[28-31] The sumatriptan iontophoretic transdermal system (Zecuity®, sumatriptan TDS, NuPathe, Inc., http://www.selleckchem.com/products/chir-99021-ct99021-hcl.html Conshohocken, PA, USA), which was developed to address the unmet needs of migraine patients, particularly those with MRN, employs iontophoretic technology to deliver sumatriptan, the most widely used treatment for migraine. Sumatriptan TDS, which circumvents the GI tract by using low-level electrical energy to transport

sumatriptan across the skin, provides clinical benefits in migraine without the need for oral, intranasal, or subcutaneous administration[32] by relying on proprietary iontophoretic technology. Migraine patients apply sumatriptan TDS to the upper arm or thigh, and the activated system drives ionized sumatriptan into the bloodstream at controlled rates over 4 hours (Fig. 1 —), resulting in a predictable pharmacology and efficacy. The pharmacological and clinical profiles of sumatriptan TDS have been characterized in multiple well-controlled studies. Selleck Tyrosine Kinase Inhibitor Library In a single-center, open-label, cross-over study, Pierce and colleagues

compared the pharmacokinetic (PK) profiles of the oral (100 mg), intranasal (20 mg), and subcutaneous (6 mg) formulations of sumatriptan with sumatriptan TDS in 25 healthy volunteers aged 21-57 years.[32] The area under the drug concentration-time

curve (AUC) for sumatriptan TDS was similar to the subcutaneous formulation, but it had a lower maximum observed drug concentration (Cmax), which decreased the relative risk 上海皓元医药股份有限公司 of triptan-like sensations believed to be attributable to peak plasma concentrations. Moreover, because the transdermal and subcutaneous formulations had lower coefficients of variation than the oral and intranasal formulations (Table 1), they achieved and sustained more predictable target drug levels.[32] Sumatriptan was detected in plasma within 15 minutes after activation of sumatriptan TDS, it reached plasma concentrations of 10 ng/mL by approximately 30 minutes after patch activation, and it maintained concentrations of approximately 20 ng/mL until 4 hours post-activation. Over the 4-hour study period, the mean drug delivery for sumatriptan TDS was approximately 6.1 mg. When drug delivery was stopped at 4 hours post-activation, steady declines in serum concentration for sumatriptan matched the gradual reductions in plasma concentrations following administration of the oral and intranasal formulations.[32] Other investigations have extended these early findings.