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)

Twelve dogs were administered oral threshold doses of copper sulfate every week. In 66 out of 85 cases, dogs vomited. One dog vomited in 1st and 2nd tests, but did not respond in the other 6 tests. Excluding this one, the reproducibility was 82%. The following method is thus proposed for application in evaluating an antiemetic for oral copper sulfate. Small dogs, weighing 7-14 kg, are to be kept in a constant condition during the quarantine and tests and given the emetic once a week. The threshold dose is determined in three dose levels; 20, 40, 80 mg/head. The dogs with a threshold of more than 80 mg or latency of less than 5 min or of more than 45 min are to be excluded. Inhibition of emesis or a considerable prolongation of latency is the sign of an antiemetic action. A positive action of an antiemetic must be followed by another test with the threshold dose of copper sulfate alone. If the dog does not respond to the threshold dose after 2 administrations, the case must be excluded. To evaluate an antiemetic at least 5 cases are needed. Inhibition of more than 50% appears to be the positive response.
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PMID:[Reproducibility of copper sulfate emesis by oral administration in dogs]. 116 92

The practicability of an intramuscular dose schedule of 10 mug of 15(S) 15 methyl prostaglandin E2 methyl ester [15(S) Me PGE2] administered every 4 hours was evaluated in 42 subjects from 7 to 20 menstrual weeks' gestation. Half of the subjects served as controls (Group I) and half of the subjects (Group II) were treated with a medication regimen of prochlorperazine, acetylsalicylic acid, diphenoxylate hydrochloride, and atropine sulfate to evaluate the regimen's effects. Although the 15(S) Me PGE2 dose schedule appeared to be effective (74 per cent aborted in 24 hours and 95 per cent aborted within 48 hours in a mean time of 18.9 hours), Group I (control) subjects frequently had side effects: 62 per cent had emesis, 86 per cent had diarrhea, 76 per cent had shivering, and 76 per cent had fever (greater than 100 degrees F.). Fewer Group II (medicated) subjects had side effects: 43 per cent had emesis, 19 per cent had diarrhea, 52 per cent had shivering, and 43 per cent had fever. The medication regimen did not appear to interfere with the abortifacient or oxytocic effects of the 15(S) Me PGE2 dose schedule, since Group I and Group II subjects had similar cumulative abortion rates, mean abortion times, and uterine activity. Although this 15(S) Me PGE2 dose schedule is effective in first-trimester patients, it is probably less satisfactory than the conventional method of vacuum aspiration. While intramuscularly administered 15(S) Me PGE2 with medications to attenuate side effects may be practicable for inducing midtrimester abortion, especially between 12 and 16 weeks' gestation, large controlled comparative studies of the intramuscular 15(S) Me PGE2 method and other experimental and conventional methods will be necessary to determine the most satisfactory method of performing midtrimester abortions.
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PMID:The efficacy and safety of intramuscularly administered 15(S) 15 methyl prostaglandin E2 methyl ester for induction of artificial abortion. 119 Feb 75

Under control (intact and laparotomized) conditions, arterial pressure of urethan-anesthetized ferrets rose significantly in response to intragastric copper sulfate (CuSO4; 10 ml of 5 mg/ml). CuSO4 was emetic 75-90% of the time, and a cardiovascular response always immediately preceded and accompanied emetic responses. The cardiovascular response was significantly reduced or abolished by hexamethonium (0.35 mg/kg) pretreatment combined with atropine methyl bromide (1 mg/kg). Addition of the alpha 2-receptor antagonist 2,3-dichloro-alpha-methylbenzylamine HCl (DCMB, 10 mg/kg) and the beta-receptor antagonist propranolol (3 mg/kg) to the hexamethonium and atropine combination prevented its reduction of the cardiovascular response. Given individually, these agents did not alter cardiovascular response, nor did yohimbine (0.30 mg/kg), RS(+/-)-zacopride (0.30 mg/kg), or granisetron (0.50 mg/kg). Only RS(+/-)-zacopride significantly reduced incidence of emesis. Atropine methyl bromide alone, with hexamethonium, or with hexamethonium, propranolol, and DCMB significantly delayed the first emetic episode. Conversely, bilateral abdominal vagotomy significantly reduced the number of vomiting animals without affecting cardiovascular response. These results suggest that the neural pathways mediating the two events are not identical. In another series of experiments, a significantly greater proportion of animals vomited in response to intragastric CuSO4 than to intraduodenal CuSO4, suggesting that the primary site of CuSO4 action in the ferret is the stomach.
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PMID:Surgical and pharmacological dissociation of cardiovascular and emetic responses to intragastric CuSO4. 135 43

Tropiestron is a potent and selective antagonist of 5-hydroxytryptamine receptors. Tropisetron was developed for the indication of cancer chemotherapy-induced emesis. The pharmacokinetic and metabolic dispositions of tropisetron were studied in 12 healthy male volunteers receiving a single oral dose of 62 or 312 mumol (20 or 100 mg) of [14C]tropisetron. Serial plasma samples and complete urine and feces were collected for 120 hr postdose. Whereas the absorption of oral doses of 62-312 mumol tropisetron was rapid and complete, bioavailability was estimated to be only 66% for the 312 mumol dose and 52% for the 62 mumol dose, apparently because of saturable first-pass metabolism. Maximal concentrations of tropisetron averaged 87 and 608 nM after doses of 62 and 312 mumol, respectively, and the parent drug accounted for 21 and 36% of the radioactivity in AUC0-24 hr pools. Approximately 90% of the drug was metabolized before excretion, and approximately 70% of the dose was recovered in the urine. Following both the 62 and 312 mumol doses, the terminal half-life of tropisetron averaged 6-7 hr and that of total radioactivity was 10-11 hr. Tropisetron and its metabolites in plasma and urine were separated by gradient elution reversed-phase HPLC. Structures of eight metabolites were assigned on the bases of NMR and MS data. Tropisetron was metabolized by oxidative hydroxylation of the indole ring at positions 5, 6, and 7. The hydroxylated derivatives are further conjugated with glucuronic acid and sulfate. N-Oxygenation and oxidative N-demethylation at the tropinyl nitrogen also occur in trace amounts.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacokinetics and metabolism of the 5-hydroxytryptamine antagonist tropisetron after single oral doses in humans. 135 42

The effect of acute ethanol administration into the cerebral ventricles on the unanesthetized cat upon emesis produced by norepinephrine and clonidine injected similarly as well as upon emesis evoked by copper sulfate given orally was compared and investigated. Ethanol inhibited the norepinephrine- and clonidine-induced emesis. The inhibitory effect of ethanol occurred after a transient and inconsistent emetic action of the drug. Norepinephrine-induced emesis was about 12 times more sensitive than clonidine-induced emesis to the inhibitory effect of ethanol. In addition, norepinephrine-, but not clonidine-induced emesis was abolished after ablation of the area postrema. On the contrary, intracerebroventricular ethanol had virtually no effect on emesis caused by intragastric copper sulfate. The inhibitory effect of ethanol is ascribed to an action on alpha-2 adrenoceptors within the area postrema and on imidazoline-preferring sites and/or muscarinic cholinoceptors outside the area postrema, but not on the emetic region of the brainstem reticular formation. It follows then that ethanol can differentiate alpha-2 adrenoceptors from imidazoline-preferring sites and/or muscarinic cholinoceptors in the brain of the cat.
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PMID:Differential inhibition by ethanol of norepinephrine- and clonidine-induced emesis in cats. 141 63

Using kaolin intake as a behavioral index of emesis in rats, we examined the relationship between susceptibility to motion sickness and to emesis induced by apomorphine or copper sulfate. Rats showed a wide variation in susceptibility to motion sickness. Significant positive correlations were found between susceptibility to motion sickness and to emesis induced by intraperitoneal administration of apomorphine and by oral administration of copper sulfate. Motion, apomorphine and copper sulfate induce emesis through different receptors, so these findings suggest that the sensitivity of a common locus of emesis, presumably the emetic center in the brain stem, is one determinant of individual differences in susceptibility to motion sickness.
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PMID:Vestibular, central and gastral triggering of emesis. A study on individual susceptibility in rats. 148 62

The antiemetic effects of a novel serotonin3 receptor antagonist, DAT-582 [(6R)-(-)-N-[1-methyl-4-(3-methylbenzyl)hexahydro-1H-1,4- diazepin-6-yl]-1H-indazole-3-carboxamide dihydrochloride] were compared with those of the existing serotonin3 receptor antagonists, ondansetron and granisetron, in experimental animals. In ferrets, DAT-582 (0.003-0.1 mg/kg i.v. twice) dose-relatedly prolonged the latency to the first emetic episode and decreased the number of emetic episodes induced by cisplatin (10 mg/kg i.v.). DAT-582 was more potent than ondansetron or granisetron in inhibiting the emesis. The emesis induced by cyclophosphamide (150 mg/kg i.v.), doxorubicin (15 mg/kg i.v.) or combination of cisplatin (3.3 mg/kg i.v.), cyclophosphamide (50 mg/kg i.v.) and doxorubicin (5 mg/kg i.v.) was also inhibited by DAT-582 (0.1 mg/kg i.v., twice). When administered 2 hr before cisplatin in ferrets, DAT-582 decreased markedly the number of emetic episodes induced by cisplatin at 0.1 mg/kg i.v., whereas ondansetron and granisetron were without effect even at 0.3 mg/kg i.v. DAT-582 (0.1 mg/kg i.v.), when administered in the ferrets which were vomiting after cisplatin, immediately and almost completely blocked the subsequent emesis. Furthermore, DAT-582 (0.1 mg/kg i.v.) completely inhibited the cisplatin (3 mg/kg i.v.)-induced emesis for 24 hr after cisplatin in three of five dogs. In addition, DAT-582, at 0.3 and 1 mg/kg, p.o., inhibited the cisplatin-induced emesis in dogs. However, DAT-582, even at 3 mg/kg s.c., did not inhibit the apomorphine (0.3 mg/kg,, s.c.)-induced emesis in dogs, or the nicotine-, copper sulfate- or motion stimulus-induced emesis in the house musk shrew, Suncus Murinus.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:DAT-582, a novel serotonin3 receptor antagonist, is a potent and long-lasting antiemetic agent in the ferret and dog. 153 32

Two new classes of potent 5-HT3 agents have been developed and examined as inhibitors of cytotoxic drug induced emesis in the ferret and dog. The absolute configuration of the most active molecules 10 and 18 have been determined by X-ray crystallography. These two compounds are more potent than known 5-HT3 receptor antagonists both in vivo and in vitro in blocking 5-HT3 receptor activation and preventing chemotherapeutic induced emesis. Compared with 5-HT3 antagonists, such as GR 38032F, zacopride, BRL 43694, and ICS 205-930, compound 10 was more potent in (1) inhibiting binding to 5-HT3 receptor binding sites in rat cortex (Ki = 0.17 nM), (2) blocking the von Bezold-Jarisch effect in the rat (lowest effective dose, 1 microgram/kg iv), and (3) inhibiting 5-HT-induced contraction of guinea pig ileum (lowest effective concentration, 10(-9) M). This novel agent was as effective given po as when given iv in reducing cisplatin-induced emetic episodes in the ferret (ED50 = 4 micrograms/kg iv or po). A 1 mg/kg po dose of 10 virtually abolished cisplatin-induced emesis for 10 h in the ferret. However, it was inactive against apomorphine or copper sulfate-induced vomiting. These data, coupled with receptor binding studies of ligands for D2-dopamine, a1, a2, 5-HT1, 5-HT2, and muscarinic receptors demonstrate that 10 is a highly selective 5-HT3 receptor antagonist with remarkable potency in vivo.
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PMID:Development of high-affinity 5-HT3 receptor antagonists. 2. Two novel tricyclic benzamides. 154 79

An overdose of up to 850 levothyroxine sodium tablets (0.2 mg) in a healthy 6-year-old 16.8-kg dog induced an episode of vomiting and hippus within 9 hours of ingestion. The dog was treated with activated charcoal and saline (magnesium sulfate) cathartic. Initially the serum concentration of thyroxine (T4) 4,900.9 nmol/L. On the second day, serum concentration of triiodothyronine (T3) was 5.3 nmol/L. Serum T4 concentration decreased slowly and was not determined to be normal until day 36. Serum T3 concentration was found to be normal on day 6. Serum alanine transaminase activity peaked on day 6 at 345 U/L. Significant abnormalities were not found during the following 36 days. Clinical signs of thyroid hormone toxicosis in dogs and cats include hyperactivity, lethargy, tachycardia, tachypnea, dyspnea, abnormal pupillary light reflexes, vomiting, and diarrhea. High overdoses of levothyroxine sodium in dogs should be managed by initial decontamination and administration of activated charcoal with a cathartic followed by supportive care.
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PMID:Acute overdose of levothyroxine in a dog. 161 89

Many physicians, Certified Registered Nurse Anesthetists (CRNAs), and registered nurses have the clinical impression that either morphine sulfate or meperidine hydrochloride is a better drug to control postoperative pain. In this study, we evaluated pain relief and side effects for these two drugs to assess their potential differences. CRNAs conducted a structured interview of 500 female patients 24 hours after major gynecologic, urologic, or breast surgery. Patients' responses on 4-point scales of none, mild, moderate, and severe were collected for pain intensity, degree of nausea, severity of vomiting and itchiness, and degree of sedation experienced since the operation. There were 91 patients who received morphine patient-controlled analgesia (PCA) and 409 patients administered meperidine PCA. No statistically significant differences for pain intensity, degree of nausea, severity and incidence of vomiting, or degree of sedation were found. However, a significant difference was found in the incidence rates of mild itchiness, which occurred more frequently in the morphine PCA group (P less than .001). Patients vomited more often after vaginal hysterectomy than patients having laparotomy, major oncology, or tuboplasty surgeries (P less than .05), and vaginal repair patients reported more vomiting than patients having major oncology or tuboplasty surgeries. Clinical impressions that either morphine or meperidine should be the preferred treatment for patients following gynecologic operations was not found by a 24-hour review of 500 patients for pain relief and side effects. Although mild itchiness occurred more frequently in the morphine PCA group, treatment was rarely necessary.
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PMID:Side effects of morphine patient-controlled analgesia and meperidine patient-controlled analgesia: a follow-up of 500 patients. 163 56


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