Title : Pharmacokinetics and tolerance of 7-methoxytacrine following the single dose administration in healthy volunteers - Filip_1991_Int.J.Clin.Pharmacol.Ther.Toxicol_29_431 |
Author(s) : Filip V , Vachek J , Albrecht V , Dvorak I , Dvorakova J , Fusek J , Havluj J |
Ref : Int J Clinical Pharmacology & Therapeutics Toxicol , 29 :431 , 1991 |
Abstract :
7-methoxy-tetrahydroaminoacridine (7-MEOTA) is a new reversible cholinesterase inhibitor. Forty-eight young male volunteers divided into six dosage groups were included into a single-dose pharmacokinetic study with either oral (p.o.) or intramuscular (i.m.) administration. The dose of 7-MEOTA was 2, 4 or 8 mg/kg body weight p.o. or 0.5, 1 or 2 mg/kg body weight i.m. in the respective six dosage groups. The plasma levels data were fitted to an open one-compartmental model. The compound showed cholinomimetic adverse effects in 2 subjects with the blood levels exceeding 1,500 micrograms/l. The red blood cells levels paralleled those in plasma and were 2.5 times higher. The tmax was 4 hours and 1 h, t1/2 8.7 +/- 3.9 hours and 6.5 +/- 5.8 hours in case of p.o. and i.m. administration, respectively. The apparent clearance (D/AUC) was 5 times higher following p.o. administration, reflecting the differences in bioavailability. |
PubMedSearch : Filip_1991_Int.J.Clin.Pharmacol.Ther.Toxicol_29_431 |
PubMedID: 1800389 |
Inhibitor | 7-Methoxytacrine |
Filip V, Vachek J, Albrecht V, Dvorak I, Dvorakova J, Fusek J, Havluj J (1991)
Pharmacokinetics and tolerance of 7-methoxytacrine following the single dose administration in healthy volunteers
Int J Clinical Pharmacology & Therapeutics Toxicol
29 :431
Filip V, Vachek J, Albrecht V, Dvorak I, Dvorakova J, Fusek J, Havluj J (1991)
Int J Clinical Pharmacology & Therapeutics Toxicol
29 :431