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Identification
NameNesiritide
Accession NumberDB04899
TypeBiotech
GroupsApproved, Investigational
DescriptionNesiritide is a medication used to treat acutely decompensated congestive heart failure with dyspnea at rest or with minimal exertion (such as talk, eating or bathing). Nesiritide is the recombinant form of the 32 amino acid human B-type natriuretic peptide, which is normally produced by the ventricular myocardium.
Protein structureDb04899
Related Articles
Protein chemical formulaNot Available
Protein average weight3464.0 Da
Sequences
>DB04899: Natriuretic peptides B
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
Download FASTA Format
Synonyms
BNP
Brain natriuretic peptide 32
Natriuretic peptides B
Nesiritide recombinant
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Natrecorinjection, powder, lyophilized, for solution1.5 mg/5mLintravenousScios LLC2001-08-01Not applicableUs
Natrecorpowder for solution1.5 mgintravenousJanssen Inc2008-02-052012-08-01Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIP7WI8UL647
CAS number124584-08-3
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationFor the intravenous treatment of patients with acutely decompensated congestive heart failure who have dyspnea at rest or with minimal activity.
PharmacodynamicsNesiritide 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 actionHuman 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 isolated human arterial and venous tissue preparations that were precontracted with either endothelin-1 or the alpha-adrenergic agonist, phenylephrine. In human studies, nesiritide produced dose-dependent reductions in pulmonary capillary wedge pressure (PCWP) and systemic arterial pressure in patients with heart failure. In animals, nesiritide had no effects on cardiac contractility or on measures of cardiac electrophysiology such as atrial and ventricular effective refractory times or atrioventricular node conduction. Naturally occurring atrial natriuretic peptide (ANP), a related peptide, increases vascular permeability in animals and humans and may reduce intravascular volume. The effect of nesiritide on vascular permeability has not been studied.
Related Articles
AbsorptionAdministration of nesiritide exhibits biphasic disposition from the plasma.
Volume of distribution
  • 0.19 L/kg
Protein bindingNot Available
Metabolism

Nesiritide undergoes proteolytic cleavage of the peptide by endopeptidases, such as neutral endopeptidase, which are present on the vascular lumenal surface.

Route of eliminationHuman 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 lifeApproximately 18 minutes
Clearance
  • 9.2 mL/min/k [patients with congestive heart failure receiving IV infusion]
ToxicityNo 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionintravenous1.5 mg/5mL
Powder for solutionintravenous1.5 mg
Prices
Unit descriptionCostUnit
Natrecor 1.5 mg vial716.36USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1339210 No1997-08-052014-08-05Canada
US5114923 No1994-05-192014-05-19Us
Properties
StateSolid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
General References
  1. Jefferies JL, Price JF, Denfield SW, Chang AC, Dreyer WJ, McMahon CJ, Grenier MA, Clunie SK, Thomas A, Moffett BS, Wann TS, Smith EO, Towbin JA: Safety and efficacy of nesiritide in pediatric heart failure. J Card Fail. 2007 Sep;13(7):541-8. [PubMed:17826644 ]
  2. Maisel AS: Nesiritide: a new therapy for the treatment of heart failure. Cardiovasc Toxicol. 2003;3(1):37-42. [PubMed:12668889 ]
  3. Vichiendilokkul A, Tran A, Racine E: Nesiritide: a novel approach for acute heart failure. Ann Pharmacother. 2003 Feb;37(2):247-58. [PubMed:12549957 ]
  4. Cheng JW: Nesiritide: review of clinical pharmacology and role in heart failure management. Heart Dis. 2002 May-Jun;4(3):199-203. [PubMed:12028606 ]
  5. Bettencourt P: Brain natriuretic peptide (nesiritide) in the treatment of heart failure. Cardiovasc Drug Rev. 2002 Winter;20(1):27-36. [PubMed:12070532 ]
External Links
ATC CodesC01DX19
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (205 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Nesiritide.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Nesiritide.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Nesiritide.
AliskirenThe risk or severity of adverse effects can be increased when Nesiritide is combined with Aliskiren.
AmilorideThe risk or severity of adverse effects can be increased when Amiloride is combined with Nesiritide.
AmlodipineThe risk or severity of adverse effects can be increased when Amlodipine is combined with Nesiritide.
AmobarbitalAmobarbital may increase the hypotensive activities of Nesiritide.
Amyl NitriteThe risk or severity of adverse effects can be increased when Amyl Nitrite is combined with Nesiritide.
ApraclonidineThe risk or severity of adverse effects can be increased when Apraclonidine is combined with Nesiritide.
AripiprazoleAripiprazole may increase the hypotensive activities of Nesiritide.
AtenololThe risk or severity of adverse effects can be increased when Atenolol is combined with Nesiritide.
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Nesiritide is combined with Azilsartan medoxomil.
BarbitalBarbital may increase the hypotensive activities of Nesiritide.
BenazeprilThe risk or severity of adverse effects can be increased when Benazepril is combined with Nesiritide.
BendroflumethiazideThe risk or severity of adverse effects can be increased when Bendroflumethiazide is combined with Nesiritide.
BetaxololThe risk or severity of adverse effects can be increased when Betaxolol is combined with Nesiritide.
BisoprololThe risk or severity of adverse effects can be increased when Bisoprolol is combined with Nesiritide.
BretyliumThe risk or severity of adverse effects can be increased when Bretylium is combined with Nesiritide.
BrimonidineThe risk or severity of adverse effects can be increased when Brimonidine is combined with Nesiritide.
BumetanideThe risk or severity of adverse effects can be increased when Bumetanide is combined with Nesiritide.
CanagliflozinThe risk or severity of adverse effects can be increased when Nesiritide is combined with Canagliflozin.
CandesartanThe risk or severity of adverse effects can be increased when Candesartan is combined with Nesiritide.
CaptoprilThe risk or severity of adverse effects can be increased when Captopril is combined with Nesiritide.
CarteololThe risk or severity of adverse effects can be increased when Carteolol is combined with Nesiritide.
CarvedilolThe risk or severity of adverse effects can be increased when Carvedilol is combined with Nesiritide.
ChlorothiazideThe risk or severity of adverse effects can be increased when Chlorothiazide is combined with Nesiritide.
ChlorthalidoneThe risk or severity of adverse effects can be increased when Chlorthalidone is combined with Nesiritide.
CilazaprilThe risk or severity of adverse effects can be increased when Cilazapril is combined with Nesiritide.
ClevidipineThe risk or severity of adverse effects can be increased when Nesiritide is combined with Clevidipine.
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Nesiritide.
DapagliflozinThe risk or severity of adverse effects can be increased when Nesiritide is combined with Dapagliflozin.
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Nesiritide.
DiclofenamideThe risk or severity of adverse effects can be increased when Diclofenamide is combined with Nesiritide.
DiltiazemThe risk or severity of adverse effects can be increased when Diltiazem is combined with Nesiritide.
DinutuximabThe risk or severity of adverse effects can be increased when Nesiritide is combined with Dinutuximab.
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Nesiritide.
DoxazosinThe risk or severity of adverse effects can be increased when Doxazosin is combined with Nesiritide.
DuloxetineNesiritide may increase the orthostatic hypotensive activities of Duloxetine.
EmpagliflozinThe risk or severity of adverse effects can be increased when Nesiritide is combined with Empagliflozin.
EnalaprilThe risk or severity of adverse effects can be increased when Enalapril is combined with Nesiritide.
EplerenoneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Nesiritide.
EprosartanThe risk or severity of adverse effects can be increased when Eprosartan is combined with Nesiritide.
EsmololThe risk or severity of adverse effects can be increased when Esmolol is combined with Nesiritide.
Etacrynic acidThe risk or severity of adverse effects can be increased when Etacrynic acid is combined with Nesiritide.
FelodipineThe risk or severity of adverse effects can be increased when Felodipine is combined with Nesiritide.
FosinoprilThe risk or severity of adverse effects can be increased when Fosinopril is combined with Nesiritide.
FurosemideThe risk or severity of adverse effects can be increased when Furosemide is combined with Nesiritide.
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Nesiritide.
HexobarbitalHexobarbital may increase the hypotensive activities of Nesiritide.
HydralazineThe risk or severity of adverse effects can be increased when Hydralazine is combined with Nesiritide.
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Hydrochlorothiazide is combined with Nesiritide.
IndapamideThe risk or severity of adverse effects can be increased when Indapamide is combined with Nesiritide.
IrbesartanThe risk or severity of adverse effects can be increased when Irbesartan is combined with Nesiritide.
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Isosorbide Dinitrate is combined with Nesiritide.
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Isosorbide Mononitrate is combined with Nesiritide.
IsoxsuprineThe risk or severity of adverse effects can be increased when Nesiritide is combined with Isoxsuprine.
IsradipineThe risk or severity of adverse effects can be increased when Isradipine is combined with Nesiritide.
LabetalolThe risk or severity of adverse effects can be increased when Labetalol is combined with Nesiritide.
LevobunololThe risk or severity of adverse effects can be increased when Levobunolol is combined with Nesiritide.
LevodopaNesiritide may increase the orthostatic hypotensive activities of Levodopa.
LisinoprilThe risk or severity of adverse effects can be increased when Lisinopril is combined with Nesiritide.
LosartanThe risk or severity of adverse effects can be increased when Losartan is combined with Nesiritide.
MannitolThe risk or severity of adverse effects can be increased when Mannitol is combined with Nesiritide.
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Nesiritide.
MethazolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Nesiritide.
MethohexitalMethohexital may increase the hypotensive activities of Nesiritide.
MethyclothiazideThe risk or severity of adverse effects can be increased when Methyclothiazide is combined with Nesiritide.
MethyldopaThe risk or severity of adverse effects can be increased when Methyldopa is combined with Nesiritide.
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Nesiritide.
MetipranololThe risk or severity of adverse effects can be increased when Metipranolol is combined with Nesiritide.
MetolazoneThe risk or severity of adverse effects can be increased when Metolazone is combined with Nesiritide.
MetoprololThe risk or severity of adverse effects can be increased when Metoprolol is combined with Nesiritide.
MinoxidilThe risk or severity of adverse effects can be increased when Minoxidil is combined with Nesiritide.
MoexiprilThe risk or severity of adverse effects can be increased when Moexipril is combined with Nesiritide.
NadololThe risk or severity of adverse effects can be increased when Nadolol is combined with Nesiritide.
NebivololThe risk or severity of adverse effects can be increased when Nebivolol is combined with Nesiritide.
NicardipineThe risk or severity of adverse effects can be increased when Nicardipine is combined with Nesiritide.
NicorandilNicorandil may increase the hypotensive activities of Nesiritide.
NifedipineThe risk or severity of adverse effects can be increased when Nifedipine is combined with Nesiritide.
NimodipineThe risk or severity of adverse effects can be increased when Nimodipine is combined with Nesiritide.
NisoldipineThe risk or severity of adverse effects can be increased when Nisoldipine is combined with Nesiritide.
NitroglycerinThe risk or severity of adverse effects can be increased when Nitroglycerin is combined with Nesiritide.
NitroprussideThe risk or severity of adverse effects can be increased when Nitroprusside is combined with Nesiritide.
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Nesiritide.
PapaverineThe risk or severity of adverse effects can be increased when Papaverine is combined with Nesiritide.
PenbutololThe risk or severity of adverse effects can be increased when Penbutolol is combined with Nesiritide.
PentobarbitalPentobarbital may increase the hypotensive activities of Nesiritide.
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Nesiritide.
PhenobarbitalPhenobarbital may increase the hypotensive activities of Nesiritide.
PindololThe risk or severity of adverse effects can be increased when Pindolol is combined with Nesiritide.
PrazosinThe risk or severity of adverse effects can be increased when Prazosin is combined with Nesiritide.
PrimidonePrimidone may increase the hypotensive activities of Nesiritide.
PropranololThe risk or severity of adverse effects can be increased when Propranolol is combined with Nesiritide.
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Nesiritide.
QuinaprilThe risk or severity of adverse effects can be increased when Quinapril is combined with Nesiritide.
RamiprilThe risk or severity of adverse effects can be increased when Ramipril is combined with Nesiritide.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Nesiritide.
RiociguatThe risk or severity of adverse effects can be increased when Nesiritide is combined with Riociguat.
RisperidoneNesiritide may increase the hypotensive activities of Risperidone.
SecobarbitalSecobarbital may increase the hypotensive activities of Nesiritide.
SotalolThe risk or severity of adverse effects can be increased when Sotalol is combined with Nesiritide.
SpironolactoneThe risk or severity of adverse effects can be increased when Spironolactone is combined with Nesiritide.
TelmisartanThe risk or severity of adverse effects can be increased when Telmisartan is combined with Nesiritide.
TerazosinThe risk or severity of adverse effects can be increased when Terazosin is combined with Nesiritide.
ThiamylalThiamylal may increase the hypotensive activities of Nesiritide.
ThiopentalThiopental may increase the hypotensive activities of Nesiritide.
TimololThe risk or severity of adverse effects can be increased when Timolol is combined with Nesiritide.
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Nesiritide.
TorasemideThe risk or severity of adverse effects can be increased when Torasemide is combined with Nesiritide.
TrandolaprilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Nesiritide.
TriamtereneThe risk or severity of adverse effects can be increased when Triamterene is combined with Nesiritide.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Nesiritide.
VerapamilThe risk or severity of adverse effects can be increased when Verapamil is combined with Nesiritide.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Protein kinase activity
Specific Function:
Receptor for the atrial natriuretic peptide NPPA/ANP and the brain natriuretic peptide NPPB/BNP which are potent vasoactive hormones playing a key role in cardiovascular homeostasis. Has guanylate cyclase activity upon binding of the ligand.
Gene Name:
NPR1
Uniprot ID:
P16066
Molecular Weight:
118918.11 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transmembrane signaling receptor activity
Specific Function:
Receptor for the C-type natriuretic peptide NPPC/CNP hormone. Has guanylate cyclase activity upon binding of its ligand. May play a role in the regulation of skeletal growth.
Gene Name:
NPR2
Uniprot ID:
P20594
Molecular Weight:
117020.97 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Peptide hormone binding
Specific Function:
Receptor for the natriuretic peptide hormones, binding with similar affinities atrial natriuretic peptide NPPA/ANP, brain natriuretic peptide NPPB/BNP, and C-type natriuretic peptide NPPC/CNP. May function as a clearance receptor for NPPA, NPPB and NPPC, regulating their local concentrations and effects. May regulate diuresis, blood pressure and skeletal development. Does not have guanylate cyc...
Gene Name:
NPR3
Uniprot ID:
P17342
Molecular Weight:
59807.34 Da
Comments
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Drug created on October 21, 2007 16:23 / Updated on August 17, 2016 12:24