Detailed description page of THPdb

Details of Th1109 which contains 1 entries.

Entry 1
(1) Primary information
ID 1530
ThPP ID Th1109
Therapeutic Peptide/Protein Name Nesiritide
Sequence SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH view full sequnce in fasta
Functional Classification Ib
Molecular Weight 3464
Chemical Formula N.A.
Isoelectric Point N.A.
Hydrophobicity N.A.
Melting Point (℃) N.A.
Half Life Approx. 18 mins
Description Recombinant, 32 amino acid human B-type natriuretic peptide, which is normally produced by the ventricular myocardium. Nesiritide is a medication used to treat acutely decompensated congestive heart failure with dyspnea at rest or with minimal exertion.
Indication/Disease For the intravenous treatment of patients with acutely decompensated congestive heart failure who have dyspnea at rest or with minimal activity.
Pharmacodynamics 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 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.
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.
Metabolism Nesiritide undergoes proteolytic cleavage of the peptide by endopeptidases, such as neutral endopeptidase, which are present on the vascular lumenal surface.
Absorption Administration of nesiritide exhibits biphasic disposition from the plasma.
Volume of Distribution 0.19 L/kg
Clearance 9.2 mL/min/k [patients with congestive heart failure receiving IV infusion]
Categories N.A.
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction N.A.
Target N.A.
Information of corresponding available drug in the market
Brand Name NATRECOR
Company Scios unit of Johnson & Johnson,
Brand Discription NATRECOR (nesiritide) is a sterile, purified preparation of human B-type natriuretic peptide (hBNP), and is manufactured from E. coli using recombinant DNA technology. Nesiritide has a molecular weight of 3464 g/mol and an empirical formula of C143H244N50O42S4. Nesiritide has the same 32 amino acid sequence as the endogenous peptide, which is produced by the ventricular myocardiu
Prescribed for NATRECOR (nesiritide) is indicated for the treatment of patients with acutely decompensated heart failure who have dyspnea at rest or with minimal activity. In this population, the use of NATRECOR reduced pulmonary capillary wedge pressure and improved short term (3 hours) symptoms of dyspnea.
Chemical Name N.A.
Formulation NATRECOR is formulated as the citrate salt of rhBNP, and is provided in a sterile, single-use vial. Each 1.5 mg vial contains a white- to off-white lyophilized powder for intravenous (IV) administration after reconstitution. The quantitative composition of the lyophilized drug per vial is: nesiritide 1.58 mg, citric acid monohydrate 2.1 mg, mannitol 20.0 mg, and sodium citrate dihydrate 2.94 mg
Physcial Appearance White- to off-white lyophilized powde
Route of Administration Intravenous
Recommended Dosage IV bolus of 2 mcg/kg followed by a continuous infusion of 0.01 mcg/kg/min
Contraindication NATRECOR is contraindicated in patients with: Persistent systolic blood pressure < 100 mm Hg prior to therapy because of an increased risk of symptomatic hypotension Known hypersensitivity to any of its components.
Side Effects Hypotension
Useful Link http://www.rxlist.com/natrecor-drug.htm https://en.wikipedia.org/wiki/Nesiritide http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=13531 http://www.fda.gov/Safety/MedWatch/SafetyInformation/ucm169897.htm
PubMed ID 17826644, 12668889, 12549957, 12070532, 12028606
3-D Structure N.A.

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

(1) Primary information
Entry 1
ID	1530
ThPP ID	Th1109
Therapeutic Peptide/Protein Name	Nesiritide
Sequence	SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH view full sequnce in fasta
Functional Classification	Ib
Molecular Weight	3464
Chemical Formula	N.A.
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	Approx. 18 mins
Description	Recombinant, 32 amino acid human B-type natriuretic peptide, which is normally produced by the ventricular myocardium. Nesiritide is a medication used to treat acutely decompensated congestive heart failure with dyspnea at rest or with minimal exertion.
Indication/Disease	For the intravenous treatment of patients with acutely decompensated congestive heart failure who have dyspnea at rest or with minimal activity.
Pharmacodynamics	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 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.
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.
Metabolism	Nesiritide undergoes proteolytic cleavage of the peptide by endopeptidases, such as neutral endopeptidase, which are present on the vascular lumenal surface.
Absorption	Administration of nesiritide exhibits biphasic disposition from the plasma.
Volume of Distribution	0.19 L/kg
Clearance	9.2 mL/min/k [patients with congestive heart failure receiving IV infusion]
Categories	N.A.
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	N.A.
Target	N.A.
Information of corresponding available drug in the market
Brand Name	NATRECOR
Company	Scios unit of Johnson & Johnson,
Brand Discription	NATRECOR (nesiritide) is a sterile, purified preparation of human B-type natriuretic peptide (hBNP), and is manufactured from E. coli using recombinant DNA technology. Nesiritide has a molecular weight of 3464 g/mol and an empirical formula of C143H244N50O42S4. Nesiritide has the same 32 amino acid sequence as the endogenous peptide, which is produced by the ventricular myocardiu
Prescribed for	NATRECOR (nesiritide) is indicated for the treatment of patients with acutely decompensated heart failure who have dyspnea at rest or with minimal activity. In this population, the use of NATRECOR reduced pulmonary capillary wedge pressure and improved short term (3 hours) symptoms of dyspnea.
Chemical Name	N.A.
Formulation	NATRECOR is formulated as the citrate salt of rhBNP, and is provided in a sterile, single-use vial. Each 1.5 mg vial contains a white- to off-white lyophilized powder for intravenous (IV) administration after reconstitution. The quantitative composition of the lyophilized drug per vial is: nesiritide 1.58 mg, citric acid monohydrate 2.1 mg, mannitol 20.0 mg, and sodium citrate dihydrate 2.94 mg
Physcial Appearance	White- to off-white lyophilized powde
Route of Administration	Intravenous
Recommended Dosage	IV bolus of 2 mcg/kg followed by a continuous infusion of 0.01 mcg/kg/min
Contraindication	NATRECOR is contraindicated in patients with: Persistent systolic blood pressure < 100 mm Hg prior to therapy because of an increased risk of symptomatic hypotension Known hypersensitivity to any of its components.
Side Effects	Hypotension
Useful Link	http://www.rxlist.com/natrecor-drug.htm https://en.wikipedia.org/wiki/Nesiritide http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=13531 http://www.fda.gov/Safety/MedWatch/SafetyInformation/ucm169897.htm
PubMed ID	17826644, 12668889, 12549957, 12070532, 12028606
3-D Structure	N.A.