Nesiritide 124584-08-3
114471-18-0
Nesiritide (Natrecor) 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. 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.
Administration
Nesiritide is only administered intravenously, usually by bolus, followed by IV infusion. For most adults and the elderly, a normal dosage is 2 micrograms/kilogram followed by a continuous IV infusion of 0. 01 mcg/kg/minute. This may be increased every three hours for a maximum of 0. 03 mcg/kg/min.
Side effects
Common side effects include:*Low blood pressure (11% of patients)*Headache *Nausea*Slow heart rateMore rare side effects include:*Confusion*Paresthesia*Somnolence*Tremors
Recommendations for use (as of 7/13/2005)
There have been several meta-analysis which have identified issues of increased mortality and increased renal dysfunction with use of nesiritide compared to usual therapy. As a result, the company which manufactures nesiritide (Scios), consulted with Dr E Braunwald to develop recommendations for use. They are as follows:*The use of nesiritide should be strictly limited to patients presenting to the hospital with acutely decompensated heart failure who have dyspnea at rest, as were the patients in the largest trial that led to approval of the drug (VMAC). Physicians considering the use of nesiritide should consider its efficacy in reducing dyspnea, the possible risks of the drug (refers to meta-analysis), and the availability of alternate therapies to relieve the symptoms of congestive heart failure. *Nesiritide should not be used to replace diuretics. Furthermore, because sufficient evidence is not currently available to demonstrate benefit for the applications listed below, **NESIRITIDE SHOULD NOT BE USED: **for intermittent outpatient infusion**for scheduled repetitive use**to improve renal function**to enhance diuresis
Notes
| Systematic (IUPAC) name: | |
|---|---|
| Nesiritide CAS number: | 124584-08-3 114471-18-0 |
| ATC code: | C01DX19 |
| PubChem: | 16134381 |
| DrugBank: | |
| Formula: | C143H244O42N50 |
| Molecular mass: | 3464 gm/mol g/mol |
| Nesiritide Assay/Purity: | Typically NLT 98% |
