生物活性

• 描述Prochlorperazine (Dimaleate) is a D(2) antagonist. Prochlorperazine (1-2 mg/kg s.c./i.p.) produced an increase of the pain threshold in the mouse hot-plate test. Prochlorperazine also elicited a dose-dependent increase in ACh release from rat cerebral cortex. In the antinociceptive dose-range, prochlorperazine did not impair mouse performance evaluated by the rota-rod and hole-board tests. Thus, prochlorperazine exerted an antinociceptive effect mediated by a central cholinergic mechanism^[3]. Prochlorperazine is a phenothiazine-class antipsychotic drug and induces concentration-dependent loss in cell viability with EC50 value of 18.49 μM. Prochlorperazine in a concentration of 0.001 μM stimulated melanogenesis, while in concentrations 1.0 and 10.0 μM melanization process was inhibited. Furthermore, the drug in concentrations of 0.1, 1.0 and 10.0 μM caused changes in cellular antioxidant defense system, what indicated the induction of oxidative stress^[4]. Prochlorperazine is recommended for adults with breakthrough or refractory chemotherapy-induced nausea and vomiting (CINV). The most common AEs (adverse effects) reported with the pediatric use of prochlorperazine are EPS (extrapyramidal symptoms) and sedation. Fatalities, life-threatening, and persistent AEs have also been reported^[5]. IV hydromorphone is substantially less effective than IV prochlorperazine for the treatment of acute migraine in the ED (emergency department) and should not be used as first-line therapy^[6]. Buccally absorbed prochlorperazine (BAP) is an effective, non-invasive treatment for migraine headaches when compared to intravenous prochlorperazine (IVP)^[7].