Expert review of clinical pharmacology
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Sugammadex, a modified γ-cyclodextrin, is the first selective relaxant binding agent. Sugammadex forms very tight complexes in a 1:1 ratio with steroidal neuromuscular blocking agents (rocuronium > vecuronium > pancuronium). This guest-host complex, which exists in equilibrium, is stable because of its very high association rate and very low dissociation rate. ⋯ Sugammadex in doses ranging from 2 to 16 mg/kg is recommended, depending of the level of rocuronium- or vecuronium-induced blockade. Common (incidence of 1-10%) adverse effects are similar for sugammadex and placebo, and include anesthetic complications (movement, coughing, grimacing or suckling on the tracheal tube) and cough. The US FDA has had concerns regarding the safety of sugammadex (hypersensitivity and allergic reactions), but upcoming international studies and the drug's widespread use in the EU will provide additional information.
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Expert Rev Clin Pharmacol · Nov 2008
Transdermal buprenorphine in chronic pain: indications and clinical experience.
Transdermal buprenorphine has been shown to be effective in managing moderate-to-severe cancer pain and severe pain that is unresponsive to nonopioid analgesics. In clinical trials, it provided better pain relief than placebo, despite a higher consumption of rescue analgesia by placebo patients. Analgesia was rated as satisfactory or better by 90% of patients in a long-term follow-up study and 94.6% considered the buprenorphine matrix patch to be user friendly. ⋯ No problems have been encountered when switching from another opioid to transdermal buprenorphine, or in combining the buprenorphine patch with intravenous morphine or tramadol for breakthrough pain. There is a growing body of evidence that transdermal buprenorphine may be particularly useful for managing neuropathic pain. Most notably, it appears to be effective in treating hyperalgesic states and syndromes characterized by pronounced central sensitization.
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Expert Rev Clin Pharmacol · Jan 2008
Clinical pharmacology of fentanyl buccal tablet for the treatment of breakthrough pain.
Fentanyl buccal tablet (FBT) is a new formulation of fentanyl providing rapid-onset analgesia for the treatment of breakthrough pain. FBT has been approved for the management of breakthrough pain in patients with cancer who are already receiving and who are tolerant to opioid therapy for underlying persistent pain. FBT has demonstrated a favorable pharmacokinetic profile, which is closely aligned to the rapid onset and duration of an episode of breakthrough pain, and is generally safe and well tolerated.
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Expert Rev Clin Pharmacol · Jan 2008
Aprepitant for the prevention of nausea and vomiting associated with chemotherapy and postoperative recovery.
Chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) can negatively impact patient quality of life, functional performance and activities of daily living. Although the development of serotonin receptor antagonists has greatly improved the control of acute emesis, delayed CINV remains a significant clinical issue. Aprepitant (Emend(®)) is the first commercially available drug from a new class of agents, the neurokinin-1 receptor antagonists. ⋯ By contrast, aprepitant as monotherapy is indicated for the prevention of PONV. Aprepitant represents an emerging class of agents and its addition to standard therapy provides an advanced benefit in the prevention and treatment of CINV and PONV. Investigations of aprepitant for other indications are ongoing.