Andrew Davies1, Gill Mundin2, Joanna Vriens3, Kath Webber4, Alison Buchanan4, Melanie Waghorn4. 1. Royal Surrey County Hospital, Guildford, Surrey, United Kingdom. Electronic address: adavies12@nhs.net. 2. Mundipharma Research Ltd., Cambridge, Cambridgeshire, United Kingdom. 3. Princess Alice Hospice, Esher, Surrey, United Kingdom. 4. Royal Surrey County Hospital, Guildford, Surrey, United Kingdom.
Abstract
CONTEXT: Salivary gland hypofunction may affect the absorption of drugs through the oral mucosa, which in turn may affect their clinical efficacy (e.g., onset of action). OBJECTIVES: The aim of this study was to assess the pharmacokinetics of a sublingual fentanyl orally disintegrating tablet (Abstral, Prostrakan Inc.) in a group of cancer patients with salivary gland hypofunction. METHODS: Nine cancer patients with salivary gland hypofunction underwent a series of three pharmacokinetic studies with the sublingual fentanyl orally disintegrating tablet. In the first phase, the patients received no pretreatment; in the second phase, the patients were allowed to moisten the oral cavity before dosing; in the third phase, the patients were given pilocarpine hydrochloride (saliva stimulant) before dosing. Fentanyl concentrations were measured using a method of high-performance liquid chromatography with validated tandem mass spectrometric detection. RESULTS: The Tmax was longer, the Cmax was lower, the AUC0-30 lower, and the AUClast lower in the phase involving no pretreatment; the Tmax/Cmax/AUC0-30/AUClast were similar in the phase involving moistening of the oral cavity and the phase involving giving pilocarpine hydrochloride. CONCLUSION: The pharmacokinetics of the sublingual fentanyl orally disintegrating tablet appear to be negatively affected by the presence of salivary gland hypofunction, although the moistening of the oral cavity before dosing results in a pharmacokinetic profile similar to that seen with the giving of pilocarpine hydrochloride.
CONTEXT: Salivary gland hypofunction may affect the absorption of drugs through the oral mucosa, which in turn may affect their clinical efficacy (e.g., onset of action). OBJECTIVES: The aim of this study was to assess the pharmacokinetics of a sublingual fentanyl orally disintegrating tablet (Abstral, Prostrakan Inc.) in a group of cancerpatients with salivary gland hypofunction. METHODS: Nine cancerpatients with salivary gland hypofunction underwent a series of three pharmacokinetic studies with the sublingual fentanyl orally disintegrating tablet. In the first phase, the patients received no pretreatment; in the second phase, the patients were allowed to moisten the oral cavity before dosing; in the third phase, the patients were given pilocarpine hydrochloride (saliva stimulant) before dosing. Fentanyl concentrations were measured using a method of high-performance liquid chromatography with validated tandem mass spectrometric detection. RESULTS: The Tmax was longer, the Cmax was lower, the AUC0-30 lower, and the AUClast lower in the phase involving no pretreatment; the Tmax/Cmax/AUC0-30/AUClast were similar in the phase involving moistening of the oral cavity and the phase involving giving pilocarpine hydrochloride. CONCLUSION: The pharmacokinetics of the sublingual fentanyl orally disintegrating tablet appear to be negatively affected by the presence of salivary gland hypofunction, although the moistening of the oral cavity before dosing results in a pharmacokinetic profile similar to that seen with the giving of pilocarpine hydrochloride.
Authors: Ahsan Azhar; Yu Jung Kim; Ali Haider; David Hui; Vishidha R Balankari; Margeaux Chiou Epner; Minjeong Park; Diane D Liu; Janet Williams; Susan E Frisbee-Hume; Julio A Allo; Eduardo Bruera Journal: Oncologist Date: 2018-09-25
Authors: Robert Janknegt; Marieke van den Beuken; Sjouke Schiere; Michael Überall; Roger Knaggs; Jaquie Hanley; Morten Thronaes Journal: Eur J Hosp Pharm Date: 2017-01-11
Authors: Evelien J M Kuip; Wendy H Oldenmenger; Esther Oomen-de Hoop; Gerda M Verduijn; Martine F Thijs-Visser; Peter de Bruijn; Esther van Meerten; Stijn L W Koolen; Ron H J Mathijssen; Carin C D van der Rijt Journal: Cancers (Basel) Date: 2018-11-15 Impact factor: 6.639