderly. Neonates. Pregnancy (esp. during 3rd trimester). Nursing mothers: monitor infants.

Kapspargo Sprinkle Pharmacokinetics

Absorption

  • Peak plasma concentration is attained at 10 hours after administration.

Distribution

  • About 12% of the drug is bound to human serum albumin. Metoprolol crosses the blood-brain barrier and has been reported in the CSF in a concentration 78% of the simultaneous plasma concentration.

Metabolism

  • Hepatic.

Elimination

  • Renal. Half-life: 3–7 hours.

Kapspargo Sprinkle Interactions

Interactions

May potentiate catecholamine depleting drugs (eg, reserpine, MAO inhibitors); monitor. Increased risk of bradycardia with digitalis glycosides, clonidine, diltiazem, verapamil. Increased rebound hypertension with clonidine withdrawal. May be potentiated by strong CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone). Avoid alcohol. May block epinephrine.

Kapspargo Sprinkle Adverse Reactions

Adverse Reactions

Tiredness, dizziness, depression, shortness of breath, bradycardia, hypotension, diarrhea, pruritus, rash; worsening angina, heart failure, AV block.

Kapspargo Sprinkle Clinical Trials

See Literature

Kapspargo Sprinkle Note

Not Applicable

Kapspargo Sprinkle Patient Counseling

See Literature

Kapspargo Sprinkle Generic Name & Formulations

General Description

Metoprolol succinate 25mg, 50mg, 100mg, 200mg; ext-rel caps.

Pharmacological Class

Beta-blocker.

How Supplied

Ext-rel caps—30

Generic Availability

NO

Mechanism of Action

Metoprolol is a beta1-selective (cardioselective) adrenergic receptor blocking agent. This preferential effect is not absolute, however, and at higher plasma concentrations, metoprolol also inhibits beta2-adrenoreceptors, chiefly located in the bronchial and vascular musculature. The precise mechanism for the beneficial effects of beta-blockers in heart failure has not been elucidated.

Kapspargo Sprinkle Indications

Indications

Heart failure, to reduce risk of cardiovascular mortality and heart failure hospitalization.

Kapspargo Sprinkle Dosage and Administration

Adult

Swallow whole. If difficulty swallowing cap, may open and sprinkle contents over a teaspoonful of soft food (eg, applesauce, yogurt, pudding) and consume mixture within 60mins; or, can give via NG tube (mix contents with 15mL of water first). Individualize. Initially 25mg once daily for 2 weeks. May double dose as tolerated every 2 weeks; max 200mg/day. Reduce dose if symptomatic bradycardia occurs.

Children

Not established.

Kapspargo Sprinkle Contraindications

Contraindications

Severe bradycardia. 2nd or 3rd degree heart block. Cardiogenic shock. Decompensated heart failure. Sick sinus syndrome (unless paced).

Kapspargo Sprinkle Boxed Warnings

Not Applicable

Kapspargo Sprinkle Warnings/Precautions

Warnings/Precautions

Worsening heart failure; increase diuretic and stabilize before up-titration; reduce or discontinue dose if necessary. Ischemic heart or peripheral vascular disease. 1st-degree AV block. Sinus node dysfunction. Conduction disorders (eg, Wolff-Parkinson-White). Monitor HR during therapy. Discontinue or reduce dose if severe bradycardia develops. Bronchospastic disease. Pheochromocytoma (initiate with an alpha-blocker first). Surgery. May mask signs and increased risk for hypoglycemia. Hyperthyroidism. History of severe anaphylactic reactions to allergens. Avoid abrupt cessation. Hepatic impairment. Elderly. Neonates. Pregnancy (esp. during 3rd trimester). Nursing mothers: monitor infants.

Kapspargo Sprinkle Pharmacokinetics

Absorption

  • Peak plasma concentration is attained at 10 hours after administration.

Distribution

  • About 12% of the drug is bound to human serum albumin. Metoprolol crosses the blood-brain barrier and has been reported in the CSF in a concentration 78% of the simultaneous plasma concentration.

Metabolism

  • Hepatic.

Elimination

  • Renal. Half-life: 3–7 hours.

Kapspargo Sprinkle Interactions

Interactions

May potentiate catecholamine depleting drugs (eg, reserpine, MAO inhibitors); monitor. Increased risk of bradycardia with digitalis glycosides, clonidine, diltiazem, verapamil. Increased rebound hypertension with clonidine withdrawal. May be potentiated by strong CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone). Avoid alcohol. May block epinephrine.

Kapspargo Sprinkle Adverse Reactions

Adverse Reactions

Tiredness, dizziness, depression, shortness of breath, bradycardia, hypotension, diarrhea, pruritus, rash; worsening angina, heart failure, AV block.

Kapspargo Sprinkle Clinical Trials

See Literature

Kapspargo Sprinkle Note

Not Applicable

Kapspargo Sprinkle Patient Counseling

See Literature

Kapspargo Sprinkle Generic Name & Formulations

General Description

Metoprolol succinate 25mg, 50mg, 100mg, 200mg; ext-rel caps.

Pharmacological Class

Beta-blocker.

How Supplied

Ext-rel caps—30

Generic Availability

NO

Mechanism of Action

Metoprolol is a beta1-selective (cardioselective) adrenergic receptor blocking agent. This preferential effect is not absolute, however, and at higher plasma concentrations, metoprolol also inhibits beta2-adrenoreceptors, chiefly located in the bronchial and vascular musculature. The mechanism of the antihypertensive effects of beta-blocking agents has not been elucidated. However, several possible mechanisms have been proposed: (1) competitive antagonism of catecholamines at peripheral (especially cardiac) adrenergic neuron sites, leading to decreased cardiac output; (2) a central effect leading to reduced sympathetic outflow to the periphery; and (3) suppression of renin activity.

Kapspargo Sprinkle Indications

Indications

Hypertension.

Kapspargo Sprinkle Dosage and Administration

Adult

Swallow whole. If difficulty swallowing cap, may open and sprinkle contents over a teaspoonful of soft food (eg, applesauce, yogurt, pudding) and consume mixture within 60mins; or, can give via NG tube (mix contents with 15mL of water first). Initially 25–100mg once daily, alone or with other antihypertensives. May increase at 1-week intervals; max 400mg/day.

Children

<6yrs: not established. Swallow whole. If difficulty swallowing cap, may open and sprinkle contents over a teaspoonful of soft food (eg, applesauce, yogurt, pudding) and consume mixture within 60mins; or, can give via NG tube (mix contents with 15mL of water first). ≥6yrs: initially 1mg/kg once daily (max 50mg dose). May increase at 1-week intervals; max 2mg/kg once daily.

Kapspargo Sprinkle Contraindications

Contraindications

Severe bradycardia. 2nd or 3rd degree heart block. Cardiogenic shock. Decompensated heart failure. Sick sinus syndrome (unless paced).

Kapspargo Sprinkle Boxed Warnings

Not Applicable

Kapspargo Sprinkle Warnings/Precautions

Warnings/Precautions

Worsening heart failure; increase diuretic and stabilize before up-titration; reduce or discontinue dose if necessary. Ischemic heart or peripheral vascular disease. 1st-degree AV block. Sinus node dysfunction. Conduction disorders (eg, Wolff-Parkinson-White). Monitor HR during therapy. Discontinue or reduce dose if severe bradycardia develops. Bronchospastic disease. Pheochromocytoma (initiate with an alpha-blocker first). Surgery. May mask signs and increased risk for hypoglycemia. Hyperthyroidism. History of severe anaphylactic reactions to allergens. Avoid abrupt cessation. Hepatic impairment. Elderly. Neonates. Pregnancy (esp. during 3rd trimester). Nursing mothers: monitor infants.

Kapspargo Sprinkle Pharmacokinetics

Absorption

  • Peak plasma concentration is attained at 10 hours after administration.

Distribution

  • About 12% of the drug is bound to human serum albumin. Metoprolol crosses the blood-brain barrier and has been reported in the CSF in a concentration 78% of the simultaneous plasma concentration.

Metabolism

  • Hepatic.

Elimination

  • Renal. Half-life: 3–7 hours.

Kapspargo Sprinkle Interactions

Interactions

May potentiate catecholamine depleting drugs (eg, reserpine, MAO inhibitors); monitor. Increased risk of bradycardia with digitalis glycosides, clonidine, diltiazem, verapamil. Increased rebound hypertension with clonidine withdrawal. May be potentiated by strong CYP2D6 inhibitors (eg, quinidine, fluoxetine, paroxetine, propafenone). Avoid alcohol. May block epinephrine.

Kapspargo Sprinkle Adverse Reactions

Adverse Reactions

Tiredness, dizziness, depression, shortness of breath, bradycardia, hypotension, diarrhea, pruritus, rash; worsening angina, heart failure, AV block.

Kapspargo Sprinkle Clinical Trials

See Literature

Kapspargo Sprinkle Note

Not Applicable

Kapspargo Sprinkle Patient Counseling

See Literature