Summary
Amlodipine was administered as 14 single 5-mg oral daily doses to 27 male subjects with renal function ranging from normal to haemodialysis-dependent. Blood specimens were obtained for measurement of plasma amlodipine concentrations for 24 h following the first dose, for 168 h following the final dose and during daily administration of amlodipine. Amlodipine was well tolerated.
Renal impairment had little effect on the pharmacokinetics of amlodipine. The elimination half-life was of the order of 50 h, similar to previously reported values and did not vary with renal function. Steady-state pre-dose concentrations were observed after the ninth dose. Accumulation of amlodipine was not significantly different from that expected on theoretical grounds and did not significantly change with renal function.
These results suggest that once daily administration of amlodipine is suitable for all degrees of renal function and that dosage adjustment is not necessary in renal impairment.
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References
Dodd MG, Machin I (1985) Anti-hypertensive effects of amlodipine, a novel dihydropyridine calcium channel blocker. Br J Pharmacol 85: 335
Jackson, NC, Lee PS, Reynolds G, Frais M, Taylor SH (1985) Improvement of treadmill time to angina by amlodipine. Br J Clin Pharmacol 20: 248
Faulkner JK, Mc Gibney D, Chasseaud LF, Perry JG, Taylor IW (1986) The pharmacokinetics of amlodipine in healthy volunteers after single intravenous and oral doses and after 14 repeated oral doses given once daily. Br J Clin Pharmacol 22: 21–25
Baez MA, Weidler DJ (1986) Antihypertensive effects of amlodipine in hypertensive patients. J Hypertension 4 [Suppl 5]: S 458-S 460
Webster J, Robb OJ, Jeffers TA, Scott AK, Petrie JC (1987) Once daily amlodipine in the treatment of mild to moderate hypertension. Br J Clin Pharmacol 24: 713–719
Beresford AP, Macrae PV, Stopher DA, Wood BA (1987) Analysis of amlodipine in human plasma by gas chromatography. J Chromatogr 420: 178–183
Gibaldi M, Perrier D (1982) Pharmacokinetics, 2nd edn. Marcel Dekker, New York, p 121
Beresford AP, Mc Gibney D, Humphrey MJ, Macrae PA, Stopher DA (1988) Metabolism and kinetics of amlodipine in man. Xenobiotica (in press)
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Doyle, G.D., Donohue, J., Carmody, M. et al. Pharmacokinetics of amlodipine in renal impairment. Eur J Clin Pharmacol 36, 205–208 (1989). https://doi.org/10.1007/BF00609197
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DOI: https://doi.org/10.1007/BF00609197