title: [Opioid effects - galenics make the difference].
abstract: The galenics of extended-release opioids is highly variable and often insufficently. The quality of retard formulations can roughly be evaluated by means of 3 parameters: 1. PTF-Value (peak-trough fluctuation) [PTF (%) = [Cmax - Cmin] ×100/Cav] which should be as small as possible in order to minimize the fluctuation of plasma levels e.g. Morphin ratiopharm®: 120 ± 35%; Oxygesic® 120 ± 38%; Jurnista® 61 ± 41%. 2. A maximized Tmax-value (viz. the time required to achieve Cmax) to induce a more gradual onset of opioid effects e.g. MST Continus®: 2,3 ± 1,1h; Palladon® retard: 4,8 ± 0,8h; Hydromorphon STADA®: 5,1 ± 1,4h and Jurnista®: 12-16h. 3. Half-Value-Duration (HVD) is defined as the total time period in which the plasma concentration of opioids is above one-half of Cmax. Therefore, HVD is a parameter for the extent of controlled release. A too short HVD can induce end-of-dose-failure. HVD of most opioid formulations (b.i.d.) is only 6h, better are Morphin-KREWEL® with a HVD of 8,4h and especially Jurnista® (q.d.) with HVD =21,8h. These different galenics ban a so-called "Aut-idem-Substitution" of extended-release opioids.
authors.affiliation: Uniklinik Köln. kuno.guettler@uk-koeln.de
authors.forename: Kuno
authors.initials: K
authors.lastname: Güttler
mesh_terms: D000701:Analgesics, Opioid / Q000737:chemistry* / Q000493:pharmacokinetics* / Q000627:therapeutic use; D000818:Animals; D004305:Dose-Response Relationship, Drug; D004339:Drug Compounding / Q000379:methods* / Q000639:trends*; D006801:Humans; D010146:Pain / Q000517:prevention & control*; D010147:Pain Measurement / Q000187:drug effects; D013810:Therapeutic Equivalency
chemical_list: D000701:Analgesics, Opioid