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1.
J Vet Intern Med ; 38(4): 2305-2315, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38888250

RESUMO

BACKGROUND: Acid suppressant drugs (ASDs) are commonly used to decrease gastric acid production, but some evidence exists that ASDs exert immunomodulatory effects. Such an effect has not been investigated in dogs for which ASDs are routinely prescribed. HYPOTHESIS: Compared to naïve subjects, dogs treated with ASDs will exhibit differences in leukocyte ratios after treatment. ANIMALS: Fifty-one dogs with mast cell tumors (MCTs). MATERIALS AND METHODS: Dogs with MCT that were either AS naïve or treated with ASDs (i.e., histamine-2-receptor antagonists [H2RA] or proton pump inhibitors [PPI]) were included in this retrospective study. Subjects were categorized into 3 treatment groups (AS naïve, H2RA treated, and PPI treated), and leukocyte ratios (neutrophil:eosinophil, lymphocyte:monocyte, and neutrophil:lymphocyte [NLR]) were calculated before and after treatment. A mixed effects analysis of variance on ranks was used to assess differences in ratios between treatments, between pre- and post-treatment time points, and between pre- and post-time points for each treatment. Concurrent administration of antihistamines, corticosteroids, and chemotherapeutic drugs was assessed as a confounding factor. RESULTS: Famotidine (n = 14/14) and omeprazole (n = 12/12) were the only H2RA and PPI used, respectively. Dogs receiving famotidine had a significant increase in median NLR from pre- to post-treatment (3.429; range, 1.417-15 to 5.631; range, 2.654-92; P < 0.01) compared to PPI treated or AS naïve dogs. No differences existed in chemotherapeutic drug or corticosteroid use between groups. CONCLUSIONS: A significant difference in NLR was identified in famotidine treated dogs compared with omeprazole treated or AS naïve dogs.


Assuntos
Doenças do Cão , Famotidina , Antagonistas dos Receptores H2 da Histamina , Omeprazol , Inibidores da Bomba de Prótons , Animais , Cães , Doenças do Cão/tratamento farmacológico , Estudos Retrospectivos , Famotidina/uso terapêutico , Famotidina/farmacologia , Antagonistas dos Receptores H2 da Histamina/farmacologia , Antagonistas dos Receptores H2 da Histamina/uso terapêutico , Feminino , Masculino , Omeprazol/uso terapêutico , Omeprazol/farmacologia , Inibidores da Bomba de Prótons/uso terapêutico , Inibidores da Bomba de Prótons/farmacologia , Contagem de Leucócitos/veterinária , Mastocitoma/veterinária , Mastocitoma/tratamento farmacológico
2.
Int J Clin Pharmacol Ther ; 62(8): 353-362, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38699974

RESUMO

OBJECTIVE: Visual analog scale (VAS) can be used to evaluate multiple parameters. There have been no reports on the verification of order effects or reproducibility of the VAS method for overall palatability of oral dosage forms. The purpose of this study was to assess the validity of a method for evaluating the palatability of orally disintegrating tablets (ODTs) using a 100-mm VAS. MATERIALS AND METHODS: We conducted clinical trials to evaluate the overall palatability, taste, and scent of 3 ODTs (F1, F2, F3) that contained famotidine (20, 10, and 5 mg, respectively). The study protocol was approved by the Research Ethics Committee of the University of Shizuoka, Japan (No. 21 - 36). To investigate the intergroup reproducibility of the VAS evaluation, 40 participants were divided into three groups, and each group underwent human gustatory sensation test of F1, F2, and F3, performed using a crossover design with 6 different tasting sequences. To evaluate intragroup reproducibility of the VAS evaluation, the participants assessed the same ODTs twice. RESULTS: The VAS scores for overall palatability followed the same order (F3>F2>F1) in all groups. The VAS scores for the overall palatability of F1, F2, and F3 did not significantly differ between the first and second evaluations. The Kruskal-Wallis test indicated a minimal impact of the assessment order on ODT evaluations. We confirm the reliability and reproducibility of the VAS method for evaluating ODT palatability. CONCLUSION: The VAS method for assessing ODT palatability provides accurate information and can contribute to the design and manufacture of patient-friendly pharmaceutical products.


Assuntos
Estudos Cross-Over , Comprimidos , Paladar , Escala Visual Analógica , Humanos , Administração Oral , Reprodutibilidade dos Testes , Masculino , Adulto , Feminino , Famotidina/administração & dosagem , Adulto Jovem
3.
Int J Biol Macromol ; 269(Pt 2): 131964, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38692525

RESUMO

This study aims to identify FDA-approved drugs that can target the kappa-opioid receptor (KOR) for the treatment of demyelinating diseases. Demyelinating diseases are characterized by myelin sheath destruction or formation that results in severe neurological dysfunction. Remission of this disease is largely dependent on the differentiation of oligodendrocyte precursor cells (OPCs) into mature oligodendrocytes (OLGs) in demyelinating lesions. KOR is an important regulatory protein and drug target for the treatment of demyelinating diseases. However, no drug targeting KOR has been developed due to the long clinical trials for drug discovery. Here, a structure-based virtual screening was applied to identify drugs targeting KOR among 1843 drugs of FDA-approved drug libraries, and famotidine was screen out by its high affinity cooperation with KOR as well as the clinical safety. We discovered that famotidine directly promoted OPC maturation and remyelination using the complementary in vitro and in vivo models. Administration of famotidine was not only effectively enhanced CNS myelinogenesis, but also promoted remyelination. Mechanically speaking, famotidine promoted myelinogenesis or remyelination through KOR/STAT3 signaling pathway. In general, our study provided evidence of new clinical applicability of famotidine for the treatment of demyelinating diseases for which there is currently no effective therapy.


Assuntos
Diferenciação Celular , Famotidina , Receptores Opioides kappa , Remielinização , Fator de Transcrição STAT3 , Transdução de Sinais , Animais , Humanos , Camundongos , Diferenciação Celular/efeitos dos fármacos , Sistema Nervoso Central/efeitos dos fármacos , Sistema Nervoso Central/metabolismo , Doenças Desmielinizantes/tratamento farmacológico , Doenças Desmielinizantes/metabolismo , Famotidina/farmacologia , Bainha de Mielina/metabolismo , Bainha de Mielina/efeitos dos fármacos , Células Precursoras de Oligodendrócitos/efeitos dos fármacos , Células Precursoras de Oligodendrócitos/metabolismo , Células Precursoras de Oligodendrócitos/citologia , Oligodendroglia/efeitos dos fármacos , Oligodendroglia/metabolismo , Oligodendroglia/citologia , Receptores Opioides kappa/metabolismo , Remielinização/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Fator de Transcrição STAT3/metabolismo , Feminino , Camundongos Endogâmicos C57BL , Células HEK293
4.
Int J Immunopathol Pharmacol ; 38: 3946320241249429, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38721971

RESUMO

OBJECTIVE: This study investigated the raft-forming suspension of famotidine as an anti-reflux formulation to improve the oral bioavailability of narrow absorption window drugs by enhancing gastric residence time (GRT) and preventing gastro-esophageal reflux disease (GERD). METHOD: Various combinations of raft-forming agents, such as Tragacanth gum (TG), guar gum (GG), and xanthan gum (XG), were evaluated alongside sodium alginate (SA) to develop an effective raft. Preformulation studies and preliminary screening were conducted to identify the most suitable raft-forming agent, and GG was chosen due to its mucilaginous properties. The formulation was optimized using a 32 full factorial design, with the quantities of GG and SA as independent factors and apparent viscosity and in-vitro drug release (%) as dependent factors. The in vivo floating behavior study was performed for optimized and stabilized formulation. RESULTS: Among the tested batches, F6 was selected as the optimized formulation. It exhibited desirable characteristics such as adequate raft weight for extended floating in gastric fluid, improved apparent viscosity, and a significant percentage of drug release at 12 h. A mathematical model was applied to the in-vitro data to gain insights into the drug release mechanism of the formulation. The stability of the suspension was assessed under accelerated conditions, and it demonstrated satisfactory stability. The formulation remains floating in the Rabbit stomach for more than 12 h. CONCLUSION: It concludes that the developed formulation has enhanced bioavailability in the combination of GG and SA. The floating layer of the raft prevents acid reflux, and the famotidine is retained for an extended period of time in the gastric region, preventing excess acid secretion. The developed formulations are effective for stomach ulcers and GERD, with the effect of reducing acid secretion by H2 receptor antagonists.


Assuntos
Sistemas de Liberação de Medicamentos , Famotidina , Galactanos , Famotidina/administração & dosagem , Famotidina/farmacocinética , Animais , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos , Alginatos , Refluxo Gastroesofágico/tratamento farmacológico , Refluxo Gastroesofágico/metabolismo , Disponibilidade Biológica , Mananas/administração & dosagem , Gomas Vegetais , Viscosidade , Masculino , Coelhos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/efeitos dos fármacos , Polissacarídeos Bacterianos , Estabilidade de Medicamentos , Administração Oral
5.
Pak J Pharm Sci ; 37(2): 405-416, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38767108

RESUMO

To develop a new kind of famotidine-resin microcapsule for gastric adhesion sustained release by screening out suitable excipients and designing reasonable prescriptions to improve patient drug activities to achieve the expected therapeutic effect. The famotidine drug resin was prepared using the water bath method with carbomer 934 used as coating material. Microcapsules were prepared using the emulsified solvent coating method and appropriate excipients were used to prepare famotidine sustained release suspension. Pharmacokinetics of the developed microcapsules were studied in the gastrointestinal tract of rats. The self-made sustained-release suspension of famotidine hydrochloride effectively reduced the blood concentration and prolonged the action time. The relative bioavailability of the self-made suspension of the famotidine hydrochloride to the commercially available famotidine hydrochloride was 146.44%, with an average retention time of about 5h longer, which indicated that the new suspension had acceptable adhesion properties. The findings showed that the newly developed famotidine-resin microcapsule increased the bioavailability of the drug with a significant sustained-release property.


Assuntos
Disponibilidade Biológica , Preparações de Ação Retardada , Famotidina , Famotidina/farmacocinética , Famotidina/administração & dosagem , Famotidina/química , Famotidina/farmacologia , Animais , Ratos , Masculino , Excipientes/química , Suspensões , Cápsulas , Liberação Controlada de Fármacos , Resinas Acrílicas/química , Antagonistas dos Receptores H2 da Histamina/farmacocinética , Antagonistas dos Receptores H2 da Histamina/administração & dosagem , Antagonistas dos Receptores H2 da Histamina/farmacologia , Antagonistas dos Receptores H2 da Histamina/química , Adesividade , Composição de Medicamentos , Acrilatos
6.
Pharm Dev Technol ; 29(5): 429-444, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38607310

RESUMO

In this study, a new gastro-floating sustained-release tablet (GFT) with a combination of Etoricoxib (ET) and Famotidine (FM) was successfully developed. GFTs were prepared by using a combination of hydrophilic swellable natural/semi-synthetic polymers as a controlled-release layer. Through a 24 full factorial statistical experimental design, the effects of formulation factors on the release of GFTs were conducted. The ideal floating tablet (FT) comprised konjac-gum (150 mg), guar-gum (26.57 mg), xanthan-gum (54.17 mg), and HPMC-K15-M (69.25 mg). The ideal FT exhibited a high swelling index (SI) (297.7%) and rapid FLT (around 50 s) in 0.1 N HCl as well as controlled release of ET (22.43% in 1 h and 77.47% in 8 h) and FM (24.89% in 1 h and 93.82% in 8 h) with the absence of any drug-excipient interactions. The AUC0∼72 (ng h/mL) of ET and FM in the GFTs were approximately double-fold of the market, respectively. The relative bioavailability was (207.48 ± 12.02% and 208.51 ± 13.11%) compared with commercial tablets. The X-ray imaging showed a promising buoyancy ability for approximately 8 h. These findings revealed the successful preparation of the sustained-release floating tablet with improved dual drug delivery.


Assuntos
Preparações de Ação Retardada , Liberação Controlada de Fármacos , Etoricoxib , Famotidina , Comprimidos , Famotidina/administração & dosagem , Famotidina/farmacocinética , Famotidina/química , Etoricoxib/administração & dosagem , Etoricoxib/farmacocinética , Etoricoxib/química , Animais , Masculino , Coelhos , Excipientes/química , Disponibilidade Biológica
7.
Rev. chil. infectol ; 41(1): 7-19, feb. 2024. ilus, tab
Artigo em Espanhol | LILACS | ID: biblio-1559661

RESUMO

Introducción: El síndrome respiratorio agudo severo coronavirus 2 (SARS-CoV-2), de alta morbimortalidad, carece a la fecha de preparar esta revisión, de una terapia específica altamente eficaz. Famotidina se ha postulado como una opción terapéutica viable, basado en trabajos de cohorte retrospectiva y modelos computacionales guiados por inteligencia artificial. Objetivo: Recopilar la mejor evidencia científica disponible para determinar la efectividad y eficacia de famotidina en el tratamiento de pacientes hospitalizados con COVID-19, para reducir el riesgo de progresión de la enfermedad, intubación, muerte y tiempo de estancia hospitalaria. Material y Métodos: Se realizó una búsqueda en PubMed, EBSCO, Scopus, Web of Science y Cochrane Central, de artículos originales que reporten las variables de interés asociadas al uso de famotidina en pacientes hospitalizados con COVID- 19. Los investigadores independientemente evaluaron y seleccionaron los estudios, se extrajeron los datos expuestos para las asociaciones de interés y se procesaron con el software Revman 5.3. Resultados: En la búsqueda se obtuvo un total de 126 artículos potenciales para la revisión, de los cuales 14 fueron seleccionados para el análisis. En el metaanálisis se incluyeron un total de 47.044 pacientes, de los cuales 6.647 fueron los usuarios de famotidina. El riesgo de intubación se vio reducido en el grupo no expuesto a famotidina, aunque sin significancia estadística, (RR 1,43 IC95% 0,42-4,83), en cuanto a la mortalidad no se evidenció reducción significativa en el grupo de famotidina (RR 0,95 IC 95% 0,70-1,29). Se observó reducción en el tiempo de estancia hospitalaria (DM -1,60 -2,89, -0,31) y finalmente se mostró que no hay presencia de asociación entre el uso de famotidina y el desenlace compuesto de reducción del riesgo de ingreso a UCI, intubación y muerte (RR 1,03 IC 95% 0,46-2,34). Conclusión: Famotidina no presenta efectividad ni eficacia en la reducción de riesgo de intubación o ingreso a UCI ni de mortalidad en pacientes hospitalizados por COVID-19. La eficacia en la reducción de la estancia hospitalaria no es consistente y se necesitan más ensayos clínicos con buena calidad metodológica para definirla.


Background: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), with high morbidity and mortality, lacks, at the time of preparing this review, a highly effective specific therapy. Famotidine has been postulated as a viable therapeutic option, based on retrospective cohort investigations and computational models guided by artificial intelligence. Aim: The objective of this study was to compile the best scientific evidence available to determine the effectiveness and efficacy of famotidine in the treatment of hospitalized patients with COVID-19, to reduce the risk of disease progression, intubation, death, and time to hospital stay. Methods: A search was carried out in PubMed, EBSCO, Scopus, Web of Science, and Central Cochrane, for original articles that report the variables of interest associated with the use of famotidine in hospitalized patients with COVID-19. The investigators independently evaluated and selected the studies, the exposed data for the associations of interest were extracted and processed with Revman 5.3 software. Results: The search yielded a total of 126 potential articles for the review, of which 14 were selected for analysis. A total of 47,044 patients were included in the meta-analysis of which 6,647 were famotidine users. The risk of intubation was reduced in the group not exposed to famotidine, although without statistical significance (RR 1.43 IC95% 0.42 - 4.83), regarding mortality there was no significant reduction in the famotidine group (RR 0.95 IC 95 % 0.70-1.29). A reduction in the length of hospital stay was observed (MD -1.60 -2.89, -0.31) and finally it was shown that there is no association between the use of famotidine and the composite outcome of reduced risk of ICU admission, intubation and death. (RR 1.03 95% CI 0.46-2.34). Conclusion: Famotidine does not show effectiveness or efficacy in reducing the risk of intubation or ICU admission or mortality in patients hospitalized for COVID-19. The efficacy in reducing hospital stay is not consistent and more clinical trials with good methodological quality are needed to define it.


Assuntos
Humanos , Famotidina/uso terapêutico , SARS-CoV-2 , Tratamento Farmacológico da COVID-19 , Risco , COVID-19/mortalidade , Antagonistas dos Receptores H2 da Histamina/uso terapêutico , Hospitalização , Intubação Intratraqueal
8.
Sci Rep ; 14(1): 3661, 2024 02 13.
Artigo em Inglês | MEDLINE | ID: mdl-38351288

RESUMO

A straightforward and efficient spectrum technique was created using Ortho-chloranil as the electron acceptor (-acceptor) in a charge transfer (CT) complex formation reaction to determine the concentration of famotidine (FMD) in solutions. Compared to the double-distilled blank solution, the reaction result detected a definite violet colour at a maximum absorption wavelength of 546 nm, For concentrations range 2-28 µg/ml, the technique demonstrated excellent compliance with Beer-Law and Lambert's, as evidenced by its molar absorptivity of 2159.648 L mol-1 cm-1. Lower detection limits of 0.3024 µg/ml and 1.471 µg/ml, respectively, were discovered. The complexes of famotidine and Ortho-chloranil were found to have a 2:1 stoichiometry. Additionally, the suggested approach effectively estimated famotidine concentrations in pharmaceutical formulations, particularly in tablet form.


Assuntos
Cloranila , Famotidina , Espectrofotometria/métodos , Comprimidos , Formas de Dosagem
9.
Clin Pharmacol Drug Dev ; 13(6): 677-687, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38346861

RESUMO

Cilofexor is a nonsteroidal farnesoid X receptor agonist being developed in combination with firsocostat/semaglutide for the treatment of nonalcoholic steatohepatitis. This phase 1 study evaluated the effects of food and acid-reducing agents (ARAs) on the pharmacokinetics of cilofexor (100- or 30-mg fixed-dose combination with firsocostat) in healthy participants. Cohorts 1 (n = 20, 100 mg) and 2 (n = 30, 30 mg) followed a 3-period, 2-sequence crossover design and evaluated effects of light-fat and high-fat meals. Cohort 3 (n = 30, 100 mg fasting) followed a 2-period, 2-sequence crossover design and evaluated the effects of a 40-mg single dose of famotidine. Cohort 4 (n = 18, 100 mg) followed a 3-period, 2-sequence crossover design and evaluated the effects of a 40-mg once-daily regimen of omeprazole administered under fasting conditions or following a light-fat meal. Administration with light-fat or high-fat meals resulted in no change and an ∼35% reduction in cilofexor AUC, respectively, relative to the fasting conditions. Under fasting conditions, famotidine increased cilofexor AUC by 3.2-fold and Cmax by 6.1-fold, while omeprazole increased cilofexor AUC by 3.1-fold and Cmax by 4.8-fold. With a low-fat meal, omeprazole increased cilofexor exposure to a lesser extent (Cmax 2.5-fold, AUC 2.1-fold) than fasting conditions. This study suggests that caution should be exercised when cilofexor is administered with ARAs under fed conditions; coadministration of cilofexor (100 or 30 mg) with ARAs under fasting conditions is not recommended with the current clinical trial formulations.


Assuntos
Estudos Cross-Over , Interações Alimento-Droga , Receptores Citoplasmáticos e Nucleares , Humanos , Masculino , Receptores Citoplasmáticos e Nucleares/agonistas , Adulto , Feminino , Adulto Jovem , Pessoa de Meia-Idade , Refeições , Famotidina/farmacocinética , Famotidina/administração & dosagem , Jejum/metabolismo , Combinação de Medicamentos , Voluntários Saudáveis , Gorduras na Dieta/administração & dosagem , Área Sob a Curva
10.
Gut Liver ; 18(1): 70-76, 2024 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-37309193

RESUMO

Background/Aims: H2 receptor antagonists (H2RA) have been used to treat gastritis by inhibiting gastric acid. Proton pump inhibitors (PPIs) are more potent acid suppressants than H2RA. However, the efficacy and safety of low-dose PPI for treating gastritis remain unclear. The aim was to investigate the efficacy and safety of low-dose PPI for treating gastritis. Methods: A double-blind, noninferiority, multicenter, phase 3 clinical trial randomly assigned 476 patients with endoscopic erosive gastritis to a group using esomeprazole 10 mg (DW1903) daily and a group using famotidine 20 mg (DW1903R1) daily for 2 weeks. The full-analysis set included 319 patients (DW1903, n=159; DW1903R1, n=160) and the per-protocol set included 298 patients (DW1903, n=147; DW1903R1, n=151). The primary endpoint (erosion improvement rate) and secondary endpoint (erosion and edema cure rates, improvement rates of hemorrhage, erythema, and symptoms) were assessed after the treatment. Adverse events were compared. Results: According to the full-analysis set, the erosion improvement rates in the DW1903 and DW1903R1 groups were 59.8% and 58.8%, respectively. According to the per-protocol analysis, the erosion improvement rates in the DW1903 and DW1903R1 groups were 61.9% and 59.6%, respectively. Secondary endpoints were not significantly different between two groups except that the hemorrhagic improvement rate was higher in DW1903 with statistical tendency. The number of adverse events were not statistically different. Conclusions: DW1903 of a low-dose PPI was not inferior to DW1903R1 of H2RA. Thus, lowdose PPI can be a novel option for treating gastritis (ClinicalTrials.gov Identifier: NCT05163756).


Assuntos
Famotidina , Gastrite , Humanos , Famotidina/uso terapêutico , Antagonistas dos Receptores H2 da Histamina/uso terapêutico , Gastrite/tratamento farmacológico , Inibidores da Bomba de Prótons/uso terapêutico , Método Duplo-Cego
11.
J Oncol Pharm Pract ; 30(2): 412-416, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-37936371

RESUMO

INTRODUCTION: Cetuximab, an IgG1 monoclonal antibody, is utilized in the treatment of metastatic colorectal cancer and squamous cell head and neck cancers. Due to the risk of hypersensitivity reactions, standard premedication with a histamine-1 (H-1) antagonist is recommended prior to administration, however, there is less guidance for premedication strategies to assist with rechallenge after infusion reactions. Here, we describe two cases of successful cetuximab treatment after Grade 2 reactions, in addition to risk factors and proposed premedication strategies for successful rechallenge. CASE REPORT: Two patients who experienced Grade 2 hypersensitivity reactions were both successfully rechallenged with increased premedications 1-2 weeks after initial infusions. The first patient was a 56-year-old male diagnosed with metastatic colorectal cancer receiving cetuximab as part of a clinical trial. The second patient was a 73-year-old male diagnosed with head and neck cancer receiving cetuximab as part of standard of care concurrent with radiation. MANAGEMENT AND OUTCOME: Each patient was rechallenged with an increased premedication strategy including dexamethasone, famotidine, diphenhydramine, and acetaminophen in addition to reducing the infusion rate. Both patients either continued treatment or successfully completed therapy, without any additional infusion-related reactions. DISCUSSION: We aimed to review risk factors related to cetuximab infusion reactions and propose a premedication strategy for rechallenge postreaction. Known risk factors include male sex and the accumulation of cetuximab-specific IgE. These may be mitigated by the addition of increased premedication with dexamethasone and famotidine with concurrent reduced infusion rate.


Assuntos
Neoplasias Colorretais , Hipersensibilidade a Drogas , Neoplasias de Cabeça e Pescoço , Idoso , Humanos , Masculino , Pessoa de Meia-Idade , Cetuximab/efeitos adversos , Neoplasias Colorretais/tratamento farmacológico , Dexametasona , Hipersensibilidade a Drogas/etiologia , Hipersensibilidade a Drogas/prevenção & controle , Hipersensibilidade a Drogas/tratamento farmacológico , Famotidina/uso terapêutico , Neoplasias de Cabeça e Pescoço/tratamento farmacológico , Antagonistas dos Receptores Histamínicos/uso terapêutico , Pré-Medicação
12.
Br J Haematol ; 204(1): 346-351, 2024 01.
Artigo em Inglês | MEDLINE | ID: mdl-37722599

RESUMO

Plasma histamine levels are increased in patients with sickle cell disease (SCD), potentially promoting endothelial P-selectin expression and vaso-occlusion via histamine type 2 (H2) receptors. We conducted a prospective, non-comparative, single-centre study to determine whether famotidine, a H2 receptor antagonist, reduces P-selectin expression in SCD children. The median plasma P-selectin level was significantly reduced after 29 days of oral famotidine (53.2 ng/mL [IQR: 46.7-63.4] vs. 69.9 ng/mL [IQR: 53.6-84.2], median difference -10.2 ng/mL [IQR: -21.8 to -2.7], p = 0.005) in 28 patients. No effect was observed on other adhesion molecules, inflammation or haemolysis markers, except decreased reticulocyte count. No adverse events deemed related to famotidine were observed. Randomized controlled trials are now needed to assess the efficacy of famotidine in preventing vaso-occlusion in SCD.


Assuntos
Anemia Falciforme , Famotidina , Criança , Humanos , Famotidina/uso terapêutico , Selectina-P/metabolismo , Histamina , Estudos Prospectivos
13.
Ann Pharm Fr ; 82(2): 271-284, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38135035

RESUMO

OBJECTIVE: A simple and efficient drug delivery device was designed, viz. specialized straw comprising of famotidine-loaded fast disintegrating pellets. SIGNIFICANCE: Pediatric dosage forms are designed and developed considering the palatability in children of all ages. This specialized straw was intended for pediatrics presenting with dysphagia or associated symptoms. METHODS: The pellets were formulated using an extruder spheronization technique incorporated with Kyron T-314 as a super disintegrant. These pellets were characterized for their micromeritic properties, disintegration, and in vitro drug release. The specialized straw was evaluated for various parameters like flow rate of water siphoned through the straw and solvation volume. RESULTS: Pellets were found to have excellent flow properties, disintegration time was found to be 25-30s, and dissolution studies showed 96.1% drug release in 45min. In vitro flow rate was determined to simulate sipping action through this specialized straw. The results indicated that water flowing through the hollow straw at the rate of 13.8±1.3 mLs-1, when tested in prefilled specialized straw, 6.3±1.1 mLs-1 flow rate was observed to be sufficient to dissolve the pellets. CONCLUSION: Finally, the fast-disintegrating pellets demonstrated excellent in vitro performance and relative ease of manufacturing as compared to other solid dosage forms. Furthermore, the developed specialized straw can be used as a convenient and attractive drug delivery device for pediatrics.


Assuntos
Celulose , Famotidina , Humanos , Criança , Solubilidade , Implantes de Medicamento , Preparações Farmacêuticas , Água , Tamanho da Partícula
14.
Pak J Pharm Sci ; 36(3): 829-841, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-37580932

RESUMO

Sparfloxacin is a quinolone carboxylic acid derivative that shows activity as an antimicrobial agent, against a wide range of Gram-negative and Gram-positive organisms. It is clinically useful for the treatment of urinary tract infections, respiratory tract infections and gynecological infections. In this study in vitro drug-drug interaction of sparfloxacin has been carried out with famotidine and ranitidine. For these studies a two-component spectrophotometric process has been developed for sparfloxacin assay in the presence of famotidine or ranitidine. The reproducibility of the method is within ±5%. The technique has been applied to the development of sparfloxacin in methanol. The interaction studies of sparfloxacin with ranitidine and famotidine were carried out in methanol and methanol: Water mixtures (30:70, v/v; 50:50, v/v) and the kinetics of sparfloxacin degradation were evaluated in the presence and absence of famotidine and ranitidine. The decrease in the rate of degradation of sparfloxacin in the presence of famotidine or ranitidine, compared to that of sparfloxacin alone, indicated the possibility of interaction between the sparfloxacin and famotidine or ranitidine. The Thin layer chromatography (TLC) of the degraded solution showed the presence of a degradation product of sparfloxacin. The studies show that complexation with famotidine or ranitidine may affect the bioavailability of sparfloxacin.


Assuntos
Famotidina , Ranitidina , Famotidina/análise , Ranitidina/análise , Reprodutibilidade dos Testes , Cinética , Metanol , Antagonistas dos Receptores H2 da Histamina/análise
15.
J Bacteriol ; 205(8): e0018723, 2023 08 24.
Artigo em Inglês | MEDLINE | ID: mdl-37439688

RESUMO

The development of novel antibiotic adjuvants is imminent because of the frequent emergence of resistance in Gram-negative bacteria, which severely restricts the efficiency and longevity of commonly used clinical antibiotics. It is reported that famotidine, a clinical inhibitor of gastric acid secretion, enhances the antibacterial activity of rifamycin antibiotics, especially rifampicin, against Gram-negative bacteria and reverses drug resistance. Studies have shown that famotidine disrupts the cell membrane of Acinetobacter baumannii and inhibits the expression of the outer membrane protein ompA gene, while causing a dissipation of the plasma membrane potential, compensatively upregulating the pH gradient and ultimately increasing the accumulation of reactive oxygen species by leading to increased bacterial mortality. In addition, famotidine also inhibited the efflux pump activity and the biofilm formation of A. baumannii. In the Galleria mellonella and mouse infection models, the combination of famotidine and rifampicin increased the survival rate of infected animals and decreased the bacterial load in mouse organs. In conclusion, famotidine has the potential to be a novel rifampicin adjuvant, providing a new option for the treatment of clinical Gram-negative bacterial infections. IMPORTANCE In this study, famotidine was discovered for the first time to have potential as an antibiotic adjuvant, enhancing the antibacterial activity of rifamycin antibiotics against A. baumannii and overcoming the limitations of drug therapy. With the discovery of novel applications for the guanidine-containing medication famotidine, the viability of screening prospective antibiotic adjuvants from guanidine-based molecules was further explored. In addition, famotidine exerts activity by affecting the OmpA protein of the cell membrane, indicating that this protein might be used as a therapeutic drug target to treat A. baumannii infections.


Assuntos
Acinetobacter baumannii , Rifampina , Animais , Camundongos , Rifampina/farmacologia , Acinetobacter baumannii/metabolismo , Famotidina/metabolismo , Estudos Prospectivos , Antibacterianos/metabolismo , Modelos Animais de Doenças , Testes de Sensibilidade Microbiana , Farmacorresistência Bacteriana Múltipla
16.
J Chromatogr Sci ; 61(9): 807-813, 2023 Nov 05.
Artigo em Inglês | MEDLINE | ID: mdl-37415425

RESUMO

A method has been designed based on gas chromatography with flame ionization detection (FID) for the separation and analyses of ranitidine, famotidine and metformin after pre-column derivatization with trifluoroacetylacetone and ethyl chloroformate. DB-1 (30 m × 0.32 mm id) column with film thickness 0.25 µm was used for the separation at an initial temperature of column was 100°C for 2 min, and ramping at 20°C/min up to 250°C, with a hold time of 3 min. The rate of nitrogen flow was 2.5 mL/min and FID was used for detection. Complete separation was obtained between all the three drugs including excess of derivatization reagents. Linear calibration curves and detection limits were obtained in the ranges 0.1-30 µg/mL and 0.011-0.015 µg/mL. The procedure was repeatable in terms of peak heights/peak areas and retention time (n = 5) for derivatization, quantitation and separation with relative standard deviations (RSDs) within 2.0-3.0%. The approach was examined for the analyses of drug products and serum after the intake of the drugs by healthy volunteers, and recoveries were obtained within 95-98% with RSDs 2.4-3.1%.


Assuntos
Famotidina , Metformina , Humanos , Ranitidina , Cromatografia Gasosa/métodos , Preparações Farmacêuticas
18.
Sci Total Environ ; 900: 165886, 2023 Nov 20.
Artigo em Inglês | MEDLINE | ID: mdl-37524191

RESUMO

This study tracked five pharmaceutically active compounds (PhACs) in Mexico City's sewage, namely, famotidine, indomethacin, dexamethasone, azithromycin, and ivermectin, which were used to treat COVID-19. The monitoring campaign was carried out over 30 months (May 2020 to November 2022), covering the five COVID-19 waves in Mexico. In the Central Emitter, the main sewage outflow, famotidine displayed levels of 132.57 ± 28.16 ng L-1 (range from < LOQ to 189.1 ng L-1), followed by indomethacin (average 672.46 ± 116.4 ng L-1, range from 516.7 to 945.2 ng L-1), dexamethasone (average 610.4 ± 225.7 ng L-1, range from 233.4 to 1044.5 ng L-1), azithromycin (average 4436.2 ± 903.6 ng L-1, range from 2873.7 to 5819.6 ng L-1), and ivermectin (average 3413.3 ± 1244.6 ng L-1, range from 1219.8 to 4622.4 ng L-1). The concentrations of dexamethasone, azithromycin and ivermectin were higher in sewage from a temporary COVID-19 care unit, by a factor of 3.48, 3.52 and 2.55, respectively, compared with those found in municipal wastewater. In the effluent of the Atotonilco Wastewater Treatment Plant (AWWTP), which treats near 60 % of the Mexico City's sewage, famotidine was absent, while concentrations of indomethacin, dexamethasone, azithromycin and ivermectin were 78.2 %, 76.7 %, 74.4 %, and 88.1 % lower than those in the influent, respectively. The occurrence of PhACs in treated and untreated wastewater resulted in medium to high environmental risk since Mexico City's wastewater is reused for irrigation in the Mezquital Valley. There, PhACs were found in irrigation canals at lower levels than those observed in Mexico City throughout the monitoring. On the other hand, famotidine, indomethacin, and dexamethasone were not found in surface water resulting from the infiltration of wastewater through soil in Mezquital Valley, while azithromycin and ivermectin sporadically appeared in surface water samples collected through 2021. Using an optimized risk assessment based on a semi-probabilistic approach, the PhACs were prioritized as ivermectin > azithromycin > dexamethasone > famotidine > indomethacin.


Assuntos
COVID-19 , Poluentes Químicos da Água , Humanos , Águas Residuárias , Esgotos , Vigilância Epidemiológica Baseada em Águas Residuárias , Monitoramento Ambiental , México/epidemiologia , Azitromicina , Famotidina , Ivermectina , Pandemias , Poluentes Químicos da Água/análise , COVID-19/epidemiologia , Medição de Risco , Preparações Farmacêuticas , Dexametasona
19.
Int J Clin Pharmacol Ther ; 61(9): 377-385, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37382329

RESUMO

OBJECTIVE: Famotidine, an H2 receptor antagonist (H2RA), is mainly prescribed to alleviate the early symptoms of gastritis. Our aim was to explore the possibilities of low-dose esomeprazole as a treatment of gastritis as well as the pharmacodynamic (PD) properties of esomeprazole and famotidine. MATERIALS AND METHODS: A randomized, multiple-dose, 6-sequence, 3-period crossover study was conducted with a 7-day washout between periods. For each period, the subjects were administered one dose of esomeprazole 10 mg or famotidine 20 mg or esomeprazole 20 mg each day. To evaluate the PDs, the 24-hour gastric pH was recorded after single and multiple doses. The mean percentage of time during which the gastric pH was above 4 was evaluated for PD assessment. To confirm the pharmacokinetic (PK) characteristics of esomeprazole, blood was collected for up to 24 hours after multiple doses. RESULTS: 26 subjects completed the study. Following the multiple doses of esomeprazole 10 mg, esomeprazole 20 mg, and famotidine 20 mg, the mean percentages of time during which the gastric pH was above 4 over the course of 24 hour were 35.77 ± 19.56%, 53.75 ± 20.55%, and 24.48 ± 17.36%, respectively. After multiple doses, the time of peak plasma concentration at steady state (tmax,ss) was 1.00 and 1.25 hours for 10 and 20 mg of esomeprazole, respectively. The geometric mean ratio and its 90% confidence interval of area under the plasma drug concentration-time curve in steady state (AUCT,ss) and maximum concentration of drug in plasma in steady state (Cmax,ss) for esomeprazole 10 mg compared to 20 mg were 0.3654 (0.3381 - 0.3948) and 0.5066 (0.4601 - 0.5579), respectively. CONCLUSION: The PD parameters of esomeprazole 10 mg were comparable to those of famotidine after multiple doses. These findings provide support for further evaluating the use of 10 mg of esomeprazole as a treatment option for gastritis.


Assuntos
Esomeprazol , Gastrite , Humanos , Esomeprazol/farmacocinética , Famotidina/farmacologia , Voluntários Saudáveis , Estudos Cross-Over , Gastrite/diagnóstico , Gastrite/tratamento farmacológico
20.
Exp Anim ; 72(4): 505-512, 2023 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-37316263

RESUMO

Felodipine is a calcium channel blocker with antioxidant and anti-inflammatory properties. Researchers have stated that oxidative stress and inflammation also play a role in the pathophysiology of gastric ulcers caused by nonsteroidal anti-inflammatory drugs. The aim of this study was to investigate the antiulcer effect of felodipine on indomethacin-induced gastric ulcers in Wistar rats and compare it with that of famotidine. The antiulcer activities of felodipine (5 mg/kg) and famotidine were investigated biochemically and macroscopically in animals treated with felodipine (5 mg/kg) and famotidine in combination with indomethacin. The results were compared with those of the healthy control group and the group administered indomethacin alone. It was observed that felodipine suppressed the indomethacin-induced malondialdehyde increase (P<0.001); reduced the decrease in total glutathione amount (P<0.001), reduced the decrease superoxide dismutase (P<0.001), and catalase activities (P<0.001); and significantly inhibited ulcers (P<0.001) at the tested dose compared with indomethacin alone. Felodipine at a dose of 5 mg/kg reduced the indomethacin-induced decrease in cyclooxygenase-1 activity (P<0.001) but did not cause a significant reduction in the decrease in cyclooxygenase-2 activity. The antiulcer efficacy of felodipine was demonstrated in this experimental model. These data suggest that felodipine may be useful in the treatment of nonsteroidal anti-inflammatory drug-induced gastric injury.


Assuntos
Indometacina , Úlcera Gástrica , Ratos , Animais , Indometacina/efeitos adversos , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/prevenção & controle , Famotidina/efeitos adversos , Felodipino/efeitos adversos , Ratos Wistar , Anti-Inflamatórios não Esteroides/efeitos adversos , Antioxidantes/farmacologia
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