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QuickView for nesiritide (compound)


DrugBank
Identification
Name: Natriuretic Peptide, Brain
Name (isomeric): DB04899
Drug Type: biotech
Description: A PEPTIDE that is secreted by the BRAIN and the HEART ATRIA, stored mainly in cardiac ventricular MYOCARDIUM. It can cause NATRIURESIS; DIURESIS; VASODILATION; and inhibits secretion of RENIN and ALDOSTERONE. It improves heart function. It contains 32 AMINO ACIDS.
Synonyms:
Natriuretic peptides B; BNP; Brain natriuretic peptide 32
Brand: Natrecor
Category: Cardiac drugs
CAS number: 124584-08-3
Pharmacology
Indication: For the intravenous treatment of patients with acutely decompensated congestive heart failure who have dyspnea at rest or with minimal activity.
Pharmacology: Nesiritide works to facilitate cardiovascular fluid homeostasis through counterregulation of the renin-angiotensin-aldoesterone system, stimulating cyclic guanosine monophosphate, leading to smooth muscle cell relaxation. In simpler terms, it promotes vasodilation, natriuresis, and diuresis.
Mechanism of Action:
Human BNP binds to the particulate guanylate cyclase receptor of vascular smooth muscle and endothelial cells, leading to increased intracellular concentrations of guanosine 3'5'-cyclic monophosphate (cGMP) and smooth muscle cell relaxation. Cyclic GMP serves as a second messenger to dilate veins and arteries. Nesiritide has been shown to relax iso...
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Absorption: Administration of nesiritide exhibits biphasic disposition from the plasma.
Biotransformation: Nesiritide undergoes proteolytic cleavage of the peptide by endopeptidases, such as neutral endopeptidase, which are present on the vascular lumenal surface.
Route of elimination: Human BNP is cleared from the circulation via the following three independent mechanisms, in order of decreasing importance: 1) binding to cell surface clearance receptors with subsequent cellular internalization and lysosomal proteolysis; 2) proteolytic cleavage of the peptide by endopeptidases, such as neutral endopeptidase, which are present on the vascular lumenal surface; and 3) renal filtration.
Half Life: Approximately 18 minutes
Clearance: 9.2 mL/min/k [patients with congestive heart failure receiving IV infusion]
Toxicity: No data are available with respect to overdosage in humans. The expected reaction would be excessive hypotension, which should be treated with drug discontinuation or reduction and appropriate measures.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
TreprostinilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

Targets