Literature DB >> 7416883

The antiemetic effects of domperidone, a novel potent gastrokinetic.

C J Niemegeers, K H Schellekens, P A Janssen.   

Abstract

Domperidone is the prototype of a new chemical class of compounds with potent gastrokinetic properties. The present study reports on the antiemetic activity and safety of domperidone in dogs. The lowest ED50-values protecting from apomorphine (0.31 mg/kg s.c.) induced emesis are 0.003 mg/kg intravenously, 0.007 mg/kg subcutaneously, 0.03 mg/kg orally and 0.10 mg/kg rectally. Emesis induced by i.v. hydergine, s.c. morphine and oral levodopa is also prevented by low doses of intravenous domperidone, whereas oral copper sulphate-induced emesis is not antagonized. The doses of domperidone needed to induce central depressant effects in dogs (inhibition of conditioned reactions) are at least 300 times higher than the antiemetic doses (apomorphine-induced emesis). Domperidone is also devoid of sedative, adrenolytic and cardiovascular side-effects. The LD50-values in dogs are 42.7 mg/kg intravenously, and more than 160 mg/kg subcutaneously and orally.

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Year:  1980        PMID: 7416883

Source DB:  PubMed          Journal:  Arch Int Pharmacodyn Ther        ISSN: 0003-9780


  12 in total

1.  Interactions between domperidone and ropinirole, a novel dopamine D2-receptor agonist.

Authors:  C de Mey; D Enterling; I Meineke; S Yeulet
Journal:  Br J Clin Pharmacol       Date:  1991-10       Impact factor: 4.335

2.  On the pharmacokinetics of domperidone in animals and man. IV. The pharmacokinetics of intravenous domperidone and its bioavailability in man following intramuscular, oral and rectal administration.

Authors:  J Heykants; R Hendriks; W Meuldermans; M Michiels; H Scheygrond; H Reyntjens
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1981       Impact factor: 2.441

3.  Seizures after antiemetic treatment with high dose domperidone: report of four cases.

Authors:  A Weaving; W R Bezwoda; D P Derman
Journal:  Br Med J (Clin Res Ed)       Date:  1984-06-09

4.  Domperidone prolongs oral to duodenal transit time in video capsule endoscopy.

Authors:  Michael Mcfarlane; B Liu; C Nwokolo
Journal:  Eur J Clin Pharmacol       Date:  2017-12-08       Impact factor: 2.953

5.  On the pharmacokinetics of domperidone in animals and man. I. Plasma levels of domperidone in rats and dogs. Age related absorption and passage through the blood brain barrier in rats.

Authors:  J Heykants; A Knaeps; W Meuldermans; M Michiels
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1981       Impact factor: 2.441

6.  On the pharmacokinetics of domperidone in animals and man II. Tissue distribution, placental and milk transfer of domperidone in the Wistar rat.

Authors:  M Michiels; R Hendriks; J Heykants
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1981       Impact factor: 2.441

7.  Apomorphine-induced limb flicks in cats: the role of dopamine receptors located outside the blood-brain barrier.

Authors:  B R Stewart; C L Broekkamp
Journal:  Psychopharmacology (Berl)       Date:  1988       Impact factor: 4.530

8.  Antiemetic effect of haloperidol in the dog as related to plasma level and dose.

Authors:  C J Niemegeers; J J Heykants; P A Janssen
Journal:  Psychopharmacology (Berl)       Date:  1981       Impact factor: 4.530

9.  Antiemetic specificity of dopamine antagonists.

Authors:  C J Niemegeers
Journal:  Psychopharmacology (Berl)       Date:  1982       Impact factor: 4.530

Review 10.  Domperidone. A review of its pharmacological activity, pharmacokinetics and therapeutic efficacy in the symptomatic treatment of chronic dyspepsia and as an antiemetic.

Authors:  R N Brogden; A A Carmine; R C Heel; T M Speight; G S Avery
Journal:  Drugs       Date:  1982-11       Impact factor: 9.546

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