Drugs
-
Nintedanib (Ofev(®)) inhibits receptor tyrosine kinases implicated in the pathogenesis of idiopathic pulmonary fibrosis (IPF). This article reviews the efficacy and tolerability of oral nintedanib in the treatment of IPF, as well as summarizing its pharmacological properties. ⋯ Nintedanib had an acceptable tolerability profile in patients with IPF; gastrointestinal adverse events (diarrhoea, nausea, vomiting) were reported most commonly. In conclusion, nintedanib is an important new option for the treatment of IPF.
-
Dexmedetomidine (Dexdor(®)) is a highly selective α2-adrenoceptor agonist. It has sedative, analgesic and opioid-sparing effects and is suitable for short- and longer-term sedation in an intensive care setting. In the randomized, double-blind, multicentre MIDEX and PRODEX trials, longer-term sedation with dexmedetomidine was noninferior to midazolam and propofol in terms of time spent at the target sedation range, as well as being associated with a shorter time to extubation than midazolam or propofol, and a shorter duration of mechanical ventilation than midazolam. ⋯ Dexmedetomidine had beneficial effects on delirium in some randomized, controlled trials (e.g. patients receiving dexmedetomidine were less likely to experience delirium than patients receiving midazolam, propofol or remifentanil and had more delirium- and coma-free days than patients receiving lorazepam). Intravenous dexmedetomidine had an acceptable tolerability profile; hypotension, hypertension and bradycardia were the most commonly reported adverse reactions. In conclusion, dexmedetomidine is an important option for sedation in the intensive care setting.
-
Oral naltrexone extended-release/bupropion extended-release (naltrexone ER/bupropion ER; Contrave(®), Mysimba(™)) is available as an adjunct to a reduced-calorie diet and increased physical activity in adults with an initial body mass index (BMI) of ≥ 30 kg/m(2) (i.e. obese) or a BMI of ≥ 27 kg/m(2) (i.e. overweight) in the presence of at least one bodyweight-related comorbidity, such as type 2 diabetes mellitus, hypertension or dyslipidaemia. In 56-week phase III trials in these patient populations, oral naltrexone ER/bupropion ER 32/360 mg/day was significantly more effective than placebo with regard to percentage bodyweight reductions from baseline and the proportion of patients who achieved bodyweight reductions of ≥ 5 and ≥ 10%. ⋯ Naltrexone ER/bupropion ER was generally well tolerated in phase III trials, with nausea being the most common adverse event. Thus, naltrexone ER/bupropion ER 32/360 mg/day as an adjunct to a reduced-calorie diet and increased physical activity, is an effective and well tolerated option for chronic bodyweight management in obese adults or overweight adults with at least one bodyweight-related comorbidity.
-
Eluxadoline (Viberzi(™)), developed by Actavis (now Allergan), is an orally administered, first-in-class compound that functions as both a µ-opioid receptor agonist and a δ-opioid receptor antagonist, and is indicated for the treatment of diarrhoea-predominant irritable bowel syndrome (IBS-D) in adults. The agent was originally developed by Janssen Pharmaceutica. Eluxadoline has been approved in the US, and submissions to other global authorities are being contemplated or planned. This article summarizes the milestones in the development of eluxadoline leading to this first approval for IBS-D.