Literature DB >> 4455331

The pharmacokinetics of neostigmine and 3-hydroxyphenyltrimethyl- ammonium in the rat: dose-dependent effects after portal vein administration.

H E Barber, G R Bourne.   

Abstract

1 The elimination kinetics of [(14)C]-neostigmine iodide and [(14)C]-3-hydroxyphenyltrimethyl-ammonium iodide (3-OH PTMA) have been studied in the rat.2 The presence of a renal secretory pathway for neostigmine and 3-OH PTMA has been confirmed.3 For neostigmine and 3-OH PTMA, at a given dose level, the fraction of the dose eliminated unchanged was reduced and the metabolite fraction was increased after portal vein administration when compared to jugular vein administration. This indicates that both compounds are subject to extensive metabolism during the first passage through the liver.4 Neostigmine was eliminated by dose-independent kinetics after jugular vein administration but dose-dependent after portal vein administration. In the latter case the fraction eliminated as neostigmine increased with increasing dose. This increase was not accompanied by any change in the fraction of the metabolites eliminated.5 After portal vein administration of 3-OH PTMA, the fraction of the dose eliminated as 3-OH PTMA also increased with increasing dose. This change was accompanied by a decrease in the fraction of the metabolites eliminated which were excreted at a constant rate.

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Year:  1974        PMID: 4455331      PMCID: PMC1776893          DOI: 10.1111/j.1476-5381.1974.tb09725.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  13 in total

1.  The pharmacokinetics of inulin and urea: a comparison of the dose eliminated from a compartmental model and that eliminated in urine.

Authors:  G R Bourne; H E Barber
Journal:  J Pharm Pharmacol       Date:  1972-07       Impact factor: 3.765

2.  Relationship between dose and plateau levels of drugs eliminated by parallel first-order and capacity-limited kinetics.

Authors:  T Tsuchiya; G Levy
Journal:  J Pharm Sci       Date:  1972-04       Impact factor: 3.534

3.  Pharmacokinetics of highly ionized drugs. 3. Methylene blue--blood levels in the dog and tissue levels in the rat following intravenous administration.

Authors:  A R DiSanto; J G Wagner
Journal:  J Pharm Sci       Date:  1972-07       Impact factor: 3.534

4.  Some considerations as to the determination and significance of biologic half-life.

Authors:  M Gibaldi; H Weintraub
Journal:  J Pharm Sci       Date:  1971-04       Impact factor: 3.534

5.  Fitting a double-exponential curve to observed salicylate concentrations in blood.

Authors:  F W Mueller; S V Lieberman
Journal:  J Pharm Sci       Date:  1970-04       Impact factor: 3.534

6.  The biliary excretion of trimethyl-14C(3-hydroxyphenyl)ammonium iodide and its metabolic products.

Authors:  S M Somani; A Wright; T N Calvey
Journal:  Eur J Pharmacol       Date:  1970-09-01       Impact factor: 4.432

7.  Isolation and characterisation of metabolites of neostigmine from rat urine.

Authors:  S M Somani; J B Roberts; B H Thomas; A Wilson
Journal:  Eur J Pharmacol       Date:  1970-09-01       Impact factor: 4.432

8.  Metabolism of [14C]-neostigmine in the rat.

Authors:  J B Roberts; B H Thomas; A Wilson
Journal:  Br J Pharmacol Chemother       Date:  1965-12

9.  Renal tubular reabsorption of p-aminohippuric acid (PAH)in the dog.

Authors:  K C Cho; E J Cafruny
Journal:  J Pharmacol Exp Ther       Date:  1970-05       Impact factor: 4.030

10.  Metabolism and exretion of 3-hydroxyphenyltrimethylammonium and neostigmine.

Authors:  M A Husain; J B Roberts; B H Thomas; A Wilson
Journal:  Br J Pharmacol       Date:  1969-02       Impact factor: 8.739

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  2 in total

1.  The relationship between the pharmacokinetics, cholinesterase inhibition and facilitation of twitch tension of the quaternary ammonium anticholinesterase drugs, neostigmine, pyridostigmine, edrophonium and 3-hydroxyphenyltrimethylammonium.

Authors:  H E Barber; T N Calvey; K T Muir
Journal:  Br J Pharmacol       Date:  1979-08       Impact factor: 8.739

2.  The pharmacokinetics of pyridostigmine and 3-hydroxy-N-methylpyridinium in the rat: dose-dependent effects after portal vein administration.

Authors:  H E Barber; G R Bourne; T N Calvey; K T Muir
Journal:  Br J Pharmacol       Date:  1975-11       Impact factor: 8.739

  2 in total

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