Disease relevance of SPM 927

• In diabetic rats, lacosamide attenuated cold (10, 30 mg/kg, i.p.), warm (3, 10, 30 mg/kg, i.p.) and mechanical allodynia (30 mg/kg, i.p.). Streptozotocin-induced thermal and mechanical hyperalgesia were reduced by lacosamide at doses of 10 and 30 mg/kg, i.p. Morphine (3 mg/kg) showed similar efficacy on allodynia and hyperalgesia [1].
• Antinociceptive efficacy of lacosamide in a rat model for painful diabetic neuropathy [1].
• Lacosamide also produced hypothermia at antinociceptive doses in rats [2].
• In rats with infraorbital nerve injury, lacosamide reduced mechanical hypersensitivity and the effect was markedly stronger in female than in male rats [2].
• Lacosamide in painful diabetic peripheral neuropathy: a phase 2 double-blind placebo-controlled study [3].

Psychiatry related information on SPM 927

• Lacosamide was administered to rats 30min before pain threshold measurements [4].

High impact information on SPM 927

• Lacosamide (LCM) is anticonvulsant in animal models and is in phase 3 assessment for epilepsy and neuropathic pain [5].
• Effects of the novel antiepileptic drug lacosamide on the development of amygdala kindling in rats [6].
• We conclude that lacosamide blocks 4-AP induced epileptiform activity in the visual cortex [7].
• Physiological synaptic transmission (fEPSP amplitude and duration) in CA1 of rat hippocampus was not significantly altered (P > 0.05, n = 4) by lacosamide (1 microM-1 mM) [7].
• In spinal cord injured female rats 10-20 mg/kg lacosamide dose-dependently alleviated the mechanical and cold allodynia-like behaviors without causing motor impairments or marked sedation [2].

Chemical compound and disease context of SPM 927

• Moreover, thermal hyperalgesia induced by carrageenan as well as the formalin-induced licking response were dose-dependently attenuated by lacosamide [4].
• Lacosamide (3, 10, and 30 mg/kg) was able to reduce secondary mechanical allodynia and hyperalgesia similarly to morphine (3 mg/kg) [8].
• Antinociceptive efficacy of lacosamide in the monosodium iodoacetate rat model for osteoarthritis pain [8].

Biological context of SPM 927

• In addition, effects of the new antiepileptic drug lacosamide were examined on the stimulation-induced metabolic activation [9].
• Lacosamide (N=60) titrated from 100 to 400 mg/d or maximum tolerated dose and placebo (N=59) were the trial interventions [3].
• Additionally, lacosamide exhibits linear, dose-proportional pharmacokinetics with low intra- and interpatient variability [10].
• Rapidly and completely absorbed after oral administration, lacosamide has an elimination half-life of approximately 13 hours and a low potential for drug interactions [10].

Analytical, diagnostic and therapeutic context of SPM 927

• Lacosamide (20 mg/kg) injected i.p. 30 min before application of electrical stimulation antagonized completely the seizure-induced brain metabolic activation but did not affect basal 2-DG uptake [9].
• Randomized controlled trials of adjunctive lacosamide (200, 400, and 600 mg/day) have demonstrated statistically significant reduction in median seizure frequency compared with placebo [10].
• The efficacy and safety results from completed clinical trials, as well as the favorable pharmacokinetic profile, suggest that lacosamide may represent a significant advance in antiepileptic drug therapy [10].

References