Fosinopril

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Fosinopril
Clinical data
Trade namesMonopril
AHFS/Drugs.comMonograph
MedlinePlusa692020
Pregnancy
category
  • AU: D
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • US: WARNING[1]
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability~36%
Protein binding87% (fosinoprilat)
Metabolismliver, GIT mucosa (to fosinoprilat)
Elimination half-life12 hours (fosinoprilat)
Excretionkidney
Identifiers
  • (2S,4S)-4-cyclohexyl-1-[2-[hydroxy(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylic acid
JSmol)
  • O=C(CP(=O)(CCCCc1ccccc1)OC(OC(=O)CC)C(C)C)N2C[C@@H](C[C@H]2C(O)=O)C3CCCCC3
  • InChI=1S/C30H46NO7P/c1-4-28(33)37-30(22(2)3)38-39(36,18-12-11-15-23-13-7-5-8-14-23)21-27(32)31-20-25(19-26(31)29(34)35)24-16-9-6-10-17-24/h5,7-8,13-14,22,24-26,30H,4,6,9-12,15-21H2,1-3H3,(H,34,35)/t25-,26+,30?,39-/m1/s1 checkY
  • Key:BIDNLKIUORFRQP-YYTCENNOSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Fosinopril is an

Bristol-Myers Squibb
under the trade name Monopril. Fosinopril is a cascading pro-drug. The special niche for the medication that differentiates it from the other members of the ACE Inhibitor drug class is that was specifically developed for the use for patients with renal impairment. This was through manipulation of the metabolism and excretion, and is seen that fifty percent of the drug is hepatobiliary cleared, which can compensate for diminished renal clearance. The remaining fifty percent is excreted in urine. It does not need dose adjustment.

It was patented in 1980 and approved for medical use in 1991.[3]

Medical uses

In

myocardium[6] which reduces the functionality of the heart.[5]

In heart failure patients, fosinopril increases exercise tolerance and lowers the frequency of events associated with worsening heart failure, such as

dyspnea, the need for supplemental diuretics, fatigue, and hospitalizations.[7]

Chemistry

Unlike other ACE inhibitors that are primarily excreted by the kidneys, fosinopril is eliminated from the body by both

hepatic pathways.[8] This characteristic of fosinopril makes the drug a safer choice than other ACE inhibitors for heart failure patients with impaired kidney function resulting from poor perfusion[9] as fosinopril can still be eliminated by the liver, preventing accumulation of the drug in the body.[8]

Fosinopril is de-esterified by the liver or gastrointestinal mucosa and is converted to its active form, fosinoprilat.

peripheral vascular resistance, decreases afterload, and decreases blood pressure,[5]
thus helping to alleviate the negative effects of AII on cardiac performance.

References

  1. FDA
    . Retrieved 22 Oct 2023.
  2. PMID 18458262
    .
  3. ISBN 9783527607495
    .
  4. ISBN 978-0-7216-0240-0
    .
  5. ^
    ISBN 978-0-07-160405-5
    .
  6. PMID 8301670
    .
  7. PMID 8682023
    .
  8. ^
    PMID 9778071
    .
  9. PMID 10606834
    .
  10. S2CID 24683211
    .
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