Drugs of today
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Review
Milnacipran hydrochloride: its efficacy, safety and tolerability profile in fibromyalgia syndrome.
Milnacipran is a serotonin-norepinephrine reuptake inhibitor (SNRI), although its norepinephrine reuptake inhibition predominates. It has been marketed in Europe and Japan as an antidepressant for many years, but only recently has it been investigated as a treatment for fibromyalgia syndrome (FMS). Both open-label and double-blind, placebo-controlled trials have confirmed its efficacy in FMS, not only on the pain component but also on the fluctuating array of other symptoms such as sleep and cognitive disturbances and fatigue The phase III trials have employed comprehensive composite endpoints to more accurately capture the many complex domains of FMS. ⋯ It also demonstrated durability of response for up to 1 year. Its safety and tolerability were typical of its class, and it was generally well tolerated. Further work will be required to establish its place in FMS therapy by comparing it directly with other agents.
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Armodafinil is the (R)-enantiomer of the wakepromoting compound modafinil (racemic), with a considerably longer half-life of 10-15 hours. Armodafinil (developed by Cephalon, Frazer, PA, USA) was approved in June 2007 for the treatment of excessive sleepiness associated with narcolepsy, obstructive sleep apnea syndrome and shift work disorder, and the indications are the same as those for modafinil. Like modafinil, the mechanisms of action of armodafinil are not fully characterized and are under debate. ⋯ Like modafinil, armodafinil is classified as a non-narcotic Schedule IV compound. Many patients with excessive sleepiness may prefer the longer duration of effect and may have better compliance (with low doses) with armodafinil. The commercial challenge to armodafinil may come from generic modafinil, which may become available in 2012, as well as from classical amphetamine and amphetamine-like compounds (for the treatment of narcolepsy).
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Gabapentin is an antiepileptic drug (AED) by design expected to mimic the action of the neurotransmitter gamma-aminobutyric acid (GABA). However, its principal proposed mechanism of action is the interaction with the alpha 2-delta subunit of L-type voltage-regulated calcium channels. Gabapentin possesses several desirable pharmacokinetic properties, along with few drug interactions, particularly with other AEDs. ⋯ Nowadays, most worldwide prescriptions for gabapentin are for conditions other than epilepsy, especially the treatment of chronic pain of different etiologies. This article will review the pharmacology, mechanism of action, drug interactions and adverse effects of gabapentin. In addition, the clinical trial data, cost analysis and recommended schedule of administration, are also reviewed.
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Studies of populations with chronic cancer pain have shown a high prevalence of breakthrough pain (BTP), defined as transitory, severe flares of pain that occur on a background of otherwise controlled, persistent pain. High BTP prevalence rates have also been reported in patients with chronic noncancer pain, although data in these patient populations are more limited. The incidence of BTP appears to be associated with progression of chronic disease, with more than 80% of patients reporting BTP with far-advanced, end-stage cancer and noncancer terminal conditions (1). ⋯ As in the study of cancer patients, treatment with FBT was well tolerated (9). Across all studies, there was no simple linear relationship between the effective dose of FBT and the dose of the around-the-clock opioid regimen or the previous supplemental opioid, indicating that doses of FBT should be individually titrated to effectiveness rather than calculated as a percentage of existing opioid regimens. This monograph summarizes current data on the clinical pharmacology, efficacy, safety and tolerability of FBT relating to the management of opioid-tolerant patients with BTP in association with chronic pain.
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Lacosamide, (R)-2-acetamido-N-benzyl-3-meth- oxypropionamide, is a new chemical entity specifically synthesized as an anticonvulsive drug candidate, which appears to have a novel dual mode of action. Its pharmacokinetic characteristics have been studied in young and elderly healthy adults, as well as in adults with epilepsy or diabetic neuropathic pain. After oral administration, lacosamide is rapidly and completely absorbed. ⋯ For patients treated with lacosamide, the most frequently reported adverse events in placebo-controlled trials include dizziness, headache, nausea and diplopia. When used as short-term replacement for oral lacosamide, intravenous lacosamide has a comparable safety profile to oral lacosamide. Results from clinical trials to date suggest that lacosamide may be a useful pharmacological treatment option for patients with partial-onset seizures.