• Molecular NameIsradipine
  • Synonym(+/-)-Isradipine; Isradipin; Isradipino [Spanish]; Isradipinum [Latin]; Isrodipine
  • Weight371.393
  • Drugbank_IDDB00270
  • ACS_NO75695-93-1
  • Show 3D model
  • LogP (experiment)4.18
  • LogP (predicted, AB/LogP v2.0)3.85
  • pkaN/A
  • LogD (pH=7, predicted)3.85
  • Solubility (experiment)Insoluble
  • LogS (predicted, ACD/Labs)(ph=7)-4.61
  • LogSw (predicted, AB/LogsW2.0)0.02
  • Sw (mg/ml) (predicted, ACD/Labs)0.01
  • No.of HBond Donors1
  • No.of HBond Acceptors8
  • No.of Rotatable Bonds6
  • TPSA103.55
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyIsradipine, the most potent calcium-channel blocking agent of the dihydropyridine class, is similar to nifedipine, amlodipine, and felodipine.
  • Absorption_value92.0
  • Absorption (description)Isradipine is rapidly and almost completely absorbed (90 to 95%) after oral administration with peak plasma concentrations after 2 h.
  • Caco_2N/A
  • Bioavailability19.5
  • Protein binding97.0
  • Volume of distribution (VD)2.9 L/kg (283 L)
  • Blood/Plasma Partitioning ratio (D_blood)Erythrocyte:plasma ratio is 0.24.
  • MetabollsmIt undergoes rapid and extensive first-pass hepatic metabolism to produce inactive pyridine and carboxylic acid derivatives. Four major metabolites have been isolated but only one has considerable pharmacological activity.
  • Half life8 h (< 4 h also reported).
  • ExcretionThe drug is excreted as metabolites in urine (70% of the dose) and the remainder in faeces (mostly as the unchanged drug). No unchanged drug is detected in urine. Excretion is virtually complete within 120 h. The pharmacokinetics of isradipine, especially the peak concentrations, half-lives and bioavailability, are increased in the elderly and those with hepatic dysfunction.
  • Urinary ExcretionN/A
  • Clerance40 L/h
  • ToxicitySymptoms of overdose include lethargy, sinus tachycardia, and transient hypotension. Significant lethality was observed in mice given oral doses of over 200 mg/kg and rabbits given about 50 mg/kg of isradipine. Rats tolerated doses of over 2000 mg/kg without effects on survival.
  • LD50 (rat)N/A
  • LD50 (mouse)N/A