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)

Metoclopramide antagonizes the effect of dopamine in the central nervous system and other organ systems. Metoclopramide's effect on the medullary chemoreceptor trigger zone makes it useful as a routine anti-emetic and in preventing vomiting induced by antineoplastic drugs, particularly cisplatin. Metoclopramide's gastrointestinal smooth muscle stimulatory effects are related to its ability to antagonize the inhibitory neurotransmitter, dopamine; to augment acetylcholine release and sensitize the muscarinic receptors of the gastrointestinal smooth muscle; and to coordinate gastric-pyloric-small intestinal motor function. The indications for which metoclopramide is approved in the United States are reviewed. Adverse effects, which may occur in up to 20% of patients, include drowsiness, lassitude, and akathisia; all are usually mild, transient, and reversible. Tremor, dystonic reactions, and extrapyramidal effects are infrequent; breast enlargement, galactorrhea, and menstrual irregularities are related to prolactin release.
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PMID:Metoclopramide: pharmacology and clinical application. 633 44

Bulimia is a disorder characterized by episodes of binge-eating. Patients with this problem consume large amounts of food when binge-eating and, subsequently, to avoid weight gain, usually self-induce vomiting or induce diarrhea with laxatives. Metabolic and endocrine investigations in six bulimic subjects of normal weight are reported. Normal fasting plasma glucose concentrations and glucose tolerance were present in all. Five subjects had normal serum T4 and T3 concentrations. Only one subject had depressed serum T4 and T3 concentrations and this subject had a normal serum TSH level. Menstrual irregularities were present in all patients and, in three, were associated with modestly elevated serum prolactin levels. In four subjects there was an abnormal increase in serum growth hormone following TRH administration and in three, growth hormone failed to suppress normally after oral glucose. Two subjects were found to have a hypokalimic metabolic alkalosis, presumably due to vomiting. Urinary 17-OH steroid excretion and urinary concentrating ability were normal or nearly so in all subjects.
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PMID:Metabolic and endocrine investigations in women of normal weight with the bulimia syndrome. 640 13

The space adaptation syndrome is one of the more vexing problems confronted by our nation's astronauts during their journeys. This syndrome may be a variant of motion sickness, although this possibility has been questioned. Physostigmine, a centrally active cholinesterase inhibitor which increases brain acetylcholine, was found to cause a motion sickness-like syndrome--in psychiatric patients and normals--including nausea, emesis, malaise, dysphoria, increases in serum ACTH, beta-endorphin, cortisol, and prolactin, Neostigmine, a non-centrally acting cholinesterase inhibitor, and saline placebo caused no such effects. The above effects closely parallel those of motion sickness. Thus, the effects of physostigmine may be a convenient model for screening for treatments for motion sickness or space adaptation syndrome, or for predicting who will develop these syndromes.
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PMID:A cholinomimetic model of motion sickness and space adaptation syndrome. 648 3

The tolerance and prolactin (PRL) release-inhibiting action of the 8 alpha-aminoergoline, mesurlergine, were investigated. In a blind crossover study in six subjects with hyperprolactinemia, 0.5 mg mesulergine induced fewer side effects than did 2.5 mg bromocriptine, while the PRL release-inhibiting effect of the two was of the same order. Six different subjects with suspected PRL-secreting pituitary adenomas who (repeatedly) had to discontinue bromocriptine because of nausea, vomiting, or symptoms of orthostatic hypotension were treated for 20 mo with mesulergine (1 to 2 mg/day). Mesulergine did not induce side effects and its actions resembled those of bromocriptine. Mesulergine induced cessation of galactorrhea and resumption of normal menstrual cycles in five subjects, while in one subject an insufficient luteal phase persisted. No abnormalities in routine blood parameter estimations were observed. In two of three subjects there was shrinkage of a pituitary tumor after 12 to 15 mo on mesulergine. Mesulergine did not directly inhibit PRL release by cultured normal rat pituitary cells and human prolactinoma cells and it antagonized the action of dopamine in a dose-dependent manner. This suggests that the dopaminergic action is carried out by a metabolite of mesulergine, while the parent drug probably prevents the well-known side effects of dopamine-agonistic drugs by its dopamine receptor blocking activity. Because of its acceptability, mesulergine might be important in the treatment of hyperprolactinemia and perhaps also of acromegaly and Parkinson's disease.
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PMID:Mechanism of action and tolerance of mesulergine. 648 83

The selectivity, peripheral vs. central actions, of the antidopaminergic agent L-646,462 was assessed in two ways. First, elevation of prolactin in serum (peripheral) and homovanillic acid in the striatum were measured in rats. L-646,462 was found to have a central/peripheral activity ratio of 143, whereas comparable values derived for haloperidol, metoclopramide and domperidone were 1.4, 9.4 and 1305, respectively. Second, the ID50 values required to block apomorphine-induced emesis in beagles (peripheral receptor-mediated response) were compared with those required to block apomorphine-induced stereotypy (central receptor-mediated response) in rats. Central/peripheral ID50 ratios of 234, 9.2, 129 and 7040 were obtained, respectively, for L-646,462, haloperidol, metoclopramide and domperidone. The selectivity of L-646,462 for peripheral serotonin (5-HT) receptors in rats was determined by measuring its effectiveness in blocking 5-HT-induced paw edema (peripheral response) and 5-hydroxytryptophan-induced head twitch (central response); a ratio of 114 was obtained. This value agrees nicely with the ratio of 143 derived in the rat ( vide supra) for peripheral selectivity for dopamine receptors. L-646,462 is, therefore, selective in vivo, preferentially blocking dopamine and 5-HT receptors located outside the blood-brain barrier. With regard to dopamine-receptors, L-646,462 was about equipotent and more selective than metoclopramide, while being less potent and less selective than domperidone. Unlike metoclopramide or domperidone, L-646,462 also possessed a reasonably potent 5-HT receptor antagonist effect in vivo.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:L-646,462, a cyproheptadine-related antagonist of dopamine and serotonin with selectivity for peripheral systems. 654 78

A depot-estrogen preparation (12.5 mg of estradiol benzoate and 10 mg of estradiol phenylpropionate in 1 ml oily solution) was used as a 'morning-after' injection (MAI) in 100 women (average age, 26 years; range, 15 to 45) within 72 hours after unprotected coitus. Venous blood samples obtained before and after drug injection were analyzed for radioimmunology measurements of plasma LH, FSH, prolactin (Prl), estradiol-17B and progesterone. In 80% of cases, unprotected coitus occurred between days 10 and 18 of the cycle. In 97.8%, MAI was administered within 48 hours after unprotected coitus. The preparation induced minimal cycle and bleeding pattern changes. 4 pregnancies were observed after MAI administration within 37 hours. However, it was found that in 1 case, pregnancy had already existed before the MAI. Thus, postcotal contraceptive efficiency of MAI was 97%, or failure rate was 3%. The side effects (eg, nausea, vomiting, breast tenderness, discomfort at injection site) are minimal and incidence is lower than those associated with oral postcoital estrogens. Increasing dose of injectable estrogens may result in a more acceptable failure rate.
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PMID:Postcoital contraception with an injectable estrogen preparation (Org 369 - 2). 677 52

1. The clinical and experimental pharmacology of sulpiride, its effects on the CNS, gastrointestinal tract and cardiovascular system have been reviewed. 2. The majority of its actions are attributable to blockade of dopamine receptors. 3. Although sulpiride has a high affinity for dopamine receptors involved in emesis and prolactin secretion, it lacks part of the behavioural and biochemical profiles of the classical dopamine receptor antagonist neuroleptics. 4. In the cardiovascular system, sulpiride is a potent prejunctional dopamine receptor antagonist but has variable effectiveness in postjunctional dopamine receptor models. 5. These properties are discussed with reference to the mechanisms of action of sulpiride and the classification of dopamine receptors.
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PMID:The pharmacology of sulpiride--a dopamine receptor antagonist. 704 91

Ten women ages 22 to 39 years were treated with a single injection of Delestrogen on day 19 of the menstrual cycle and increasing doses of Parlodel on days 19 to 23. This treatment resulted in a shortening of the luteal phase and a decrease in the production of progesterone and had no effect on serum luteinizing hormone (LH), follicle-stimulating hormone (FSH), or prolactin levels. Side effects reported with this therapy included lethargy, dizziness, nausea, vomiting, hot flashes, depression, and nasal congestion. These preliminary clinical data suggest a combination of estrogen and bromocriptine regimen is luteolytic and may be useful as an interceptive abortifacient preparation in the human being.
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PMID:Evaluation of Delestrogen and Parlodel as a luteolytic agent in humans. 706 Jul 69

A 28-year-old woman with bilateral headaches and vomiting was found to have normal prolactin levels despite an eight-year history of intermittent galactorrhea and amenorrhea and the current finding of a pituitary microadenoma. The microadenoma contained hemosiderin. It is concluded that pituitary apoplexy is not confined to large tumors that have outgrown their blood supply, but can occur in microadenomas with regression of a positive endocrinopathy.
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PMID:Apoplexy in a prolactin microadenoma leading to remission of galactorrhea and amenorrhea. 719 10

Cabergoline is a synthetic ergoline which shows high specificity and affinity for the dopamine D2 receptor. It is a potent and very long-acting inhibitor of prolactin secretion. Prolactin-lowering effects occur rapidly and, after a single dose, were evident at the end of follow up (21 days) in puerperal women, and up to 14 days in patients with hyperprolactinaemia. In the only comparative study to date, cabergoline 0.5 to 1.0 mg twice weekly was more effective than bromocriptine 2.5 to 5.0 mg twice daily in the treatment of hyperprolactinaemic amenorrhoea, restoring ovulatory cycles in 72% of women and normalising plasma prolactin levels in 83%, compared with 52 and 58%, respectively, for bromocriptine. In the prevention of puerperal lactation, a single dose of cabergoline 1.0mg was as effective as bromocriptine 2.5mg twice daily for 14 days. A significantly lower incidence of rebound lactation in the third postpartum week was seen with cabergoline. Unpublished data suggest cabergoline 0.25mg twice daily for 2 days is effective in suppressing established puerperal lactation in about 85% of women. Nausea, vomiting, headache and dizziness are characteristic adverse events of the dopaminergic ergot derivatives. Cabergoline appears to be better tolerated than bromocriptine in both patients with hyperprolactinaemia and postpartum women. Most patients intolerant of other ergot derivatives can tolerate cabergoline. Bromocriptine use in the puerperium has been associated with an increased risk of serious thromboembolic events. However, there are no such reports with cabergoline and whether these events will become associated with other dopaminergic agents is unknown. The teratogenic potential of cabergoline has not been extensively investigated in humans. Ten congenital abnormalities have been reported in 199 cabergoline-associated pregnancies. Although there is no pattern to these abnormalities, the limited experience with cabergoline in pregnancy means the drug cannot be considered as a first-line therapy for the treatment of infertility associated with hyperprolactinaemia. At this stage of its development, cabergoline will prove useful in patients with hyperprolactinaemia who have failed treatment with, or are intolerant of, other dopamine agonists such as bromocriptine. If drug treatment is required for the prevention or suppression of puerperal lactation, cabergoline offers significant advantages over bromocriptine and should become the drug treatment of first choice for this indication.
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PMID:Cabergoline. A review of its pharmacological properties and therapeutic potential in the treatment of hyperprolactinaemia and inhibition of lactation. 772 32


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