- Molecular NameAmlodipine
- SynonymTrospiumAmlodipine Benzenesulfonate; Amlodipine Besilate; Amlodipine Besylate; Amlodipine Free Base; Amlodipino [Spanish]; Amlodipinum [Latin]
- Weight408.882
- Drugbank_IDDB00381
- ACS_NO88150-42-9
- Show 2D model
- LogP (experiment)3.17
- LogP (predicted, AB/LogP v2.0)3.09
- pka8.6
- LogD (pH=7, predicted)0.8
- Solubility (experiment)0.0753 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-3.13
- LogSw (predicted, AB/LogsW2.0)0.01
- Sw (mg/ml) (predicted, ACD/Labs)0.01
- No.of HBond Donors3
- No.of HBond Acceptors7
- No.of Rotatable Bonds10
- TPSA99.88
- StatusFDA approved
- AdministrationN/A
- PharmacologyA long-acting calcium channel blocker (dihydropyridine class) used as an anti-hypertensive and in the treatment of angina.
- Absorption_value100.0
- Absorption (description)Amlodipine is slowly and almost completely absorbed after oral administration; peak plasma concentrations occur after 6 to 12 h. Absorption is not affected by food.
- Caco_2N/A
- Bioavailability74.0
- Protein binding93.0
- Volume of distribution (VD)16 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmIt undergoes minimal presystemic metabolism; bioavailability is about 60 to 65% and it undergoes extensive but slow metabolism in the liver. Metabolites lack significant pharmacological activity.
- Half life39 h
- ExcretionExcreted predominantly in urine (about 60% of a dose); less than 10% of a dose is excreted as the unchanged drug. About 20 to 25% of a dose is eliminated via bile. It is not removed by haemodialysis.
- Urinary Excretion10
- Clerance5.9 ml/min/kg.
- ToxicityGross overdosage could result in excessive peripheral vasodilatation and possibly reflex tachycardia. Marked and probably prolonged systemic hypotension up to an including shock with fatal outcome have been reported.
- LD50 (rat)N/A
- LD50 (mouse)N/A