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Results for “Antiemetics”

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PubMedDate not supplied

An apomorphine-induced vomiting model for antiemetic studies in man.

Apomorphine-induced vomiting is often used for preclinical efficacy testing of putative antiemetics in normal volunteers. The usual technique of individual intravenous titration for finding the threshold emitic dose of apomorphine in each subject is slow and tedious. We used a uniform dose of 0.05 mg/kg apomorphine given subcutaneously to test the antiemetic action of metoclopramide and votracon in ten healthy, young male volunteers. All ten subjects vomited in response to this dose of apomorphine when pretreated with placebo. Pretreatment with metoclopramide prevented vomiting in all subjects, and votracon prevented vomiting in two. Apomorphine, 0.05 mg/kg, subcutaneously appears to be an appropriate challenge dose for testing compounds for antiemetic activity in normal human volunteers.

Adult↗

PubMed1978

Rapid emesis from high-dose ipecac syrup in adults and children intoxicated with antiemetics or other drugs.

The effect of ipecac syrup as an emetic in adults as well as children who had ingested antiemetics or other drugs was evaluated. Adults or children over five years of age were given 30 ml of ipecac syrup followed by 360 ml of water; children aged one to five years were given 15 ml ipecac syrup followed by 240 ml of water. If emesis was not induced within 30 minutes, a second dose was administered. Of 232 patients studied (199 adults and 33 children), 188 (81%) vomited following the first dose, 34 (15%) required two doses and seven (3%) did not vomit. Of 63 patients who had ingested drugs with antiemetic properties, 51 (81%) vomited following the first dose, nine (14%) required a second dose and three (5%) did not vomit. The time from ipecac administration to the onset of emesis in all 232 patients averaged 24.2 minutes. Ipecac was successful in inducing rapid emesis in both adults and children who had ingested antiemetics or other drugs, probably as a result of its irritating effect on the gastric mucosa.

Adolescent↗

PubMed1979

delta 9-Tetrahydrocannabinol (THC) as an antiemetic in patients treated with cancerchemotherapy; a double-blind cross-over trial against placebo.

A double-blind cross-over trial with delta 9-tetrahydrocannabinol (THC) and placebo was employed to test the antiemetic effect on nausea and vomiting after MOPP-therapy. Although THC had remarkable antiemetic effects, the side effects were severe. Most patients preferred the nausea and the vomiting after MOPP-therapy to the use of THC. A relation between the antiemetic action or the side-effects and the blood-level of THC could not be demonstrated.

Adult↗

PubMed1977

Nabilone: a potent antiemetic cannabinol with minimal euphoria.

Nabilone is a cannabinol derivative which has potent central antiemetic effects in animals. We observed that the drug significantly reduced the nausea and vomiting induced by cancer chemotherapy in 10 of 13 patients who were refractory to conventional antiemetics. A dose-response effect was apparent. The drug was generally well-tolerated, although it also had sedative effects. Additionally, dizziness, decreased coordination and postural hypotension were observed in some patients. Euphoric effects of the agent were minimal at antiemetic dosage levels.

Adolescent↗

PubMed1976

[Effectiveness of several antiemetics in vomiting induced by orally administrated copper sulfate in cats and dogs].

Long marketed antiemetics, which are still used in medicine or veterinary medicine and whose sites of actions were either assumed to be peripheral or unknown, were subjected to evaluation as antiemetics, against oral copper sulfate emesis. In cats, ethyl aminobenzoate 0.5 g/head, cerium oxalate 0.1 g/head, pinelliae tuber 0.5 g/head and gelatin 2.0 g/head were not effective. In dogs, ethyl aminobenzoate 0.5 g/head, pinelliae tuber 2.0 g/head and hange-syasintoo 2.0 g/head were not effective. Cerium oxalate 0.1 g/head was found to have a slight antiemetic action.

Aminobenzoates↗

PubMed1978

Antiemetic effect of droperidol after ophthalmic surgery.

Postoperative nausea with emesis is an undesirable side effect of general anesthesia in patients who have undergone ophthalmic surgery. The antiemetic effect of intravenous droperidol (Inapsine) was measured in a double-blind, controlled study of 78 patients undergoing general (enflurane [Ethrane]) anesthesia for a variety of ophthalmic procedures. There was a significant difference in the incidence of postoperative nausea and/or emesis in the droperidol-treated group, 13 of 78 (16%) as compared with the control population (37 of 87 [42%]). No complications of droperidol administration were observed. Droperidol may be an effective antiemetic drug if used prophylactically in patients who receive general anesthesia for ophthalmic surgery.

Adolescent↗

PubMed1978

The attenuation of a specific cue-to-consequence association by antiemetic agents.

Previous research has been shown that rats develop a conditioned taste aversion after a single pairing of a distinct taste and subsequent toxicosis. The experiments reported here test the hypothesis that the expression of a taste aversion may reflect classically conditioned nausea mediated by activation of brainstem emetic centers by taste stimuli. Rats were allowed to drink a saccharin solution (1 g/l) and 10 min later were intubated with LiCl (180 mg/kg) to produce nausea. When control rats were posttested for saccharin preference they consumed less than 50% of their pretest intake. Experimental rats were injected with one of four pharmacologically distinct antiemetic drugs 30 min prior to their posttest with saccharin. Each drug significantly attenuated the aversion to saccharin at one dose level. The antiemetic drugs we used were scopolamine HBr, cyclizine, prochlorperazine dimaleate, and trimethobenzamide. These drugs had no effect on the conditioned fear of a noise that signaled foot shock or on a natural aversion to a bitter fluid (quinine monohydrochloride, 100 mg/l). Our data suggest that pharmacological suppression of the neural mechanisms of emesis selectively disrupts conditioned taste aversions, and that moderate dose levels are critical for obtaining this effect.

Animals↗

PubMed1979

Delata-9-tetrahydrocannabinol as an antiemetic in cancer patients receiving high-dose methotrexate. A prospective, randomized evaluation.

Fifteen patients with osteogenic sarcoma receiving high-dose methotrexate chemotherapy were studied in a randomized, double-blind, placebo-controlled trial of oral and smoked delta-9-tetrahydrocannabinol (THC) as an antiemetic. Each patient served as his or her own control. Fourteen of 15 patients had a reduction in nausea and vomiting on THC as compared to placebo. Delta-9-tetrahydrocannabinol was significantly more effective than placebo in reducing the number of vomiting and retching episodes, degree of nausea, duration of nausea, and volume of emesis (P less than 0.001). There was a 72% incidence of nausea and vomiting on placebo. When plasma THC concentrations measured less than 5.0 ng/mL, 5.0 to 10.0 ng/mL, and greater than 10.0 ng/mL, the incidences of nausea and vomiting were 44%, 21%, and 6%, respectively. Delta-9-tetrahydrocannabinol appears to have significant antiemetic properties when compared with placebo in patients receiving high-dose methotrexate.

Adolescent↗

PubMed1979

Delta-9-tetrahydrocannabinol as an antiemetic for patients receiving cancer chemotherapy. A comparison with prochlorperazine and a placebo.

The antiemetic activity and side-effects of delta-9-tetrahydrocannabinol (THC) were evaluated in 116 patients (median age 61 years) receiving combined 5-fluorouracil and semustine (methyl CCNU) therapy for gastrointestinal carcinoma. In a double-blind study, patients were randomized to receive THC, 15 mg orally three times a day, prochlorperazine, 10 mg orally three times a day, or placebo. The THC had superior antiemetic activity in comparison to placebo, but it showed no advantage over prochlorperazine. Central nervous system side-effects, however, were significantly more frequent and more severe with THC. With the dosage and schedule we used, and in our patient population of largely elderly adults, THC therapy resulted in an overall more unpleasant treatment experience than that noted with prochlorperazine or placebo. Although THC may have a role in preventing nausea and vomiting associated with cancer chemotherapy, this role must be more clearly defined before THC can be recommended for general use.

Adult↗

PubMed1976

The antiemetic effect of dixyrazine in postoperative patients-- a double-blind study.

A double-blind controlled study based on 197 women undergoing legal abortion (part I) or gynaecological surgery (part II) was employed to estimate the antiemetic effect of dixyrazine. Dixyrazine or part I) or intramuscularly at the end of anaesthesia (part II) and repeated when necessary. The follow-up period lasted 12 and 18 hours, respectively. Overall, a marked antiemetic response in the dixyrazine groups was observed when compared with the placebo treated groups in both part I and II (p less than 0.001). Dixyrazine proved to be superior to placebo especially in patients who were not prone to nausea or who received no major postoperative analgesics (p less than 0.001).

Abortion, Induced↗

PubMed1979

Antiemetic effect of intravenous diazepam in patients receiving cis-diamminedichloroplatinum II: a pilot study.

A pilot study suggesting the usefulness of intravenous diazepam as an antiemetic for adult patients receiving cis-diamminedichloroplatinum is presented. Observations included 24 patients and 34 courses of therapy. Patients received diazepam and prochlorperazine, and the incidence of vomiting and subjective evaluation of nausea were compared to previous courses of therapy with prochlorperazine alone. A positive response was observed in 87% of the patients. Use of other antiemetics is briefly reviewed.

Adolescent↗

PubMed1976

Antinauseant and antiemetic properties of bismuth subsalicylate in dogs and humans.

Laboratory and clinical investigations were carried out to determine the effectiveness of bismuth subsalicylate in allaying nausea by preventing the physical symptom of emesis. In normal conscious dogs, a bismuth subsalicylate formulation caused a dose-related reduction in the incidence of vomiting in response to an emetic dose of ipecac syrup. In normal human subjects, a bismuth subsalicylate suspension, unlike the placebo formulation, successfully subdued nausea and vomiting in 66.7 and 80% of the subjects, respectively, in response to ipecac syrup. Both findings demonstrate that bismuth subsalicylate can provide antiemetic action and that the decreases in the occurrence of emesis in humans and dogs parallels the decrease in nausea found in humans and the nausea suspected to occur prior to emesis in dogs.

Adult↗

PubMed1979

Superiority of nabilone over prochlorperazine as an antiemetic in patients receiving cancer chemotherapy.

Two double-blind, crossover trials comparing the antiemetic effectiveness of nabilone, a new synthetic cannabinoid, with that of prochlorperazine were conducted in patients with severe nausea and vomiting associated with anticancer chemotherapy. Of 113 patients evaluated, 90 (80 per cent) responded to nabilone therapy, whereas only 36 (32 per cent) responded to prochlorperazine (P less than 0.001). Complete relief of symptoms was infrequent, occurring only in nine patients (8 per cent) given nabilone. When both drugs were compared, both nausea (P less than 0.01) and vomiting episodes (P less than 0.001) were significantly lower in patients given nabilone. Moreover, patients clearly favored nabilone for continued use (P less than 0.001). Predominant side effects noted by patients were similar for both agents and included somnolence, dry mouth and dizziness but were about twice as frequent and more often severe in patients receiving nabilone. In addition, four patients (3 per cent) taking nabilone had side effects (hallucinations in three, hypotension in one) that required medical attention. Euphoria associated with nabilone was infrequent (16 per cent) and mild.

Adolescent↗

PubMed1978

The action of commonly used antiemetics on the lower oesophageal sphincter.

The effects of five antiemetic drugs on the lower oesophageal sphincter (LOS) were studied in five groups, each comprising eight healthy volunteers. Cyclizine, prochlorperazine and metoclopramide have a desirable functional effect on LOS, while promethazine and droperidol were associated with evidence of increased gastro-oesophageal reflux.

Adult↗

PubMed1978

A controlled trial of antiemetics in abortion by PGF2alpha and laminaria.

Women undergoing abortion by intraamniotic prostaglandin F2alpha were randomized to receive either prochlorperazine edisylate 10mg, hydroxyzine hydrochloride 100mg, or a placebo every four hours by intramuscular injection in a double-blind fashion. Vomiting was significantly more frequent in the placebo-treated group [0.2 +/- 1.5 SD episodes per patient, n=21] than in the groups treated with prochlorperazine [1.2 +/- 0.5 episodes per patient, n=21] or hydroxyzine [0.3 +/- 0.8 episodes per patient, n=19]. The mean number of merperidine injections in the antiemetic-treated groups was lower than in the control group, but this effect was not statistically significant. There was no significant difference between the treated and the control groups in the interval from prostaglandin treatment to abortion.

Abortion, Induced↗

PubMed1979

[R 33812 (domperidon) i.v. and orally as antiemetic adjuvans for short anaesthetics induced with etomidate. A comparative study (author's transl)].

R 33812 is being studied as an antiemetic adjuvant to anaesthesia for minor gynecological surgery. 150 patients received 10 mg Diazepam orally as a premedication and of these 3 groups of 50 received R 33812 in doses of 4 mg or 8 mg i.v. before anaesthesia or 10 mg orally together with premedication. Between series I and II a dose-related trend p = 0,065 was observed. No side effects were reported. The pharmacological interdependence of this combination is discussed as well as the consequences for general practice especially for the improved form of oral medication with R 33812.

Adjuvants, Anesthesia↗

PubMed1977

Gastrointestinal prokinetic and antiemetic effects of a new substituted pyrimidinO 6553 (2-methylamino-4-N-methylpiperazino-5-thiomethyl-6-chloropyrimidine hydrochloride).

2-Methylamino-4-N-methylpiperazino-5-methylthio-6-chloropyrimidine hydrochloride (O 6553) is a new molecule showing an original pharmacological profile in the laboratory tests. It possesses at the same time potent gastro-intestinal prokinetic and central antiemetic properties, demonstrated on the one hand by the gastro-duodenal transit of barium meal in rats, and on the other hand by apomorphine-induced vomiting in dogs. The drug also has interesting anxiolytic and antiserotonin properties and, at doses which change gastro-intestinal behaviour, it is devoid of any untoward side effect. The acute and subacute toxicities of O 6553 show that the drug has a very good safety margin.

Animals↗

PubMed1977

Preliminary report of domperidone (R 33182), a new antiemetic compound. A pilot study.

The effect of domperidone (R 33 812), a new antiemetic, was studied in 27 patients presenting with postoperative vomiting and staying for at least six hours in a recovery room. All patients received 4 mg domperidone intravenously because of the vomiting. Nineteen patients were fully protected during the subsequent 6 hours observation period, 8 patients required a second 4 mg-dose: only one of these 8 patients was not protected at all. No side-effects were observed.

Adult↗