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- The Antihistamine Drugs Carbinoxamine Maleate and Chlorpheniramine Maleate Exhibit Potent Antiviral Activity Against a Broad Spectrum of Influenza Viruses. [Journal Article]
- FMFront Microbiol 2018; 9:2643
- Influenza A viruses (IAV) comprise some of the most common infectious pathogens in humans, and they cause significant mortality and morbidity in immunocompromised people as well as children and the e...
Influenza A viruses (IAV) comprise some of the most common infectious pathogens in humans, and they cause significant mortality and morbidity in immunocompromised people as well as children and the elderly. After screening an FDA-approved drug library containing 1280 compounds by cytopathic effect (CPE) reduction assay using the Cell Counting Kit-8, we found two antihistamines, carbinoxamine maleate (CAM) and S-(+)-chlorpheniramine maleate (SCM) with potent antiviral activity against A/Shanghai/4664T/2013(H7N9) infection with IC50 (half-maximal inhibitory concentration) of 3.56 and 11.84 μM, respectively. Further studies showed that CAM and SCM could also inhibit infection by other influenza A viruses, including A/Shanghai/37T/2009(H1N1), A/Puerto Rico/8/1934(H1N1), A/Guizhou/54/1989(H3N2), and one influenza B virus, B/Shanghai/2017(BY). Mice were challenged intranasally with A/H7N9/4664T/2013 (H7N9) virus and intraperitoneally injected with CAM (10 mg/kg per day) or SCM (1 mg/kg per day) for 5 days. CAM or SCM (10 mg/kg per day) were fully protected against challenge with A/Shanghai/4664T/2013(H7N9). The results from mechanistic studies indicate that both could inhibit influenza virus infection by blocking viral entry into the target cell, the early stage of virus life cycle. However, CAM and SCM neither blocked virus attachment, characteristic of HA activity, nor virus release, characteristic of NA activity. Such data suggest that these two compounds may interfere with the endocytosis process. Thus, we have identified two FDA-approved antihistamine drugs, CAM and SCM, which can be repurposed for inhibiting infection by divergent influenza A strains and one influenza B strain with potential to be used for treatment and prevention of influenza virus infection.
- Efficacy of Oral Acetaminophen and Intravenous Chlorpheniramine Maleate versus Placebo to Prevent Red Cell Transfusion Reactions in Children and Adolescent with Thalassemia: A Prospective, Randomized, Double-Blind Controlled Trial. [Journal Article]
- AAnemia 2018; 2018:9492303
- CONCLUSIONS: Administration of premedications in thalassemia patients receiving RBC transfusion without a history of transfusion reactions does not decrease the overall risk of transfusion reactions. However, the use of CPM might be beneficial to prevent delayed urticarial rash in those patients especially in females (Thai Clinical Trial Registry (TCTR) study ID: 20140526001).
- Polypharmacy leads to increased prevalence of potentially inappropriate medication in the Indonesian geriatric population visiting primary care facilities. [Journal Article]
- TCTher Clin Risk Manag 2018; 14:1591-1597
- CONCLUSIONS: PIM is a concern in the Indonesian geriatric population. Health care professionals are encouraged to review the medications of their geriatric patients using updated safety guidelines to prevent risks associated with PIM.
- Time-to-onset of cold and flu symptom relief: A randomized, double-blind, placebo-controlled pilot study for a multi-symptom combination product. [Journal Article]
- IJInt J Clin Pharmacol Ther 2018; 56(12):604-611
- CONCLUSIONS: In this exploratory pilot study, a multisymptom cold and flu tablet was well tolerated but did not differ from placebo tablet with regard to onset of action following a single dose. .
- Intracerebellar microinjection of histaminergic compounds on locomotor and exploratory behaviors in mice. [Journal Article]
- NLNeurosci Lett 2018 Nov 20; 687:10-15
- The neural histaminergic system innervates the cerebellum, with a high density of fibers in the vermis and flocculus. The cerebellum participates in motor functions, but the role of the histaminergic...
The neural histaminergic system innervates the cerebellum, with a high density of fibers in the vermis and flocculus. The cerebellum participates in motor functions, but the role of the histaminergic system in this function is unclear. In the present study, we investigated the effects of intracerebellar histamine injections and H1, H2 and H3 receptor antagonist injections (chlorpheniramine, ranitidine, and thioperamide, respectively) and H4 receptor agonist (VUF-8430) on locomotor and exploratory behaviors in mice. The cerebellar vermis of male mice was implanted with guide cannula. After three days of recovery,the animals received microinjections of saline or histamine (experiment1), saline or chlorpheniramine (experiment 2), saline or ranitidine(experiment 3), saline or thioperamide (experiment 4), and saline or VUF-8430 (experiment 5) in different concentrations. Five minutes postinjection,the open field test was performed. The data were analyzed using one-way ANOVA and Duncan's post hoc test. The microinjections of histamine, ranitidine or thioperamide did not lead any behavioral effects at the used doses. In contrast, animals that received chlorpheniramine at the highest dose (0.16 nmol) and VUF-8430 at the highest dose (1.48 nmol)were more active in the open field apparatus, with an increase in the number of crossed quadrants, number of rearings and time spent in the central area of the arena, suggesting that chlorpheniramine and VUF-8430 modulates locomotor and exploratory behaviors in mice.
- Therapeutic effect of chlorpheniramine in treatingupper airway cough syndrome (UACS) and chronic rhinitis/sinusitis. [Journal Article]
- PJPak J Pharm Sci 2018; 31(4(Special)):1679-1682
- This paper aims to analyze the specific effect of chlorpheniramine on upper airway cough syndrome is related to its treatment of chronic rhinitis and sinusitis. A total of 218 patients admitted to ho...
This paper aims to analyze the specific effect of chlorpheniramine on upper airway cough syndrome is related to its treatment of chronic rhinitis and sinusitis. A total of 218 patients admitted to hospital between March 2014 and June 2016 were treated with chlorpheniramine. The patients were divided into two groups based on treatment effect in follow-up visits (all were effective): effective group (114 cases, 52.29%) and ineffective group (104 cases, 47.71%). The proportion of complicated rhinitis or sinusitis of the two groups were compared, and improvement effect on clinical symptoms of chronic rhinitis and sinusitis after treatment was compared. The probability of rhinitis / sinusitis was 65.79% (75/114) in the effective group and 69.23% (72/104) in the ineffective group. There was no statistical difference between the two groups (P>0.05). In both effective and ineffective group, the symptoms such as chest tightness and shortness of breath and pharyngeal discomfort were improved to a certain extent, and the effective group had better improvement effect, but there was no statistical difference between the two groups (P>0.05). In addition, there was no correlation between improvement of cough and improvement of symptoms in the effective group, 21 cases of cough disappeared completely, while complete disappearance rate of other symptoms was only 57.15% (12/21). Chlorpheniramine is effective to some extent in treatment of upper airway cough syndrome, but chlorpheniramine in treatment of upper airway cough syndrome is not associated with rhinitis/sinusitis treatment.
- Fabrication of Hierarchical Polymeric Thin Films by Spin Coating Toward Production of Amorphous Solid Dispersion for Buccal Drug Delivery System: Preparation, Characterization, and In Vitro Release Investigations. [Journal Article]
- JPJ Pharm Sci 2018; 107(12):3112-3122
- The landscape of thin films is continuously evolving as an attractive self-administration mean to drive patient compliance. This work reports incorporation of drugs into various polymeric composition...
The landscape of thin films is continuously evolving as an attractive self-administration mean to drive patient compliance. This work reports incorporation of drugs into various polymeric compositions using spin coating technology to screen amorphous solid dispersion film formation for buccal applications. Polarized light microscopy and differential scanning calorimetry were used for characterization. Physical stability was assessed after films storage at 0% RH/25°C for 6 months. Chlorpheniramine maleate, theophylline, and famotidine were used as model drugs and mixed with Opadry amb II® or Kollicoat IR®. Acryl-EZE II® or Zein was also used as surface (design I) or surface and base polymers (design II). Of all the drug-Opadry combinations, only chlorpheniramine was amorphously dispersed up to 25% (w/w). In contrast, Kollicoat IR® resulted in amorphous dispersions of all the tested drugs, suggesting that it has a better solubilization capacity. Drugs prepared in design II achieved higher in vitro release compared to respective design I, indicating that lower content of Acryl-EZE II® or Zein can decrease drug release over 3 h. It has been also revealed that Zein could improve physical stability of the aged theophylline solid-dispersed films. Release kinetics of model drugs were satisfactory when described by first-order kinetics, facilitated through anomalous transport of both diffusion and polymer swelling.
- Multi-residue analysis of chiral and achiral trace organic contaminants in soil by accelerated solvent extraction and enantioselective liquid chromatography tandem-mass spectrometry. [Journal Article]
- JCJ Chromatogr A 2018 Oct 19; 1572:62-71
- Reported here is the first analytical methodology for the enantiomeric determination of chiral trace organic contaminants (TOrCs) in soil. Direct enantioselective separations were achieved on a Chiro...
Reported here is the first analytical methodology for the enantiomeric determination of chiral trace organic contaminants (TOrCs) in soil. Direct enantioselective separations were achieved on a Chirobiotic V2® column operated in polar ionic mode. Initial screening of vancomycin stationary phases found Chirobiotic V2® better suited for multi-residue separation of chiral TOrCs than Chirobiotic V® due to differences in the ligand linkage chemistry. Simultaneous enantioseparation of beta-blockers, beta-agonists, anti-depressants, anti-histamines and stimulants was achieved for the first time. This included the first separation of chlorpheniramine enantiomers with a method suitable for environmental analysis (i.e., coupled to MS). Investigation of mobile phase composition found the concentration of liophilic ions had the greatest influence on enantioseparations and of most importance during method development. The optimized method achieved simultaneous separation of salbutamol, propranolol, atenolol, amphetamine, chlorpheniramine and fluoxetine enantiomers with satisfactory resolution (>1.0). For completeness, such methods also need to support analysis of achiral TOrCs. Therefore three achiral TOrCs (carbamazepine, carbamazepine 10,11 epoxide and triclocarban) were included to demonstrate the methods suitability. Method recoveries for all analytes ranged from 76 to 122% with method quantitation limits (MQLs) <1 ng g-1. Application of the method to soil microcosm studies revealed stereoselective degradation of chiral TOrCs for the first time. For example, S(+)-amphetamine degraded at a faster rate than its corresponding enantiomer leading to an enrichment of R(-)-amphetamine. Therefore to better understand the risk posed from TOrCs on the terrestrial environment, chiral species need profiled at the enantiomeric level. This can now be addressed using the proposed methodology whilst simultaneously profiling achiral TOrCs.
- Intracerebroventricular injection of histamine induces the hypothalamic-pituitary-gonadal axis activation in male rats. [Journal Article]
- BRBrain Res 2018 Nov 15; 1699:150-157
- Brain histamine holds a key position in the regulation of behavioral states, biological rhythms, body weight, energy metabolism, thermoregulation, fluid balance, stress and reproduction in female ani...
Brain histamine holds a key position in the regulation of behavioral states, biological rhythms, body weight, energy metabolism, thermoregulation, fluid balance, stress and reproduction in female animals. However, it is not clear whether central histamine exerts any effect on hypothalamic-pituitary-testicular in male rats and if so, the involvement of type of central histamine receptors. The current study was designed to determine the effect of centrally administrated histamine on plasma gonadotropin hormone-releasing hormone (GnRH), luteinizing hormone (LH), follicle stimulating hormone (FSH) and testosterone level, and sperm parameters, and to show the mediation of the central histaminergic H1, H2 and H3/H4 receptors on histamine-evoked hormonal and sperm parameters' effects. Studies were performed in male Sprague-Dawley rats. A total of 50 or 100 nmol doses of histamine were injected intracerebroventricularly (icv). 100 nmol dose of histamine significantly caused increases in plasma GnRH, LH, FSH and testosterone levels of animals, but not 50 nmol dose of histamine. Moreover, central pretreatment with chlorpheniramine, histaminergic H1 receptor antagonist (100 nmol), ranitidine and histaminergic H2 receptor antagonist (100 nmol) completely prevented histamine evoked increase in plasma GnRH, LH, FSH and testosterone levels, while thioperamide, histaminergic H3/H4 receptor antagonist (100 nmol) pretreatment failed to reverse sex hormones responses to histamine. Both central histamine treatment alone and central histamine treatment after central histaminergic receptors antagonists' pretreatments did not alter any sperm parameters in rats. In conclusion, our findings show that centrally administered histamine increases plasma GnRH, LH, FSH and testosterone levels of conscious male rats without change any sperm parameters. Moreover, according to our findings, central histaminergic H1, and H2 receptors mediate these histamine-induced effects.
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- Investigation of the distributional homogeneity on chlorpheniramine maleate tablets using NIR-CI. [Journal Article]
- SASpectrochim Acta A Mol Biomol Spectrosc 2018 Nov 05; 204:783-790
- Homogeneity is the basic element of pharmaceutical analysis. Distributional Homogeneity Index (DHI) was proposed to assess the distributional homogeneity of commercial chlorpheniramine maleate (CPM) ...
Homogeneity is the basic element of pharmaceutical analysis. Distributional Homogeneity Index (DHI) was proposed to assess the distributional homogeneity of commercial chlorpheniramine maleate (CPM) tablets. Furthermore, the divergence value of DHI value from expectation DHI (value = 1) was calculated to obtain the CPM distributional homogeneity. The distribution of commercial CPM tablets from six brands was successfully visualized using near infrared chemical imaging (NIR-CI) coupled with characteristic wavenumber method and binary image. Besides, content homogeneity of CPM was obtained through calculating the proportion of white region in the binary image. The result demonstrated that the distributional homogeneity of brand 4 was to be the best among all the brands, following by brand 2, brand 3, brand 5, brand 6 and brand 1. Furthermore, the sequence of the content uniformity was different from the distributional homogeneity, which demonstrated that content uniformity could not represent the distributional homogeneity. This work was a significant method guideline to assess the distributional homogeneity in pharmaceutical field.