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At least 1,297 records · Page 72Linked to original sources
PubMed1986

Antiemetic combination for cisplatin-induced emesis. Results from a controlled study.

Thirty-six patients suffering from disseminated epithelial tumors under treatment with Cisplatin alone or in combination with Vindesine entered a randomized, double-blind, cross-over study comparing the antiemetic activity of low-dose IV Metoclopramide (total dose: 0.8 mg/kg) with that of a combination of Metoclopramide (same schedule) plus Nortriptyline (2 X 50 mg PO) plus Thiethylperazine (3 X 10 mg IV). This combination was designed in an attempt to act simultaneously on gastrointestinal motility and neuroreceptors at central emetic pathways (Dopamine D-2, Histamine H-1 and muscarinic cholinergic). The antiemetic combination significantly reduces the median number of emetic episodes (p less than 0.01), the median volume of vomiting (p less than 0.01) and the median time of emesis (p less than 0.01) when compared with Metoclopramide alone and was also preferred by a significant number of patients (p = 0.0001) after passing through both antiemetic treatment arms being compared.

Adult↗
PubMed1985

Droperidol prevents and treats nausea and vomiting after enflurane anaesthesia.

One hundred and twelve women undergoing elective orthopaedic surgery under enflurane anaesthesia were given, in a double-blind random fashion, 2.5 mg of droperidol i.m. before anaesthesia, or 1.25 mg of droperidol or a saline placebo i.v. at the end of anaesthesia in an attempt to prevent post-operative vomiting. The administration of droperidol 1.25 mg (for those receiving initially 1.25 mg of droperidol) or saline (for those receiving initially 2.5 mg of droperidol or saline) was repeated i.m. during the 24 post-operative hours in a blind manner if the patient complained of nausea, retched or vomited. Significantly fewer patients (P less than 0.05) given i.m. or i.v. droperidol had emetic symptoms than patients given saline. Furthermore, 51% of the patients given saline needed additional doses of saline, whereas only 27% of the patients given i.m. and 36% of the patients given i.v. droperidol required a second dose (P less than 0.05 between groups). More of the patients given saline (23%) than those given droperidol (8% to 9%), as a blind drug (P less than 0.05), needed to be given additional droperidol as a known anti-emetic because of the failure of the blind drug to prevent or treat symptoms. It is concluded that droperidol given either as a single dose of 2.5 mg i.m. or in repeated doses of 1.25 mg i.v. is effective in the prevention and treatment of post-operative nausea and vomiting after enflurane anaesthesia.

Adult↗
PubMed1985

A misconception of motion sickness leads to false therapeutic expectations.

The emetic chemoreceptor trigger zone (CTZ), located in the area postrema of the medulla oblongata, is generally believed to be indispensable for the vomiting in motion sickness and, by extrapolation, also in space sickness. Accordingly, it has been postulated that a "motion vomiting substance" is secreted into the cerebrospinal fluid in the emetic process. Furthermore, certain therapeutic measures against motion sickness are aimed at preventing the presumed chemical stimulation of the CTZ. This concept originated from laboratory experiments in which ablation of the area postrema protected some dogs and monkeys against motion-induced vomiting. More recent experiments, however, showed that verified lesions of the area postrema were not effective in preventing motion sickness in cats. It appears that an indispensable unidentified element close to but separate from the area postrema was fortuitously destroyed in the earlier experiments. The overall evidence leads to the conclusion that the area postrema is not essential for motion-induced vomiting. Therefore, no functional basis exists for the postulation of a motion vomiting substance, and it is irrational for the treatment of motion sickness to seek pharmacologic blocking agents that act at the CTZ.

Aerospace Medicine↗
PubMed1979

[Vagal control of larynx resistance to the air flow (author's transl)].

Air flow larynx resistance changes have been recorded in dogs after electrical stimulation and lesion of the recurrent and vagus cervicalis nerves respectively. Experiments were carried out with glottis in situ and isolated. The effects of the administration of athropine i.v. (0.3 mg/kg) were also studied. Air flow larynx resistance decreased after secting the right recurrent nerves as well as after athropine administration. Electrical stimulation of the central end of the right vagus nerve produced a complex response characterized by an initial apnaea followed by a larynx resistance decrease. After a few seconds the response continued with glottis spasms followed by typical emetic movements. During the emetic movements larynx closed and opened throughout the respiratory cycle, the closing movement being simultaneous with the inspiratory position of the thorax and with minimal values of the intraabdominal pressure. Larynx resistance increased after uni- and bilateral sections of the vagus cervicalis and after the electrical stimulation of the peripheral end of the right vagus cervicalis. According to the present results, the possible existence of a controlling reflex of laryngeal sphincter motility, generated at the bronchopulmonary level, is postulated.

Airway Resistance↗
PubMed1978

Pharmacological studies on 3-[gamma-(p-fluorobenzoyl)propyl]-2,3,4,4a,5,6-hexahydro-1-(H)-pyrazino(1,2-a)quinoline hydrochloride (compound 69/183). Part IV: other CNS effects and acute toxicity.

3-[gamma-(p-Fluorobenzoyl)propyl]-2,3,4,4a,5,6-hexahydro-1-(H)-pyrazino(1,2-a)quinoline hydrochloride (centpyraquin), a potent antihypertensive and tranquillising agent, was tested for anticonvulsant, analgesic and anti-inflammatory activities in mice and for anti-emetic activity in dogs. It did not modify supramaximal electroshock seizures and failed to protect the animals against pentylenetetrazole and strychnine induced convulsions. It, however, produced some elevation in the threshold dose of strychnine. Tremorine induced tremors and salivation were not antagonised. The compound had weak analgesic activity as detected by antagonism to phenylquinone writhing and the hot plate test. It had no anti-inflammatory activity. Centpyraquin had strong anti-emetic activity against apomorphine as well as morphine. At high doses it produced fall out in the rota-rod test. The LD50 of centpyraquin in mice was 296 mg/kg i.p. and more than 1000 mg/kg p.o. and in rats it was 161 mg/kg i.p. and more than 800 mg/kg p.o. The observed CNS effects resemble those of other neuroleptics.

Analgesics↗
PubMed1981

Ipecac syrup for poisonings at home: availability, compliance, and response monitored by telephone.

Ipecac syrup administration at home, following advice by a poison center, was evaluated with respect to the availability of ipecac syrup, length of storage time, compliance with recommended procedures for administration, and time for emetic response. In a three-month period, staff pharmacists of the center completed a survey from when they advised 60 callers to administer ipecac syrup at home. Two follow-up phone calls were made to collect additional data. Fifty-five callers provided adequate data for analysis. Ipecac syrup was available at home for 36%, from a pharmacy for 53%, and from a neighbor for 11% of the callers. Compliances with the recommended doses of ipecac syrup and fluids (+/- S.D.) were 92 +/- 20% and 71 +/- 29%, respectively. Following one dose of ipecac syrup, 86% vomited in 19 +/- 8 minutes; after a second dose, 13% responded in 34 +/- 21 minutes after the first dose. By comparison with those who had ipecac syrup at home, there was an insignificant delay in administration when it was obtained from a neighbor; a significant delay (p less than 0.005) occurred when it was obtained by a pharmacy. The onset of emesis did not correlate with the length of time the ipecac syrup had been stored at home. The findings support the use of ipecac syrup at home based on ready availability, adequate compliance, and rapid emetic response.

Child↗
PubMedDate not supplied

Double-blind comparison of the antiemetic effects of nabilone and prochlorperazine on chemotherapy-induced emesis.

The antiemetic effect of oral nabilone, a synthetic cannabinoid, given at a dose of 2 mg every 12 hours was compared to oral slow-release capsules of prochlorperazine given at a dose of 10 mg every 12 hours by a double-blind crossover method in 37 patients receiving cancer chemotherapy. Patients received one of the following as the primary emetic stimulus: high-dose cis-dichlorodiammineplatinum(II) (DDP), low-dose DDP, mechlorethamine, streptozotocin, actinomycin D, or DTIC. Although results varied according to strength of emetic stimulus received, both nabilone and prochlorperazine appeared to produce antiemetic effects. Eighteen of the 37 patients achieved a complete or partial elimination of symptoms: seven with nabilone alone, three with prochlorperazine alone, and eight with each drug. Nabilone appeared to be the more effective antiemetic for patients who received chemotherapy agents other than high dose DDP; it was equivalent to prochlorperazine for those who did receive high-dose DDP. Side effects from prochlorperazine were limited to mild drowsiness occurring among 35% of the patients. The side effects from nabilone were drowsiness and dizziness which occurred frequently and were dose-limiting in 25% of patients.

Adult↗
PubMedDate not supplied

Double-blind crossover trial of droperidol, metoclopramide, and prochlorperazine as antiemetics in cisplatin therapy.

Droperidol, metoclopramide, and prochlorperazine were compared in a double-blind crossover trial to determine their relative effectiveness in preventing and controlling the nausea and vomiting caused by cisplatin-containing chemotherapy. Twenty-five patients receiving cisplatin-containing chemotherapy for various malignancies were entered into this trial with 14 patients completing the three-drug randomization sequence. This was the patient's first exposure to cisplatin. Each antiemetic was administered in a diluted 50 ml i.v. injection over 15 minutes beginning 0.5 hour before cisplatin and 1.5, 3.5, 5.5, and 8.5 hours after cisplatin. Dosages of antiemetics for doses of cisplatin greater than or equal to 100 mg/sq m were droperidol 2.5 mg, metoclopramide 2 mg/kg, or prochlorperazine 5 mg in each infusion. For doses of cisplatin less than 100 mg/sq m, the dosages were droperidol 2.5 mg for the first two doses and 1.25 mg for subsequent doses, metoclopramide 1 mg/kg, or prochlorperazine 5 mg for each dose. The median number of emetic episodes for the first 24 hours were as follows: droperidol 3.2; metoclopramide 1.8; prochlorperazine 3.7. There was a significant difference in number of emetic episodes demonstrating antiemetic superiority of metoclopramide over both droperidol and prochlorperazine. For these 14 patients completing the trial, eight preferred metoclopramide, two preferred prochlorperazine, one preferred droperidol, and three had no preference. At the doses used in this study, the antiemetic efficacy of metoclopramide was superior to either droperidol or prochlorperazine.

Adult↗
PubMed1984

Cisplatin-induced vomiting eliminated by ablation of the area postrema in cats.

Cisplatin-induced emesis was characterized using the cat as an experimental model. The incidence, latency, and number of vomiting episodes which occurred over an 8-hour period were determined for iv doses ranging from 3 to 10 mg/kg. Oscillographic recording of physiologic pressures which produce vomiting served to document the observation that 7.5 mg/kg iv was the most effective dose. This dose produced vomiting in seven animals with a latency of 71 +/- 7.04 minutes (mean +/- SE) and subsequent emetic episodes (averaging 3.86/animal) followed a linear relationship with respect to the logarithm of time. The larger dose of 10 mg/kg appeared to be less effective, because not all animals responded. Those animals that vomited in response to this dose did so only after a significantly increased latency. Four animals with longstanding lesions of area postrema were tested with cisplatin (7.5 mg/kg); all four failed to vomit during a 6-hour observation period. In addition, none of the animals exhibited the sustained malaise associated with cisplatin administration to intact animals and only one displayed any prodromal emetic signs. These findings demonstrate that the area postrema, the anatomic site of the chemoreceptor trigger zone for emesis, is essential for cisplatin-induced vomiting. Elucidation of this action suggests a possible mechanism for other emetogenic anticancer agents.

Animals↗
PubMed1981

A comparison of droperidol and metoclopramide in the treatment of nausea and vomiting during cis-platinum polichemotherapy in ovarian carcinoma.

A comparison was made of the anti-emetic effects of Droperidol (total dose: 5 mg e.v.) and Metoclopramide (total dose: 30 mg e.v.), on 7 patients affected by advanced ovarian carcinoma and undergoing polychemotherapeutical treatment with courses including 50 mg/mq-doses of Cis-Dichlorodiaminoplatinum (DDP). Although no significant difference was observed between the emetic-control effects of the two substances, Droperidol was preferred by all patients, owing to its subjective effects.

Antineoplastic Agents↗
PubMed1980

A comparative study on the clinical effects of rectal diazepam and pentobarbital on small children. Relationship between plasma level and effect.

In order to test the possible differences in the clinical effects between benzodiazepines and barbiturates, 5 mg of diazepam and 60 mg of pentobarbital were used in a double-blind study as rectal premedication in 75 small children before major surgery. There were no significant differences between the two groups in the six parameters tested (demeanour in the anaesthetic room, preoperative emetic effect, response to venepuncture, degree of salivary suppression, postoperative state in the recovery room, postoperative emetic effect). The concentrations of pentobarbital and diazepam (and its 3 active metabolites) in the plasma were determined by gas chromatography and correlated with the clinical effects. No significant correlation was found between the total active benzodiazepine concentrations and the clinical effects of rectal diazepam. In contrast to diazepam, a weak but significantly positive correlation between the plasma concentrations of pentobarbital and the total score was found. Similarly, the plasma level of pentobarbital and the response to venepuncture and the degree of salivary secretion were in correlation with each other. In the plasma concentrations of both pentobarbital and total benzodiazepines, a wide interindividual variation was observed, indicating irregular rectal drug absorption.

Child, Preschool↗
PubMed1995

[Pharmacokinetic investigation of 5-day multiple dose of tropisetron capsule in patients who had received cisplatin and the usefulness of tropisetron capsule in the treatment of nausea and vomiting].

We have investigated the pharmacokinetics of a 5-day multiple oral dose of 5 mg tropisetron capsule in patients with malignant tumour who had received cisplatin single administration. Its anti-emetic effects on acute and delayed emesis and vomiting were also investigated. During the 5 days after this administration, changes in the release and metabolism of serotonin were investigated. The results may be summarized as follows: 1) The pharmacokinetic parameters of tropisetron revealed no significant change in the data between day 1 and day 5. Also, the parameters were almost similar to those observed in healthy adult males (clinical phase I study); Cmax. T1/2 and AUC 0-24 hrs on day 1 were 9.1 +/- 2.1 ng/ml, 12.5 +/- 4.2 hrs, 85.5 +/- 22.7 ng.hr/ml, respectively. The urinary excretion of the parent drug up until 24 hours after administration on day 1 was 3.8% of the dose administered and 2.9% of the total dose after the last administration; no difference in the urinary excretion rate was observed in healthy subjects. It was thus suggested that hydration accompanied by cisplatin administration did not affect the pharmacokinetics of tropisetron. 2) The changes in the amount of urinary excretion of 5-hydroxy-indoleacetic acid (5-HIAA) during 5 days after cisplatin administration were observed; urinary excretion of 5-HIAA increased 2.3 times (1.3-5.4 times) the baseline on the average during 6 to 12 hours on day 1. In 6 out of 10 patients, the increases in urinary excretion of 5-HIAA showed double or more the baseline during 2 to 5 days after cisplatin administration. Serotonin was thus deemed to be related to the development of delayed emesis. 3) The anti-emetic effects of tropisetron on acute and delayed emesis and vomiting were rated as "markedly effective" in 6 out of 11 patients (54.6%) and "effective" in 1 out of 11 patients (9.1%) on day 1; vomiting did not occur in any of these 7 patients. Tropisetron also controlled emesis and vomiting during days 2-5, and was rated as "almost favorable" in 6 out of 11 patients (54.5%). Further, in 4 out of 6 patients, in whom the urinary excretion of 5-HIAA was increased on day 2 onwards, vomiting did not occur during the time when the urinary excretion of 5-HIAA was increasing. On the basis of the above results, tropisetron is deemed to have certain antiemetic effects on delayed vomiting as well. Its 5-HT3 receptor mediated mechanism was similarly seen to inhibit acute nausea and vomiting.

Adult↗
PubMed1978

Apomorphine as a preferential stimulant of self-inhibitory dopamine receptors in man.

In man, non emetic doses of apomorphine elicit a series of behavioural, neurological and psychological changes which are difficult to ascribe to the stimulation of postsynaptic dopamine receptors. Since similar effects are elicited by neuroleptic drugs, the functional changes induced by apomorphine in man might be interpreted as being the result of a decreased dopaminergic activity. The sedation and sleep, the improvement of choreic movements and the antipsychotic effect induced by non emetic doses of apomorphine are prevented by specific dopamine receptor blockers. These responses therefore are mediated through a stimulation of dopamine receptors leading to a decreased dopaminergic transmission. This new type of receptors might be identified with the so called "self-inhibitory" dopamine receptors.

Apomorphine↗
PubMed1994

[Efficacy of ondansetron in radiation-induced nausea and vomiting: review of the literature].

Radiotherapy-induced emesis depends on the site of irradiation, the field size and the dose per fraction and is generally less intense than chemotherapy-induced emesis. Established anti-emetic drugs offer only limited symptom control (50%). Ondansetron, a 5HT3 receptors antagonist, had proven a complete or a major control efficacy (0-2 emetic episodes) of 68 to 95% in three pilot studies (fractionated, single-dose and total body irradiations). In controlled studies, ondansetron efficacy was significantly higher than placebo, metoclopramide and prochlorperazine. The treatment was well tolerated in the different studies.

Humans↗
PubMed1975

Biological activity and complementation of the two peptides of staphylococcal enterotoxin B formed by limited tryptic hydrolysis.

Tryptic hydrolysis after reduction and carboxamidomethylation of staphylococcal enterotoxin B cleaved the single susceptible bond located between the 2 half-cystines of the molecule, Lys-Thr at positions 97 and 98 (Spero, L., Warren, J. R., and Metzger, J. F. (1973) J. Biol. Chem. 248, 7289-7294). The product remained as a single particle but was separated into the two constituent peptides by denaturants, and purification of the two fragments was accomplished by chromatography on CM-cellulose in 8 M urea. Antigenic activity was exhibited by the separated peptides after dialysis of urea solutions against dilute buffer, but was very labile. No emetic activity in rhesus monkeys was found for either separated peptide. The derivative behaved as two random coil peptides in 6 M guanidine hydrochloride but upon removal of guanidine refolded to a single molecular entity. Viscosity and unfolding kinetics in 1.5 M guanidine indicated physical identity of the recombined peptides with the derivative prior to treatment with guanidine. Three biological measures (serological, mitogenic, and emetic activity) were also essentially unaltered for the recombined material. Since these biological activities are dependent upon different aspects of enterotoxin structure, it is concluded that the recombined derivative was restored to its original conformation.

Animals↗
PubMed1975

Preliminary report on some clinical and biochemical observations in patients treated with Bilharcid.

Tartar emetic (potassium antimony tartrate) has been used since a long time as the drug of choice for the treatment of Bilharziasis in Egypt. This drug, though effective, has severe side effects. A newly synthesized trivalent antimony preparation (piperazine di-antimonyl tratrate) Bilharcid, has proved in animal experiments to be less toxic, more effective, and having little side effects. The drug was tried in various schemes on various age groups of patients infected with S. haematobium. Control cases were treated with tartar emetic. Urine analysis was done for the detection of living or dead ova before and after treatment. E.C.G., alkaline phosphatase, serum transaminase, lactic dehydrogenase, and urea tests were done before and after treatment. Follow up studies were recorded for three months after treatment. Results are presented in the full text.

Adolescent↗
PubMed1993

[Antiemetic effect of ondansetron in recurrent chemotherapy with cisplatin].

Six hundred and twenty-eight courses of cisplatin containing chemotherapy were recorded in patients receiving up to three courses of cytotoxic drugs with ondansetron (OND) given as an antiemetic agent (32 mg as a single iv dose or as a continuous infusion). The sample size of patients decreases from one course to another due to phenomena which may or may not be related to the chemotherapy and the anti-emetic treatment or to the evolution of the cancer disease. For patients with incomplete response to ondansetron, withdrawals could be related to an insufficient antiemetic effect as is known with other antiemetic drugs. Conversely, it is not the case for patients who had a complete response. Therefore, to avoid any bias due to patient selection, the analysis is based on the probability of changes from complete to incomplete response or from complete to complete response between two subsequent courses (i and i + 1). The response to OND treatment for the course i + 1 depends not only on the efficacy during this course (i + 1) but also on the response during the prior course (i). A discrete time-dependent statistical model (Markov chain) was used to test the evolution of the probability of remaining in complete response. This probability was equal to 66% between the first and the second course, and to 88% between the second and the third one. The probability of remaining in complete response significantly increased during repeated courses (P = 0.001). These results show that in patients for whom OND treatment allows a complete antiemetic control during the first course of chemotherapy, the probability of remaining with no emetic episodes at all increases during the two subsequent courses.

Adult↗
PubMed1993

[An outline of 5-HT3 receptor antagonists (1)--In pharmacological actions].

This paper described an outline of pharmacological studies of 5-HT3 receptor antagonists, mainly on ondansetron, which control nausea and vomiting associated with cancer chemotherapy. Administration of cytotoxic drugs is known to increase serotonin (5-HT) concentrations, and when released, 5-HT provokes the emetic responses via two routes; 1) 5-HT acts as an intrinsic transmitter substance and stimulates the emetic response via 5-HT3 receptors on vagal afferent terminals; 2) 5-HT transmits impulses to the vomiting center via 5-HT3 receptors on the chemoreceptor trigger zone in the area postrema of the central nervous system. 5-HT3 receptor antagonists are thought to exert an antiemetic action by specifically and competitively blocking 5-HT3 receptors.

Antiemetics↗