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Antiemetic Agent (antiemetic + agent)

Distribution by Scientific Domains

Medical Sciences	75%

Selected Abstracts

The neurokinin-1 antagonist activity of maropitant, an antiemetic drug for dogs, in a gerbil model

JOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 4 2007
V. DE LA PUENTE-REDONDO
Maropitant is a novel synthetic nonpeptide neurokinin type 1 (NK1) selective receptor antagonist, recently developed for use in the dog as an antiemetic. The in vivo functional activity of maropitant was investigated in the gerbil foot-tapping model, to determine the ability of maropitant to penetrate the central nervous system and inhibit foot-tapping induced by the selective NK1 agonist GR73632. In comparison with CP-122,721, a previously characterized NK1 receptor antagonist, maropitant (1 mg/kg by s.c. injection) was found to inhibit foot-tapping for significantly longer (P < 0.01). Inhibition of foot-tapping by maropitant was 100% at 2 h and approximately 50% at 8 h postdosing. The mean brain:plasma concentration ratio at 8 h post-treatment was 3.59. These data demonstrate the central functional action of maropitant as a selective and potent NK1 receptor antagonist and help to support and explain its clinical potential as a broad-spectrum antiemetic agent. [source]

Granisetron, an antiemetic drug, and its cobalt complex

ACTA CRYSTALLOGRAPHICA SECTION C, Issue 2 2010
Krishnan Ravikumar
The crystal structures of granisetron [systematic name: 1-methyl- N -(9-methyl-9-azabicyclo[3.3.1]nonan-7-yl)indazole-3-carboxamide], C18H24N4O, (I), an antinauseant and antiemetic agent, and its CoII complex, diaqua[1-methyl- N -(9-methyl-9-azoniabicyclo[3.3.1]nonan-7-yl)indazole-3-carboxamide]cobalt(II) tetrachloride dodecahydrate, [Co(C18H25N4O)2(H2O)2]Cl4·12H2O, (II), have been determined by X-ray diffraction. The granisetron molecule is in an extended conformation in both structures. Twisting of the central carboxamide group facilitates the CoII coordination in (II). The CoII atom is located on an inversion centre. The azabicyclononane ring adopts a chair,boat conformation in both structures. The molecules in (I) are linked into centrosymmetric dimers and form tetracyclic rings through C,H...O hydrogen-bonding interactions. The simultaneous presence of free chloride ions in conjunction with a number of hydration water molecules in (II) provides interesting hydrogen-bond patterns. This study can aid in the investigation of the properties of metal complexes with active pharmaceuticals in which the drug molecules play the role of a ligand. [source]

Ondansetron versus Promethazine to Treat Acute Undifferentiated Nausea in the Emergency Department: A Randomized, Double-blind, Noninferiority Trial

ACADEMIC EMERGENCY MEDICINE, Issue 3 2008
Darren Braude MD
Abstract Objectives:, The authors sought to compare ondansetron and promethazine among emergency department (ED) patients with undifferentiated nausea. The hypothesis was that ondansetron was not inferior to promethazine and that rates of adverse effects were similar. Methods:, This was a randomized double-blind noninferiority clinical trial conducted in an urban academic ED. A convenience sample of nonpregnant adults with at least 40 mm of self-reported nausea measured on a 100-mm visual analog scale (VAS) were enrolled. Patients who had already received more than 1 L of intravenous fluid or an antiemetic agent were excluded. Subjects were block-randomized in groups of 10 to either 4 mg of ondansetron or 25 mg of promethazine delivered intravenously. The primary outcome was change in nausea over 30 minutes. The authors used a 15-mm margin of noninferiority. Secondary endpoints included changes in anxiety, sedation, and other adverse effects. Analyses included t-tests, tests for proportions, and 95% confidence intervals (CIs). Results:, A total of 120 subjects completed the study, 60 in each arm. Baseline nausea, anxiety, and sedation scores were similar. Ondansetron and promethazine reduced nausea similarly (ondansetron ,34 mm, promethazine ,36 mm; difference ,2 mm; 95% CI = ,13 to 8 mm). The reduction in anxiety was similar (ondansetron ,13 mm, promethazine ,14 mm; difference ,1 mm; 95% CI = ,10 to 10 mm). Promethazine was associated with significantly more sedation than ondansetron (ondansetron 5 mm, promethazine 19 mm; difference 14 mm; 95% CI = 5 to 24 mm). There were no cases of akathisia in the ondansetron group and 2 cases in the promethazine group. Conclusions:, Promethazine and ondansetron have similar efficacy in reducing nausea among ED patients. Change in anxiety was similar, but promethazine was associated with greater sedation. [source]

Nausea and Vomiting Side Effects with Opioid Analgesics during Treatment of Chronic Pain: Mechanisms, Implications, and Management Options

PAIN MEDICINE, Issue 4 2009
Frank Porreca PhD
ABSTRACT Objectives., Gastrointestinal (GI) side effects such as nausea and vomiting are common following opioid analgesia and represent a significant cause of patient discomfort and treatment dissatisfaction. This review examines the mechanisms that produce these side effects, their impact on treatment outcomes in chronic pain patients, and counteractive strategies. Results., A number of mechanisms by which opioids produce nausea and vomiting have been identified. These involve both central and peripheral sites including the vomiting center, chemoreceptor trigger zones, cerebral cortex, and the vestibular apparatus of the brain, as well as the GI tract itself. Nausea and vomiting have a negative impact on treatment efficacy and successful patient management because they limit the effective analgesic dosage that can be achieved and are frequently reported as the reason for discontinuation of opioid pain medication or missed doses. While various strategies such as antiemetic agents or opioid switching can be employed to control these side effects, neither option is ideal because they are not always effective and incur additional costs and inconvenience. Opioid-sparing analgesic agents may provide a further alternative to avoid nausea and vomiting due to their reduced reliance on mu-opioid signalling pathways to induce analgesia. Conclusions., Nausea and vomiting side effects limit the analgesic efficiency of current opioid therapies. There is a clear need for the development of improved opioid-based analgesics that mitigate these intolerable effects. [source]