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1.
Curr Pain Headache Rep ; 24(3): 6, 2020 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-32002676

RESUMEN

PURPOSE OF REVIEW: Acute postoperative pain reduction is a major target against the opioid crisis. While opioids have traditionally been the mainstay for postoperative analgesia, current practice has focused on a multimodal approach to pain control, including ultrasound-guided blocks with longer acting local anesthetic agents. RECENT FINDINGS: Non-steroidal anti-inflammatory drugs (NSAIDs), such as meloxicam, are an important class of medications utilized to manage pain in the perioperative period. An additional treatment used in perioperative or postoperative pain relief is Exparel, a bupivacaine (sodium channel blocker) liposomal injectable suspension with a 3-4-day duration of action. The long-acting mechanism and formulation of Exparel consistently has demonstrated decreased opioid use and pain scores in patients undergoing many different surgical procedures. A concern is that pH negatively alters the efficacy of bupivacaine, as in cases of inflamed tissue and acidic fluid pH. For this reason, a combination medication with both meloxicam and bupivacaine has been developed, which normalizes pH and has anti-inflammatory and anti-pain conduction properties. Clinical studies demonstrate that this combination agent can be extremely beneficial in treating postoperative pain. This manuscript summarizes the newest developments with regard to liposomal bupivacaine and the non-steroidal meloxicam, their roles in effective treatment of postoperative pain, contraindications, special considerations of using these medications, and future considerations. HTX-011 pairs up a new extended-release formulation of the local anesthetic bupivacaine with meloxicam, a well-established non-steroidal anti-inflammatory drug (NSAID).


Asunto(s)
Anestésicos Locales/administración & dosificación , Antiinflamatorios no Esteroideos/administración & dosificación , Bupivacaína/administración & dosificación , Meloxicam/administración & dosificación , Manejo del Dolor/métodos , Dolor Postoperatorio/tratamiento farmacológico , Preparaciones de Acción Retardada/administración & dosificación , Quimioterapia Combinada/métodos , Humanos , Liposomas
2.
ChemMedChem ; 14(11): 1096-1107, 2019 06 05.
Artículo en Inglés | MEDLINE | ID: mdl-30921497

RESUMEN

Histone deacetylase (HDAC) activity is modulated in vivo by post-translational modifications and formation of multiprotein complexes. Novel chemical tools to study how these factors affect engagement of HDAC isoforms by HDAC inhibitors (HDACi) in cells and tissues are needed. In this study, a synthetic strategy to access chemically diverse photoreactive probes (PRPs) was developed and used to prepare seven novel HDAC PRPs 9-15. The class I HDAC isoform engagement by PRPs was determined in biochemical assays and photolabeling experiments in live SET-2, HepG2, HuH7, and HEK293T cell lines and in mouse liver tissue. Unlike the HDAC protein abundance and biochemical activity against recombinant HDACs, the chemotype of the PRPs and the type of cells were key in defining the engagement of HDAC isoforms in live cells. Our findings suggest that engagement of HDAC isoforms by HDACi in vivo may be substantially modulated in a cell- and tissue-type-dependent manner.


Asunto(s)
Diseño de Fármacos , Colorantes Fluorescentes/farmacología , Inhibidores de Histona Desacetilasas/farmacología , Histona Desacetilasas/metabolismo , Imagen Óptica , Etiquetas de Fotoafinidad/farmacología , Animales , Células Cultivadas , Colorantes Fluorescentes/síntesis química , Colorantes Fluorescentes/química , Inhibidores de Histona Desacetilasas/síntesis química , Inhibidores de Histona Desacetilasas/química , Humanos , Isoenzimas/antagonistas & inhibidores , Isoenzimas/metabolismo , Hígado/diagnóstico por imagen , Ratones , Ratones de la Cepa 129 , Etiquetas de Fotoafinidad/síntesis química , Etiquetas de Fotoafinidad/química
3.
Int J Anal Chem ; 2011: 840178, 2011.
Artículo en Inglés | MEDLINE | ID: mdl-21647288

RESUMEN

A simple spectrofluorometric method has been developed, adapted, and validated for the quantitative estimation of drugs containing α-methylene sulfone/sulfonamide functional groups using N(1)-methylnicotinamide chloride (NMNCl) as fluorogenic agent. The proposed method has been applied successfully to the determination of methyl sulfonyl methane (MSM) (1), tinidazole (2), rofecoxib (3), and nimesulide (4) in pure forms, laboratory-prepared mixtures, pharmaceutical dosage forms, spiked human plasma samples, and in volunteer's blood. The method showed linearity over concentration ranging from 1 to 150 µg/mL, 10 to 1000 ng/mL, 1 to 1800 ng/mL, and 30 to 2100 ng/mL for standard solutions of 1, 2, 3, and 4, respectively, and over concentration ranging from 5 to 150 µg/mL, 10 to 1000 ng/mL, 10 to 1700 ng/mL, and 30 to 2350 ng/mL in spiked human plasma samples of 1, 2, 3, and 4, respectively. The method showed good accuracy, specificity, and precision in both laboratory-prepared mixtures and in spiked human plasma samples. The proposed method is simple, does not need sophisticated instruments, and is suitable for quality control application, bioavailability, and bioequivalency studies. Besides, its detection limits are comparable to other sophisticated chromatographic methods.

5.
Neurologist ; 11(5): 285-93, 2005 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-16148735

RESUMEN

Chronic pain is one of the most common and challenging medical problems facing our society. The specialty of pain medicine has grown steadily in recent years, largely because of the recognition that multiple factors contribute to chronic pain. The practice of pain medicine is multidisciplinary in approach, incorporating modalities from various specialties to ensure the comprehensive evaluation and treatment of the pain patient. The integration of various specialties such as anesthesiology, neurology, neurologic surgery, orthopedic surgery, physical medicine, and psychiatry is essential to treating patients with chronic pain and to establishing continuity of care. Research in the last 30 years has developed a variety of alternatives or adjuncts to opiates for chronic pain, including neuroactive medications, counterstimulation methods, and cognitive-behavioral therapies. Pain medicine specialists have provided leadership in the development of the practice, with the application of a wide verity of central and peripheral nerve blocks, sympathetic and neurolytic blocks, intradiscal procedures, neuromodulation techniques, intrathecal infusion systems, and other technical procedures that are firmly linked to a biomedical model of pain.


Asunto(s)
Manejo del Dolor , Animales , Dolor de Espalda/tratamiento farmacológico , Dolor de Espalda/terapia , Terapia por Estimulación Eléctrica , Humanos , Bloqueo Nervioso , Bloqueo Neuromuscular , Dolor/diagnóstico , Dolor/tratamiento farmacológico , Dolor/patología
6.
Reg Anesth Pain Med ; 28(4): 344-6, 2003.
Artículo en Inglés | MEDLINE | ID: mdl-12945030

RESUMEN

OBJECTIVE: We present a case of intense herpes zoster-related pain and itching in the ophthalmic division of the trigeminal nerve (V1). Successful pain and itch management was achieved after insertion of a high thoracic epidural catheter with a continuous infusion of bupivacaine and clonidine. CASE REPORT: A 73-year-old woman with metastatic malignant melanoma developed acute herpes zoster-related pain and itching unresponsive to conventional oral medications. The patient described severe and frequent attacks of lancinating pain occurring in the dermatomal distribution of the left ophthalmic division of the trigeminal nerve. She also had a disturbing itch in the same distribution as her pain. The patient had significant reduction in the frequency and intensity of the lancinating attacks after placement of a thoracic epidural catheter with continuous infusion of 1 microg/mL clonidine and 0.05% bupivacaine. The itching resolved completely as well. CONCLUSION: High thoracic epidural infusion of bupivacaine and clonidine was beneficial in relieving neuropathic itch in a patient with acute herpes zoster-related pain in the distribution of the trigeminal nerve.


Asunto(s)
Agonistas alfa-Adrenérgicos/uso terapéutico , Analgesia Epidural , Clonidina/uso terapéutico , Herpes Zóster/complicaciones , Dolor Intratable/tratamiento farmacológico , Prurito/tratamiento farmacológico , Agonistas alfa-Adrenérgicos/administración & dosificación , Anciano , Anestésicos Locales/administración & dosificación , Anestésicos Locales/uso terapéutico , Bupivacaína/administración & dosificación , Bupivacaína/uso terapéutico , Clonidina/administración & dosificación , Resistencia a Medicamentos , Femenino , Humanos , Melanoma/complicaciones , Dolor Intratable/etiología , Prurito/etiología , Neuralgia del Trigémino/tratamiento farmacológico , Neuralgia del Trigémino/etiología
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