Características farmacológicas y clínicas de insulina aspártica más rápida (Fiasp®) / Pharmacological and clinical characteristics of Insulin Faster Aspart (Fiasp®)

Resumen La insulina aspártica de acción rápida es una formulación más rápida de la insulina aspártica convencional, a la que se adicionan nicotinamida y L-arginina para lograr una absorción más rápida en el tejido celular subcutáneo. Estudios farmacocinéticos y farmacodinámicos demostraron un desplazamiento de las curvas de concentración sérica de insulina/tiempo hacia la izquierda en comparación con la formulación conven cional. Su perfil de eficacia se destaca en términos del control de la glucemia posprandial temprana. Además, la insulina aspártica de acción rápida aporta flexibilidad al tratamiento, ya que puede aplicarse al momento de la comida, inmediatamente antes o hasta 20 minutos después, lo que constituye una ventaja en cuanto a calidad de vida en los pacientes con diabetes en tratamiento con insulina prandial, especialmente en poblaciones como los niños, las embarazadas o los ancianos. El patrón de seguridad y tolerabilidad es comparable al de la insulina aspártica convencional.

Abstract Fast acting aspart insulin is a faster-acting formulation of aspart insulin, having nicotinamide and L-arginine added to the molecule, in order to achieve a faster absorption through the subcutaneous cellular tissue. Pharmacokinetic and pharmacodynamic studies showed a left-shifted mean serum concentration-time profile compared to the conventional formulation. Its efficacy profile is highlighted in terms of early postprandial glycemic control. In addition, fast acting aspart insulin allows a more flexible treatment schedule, as it may be administrated at mealtime, immediately before or up to 20 minutes after; this schedule represents an advantage regarding quality of life in patients with diabetes treated with prandial insulin, especially in populations such as children, pregnant women or elderly subjects. The safety and tolerability profiles are comparable to conventional aspart insulin.

Insulinización en la diabetes mellitus tipo 2: Alternativas de intensificación / Insulinization in type 2 diabetes mellitus. Intensification options

La diabetes mellitus se asocia con complicaciones vasculares y elevadas tasas de morbimortalidad. La terapia oportuna con insulina y su intensificación cuando es necesaria, representan estrategias apropiadas para evitar o retardar la aparición de dichas complicaciones. Sin embargo, la incidencia de hipoglucemia y las dificultades en la adherencia al tratamiento representan barreras para alcanzar el éxito terapéutico. Las nuevas combinaciones de análogos de insulina constituyen tratamientos que presentarían ventajas farmacocinéticas y farmacodinámicas, logrando beneficios clínicos tales como un mejor control metabólico, la disminución de eventos hipoglucémicos y, por su simplicidad, potencialmente una mayor adherencia al tratamiento.

Diabetes mellitus is associated with vascular complications and high rates of morbidity and mortality. Timely insulin therapy, intensified when necessary, represent appropriate measures to prevent or delay the onset of complications. However, the incidence of hypoglycemia and difficulties in treatment adherence represent barriers to achieve therapeutic success. Premixes analogs and, specially, combinations of insulin analogues are associated with pharmacokinetic and pharmacodynamic advantages, that translate into clinical benefits such as improved metabolic control, decreased hypoglycemic events and, for their simplicity, potentially greater adherence.

Efficacy and Safety of Biphasic Insulin Aspart 30/70 in Type 2 Diabetes Suboptimally Controlled on Oral Antidiabetic Therapy in Korea: A Multicenter, Open-Label, Single-Arm Study

BACKGROUND: The purpose of this study was to evaluate change in glycosylated hemoglobin (HbA1c), side effects, and quality of life (QOL) after a 16-week treatment period with Biphasic insulin aspart 30/70 (BIasp30) in patients with type 2 diabetes mellitus (T2DM) who had been suboptimally controlled with oral antidiabetic drugs (OADs). METHODS: The study consisted of a 4-week titration period when concurrent OAD(s) were replaced with BIasp30 and followed by a 12-week maintenance period. All patients completed the Diabetes Treatment Satisfaction Questionnaire at the beginning and the end of the trial. Hypoglycemic episodes were recorded by the patient throughout the trial. RESULTS: Sixty patients were included, of whom 55 patients (92%) completed the full 16-week treatment period. Seven-point blood glucose was significantly improved as compared with the baseline, except for the postlunch blood glucose level. HbA1c at the end of period was significantly improved from 9.2% to 8.2% (P<0.001). Eleven percent (n=6) of patients achieved HbA1c values < or =6.5% and 22% (n=12) of patients achieved <7.0%. There were 3.4 episodes/patients-year of minor hypoglycemia and 0.05 episodes/patients-year of major hypoglycemia. QOL showed significant changes only in the acceptability of high blood glucose category (P=0.003). CONCLUSION: Treatment with once or twice daily BIasp30 may be an option for the patients with T2DM suboptimally controlled with OADs in Korea. However, considering the low number of patients achieving the HbA1c target and the high postlunch blood glucose levels, additional management with another modality may be required for optimal control.