Quốc gia: Úc
Ngôn ngữ: Tiếng Anh
Nguồn: Department of Health (Therapeutic Goods Administration)
Oxpentifylline
Sanofi-Aventis Australia Pty Ltd
Medicine Registered
PRODUCT INFORMATION TRENTAL ® 400 NAME OF THE DRUG NON-PROPRIETARY NAME Oxpentifylline Oxpentifylline and Pentoxifylline are interchangeable and refer to the same molecule. CHEMICAL STRUCTURE C 13 H 18 N 4 O 3 278.3102 CAS NUMBER 6493-05-6 DESCRIPTION A trisubstituted xanthine derivative designated chemically as 1-(5-oxohexyl)-3, 7-dimethylxanthine, IUPAC name: 3,7-dimethyl-1-(5-oxohexyl)-3.7-dihydro-1H-purine-2,6-dione. Oxpentifylline is soluble in water and ethanol, and sparingly soluble in toluene. Trental 400 controlled-release tablets also contain the following excipients: hydroxyethylcellulose, povidone, talc-purified, magnesium stearate, hypromellose, titanium dioxide, erythrosine, and macrogol 8000. PHARMACOLOGY SITE AND MODE OF ACTION It is thought that oxpentifylline and its metabolites improve the flow properties of blood by decreasing its viscosity. In patients with chronic peripheral arterial disease, this increases blood flow to the affected microcirculation and enhances tissue oxygenation. Some of the mechanisms by which this is thought to occur include dose-related haemorrheological effects, such as decreased blood viscosity, improved erythrocyte flexibility, decreased plasma fibrinogen and enhanced platelet deaggregation. However, the precise mode of action of oxpentifylline and the sequence of events leading to clinical improvement are still to be clearly defined. PHARMACOKINETICS After oral administration in aqueous solution oxpentifylline is almost completely absorbed. It undergoes a first-pass effect and the various metabolites appear in plasma very soon after dosing. Peak plasma levels of the parent compound and its metabolites are reached within 1 hour. The major metabolites are Metabolite I (1-[5-hydroxy-hexyl]-3,7-dimethylxanthine) and Metabolite V (1- [3-carboxypropyl]-3,7-dimethylxanthine), and plasma levels of these metabolites are 5 and 8 times greater, respectively, Đọc toàn bộ tài liệu