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Antiepileptic Drugs: Potassium Channel Activators01:20

Antiepileptic Drugs: Potassium Channel Activators

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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FDA Approved Drugs: Changes to Approved Drugs

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Updated: Jul 5, 2026

Urethral Stricture Induction Followed by Buccal Mucosa Graft Urethroplasty in a Rat Model
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Urethral Stricture Induction Followed by Buccal Mucosa Graft Urethroplasty in a Rat Model

Published on: April 28, 2023

Rifalazil(Kaneka corp).

M Pregnolato

    Idrugs : the Investigational Drugs Journal
    |May 10, 2008
    PubMed
    Summary
    This summary is machine-generated.

    Rifalazil, a novel rifamycin derivative, shows promise in treating tuberculosis and MAC infections. Early trials indicate potent efficacy and a favorable safety profile compared to rifampin.

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    Published on: July 23, 2016

    Area of Science:

    • Pharmacology and Infectious Diseases
    • Drug Development
    • Microbiology

    Background:

    • Rifalazil is a rifamycin derivative developed for Mycobacterium tuberculosis (TB) and Mycobacterium avium complex (MAC) infections.
    • It is undergoing Phase II clinical trials for TB and AIDS-associated MAC infections.
    • PathoGenesis holds exclusive rights for its development and marketing in the US and Mexico.

    Purpose of the Study:

    • To evaluate the efficacy and safety of rifalazil in treating TB and MAC infections.
    • To compare rifalazil in combination regimens with standard treatments.
    • To assess the early bactericidal activity of rifalazil.

    Main Methods:

    • Phase II clinical trial in Brazil with 60 pulmonary TB patients.
    • Four dosing regimens comparing rifalazil plus isoniazid against isoniazid alone or with rifampin over 14 days.
    • Phase I trials in the US for both indications completed in 1996.

    Main Results:

    • Preclinical studies show rifalazil is 30-fold more potent than rifampin against M tuberculosis and MAC.
    • Phase I trials demonstrated a favorable safety profile at low doses, with no side-effects seen with rifampin.
    • Rifalazil exhibits a longer half-life (24h) compared to rifampin (2-3h).

    Conclusions:

    • Rifalazil demonstrates significant preclinical potency and a promising safety profile for TB and MAC treatment.
    • Its longer half-life and improved efficacy suggest potential as a valuable therapeutic agent.
    • Ongoing clinical trials will further elucidate its clinical utility.