Feb 112015
 
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Naloxegol: A Review of Its Use in Patients with Opioid-Induced Constipation.

Drugs. 2015 Feb 10;

Authors: Garnock-Jones KP

Abstract
Oral naloxegol (Movantik™, Moventig(®)), a peripherally acting μ-opioid receptor antagonist, inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract. This article reviews the pharmacological properties of naloxegol and its clinical efficacy and tolerability in patients with opioid-induced constipation. It demonstrated clinical efficacy and was well tolerated in placebo-controlled trials in patients with non-cancer pain and opioid-induced constipation, including those with an inadequate response to laxatives, and was well tolerated in a long-term safety study. As a PEGylated naloxone derivative, naloxegol is associated with significant improvements in spontaneous bowel movements, while maintaining levels of opioid-related analgesia (a result of its reduced ability to cross the blood-brain barrier). Naloxegol is a useful option in the treatment of opioid-induced constipation.

PMID: 25666542 [PubMed - as supplied by publisher]

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Feb 112015
 
Related Articles

Identification and Management of Alcohol Withdrawal Syndrome.

Drugs. 2015 Feb 10;

Authors: Mirijello A, D'Angelo C, Ferrulli A, Vassallo G, Antonelli M, Caputo F, Leggio L, Gasbarrini A, Addolorato G

Abstract
Symptoms of alcohol withdrawal syndrome (AWS) may develop within 6-24 h after the abrupt discontinuation or decrease of alcohol consumption. Symptoms can vary from autonomic hyperactivity and agitation to delirium tremens. The gold-standard treatment for AWS is with benzodiazepines (BZDs). Among the BZDs, different agents (i.e., long-acting or short-acting) and different regimens (front-loading, fixed-dose or symptom-triggered) may be chosen on the basis of patient characteristics. Severe withdrawal could require ICU admission and the use of barbiturates or propofol. Other drugs, such as α2-agonists (clonidine and dexmetedomidine) and β-blockers can be used as adjunctive treatments to control neuroautonomic hyperactivity. Furthermore, neuroleptic agents can help control hallucinations. Finally, other medications for the treatment for AWS have been investigated with promising results. These include carbamazepine, valproate, sodium oxybate, baclofen, gabapentin and topiramate. The usefulness of these agents are discussed.

PMID: 25666543 [PubMed - as supplied by publisher]

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Feb 052015
 
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Fluticasone Furoate/Vilanterol: a Review of Its Use in Patients with Asthma.

Drugs. 2015 Feb 4;

Authors: Syed YY

Abstract
Fluticasone furoate/vilanterol (Relvar(®)) is a once-daily, fixed combination of an inhaled corticosteroid (ICS) and a long-acting β2-adrenoreceptor agonist (LABA), delivered via a dry powder inhaler (Ellipta(®)). It is approved for the treatment of asthma in the EU and Japan, and is the first once-daily ICS/LABA to be available for this indication. Fluticasone furoate is an enhanced-affinity glucocorticoid receptor agonist, with potent anti-inflammatory activity. Vilanterol produces rapid and prolonged bronchodilation. In phase III trials in adolescents and adults with various levels of asthma uncontrolled on ICS and/or ICS/LABA, fluticasone furoate/vilanterol 100/25 or 200/25 µg once daily (approved dosages in the EU) significantly improved pulmonary function compared with placebo or equivalent dosages of fluticasone furoate alone (in some trials) or fluticasone propionate. In similar trials, fluticasone furoate/vilanterol 100/25 µg once daily was as effective as fluticasone propionate/salmeterol 250/50 µg twice daily in improving pulmonary function and significantly reduced the risk of severe asthma exacerbation relative to fluticasone furoate alone. In clinical trials, fluticasone furoate/vilanterol was generally well tolerated with fewer than 15 % of patients experiencing treatment-related adverse events, the most common of which were oral/oropharyngeal candidiasis, dysphonia, extrasystoles and cough. The tolerability profile of fluticasone furoate/vilanterol was generally similar to that of fluticasone propionate/salmeterol. Thus, fluticasone furoate/vilanterol is an effective and generally well tolerated ICS/LABA option for the treatment of uncontrolled asthma.

PMID: 25648266 [PubMed - as supplied by publisher]

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Jan 182015
 
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Posaconazole: A Review of the Gastro-Resistant Tablet and Intravenous Solution in Invasive Fungal Infections.

Drugs. 2015 Jan 17;

Authors: McKeage K

Abstract
Posaconazole (Noxafil(®)) is a triazole antifungal agent with an extended spectrum of antifungal activity. It is approved for the prophylaxis of invasive fungal infections in patients with neutropenia or in haematopoietic stem cell transplant recipients undergoing high-dose immunosuppressive therapy for graft-versus-host disease, and for the treatment of fungal infections. The efficacy and good tolerability of posaconazole oral suspension administered three or four times daily is well established. However, in order to overcome pharmacokinetic limitations associated with the suspension, a new gastro-resistant tablet and intravenous (IV) solution were developed. This article reviews the pharmacokinetic properties of the new posaconazole formulations and briefly summarizes efficacy data relating to the suspension. The pharmacokinetic advantages of the posaconazole gastro-resistant tablet compared with the suspension formulation include less interpatient variability, better systemic availability enabling once-daily administration, and absorption that is unaffected by changes in gastric pH or motility; in addition the tablets may be taken with or without food. The posaconazole tablet achieves higher and more consistent mean plasma concentrations than the suspension and, therefore, it is the preferred option to optimize efficacy in the prophylaxis or treatment of invasive fungal disease. The posaconazole IV solution provides an option for these same indications in patients who are unable to receive oral formulations.

PMID: 25595699 [PubMed - as supplied by publisher]

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Jan 072015
 

Droxidopa: A Review of Its Use in Symptomatic Neurogenic Orthostatic Hypotension.

Drugs. 2015 Jan 6;

Authors: Keating GM

Abstract
The norepinephrine prodrug droxidopa (NORTHERA™) is approved in the US for the treatment of orthostatic dizziness, lightheadedness, or the 'feeling that you are about to black out' in adults with symptomatic neurogenic orthostatic hypotension associated with primary autonomic failure (e.g. Parkinson's disease, multiple system atrophy or pure autonomic failure), dopamine β-hydroxylase deficiency or nondiabetic autonomic neuropathy. This article reviews the clinical efficacy and tolerability of droxidopa in symptomatic neurogenic orthostatic hypotension, as well as summarizing its pharmacological properties. Oral droxidopa was effective in the shorter-term treatment of patients with symptomatic neurogenic orthostatic hypotension, with improvements seen in symptoms, the impact of symptoms on daily activities and standing systolic blood pressure. More data are needed to confirm the longer-term efficacy of droxidopa. Droxidopa was generally well tolerated, although patients should be monitored for supine hypertension.

PMID: 25559422 [PubMed - as supplied by publisher]

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Nov 282014
 

Ferric Carboxymaltose: A Review of Its Use in Iron Deficiency.

Drugs. 2014 Nov 27;

Authors: Keating GM

Abstract
Ferric carboxymaltose (Ferinject(®), Injectafer(®)) is an intravenous iron preparation approved in numerous countries for the treatment of iron deficiency. A single high dose of ferric carboxymaltose (up to 750 mg of iron in the US and 1,000 mg of iron in the EU) can be infused in a short time frame (15 min). Consequently, fewer doses of ferric carboxymaltose may be needed to replenish iron stores compared with some other intravenous iron preparations (e.g. iron sucrose). Ferric carboxymaltose improved self-reported patient global assessment, New York Heart Association functional class and exercise capacity in patients with chronic heart failure and iron deficiency in two randomized, placebo-controlled trials (FAIR-HF and CONFIRM-HF). In other randomized controlled trials, ferric carboxymaltose replenished iron stores and corrected anaemia in various populations with iron-deficiency anaemia, including patients with chronic kidney disease, inflammatory bowel disease or heavy uterine bleeding, postpartum iron-deficiency anaemia and perioperative anaemia. Intravenous ferric carboxymaltose was generally well tolerated, with a low risk of hypersensitivity reactions. It was generally better tolerated than oral ferrous sulfate, mainly reflecting a lower incidence of gastrointestinal adverse effects. The most common laboratory abnormality seen in ferric carboxymaltose recipients was transient, asymptomatic hypophosphataemia. The higher acquisition cost of ferric carboxymaltose appeared to be offset by lower costs for other items, with the potential for cost savings. In conclusion, ferric carboxymaltose is an important option for the treatment of iron deficiency.

PMID: 25428711 [PubMed - as supplied by publisher]

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