Fundamental & clinical pharmacology
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Fundam Clin Pharmacol · Feb 2012
Review Comparative StudyClinical effects and outcomes with new P2Y12 inhibitors in ACS.
Thienopyridines have become the cornerstone of treatment for percutaneous coronary intervention although no survival benefit has ever been shown with clopidogrel despite increasing loading doses. Newly developed P2Y12 inhibitors are more potent, more predictable, and have a faster onset of action than clopidogrel, characteristics that make them particularly attractive for high-risk percutaneous coronary intervention (PCI). Four new P2Y12 inhibitors have been tested each of them having particular individual properties. ⋯ Because in clinical trials, patients perceived to be at higher risk of bleeding usually are excluded, the risk of major and even fatal bleeding might even be higher in a 'real-world' setting, i.e. in the elderly patient with comorbidities. On the other hand, these newly developed P2Y12 inhibitors decrease mortality after PCI compared with clopidogrel. The risk/benefit ratio is particularly favorable in PCI for patients with STEMI.
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Fundam Clin Pharmacol · Feb 2012
Review Comparative StudyManagement of the airway without the use of neuromuscular blocking agents: the use of remifentanil.
Remifentanil belongs to opioid drugs, and its pharmacokinetic characteristics make it unique in this class of drugs and appropriate for use during intubation without neuromuscular blockage. This up-to-date review aims to summarize the findings of recent studies regarding remifentanil and intubation. ⋯ Strong evidence exists that illuminates the usefulness of the drug in cases of difficult airway as well as in neuromuscular diseases. Beyond all these favorable characteristics, anesthesiologists must be conscious with the use of remifentanil.
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Rivaroxaban, an oral, direct factor Xa inhibitor, is a small molecule drug capable of inhibiting not only free factor Xa with high selectivity but also prothrombinase-bound and clot-associated factor Xa in a concentration-dependent manner. Clinical studies have demonstrated predictable anticoagulation and confirmed dose-proportional effects for rivaroxaban in humans with a rapid onset (within 2-4 h) and a half-life of 7-11 h and 11-13 h for young and elderly subjects, respectively. For a 10 mg dose, the oral bioavailability of rivaroxaban is high (80-100%) and is not affected by food intake. ⋯ Rivaroxaban is currently approved for the prevention of venous thromboembolism (VTE) in adult patients undergoing elective hip or knee replacement surgery. Studies using 10 mg rivaroxaban once daily in this indication demonstrated its suitability for a wide range of patients regardless of age, gender or body weight. Further studies in the treatment of VTE, prevention of cardiovascular events in patients with acute coronary syndrome, prevention of stroke in those with atrial fibrillation and prevention of VTE in hospitalized medically ill patients have been reported or are ongoing.