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Antiepileptic Drugs: Potassium Channel Activators01:20

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Ezocgabine or retigabine, an antiepileptic drug of remarkable efficacy, has revolutionized the management of seizures. It is a potassium channel activator, explicitly targeting the family of Q subtype potassium channels. It enhances the transmembrane potassium currents, regulating neuronal excitability. This action stabilizes the resting membrane potential, a pivotal factor in mitigating the hyperexcitability that characterizes epilepsy.
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Thiazide diuretics are sulfonamide derivatives featuring a benzothiadiazine ring system in their molecular structure. Based on this structure, thiazide diuretics can be categorized into two groups: thiazide-type and thiazide-like diuretics. Thiazide-type diuretics, including hydrochlorothiazide and chlorothiazide, consist of a benzothiadiazine backbone with an attached sulfonamide group. Thiazide-like diuretics, such as chlorthalidone and indapamide, lack the thiazide ring but demonstrate...
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Serotonin, a crucial neurotransmitter synthesized by enterochromaffin cells, plays a cardinal role in regulating gastrointestinal (GI) motility. With over 90% of the body's total serotonin in the GI tract, its influence on digestive processes is profound. Serotonin is swiftly released upon various stimuli, such as food boluses or certain drugs, triggering intrinsic sensory neurons in the myenteric plexus and extrinsic vagal and spinal sensory neurons. This leads to the activation of the...
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Antiepileptic Drugs: Glutamate Antagonists01:14

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Glutamate is a fundamental neurotransmitter in the central nervous system, playing a vital role in neuronal communication and various cognitive processes. Glutamate stands as the principal excitatory neurotransmitter in the brain. Its presence is crucial for the communication between neurons, underpinning essential processes such as synaptic transmission, neuronal excitability, and plasticity. These functions are vital for higher-order cognitive processes, including learning and memory. The...
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Sedatives and hypnotics encompass a wide range of substances, each with its unique mechanism of action, uses, and potential adverse effects.
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Niclosamide: A career builder.

David Needham1

  • 1Department of Mechanical Engineering and Material Science, Duke University, Durham, NC 27708, USA; Translational Therapeutics, School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, UK.

Journal of Controlled Release : Official Journal of the Controlled Release Society
|August 6, 2023
PubMed
Summary
This summary is machine-generated.

Niclosamide, a protonophore drug, shows broad-spectrum potential against various diseases including cancer and viral infections. Further research and formulation development are crucial for its clinical application.

Keywords:
Carrier-free nanomedicinesDrug deliveryNiclosamideProtonophoresViral infectionscancer

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Area of Science:

  • Drug delivery and formulation science.
  • Molecular pharmacology and therapeutics.
  • Translational medicine.

Background:

  • Professor Kinam Park's legacy in drug delivery and clinically effective formulations.
  • Niclosamide as a protonophore targeting cellular membranes.
  • Broad-spectrum therapeutic potential of niclosamide.

Purpose of the Study:

  • To honor Professor Kinam Park's contributions.
  • To explore niclosamide's mechanism and therapeutic applications.
  • To highlight opportunities for next-generation researchers in drug development.

Main Methods:

  • Review of existing literature on niclosamide and proton shunts.
  • Discussion of physicochemical properties and mechanism of action.
  • Presentation of novel carrier-free formulations for cancer and viral infections.

Main Results:

  • Niclosamide demonstrates potential in treating cancer, bacterial and viral infections, and metabolic diseases.
  • Two carrier-free formulations are proposed: niclosamide stearate prodrug for cancer and a nasal spray formulation for respiratory viruses.
  • The study identifies research gaps and proposes future directions for niclosamide development.

Conclusions:

  • Niclosamide is a promising molecule with broad therapeutic potential.
  • Reformulation strategies, such as carrier-free approaches, can enhance its efficacy.
  • Further preclinical and clinical studies are warranted to realize niclosamide's full potential in disease control.