TY - JOUR
T1 - Pharmacokinetics of tetrahydroaminoacridine
T2 - Relations to clinical and biochemical effects in Alzheimer patients
AU - Åhlin, A.
AU - Adem, A.
AU - Junthé, T.
AU - Öhman, G.
AU - Nybäck, H.
PY - 1992
Y1 - 1992
N2 - The pharmacokinetics of tetrahydroaminoacridine (THA) was studied in patients suffering from Alzheimer's dementia. Single doses of the drug were administered by intravenous (15 mg), oral (50 mg) and rectal routes (25 mg). Pharmacokinetic parameters were related to clinical and biochemical effects in patients who, in a separate study, participated in a clinical trial of oral THA. The bioavailability of THA was low and varied considerably between subjects. Clinical improvement and occurrence of elevated liver enzymes correlated positively with drug bioavailability. Acetyl and buturyl cholinesterase activities in the plasma did not change following THA administration. Rectally administered THA had a higher bioavailability than orally administered THA in three subjects who were given the drug by both routes. These results indicate that a clinical trial of rectal THA would be justified as this administration route may improve resorption and diminish first-pass metabolism of the drug in the liver compared with oral administration.
AB - The pharmacokinetics of tetrahydroaminoacridine (THA) was studied in patients suffering from Alzheimer's dementia. Single doses of the drug were administered by intravenous (15 mg), oral (50 mg) and rectal routes (25 mg). Pharmacokinetic parameters were related to clinical and biochemical effects in patients who, in a separate study, participated in a clinical trial of oral THA. The bioavailability of THA was low and varied considerably between subjects. Clinical improvement and occurrence of elevated liver enzymes correlated positively with drug bioavailability. Acetyl and buturyl cholinesterase activities in the plasma did not change following THA administration. Rectally administered THA had a higher bioavailability than orally administered THA in three subjects who were given the drug by both routes. These results indicate that a clinical trial of rectal THA would be justified as this administration route may improve resorption and diminish first-pass metabolism of the drug in the liver compared with oral administration.
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U2 - 10.1097/00004850-199200710-00004
DO - 10.1097/00004850-199200710-00004
M3 - Article
C2 - 1624754
AN - SCOPUS:0026649290
SN - 0268-1315
VL - 7
SP - 29
EP - 36
JO - International Clinical Psychopharmacology
JF - International Clinical Psychopharmacology
IS - 1
ER -