Trade Names:Natrecor- Powder for injection, lyophilized 1.58 mg
Binds to the particulate guanylate cyclase receptor of vascular smooth muscle and endothelial cells, leading to dose-dependent reductions in pulmonary capillary wedge pressure and systemic arterial pressure in patients with heart failure.
The mean Vd of the central compartment is estimated to be 0.073 L/kg and the mean Cl is approximately 9.2 mL/min/kg. Following IV administration to patients with CHF, disposition from the plasma is biphasic.
The mean terminal elimination t ½ is approximately 18 min and is associated with approximately 2/3 of the AUC. The mean initial elimination phase is about 2 min.
With administration of the recommended dosing regimen of 2 mcg/kg IV bolus followed by 0.01 mcg/kg/min, 60% of the 3-h effect on pulmonary capillary wedge pressure reduction is achieved within 15 min after the bolus. Approximately 70% of the 3-h effect on standing BP reduction is reached within 15 min.
95% of the 3-h effect is achieved within 1 h.
The pharmacodynamic t ½ of the onset and offset of the hemodynamic effect is longer than predicted by the pharmacokinetic t ½ .
Treatment of patients with acutely decompensated CHF who have dyspnea at rest or with minimal activity.
Primary treatment for patients with cardiogenic shock; systolic BP less than 90 mm Hg; hypersensitivity to any component of the product.
IV Recommended dose is 2 mcg/kg IV bolus over 60 sec followed by continuous infusion at a dose of 0.01 mcg/kg/min. If hypotension occurs during administration, reduce or discontinue the dose and start other measures to support BP.
Store vials at controlled room temperature (68° to 77°F) in original carton. Use reconstituted solution immediately. If immediate use is not possible, the reconstituted solution may be stored for up to 24 h in refrigerator (36° to 46°F) or at controlled room temperature.
Coadministration may cause an increase in symptomatic hypotension.
Physically and chemically incompatible with injectable formulations of bumetanide, enalaprilat, ethacrynate sodium, furosemide, hydralazine, heparin, and insulin. These agents should not be administered as infusions with nesiritide through the same IV catheter. Sodium metabisulfite preservative is incompatible with nesiritide. Since nesiritide binds with heparin, do not administer through a central heparin-coated catheter.
None well documented.
Hypotension (symptomatic and asymptomatic) (11%); ventricular tachycardia (3%); nonsustained ventricular tachycardia (3%); ventricular extrasystoles (3%); angina pectoris; bradycardia; tachycardia; atrial fibrillation; AV node conduction abnormalities.
Headache (8%); insomnia; dizziness (3%); anxiety (3%); confusion; paresthesia; somnolence; tremor.
Sweating; pruritus; rash.
Nausea (4%); vomiting.
Increased cough; hemoptysis; apnea.
Abdominal pain; back pain; catheter pain; fever; injection site reaction; increased creatinine; leg cramps.
Category C .
Safety and efficacy not established.
Renal function may be affected in susceptible patients; azotemia may occur in patients with severe heart failure whose renal function may depend on the activity of the renin-angiotensin-aldosterone system.
Avoid administration in patients suspected of having or known to have low cardiac filling pressures. Not recommended for use in patients for whom vasodilating agents are not approved (eg, significant valvular stenosis; restrictive or obstructive cardiomyopathy).
May occur at recommended or adjustable doses.
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