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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB01340
rdf:type
n3:Drug
n3:description
Cilazapril is an ACE inhibtor class drug used in the treatment of hypertension and heart failure. It belongs to the angiotensin-converting enzyme inhibitors (ACE inhibitors) class of drugs. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat. It is branded as Inhibace in Canada and other countries, Vascace and Dynorm in a number of European countries, among many other names. None of these varieties are available in the United States.
n3:dosage
n21:271B4050-363D-11E5-9242-09173F13E4C5 n21:271B4051-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Fasanella d'Amore T, Bussien JP, Nussberger J, Waeber B, Turini GA, Brunner HR, Kler L, Francis RJ: Effects of single doses of the converting enzyme inhibitor cilazapril in normal volunteers. J Cardiovasc Pharmacol. 1987 Jan;9(1):26-31. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/2434790
n3:group
approved
n3:halfLife
Half-lives for the periods 1 to 4 hours and 1 to 7 days after the intravenous administration of 2.5 mg cilazaprilat are 0.90 and 46.2 hours respectively.
n3:indication
Cilazapril is an ACE inhibtor class drug used in the treatment of hypertension and heart failure.
owl:sameAs
n18:DB01340 n24:DB01340
dcterms:title
Cilazapril
adms:identifier
n8:PA164748302 n9:Cilazapril n11:D07699 n23:DB01340
n3:mechanismOfAction
Cilazapril is a pyridazine ACE inhibitor. It competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. As angiotensin II is a vasoconstrictor and a negative feedback mediator for renin activity, lower angiotensin II levels results in a decrease in blood pressure, an increase in renin activity, and stimulation of baroreceptor reflex mechanisms. Kininase II, an enzyme which degrades the vasodilator bradykinin, is identical to ACE and may also be inhibited.
n3:patent
n19:20060293517
n3:routeOfElimination
Cilazaprilat is eliminated unchanged by the kidneys. The total urinary recovery of cilazaprilat after intravenous administration of 2.5 mg is 91%.
n3:synonym
Cilazaprilum Cilazapril
n3:toxicity
Limited data are available with regard to overdosage in humans. The most likely manifestations are hypotension, which may be severe, hyperkalaemia, hyponatraemia and renal impairment with metabolic acidosis. Treatment should be mainly symptomatic and supportive.
n5:hasAHFSCode
n22:24-32-04
n3:foodInteraction
Take without regard to meals. Food decreases cilazapril absorption with no significant clinical impact.
n3:mixture
n10:271B403D-363D-11E5-9242-09173F13E4C5 n10:271B403E-363D-11E5-9242-09173F13E4C5 n10:271B403B-363D-11E5-9242-09173F13E4C5 n10:271B403C-363D-11E5-9242-09173F13E4C5 n10:271B403A-363D-11E5-9242-09173F13E4C5
n3:proteinBinding
Maximum ACE inhibition is greater than 90% after 1 to 5 mg cilazapril. Maximum ACE inhibition is 70 to 80% after 0.5 mg cilazapril. Dose proportionality is observed following the administration of 1 to 5 mg cilazapril. Apparent non-proportionality is observed at 0.5 mg reflective of the binding to ACE. The higher doses of cilazapril are associated with longer duration of maximum ACE inhibition.
n3:salt
n3:synthesisReference
Attwood, M. R.; Hassall, C. H.; Kr�Hn, A.; Lawton, G.; Redshaw, S. (1986). "The design and synthesis of the Angiotensin Converting Enzyme inhibitor Cilazapril and related bicyclic compounds". Journal of the Chemical Society, Perkin Transactions 1: 1011. doi:10.1039/P19860001011
n12:hasConcept
n13:M0026294
foaf:page
n15:cilazapril.html
n3:IUPAC-Name
n4:271B4056-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B405C-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B405B-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B4058-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B4059-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B405A-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B406C-363D-11E5-9242-09173F13E4C5 n4:271B4054-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B406E-363D-11E5-9242-09173F13E4C5 n4:271B4052-363D-11E5-9242-09173F13E4C5 n4:271B4055-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B4053-363D-11E5-9242-09173F13E4C5
n5:hasATCCode
n6:C09AA08
n3:H-Bond-Acceptor-Count
n4:271B4062-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B4063-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B405D-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B405E-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B4060-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B405F-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B4061-363D-11E5-9242-09173F13E4C5
n3:absorption
Maximum plasma concentrations of cilazaprilat are reached within two hours after administration of cilazapril.
n3:casRegistryNumber
92077-78-6
n3:category
n3:clearance
Total clearance is 12.3 L/h and renal clearance is 10.8 L/h. The total urinary recovery of cilazaprilat following the oral administration of 2.5 mg cilazapril is 52.6%.
n3:containedIn
n20:271B4041-363D-11E5-9242-09173F13E4C5 n20:271B4042-363D-11E5-9242-09173F13E4C5 n20:271B403F-363D-11E5-9242-09173F13E4C5 n20:271B4040-363D-11E5-9242-09173F13E4C5 n20:271B4045-363D-11E5-9242-09173F13E4C5 n20:271B4046-363D-11E5-9242-09173F13E4C5 n20:271B4043-363D-11E5-9242-09173F13E4C5 n20:271B4044-363D-11E5-9242-09173F13E4C5 n20:271B4049-363D-11E5-9242-09173F13E4C5 n20:271B404A-363D-11E5-9242-09173F13E4C5 n20:271B4047-363D-11E5-9242-09173F13E4C5 n20:271B4048-363D-11E5-9242-09173F13E4C5 n20:271B404B-363D-11E5-9242-09173F13E4C5 n20:271B404C-363D-11E5-9242-09173F13E4C5 n20:271B404F-363D-11E5-9242-09173F13E4C5 n20:271B404D-363D-11E5-9242-09173F13E4C5 n20:271B404E-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B4068-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B406A-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B406B-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B406D-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B4067-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B4066-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B4069-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B4057-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B4064-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B4065-363D-11E5-9242-09173F13E4C5