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
Molecular 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
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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.

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.

Side effects

Common side effects include:

• Low blood pressure (11% of patients)
• Headache
• Nausea
• Slow heart rate
• Kidney failure

More rare side effects include:

• Confusion
• Paresthesia
• Somnolence
• Tremor

References

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.[1]

External links

• Natrecor.com