AMRINONE LACTATE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for AMRINONE LACTATE (AMRINONE LACTATE).

How it works

Selective phosphodiesterase III (PDE3) inhibitor; increases intracellular cAMP and calcium in cardiac and vascular smooth muscle, resulting in positive inotropy and vasodilation.

What the body does with it

Metabolism	Hepatic metabolism via acetylation and glucuronidation; approximately 10-20% undergoes N-acetylation to N-acetylamrinone, with glucuronide conjugation as the primary route.
Excretion	Primarily renal (30-40% unchanged), with biliary/fecal excretion as a minor pathway (about 10-15% total).
Half-life	3.6 hours in adults with normal renal function; may be prolonged in congestive heart failure or renal impairment.
Protein binding	10-20% bound to plasma proteins (albumin).
Volume of Distribution	1.2-1.6 L/kg, indicating extensive extravascular distribution.
Bioavailability	Not orally available (inactive); intravenous route only.
Onset of Action	Intravenous: 2-5 minutes.
Duration of Action	Approximately 30-60 minutes after a single IV dose; clinical effects persist for several hours due to active metabolites.

Classification & Brands

Dosing & administration

Intravenous loading dose: 0.75 mg/kg over 2-3 minutes; followed by continuous IV infusion of 5-10 mcg/kg/min. Maximum single dose: 3 mg/kg per 24 hours.

Dosage form	INJECTABLE
Renal impairment	No specific adjustment defined; however, caution in severe renal impairment due to potential accumulation. GFR <30 mL/min: consider dose reduction or extended intervals.
Liver impairment	Reduce dose by 25-50% in Child-Pugh class B or C due to decreased clearance. Monitor closely for toxicity.
Pediatric use	Children: IV loading dose 0.75 mg/kg over 2-3 minutes; maintenance infusion initially 5 mcg/kg/min, titrate up to 10 mcg/kg/min. Maximum total dose: 10 mg/kg per 24 hours.
Geriatric use	Elderly patients may have reduced clearance; start at lower end of dosing range (e.g., 5 mcg/kg/min) and titrate slowly based on response and renal function.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for AMRINONE LACTATE (AMRINONE LACTATE).

Breastfeeding

No human data on excretion in breast milk. M/P ratio unknown. Due to potential for serious adverse reactions (e.g., cardiotoxicity) in nursing infants, advise against breastfeeding during therapy.

Teratogenic Risk

FDA Pregnancy Category C. Animal studies have shown teratogenic effects (skeletal and cardiovascular anomalies) at doses 1-2 times the human therapeutic dose. In first trimester, potential for fetal harm cannot be ruled out. Second and third trimester: limited human data; no documented malformations, but risk of fetal tachycardia and hypotension due to maternal hemodynamic effects. Use only if potential benefit justifies risk.

Warnings & precautions

■ FDA Black Box Warning

Increased mortality and risk of arrhythmias (including ventricular tachycardia/fibrillation) with prolonged use in heart failure; short-term use only recommended.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to amrinone or bisulfites, severe aortic or pulmonic valvular disease (e.g., aortic stenosis) due to increased cardiac output across obstruction, hypertrophic cardiomyopathy with outflow obstruction.

Clinical Precautions

Precautions	Arrhythmias (especially ventricular), hypotension, thrombocytopenia (dose-dependent), hepatotoxicity, hypersensitivity reactions, renal impairment monitoring, electrolyte imbalances.
Food/Dietary	Avoid grapefruit products (grapefruit juice, whole grapefruit) as they may inhibit CYP3A4 metabolism, increasing drug levels and risk of toxicity.

Clinical Tips & Counseling

Drug interactions

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AMRINONE LACTATE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for AMRINONE LACTATE (AMRINONE LACTATE).

How it works

Selective phosphodiesterase III (PDE3) inhibitor; increases intracellular cAMP and calcium in cardiac and vascular smooth muscle, resulting in positive inotropy and vasodilation.

What the body does with it

Metabolism	Hepatic metabolism via acetylation and glucuronidation; approximately 10-20% undergoes N-acetylation to N-acetylamrinone, with glucuronide conjugation as the primary route.
Excretion	Primarily renal (30-40% unchanged), with biliary/fecal excretion as a minor pathway (about 10-15% total).
Half-life	3.6 hours in adults with normal renal function; may be prolonged in congestive heart failure or renal impairment.
Protein binding	10-20% bound to plasma proteins (albumin).
Volume of Distribution	1.2-1.6 L/kg, indicating extensive extravascular distribution.
Bioavailability	Not orally available (inactive); intravenous route only.
Onset of Action	Intravenous: 2-5 minutes.
Duration of Action	Approximately 30-60 minutes after a single IV dose; clinical effects persist for several hours due to active metabolites.

Classification & Brands

Dosing & administration

Intravenous loading dose: 0.75 mg/kg over 2-3 minutes; followed by continuous IV infusion of 5-10 mcg/kg/min. Maximum single dose: 3 mg/kg per 24 hours.

Dosage form	INJECTABLE
Renal impairment	No specific adjustment defined; however, caution in severe renal impairment due to potential accumulation. GFR <30 mL/min: consider dose reduction or extended intervals.
Liver impairment	Reduce dose by 25-50% in Child-Pugh class B or C due to decreased clearance. Monitor closely for toxicity.
Pediatric use	Children: IV loading dose 0.75 mg/kg over 2-3 minutes; maintenance infusion initially 5 mcg/kg/min, titrate up to 10 mcg/kg/min. Maximum total dose: 10 mg/kg per 24 hours.
Geriatric use	Elderly patients may have reduced clearance; start at lower end of dosing range (e.g., 5 mcg/kg/min) and titrate slowly based on response and renal function.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for AMRINONE LACTATE (AMRINONE LACTATE).

Breastfeeding

No human data on excretion in breast milk. M/P ratio unknown. Due to potential for serious adverse reactions (e.g., cardiotoxicity) in nursing infants, advise against breastfeeding during therapy.

Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

Increased mortality and risk of arrhythmias (including ventricular tachycardia/fibrillation) with prolonged use in heart failure; short-term use only recommended.

Side Effect Profile

Serious Effects

Absolute Contraindications

Clinical Precautions

Precautions	Arrhythmias (especially ventricular), hypotension, thrombocytopenia (dose-dependent), hepatotoxicity, hypersensitivity reactions, renal impairment monitoring, electrolyte imbalances.
Food/Dietary	Avoid grapefruit products (grapefruit juice, whole grapefruit) as they may inhibit CYP3A4 metabolism, increasing drug levels and risk of toxicity.

Clinical Tips & Counseling

Drug interactions

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Clinical Pearls	Amrinone lactate, a phosphodiesterase III inhibitor with positive inotropic and vasodilator effects, is used for short-term management of acute decompensated heart failure. Monitor for thrombocytopenia (dose-dependent, reversible) and hypotension. Dose adjustment required in renal impairment. Contraindicated in severe aortic or pulmonic valvular disease.
Patient Advice	This medication is given intravenously in a hospital setting for acute heart failure. · Report any unusual bleeding or bruising, as it can lower platelet counts. · You may feel dizzy or lightheaded due to blood pressure lowering effects; avoid sudden position changes. · Do not consume grapefruit or grapefruit juice during treatment due to potential interaction.