Clinical drug investigation
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Review
Diclofenac sodium injection (akis(®), dicloin (®)): a review of its use in the management of pain.
A novel formulation of diclofenac sodium suitable for subcutaneous or intramuscular injection (Akis(®), Dicloin(®)) has been developed using the complexing agent hydroxypropyl-β-cyclodextrin (HPβCD) as a solubility enhancer. Diclofenac HPβCD is available in several European countries, where it is indicated for use in adults with acute forms of pain, including postoperative pain. Clinical trials have demonstrated the analgesic efficacy of diclofenac HPβCD in terms of relieving moderate to severe postoperative pain in patients undergoing dental surgery or minor orthopaedic surgery. ⋯ The local tolerability of diclofenac HPβCD was consistently rated as 'good' or 'excellent' across all studies. Subcutaneous administration of diclofenac is a valid alternative to intramuscular delivery, with the advantages of easier administration, the availability of additional body sites suitable for injection and the potential for self-administration. Thus, diclofenac HPβCD 25, 50 or 75 mg/mL solution for subcutaneous or intramuscular injection extends the treatment options available for use in the management of pain in adults.
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Randomized Controlled Trial
Safety, Tolerability and Pharmacokinetic and Pharmacodynamic Learnings from a Double-Blind, Randomized, Placebo-Controlled, Sequential Group First-in-Human Study of the TRPV1 Antagonist, JNJ-38893777, in Healthy Men.
Nociceptive and neuropathic pain, one of common reasons of disability and loss of quality life, are often undertreated due to safety concerns with current therapies. This study assessed the safety, tolerability, pharmacokinetics and pharmacodynamics of JNJ-38893777, a potent and selective transient receptor potential vanilloid 1 (TRPV1) channel antagonist in healthy men. ⋯ JNJ-38893777 was tolerated at single doses up to 500 mg (fed) and is suitable for further clinical development.
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Randomized Controlled Trial
Dose proportionality of a hydrocodone extended-release tablet formulated with abuse-deterrence technology.
This open-label, crossover study evaluated the dose proportionality of a hydrocodone extended-release (ER) tablet employing the CIMA(®) Abuse-Deterrence Technology platform. ⋯ Hydrocodone exposure increased in a dose-proportional manner after administration of hydrocodone ER 15-90 mg tablets in healthy, naltrexone-blocked subjects.
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Teduglutide (Gattex(®)) is a recombinant analogue of human glucagon-like peptide-2 and is indicated for the treatment of adults with short bowel syndrome (SBS) dependent on parenteral support (PS). In a pivotal, 24-week clinical trial in SBS patients, subcutaneous teduglutide 0.05 mg/kg once daily increased absorption from the remnant intestine as evidenced by significant reductions in PS volume requirements versus placebo. ⋯ Among patients who received teduglutide treatment for up to 30 months, 11 of 30 were able to achieve at least one additional day off PS and another ten achieved complete independence from PS. Subcutaneous teduglutide was generally well tolerated in clinical trials, including over the long term, with most adverse events that led to study discontinuation being gastrointestinal in origin.
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Randomized Controlled Trial
Effect of the gastrointestinal prokinetic agent erythromycin on the pharmacokinetics of pregabalin controlled-release in healthy individuals: a phase I, randomized crossover trial.
The controlled-release (CR) formulation of pregabalin is designed to remain in the stomach for a prolonged period while slowly releasing pregabalin for absorption in the small intestine. This study evaluated the effect of the gastrointestinal prokinetic agent, erythromycin, on the pharmacokinetics of a single dose of pregabalin CR 330 mg administered following an evening meal and the safety and tolerability of a single dose of pregabalin CR 330 mg when administered with and without multiple doses of erythromycin 500 mg. ⋯ Co-administration of multiple high doses of erythromycin resulted in 17 % lower pregabalin exposure for a single dose of pregabalin CR 330 mg than for pregabalin CR 330 mg administered alone. Although the two treatments did not achieve formal bioequivalence, the impact of co-administered erythromycin treatment was small and not considered clinically relevant.