Nesiritide

Nesiritide
Clinical data

AHFS/Drugs.com	monograph
Routes of administration	IV only
Identifiers
CAS Number	124584-08-3^N
ATC code	C01DX19 (WHO)
PubChem	CID 16134381
DrugBank	DB04899^N
ChemSpider	24603113^N
UNII	P7WI8UL647^N
ChEMBL	CHEMBL1201668^N
Chemical data
Formula	C₁₄₃H₂₄₄N₅₀O₄₂S₄
Molar mass	3464 g/mol
SMILES CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCCNC(=N)N)CC(=O)O)CCSC)CCCCN)CCCNC(=N)N)CC2=CC=CC=C2)NC(=O)CNC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CO)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC4=CNC=N4)C(=O)O)CC(C)C)CO)CO)CO)CO
InChI InChI=1S/C143H244N50O42S4/c1-13-76(10)112-137(232)189-99(68-199)131(226)188-98(67-198)130(225)187-97(66-197)129(224)186-96(65-196)117(212)166-59-105(202)169-90(52-72(2)3)114(209)163-61-107(204)171-100(132(227)177-83(32-19-22-44-146)124(219)190-111(75(8)9)136(231)184-91(53-73(4)5)127(222)175-84(34-24-46-159-141(151)152)121(216)174-85(35-25-47-160-142(153)154)122(217)185-94(139(234)235)55-78-57-157-71-167-78)69-238-239-70-101(172-108(205)62-165-116(211)95(64-195)170-106(203)60-162-113(208)87(38-39-103(148)200)181-135(230)110(74(6)7)191-126(221)89(41-51-237-12)179-120(215)82(31-18-21-43-145)180-134(229)102-37-27-49-193(102)138(233)79(147)63-194)133(228)182-92(54-77-28-15-14-16-29-77)115(210)164-58-104(201)168-80(33-23-45-158-140(149)150)118(213)173-81(30-17-20-42-144)119(214)178-88(40-50-236-11)123(218)183-93(56-109(206)207)128(223)176-86(125(220)192-112)36-26-48-161-143(155)156/h14-16,28-29,57,71-76,79-102,110-112,194-199H,13,17-27,30-56,58-70,144-147H2,1-12H3,(H2,148,200)(H,157,167)(H,162,208)(H,163,209)(H,164,210)(H,165,211)(H,166,212)(H,168,201)(H,169,202)(H,170,203)(H,171,204)(H,172,205)(H,173,213)(H,174,216)(H,175,222)(H,176,223)(H,177,227)(H,178,214)(H,179,215)(H,180,229)(H,181,230)(H,182,228)(H,183,218)(H,184,231)(H,185,217)(H,186,224)(H,187,225)(H,188,226)(H,189,232)(H,190,219)(H,191,221)(H,192,220)(H,206,207)(H,234,235)(H4,149,150,158)(H4,151,152,159)(H4,153,154,160)(H4,155,156,161)/t76-,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,110-,111-,112-/m0/s1^N Key:HPNRHPKXQZSDFX-OAQDCNSJSA-N^N
^NY (what is this?) (verify)

Nesiritide (Natrecor) is the recombinant form of the 32 amino acid human B-type natriuretic peptide, which is normally produced by the ventricular myocardium. 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.

Neseritide was believed initially to be beneficial for acute decompensated congestive heart failure. It received approval from the United States' Food and Drug Administration for this purpose in 2001 after initial non-approval. In July 2011 the results of the largest study so far for nesiritide was published in The New England Journal of Medicine; it showed that nesiritide was not associated with a change in mortality or re-hospitalizations.^[1]

Administration

Nesiritide is only administered intravenously, usually by bolus, followed by IV infusion. For most adults and the elderly, a normal dosage is 2 µg/kg followed by a continuous IV infusion of 0.01 µg/kg/min. This may be increased every three hours for a maximum of 0.03 µg/kg/min.

Controversy

In 2005, after several academic papers ^[2]^[3] on the efficacy and side effects of Nesiritide, Johnson & Johnson met with the FDA and altered its stated plans for the drug and agreed to revise its labeling.^[4]^[5]

Heart doctors at the Cleveland Clinic then voted unanimously not to permit the prescription of the drug to its patients.^[6] Following this, the United States Department of Justice announced an inquiry into the marketing of the drug.^[7]

Side effects

Common side effects include:

More rare side effects include:

References

↑ O'Connor (2011). "Effect of nesiritide in patients with acute decompensated heart failure". New England Journal of Medicine 365 (32): 32–43. doi:10.1056/NEJMoa1100171. PMID 21732835. |access-date= requires |url= (help)
↑ http://www.biomedcentral.com/content/pdf/cc4945.pdf
↑ http://circ.ahajournals.org/content/111/12/1487.short
↑ http://www.nytimes.com/2005/05/17/business/the-marketing-and-success-of-natrecor.html?_r=0
↑ http://query.nytimes.com/gst/fullpage.html?res=9D0CE4D81630F937A35756C0A9639C8B63
↑ http://query.nytimes.com/gst/fullpage.html?res=9D0CE4D81630F937A35756C0A9639C8B63
↑ http://www.nytimes.com/2005/07/21/business/us-looking-at-marketing-by-johnson-johnson.html
↑ https://online.epocrates.com/noFrame/showPage.do?method=drugs&MonographId=2511&ActiveSectionId=5

Science or Fiction: Use of Nesiritide as a First-Line Agent? John A. Noviasky, Pharm.D., Michael Kelberman, M.D., Karen M. Whalen, B.S., Roy Guharoy, Pharm.D., William Darko, Pharm.D.

External links

Natrecor.com

Vasodilators used in cardiac diseases (C01D)

Nitrovasodilators	Nitroglycerin # Isosorbide dinitrate # Isosorbide mononitrate Linsidomine Molsidomine Nicorandil Pentaerythritol tetranitrate Propatylnitrate Tenitramine Trolnitrate

Quinolone vasodilators	Flosequinan^‡

Others	Benziodarone Carbocromen Cinepazet Cloridarol Dilazep Efloxate Etafenone Gapicomine Heptaminol Hexobendine Imolamine Itramin tosilate Levosimendan Nesiritide Nicorandil Oxyfedrine Pimobendan Prenylamine Serelaxin Trapidil

^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

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