Disease relevance of Motilium

• Domperidone in reflux oesophagitis and gastric stasis [1].
• The therapeutic efficacy of apomorphine was not reduced by domperidone, while nausea, drowsiness, sedation, and arterial hypotension were prevented [2].
• Sudden death in cancer patient on high-dose domperidone [3].
• Domperidone in chronic intestinal pseudoobstruction [4].
• Gynecomastia in a male infant given domperidone [5].

Psychiatry related information on Motilium

• A novel water-soluble dopamine-2 antagonist with anticholinesterase activity in gastrointestinal motor activity. Comparison with domperidone and neostigmine [6].
• A woman with anorexia nervosa who displayed severe bloating after eating was treated with domperidone, a novel compound with prokinetic properties [7].
• Impaired gastric slow waves induced by spatial disorientation and effect of domperidone [8].
• Akathisia, asthenia, anxiety, and depression were also acknowledged less often, and at a lower severity, after 4 wk of domperidone, although these differences were not statistically significant [9].
• Does domperidone potentiate mirtazapine-associated restless legs syndrome [10]?

High impact information on Motilium

• We demonstrate here that 3H-apomorphine labels two classes of DA receptor, distinguishable using domperidone, a selective DA antagonist [11].
• We show here that the drugs loperamide, domperidone, and ondansetron are transported substrates for the mouse mdr1a P-GP and its human homologue MDR1 [12].
• Furthermore, domperidone prevents vomiting produced by ionizing radiation but does not alter the accompanying delay of gastric emptying [13].
• On a third day, they received 8 Gy (800 rads) whole body irradiation with cobalt 60 gamma-rays after either placebo (n = 10) or domperidone (n = 10) [13].
• Domperidone and lactation [14].

Chemical compound and disease context of Motilium

• The effect of metoclopramide and domperidone, two dopamine antagonists, administered to cirrhotic patients with ascites and secondary hyperaldosteronism, was examined to evaluate the changes in plasma aldosterone levels and in spironolactone-induced diuresis [15].
• Effects of metoclopramide and domperidone on blood flow in portal hypertension [16].
• Current pharmacological agents for treating gastroparesis include metoclopramide, erythromycin, cisapride (only available via a company-sponsored programme) and domperidone (not US FDA approved) [17].
• Carotid body chemoreceptor response to prolonged hypoxia in the rabbit: effects of domperidone and propranolol [18].
• The drugs that are most frequently implicated in movement disorders are antipsychotics, calcium antagonists, orthopramides and substituted benzamides (e.g. metoclopramide, sulpiride, clebopride, domperidone), CNS stimulants, antidepressants, anticonvulsants, antiparkinsonian drugs and lithium [19].

Biological context of Motilium

• Gastric emptying of liquids and solids was significantly suppressed by irradiation (p less than 0.01) after both placebo and domperidone [13].
• The two classes of receptors labeled with [3H]spiroperidol had affinities for domperidone that were similar to those of the two populations of binding sites for [3H]domperidone [20].
• Furthermore, it was observed that bromocriptine produced a time-dependent increase in the phosphorylation (activation) of p44/42 MAPK, which was blocked by domperidone, pertussis toxin, or PD 98059 [21].
• Acute domperidone did not change the blood pressure response to UP [22].
• Before domperidone the mean blood pressure observed in supine position of 132 +/- 37/75 +/- 6 mm Hg fell to 75 +/- 22/57 +/- 13 mm Hg after 2 hours in UP [22].

Anatomical context of Motilium

• The competition for binding of [125I]epidepride by domperidone, quinpirole, and 7-hydroxy-N,N-di(1-propyl)-2-aminotetralin (7-OH-DPAT) was best fit by assuming one site in the caudate but two sites in nucleus accumbens [23].
• Since domperidone does not cross the blood-brain barrier, the hormonal changes observed may be mediated through the pituitary and median eminence, tissues which lie outside of the blood-brain barrier [24].
• Further, we examined the central effects of L-dopa after selectively blocking peripheral (median eminence and pituitary) DA receptors with domperidone (a DA D2 receptor blocker which does not cross the BBB) [25].
• In anaesthetised rats, domperidone (50 and 20 micrograms.kg-1) given via a lateral cerebral ventricle abolished the bromocriptine induced tachycardia without affecting the hypotensive response [26].
• Effect of domperidone on lower esophageal sphincter tone in late pregnancy [27].

Associations of Motilium with other chemical compounds

• The order of potency of D-2 agonists (N-propylnorapomorphine greater than NO434 greater than apomorphine greater than dopamine) and antagonists (spiroperidol greater than (+)-butaclamol greater than domperidone) with the purified preparation was found to be similar to that of the solubilized dopamine D-2 receptor [28].
• On separate occasions, the prokinetic drugs metoclopramide (10 mg), domperidone (10 mg), cisapride (10 mg, all at -30 min per oral), or erythromycin (200 mg intravenously from -30 to -15 min) were administered in addition to GLP-1 [29].
• When the binding of [3H]dopamine and [3H]apomorphine to D2 dopamine receptors is blocked by the inclusion of D2 selective concentrations of unlabeled spiroperidol or domperidone, these ligands appear to label selectively the previously termed "D3" binding site [30].
• The use of prokinetic agents such as metoclopramide, domperidone, cisapride, and erythromycin can improve gastric emptying, but these agents are not without deleterious adverse effects [31].
• Sulpiride (100 mg iv), haloperidol (2 mg, iv), and domperidone (20 mg, iv), three chemically unrelated antidopaminergic agents, as well as TRH (200 micrograms, iv), failed to modify plasma vasopressin, thus suggesting that the MCP effect on vasopressin is not linked to its antidopaminergic and/or PRL-releasing properties [32].

Gene context of Motilium

• Unlike GH, plasma PRL responses to domperidone infusion were not modified by the additional administration of L-dopa [25].
• Mean plasma GH levels did not change during domperidone alone [25].
• VIP-A infusion had no effect on the PRL secretory responses to DOM given at 1200 or 1700 h but attenuated the heightened response at 0300 h [33].
• Twenty-six women diagnosed by dynamic tests and radiologic examination as having PRL-secreting adenoma were treated surgically (15) or with bromocriptine (11) and their condition was evaluated one to three years later by TRH, nomifensine, and domperidone tests [34].
• Domperidone (5 and 50 microm) hydroxylation and N-dealkylation was catalyzed by expressed CYP3A4 at a higher rate than the other CYPs [35].

Analytical, diagnostic and therapeutic context of Motilium

• Dom and TRH elicited a significant rise of basal PRL levels, but the rise was markedly lower than that occurring in the control group [36].
• Blood samples were withdrawn via indwelling catheters before, 5, 20, 40, and 70 min after domperidone or vehicle administration, and 5 and 10 min after TRH administration [37].
• The use of radioligand-binding techniques with tritiated DOM ([3H]DOM) and dihydroergocriptine ([3H]DHE) has demonstrated a high affinity dopaminergic binding site upon rat AP cells under the same conditions as the cell cultures used in the hormone secretion studies [38].
• Each subject participated in two sessions and received oral administration of 10 mg domperidone before the study in one of the sessions [8].
• Patients receiving outpatient chemotherapy, without cisplatin, were randomised to receive four doses of either domperidone 60 mg or prochlorperazine 25 mg suppositories every 4 h, starting 30 min before the chemotherapy [39].

References