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C2230, a preferential use- and state-dependent CaV2.2 channel blocker, mitigates pain behaviors across multiple pain models.
J Clin Invest
December 2024
Department of Pharmacology and Therapeutics, College of Pharmacy, University of Florida, Gainesville, United States of America.
Article Synopsis
- - Antagonists like Ziconotide and Gabapentin target CaV2.2 calcium channels to relieve chronic pain, but their clinical use is limited due to issues like narrow therapeutic windows and potential for misuse or side effects.
- - A new compound called C2230 has been identified as a blocker of CaV2.2 channels, showing multiple beneficial effects such as trapping the channel in an inactivated state and specifically targeting pain without affecting other ion channels or motor functions.
- - C2230 effectively reduced pain-like behaviors in various animal models and human neurons, suggesting it could be developed as a new analgesic with a unique binding mechanism that differentiates it from existing treatments.
SPIDOL study protocol for the assessment of intrathecal ziconotide antalgic efficacy for severe refractory neuropathic pain due to spinal cord lesions.
Trials
September 2024
Hospices Civils de Lyon, Lyon, France.
Rationale: Central neuropathic pain resulting from spinal cord injury is notoriously debilitating and difficult to treat with few currently available treatments. A novel molecule with intrathecal administration: Ziconotide has been approved for treatment of refractory neuropathic pain in general. It acts as a presynaptic calcium channel blocker.
View Article and Find Full Text PDFReal-World Prescription Data for Intrathecal Drug Delivery: A Retrospective Analysis in 32,784 Patients.
Neuromodulation
September 2024
Department of Anesthesiology, Critical Care and Pain Medicine, Beth Israel Deaconess Medical Center, Beth Israel Lahey Health, Boston, MA, USA.
Objectives: Currently, there are three monotherapy drugs approved by the United States Food and Drug Administration (FDA) for use in intrathecal drug delivery systems (IDDS): morphine, ziconotide, and baclofen. In practice, use includes alternate drugs, drug combinations, and drug concentrations. There is a paucity of real-world data examining prescription patterns for IDDS.
View Article and Find Full Text PDFNatural pain killers from marine sources: a new frontier in neurosurgical pain management.
Neurosurg Rev
August 2024
Center for Global Health Research, Saveetha Medical College and Hospital, Saveetha Institute of Medical and Technical Sciences (SIMATS), Saveetha University, Thandalam, Chennai, Tamil Nadu, 602105, India.
The development of new analgesics for the management of neurosurgical pain is a great opportunity in marine environments. Particular secondary metabolites with strong biological activity that have developed for defense are produced by marine bioresources. The analgesic potential of marine-derived peptides, alkaloids, terpenes and polyketides-such as discodermolide from marine sponges and ziconotide from cone snail venom-is highlighted in this letter.
View Article and Find Full Text PDFIntrathecal ziconotide for the treatment of chronic pain: a collection of clinical experiences and literature review.
Eur Rev Med Pharmacol Sci
August 2024
Azienda Ospedaliera di Rilievo Nazionale e di Alta Specializzazione (AORN) "S. Anna e S. Sebastiano", Caserta, Italy.
Objective: Despite the wide use of ziconotide in the USA for treating refractory cancer- and noncancer-related pain, this agent is little used in Europe, even if licensed by the European Medicines Agency (EMA). The reason could be attributed to the high, fixed starting dose required for ziconotide, as stated in the EMA Summary of Product Characteristics (SmPC). This dosage recommendation is based on the results of pivotal clinical studies of ziconotide, which utilized aggressive titration schedules.
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