Domperidone or metoclopramide in preventing chemotherapeutically induced nausea and vomiting.

Swann, I L; Thompson, E N; Qureshi, Kahekashan

doi:10.1136/bmj.2.6199.1188

Cited by 46 publications

(9 citation statements)

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“…Several of these drugs have been shown to block the inhibitory action of dopamine and dopamine agonists on prolactin secretion by pituitary cells in vitro (Macleod & Lehmeyer, 1974;Yeo, Thomer, Jones, Lowry & Besser, 1979), and binding studies have suggested that these drugs may act as antagonists at dopamine receptors on these cells (Creese, Burt & Snyder, 1975;1976;Calabro & Macleod, 1978;Caron, Beaulieu, Raymond, Gagne, Drovin, Lefkowitz & Labrie, 1978). In this study, we have investigated the in vitro dose-response relationships of four drugs that are known prolactin secretagogues in vivo: chlorpromazine, a phenothiazine; haloperidol, a butyrophenone; metoclopramide, a substituted benzamide; and domperidone, a new anti-emetic structurally related to pimozide (Swann, Thompson & Qureshi, 1979). We have demonstrated that all four 0007-1188/80/140569-05 101.00 appear to act as competitive antagonists to dopamine at low concentrations, but paradoxically reduce prolactin secretion in the absence of dopamine when administered at high concentration.…”

Section: Introductionmentioning

confidence: 99%

Chlorpromazine, Haloperidol, Metoclopramide and Domperidone Release Prolactin Through Dopamine Antagonism at Low Concentrations but Paradoxically Inhibit Prolactin Release at High Concentrations

Besser

Delitala

Grossman

et al. 1980

British J Pharmacology

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Section: Introductionmentioning

confidence: 99%

Chlorpromazine, Haloperidol, Metoclopramide and Domperidone Release Prolactin Through Dopamine Antagonism at Low Concentrations but Paradoxically Inhibit Prolactin Release at High Concentrations

Besser

Delitala

Grossman

et al. 1980

British J Pharmacology

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“…In two of these studies a comparison with domperidone was included, and metoclopramide was superior in patients receiving CMF [101] but not in those receiving doxorubicin [8]. Single intravenous doses of metoclopramide 10-20 mg were not different from placebo in effect [97] or were equal [31,117] or inferior [38,109] to single doses of domperidone, and inferior to multiple doses of dexamethasone [97]. In three recent trials, metoclopramide given as a loading dose of 60-80 mg i.v.…”

Section: Substituted Benzamidesmentioning

confidence: 99%

Corticosteroids, dopamine antagonists and other drugs

Herrstedt

Aapro

Smyth

et al. 1998

Supportive Care in Cancer

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“…Domperidone is used for nausea and vomiting [10] associated with migraine [11], gastroparesis [12], in combination with levodopa in the management of Parkinson's disease [13], functional dyspepsia [14], in lactation acting as an antidopaminergic agent to promote lactation [15,16].…”

mentioning

confidence: 99%

Formulation of Domperidone Microspheres Using a Combination of Locally Extracted Chitosan and Hpmc as Polymers

Majekodunmi¹,

Uzoaganobi²

2017

JCCE

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Abstract:Commercially available domperidone -a D2 receptor antagonist-is an immediate release formulation which has never been formulated into microspheres for sustained release. The present work aims towards studying the effect of combination of a natural chitosan from an oyster shell of Mystilis edulis and HPMC (hydroxy propyl methyl cellulose) (spectracel 15 E) as polymer and tripolyphosphate as cross linking agent using wet gelation technique. The various polymer combination ratios for different batches were compared with a low molecular weight standard chitosan. The extracted chitosan -HPMC polymer combination ratios were chosen at ten levels: as batches B1, B2, B3, B4, B5, B6, B7, B8, B9, B10 for 1:1, 1:2, 2:1, 1:0, 0:1, 3:1, 1:3, 5:1, and 1:5 and 1:1 having 450:450, 300:600, 600:300, 900:0, 0: 900, 675:225, 225:675, 750:150, 150:750, 450:450 mg respectively, while the quantity of domperidone and tripolyphosphate remained constant. B11 and B12 were formulated with standard chitosan and HPMC. The percentage yield of the formulated microspheres was determined and then evaluated for flowability, drug entrapment efficiency, drug release and mechanism of drug release by Fickian diffusion. The best batches of the domperidone loaded microspheres produced from the combination polymer were compared with the standard chitosan. The highest yields of microspheres were given by batches B12, B11, B10, and B4 with values of 50.1 ± 0.1%, 49.6 ± 0.1%, 46.6 ± 0.1%, and 46.1 ± 0.0% respectively while the lowest yield were 23.3 ± 0.2% and 23.6 ± 0.2%. B5 and B6 and B9 did not yield any microsphere. The bulk density, tapped density, compressibility and Hausner's ratio of the microspheres showed good flowability and high percent compressibility. The drug entrapment efficiency showed that the entrapment ranged from 54.2 to 97.2, where the least entrapment was B4 (54.2 ± 0.1) and the highest B12 (97.2 ± 0.2). The polymer surface of the microspheres as observed by SEM (scanning electron microscopy) was heterogeneous and porous which offers enhanced bioadhesivity. The dissolution study was used to determine the percentage drug release which ranged from 12.1% to 68.9% after 5 hours. Batches 1, 2, 3, 4, 7, and 11 follow zero order kinetics via Fickian diffusion. The results indicate that microspheres of domperidone could be successfully formulated with a natural chitosan either alone or in combination with HPMC for sustained delivery of domperidone. Furthermore, the concentration of the natural polymer and HPMC employed in the formulation need to be carefully selected to enable the production of microspheres with the desired sustained release properties.

show abstract

Domperidone or metoclopramide in preventing chemotherapeutically induced nausea and vomiting.

Cited by 46 publications

References 1 publication

Chlorpromazine, Haloperidol, Metoclopramide and Domperidone Release Prolactin Through Dopamine Antagonism at Low Concentrations but Paradoxically Inhibit Prolactin Release at High Concentrations

Chlorpromazine, Haloperidol, Metoclopramide and Domperidone Release Prolactin Through Dopamine Antagonism at Low Concentrations but Paradoxically Inhibit Prolactin Release at High Concentrations

Corticosteroids, dopamine antagonists and other drugs

Formulation of Domperidone Microspheres Using a Combination of Locally Extracted Chitosan and Hpmc as Polymers

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