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1.
Sci Rep ; 13(1): 19678, 2023 11 11.
Artigo em Inglês | MEDLINE | ID: mdl-37952008

RESUMO

This work is concerned with exploiting the power of chemometrics in the assay and purity determination of naphazoline HCl (NZ) and pheniramine maleate (PN) in their combined eye drops. Partial least squares (PLS) and artificial neural network (ANN) were the chosen models for that purpose where three selected official impurities, namely; NZ impurity B and PN impurities A and B, were successfully determined. The quantitative determinations of studied components were assessed by percentage recoveries, standard errors of prediction as well as root mean square errors of prediction. The developed models were constructed in the ranges of 5.0-13.0 µg mL-1 for NZ, 10.0-60.0 µg mL-1 for PN, 1.0-5.0 µg mL-1 for NZ impurity B and 2.0-14.0 µg mL-1 for two PN impurities. The proposed models could determine NZ and PN with respective detection limits of 0.447 and 1.750 µg mL-1 for PLS, and 0.494 and 2.093 µg mL-1 for ANN. The two established models were compared favorably with official methods where no significant difference observed.


Assuntos
Nafazolina , Feniramina , Soluções Oftálmicas , Quimiometria , Espectrofotometria/métodos , Análise dos Mínimos Quadrados
2.
Int J Mol Sci ; 24(18)2023 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-37762498

RESUMO

Rhabdomyosarcoma (RMS) is the most common pediatric soft-tissue cancer with a survival rate below 27% for high-risk children despite aggressive multi-modal therapeutic interventions. After decades of research, no targeted therapies are currently available. Therapeutically targeting actin-binding proteins, although promising, has historically been challenging. Recent advances have made this possibility more salient, including our lab's identification of advillin (AVIL), a novel oncogenic actin-binding protein that plays a role in many cytoskeletal functions. AVIL is overexpressed in many RMS cell lines, patient-derived xenograft models, and a cohort of 30 clinical samples of both the alveolar (ARMS) and embryonal (ERMS) subtypes. Overexpression of AVIL in mesenchymal stem cells induces neoplastic transformation both in vitro and in vivo, and reversing overexpression through genetic modulation reverses the transformation. This suggests a critical role of AVIL in RMS tumorigenesis and maintenance. As an actin-binding protein, AVIL would not traditionally be considered a druggable target. This perspective will address the feasibility of targeting differentially expressed actin-binding proteins such as AVIL therapeutically, and how critical cell infrastructure can be damaged in a cancer-specific manner.


Assuntos
Proteínas dos Microfilamentos , Rabdomiossarcoma , Criança , Humanos , Proteínas dos Microfilamentos/genética , Rabdomiossarcoma/genética , Citoesqueleto , Agressão , Transformação Celular Neoplásica , Feniramina
3.
Clin Exp Optom ; 106(5): 498-502, 2023 07.
Artigo em Inglês | MEDLINE | ID: mdl-35815690

RESUMO

CLINICAL RELEVANCE: This study found 0.7% olopatadine (Pataday Once Daily Relief Extra Strength) eye drops to provide better initial comfort than 0.3% pheniramine maleate/0.025% naphazoline hydrochloride (VISINE® Allergy Eye Relief Multi-Action Antihistamine and Redness Reliever) eye drops suggesting that patients may comply better with the Pataday than VISINE. BACKGROUND: To compare the ocular comfort at instillation of Pataday and VISINE allergy eye drops. METHODS: Minimally symptomatic participants were recruited based upon Standard Patient Evaluation of Eye Dryness (SPEED) questionnaire scores (≤3 units); they also had minimal between-eye inter-ocular comfort differences as judged by visual analogue scale scores (VAS; ≤7 units). Baseline comfort was evaluated by eye with a VAS. One drop of Pataday or VISINE was then applied to the right eye with the alternative drop being applied to the left eye. The same VAS evaluated comfort by eye at drop instillation, and then at 30 seconds, 1 minute, and 2 minutes post-instillation. Drop experience was also evaluated with Likert questions. LogMAR visual acuities and bulbar conjunctival redness were evaluated pre- and post-drop instillation. RESULTS: A total of 159 participants were recruited (mean ± SD age = 26.2 ± 7.5). The VAS found that eyes treated with Pataday were significantly more comfortable at instillation than eyes treated with VISINE. Likert questions indicated that participants significantly preferred Pataday drops compared to the VISINE drops at instillation with regards to overall eye comfort, eye stinging, eye burning, and foreign body sensation. There were no between drop differences in visual acuity, though eyes treated with VISINE were less red than eyes treated with Pataday. CONCLUSIONS: Topically applied Pataday drops were more comfortable than VISINE drops.


Assuntos
Conjuntivite Alérgica , Dibenzoxepinas , Humanos , Adolescente , Adulto Jovem , Adulto , Cloridrato de Olopatadina/uso terapêutico , Feniramina/uso terapêutico , Nafazolina/uso terapêutico , Conjuntivite Alérgica/tratamento farmacológico , Soluções Oftálmicas/uso terapêutico , Dibenzoxepinas/uso terapêutico , Método Duplo-Cego
4.
J Biomol Struct Dyn ; 41(6): 2202-2210, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-35098895

RESUMO

Antihistamines and glucocorticoids are commonly used to treat allergy symptoms and the inflammatory conditions. In present study, the in-vitro binding interactions a glucocortikoid, dexamethasone/an antihistamine, pheniramine with TSN (TSN) secreted from pancreas to small intestine for protein digestion were investigated by fluorescence emission spectroscopy (FES), UV-Vis spectroscopy, synchronous fluorescence spectroscopy (SFS), CD spectroscopy, FT-IR and molecular modeling methods. Also, the effect of these drugs on the catalytic activity of trypsin (TSN) was determined. The fluorescence quenching experiments indicated that each drugs quenched the intrinsic fluorescence of TSN with their increased concentrations. The results of SFS and UV-Vis spectra proved the interaction of dexamethasone and pheniramine with TSN. CD spectra showed that the secondary structure of enzyme was altered in the presence of the drugs. All these spectroscopy results were validated and explained by molecular docking and molecular dynamic simulation (MD) studies. The IC50 values were determined as 0.0049 mM and 0.0038 mM for dexamethasone and pheniramine, respectively. So, both drugs have inhibition effect on the catalytic activity of TSN. The results of this study can provide valuable information in the field of pharmacokinetics and pharmacodynamics.Communicated by Ramaswamy H. Sarma.


Assuntos
Simulação de Dinâmica Molecular , Feniramina , Simulação de Acoplamento Molecular , Tripsina/química , Espectroscopia de Infravermelho com Transformada de Fourier , Termodinâmica , Espectrometria de Fluorescência , Dexametasona/farmacologia , Ligação Proteica , Sítios de Ligação , Dicroísmo Circular
5.
Ulus Travma Acil Cerrahi Derg ; 28(12): 1667-1673, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36453778

RESUMO

BACKGROUND: Skeletal muscle ischemia-reperfusion injury (IRI) is a common clinical problem encountered after tourniquet ap-plication or replantation. This study investigated the effect of pheniramine maleate (Ph), which is frequently used in clinical practice to reduce IRI, and compared its efficacy in IRI with N-acetylcysteine (NAC), a molecule that has been shown to be effective in IRI. METHODS: Twenty-eight male Sprague-Dawley rats were randomly divided into four groups (sham, ischemia-reperfusion [IR], IR+Ph, IR+NAC; n=7 rats per group). Ischemia was induced in the lower right extremities of rats for 3 h using a femoral artery clamp and an elastic tourniquet. Ph and NAC were administered intraperitoneally 15 min before ischemia was terminated. At 24 h after reperfusion, levels of thiobarbituric acid reactive substance (TBARS), catalase (CAT), myeloperoxidase (MPO), superoxide dismutase (SOD), polyadenosine diphosphate ribose polymerase (PARP), and neutrophil infiltration were evaluated. Inducible nitric oxide syn-thase (iNOS) density in muscle tissue was evaluated by immunohistochemical methods after 1 week. RESULTS: SOD, MPO, PARP, CAT, and TBARS levels in muscle tissue were significantly lower in the sham group compared with the other groups (p<0.001). All parameters except TBARS were lower in the NAC and Ph groups than in the IR group (p<0.001). Neu-trophil infiltration in the muscle tissue samples from the IR group was significantly increased compared with the NAC and Ph groups (p<0.05). iNOS staining was not observed in the sham and NAC groups. CONCLUSION: Ph is effective at reducing experimental rat skeletal muscle IRI.


Assuntos
Feniramina , Traumatismo por Reperfusão , Masculino , Animais , Ratos , Ratos Sprague-Dawley , Inibidores de Poli(ADP-Ribose) Polimerases , Substâncias Reativas com Ácido Tiobarbitúrico , Traumatismo por Reperfusão/tratamento farmacológico , Acetilcisteína , Superóxido Dismutase , Artéria Femoral , Músculo Esquelético , Óxido Nítrico
6.
Indian J Public Health ; 66(3): 331-333, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36149115

RESUMO

This study explored the profile of HIV positive patients seeking treatment at a tertiary care addiction treatment facility. A retrospective study was done to collet detailed information on clinical characteristics: drug use (type, age of initiation, duration), general medical condition and past treatment history. The study included 138 patients with mean (SD) age 30.2 (8.3) years. Opioid dependence with injecting drug use (IDU) was diagnosed in 97% of the patients. The median age of injecting onset was 24.5 years (IQR 20-31 years). The most frequently injected substances were pheniramine (60.1%) and buprenorphine (59.4%). Past treatment seeking was reported by 57% patients and interestingly they were less likely to present any medical condition (2 =69.611, p < 0.001). Variability in the age of onset of drug use indicates the need for broad based approach to prevent IDU and motivation to seek treatment may lead to better health conditions.


Assuntos
Buprenorfina , Infecções por HIV , Soropositividade para HIV , Transtornos Relacionados ao Uso de Opioides , Abuso de Substâncias por Via Intravenosa , Adulto , Buprenorfina/uso terapêutico , Infecções por HIV/tratamento farmacológico , Infecções por HIV/epidemiologia , Infecções por HIV/prevenção & controle , Humanos , Índia/epidemiologia , Feniramina , Estudos Retrospectivos , Abuso de Substâncias por Via Intravenosa/epidemiologia , Adulto Jovem
7.
J Mol Recognit ; 35(10): e2979, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-35642097

RESUMO

Infections caused by the bacteria Enterococcus faecalis (also known as E. faecalis) are common in hospitals. This bacterium is resistant to a wide range of medicines and causes a variety of nosocomial infections. An increase in the number of infections caused by multidrug-resistant (MDR) bacteria is causing substantial economic and health issues around the world. Consequently, new therapeutic techniques to tackle the growing threat of E. faecalis infections must be developed as soon as possible. In this regard, we have targeted a protein that is regarded to be critical for the survival of bacteria in this experiment. Homoserine kinase (HSK) is a threonine metabolism enzyme that belongs to the GHMP kinase superfamily. It is a crucial enzyme in threonine metabolism. This enzyme is responsible for a critical step in the threonine biosynthesis pathway. Given the important function that E. faecalis Homoserine Kinase (ESK) plays in bacterial metabolism, we report here cloning, expression, purification and structural studies of E. faecalis HSK using homology modelling. In addition, we have reported on the model's molecular docking and Molecular Dynamic Stimulation (MD Stimulation) investigations to validate the results of the docking experiments. The results were promising. In silico investigations came up with the conclusion: pheniramine has good binding affinity for the E. faecalis HSK.


Assuntos
Enterococcus faecalis , Feniramina , Antibacterianos , Enterococcus faecalis/genética , Simulação de Acoplamento Molecular , Feniramina/metabolismo , Fosfotransferases (Aceptor do Grupo Álcool) , Treonina/metabolismo
9.
Asian J Psychiatr ; 71: 103080, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35305452

RESUMO

BACKGROUND: Strict adherence to pharmacological dosage regimens is a prerequisite to the success of most treatments, particularly for patients in drug abuse programs. The compliance of tramadol, an atypical non-scheduled narcotic analgesic, using objective method has not been adequately studied in an Indian setting. AIM: To evaluate the compliance and pattern of drug use among opioid-dependent subjects prescribed tramadol based on urinalysis. METHOD: Fifty male opioid-dependent patients (ICD 10), seeking treatment at a tertiary de-addiction treatment centre of North India on tramadol prescription for atleast past four weeks were included. Self-reported substance use was recorded using semi-structured proforma. Ten ml of urine was collected for the assessment of compliance of tramadol of other substance use (morphine, buprenorphine, dextropropoxyphene, pentazocine, cannabis, benzodiazepines, pheniramine). All these drugs were analyzed using the immunoassay-based Cassette test and Gas Chromatography in human urine. RESULT: Mean age of the participants was 42.8 years and the mean duration of opioid use was 15.9years. The urine specimen of all subjects tested positive for tramadol. Urinalysis revealed benzodiazepines, cannabis, and pheniramine to be the most common substances of use in this population. It was seen that agreement of self-reporting and urine test results was good for morphine (κ = 0.558) and cannabis (κ = 0.312) and was poor for buprenorphine, pentazocine, and pheniramine. CONCLUSION: The study demonstrates the continued use of several illicit or non-prescribed medications in a medication-assisted opioid treatment population. The results affirm the reliability of urinalysis as an adjunct for testing compliance in such a population.


Assuntos
Buprenorfina , Transtornos Relacionados ao Uso de Opioides , Tramadol , Adulto , Analgésicos/uso terapêutico , Analgésicos Opioides/uso terapêutico , Benzodiazepinas , Buprenorfina/uso terapêutico , Estudos Transversais , Humanos , Masculino , Morfina , Transtornos Relacionados ao Uso de Opioides/tratamento farmacológico , Pentazocina , Feniramina , Reprodutibilidade dos Testes , Centros de Atenção Terciária , Tramadol/uso terapêutico , Urinálise
10.
Proc Natl Acad Sci U S A ; 119(24): e2118048119, 2022 06 14.
Artigo em Inglês | MEDLINE | ID: mdl-37146302

RESUMO

Rhabdomyosarcoma (RMS) is one of the most common pediatric soft-tissue cancer. Previously, we discovered a gene fusion, MARS-AVIL formed by chromosomal inversion in RMS. Suspecting that forming a fusion with a housekeeping gene may be one of the mechanisms to dysregulate an oncogene, we investigated AVIL expression and its role in RMS. We first showed that MARS-AVIL translates into an in-frame fusion protein, which is critical for RMS cell tumorigenesis. Besides forming a gene fusion with the housekeeping gene, MARS, the AVIL locus is often amplified, and its RNA and protein expression are overexpressed in the majority of RMSs. Tumors with AVIL dysregulation exhibit evidence of oncogene addiction: Silencing MARS-AVIL in cells harboring the fusion, or silencing AVIL in cells with AVIL overexpression, nearly eradicated the cells in culture, as well as inhibited in vivo xenograft growth in mice. Conversely, gain-of-function manipulations of AVIL led to increased cell growth and migration, enhanced foci formation in mouse fibroblasts, and most importantly transformed mesenchymal stem cells in vitro and in vivo. Mechanistically, AVIL seems to serve as a converging node functioning upstream of two oncogenic pathways, PAX3-FOXO1 and RAS, thus connecting two types of RMS associated with these pathways. Interestingly, AVIL is overexpressed in other sarcoma cells as well, and its expression correlates with clinical outcomes, with higher levels of AVIL expression being associated with worse prognosis. AVIL is a bona fide oncogene in RMS, and RMS cells are addicted to its activity.


Assuntos
Rabdomiossarcoma Alveolar , Rabdomiossarcoma , Humanos , Animais , Camundongos , Fatores de Transcrição Box Pareados/metabolismo , Linhagem Celular Tumoral , Rabdomiossarcoma/genética , Rabdomiossarcoma/patologia , Oncogenes/genética , Feniramina , Proteínas de Fusão Oncogênica/genética , Proteínas de Fusão Oncogênica/metabolismo , Regulação Neoplásica da Expressão Gênica , Rabdomiossarcoma Alveolar/genética , Proteínas dos Microfilamentos/metabolismo
11.
Int J Risk Saf Med ; 33(1): 23-26, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33967060

RESUMO

BACKGROUND: Pheniramine abuse is reported not only in patients with psychiatric disorders but also in the general population. CASE REPORT: We report a case of pheniramine dependence in a patient with obsessive-compulsive disorder. The patient took about 250 mg orally daily and injected about 90 mg every week from the last six months. It reduced his anxiety, was cheaper than his other psychiatric medications, and free of stigma. He had lethargy, headache, uneasiness, anxiety, and poor sleep as withdrawal symptoms. RESULTS: This case highlights the vulnerability of those with psychiatric disorders towards pheniramine abuse. Hence, this report advocates the strict evaluation of over-the-counter drugs for patients with pre-existing psychiatric disorders.


Assuntos
Transtorno Obsessivo-Compulsivo , Síndrome de Abstinência a Substâncias , Ansiedade , Transtornos de Ansiedade/induzido quimicamente , Transtornos de Ansiedade/diagnóstico , Humanos , Transtorno Obsessivo-Compulsivo/diagnóstico , Transtorno Obsessivo-Compulsivo/tratamento farmacológico , Transtorno Obsessivo-Compulsivo/epidemiologia , Feniramina/efeitos adversos
12.
Molecules ; 25(22)2020 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-33182534

RESUMO

The rapid sensing of drug compounds has traditionally relied on antibodies, enzymes and electrochemical reactions. These technologies can frequently produce false positives/negatives and require specific conditions to operate. Akin to antibodies, molecularly imprinted polymers (MIPs) are a more robust synthetic alternative with the ability to bind a target molecule with an affinity comparable to that of its natural counterparts. With this in mind, the research presented in this article introduces a facile MIP-based dye displacement assay for the detection of (±) amphetamine in urine. The selective nature of MIPs coupled with a displaceable dye enables the resulting low-cost assay to rapidly produce a clear visual confirmation of a target's presence, offering huge commercial potential. The following manuscript characterizes the proposed assay, drawing attention to various facets of the sensor design and optimization. To this end, synthesis of a MIP tailored towards amphetamine is described, scrutinizing the composition and selectivity (ibuprofen, naproxen, 2-methoxphenidine, quetiapine) of the reported synthetic receptor. Dye selection for the development of the displacement assay follows, proceeded by optimization of the displacement process by investigating the time taken and the amount of MIP powder required for optimum displacement. An optimized dose-response curve is then presented, introducing (±) amphetamine hydrochloride (0.01-1 mg mL-1) to the engineered sensor and determining the limit of detection (LoD). The research culminates in the assay being used for the analysis of spiked urine samples (amphetamine, ibuprofen, naproxen, 2-methoxphenidine, quetiapine, bupropion, pheniramine, bromopheniramine) and evaluating its potential as a low-cost, rapid and selective method of analysis.


Assuntos
Anfetaminas/urina , Corantes/química , Polímeros Molecularmente Impressos , Polímeros/química , Detecção do Abuso de Substâncias/métodos , Urina/química , Anfetamina/urina , Bromofeniramina/urina , Bupropiona/urina , Relação Dose-Resposta a Droga , Técnicas Eletroquímicas , Reações Falso-Positivas , Humanos , Ibuprofeno/urina , Limite de Detecção , Impressão Molecular , Naproxeno/urina , Feniramina/urina , Piperidinas/urina , Pós , Fumarato de Quetiapina/urina
13.
J Am Chem Soc ; 142(19): 8602-8607, 2020 05 13.
Artigo em Inglês | MEDLINE | ID: mdl-32336088

RESUMO

Here we report the design of an enzyme-inspired metal-organic framework (MOF), 1-OTf-Ir, by installing strong Lewis acid and photoredox sites in engineered mesopores. Al-MOF (1), with mixed 2,2'-bipyridyl-5,5-dicarboxylate (dcbpy) and 1,4-benzenediacrylate (pdac) ligands, was oxidized with ozone and then triflated to generate strongly Lewis acidic Al-OTf sites in the mesopores, followed by the installation of [Ir(ppy)2(dcbpy)]+ (ppy = 2-phenylpyridine) sites to afford 1-OTf-Ir with both Lewis acid and photoredox sites. 1-OTf-Ir effectively catalyzed reductive cross-coupling of N-hydroxyphthalimide esters or aryl bromomethyl ketones with vinyl- or alkynyl-azaarenes to afford new azaarene derivatives. 1-OTf-Ir enabled catalytic synthesis of anticholinergic drugs Pheniramine and Chlorpheniramine.


Assuntos
Compostos Aza/síntese química , Clorfeniramina/síntese química , Antagonistas Colinérgicos/síntese química , Estruturas Metalorgânicas/química , Feniramina/síntese química , Compostos Aza/química , Sítios de Ligação , Catálise , Clorfeniramina/química , Antagonistas Colinérgicos/química , Ácidos de Lewis/química , Ligantes , Estrutura Molecular , Tamanho da Partícula , Feniramina/química , Porosidade , Propriedades de Superfície
14.
Talanta ; 200: 1-8, 2019 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-31036161

RESUMO

In this work, a novel sulfated-ß-cyclodextrin (S-ß-CD) coated stationary phase was prepared for open-tubular capillary electrochromatography (OT-CEC). The capillary was developed by attaching polydopamine/sulfated-ß-cyclodextrin (PDA/S-ß-CD) onto the gold nanoparticles (AuNPs) coated capillary which was pretreated with polydopamine. The results of scanning electron microscopy (SEM) and energy dispersive X-ray analysis spectroscopy (EDS) indicated that polydopamine/sulfated-ß-cyclodextrin was successfully fixed on the gold nanoparticles coated capillary. To evaluate the performance of the prepared open tubular (OT) column, the enantioseparation was carried out by using ten chiral drugs as model analytes. Under the optimal conditions, salbutamol, terbutaline, trantinterol, tulobuterol, clorprenaline, pheniramine, chlorpheniramine, brompheniramine, isoprenaline and tolterodine were baseline separated with the resolution (Rs) values of 3.25, 1.76, 2.51, 1.89, 3.17, 2.17, 1.99, 1.72, 2.01 and 3.20, respectively. Repeatability of the column was studied, with the relative standard deviations for run-to-run, day-to-day and column-to-column lower than 5.7%.


Assuntos
beta-Ciclodextrinas/química , Albuterol/química , Albuterol/isolamento & purificação , Bromofeniramina/química , Bromofeniramina/isolamento & purificação , Eletrocromatografia Capilar , Clorfeniramina/química , Clorfeniramina/isolamento & purificação , Clembuterol/análogos & derivados , Clembuterol/química , Clembuterol/isolamento & purificação , Isoproterenol/análogos & derivados , Isoproterenol/química , Isoproterenol/isolamento & purificação , Tamanho da Partícula , Feniramina/química , Feniramina/isolamento & purificação , Propriedades de Superfície , Terbutalina/análogos & derivados , Terbutalina/química , Terbutalina/isolamento & purificação , Tartarato de Tolterodina/química , Tartarato de Tolterodina/isolamento & purificação
15.
Trop Anim Health Prod ; 51(8): 2127-2137, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31076996

RESUMO

Therapeutic management of contagious caprine pleuroneumonia (CCPP) involves mostly the use of oxytetracycline followed by enrofloxacin and rarely tylosin. In many parts of the world including India, the former antibiotics are commonly available than the latter. Therefore, prolonged use of the same leads to the development of antibiotic resistance and decreased efficacy of drug. Besides, inflammatory and allergic pathogenesis of CCPP envisages combination therapy. In this study, we evaluated the effectiveness of the combination therapy using different antibiotics (oxytetracycyline @ 10: group I, enrofloxacin @ 5 group II, and tylosin: group III, @ 10 mg/kg body weight), along with anti-inflammatory (meloxicam @ 0.5 mg/kg) and anti-allergic (pheneramine maleate @ 1.0 mg/kg) drugs. These drugs were given intramuscularly at the interval of 48 h for four times in three test groups (n = 10) of Pashmina goats, viz. groups I, II, and III, respectively, affected with CCPP. Group IV (n = 10) was kept as healthy control when group V (n = 10) treated with oxytetracycline @ 10 mg/kg alone was used as positive control. Clinical signs, clinical parameters, pro-inflammatory cytokine (tumor necrosis factor alpha (TNF-α)), and oxidative stress indices (total oxidant status (TOS), total antioxidant status (TAS)) were evaluated at hours 0, 48, 96, and 144 of experimental trial. Tylosin-based combination therapy resulted in a rapid and favorable recovery resulting in restoration of normal body temperature (102.46 ± 0.31 °F), respiration rate (16.30 ± 0.79 per minute), and heart rate (89.50 ± 2.63 per minute) compared to the oxytetracycline (102.95 ± 0.13, 21.30 ± 1.12, 86.00 ± 2.33, respectively) and enrofloxacin (102.97 ± 0.19, 21.00 ± 1.25, 90.00 ± 2.58, respectively) treated groups. By hour 144, all the groups showed restoration of clinical parameters of normal health and diminishing signs of CCPP, viz. fever, dyspnea, coughing, nasal discharge, weakness, and pleurodynia. Significant (P ≤ 0.05) decrease in levels of TNF-α and non-significant (P > 0.05) decrease in levels of TOS and an increase in levels of TAS were noted from hour 0 to 144 in all the test groups. Within the groups, no significant (P > 0.05) change was noted in TNF-α, TOS, and TAS levels; however, TNF-α levels were comparatively lower in group III. Hematological parameters did not differ significantly (P > 0.05). From these findings, it can be inferred that tylosin-based combination therapy is relatively better for early, rapid, and safe recovery besides minimizing inflammatory and oxidative cascade in CCPP affected Pashmina goats compared to oxytetracycline- and enrofloxacin-based therapies.


Assuntos
Antibacterianos/uso terapêutico , Doenças das Cabras/tratamento farmacológico , Pleuropneumonia Contagiosa/tratamento farmacológico , Tilosina/uso terapêutico , Animais , Antialérgicos/uso terapêutico , Anti-Inflamatórios não Esteroides/uso terapêutico , Quimioterapia Combinada/veterinária , Enrofloxacina/uso terapêutico , Feminino , Cabras , Índia , Meloxicam/uso terapêutico , Oxitetraciclina/uso terapêutico , Feniramina/uso terapêutico , Pleuropneumonia/veterinária , Pneumonia por Mycoplasma
17.
Res Social Adm Pharm ; 15(8): 943-948, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-30737195

RESUMO

BACKGROUND: There has been a trend in the past five years in Jordan for ophthalmic anticholinergic preparations to be misused or abused. This is done mainly to experience mental altering effects such as mood changes, euphoria or hallucinations. Such products are mostly obtained from community pharmacies without a prescription. OBJECTIVES: This study aimed to observe the requests of ophthalmic preparations in community pharmacies in Amman, Jordan, and evaluating the most popular and frequently requested ophthalmic drops suspected of abuse. Also, it aimed to describe the current methods that Jordanian community pharmacists use to manage such requests. METHODS: A prospective cross-sectional observational study was conducted between November 2016 and January 2017 at sixteen different community pharmacies in Amman. All ophthalmic products requested were observed during this period. RESULTS: A total of 140 ophthalmic product requests for 130 customers were observed. Dry eye was the most common complaint for which the customer requested the medication (n = 30, 23.1%) and direct self-medication (ie-requesting the product by name), was the most frequent method of purchase (n = 63, 48.5%). In 19 cases (14.6%), product requests were suspected to be for non-medical (ie-abuse) purposes. Most of the suspected cases were for Pentolate® (n = 11, 57.9%), whereas 7 were for Prisoline® (36.8%) and 1 for Naphcon-A® (5.3%). The majority of observed cases were for products requested without a prescription (n = 16, 84.2%), and in 12 cases out of which, sale was refused (63.2%). CONCLUSION: More effort and enforcement of pharmacy regulation for safe dispensing is needed to reduce the abuse of ophthalmic products. Educating pharmacists and ophthalmologists would help raise awareness and control the type of drug abuse.


Assuntos
Soluções Oftálmicas/administração & dosagem , Farmácias/estatística & dados numéricos , Transtornos Relacionados ao Uso de Substâncias , Adulto , Compostos de Benzalcônio , Oftalmopatias/tratamento farmacológico , Feminino , Humanos , Jordânia , Masculino , Pessoa de Meia-Idade , Nafazolina , Feniramina , Adulto Jovem
18.
Talanta ; 192: 226-232, 2019 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-30348382

RESUMO

For the aim of simultaneously performing the enantioseparation and determination of the trace enantiomers in plasma samples, enantioseparation by HPLC using five kinds of chiral stationary phases were initially investigated. But unfortunately, enantioseparation could not be detected in reversed mobile phase mode with all the five columns. For this reason, two simple, economical and highly efficient online preconcentration methods, large volume sample stacking and sweeping (LVSS-sweeping) and cation-selective exhaustive injection and sweeping (CSEI-sweeping) both followed by the cyclodextrin modified electrokinetic chromatography (CDEKC) were examined in the present work. Parameters affecting the enantioseparation and enhancement efficiency of these two injection modes were monitored in detail, and migration order of the two enantiomers was identified by circular dichroism (CD) and HPLC. Upon optimization, two enantiomers were best separated with the improvement of sensitivity reaching 160-fold and 4000-fold respectively for LVSS-sweeping and CSEI-sweeping comparing with the normal CDEKC separation. Then the optimal condition of CSEI-sweeping-CDEKC was validated and showed high sensitivity (10 ng/mL for lower limit of quantification, LLOQ), satisfactory accuracy (96.8-111.6%) and precision (relative standard deviation, RSD within 9.4%). This demonstrated it to be a suitable strategy for the rapid enantioselective determination and quantitative analysis of pheniramine enantiomers in plasma samples. Therefore, the method was further applied in the enantiomeric analysis of pheniramine in rat pharmacokinetics and plasma protein binding investigations. Stereoselectivity in pharmacokinetics as well as plasma protein binding were observed, suggesting that the stereoselective protein binding might be responsible for the stereoselectivity in pharmacokinetics.


Assuntos
Cromatografia/métodos , Feniramina/sangue , Administração Oral , Animais , Soluções Tampão , Masculino , Feniramina/administração & dosagem , Feniramina/química , Feniramina/farmacocinética , Fosfatos/química , Ratos Wistar , Estereoisomerismo , beta-Ciclodextrinas/química
19.
Dermatol Online J ; 24(6)2018 08 23.
Artigo em Inglês | MEDLINE | ID: mdl-30142724

RESUMO

Fixed drug eruption is a delayed type hypersensitivity reaction to a drug seen most frequently with antibiotics such as tetracyclines, sulfonamides, and NSAIDs such as naproxen and ibuprofen. Although H1-antihistamines rarely elicit cutaneous adverse effects, there have been a few reports in the literature implicating them in causing fixed drug eruption, particularly the piperazine derivatives (hydroxyzine, cetirizine, levocetirizine), and loratadine. However, cutaneous drug reactions with the alkylamine derivatives like pheniramine maleate are extremely uncommon and fixed drug eruptions have not been reported with any of the alkylamine antihistamines to date. We herein report a case of multifocal bullous fixed drug eruption following ingestion of pheniramine maleate.


Assuntos
Erupção por Droga/etiologia , Antagonistas dos Receptores Histamínicos H1/efeitos adversos , Feniramina/efeitos adversos , Infecções Respiratórias/tratamento farmacológico , Dermatopatias Vesiculobolhosas/induzido quimicamente , Adulto , Erupção por Droga/tratamento farmacológico , Erupção por Droga/patologia , Feminino , Glucocorticoides/administração & dosagem , Antagonistas dos Receptores Histamínicos H1/uso terapêutico , Humanos , Feniramina/uso terapêutico , Dermatopatias Vesiculobolhosas/tratamento farmacológico , Dermatopatias Vesiculobolhosas/patologia
20.
Acta Cir Bras ; 33(2): 125-133, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29513811

RESUMO

PURPOSE: To investigate the biochemical, histopathologic, and spermatogenetic changes in the detorsionated testicle after experimental torsion and to study the antioxidant effects of pheniramine maleate and nebivolol. METHODS: Twenty-four Sprague-Dawley male rats were divided into 4 groups: Group 1: Sham; Group 2: Torsion/Detorsion (T/D); Group 3: T/D + Pheniramine maleate (PM); Group 4: T/D + Nebivolol (NB) group. Paroxanase (PON), total antioxidant status (TAS), total oxidant status (TOS), and oxidative stres index (OSI) were measured, and spermatogenetic and histopathologic evaluation was performed in tissue and blood samples. RESULTS: The evaluation of tissue TAS indicated no statistically significant difference in Group 3 compared to Group 2. A statistically significant increase was detected in Group 4 compared to Group 2. Serum PON levels revealed a statistically significant increase in Groups 3 and 4 compared to Groups 1 and 2. The Johnsen testicular biopsy score decreased in Groups 3 and 4, but the decrease was not statistically significant. CONCLUSIONS: Pheniramine maleate and nebivolol have antioxidant effects against ischemia-reperfusion damage. They also support tissue recovery, which is more significantly observed by nebivolol.


Assuntos
Antioxidantes/farmacologia , Nebivolol/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Feniramina/farmacologia , Torção do Cordão Espermático/tratamento farmacológico , Testículo/efeitos dos fármacos , Antagonistas Adrenérgicos beta/farmacologia , Animais , Arildialquilfosfatase/sangue , Antagonistas dos Receptores Histamínicos H1/farmacologia , Masculino , Ratos , Ratos Sprague-Dawley , Traumatismo por Reperfusão/tratamento farmacológico , Torção do Cordão Espermático/patologia , Espermatogênese/efeitos dos fármacos , Testículo/irrigação sanguínea , Testículo/patologia , Fatores de Tempo
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