Macitentan is an orphan drug for the treatment of pulmonary arterial hypertension (PAH). Endothelin-1 (ET-1) plays a critical role of pathophysiology of PAH. Macitentan, a new dual endothelin receptor antagonist, has reportedly improved prognosis of PAH patients by delaying the progression of disease. It prevents the binding of ET-1 to both endothelin A (ETA) and endothelin B (ETB) receptors. Macitentan displays higher efficacy, lesser adverse effects and drug interactions. It has completed phase III trials in 2012 for treatment of PAH and has been tried for ischemic digital ulcers in systemic sclerosis, recurrent glioblastoma and combination with chemotherapeutic agents against various cancers. Safety data for macitentan were obtained primarily from a placebo-controlled clinical study in 742 patients with PAH. The Food and Drug Administration (FDA) approved the drug on 13 October 2013. It is an important addition to long-term treatment of PAH.
Opioid-induced constipation (OIC) is one of the most troublesome and the most common effects of opioid use leading to deterioration in quality of life of the patients and also has potentially deleterious repercussions on adherence and compliance to opioid therapy. With the current guidelines advocating liberal use of opioids by physicians even for non-cancer chronic pain, the situation is further complicated as these individuals are not undergoing palliative care and hence there cannot be any justification to subject these patients to the severe constipation brought on by opioid therapy which is no less debilitating than the chronic pain. The aim in these patients is to prevent the opioid-induced constipation but at the same time allow the analgesic activity of opioids. Many drugs have been used with limited success but the most specific among them were the peripherally acting mu opioid receptor antagonists (PAMORA). Methylnaltrexone and alvimopan were the early drugs in this group but were not approved for oral use in OIC. However naloxegol, the latest PAMORA has been very recently approved as the first oral drug for OIC. This article gives an overview of OIC, its current management and more specifically the development and approval of naloxegol, including pharmacokinetics, details of various clinical trials, adverse effects and its current status for the management of OIC.
Diabetes is a metabolic disorder characterized by relative or absolute deficiency of insulin, resulting in hyperglycemia. The main treatment of diabetes relies on subcutaneous insulin administration by injection or continuous infusion to control glucose levels, besides oral hypoglycemic agents for type 2 diabetes. Novel routes of insulin administration are an area of research in the diabetes field as insulin injection therapy is burdensome and painful for many patients. Inhalational insulin is a potential alternative to subcutaneous insulin in the management of diabetes. The large surface area, good vascularization, immense capacity for solute exchange and ultra-thinness of the alveolar epithelium facilitates systemic delivery of insulin via pulmonary administration. Inhaled insulin has been recently approved by Food and Drug Administration (FDA). It is a novel, rapid-acting inhaled insulin with a pharmacokinetic profile that is different from all other insulin products and comparatively safer than the previous failed inhaled insulin (Exubera).
Hepatitis C virus (HCV) continues to be a global problem but with the arrival of new drugs it is expected to move towards exile. The health care community has finally woken up to the need to tackle this infection especially because HCV-induced hepatitis in combination with HIV has turned out to be a formidable foe. So far the management of HCV has concentrated mainly on interferon-based therapies. The focus is now increasingly on drugs targeting various other components of hepatitis C, which are essential for its survival in the host like HCV non-structural (NS) 3/4A serine protease inhibitors: Boceprevir, telaprevir, simeprevir; NS5A inhibitors (daclatasvir, ledipasvir); NS5B polymerase inhibitors (sofosbuvir), cyclophilin inhibitors and many others in the pipeline like the NS4B inhibitors and the micro-RNA122 inhibitors. These new drugs have shown excellent sustained virological response (SVR) compared to the presently available drugs and their combinations. Adding to this is the new HCV vaccine which although facing various hurdles is making good inroads and expected to meet its endpoints in the near future. This review gives a brief overview of epidemiology, pathogenesis, followed by the description of current regimens in the treatment of hepatitis C and the much eagerly awaited future all new oral anti-hepatitis C regimen, which can potentially eliminate the use of painful injections of interferon.
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