Expert opinion on drug metabolism & toxicology
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Fosphenytoin, phosphate ester pro-drug of phenytoin, was developed to overcome complications associated with parenteral phenytoin administration in treatment of acute symptomatic seizures, short-term prophylaxis and treatment of repetitive or prolonged seizures and status epilepticus. ⋯ Published literature shows that intravenous fosphenytoin has a similar adverse effect profile than phenytoin when it is administered as recommended. There is no evidence of clear benefit that would justify the higher price of the fosphenytoin compared to phenytoin.
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Expert Opin Drug Metab Toxicol · May 2009
ReviewThe butyrylcholinesterase knockout mouse a research tool in the study of drug sensitivity, bio-distribution, obesity and Alzheimer's disease.
Butyrylcholinesterase (BChE) mutations common in the human population may result in complete or partial BChE deficiency, making the BChE knockout (KO) mouse a model for human deficiencies. The BChE KO mouse cannot tolerate standard doses of the muscle relaxant succinylcholine or the Alzheimer's disease drugs huperzine A and donepezil. It is resistant to the asthma drug bambuterol. ⋯ Future studies will make a double knockout that has neither BChE nor carboxylesterase. The double knockout is expected to be unusually sensitive to the toxicity of organophosphorus pesticides. Knowledge of drug sensitivities in the mouse model of human BChE deficiency will aid in understanding adverse drug effects in humans.
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Expert Opin Drug Metab Toxicol · Mar 2009
ReviewSolifenacin succinate for the treatment of overactive bladder.
Solifenacin succinate, a competitive muscarinic receptor antagonist, is one of the newer options for the treatment of overactive bladder in men and women. ⋯ Solifenacin succinate was shown to be effective for symptom control with an increase in volume voided, improvement in quality of life and a decrease in a common side effect of dry mouth compared to other medications.
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Restless legs syndrome (RLS) is a chronic neurological disorder associated with sleep disturbance. Ropinirole, a non-ergot dopamine agonist, has been widely studied for the treatment of moderate-to-severe primary RLS in a comprehensive clinical development program. In these studies, ropinirole was effective in significantly improving the symptoms of RLS, compared with placebo, in patients with moderate-to-severe primary RLS. ⋯ Significant improvements in RLS symptoms were observed within 2 nights of treatment. Ropinirole also produced significant benefits on objective measures of RLS motor symptoms, such as periodic leg movements; and on subjective measures of sleep, ropinirole was generally well tolerated. A newly developed extended-release formulation of ropinirole may benefit patients who warrant an extended duration of therapy.
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Dexmedetomidine is an alpha-2 adrenoreceptor agonist with sedative, analgesic and anxiolytic properties. Since its release in the US market in late 1999, it has gained remarkable attention in the adult, pediatric and geriatric populations, predominantly because of its minimal respiratory depression. However, beyond its well-known properties, dexmedetomidine has recently been investigated for its potential in many other clinical scenarios, including neuroprotection, cardioprotection and renoprotection, with promising results. ⋯ Dexmedetomidine is a novel agent with a wide safety margin and excellent sedative and moderate analgesic properties. Though its broadest use is currently in surgical and nonsurgical intensive care unit patients, dexmedetomidine appears to have promising future applications in the areas of neuroprotection, cardioprotection and renoprotection.