Clinical drug investigation
-
Bosutinib is an orally bioavailable, dual Src and Abl tyrosine kinase inhibitor approved in the USA for the treatment of Philadelphia chromosome-positive chronic myeloid leukemia following development of resistance or intolerance to prior therapy. In vitro studies demonstrated that bosutinib displays pH-dependent aqueous solubility, suggesting that concomitant administration of agents that alter gastric pH could affect bosutinib absorption. ⋯ This study demonstrated that bosutinib absorption may be reduced when co-administered with lansoprazole or other proton pump inhibitors. Caution should be used with such drug combinations, as subtherapeutic exposure of bosutinib may limit its clinical antitumor activity; short-acting antacids are recommended instead.
-
Opioids are an established therapy for cancer pain and have become an accepted therapy for chronic noncancer pain. However, increased prescribing of opioids in recent years has been accompanied by an increase in prescription opioid abuse. ⋯ The ER/LA opioid REMS require a partnership between the pharmaceutical industry, regulators, and healthcare providers to develop educational materials for physicians and patients that are not promotional. This article addresses challenges associated with improving the quality of pain care through support of prescriber education, developing formulations that combine efficacy with tamper-resistant properties, and encouraging collaborative efforts by regulatory bodies, legislators, healthcare providers, and patient advocacy groups to achieve these ends.
-
Morphine clearance has been successfully scaled from preterm neonates to 3-year-old children on the basis of a bodyweight-based exponential (BDE) function and age younger or older than 10 days. The aim of the current study was to characterize the developmental changes in morphine clearance across the entire paediatric age range. ⋯ The BDE model was able to scale both total morphine clearance and glucuronidation clearance through the M3G pathway across all age ranges between (pre)term neonates and adults by allowing the allometric exponent to decrease across the paediatric age range from values higher than 1 for neonates to values lower than 1 for infants and children.
-
Historical Article
Dose-dependent effect of landiolol, a new ultra-short-acting β(1)-blocker, on supraventricular tachyarrhythmias in postoperative patients.
β-Adrenoceptor antagonists (β-blockers) have been reported to be effective for regulation of heart rate (HR) and restoring sinus rhythm in postoperative atrial fibrillation and atrial flutter, as well as in the prevention of those arrhythmias after open-heart surgery. ⋯ The overall results, including those pertaining to patient safety, demonstrate that landiolol is effective and useful for the treatment of postoperative SVT.
-
Randomized Controlled Trial Comparative Study
Pharmacokinetics and dose proportionality of fentanyl sublingual spray: a single-dose 5-way crossover study.
Fentanyl sublingual spray is a novel formulation of fentanyl for sublingual delivery that was designed to enhance the rate and extent of absorption of fentanyl for management of breakthrough cancer pain (BTCP). ⋯ In healthy subjects, administration of fentanyl sublingual spray produced a rapid rise in fentanyl plasma concentrations. Dose-dependent parameters (C max and AUC) showed dose proportionality across the range of 100-800 μg. Altering the local environment of the oral cavity (temperature and pH) showed no effects on the bioavailability of fentanyl. The rapid and predictable rise in plasma fentanyl concentrations following administration of fentanyl sublingual spray corresponds with the rapid onset and duration of many BTCP episodes.