Pharmacokinetics of almitrine in healthy volunteers and patients with essential hypertension.
Pharmacokinetic studies with the arterial chemoreceptor stimulant almitrine (100 mg per os) were performed in 12 healthy volunteers and 8 patients with essential hypertension stage I in order to evaluate the suitability of the drug for physiological tests. The parent compound was determined gas-chromatographically. Almitrine was absorbed with maximal serum levels after 1.8 +/- 0.4 h in healthy volunteers and 1.5 +/- 0.3 h in patients. The elimination proceeded biexponentially with terminal half-lives from 14.6 to 43.4 h in volunteers and 12.5-45.0 h in patients. Further characteristics were large distribution volumes (16.1 +/- 4.5 ml/g in healthy volunteers, 13.9 +/- 4.7 ml/g in patients) and large interindividual variations of all pharmacokinetic parameters by a factor of 2 to 6. Significant differences between healthy individuals and patients were not observed. The drug was well tolerated. The pharmacokinetic properties of almitrine should be included into its evaluation as a test compound.
Wilke
A
A
Department of Clinical Pharmacology, Ernst Moritz Arndt University, Greifswald, FRG.
Siegmund
W
W
Schneider
T
T
Wiersbitzky
M
M
Franke
G
G
D000284:Administration, Oral; D000328:Adult; D015765:Almitrine / Q000493:pharmacokinetics*; D001682:Biological Availability; D001835:Body Weight; D006207:Half-Life; D006801:Humans; D006973:Hypertension / Q000378:metabolism*; D008297:Male; D012995:Solubility
D015765:Almitrine