Table 1.

Pharmacokinetic properties of amlodipine

Pharmacokinetics	Effect	Reference
Bioavailability	Amlodipine is orally administrated with a bioavailability of 64–90%.	[2, 19, 22]
Absorption	Amlodipine reach peak plasma concentration (tmax) 6–12 h after administration, while steady state plasma concentrations will be reached within 7–8 days of daily dosing.	[2, 23]
Distribution	Amlodipine has a high volume of distribution (21 L/kg) and a large proportion of the dose is distributed in the tissue with ~ 90% of the circulating drug being bound to the plasma membrane.	[2, 22, 23]
Metabolism	Amlodipine is extensively metabolized in the liver into its inactive metabolites via CYP3A4/5.	[2, 22, 23]
Elimination	Amlodipine is slowly cleared with an elimination half-life of 40 to 60 h. If discontinued, BP returned to baseline after 1 week. Urine is the major route of elimination. Amlodipine is converted to inactive metabolites (60%), which are excreted into the urine while 10% of the excreted drug remains unchanged. Amlodipine is converted from dihydropyridinebmoiety to a pyridine derivative (M9). Fecal excretion accounts for 20–25% of the dose	[2, 19, 22, 24, 25]