Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0042963 (vomiting)
 31,883 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

In a double-blind study vs bromocriptine, 30 women who wished to interrupt breast-feeding after a physiological delivery and at least 3 months of nursing were given at random 10 mg dihydroergocristine capsules or 2.5 mg bromocriptine capsules twice a day for 5 days, then 3 times a day for 5 days if treatment had failed to produce an effect. The parameters considered were PRL plasma levels, which were measured at baseline, on the 5th day and, where necessary, on the 10th day of treatment. Milk secretion, breast swelling and pain were recorded at baseline and daily during treatment. The appearance of any side-effect was accurately reported. A prolactin decrease was observed in both groups (p less than 0.01). After 5 days milk secretion was reduced more significantly in the dihydroergocristine group; after 10 days of treatment 6 cases treated with bromocriptine and 1 case treated with dihydroergocristine still revealed a low milk secretion. Breast congestion and pain were absent in both groups. As regards side-effects, a significant decrease in systolic blood pressure (standing position) was reported in the bromocriptine group. Other symptoms, such as nausea, vomiting, insomnia and headache, were reported in 8 patients in the bromocriptine group vs 6 patients in the dihydroergocristine group.
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PMID:Dihydroergocristine in stopping lactation: double-blind study vs bromocriptine. 314 May 92

The influence of food on release of drug from a modified release capsule of bromocriptine 5 mg (Parlodel SRO) and a conventional formulation of bromocriptine 5 mg has been studied in 8 healthy male volunteers. Both formulations produced objective and subjective effects, such as orthostatic reactions, nausea, dizziness, vomiting and nasal congestion. The modified release capsule caused fewer side-effects than the normal capsule. Both formulations had less cardiovascular effect in the fed than in the fasting state. There was no significant difference between the normal and the modified release capsules taken fasting or after a meal in terms of the AUC extrapolated to infinity. The relative bioavailability of the 5 mg modified release capsule was 84.6% of the normal capsule under fasting conditions and 107.5% after food. In contrast to the virtually unchanged extent of absorption, the rate of absorption was markedly affected by food, especially from the conventional capsule. The mean time of 50% absorption increased from 1.06 h (fasting) to 3.2 h (fed), whereas for the modified release capsule food mainly resulted in an increased lag time of absorption. The almost instantaneous dissolution of bromocriptine from the normal capsule in vitro (both in HCl and fasting human gastric juice) and the delay of absorption after a meal in vivo suggest that the rate limiting step in absorption of the normal capsules is delivery of released drug from the stomach to the small intestine, which is delayed by food. Both the modified release 5-mg capsule and the normal 5-mg capsule showed extended suppression of prolactin over 36 h, in all subjects, both fasted and after a meal.
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PMID:Differential effect of food on kinetics of bromocriptine in a modified release capsule and a conventional formulation. 323 63

Seventeen patients with refractory malignant tumors were treated with recombinant human interleukin-2 (IL-2) administered by weekly bolus intravenous (IV) injection in a phase I dose escalation trial. Patients received 10,000 to 1,000,000 U/m2 per injection over a course of 3 to 33 weeks. Toxicity was dose related and consisted primarily of fever, chills, nausea, and vomiting. Hypotension was observed at doses of 500,000 U/m2 or higher and in one instance was sufficiently severe to require pressors. No tumor regression was seen and all patients eventually developed progressive disease. Blood levels of cortisol, ACTH, prolactin, and growth hormone as well as the acute phase reactant C-reactive protein (CRP) increased after the administration of IL-2 in most patients. Serum IL-2 levels in excess of 250 U/mL were detected five minutes after an IV injection of 1,000,000 U/m2, after which the levels declined with a half-life of approximately 25 minutes. No alteration in lymphocyte surface phenotype or enhancement in natural cell-mediated cytotoxicity against natural killer (NK)-sensitive and resistant tumor cell lines was observed when these parameters were measured weekly just before the IL-2 injections. However, a dramatic but transient decline in circulating lymphocytes and NK activity was noted within hours of receiving IL-2. This effect was independent of fever and was not abrogated by pretreatment with ibuprofen or metyrapone. The majority of patients developed serum IgG antibodies of IL-2 detectable with a sensitive enzyme-linked immunosorbent assay (ELISA) and a nitrocellulose dot blot assay. The development of anti-IL-2 antibodies was not associated with symptoms suggestive of serum sickness, reductions in serum complement levels, or deterioration in lymphocyte tumoricidal activity. This investigation provides insight into the in vivo actions of this potent biological response modifier and will assist in the design of future studies with IL-2 administered alone or in conjunction with other treatment modalities.
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PMID:Phase I evaluation of recombinant interleukin-2 in patients with advanced malignant disease. 348 80

The efficacy of bromocriptine in the treatment of hypertension was assessed in a double-blind placebo controlled cross-over study preceded by a dose titration phase. A diuretic and/or a beta-blocker were administered concomitantly in constant dosage to 11 of the 20 patients who received bromocriptine. A wide range of doses of bromocriptine was tolerated. Side-effects of vomiting and postural hypertension did not occur, possibly due to the gradual increase in the administered doses. Plasma prolactin was not raised in this population of hypertensives. In the dose titration phase (n = 20), a small fall in diastolic but not in systolic blood pressure occurred with bromocriptine, but only with the patient standing and after exercise. In the double-blind phase (n = 9), there was no significant difference in blood pressure between the bromocriptine and placebo treatments. It is concluded that bromocriptine was not effective in lowering blood pressure in the present patients with essential hypertension.
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PMID:Bromocriptine in the treatment of hypertension. 351 42

Fifteen patients with hyperprolactinaemia and pituitary macroadenomas (5 patients), microadenomas (6 patients), or acromegaly (4 patients) were given a single intramuscular injection of 50 mg bromocriptine bound to polylactic acid microspheres, depot-bromocriptine. None of the patients had any short-term or long-term discomfort from the injection. In the 11 patients with prolactinomas, serum prolactin fell to minimum levels 12-72 h post-injection; nine patients were highly responsive to depot-bromocriptine, with a mean serum prolactin of 12.9% of basal levels 24 h post-injection, rising to 19% at 28 days. Two patients with prolactinomas were resistant to both depot-bromocriptine, and large doses of oral dopamine agonists. Initiating side-effects (nausea, vomiting, symptomatic postural hypotension) were seen in five patients in the first 24 h post-injection, but were minimal or absent thereafter. Five of six patients previously intolerant of oral dopamine agonists were able to be transferred successfully to bromocriptine 5 mg daily at 4 weeks. Of the four patients with acromegaly, raised prolactin levels were successfully lowered to normal for 4 weeks after injection; serum GH was also partially lowered, but returned to baseline levels at 2-4 weeks. In one patient serum GH was resistant to suppression by both depot bromocriptine and high doses of oral bromocriptine. One patient with a large tumour and visual field defects showed a rapid and maintained improvement in visual fields and acuity after depot-bromocriptine, and was successfully transferred to high-dose oral bromocriptine at 4 weeks.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Depot-bromocriptine treatment for prolactinomas and acromegaly. 370 74

Macroprolactinomas have a well-recognized potential for marked expansion during pregnancy. Measures advocated to minimize this risk include prior treatment with dopamine agonists, radiotherapy and pituitary surgery. We describe a patient who underwent transsphenoidal surgery with the removal of an histologically proven prolactin-secreting adenoma with the intention of rendering subsequent pregnancy safe. The patient remained hyperprolactinaemic and received prolonged therapy with metergoline and bromocriptine which suppressed prolactin to normal and she conceived after induction of ovulation with human menopausal gonadotrophin and human chorionic gonadotrophin. At 3 months gestation she developed headaches, vomiting, reduced visual acuity and bitemporal hemianopia caused by massive pituitary expansion. Reintroduction of bromocriptine rapidly abolished features of tumour expansion and after delivery of a full-term normal female infant, repeat CT scan documented tumour shrinkage.
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PMID:Failure of prophylactic surgery to avert massive pituitary expansion in pregnancy. 379 72

In order to investigate further the endocrine and metabolic features of the common condition emesis gravidarum, serum concentrations of some non-steroid hormones and tissue polypeptide antigen (TPA) were determined in 102 healthy pregnant women. 62 complained of nausea and vomiting in early pregnancy. Significantly higher and lower levels of human chorionic gonadotropin were noted in early and late pregnancy, respectively, in women with emesis gravidarum. A significant rise in serum prolactin and TPA was found throughout pregnancy in all subjects, no differences between emetic and non-emetic pregnancies being registered. Serum concentrations of growth hormone (hGH) showed a significant decline as pregnancy advanced. Emetic women demonstrated higher hGH levels in late pregnancy than did asymptomatic subjects. Free T4 concentrations remained stable when comparing early with late pregnancy, no dissimilarities being found between women with and without nausea and vomiting in pregnancy. These data do not support the hypothesis of major metabolic disturbances as an etiologic factor for nausea and vomiting in pregnancy. However, as overt differences between emetic and non-emetic pregnancy were found, hormonal factors may be involved in the pathogenesis of this condition.
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PMID:Non-steroid hormones and tissue polypeptide antigen (TPA) in emetic and non-emetic pregnancy. 381 48

Metoclopramide is a widely used anti-emetic drug with potent dopamine-blocking effects on brain structures involved in emesis and prolactin secretion but it is apparently devoid of therapeutic effect in schizophrenia, thus calling into question the supposed role of dopamine blockade in the action of antischizophrenic drugs. This investigation compared the depression of hypothalamic self-stimulation produced by metoclopramide and by a 'typical' neuroleptic, spiroperidol (spiperone), when injected by different routes. Metoclopramide was found to9 be nearly 30 times more potent when administered directly into the brain via the cerebral ventricles than when injected intraperitoneally; on the other hand the potency of spiroperidol was virtually unaffected by the route of administration. The blood-brain barrier is known to be absent from brain sites controlling emesis and prolactin secretion; thus the potency of metoclopramide as an anti-emetic and in releasing prolactin, and its relative ineffectiveness as an antipsychotic can be accounted for by a failure to enter the brain freely except at privileged sites. Thus its anomalous properties are not necessarily inconsistent with the dopamine theory of schizophrenia.
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PMID:Selective permeation of the blood-brain barrier as a cause of the anomalous properties of 'atypical'neuroleptics. 610 75

The substituted benzamide sulpiride is considered an "atypical" neuroleptic and antipsychotic in that its pharmacology and clinical effects differ significantly from "classical" dopamine antagonists such as the butyrophenones and phenothiazines. Sulpiride increases dopamine turnover, elevates prolactin release, inhibits emesis, and is an effective antipsychotic. Sulpiride does not affect other transmitters, requires sodium for binding, does not induce catalepsy in rats or strong sedation and extrapyramidal side effects in humans. Compared to the butyrophenone and phenothiazine neuroleptics sulpiride is chemically distinct because it lacks certain properties associated with other dopamine antagonists. Poor blood-brain barrier penetration and preferential receptor affinities in different brain regions are the most probable reasons for sulpiride's effects in vivo. Nevertheless, the atypical conformation of sulpiride merits study of its structure-activity relationships. Experimental determination of specific pharmacophores could provide the data necessary for a computer analysis of structure. Comparison of relative orientation of sulpiride's pharmacophores with similar data on classical neuroleptics is suggested for study of structural requirements for dopamine antagonism.
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PMID:Sulpiride: assessment of a pharmacologically and chemically distinct neuroleptic. 614 15

The endogenous catecholamine dopamine lowers blood pressure by acting on two receptor subtypes: dopamine 1 and dopamine 2. Dopamine 1 receptors subserve vasodilation, especially in the renal, coronary, mesenteric, and cerebral vascular beds. Dopamine 2 receptors have been located at the endings of postganglionic sympathetic nerves and, when activated, inhibit norepinephrine release. Inhibition of emesis and inhibition of prolactin release also appear to be dopamine 2-mediated phenomena. The receptor subtypes have been classified by differences in chemical structure of agonists and by specific antagonists. Dopamine also acts on beta 1 receptors to stimulate the heart and alpha 1 and alpha 2 receptors to cause vasoconstriction. Alpha adrenergic activity and lack of oral availability limit the use of dopamine in the treatment of hypertension. However, studies with the selective dopamine 1 agonist, fenoldopam, and dopamine 2 agonists such as LY 141865 and bromocriptine, indicate that agonists of both receptor subtypes can lower blood pressure in experimental animals and in hypertensive patients. Initial use of dopamine agonists in the treatment of hypertension and its possible involvement in the etiology and maintenance of hypertension are discussed.
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PMID:Dopamine receptors and hypertension. Physiologic and pharmacologic implications. 614 92


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