Title : Comparative pharmacokinetics of four cholinesterase inhibitors in rats - Yamamoto_1995_Biol.Pharm.Bull_18_1292
Author(s) : Yamamoto K , Sawada Y , Iga T
Ref : Biol Pharm Bull , 18 :1292 , 1995
Abstract :

Pharmacokinetics of a very short-acting, a short-acting and two long-acting cholinesterase (ChE) inhibitors, edrophonium, neostigmine, pyridostigmine and ambenonium, respectively, were compared to elucidate the major determinant of their pharmacokinetics. No dose-dependency in pharmacokinetic behavior was observed within the range of 2-10 mumol/kg for edrophonium, 0.5-2 mumol/kg for pyridostigmine, 0.1-0.5 mumol/kg for neostigmine and 0.3-3 mumol/kg for ambenonium, respectively. Neostigmine has the shortest elimination half-life, and edrophonium, pyridostigmine and ambenonium follow in that. Four ChE inhibitors have similar Vdss values within the range of 0.3-0.7 l/kg, which is similar to the muscle/plasma concentration ratio of these drugs. The liver or kidney to plasma concentration ratio of all ChE inhibitors at 20min after i.v. administration ranged from 5 to 15. Small distribution volumes estimated from the plasma concentration profiles may reflect the distribution to muscle and to the extracellular space of other organs/tissues, while the rapid disappearance of ChE inhibitors from plasma may reflect the concentrative uptake to the liver and kidney.

PubMedSearch : Yamamoto_1995_Biol.Pharm.Bull_18_1292
PubMedID: 8845827

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Citations formats

Yamamoto K, Sawada Y, Iga T (1995)
Comparative pharmacokinetics of four cholinesterase inhibitors in rats
Biol Pharm Bull 18 :1292

Yamamoto K, Sawada Y, Iga T (1995)
Biol Pharm Bull 18 :1292