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Pharmacokinetics of heptastigmine in rats

Segre, G. ; Cerretani, D. ; Baldi, A. ; Urso, R.

Pharmacological research, 1992-02, Vol.25 (2), p.139-146 [Periódico revisado por pares]

LONDON: Elsevier Ltd

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Título:
Pharmacokinetics of heptastigmine in rats
Autor: Segre, G. ; Cerretani, D. ; Baldi, A. ; Urso, R.
Assuntos: Administration, Oral ; Animals ; Biological and medical sciences ; Cholinesterase Inhibitors - pharmacokinetics ; hepastigmine ; Injections, Intramuscular ; Injections, Intravenous ; Life Sciences & Biomedicine ; Male ; Medical sciences ; Neuropharmacology ; pharmacokinetics ; Pharmacology & Pharmacy ; Pharmacology. Drug treatments ; Physostigmine - administration & dosage ; Physostigmine - analogs & derivatives ; Physostigmine - blood ; Physostigmine - pharmacokinetics ; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) ; Psychology. Psychoanalysis. Psychiatry ; Psychopharmacology ; Rats ; Rats, Inbred Strains ; Science & Technology ; Tissue Distribution
É parte de: Pharmacological research, 1992-02, Vol.25 (2), p.139-146
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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Descrição: Heptastigmine is a new long acting cholinesterase inhibitor that affects behaviour in a number of cognitive tests in animals. We have studied its pharmacokinetics in rats: plasma kinetics were evaluated after single intravenous dose (2 mg/kg), intramuscular (4 mg/kg) and oral (4 and 8 mg/kg) administration. Tissue distribution (heart, liver, kidney and brain) was studied after single intramuscular (4 mg/kg) and oral (8 mg/kg) administration. Plasma and tissue kinetics were also investigated after repeated oral doses (8 mg/kg b.i.d. for 7 days). Heptastigmine levels in plasma and tissues were determined using an HPLC method with an electrochemical detector. After a single dose, heptastigmine remained for a long time in plasma (the terminal half-life was about 12 h), distributed widely in tissue (the volume of distribution was about 61) and brain concentrations were very high (4–22 times those found in plasma). After repeated oral doses, the drug levels increased plasma and, to a lesser extent, in liver and kidney.
Editor: LONDON: Elsevier Ltd
Idioma: Inglês

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Pharmacokinetics of heptastigmine in rats

Segre, G. ; Cerretani, D. ; Baldi, A. ; Urso, R.

LONDON: Elsevier Ltd

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