University of Siena, Departments of Mental Health and Molecular Medicine, Viale Bracci 1, Siena 53100, Italy.
Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29.
Asenapine is a sublingually administered second-generation antipsychotic with proven efficacy for the treatment of moderate to severe manic episodes associated with bipolar I disorder in adults. Its relatively favorable weight and metabolic profile, as well as the lack of appreciable activity at muscarinic cholinergic receptors and the sublingual administration are of clinical interest.
This paper comprises a review and commentary regarding the use of sublingual asenapine in the treatment of acute manic and mixed episodes of bipolar disorder. Basic principles in dosing, switching, management of side effects and co-administration with other medications are provided.
Asenapine displays quick and reliable effects on manic symptoms, very low risk of depressive switches, efficacy on depressive symptoms during manic and mixed episodes, usually good tolerability and continued longer-term efficacy on residual and subthreshold symptoms. The fast-dissolving sublingual route of administration may favor those who have difficulties in swallowing medications. Also, the sublingual administration reduces the risk of overdose when more than the prescribed tablets are swallowed. The relatively low metabolic risk and the lack of anticholinergic side effects contribute to making this medication a useful tool for the treatment of patients with bipolar disorder.
阿塞那平是一种舌下给药的第二代抗精神病药，已被证明可有效治疗成人双相情感障碍中与中度至重度躁狂发作相关的疾病。其相对有利的体重和代谢特征，以及对毒蕈碱胆碱能受体几乎没有明显活性和舌下给药的特点具有临床意义。
本文综述并评论了舌下给予阿塞那平治疗双相情感障碍急性躁狂和混合发作的应用。提供了剂量、转换、不良反应管理以及与其他药物联合使用的基本原则。
阿塞那平对躁狂症状有快速可靠的疗效，抑郁转换风险非常低，在躁狂和混合发作期间对抑郁症状有效，通常具有良好的耐受性，并对残留和亚阈值症状持续具有长期疗效。快速溶解的舌下给药途径可能对那些吞咽药物有困难的患者有益。此外，当超过规定剂量的片剂被吞下时，舌下给药可降低过量的风险。相对较低的代谢风险和缺乏抗胆碱能副作用有助于使这种药物成为治疗双相情感障碍患者的有用工具。
