在偏头痛发作期间和之间对单剂量zavegepant的比较生物可用性:一期,随机化,开放标签,固定的序列,两期研究
Richard J Bertz1, Julie L Collins2, Jennifer Madonia1
1Biohaven Pharmaceuticals Inc., New Haven, Connecticut, USA.
Headache
|November 7, 2024
概括
在偏头痛发作和非偏头痛期间,Zavegepant鼻喷剂的吸收率相似,特别是在10mg剂量时. 这种偏头痛治疗是安全有效的,药物度和症状缓解之间没有明确的联系.
科学领域:
- 药理学和治疗学 药理学和治疗学
- 神经学 神经学
- 临床试验 临床试验
背景情况:
- 偏头痛发作涉及到可能影响药物吸收的生理变化.
- 了解这些变化对于优化偏头痛治疗药理动力学至关重要.
研究的目的:
- 为了比较zavegepant鼻喷雾在偏头痛期间与非偏头痛期间的吸收.
- 评估zavegepant在偏头痛发作期间的安全性和有效性.
- 探索zavegepant度和治疗反应之间的关系.
主要方法:
- 第1期,随机化,开放标签,比较生物利用性研究.
- 参与者在偏头痛和非偏头痛期间都接受了单次鼻入剂量zavegepant (10mg或20mg).
- 测量了血zavegepant度,安全性和疗效的结果.
主要成果:
- 在偏头痛和非偏头痛期间,特别是10mg剂量时,扎维格潘特暴露 (Cmax,AUC0-inf) 是可比的.
- 将剂量从10毫克翻倍到20毫克,导致暴露的增加比例小于剂量.
- 达到最大度 (Tmax) 的中位时间为0.5小时,zavegepant耐受性良好,有效缓解偏头痛症状.
结论:
- 在偏头痛发作和非偏头痛期间,Zavegepant的吸收情况类似.
- 扎维杰潘特10mg和20mg鼻喷雾剂在急性偏头痛治疗中是安全有效的.
- 在zavegepant度和疗效结果之间没有明显的相关性.
相关概念视频
Bioequivalence: Overview
926
Pharmaceutical equivalents, by definition, are drug products with the same active ingredient in the same quantities, encapsulated in identical dosage forms, and intended for the same administration routes. These pharmaceutical equivalents are deemed bioequivalent if the bioavailability of the active entity in the drug preparations is similar. Moreover, pharmaceutical equivalents demonstrating bioequivalence are also regarded as therapeutically equivalent. This means that when used as directed,...
926
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists
175
5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
175
Bioavailability: Overview
2.7K
Bioavailability refers to the proportion of an unaltered drug that, after administration, enters the systemic circulation and can be distributed to the desired action site. Factors such as gastrointestinal (GI) absorption and liver biotransformation influence the bioavailability of a drug when it is administered orally. When a drug is administered intravenously, it enters the systemic circulation directly; by definition, its bioavailability is assumed to be 100%. The bioavailability of an...
2.7K
Drug Delivery: Enteral Route
384
The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
384
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
149
Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy. SP binds and activates...
149
Factors Influencing Drug Absorption: Presystemic Elimination
183
The pharmacokinetic journey of oral drugs begins with a crucial first pass through the hepatic portal system, called the first-pass effect. This first pass significantly impacts bioavailability — the proportion of a drug that enters systemic circulation and is available for therapeutic action. The primary route sees the drug absorbed by intestinal membranes and then shunted to the liver via the hepatic portal vein. Here, pre-systemic elimination occurs as drugs face metabolism or biliary...
183


