About: Nisoldipine     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)

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http://linked.open...gbank/description
  • Nisoldipine is a 1,4-dihydropyridine calcium channel blocker. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, nisoldipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction. Nisoldipine may be used in alone or in combination with other agents in the management of hypertension. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Mielcarek J, Grobelny P, Szamburska O: The effect of beta-carotene on the photostability of nisoldipine. Methods Find Exp Clin Pharmacol. 2005 Apr;27(3):167-71. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15834448 # Missan S, Zhabyeyev P, Dyachok O, Jones SE, McDonald TF: Block of cardiac delayed-rectifier and inward-rectifier K+ currents by nisoldipine. Br J Pharmacol. 2003 Nov;140(5):863-70. Epub 2003 Oct 6. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/14530219 # Hamilton SF, Houle LM, Thadani U: Rapid-release and coat-core formulations of nisoldipine in treatment of hypertension, angina, and heart failure. Heart Dis. 1999 Nov-Dec;1(5):279-88. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11720635 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • 7-12 hours (en)
http://linked.open...ugbank/indication
  • For the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents. (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Nisoldipine (en)
adms:identifier
http://linked.open...mechanismOfAction
  • By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nisoldipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload. (en)
http://linked.open...drugbank/packager
http://linked.open...y/drugbank/patent
http://linked.open...outeOfElimination
  • Although 60-80% of an oral dose undergoes urinary excretion, only traces of unchanged nisoldipine are found in urine. (en)
http://linked.open.../drugbank/synonym
  • Nisoldipine (en)
  • Sular (en)
  • Nisoldipin (en)
  • Nisoldipina (en)
  • Nisoldipino (en)
  • Nisoldipinum (en)
  • isobutyl methyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Do not take with grapefruit juice as this has been shown to interfere with nisoldipine metabolism, resulting in a mean increase in C<sub>max</sub> of about 3-fold (up to about 7-fold) and AUC of almost 2-fold (up to 5-fold). (en)
http://linked.open...nk/proteinBinding
  • 99% (en)
http://linked.open...ynthesisReference
  • Massimo Ferrari, Marcello Ghezzi, Manuel Alberelli, Alberto Ambrosini, "Industrial process for the synthesis of isobutyl methyl 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridine dicarboxylate (nisoldipine)." U.S. Patent US20050240022, issued October 27, 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
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http://linked.open...nd-Acceptor-Count
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http://linked.open...drugbank/InChIKey
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http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • Relatively well absorbed into the systemic circulation with 87% of the radiolabeled drug recovered in urine and feces. The absolute bioavailability of nisoldipine is about 5%. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 63675-72-9 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...gbank/containedIn
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