Promethazine

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Justin J Kavanagh - One of the best experts on this subject based on the ideXlab platform.

  • central cholinergic pathway involvement in the regulation of pupil diameter blink rate and cognitive function
    Neuroscience, 2016
    Co-Authors: Preshanta Naicker, Shailendra Anoopkumardukie, Gary D Grant, David L Neumann, Justin J Kavanagh
    Abstract:

    Anticholinergic medications can exert their effects by acting on muscarinic receptors, which mediates the function of acetylcholine in the central nervous system. Acetylcholine plays a number of roles, particularly in regard to the control of muscle activity and normal cognitive functioning. Eighteen subjects were recruited into the human, double-blind, placebo-controlled, four-way crossover study. Pupil diameter and blink rate were assessed at rest while eye tracking technology recorded eye characteristics. Thereafter a cognitive task was performed, where pupil size and blink rate were once again measured. Assessments were performed pre-ingestion, 0.5 h and 2 h following the ingestion of a strong centrally acting anticholinergic (Promethazine hydrochloride), a moderate centrally acting anticholinergic (hyoscine hydrobromide), an anticholinergic devoid of central effects (hyoscine butylbromide) and placebo. At rest, hyoscine hydrobromide was the only medication to increase pupil diameter and no drug intervention influenced blink rate. During performance of the cognitive task, hyoscine hydrobromide increased pupil diameter and Promethazine increased blink rate. Promethazine was the only medication to influence the modified attention network test (ANT) by increasing the conflict effect and grand mean reaction time (RT). Pupil diameter and blink rate were both influenced by the central anticholinergics during performance of the cognitive test, thus highlighting the importance of central cholinergic pathways in the control of pupil diameter and blink rate. The collective effects of central anticholinergics on the modified ANT and on pupil diameter and blink rate during its performance, conveys the importance of central cholinergic pathways in cognitive function.

Pedro L S Pinto - One of the best experts on this subject based on the ideXlab platform.

  • Promethazine exhibits antiparasitic properties in vitro and reduces worm burden egg production hepatomegaly and splenomegaly in a schistosomiasis animal model
    Antimicrobial Agents and Chemotherapy, 2019
    Co-Authors: Daniel B Roquini, Ramon M Cogo, Ana C Mengarda, Susana F Mazloum, Cristiane S Morais, Rogerio P Xavier, M C Salvadori, F S Teixeira, Luiz E Ferreira, Pedro L S Pinto
    Abstract:

    : The treatment and control of schistosomiasis, a neglected disease that affects more than 200 million people worldwide, rely on the use of a single drug, praziquantel. A vaccine has yet to be developed and since new drug design and development is a lengthy and costly process, drug repurposing is a promising strategy. In this study, the efficacy of Promethazine, a first-generation antihistamine, was evaluated against Schistosoma mansoniex vivo and in a murine model of schistosomiasis. In vitro assays demonstrated that Promethazine affected parasite motility, viability, and it induced severe tegumental damage in schistosomes. The LC50 of the drug was 5.84 μM. Similar to Promethazine, schistosomes incubated with atropine, a classical anticholinergic drug, displayed reduced motor activity. In an animal model, Promethazine treatment was introduced at an oral dose of 100 mg/kg for five successive days at different intervals from the time of infection, for the evaluation of the stage-specific susceptibility (pre-patent and patent infections). Various parasitological criteria indicated the in vivo antischistosomal effects of Promethazine: there were significant reductions in worm burden, egg production, and hepato- and splenomegaly. The highest worm burden reduction was achieved with Promethazine in patent infections (> 90%). Taken together, considering the importance of the repositioning of drugs in infectious diseases, especially those related to poverty, our data revealed the possibility of Promethazine repositioning as an antischistosomal agent.

  • Promethazine exhibits antiparasitic properties in vitro and reduces worm burden, egg production, hepato-, and splenomegaly in a schistosomiasis animal model.
    Antimicrobial agents and chemotherapy, 2019
    Co-Authors: Daniel B Roquini, Ramon M Cogo, Ana C Mengarda, Susana F Mazloum, Cristiane S Morais, Luiz E Ferreira, R. Xavier, Maria Cecília Barbosa Da Silveira Salvadori, Fernanda De Sá Teixeira, Pedro L S Pinto
    Abstract:

    The treatment and control of schistosomiasis, a neglected disease that affects more than 200 million people worldwide, rely on the use of a single drug, praziquantel. A vaccine has yet to be developed and since new drug design and development is a lengthy and costly process, drug repurposing is a promising strategy. In this study, the efficacy of Promethazine, a first-generation antihistamine, was evaluated against Schistosoma mansoni ex vivo and in a murine model of schistosomiasis. In vitro assays demonstrated that Promethazine affected parasite motility, viability, and it induced severe tegumental damage in schistosomes. The LC50 of the drug was 5.84 μM. Similar to Promethazine, schistosomes incubated with atropine, a classical anticholinergic drug, displayed reduced motor activity. In an animal model, Promethazine treatment was introduced at an oral dose of 100 mg/kg for five successive days at different intervals from the time of infection, for the evaluation of the stage-specific susceptibility (pre-patent and patent infections). Various parasitological criteria indicated the in vivo antischistosomal effects of Promethazine: there were significant reductions in worm burden, egg production, and hepato- and splenomegaly. The highest worm burden reduction was achieved with Promethazine in patent infections (> 90%). Taken together, considering the importance of the repositioning of drugs in infectious diseases, especially those related to poverty, our data revealed the possibility of Promethazine repositioning as an antischistosomal agent.

Preshanta Naicker - One of the best experts on this subject based on the ideXlab platform.

  • central cholinergic pathway involvement in the regulation of pupil diameter blink rate and cognitive function
    Neuroscience, 2016
    Co-Authors: Preshanta Naicker, Shailendra Anoopkumardukie, Gary D Grant, David L Neumann, Justin J Kavanagh
    Abstract:

    Anticholinergic medications can exert their effects by acting on muscarinic receptors, which mediates the function of acetylcholine in the central nervous system. Acetylcholine plays a number of roles, particularly in regard to the control of muscle activity and normal cognitive functioning. Eighteen subjects were recruited into the human, double-blind, placebo-controlled, four-way crossover study. Pupil diameter and blink rate were assessed at rest while eye tracking technology recorded eye characteristics. Thereafter a cognitive task was performed, where pupil size and blink rate were once again measured. Assessments were performed pre-ingestion, 0.5 h and 2 h following the ingestion of a strong centrally acting anticholinergic (Promethazine hydrochloride), a moderate centrally acting anticholinergic (hyoscine hydrobromide), an anticholinergic devoid of central effects (hyoscine butylbromide) and placebo. At rest, hyoscine hydrobromide was the only medication to increase pupil diameter and no drug intervention influenced blink rate. During performance of the cognitive task, hyoscine hydrobromide increased pupil diameter and Promethazine increased blink rate. Promethazine was the only medication to influence the modified attention network test (ANT) by increasing the conflict effect and grand mean reaction time (RT). Pupil diameter and blink rate were both influenced by the central anticholinergics during performance of the cognitive test, thus highlighting the importance of central cholinergic pathways in the control of pupil diameter and blink rate. The collective effects of central anticholinergics on the modified ANT and on pupil diameter and blink rate during its performance, conveys the importance of central cholinergic pathways in cognitive function.

Daniel B Roquini - One of the best experts on this subject based on the ideXlab platform.

  • Promethazine exhibits antiparasitic properties in vitro and reduces worm burden egg production hepatomegaly and splenomegaly in a schistosomiasis animal model
    Antimicrobial Agents and Chemotherapy, 2019
    Co-Authors: Daniel B Roquini, Ramon M Cogo, Ana C Mengarda, Susana F Mazloum, Cristiane S Morais, Rogerio P Xavier, M C Salvadori, F S Teixeira, Luiz E Ferreira, Pedro L S Pinto
    Abstract:

    : The treatment and control of schistosomiasis, a neglected disease that affects more than 200 million people worldwide, rely on the use of a single drug, praziquantel. A vaccine has yet to be developed and since new drug design and development is a lengthy and costly process, drug repurposing is a promising strategy. In this study, the efficacy of Promethazine, a first-generation antihistamine, was evaluated against Schistosoma mansoniex vivo and in a murine model of schistosomiasis. In vitro assays demonstrated that Promethazine affected parasite motility, viability, and it induced severe tegumental damage in schistosomes. The LC50 of the drug was 5.84 μM. Similar to Promethazine, schistosomes incubated with atropine, a classical anticholinergic drug, displayed reduced motor activity. In an animal model, Promethazine treatment was introduced at an oral dose of 100 mg/kg for five successive days at different intervals from the time of infection, for the evaluation of the stage-specific susceptibility (pre-patent and patent infections). Various parasitological criteria indicated the in vivo antischistosomal effects of Promethazine: there were significant reductions in worm burden, egg production, and hepato- and splenomegaly. The highest worm burden reduction was achieved with Promethazine in patent infections (> 90%). Taken together, considering the importance of the repositioning of drugs in infectious diseases, especially those related to poverty, our data revealed the possibility of Promethazine repositioning as an antischistosomal agent.

  • Promethazine exhibits antiparasitic properties in vitro and reduces worm burden, egg production, hepato-, and splenomegaly in a schistosomiasis animal model.
    Antimicrobial agents and chemotherapy, 2019
    Co-Authors: Daniel B Roquini, Ramon M Cogo, Ana C Mengarda, Susana F Mazloum, Cristiane S Morais, Luiz E Ferreira, R. Xavier, Maria Cecília Barbosa Da Silveira Salvadori, Fernanda De Sá Teixeira, Pedro L S Pinto
    Abstract:

    The treatment and control of schistosomiasis, a neglected disease that affects more than 200 million people worldwide, rely on the use of a single drug, praziquantel. A vaccine has yet to be developed and since new drug design and development is a lengthy and costly process, drug repurposing is a promising strategy. In this study, the efficacy of Promethazine, a first-generation antihistamine, was evaluated against Schistosoma mansoni ex vivo and in a murine model of schistosomiasis. In vitro assays demonstrated that Promethazine affected parasite motility, viability, and it induced severe tegumental damage in schistosomes. The LC50 of the drug was 5.84 μM. Similar to Promethazine, schistosomes incubated with atropine, a classical anticholinergic drug, displayed reduced motor activity. In an animal model, Promethazine treatment was introduced at an oral dose of 100 mg/kg for five successive days at different intervals from the time of infection, for the evaluation of the stage-specific susceptibility (pre-patent and patent infections). Various parasitological criteria indicated the in vivo antischistosomal effects of Promethazine: there were significant reductions in worm burden, egg production, and hepato- and splenomegaly. The highest worm burden reduction was achieved with Promethazine in patent infections (> 90%). Taken together, considering the importance of the repositioning of drugs in infectious diseases, especially those related to poverty, our data revealed the possibility of Promethazine repositioning as an antischistosomal agent.

David L Neumann - One of the best experts on this subject based on the ideXlab platform.

  • central cholinergic pathway involvement in the regulation of pupil diameter blink rate and cognitive function
    Neuroscience, 2016
    Co-Authors: Preshanta Naicker, Shailendra Anoopkumardukie, Gary D Grant, David L Neumann, Justin J Kavanagh
    Abstract:

    Anticholinergic medications can exert their effects by acting on muscarinic receptors, which mediates the function of acetylcholine in the central nervous system. Acetylcholine plays a number of roles, particularly in regard to the control of muscle activity and normal cognitive functioning. Eighteen subjects were recruited into the human, double-blind, placebo-controlled, four-way crossover study. Pupil diameter and blink rate were assessed at rest while eye tracking technology recorded eye characteristics. Thereafter a cognitive task was performed, where pupil size and blink rate were once again measured. Assessments were performed pre-ingestion, 0.5 h and 2 h following the ingestion of a strong centrally acting anticholinergic (Promethazine hydrochloride), a moderate centrally acting anticholinergic (hyoscine hydrobromide), an anticholinergic devoid of central effects (hyoscine butylbromide) and placebo. At rest, hyoscine hydrobromide was the only medication to increase pupil diameter and no drug intervention influenced blink rate. During performance of the cognitive task, hyoscine hydrobromide increased pupil diameter and Promethazine increased blink rate. Promethazine was the only medication to influence the modified attention network test (ANT) by increasing the conflict effect and grand mean reaction time (RT). Pupil diameter and blink rate were both influenced by the central anticholinergics during performance of the cognitive test, thus highlighting the importance of central cholinergic pathways in the control of pupil diameter and blink rate. The collective effects of central anticholinergics on the modified ANT and on pupil diameter and blink rate during its performance, conveys the importance of central cholinergic pathways in cognitive function.