About: Fosinopril     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

AttributesValues
rdf:type
http://linked.open...gbank/description
  • Fosinopril is a phosphinic acid-containing ester prodrug that belongs to the angiotensin-converting enzyme (ACE) inhibitor class of medications. It is rapidly hydrolyzed to fosinoprilat, its principle active metabolite. Fosinoprilat inhibits ACE, the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Fosinopril may be used to treat mild to moderate hypertension, as an adjunct in the treatment of congestive heart failure, and to slow the rate of progression of renal disease in hypertensive individuals with diabetes mellitus and microalbuminuria or overt nephropathy. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # David D, Jallad N, Germino FW, Willett MS, de Silva J, Weidner SM, Mills DJ: A Comparison of the Cough Profile of Fosinopril and Enalapril in Hypertensive Patients with a History of ACE Inhibitor-Associated Cough. Am J Ther. 1995 Oct;2(10):806-813. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11854791 # Sharma S, Deitchman D, Eni JS, Gelperin K, Ilgenfritz JP, Blumenthal M: The hemodynamic effects of long-term ACE inhibition with fosinopril in patients with heart failure. Fosinopril Hemodynamics Study Group. Am J Ther. 1999 Jul;6(4):181-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11329095 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • 12 hours (en)
http://linked.open...ugbank/indication
  • For treating mild to moderate hypertension, use as an adjunct in treating congestive heart failure, and may be used to slow the rate of progression of renal disease in hypertensive individuals with diabetes mellitus and microalbuminuria or overt nephropathy. (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Fosinopril (en)
adms:identifier
http://linked.open...mechanismOfAction
  • There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, which arise from tandem gene duplication. Although the two domains have high sequence similarity, they play distinct physiological roles. The C-domain is predominantly involved in blood pressure regulation while the N-domain plays a role in hematopoietic stem cell differentiation and proliferation. ACE inhibitors bind to and inhibit the activity of both domains, but have much greater affinity for and inhibitory activity against the C-domain. Fosinoprilat, the active metabolite of fosinopril, competes with ATI for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII as described in the Pharmacology section above. Fosinoprilat also causes an increase in plasma renin activity likely due to a loss of feedback inhibition mediated by ATII on the release of renin and/or stimulation of reflex mechanisms via baroreceptors. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • After oral administration of radiolabeled fosinopril, approximately half of the absorbed dose is excreted in the urine and the remainder is excreted in the feces. (en)
http://linked.open.../drugbank/synonym
  • Fosinopril (en)
  • (2S,4S)-4-Cyclohexyl-1-{2-[(2-methyl-1-propionyloxy-propoxy)-(4-phenyl-butyl)-phosphinoyl]-acetyl}-pyrrolidine-2-carboxylic acid (en)
  • (S)-4-Cyclohexyl-1-{2-[(2-methyl-1-propionyloxy-propoxy)-(4-phenyl-butyl)-phosphinoyl]-acetyl}-pyrrolidine-2-carboxylic acid (en)
  • (2S,4S)-4-Cyclohexyl-1-[2-[(2-methyl-1-propanoyloxypropoxy)-(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylic acid (en)
http://linked.open...drugbank/toxicity
  • Human overdoses of fosinopril have not been reported, but the most common manifestation of human fosinopril overdosage is likely to be hypotension. Oral doses of fosinopril at 2600 mg/kg in rats were associated with significant lethality. The most common adverse effects include dizzines, cough, fatigue, and headache. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Take without regard to meals. (en)
  • Herbs that may attenuate the antihypertensive effect of fosinopril include: bayberry, blue cohash, cayenne, ephedra, ginger, ginseng (American), kola and licorice. (en)
  • Do not take calcium, aluminum, magnesium or iron supplements, or antacids within 2 hours of taking this medication. (en)
  • High salt intake may attenuate the antihypertensive effect of fosinopril. (en)
  • Fosinopril may decrease the excretion of potassium. Salt substitutes containing potassium may increase the risk of hyperkalemia. (en)
http://linked.open.../drugbank/mixture
http://linked.open...nk/proteinBinding
  • Fosinoprilat is ≥95% protein bound (en)
http://linked.open...ogy/drugbank/salt
  • (en)
http://linked.open...ynthesisReference
  • Sandra Gallego Pato, Antonio Palomo Coll, Francisco Palomo Nicolau, "Preparation of crystalline polymorphs of fosinopril sodium." U.S. Patent US20050010054, issued January 13, 2005. (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...l/drug/hasATCCode
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • Average absolute absorption is 36%. The primary site of absorption is the proximal small intestine (duodenum/jejunum). Food slows the rate of absorption with no effect on the extent of absorption. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 98048-97-6 (en)
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