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Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The chemistry, pharmacology, pharmacokinetics, adverse effects, and dosage of clomipramine hydrochloride are described, and clinical studies of the use of clomipramine in treating obsessive-compulsive disorder (OCD), other psychiatric conditions, and chronic pain are reviewed. Clomipramine hydrochloride, a tricyclic antidepressant, is a potent inhibitor of serotonin reuptake and may affect dopaminergic neurotransmission, suppress rapid eye movement sleep, produce changes in electrocardiograms, and elevate plasma prolactin. The drug is well absorbed from the gastrointestinal tract and undergoes extensive first-pass metabolism. Peak plasma concentrations occur three to four hours after a 150-mg oral dose. The mean elimination half-life is 39 hours. Some 66% of a dose is excreted in the urine, the remainder being eliminated in the feces. In clinical trials, clomipramine was significantly more effective than placebo, clorgiline, amitriptyline, imipramine, and doxepin in ameliorating the symptoms of OCD. Initial effects are seen at four weeks; improvement may continue for up to 18 weeks. Clomipramine may also be effective in treating panic attacks, phobias, depression, and chronic pain. The most common adverse effects of clomipramine are anticholinergic; others include nausea, seizures, and sexual difficulties. Interactions between clomipramine and barbiturates, haloperidol, monoamine oxidase inhibitors, and cigarette smoking have been documented. The usual initial adult dosage is 25-50 mg/day, titrated gradually to 250 mg/day if necessary. Clomipramine hydrochloride is a welcome new agent for the treatment of obsessive-compulsive disorder. Although its adverse-effect profile is like that of other tricyclic antidepressants, sexual dysfunction and seizures may be more frequent with this agent and limit its use.
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PMID:Clomipramine: an antiobsessional tricyclic antidepressant. 218 Jun 23

Hyperprolactinemia can successfully be treated by dopaminagonists such as bromocriptin or lisuride. About 10% of patients complain about side effects like orthostatic hypotension, nausea or vomiting, which may lead to discontinuation of treatment. We therefore conducted a study using terguride--a new dopaminagonist--in 5 patients with hyperprolactinemia and intolerable side effects under conventional treatment. Terguride is the transdihydroderivative of lisuride (Dopergin). We treated 5 patients, 2 men with macroprolactinoma and 3 women with microprolactinoma with terguride. The mean duration of treatment was 15.6 months (7-37 months). Patients were treated with up to 5 mg terguride daily. All 5 patients had a marked initial decrease of elevated prolactin levels 8 h after administration of 0.25 mg terguride orally. Three patients became normoprolactinemic after sufficient increase of the dose of terguride, 2 female patients with a microprolactinoma got eumenorrhoeic thereafter. The treatment with terguride was tolerated without side effects by all patients. There were no significant changes of the examined parameters of clinical chemistry nor the other pituitary hormones. Results of cranial computertomography did not change in 4 patients, one patient had tumor progression. Tergurid as a dopaminagonist is an effective inhibitor of prolactin with little side effects and thus a useful drug in the treatment of hyperprolactinemia.
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PMID:[Terguride in hyperprolactinemia--experiences with 5 patients]. 218 44

To examine further the serotoninergic system in obsessive-compulsive disorder (OCD), the plasma concentrations of cortisol and prolactin and the behavioral responses after oral administration of MK-212 (6-chloro-2-[1-piperazinyl]-pyrazine), a serotonin agonist, and placebo were studied in 17 patients with OCD and nine normal controls. The two groups did not differ significantly in basal plasma prolactin or cortisol levels. Nevertheless, both the prolactin and cortisol response to oral administration of MK-212 (20 mg) were significantly blunted in the patients with OCD compared with those of the normal controls. MK-212 did not affect the intensity of OCD symptoms. However, MK-212, as compared with placebo, produced slight but statistically significant increases in self-ratings of nausea, dizziness, anxiety, feeling strange, and mixed feelings of calmness and restlessness, as well as depression and feeling high. These behavioral ratings were not significantly different in patients and normal controls. These findings are consistent with previous reports of diminished serotoninergic responsivity in OCD and raise the possibility of subsensitivity of at least some serotonin receptors in this disorder.
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PMID:Prolactin and cortisol responses to MK-212, a serotonin agonist, in obsessive-compulsive disorder. 220 27

Thirteen women with hyperprolactinemic amenorrhea were treated with lisuride (Dopergin, Schering AG, Germany). The dosage of lisuride was started with 0.1 mg per day and increased to 0.2 mg per day after one week of treatment. Further increment of the drug depended on clinical and laboratory responses of the patients. One patient dropped out from the study due to marked nausea and dizziness. In ten out of twelve patients serum prolactin decreased to normal. Most patients received lisuride 0.2-0.4 mg per day. Only one got more than 0.4 mg per day. Two patients whose serum prolactin levels did not decrease to normal range had uterine bleeding, quite regularly. Menstrual cycle resumed within 23 to 141 days. All galactorrhea disappeared during treatment. Two of five patients who desired pregnancy became pregnant during the treatment. The course and outcome of pregnancies were normal. Common side effects of lisuride treatment were nausea and dizziness. In conclusion, this study demonstrated that lisuride is another effective prolactin inhibiting agent even at low dose. This drug provides an alternative treatment to bromocriptine.
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PMID:The efficacy of lisuride in the treatment of hyperprolactinemic amenorrhea. 235 12

1. SK&F 101468, a non phenolic indolone derivative, has been characterised preclinically as a novel, potent and specific dopamine D2-receptor agonist. 2. Its tolerability and effects on serum prolactin were investigated in 14 healthy male volunteers in a study of the first administration of SK&F 101468 to man. 3. Doses between 80 micrograms and 2.5 mg caused statistically significant (P less than 0.05) lowering of basal and food stimulated serum prolactin, relative to placebo, over a 6 h post treatment period. 4. SK&F 101468 was well tolerated up to 1 mg with symptoms of nausea and postural hypotension at higher doses.
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PMID:A dose rising study of the safety and effects on serum prolactin of SK&F 101468, a novel dopamine D2-receptor agonist. 257 51

In this pilot clinical trial conducted in 10 postmenopausal women with advanced breast cancer, we evaluated the endocrine effects and toxicity of combined somatostatin analog and dopaminergic therapy in the attempt to suppress both growth hormone (GH) and prolactin (PRL) secretion. The patients' mean age was 63 years (range: 54-77) and the average number of previous treatments was 4.8 +/- 2 (SD). All patients were treated with the somatostatin analog SMS 201-995 (100-200 micrograms s.c. in a.m. and h.s.) and bromocriptine (2.5 mg orally twice a day). During treatment, GH levels following provocative testing (either L-DOPA or insulin-induced hypoglycemia) were suppressed in 7/9 patients. Basal somatomedin-S (Sm-C) levels declined in 6/9 women. Both GH and Sm-C levels decreased in 4 patients, while in the remaining 5 only one of the two parameters was lowered on treatment. PRL secretion (during provocative TRH testing) was almost totally abolished in 8/9 patients. The treatment did not affect circulating levels of FSH, LH, E1, E2, E1-S, T4, T3RU, or cortisol. Seven patients experienced no side effects. Nausea occurred in 3, but was severe enough in only one to require discontinuation of therapy. One patient experienced disease stabilization consisting of less than 50% regression of skin nodules and pleural effusion, a decline in CEA titer, and an improved performance status lasting 7 months. We conclude that combined SMS 201-995 and bromocriptine therapy is safe and frequently suppresses GH and PRL secretion. Its role in the treatment of metastatic breast cancer should be tested in patients with less advanced disease.
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PMID:Endocrine effects of combined somatostatin analog and bromocriptine therapy in women with advanced breast cancer. 257 6

CV 205-502 (Sandoz), an octahydrobenzol [g]quinoline, is a long-acting dopamine agonist which inhibits prolactin secretion. We conducted a phase 2 clinical study in 10 hyperprolactinaemic women (nine of whom were previously intolerant of bromocriptine) in order to determine (1) the dose at which CV 205-502 exerted its prolactin-lowering effect; (2) the nature of adverse reactions associated with long-term therapy; and (3) whether patients who were intolerant of bromocriptine could tolerate CV 205-502. At first patients were randomized to take initial doses of either 0.02 or 0.05 mg daily at bedtime. Thereafter these doses of medication were gradually increased either to the point of normalizing serum prolactin (to 0.70 IU/l or 20 ng/ml) or to a maximum dose of 0.14 mg daily. The lower initial dose was ineffective and had to be increased in all patients. The higher initial dose (0.05 mg) normalized prolactin in three of five women within 24 h. During chronic administration of the final dose of CV 205-502 (mean 0.09 mg a day), serum prolactin decreased from a mean level of 9.19 +/- 4.9 (SEM) IU/l to a mean level of 1.55 +/- 0.49 IU/l (n = 10 patients). Prolactin was normalized in five patients. Two patients, one of whom had been previously unresponsive to bromocriptine, and another unresponsive to pergolide with regard to prolactin inhibition, were also unresponsive to CV 205-502. Nausea, the side-effect responsible for these patients' previous intolerance of bromocriptine, occurred in six of 10 patients taking CV 205-502 but was much less disabling and did not cause any of the patients to stop this medication. Only one patient taking CV 205-502 discontinued treatment because of adverse effects (light-headedness).
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PMID:Effect of CV 205-502 in hyperprolactinaemic patients intolerant of bromocriptine. 257 97

Vomiting represents one of the most dangerous complications of general anesthesia. L-sulpiride has been able to control this complication very effectively. We studied the effect on vomiting of two doses of L-sulpiride (50/100 mg). Both these doses have been effective in reducing the episodes of vomiting other than in preventing nausea and retching if considered versus controls and also versus droperidol at the doses of 5 mg (50 mg L-sul = 12%, 100 mg = 4%, droperidol = 20%, controls = 28%). L-sulpiride is an antagonist of dopamine on D2 receptors therefore inhibits the action of dopamine increasing the secretion of prolactin. During the surgical distress per se prolactin levels are increased. Together with the increment of catecholamines, high concentration of prolactin can evoke arrhythmias. In view of this possibility we studied the time course of the administration of the two doses of L-sulpiride and of droperidol on prolactin secretion. Both of the drugs increased the plasma levels of prolactin. Droperidol-induced increase in prolactin secretion was significant already at ten minutes after the administration reaching the peak after 20 minutes. L-sulpiride increased prolactin secretion reaching the maximum increase 20 minutes after the administration of 50 mg of the drug, and 30 minutes after the administration of 100 mg doses. The hyperprolactinemizing action of droperidol lasts for at least 8 hours, whereas L-sulpiride action lasts 4 hours.
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PMID:[Antiemetic effect of the levo isomer of sulpiride (L-sulpiride) in humans]. 260 63

17 hyperprolactinemic and 2 acromegalic patients, aged 19-73, and 47 and 59 years, respectively, were treated with Lisuride (dopergin). 12 of the hyperprolactinemic patients were treated with Lisuride because they could not tolerate the side effects of bromocriptine (Group A), and the other 5 because large doses of bromocriptine failed to reduce their plasma prolactin to normal (Group B). The 2 acromegalic men, were treated with Lisuride because of persistently high levels of growth hormone after hypophysectomy and irradiation of the sella turcica, and because of intolerance to bromocriptine. Lisuride reduced prolactin to normal in 11 of the 12 in Group A (from 217 +/- 175 to 27 +/- 10 micrograms/l, p less than 0.01) and reduced it in the last patient from 3900 to 270 micrograms/l. The prolactin-lowering effect of Lisuride was unsatisfactory in Group B since like bromocriptine, it failed to reduce prolactin levels. One of the acromegalics improved both clinically and biochemically and growth hormone levels were reduced from 56 to 18 ng/ml, while the other did not respond to Lisuride. Its main side effects were somnolence, nausea, and increased appetite (4 patients). These effects lasted only a few weeks. One patient stopped Lisuride because of severe constipation, which had been caused by bromocriptine as well. Lisuride is an effective drug in hyperprolactinemia, especially in those with severe side effects after other dopaminergic drugs. It is effective in some cases of acromegaly, but has little to offer to those resistant to bromocriptine.
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PMID:[Treatment of hyperprolactinemia and acromegaly with lisuride]. 279 46

1. A phase I study of OPC-4392 (OPC), a quinolinone derivative recently developed in Japan and recognized to have an agonistic effect on dopamine autoreceptors, was performed in 7 male healthy volunteers in comparison with chlorpromazine (CPZ). 2. Clinical pharmacology The main clinical symptoms of OPC were sleepiness, weakness, fatigability, heavy headedness, disturbance of concentration, nausea, etc. The severity of these symptoms increased dose-dependently, and the upper limit dosage of OPC was considered to be 5 mg for the healthy volunteers. 3. Endocrinological research The serum prolactin level decreased dose-dependently in the OPC group, whereas it rose in the CPZ group. A significant negative correlation was recognized between the OPC-plasma level and serum prolactin level as well. 4. Psychological tests In the Kraepelin test, a decrease in the average work quantity was observed in both groups, but it was less in the OPC group. 5. Pharmacokinetic study From the pharmacokinetic parameters measured, two features were recognized: one was the slowness of Tmax (4-6 hours) and the other was the length of its biological half-life (56-88 hours). It was estimated that the plasma level of OPC-4392 would take 2 weeks to reach a steady state.
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PMID:Phase 1 study of a new antipsychotic drug, OPC-4392. 290 59


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