miércoles, 27 de noviembre de 2013

Bupivacaína liposomal/Liposomal bupivacaine

Bupivacaína en liposomas como inyección simple en bloqueos nerviosos periféricos. Estudio de dosis respuesta


Liposomal bupivacaine as a single-injection peripheral nerve block: a dose-response study.
Ilfeld BM, Malhotra N, Furnish TJ, Donohue MC, Madison SJ.
From the Department of Anesthesiology, University of California San Diego, San Diego, California.
Anesth Analg. 2013 Nov;117(5):1248-56. doi: 10.1213/ANE.0b013e31829cc6ae.
Abstract
BACKGROUND:Currently available local anesthetics approved for single-injection peripheral nerve blocks have a maximum duration of <24 hours. A liposomal bupivacaine formulation (EXPAREL, Pacira Pharmaceuticals, Inc., San Diego, CA), releasing bupivacaine over 96 hours, recently gained Food and Drug Administration approval exclusively for wound infiltration but not peripheral nerve blocks. METHODS: Bilateral single-injection femoral nerve blocks were administered in healthy volunteers (n = 14). For each block, liposomal bupivacaine (0-80 mg) was mixed with normal saline to produce 30 mL of study fluid. Each subject received 2 different doses, 1 on each side, applied randomly in a double-masked fashion. The end points included the maximum voluntary isometric contraction (MVIC) of the quadriceps femoris muscle and tolerance to cutaneous electrical current in the femoral nerve distribution. Measurements were performed from baseline until quadriceps MVIC returned to 80% of baseline bilaterally. RESULTS: There were statistically significant dose responses in MVIC (0.09%/mg, SE = 0.03, 95% confidence interval [CI], 0.04-0.14, P = 0.002) and tolerance to cutaneous current (-0.03 mA/mg, SE = 0.01, 95% CI, -0.04 to -0.02, P < 0.001), however, in the opposite direction than expected (the higher the dose, the lower the observed effect). This inverse relationship is biologically implausible and most likely due to the limited sample size and the subjective nature of the measurement instruments. While peak effects occurred within 24 hours after block administration in 75% of cases (95% CI, 43%-93%), block duration usually lasted much longer: for bupivacaine doses >40 mg, tolerance to cutaneous current did not return to within 20% above baseline until after 24 hours in 100% of subjects (95% CI, 56%-100%). MVIC did not consistently return to within 20% of baseline until after 24 hours in 90% of subjects (95% CI, 54%-100%). Motor block duration was not correlated with bupivacaine dose (0.06 hour/mg, SE = 0.14, 95% CI, -0.27 to 0.39, P = 0.707). CONCLUSIONS: The results of this investigation suggest that deposition of a liposomal bupivacaine formulation adjacent to the femoral nerve results in a partial sensory and motor block of >24 hours for the highest doses examined. However, the high variability of block magnitude among subjects and inverse relationship of dose and response magnitude attests to the need for a phase 3 study with a far larger sample size, and that these results should be viewed as suggestive, requiring confirmation in a future trial.
http://journals.lww.com/anesthesia-analgesia/pages/articleviewer.aspx?year=2013&issue=11000&article=00032&type=abstract






Bupivacaína liposomal de liberación prolongada para analgesia postoperatoria

Liposomal extended-release bupivacaine for postsurgical analgesia.

Lambrechts M, O'Brien MJ, Savoie FH, You Z.

Department of Structural and Cellular Biology, Tulane University School of Medicine, New Orleans, Louisiana, USA ; Department of Orthopaedic Surgery and Tulane institute of Sports Medicine, Tulane University School of Medicine, New Orleans, Louisiana, USA.

Patient Prefer Adherence. 2013 Sep 6;7:885-890.

Abstract

When physicians consider which analgesia to use postsurgery, the primary goal is to relieve pain with minimal adverse side effects. Bupivacaine, a commonly used analgesic, has been formulated into an aqueous suspension of multivesicular liposomes that provide long-lasting analgesia for up to 72 hours, while avoiding the adverse side effects of opioids. The increased efficacy of liposomal extended-release bupivacaine, compared tobupivacaine hydrochloride, has promoted its usage in a variety of surgeries including hemorrhoidectomy, bunionectomy, inguinal hernia repair, total knee arthroplasty, and augmentation mammoplasty. However, like other bupivacaine formulations, the liposomal extended-release bupivacaine does have some side effects. In this brief review, we provide an update of the current knowledge in the use of bupivacaine for postsurgical analgesia.

KEYWORDS: analgesia, bupivacaine, efficacy, liposome, patient satisfaction, side effects
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3772762/pdf/ppa-7-885.pdf


Bupivacaína liposomal. Revisión de una nueva formulación de bupivacaína
Liposomal bupivacaine: a review of a new bupivacaine formulation.
Chahar P, Cummings KC 3rd.
Anesthesiology Institute, Cleveland Clinic Foundation, Cleveland, Ohio, USA.
J Pain Res. 2012;5:257-64. doi: 10.2147/JPR.S27894. Epub 2012 Aug 14.
Abstract
Many attempts have been made to increase the duration of local anesthetic action. One avenue of investigation has focused on encapsulating local anesthetics within carrier molecules to increase their residence time at the site of action. This article aims to review the literature surrounding the recently approved formulation of bupivacaine, which consists of bupivacaine loaded in multivesicular liposomes. This preparation increases the duration of local anesthetic action by slow release from the liposome and delays the peak plasma concentration when compared to plain bupivacaineadministration. Liposomal bupivacaine has been approved by the US Food and Drug Administration for local infiltration for pain relief after bunionectomy and hemorrhoidectomy. Studies have shown it to be an effective tool for postoperative pain relief with opioid sparing effects and it has also been found to have an acceptable adverse effect profile. Its kinetics are favorable even in patients with moderate hepatic impairment, and it has been found not to delay wound healing after orthopedic surgery. More studies are needed to establish its safety and efficacy for use via intrathecal, epidural, or perineural routes. In conclusion, liposomal bupivacaine is effective for treating postoperative pain when used via local infiltration when compared to placebo with a prolonged duration of action, predictable kinetics, and an acceptable side effect profile. However, more adequately powered trials are needed to establish its superiority over plain bupivacaine.
KEYWORDS: efficacy, liposomal bupivacaine, pharmacodynamics, pharmacokinetics, postoperative pain, safety

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3442744/pdf/jpr-5-257.pdf




Atentamente
Anestesiología y Medicina del Dolor
www.anestesia-dolor.org

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