Ivabradine

Ivabradine, sold under the brand name Procoralan among others, is a medication, which is a pacemaker current (If) inhibitor, used for the symptomatic management of heart-related chest pain and heart failure. Patients who qualify for use of Ivabradine for coronary heart failure are patients who have symptomatic heart failure, with reduced ejection volume, and heart rate at least 70 bpm, and the condition not able to be fully managed by beta blockers.

Ivabradine
Clinical data
Pronunciation/ɪˈvæbrədn/
Trade namesCorlanor, Procoralan, others
Other namesS-16257
AHFS/Drugs.comMonograph
License data
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • CA: ℞-only
  • UK: POM (Prescription only)
  • US: ℞-only
  • EU: Rx-only
Pharmacokinetic data
Bioavailability40%
Protein binding70%
MetabolismLiver (first-pass) >50%, CYP3A4-mediated
Elimination half-life2 hours
ExcretionKidney and fecal
Identifiers
  • 3-[3-({[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino)propyl]-7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-2-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC27H36N2O5
Molar mass468.594 g·mol−1
3D model (JSmol)
SMILES
  • O=C2N(CCc1cc(OC)c(OC)cc1C2)CCCN(C[C@@H]4c3cc(OC)c(OC)cc3C4)C
  • InChI=1S/C27H36N2O5/c1-28(17-21-11-20-14-25(33-4)26(34-5)16-22(20)21)8-6-9-29-10-7-18-12-23(31-2)24(32-3)13-19(18)15-27(29)30/h12-14,16,21H,6-11,15,17H2,1-5H3/t21-/m1/s1 Y
  • Key:ACRHBAYQBXXRTO-OAQYLSRUSA-N Y
 NY (what is this?)  (verify)

Ivabradine acts by allowing negative chronotropy in the sinoatrial structure, thus reducing the heart rate via specific inhibition of the pacemaker current. It operates by a mechanism different from that of beta blockers and calcium channel blockers, which are two commonly prescribed antianginal classes of cardiac drugs. Ivabradine has no apparent inotropic properties and may be a cardiotonic agent.

This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.