We synthesized a novel phosphodiesterase type 4 (PDE4) inhibitor, YM976, that is structurally different from the other PDE4 inhibitors like rolipram. In the present study, the pharmacological profile of YM976 was investigated. YM976 exhibited a strong and competitive inhibition against PDE4 purified from human peripheral leukocytes with an IC(50) of 2.2 nM. IC(50) values of rolipram and RP73401...

BACKGROUND AND OBJECTIVES The aim of this study was to evaluate the incidence and severity of chemotherapy-induced nausea and vomiting (CINV) in oncohematology in routine clinical practice, its impact on quality of life, and caregivers' perception of the extent of the problem. DESIGN AND METHODS This was a multicenter, prospective, observational follow-up study including: (i) acute myeloid le...

V OMITING is a complicated act which involves the coordinated activities of many motor systems of the body including both the somatic and autonomic nervous outflows. The orderly sequential action of the different muscle groups used in emesis has been clearly demonstrated by the now classical work of Cannon (I). Equally complex is the question of the sensory pathways of vomiting. The roles of th...

BACKGROUND A combination of aprepitant, a 5-HT3 receptor antagonist (r.a.), and dexamethasone is recommended for the prophylaxis of cisplatin-induced nausea and vomiting in the acute phase, and aprepitant + dexamethasone (A + D) in the delayed phase. The aim of this study was to verify if A + D is superior to metoclopramide plus dexamethasone (M + D) in preventing delayed emesis in cancer patie...

PURPOSE 5-Hydroxytryptamine-3 receptor antagonists (5-HT(3) antagonists) are effective for preventing acute chemotherapy-induced emesis but the benefits of continuing administration of these agents beyond 24 hours after chemotherapy (delayed emesis) remain unclear. The purpose of this study was to provide estimates of clinical efficacy and drug acquisition cost associated with administering 5-H...

Propofol anaesthesia may reduce postoperative emesis. The purpose of this study was to compare the incidence of emesis after propofol anaesthesia with and without nitrous oxide, compared with thiopentone and halothane anaesthesia, in hospital and up to 24 hr postoperatively, in outpatient paediatric patients after strabismus surgery. Seventy-five ASA class I or II, unpremedicated patients, aged...

BACKGROUND Staphylococcal enterotoxins (SEs) are the most common cause of foodborne diseases and toxic shock throughout the world. However, no vaccine that prevents emesis induced by SEs has been described. METHODS A nontoxic mutant of SEA, SEAD227A, was constructed by site-directed mutagenesis and was purified by means of the Escherichia coli expression system. House musk shrews, a small eme...

Cancer chemotherapy is associated with numerous toxicities such as nausea and vomiting (emesis). The frequency, onset, and duration of emesis depend largely on the emetogenic potential of specific agents. An exact mechanism for chemotherapy-induced emesis (CIE) is not known but is thought to occur through several noxious actions and numerous neuronal pathways. The three types of CIE are acute, ...

OBJECTIVE A clinical study of ramosetron was carried out to evaluate its efficacy in preventing both acute and delayed emesis in cisplatin-based chemotherapy by using a double-blind method with granisetron as the comparative drug. METHODS Cisplatin at a dose of > or =70 mg/m(2) was administered as a single intravenous (i.v.) infusion over 4 h. Patients were randomly assigned to receive either...

Nausea and vomiting are the most distressing and common side effects of cancer chemotherapy which often result in patient noncompliance. In the present study, standardized methanolic and n-butanolic fractions of Bacopa monnieri were evaluated against cisplatin-induced emesis in the pigeon in relation to their activity on central and intestinal neurotransmitters levels. Cisplatin (7.0 mg/kg, i. ...