Ondansetron: 高選擇性5HT3接受體拮抗劑，為作用相當強的鎮吐和抗眩暈的藥物。適應症:細胞毒性化學療法及放射線療法所致之噁心及嘔吐，以及手術引起之噁心嘔吐。用法用量: 1. 高嘔吐性的化學療法：在化學治療之前靜脈滴注或緩慢注射8mg，之後在24小時內靜脈滴注，每小時1mg，或者2次追加劑量，間隔4小時或以上，然後每8小時口服8mg，連續5天。2. 低嘔吐性的化學療法：在化學治療之前，緩慢靜注或滴注8mg或在前1～2小時口服8mg，然後每8小時口服8mg，連續5天。3. 放射性治療誘發的噁心或嘔吐：在放射性治療之前1～2小時每8 小時口服8mg。
Absorption: Passively and completely absorbed from GI tract. Bioavailability is 48% to 75% and is slightly enhanced with food. C max for males is 24.1 to 37 ng/mL (8 mg oral dose). C max for females is 42.7 to 52.4 ng/mL (8 mg oral dose). C max for injection is 102 to 170 ng/mL. T max for males is 2 to 4.1 h (8 mg dose). T max for females is 1.7 to 4.9 h (8 mg dose).Distribution: Plasma protein binding is 70% to 76%. Metabolism: Extensively metabolized in the liver by hydroxylation, followed by glucuronide or sulfate conjugation; CYP1A2, CYP2D6, CYP3A4 are the main hepatic enzymes. Elimination: Approximately 5% is eliminated as parent compound in urine. The t ½ for males is 2.1 to 4.5 h (8 mg oral dose). The t ½ for females is 1.9 to 6.2 h (8 mg dose). The t ½ for injection is 3.5 to 5.5 h. Plasma Cl is 0.262 to 0.381 L/h/kg.
exp. Fast dissolving oral DDS for Ondansetron
Zophren (Zofran®) is a tablet which contains ondansetron as bioactive principle. Zophren is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Zophren is a highly specific and selective serotonin 5- HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. A derivative product, Sofran ODT® (for Zofran Orally Disintegrating Tablets) has been developed. When placed on top of the tongue, it dissolves in seconds, and can then be swallowed with saliva. The summary of product characteristics of Zofran ODT® reports that in children less than 6 years of age, due to the risk of aspiration with the tablet, dissolution with water or syrup prior to swallowing should be recommended. Therefore, Zofran® and Zofran ODT® are not completely suitable in case of dysphagia and risk aspiration.
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