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Statements

Subject Item
n2:DB00343
rdf:type
n3:Drug
n3:description
A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of the calcium ion in membrane functions. It is also teratogenic. [PubChem]
n3:dosage
n23:271B5BFF-363D-11E5-9242-09173F13E4C5 n23:271B5C00-363D-11E5-9242-09173F13E4C5 n23:271B5C01-363D-11E5-9242-09173F13E4C5 n23:271B5C02-363D-11E5-9242-09173F13E4C5 n23:271B5C03-363D-11E5-9242-09173F13E4C5 n23:271B5C04-363D-11E5-9242-09173F13E4C5 n23:271B5C05-363D-11E5-9242-09173F13E4C5 n23:271B5C06-363D-11E5-9242-09173F13E4C5 n23:271B5C07-363D-11E5-9242-09173F13E4C5 n23:271B5C08-363D-11E5-9242-09173F13E4C5 n23:271B5C09-363D-11E5-9242-09173F13E4C5 n23:271B5C0A-363D-11E5-9242-09173F13E4C5 n23:271B5C0B-363D-11E5-9242-09173F13E4C5 n23:271B5C0C-363D-11E5-9242-09173F13E4C5 n23:271B5C0D-363D-11E5-9242-09173F13E4C5 n23:271B5C0E-363D-11E5-9242-09173F13E4C5 n23:271B5C0F-363D-11E5-9242-09173F13E4C5 n23:271B5C10-363D-11E5-9242-09173F13E4C5 n23:271B5C11-363D-11E5-9242-09173F13E4C5 n23:271B5C12-363D-11E5-9242-09173F13E4C5 n23:271B5C13-363D-11E5-9242-09173F13E4C5 n23:271B5C14-363D-11E5-9242-09173F13E4C5 n23:271B5C15-363D-11E5-9242-09173F13E4C5 n23:271B5C16-363D-11E5-9242-09173F13E4C5 n23:271B5C17-363D-11E5-9242-09173F13E4C5 n23:271B5C18-363D-11E5-9242-09173F13E4C5 n23:271B5C19-363D-11E5-9242-09173F13E4C5 n23:271B5C1A-363D-11E5-9242-09173F13E4C5 n23:271B5C1B-363D-11E5-9242-09173F13E4C5 n23:271B5C1C-363D-11E5-9242-09173F13E4C5 n23:271B5BFB-363D-11E5-9242-09173F13E4C5 n23:271B5BFC-363D-11E5-9242-09173F13E4C5 n23:271B5BFD-363D-11E5-9242-09173F13E4C5 n23:271B5BFE-363D-11E5-9242-09173F13E4C5
n3:group
approved
n3:halfLife
3.0 - 4.5 hours
n3:indication
For the treatment of Hypertension
n3:manufacturer
n10:271B5B5D-363D-11E5-9242-09173F13E4C5 n10:271B5B5E-363D-11E5-9242-09173F13E4C5 n10:271B5B5B-363D-11E5-9242-09173F13E4C5 n10:271B5B5C-363D-11E5-9242-09173F13E4C5 n10:271B5B59-363D-11E5-9242-09173F13E4C5 n10:271B5B5A-363D-11E5-9242-09173F13E4C5 n10:271B5B57-363D-11E5-9242-09173F13E4C5 n10:271B5B58-363D-11E5-9242-09173F13E4C5 n10:271B5B4D-363D-11E5-9242-09173F13E4C5 n10:271B5B4E-363D-11E5-9242-09173F13E4C5 n10:271B5B4B-363D-11E5-9242-09173F13E4C5 n10:271B5B4C-363D-11E5-9242-09173F13E4C5 n10:271B5B49-363D-11E5-9242-09173F13E4C5 n10:271B5B4A-363D-11E5-9242-09173F13E4C5 n10:271B5B48-363D-11E5-9242-09173F13E4C5 n10:271B5B55-363D-11E5-9242-09173F13E4C5 n10:271B5B56-363D-11E5-9242-09173F13E4C5 n10:271B5B53-363D-11E5-9242-09173F13E4C5 n10:271B5B54-363D-11E5-9242-09173F13E4C5 n10:271B5B51-363D-11E5-9242-09173F13E4C5 n10:271B5B52-363D-11E5-9242-09173F13E4C5 n10:271B5B4F-363D-11E5-9242-09173F13E4C5 n10:271B5B50-363D-11E5-9242-09173F13E4C5
owl:sameAs
n25:DB00343 n30:DB00343
dcterms:title
Diltiazem
adms:identifier
n14:C06958 n15:35850 n16:DB00343 n17:50004704 n18:101278 n19:39186 n20:46505667 n21:54868-4970-0 n22:PA449334 n32:Diltiazem
n3:mechanismOfAction
Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, diltiazem, like verapamil, inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue.
n3:packager
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n3:patent
n7:2307547 n7:5286497 n7:6923984 n7:2111085
n3:synonym
(+)-cis-5-[2-(dimethylamino)Ethyl]-2,3-dihydro-3-hydroxy-2-(P-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one acetate ester Acetic acid (2S,3S)-5-(2-dimethylamino-ethyl)-2-(4-methoxy-phenyl)-4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]thiazepin-3-yl ester (2S,3S)-5-(2-(dimethylamino)Ethyl)-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepin-3-yl acetate Diltiazemum Diltiazem (2S-cis)-3-(Acetyloxy)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one
n3:toxicity
LD<sub>50</sub>=740mg/kg (orally in mice)
n8:hasAHFSCode
n11:24-28-92
n3:foodInteraction
Take this medication 30 minutes before meals. Avoid natural licorice.
n3:proteinBinding
70%-80%
n3:salt
n3:synthesisReference
Kugita, H., Inoue, H., Ikezaki, M. and Takeo, S.; U.S. Patent 3,562,257; assigned to Tanabe Seiyaku Co.,Ltd., Japan.
n26:hasConcept
n27:M0006434
foaf:page
n6:diltiazem.html n28:car1068.shtml n31:diltiaz.htm
n3:IUPAC-Name
n12:271B5C21-363D-11E5-9242-09173F13E4C5
n3:InChI
n12:271B5C27-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n12:271B5C26-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n12:271B5C23-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n12:271B5C24-363D-11E5-9242-09173F13E4C5
n3:SMILES
n12:271B5C25-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n12:271B5C37-363D-11E5-9242-09173F13E4C5 n12:271B5C1F-363D-11E5-9242-09173F13E4C5
n3:logP
n12:271B5C39-363D-11E5-9242-09173F13E4C5 n12:271B5C1D-363D-11E5-9242-09173F13E4C5 n12:271B5C20-363D-11E5-9242-09173F13E4C5
n3:logS
n12:271B5C1E-363D-11E5-9242-09173F13E4C5
n8:hasATCCode
n9:C08DB01 n9:C05AE03
n3:H-Bond-Acceptor-Count
n12:271B5C2D-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n12:271B5C2E-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n12:271B5C28-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n12:271B5C29-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n12:271B5C2B-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n12:271B5C2A-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n12:271B5C2C-363D-11E5-9242-09173F13E4C5
n3:absorption
Diltiazem is well absorbed from the gastrointestinal tract but undergoes substantial hepatic first-pass effect.
n3:affectedOrganism
Humans and other mammals
n3:caco2-Permeability
n12:271B5C3A-363D-11E5-9242-09173F13E4C5
n3:casRegistryNumber
42399-41-7
n3:containedIn
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n4:271B5B9E-363D-11E5-9242-09173F13E4C5 n4:271B5B9F-363D-11E5-9242-09173F13E4C5 n4:271B5B9C-363D-11E5-9242-09173F13E4C5 n4:271B5B9D-363D-11E5-9242-09173F13E4C5 n4:271B5BB2-363D-11E5-9242-09173F13E4C5 n4:271B5BB3-363D-11E5-9242-09173F13E4C5 n4:271B5BB0-363D-11E5-9242-09173F13E4C5 n4:271B5BB1-363D-11E5-9242-09173F13E4C5 n4:271B5BB6-363D-11E5-9242-09173F13E4C5 n4:271B5BB7-363D-11E5-9242-09173F13E4C5 n4:271B5BB4-363D-11E5-9242-09173F13E4C5 n4:271B5BB5-363D-11E5-9242-09173F13E4C5 n4:271B5BAA-363D-11E5-9242-09173F13E4C5 n4:271B5BAB-363D-11E5-9242-09173F13E4C5 n4:271B5BA8-363D-11E5-9242-09173F13E4C5 n4:271B5BA9-363D-11E5-9242-09173F13E4C5 n4:271B5BAE-363D-11E5-9242-09173F13E4C5 n4:271B5BAF-363D-11E5-9242-09173F13E4C5 n4:271B5BAC-363D-11E5-9242-09173F13E4C5 n4:271B5BAD-363D-11E5-9242-09173F13E4C5 n4:271B5BC2-363D-11E5-9242-09173F13E4C5 n4:271B5BC3-363D-11E5-9242-09173F13E4C5 n4:271B5BC0-363D-11E5-9242-09173F13E4C5 n4:271B5BC1-363D-11E5-9242-09173F13E4C5 n4:271B5BC6-363D-11E5-9242-09173F13E4C5 n4:271B5BC7-363D-11E5-9242-09173F13E4C5 n4:271B5BC4-363D-11E5-9242-09173F13E4C5 n4:271B5BC5-363D-11E5-9242-09173F13E4C5 n4:271B5BBA-363D-11E5-9242-09173F13E4C5 n4:271B5BBB-363D-11E5-9242-09173F13E4C5 n4:271B5BB8-363D-11E5-9242-09173F13E4C5 n4:271B5BB9-363D-11E5-9242-09173F13E4C5 n4:271B5BBE-363D-11E5-9242-09173F13E4C5 n4:271B5BBF-363D-11E5-9242-09173F13E4C5 n4:271B5BBC-363D-11E5-9242-09173F13E4C5 n4:271B5BBD-363D-11E5-9242-09173F13E4C5 n4:271B5BD2-363D-11E5-9242-09173F13E4C5 n4:271B5BD3-363D-11E5-9242-09173F13E4C5 n4:271B5BD0-363D-11E5-9242-09173F13E4C5 n4:271B5BD1-363D-11E5-9242-09173F13E4C5 n4:271B5BD6-363D-11E5-9242-09173F13E4C5 n4:271B5BD7-363D-11E5-9242-09173F13E4C5 n4:271B5BD4-363D-11E5-9242-09173F13E4C5 n4:271B5BD5-363D-11E5-9242-09173F13E4C5 n4:271B5BCA-363D-11E5-9242-09173F13E4C5 n4:271B5BCB-363D-11E5-9242-09173F13E4C5 n4:271B5BC8-363D-11E5-9242-09173F13E4C5 n4:271B5BC9-363D-11E5-9242-09173F13E4C5 n4:271B5BCE-363D-11E5-9242-09173F13E4C5 n4:271B5BCF-363D-11E5-9242-09173F13E4C5 n4:271B5BCC-363D-11E5-9242-09173F13E4C5 n4:271B5BCD-363D-11E5-9242-09173F13E4C5 n4:271B5BE2-363D-11E5-9242-09173F13E4C5 n4:271B5BE3-363D-11E5-9242-09173F13E4C5 n4:271B5BE0-363D-11E5-9242-09173F13E4C5 n4:271B5BE1-363D-11E5-9242-09173F13E4C5 n4:271B5BE6-363D-11E5-9242-09173F13E4C5 n4:271B5BE7-363D-11E5-9242-09173F13E4C5 n4:271B5BE4-363D-11E5-9242-09173F13E4C5 n4:271B5BE5-363D-11E5-9242-09173F13E4C5 n4:271B5BDA-363D-11E5-9242-09173F13E4C5 n4:271B5BDB-363D-11E5-9242-09173F13E4C5 n4:271B5BD8-363D-11E5-9242-09173F13E4C5 n4:271B5BD9-363D-11E5-9242-09173F13E4C5 n4:271B5BDE-363D-11E5-9242-09173F13E4C5 n4:271B5BDF-363D-11E5-9242-09173F13E4C5 n4:271B5BDC-363D-11E5-9242-09173F13E4C5 n4:271B5BDD-363D-11E5-9242-09173F13E4C5 n4:271B5BF2-363D-11E5-9242-09173F13E4C5 n4:271B5BF3-363D-11E5-9242-09173F13E4C5 n4:271B5BF0-363D-11E5-9242-09173F13E4C5 n4:271B5BF1-363D-11E5-9242-09173F13E4C5 n4:271B5BF6-363D-11E5-9242-09173F13E4C5 n4:271B5BF7-363D-11E5-9242-09173F13E4C5 n4:271B5BF4-363D-11E5-9242-09173F13E4C5 n4:271B5BF5-363D-11E5-9242-09173F13E4C5 n4:271B5BEA-363D-11E5-9242-09173F13E4C5 n4:271B5BEB-363D-11E5-9242-09173F13E4C5 n4:271B5BE8-363D-11E5-9242-09173F13E4C5 n4:271B5BE9-363D-11E5-9242-09173F13E4C5 n4:271B5BEE-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n12:271B5C33-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n12:271B5C35-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n12:271B5C36-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n12:271B5C38-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n12:271B5C32-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n12:271B5C31-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n12:271B5C34-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n12:271B5C22-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n12:271B5C2F-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n12:271B5C30-363D-11E5-9242-09173F13E4C5