PainBrake is a new patented formulation of carbamazepine (Tegretolâ) that enables accurate dose fractionation for the treatment of neuropathic pain, a condition that results from a dysfunction of nerves involved in the perception of pain and that is typically chronic and particularly prevalent in elderly patients. An NIH-supported study published in 2009 estimated that almost 16 million Americans suffer from chronic neuropathic pain (Yawn et al, 2009) and the number of patients suffering from neuropathic pain is expected to increase due to the aging population. Current drugs provide a useful degree of pain relief in only about half the patients, very few patients achieve complete relief of pain (Nightingale, 2012). Peak dose-limiting side effects, mainly sedation, somnolence, dizziness and balance problems which are poorly tolerated by the elderly (Oomens et al, 2015) cause patients to be under-dosed, thereby contributing to inadequate pain relief. This is particularly true for carbamazepine, a drug that is considered to be the first line therapy for the treatment of certain forms of neuropathic pain (Zakrzewska, 2015).
To overcome dose-limiting side effects, PainBrake tablets employ an innovative bilayered, deeply scored design patented by AccuBreak. The top layer contains carbamazepine and is pre-divided by deep scoring during the manufacturing process to provide exact doses enabling easy tablet splitting into exact doses. The bottom layer provides mechanical stability and serves as the break region when splitting the tablet. GTP has in-licensed against milestones and royalties the worldwide rights to the use of the AccuBreak technology for the delivery of voltage-gated sodium channel blockers.
Bertilsson (1978, published on line in 2012) advocated fractional dosing to help maintain the plasma concentrations within the range of 24 to 34 mmol/L that provide efficacious plasma concentrations without reaching side-effect provoking concentrations. Management believes that PainBrake could help more patients achieve nearly complete pain relief but without peak dose side effects by allowing the intake of frequent small accurate doses. Zakrzewska (2015) advocates starting treatment with low doses of carbamazepine, and titrating up slowly to the dose best adapted to each patient, especially in elderly patients. Management anticipates that "PainBrake," will allow slow, precise, upward titration.