Name: | Natriuretic Peptide, Brain |
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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
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Brand: | Natrecor |
Category: | Cardiac drugs |
CAS number: | 124584-08-3 |
Indication: | For the intravenous treatment of patients with acutely decompensated congestive heart failure who have dyspnea at rest or with minimal activity. |
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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 |
Drug interaction: |
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