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Background: The proposed research study introduces independent concentration extraction (ICE) as a novel UV–Vis spectrophotometric approach. The approach can be used for extracting the concentration of two analytes with severely overlapped spectra from their binary mixtures. ICE is based on spectral extraction platform involving simple smart successive methods that can directly extract the original zero order spectra of the analytes at their characteristic (λmax). Chlorpheniramine maleate (CPM) and Levocloperastine fendizoate (LCF) are two commonly co-formulated drugs in cough preparations. The combined mixture was used to confirm the validity of the developed ICE tool. Another less green HPTLC was developed for the first time to separate both drugs and help also in confirming the proposed tool. Methods: For the simultaneous determination of CPM and LCF, two ecologically friendly techniques were employed. The first approach encompasses the use of the ICE spectrophotometric method that could be successively applied for extracting the concentration of two analytes with severely overlapped unresolved spectra in their binary mixtures. Other complementary methods aiming at original spectral extraction; including spectrum subtraction (SS) and unity subtraction (US) were also successfully employed to resolve the zero order spectra of the combined drugs with all their characteristic features and peaks. The second technique used, a high-performance TLC-densitometric one, was performed on silica plates with silica plates F254 and a mobile phase with a ratio of 3:3:3:1 by volume of toluene, ethanol, acetone, and ammonia as a developing system at 230 nm. Results: The presented extraction approach was executed without any optimization steps or sample pretreatment for the simultaneous determination of CPM and LCF. The method was found to be valid for their determination within concentration range of 3.0–30.0 μg mL−1 for both drugs. For HPTLC method, the resulting Rf values of CPM and LCF were 0.37 and 0.78, within concentration ranges of 0.3–4.0 μg/spot and 0.8–10.0 μg/spot, respectively. Greenness assessment of both developed methodologies showed that the HPTLC method is less green than the spectrophotometric method, yet with comparable sustainability when it comes to the used technique. Conclusion: The procedures were found to be selective, accurate, and precise for analysis of the studied binary mixture. Furthermore, the environmental impact of the introduced methods was assessed using novel greenness metrics, namely AGREE and Green Analytical Procedure Index (GAPI) to prove their ecological safety. In addition, white analytical chemistry (WAC) evaluation metric was employed to ensure the synergy and coherence of analytical, practical, and ecological attributes. [ABSTRACT FROM AUTHOR]

The aim of our study is to develop a simple, delicate, precise and economical protocol for the qualitative and quantitative determination of Chlorpheniramine using spectrophotometer. Our validation is distinctive and provides a precise picture of a very weak chromophore of chlorpheniramine (CPN) that had not been accurately detected before by traditional techniques. The blue color which formed by mixing pheniramine and Cobalt- thiocyanate solution was extracted with chloroform. CPN presented a linearity range of 25 – 125 μg at 628 nm. Limit of quantification (15 μg/mL) and limit of detection (08 μg/mL) of cobalt-chloride were analyzed. The resulting data was statistically significant. Because of the appropriate reproducibility and reliability of this proposed analysis, it can be used to screen CPN in pharmaceutical preparations. It is also validated through the International Council of Harmonization for accuracy, linearity, precision, LOD and LOQ. Various dosage forms of pheniramine were evaluated and have shown that they did not exceed their relative standard deviation by 1%. Their percentage purity was within 99.62 – 103.34%. The suspected sample was treated with 2 – 3 drops of cyanocobalamine after which violet coloration appeared. The percentage relative standard deviation of accuracy and precision was acquired as 1.57 and 1.15, respectively, exactly following the authentication criteria for newly established methods. Because of the profound potential of these developed methods, including precise, fast, flawless and inexpensive, it can easily be adopted in laboratories for the routine analysis of Chlorpheniramine. [ABSTRACT FROM AUTHOR]

The intermolecular interactions and solution properties of the antihistamine drug chlorpheniramine (CP) in aqueous, aqueous solutions of electrolyte and non-electrolyte have been examined in the current work using volumetric and spectroscopic approaches to investigate how the drug is affected by co-solutes. Also, a drug's behavior in water and other aqueous systems can be studied to learn more about the chemistry of biological systems. Using an Anton Paar density and sound velocity meter, densities and sound velocities for CP (0–0.10 mol⋅kg−1) at various temperatures (298.15, 308.15, and 318.15 K) in water and in aqueous 0.05 mol⋅kg−1 urea, glucose, and sodium chloride have been measured to determine apparent molar properties: apparent molar volume ( V ϕ) and apparent molar compressibility (K ϕ , S) . A number of derived parameters, including limiting apparent molar volume V ϕ 0 , limiting apparent molar compressibility ( K ϕ , S 0) , limiting apparent molar expansibility ( ϕ E 0) , and isobaric thermal expansion coefficient (ɑ) were obtained using the data on apparent molar properties. While analyzing the data, solute–solvent interactions are taken into account, as well as their considerable effects on CP hydration when co-solutes, are introduced to the combination. The negative transfer properties suggest the predominance of ion-hydrophobic and hydrophobic-hydrophobic interactions in all the studied systems. Positive and small negative values of Hepler's constant revealed the structure-making capability of CP in aqueous urea, glucose, and sodium chloride. Also, an IR study has been done to verify the results obtained from volumetric and compressibility data. Understanding how drugs behave in various solvent systems during drug development is made easier by understanding drug interactions. [ABSTRACT FROM AUTHOR]

Chlorpheniramine (CPM) is a widely used antihistamine drug that may be desirable to quantify in a variety of samples. We developed a CPM electrochemical sensor based on a composite of reduced graphene oxide (rGO) and silver nanoparticles (AgNPs) coated on a glassy carbon electrode (GCE). Sodium dodecyl sulfate (SDS) was used as a surfactant to prevent the aggregation of AgNPs. rGO and AgNPs were co-electrodeposited by cyclic voltammetry, varying the potential from -1.5 to 1.5 V vs. Ag/AgCl 3 M KCl. The electrochemical properties of the modified electrode were characterized by cyclic voltammetry (CV) and electrochemical impedance spectroscopy (EIS). The rGO/AgNPs/GCE showed excellent electrocatalytic activity for the oxidation of CPM. The anodic peak potential, measured using CV, was 0.78 V vs. Ag/AgCl in a carbonate-bicarbonate buffer of pH 10. The modified electrode exhibited a linear response for CPM concentrations between 10 and 300 μM, with a limit of detection of 4.2 μM. Several potentially interfering species, including ionic and organic compounds, did not have any significant effect on the CPM determination. This work thus describes a versatile sensor that could be applied to measure CPM in real samples. [ABSTRACT FROM AUTHOR]

Acetaminophen, chlorpheniramine maleate syrup is an over-the-counter (OTC) non-compendial syrup dosage form. Compendial monograph methods are not available for this product. Therefore, a single stability indicating method for the estimation of acetaminophen, chlorpheniramine maleate and possible degradation products has been developed and validated. The chromatographic separation was achieved on Phenomenex Phenyl Hexyl, (150 × 4.6 mm, 5.0 μm) HPLC column at a mobile phase flow rate of 1.0 mL/min and the detection was made at 225 nm wavelength. The correlation coefficient (r) for each analyte was more than 0.99. The reported method is precise, accurate, and robust in estimating active substances, preservatives, and related impurities. To the best of authors' knowledge, the proposed method is the first report of a single stability-indicating HPLC method for the simultaneous determination of active substances, preservatives and impurities in Acetaminophen, Chlorpheniramine Maleate OTC syrup formulation throughout the product shelf-life. [ABSTRACT FROM AUTHOR]

Density (ρ), viscosity (η), and ultrasonic velocity (U) are studied for binary liquid mixtures of chlorpheniramine with 1-butanol, 1-pentanol, and 1-hexanol at 303 K. Adiabatic compressibility (β), free length (Lf), free volume (Vf), internal pressure (πi), viscous relaxation time (τ), and Gibbs free energy (ΔG) are calculated by using the experimental data. The excess values of the above parameters (βE, , , , τE, and ΔGE) from their ideal values are also determined and fitted with Redlich–Kister polynomial equation. The changes in the determined parameters are interpreted in terms of the intermolecular interaction between the liquid mixtures. The significant changes in the ideal parameters and the excess parameters have confirmed the existence of the intermolecular interactions between the selected liquid system. From the observations, strength of intermolecular interaction of chlorpheniramine with the selected alcohols is in the order of 1‑butanol < 1-pentanol < 1-hexanol. [ABSTRACT FROM AUTHOR]

Purpose: Catheter-related bladder discomfort (CRBD) is postoperative distress caused by a urinary catheter. CRBD is related to muscarinic receptor activation. Chlorpheniramine has antimuscarinic properties. Hence, this investigation was undertaken to evaluate the efficacy of chlorpheniramine in preventing CRBD in patients undergoing transurethral resection of bladder tumor (TURBT). Methods: Seventy-six patients scheduled for TURBT under general anesthesia were assigned into two groups. In the chlorpheniramine group (n = 38), 100 ml normal saline containing 0.1 mg/kg chlorpheniramine was infused after general anesthesia induction. In the control group (n = 38), 100 ml normal saline alone was infused. The incidence and severity of CRBD were assessed at 1, 6, and 24 h postoperatively. Results: The 1-h postoperative incidence of CRBD was lower in the chlorpheniramine group based on the unadjusted analysis [16 (42%) vs. 28 (74%), risk difference 32%, 95% confidence interval 8–51, p = 0.005]. After adjusting the size of the urinary catheter, post hoc analysis showed that the 1-h postoperative incidence of CRBD was lower in the chlorpheniramine group (p = 0.004). The CRBD severity score was lower in the chlorpheniramine group at 1 and 6 h after operation based on the unadjusted analysis (p = 0.012 and p = 0.007, respectively). After adjusting the urinary catheter size, post hoc analysis showed that 1- and 6-h CRBD severity score was lower in the chlorpheniramine group (p = 0.012 and p = 0.008, respectively). The incidence of rescue medication was lower in the chlorpheniramine group [10 (26%) vs. 20 (53%), risk difference 26%, 95% confidence interval 3–47, p = 0.019]. The overall incidence of complications such as nausea, vomiting, dry mouth, flushing, dizziness, and blurred vision was comparable between the two groups. Conclusions: Chlorpheniramine administration significantly reduces the incidence and severity of CRBD in the patients undergoing TURBT. Trial registration: KCT0004880 (https://cris.nih.go.kr/) [ABSTRACT FROM AUTHOR]

Some new 1-substituted-4-(4-nitrophenyl)-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones were synthesized and screened for their H1-antihistaminic activity. The structures of the newly synthesized compounds were confirmed by IR, 1H NMR, and mass spectral data and purity of the compounds was determined by elemental analysis. Antihistaminic activity of synthesized compounds was determined by the protection against histamine-induced bronchospasm on conscious guinea pigs. Percentage protection data showed that all title compounds of the series show significant protection in the range of 68–71.56% when compared to reference drug chlorpheniramine maleate (70.17%). The sedative properties of the compounds were also evaluated and found to be negligible when compared to chlorpheniramine maleate. [ABSTRACT FROM AUTHOR]

Background: Chlorpheniramine (CPA), thanks to its relatively lower side effects, is a widely prescribed medicine for alleviating allergic symptoms as well as some medical emergencies. Owning to this extensive use, many efforts have been directed to measure chlorpheniramine both in vivo and in vitro. High performance liquid chromatography (HPLC), both normal and reverse phase, as well as spectrochemical and electrochemical methods are analytical approaches which have been extensively exploited for determination of CPA. Among them, electrochemical techniques have found elegant place for analysis of CPA due to simplicity, sensitivity and ease of instrumentation. Methods: Herein, we have reported the preparation and characterization of a biosensor by immobilization of double-stranded DNA on the surface of overoxidizedpolypyrrole-reduced graphene oxide modified pencil graphite electrode (ds-DNA-PPyox/RGO/PGE) as well as its novel usability in measurement of chlorpheniramine (CPA). Scanning electron microscopy (SEM), electrochemical impedance spectroscopy (EIS), UV-Vis spectroscopy and differential pulse voltammetry (DPV) were exploited in order to characterize and evaluate the performance of the proposed biosensor. Results: Final results showed that proposed strategy for modification of PGE introduces an ultra-sensitive biosensor for CPA which offers the best detection limitamong all previously reported electrochemical sensors for CPA. Taking advantage of this biosensor for determination of CPA, a wide linear dynamic range from 0.05 to 200 μM, and a low limit of detection 0.023 μM were obtained by using DPV method. Usability of this biosensor was also confirmed by determination of CPA in tablet and spiked urine samples. Conclusions: Overoxidized polypyrrole-reduced graphene oxide offered a suitable substrate for immobilization of ds-DNA by which a new biosensor for determination of CPA was fabricated. Proposed biosensor can successfully be used for determination of CPA in urine samples taking advantage of electroanalytical methods. [ABSTRACT FROM AUTHOR]

Chlorpheniramine is a pharmaceutical pollutant and a precursor of carcinogenic nitrosamines during disinfection/oxidation. In our previous study, graphene oxide coated with magnetite (GO-Fe3O4) was capable of removing chlorpheniramine in deionized water by adsorption. This study investigated the removal of chlorpheniramine and its nitrosamine formation potentials (FPs) by adsorption onto magnetic GO-Fe3O4, with respect to the influence by using real municipal wastewaters as the background. In the results, the adsorption performances of chlorpheniramine in wastewaters decreased in the order: GO-Fe3O4 suspension > GO-Fe3O4 particles > activated carbon. Chlorpheniramine adsorptions on GO-Fe3O4 particles and activated carbon were reduced by using real wastewaters as the background, whereas chlorpheniramine adsorption on GO-Fe3O4 suspension was enhanced due to the effects of surface charge on GO-Fe3O4 and ionic strength variation in water. The fittings of adsorption isotherms indicated that the wastewater background reduced the surface heterogeneity of GO-Fe3O4 suspension and improved the adsorption performance. Appreciable removal efficiencies of NDMA and other nitrosamine FPs were observed when GO-Fe3O4 particles were added in real wastewaters. However, when chlorpheniramine was present in wastewaters, chlorpheniramine adsorption and degradation reaction simultaneously occurred on the surface of GO-Fe3O4, increasing NDMA and other nitrosamine FPs in wastewaters after GO-Fe3O4 addition for chlorpheniramine adsorption. The assumption was further demonstrated by observing the NDMA-FP increase during chlorpheniramine adsorption on GO-Fe3O4 in deionized water. GO-Fe3O4 is a potential adsorbent for chlorpheniramine removal. Nevertheless, the low treatment efficiencies at high doses limit its application for nitrosamine FP adsorptions in real wastewaters. [ABSTRACT FROM AUTHOR]

Simple, accurate, precise, sensitive, and validated high-performance liquid chromatography (HPLC) and thin-layer chromatography (TLC)--densitometric methods were developed for the simultaneous determination of chlorpheniramine maleate (CPM), pseudoephedrine HCl (PSE), and ibuprofen (IBF) in tablet dosage form. In method A, reversed-phase (RP)-HPLC analysis was performed on Zorbax C8 column (150 mm x 4.6 mm, 5 μm particle size i.d.), using a mobile phase consisting of methanol--acetonitrile--distilled water (pH 4) using orthophosphoric acid in the ratio (80:10:10, v/v) and fl ow rate of 0.7 mL min-1. Quantifi cation was achieved with ultraviolet (UV) detection at 220 nm. In method B, TLC analysis was carried out on an aluminum-backed sheet of silica gel 60 F254 layer using ethyl acetate--methanol--ammonia (8:2:0.8, v/v) as the mobile phase. Quantifi cation was carried out with UV detection at 262 nm. The validation of the proposed methods was applied according to the International Conference on Harmonization (ICH) guidelines. The suggested methods were successfully applied for the determination of the cited drugs in bulk powder and commercial dosage form. [ABSTRACT FROM AUTHOR]

Asimple, rapid isocratic liquid chromatography method was developed for the simultaneous determination of diphenhydramine, promethazine, chlorpheniramine, and ephedrine in cold-cough syrups commonly available in the Kenyan market. The influence of the percentage of organic modifier, ion pairing agent, buffer concentration as well as pH and column temperature on the selectivity with respect to analytes was investigated. Optimum chromatographic separation was achieved using a C Gemini NX column (250 mm × 4.6 mm, 5 μm) maintained at 40°C and a mobile phase comprising methanol - triethylamine - 0.2 M ammonium acetate pH 5.0 - water mixture (50 : 0.15 : 40 : 9.85, v/v) delivered at a flow rate of 1.0 mL/min. Upon validation, the proposed liquid chromatography method satisfied the International Committee on Harmonization acceptance criteria for linearity, sensitivity, precision, and robustness. The method was applied in the analysis of commercial samples obtained from Nairobi County, Kenya. The method can be used in routine analysis of cold-cough syrups containing the specified compounds. [ABSTRACT FROM AUTHOR]

A simple, rapid, isocratic, and versatile liquid chromatographic method was developed for the simultaneous determination of bromhexine, guaifenesin, ambroxol, salbutamol/terbutaline, pseudoephedrine, triprolidine, and chlorpheniramine maleate in cough-cold syrups commonly marketed in Kenya. Separation was achieved using a Gemini NX C column (250 × 4.6 mm, 5 μm) maintained at 40 °C and a mobile phase consisting of acetonitrile-0.25 M sodium hexanesulphonate-0.2 M ammonium acetate, and pH 3.0-water (35:4:10:51, % v/v/v/v) delivered at 1.0 mL min. The eluents were monitored by means of UV detection at 254 nm. During validation, the method satisfied the International Committee on Harmonization acceptance criteria for linearity, sensitivity, precision, accuracy, and robustness. The developed liquid chromatographic method was applied in the analysis of nine commercial samples obtained from Nairobi City County, Kenya. Extraction procedures were not applied during the assay of the samples, thus significantly shortening the analysis time. [ABSTRACT FROM AUTHOR]

Background Oral ketamine has been shown to induce safe and effective sedation in children, but with a high incidence of postoperative vomiting. Vendexine (dexamethasone-chlorpheniramine mixture) is a commercially available syrup used primarily to treat allergic conditions. Each of its components has antiemetic effects. In the present study, we aimed to determine whether the addition of vendexine to oral ketamine premedication affects the incidence of postoperative vomiting. Patients and methods Sixty-four children scheduled for elective dental procedures under general anesthesia were enrolled in this prospective, randomized, double-blind study. They received an oral premedication mixture (total volume of 0.42 ml/kg) of either ketamine 6 mg/kg (0.12 ml/kg) mixed with dextrose 50% and apple juice (the K group), or ketamine 6 mg/kg (0.12 ml/kg) mixed with dextrose 50% and vendexine syrup (0.25 ml/kg) (the VK group). Sedation onset was noted. Scores for drug acceptance, sedation, emotional status, and behavior during parents' separation, on venipuncture, and face mask application were rated. Incidence of postoperative vomiting, emergence agitation score, fentanyl consumption, and recovery time were also recorded. Results The two groups were comparable as regards sedation onset, scores for drug acceptance, sedation, emotional status, and behavior during parents' separation, on venipuncture, and face mask application. However, a significant reduction of postoperative vomiting in the VK group was noticed compared with the K group (9.3 vs. 37.5%). In addition, emergence agitation and fentanyl consumption were significantly reduced in the VK group. Conclusion Vendexine added to oral ketamine reduces the incidence of postoperative vomiting associated with ketamine premedication in children. [ABSTRACT FROM AUTHOR]

There are limited numbers of articles, studying combined use of antihistamines. In this study, we compare single therapy of Apo-Cetirizine with a new regimen of intermittent sequential therapy with cetirizine, loratadine and chlorpheniramine in treatment of seasonal allergic rhinitis. This randomized clinical trial was performed between April and September at the peak prevalence of seasonal allergic rhinitis. Fifty-four eligible patients diagnosed clinically to have seasonal allergic rhinitis were randomized in two groups: 24 cases in single therapy arm, received Apo-Cetirizine 10 mg tablet daily and in other arm, 30 patients received sequential regimen of cetirizine 10 mg tablet, loratadine 10 mg tablet and chlorpheniramine 4 mg tablet, one tablet each day. Major Symptom Complex Score (MSCS) and Total Symptom Complex Score (TSCS) of patients were recorded before treatment and after 30 days of treatment in two groups. The average post-treatment MSCS and TSCS in combination therapy group showed better improvement than single therapy group but difference was not statistically significant ( p value = 0.053 and p value = 0.104 respectively). Combination therapy regimen was better in improvement of nasal congestion ( p value = 0.006). There were no significant difference between two groups in efficacy, side effects and patient's satisfaction. Combination therapy would be effective on a wide spectrum of symptoms with lower price and theoretically offers lower chance of tolerance and re-appearance of complaints. [ABSTRACT FROM AUTHOR]

Chlorpheniramine maleate-paracetamol-caffeine tablet formulation is one of the common over-the-counter drugs used for the treatment of cold and cough. A reversed-phase high-performance liquid-chromatography method has been successfully developed for the simultaneous determination of chlorpheniramine maleate, paracetamol and caffeine in a drug formulation. The RP-HPLC method employed a Phenomenex C18 reversed phase column (Luna 5µ, 250 × 4.6 mm) with an isocratic mixture of methanol and 0.05 M dibasic phosphate buffer pH 4.0 in the ratio of (30:70; v/v) as the mobile phase. The column temperature was kept at 30 °C. The flow rate was 1.0 mL/min and detection was by means of a UV detector at wavelength of 215 nm. All the active components were successfully eluted with mean retention times of 2.4, 4.2, 7.2 min for chlorpheniramine maleate, paracetamol and caffeine respectively. The method was found to be linear (R > 0.99), precise (RSD < 2.0 %), accurate (recoveries 97.9-102.8 %), specific, simple, sensitive, rapid and robust. The validated method can be used in routine quality control analysis of fixed dose combination tablets containing chlorpheniramine maleate, paracetamol and caffeine without any interference by excipients. [ABSTRACT FROM AUTHOR]

The aim of this study was to investigate effects of intracerebroventricular injection of α-Fluoromethylhistidine (α-FMH; histidine decarboxylase inhibitor), Chlorpheniramine (histamine H receptor antagonist), Famotidine (histamine H receptor antagonist) and Thioperamide (histamine H receptor antagonist) on Nociceptin/Orphanin FQ-induced feed intake response in chicken. A hundred and twenty-eight broiler cockerels (four groups eight replicate), were cannula surgically implanted into the lateral ventricle, used in four separate experiments. Experiment 1, cockerels injected intracerebroventricularly with α-FMH (250 nmol) followed by Nociceptin/Orphanin FQ (16 nmol). In experiment 2, chickens received Chlorpheniramine (300 nmol) prior to injection of Nociceptin/Orphanin FQ (16 nmol). In experiment 3, birds were administered with Nociceptin/Orphanin FQ (16 nmol) after Famotidine (82 nmol) injection. In experiment 4, broilers were injected with thioperamide (300 nmol) followed by Nociceptin/Orphanin FQ (16 nmol). Cumulative food intake was measured until 3 h post-injection. According to the results, a significantly increase was observed after injection of Nociceptin/Orphanin on food intake and this effect was amplified by pre-administration of α-FMH and Chlorpheniramine in broilers ( p < 0.05). Moreover, famotidine had no effect on hyperphagia induced by Nociceptin/Orphanin FQ in chicken ( p > 0.05). Also, pre-administration of thioperamide significantly attenuated Nociceptin/Orphanin FQ-induced hyperphagia ( p < 0.05). These results suggest that, Nociceptin/Orphanin FQ-induced hyperphagia is mediated by histaminergic system via H and H receptors in broiler chickens. [ABSTRACT FROM AUTHOR]

Objective and design: The aim of this study is to evaluate the expression of the histamine receptors, particularly focusing on the HR in human renal tubules. Material: The ex vivo evaluation was carried on specimens from human renal cortex. Primary and immortalized tubular epithelial cells (TECs) and the HK-2 cell line were used as in vitro models. Treatment: Cells were pretreated for 10 min with chlorpheniramine maleate 10 μM (HR antagonist), ranitidine 10 µM (HR antagonist), GSK189254 1 µM (HR antagonist) or JNJ7777120 10 µM (HR antagonist), and then exposed to histamine (3 pM-10 nM) for 30 min. Methods: The ex vivo evaluation on specimens from human renal cortex was performed by immunohistochemistry. The expression of histamine receptors on primary and immortalized TECs and the HK-2 cell line was evaluated at both gene (RT-PCR) and protein (immunocytofluorescence) levels. The pharmacological analysis was performed by TR-FRET measurements of second messenger (IP3 and cAMP) production induced by histamine with or without the selective antagonists. Results: Our data revealed the presence of all histamine receptors in human tubules; however, only TECs expressed all the receptors. Indeed, histamine elicited a sigmoid dose-response curve for IP production, shifted to the right by chlorpheniramine maleate, and elicited a double bell-shaped curve for cAMP production, partially suppressed by the selective HR, HR and HR antagonists when each added alone, and completely ablated when combined together. Conclusions: Herein, we report the identification of all four histamine receptors in human renal tubules. [ABSTRACT FROM AUTHOR]

With more and more emerging organic contaminants (EOCs) detected in the soil and groundwater, researches on interactions between these pollutants and soils or aquifer materials have attracted greater concerns. In this study, the removal of chlorpheniramine maleate (CP), an antihistamine drug used to treat rhinitis and urticaria, by birnessite, which is a common layered manganese oxide, in aqueous solution was investigated by batch studies, X-ray diffraction (XRD) and Fourier transform infrared (FTIR) analyses, and molecular simulations. The quantum mechanics simulation showed that the final energy of the interaction between CP and the (010) edge surfaces under a strong alkaline condition was much smaller than that under a neutral to slightly alkaline condition. A higher CP adsorption were achieved from neutral to weak alkaline solution, as the broken bond effect of birnessite was strongly influenced by solution pH by protonation and deprotonation of birnessite edges. [ABSTRACT FROM AUTHOR]

We evaluated whether a fingerprint, which consists of secretions from the fingertips, is a suitable biological sample for drug testing. A commercially available cold medicine containing ibuprofen, dihydrocodeine, chlorpheniramine, and methylephedrine was administered to healthy subjects. The subjects washed their hands with tap water and hand soap to remove the external contaminants, and then pressed a fingertip onto wet filter paper at fixed sampling times (from 2 h to 7 days). The analytes on the filter paper were dissolved in 25 % methanol-water, and a large volume (50 μl) of the extract was analyzed by liquid chromatography-tandem mass spectrometry. The relationship between the sampling times and the concentration of analytes in fingerprints was examined. The results were compared with drug concentrations in blood samples. Most of the drugs and their metabolites were detected from fingerprints at 7 days after drug administration. The fingerprint sample preparation is rapid (ca. 3 min) and simple, and the limits of detection were 0.1 pg/fingerprint for dihydrocodeine, chlorpheniramine, and methylephedrine. We demonstrate that drugs can be detected in fingerprints at later sampling times with more rapid and simpler sample preparation than in blood. The method should be applicable to drug testing in criminal investigations. [ABSTRACT FROM AUTHOR]

Background: A comparative study of the use of mean centering of ratio spectra and inverse least squares for the resolution of paracetamol, methylparaben, propylparaben, chlorpheniramine maleate and pseudoephedrine hydrochloride has been achieved showing that the two chemometric methods provide a good example of the high resolving power of these techniques. Method (I) is the mean centering of ratio spectra which depends on using the mean centered ratio spectra in four successive steps that eliminates the derivative steps and therefore the signal to noise ratio is improved. The absorption spectra of prepared solutions were measured in the range of 220-280 nm. Method (II) is based on the inverse least squares that depend on updating developed multivariate calibration model. The absorption spectra of the prepared mixtures in the range 230-270 nm were recorded. Results: The linear concentration ranges were 0-25.6, 0-15.0, 0-15.0, 0-45.0 and 0-100.0 μg mL-1 for paracetamol, methylparaben, propylparaben, chlorpheniramine maleate and pseudoephedrine hydrochloride, respectively. The mean recoveries for simultaneous determination were between 99.9-101.3% for the two methods. The two developed methods have been successfully used for prediction of five-component mixture in Decamol Flu syrup with good selectivity, high sensitivity and extremely low detection limit. Conclusion: No published method has been reported for simultaneous determination of the five components of this mixture so that the results of the mean centering of ratio spectra method were compared with those of the proposed inverse least squares method. Statistical comparison was performed using t-test and F-ratio at P = 0.05. There was no significant difference between the results. [ABSTRACT FROM AUTHOR]

In experiments on mice, we examined the effects of 3-min-long forced swimming sessions on indices characterizing the state of the nociceptive system. Thirty minutes after the forced swimming episode, significantly shorter ( P < 0.05) latencies of motor reactions in the hot plate and tail flick tests were observed. At the same time, times of licking the paw within the early and late phases of the formalin test, as well as numbers of writhings in the acetic acid test, became significantly ( P < 0.05) smaller. Thus, forced swimming-induced stress results in the development of a hypoalgesia state with respect to thermoinduced pain and chemoinduced somatic (formalin test) and visceral (acetic acid test) pain. Blockers of histamine H1 (cimetidine, 10 mg/kg) and H2 (chlorpheniramine, 15 mg/kg) receptors did not influence significantly ( P > 0.05) the intensity of forced swimming-induced hypoalgesia in the tail flick and acetic acid-induced (writhing) tests. Thus, the histaminergic system is not significantly involved in the mechanisms of forced swimming-induced hypoalgesia. [ABSTRACT FROM AUTHOR]

Chlorpheniramine is an anti-histamine agent on IgE-mediated inflammation. In order to investigate the immunomodulatory effects of chlorpheniramine, we assessed the changes of peripheral mononuclear cell populations and other general clinical parameters, including hematology and clinical chemistry, following chlorpheniramine administration in rats. Since prednisolone is commonly co-prescribed with anti-histamine in many hypersensitive reactions, we also examined the changes to compare the results after the prednisolone administration. Chlorpheniramine (50, 100 and 200 ∝g/kg) and prednisolone (1, 2 and 4 mg/kg) were intramuscularly administered to female Sprague-Dawley (SD) rats 3 times, at intervals of 1 week. Except the clinical signs, such as stiffness and abnormal gait due to the local toxicity at injection sites, no other significant changes in body weights, urinalysis, and macroscopic examination were noted in the animals given chlorpheniramine. On the other hand, white blood cells, especially B cells and monocytes, showed a dose-dependent increase in the chlorpheniramine-treated animals; whereas, the numbers of both B and T cells (helper T and cytotoxic T, NKT cells) were decreased in the prednisolone-treated animals. Taken together, these results suggest that chloropheniramine administration enhances white blood cells in the peripheral blood, mostly due to increases of the B cells and monocytes, but no T cells and NK cells. [ABSTRACT FROM AUTHOR]

Background: There is an increasing evidence of medicines related issues such as inappropriate prescribing among older people. Inappropriate prescribing is an important risk factor for adverse drug reactions and hospitalizations in the older people. Objective : To assess and characterize the prevalence of Potentially Inappropriate Medications (PIMs) in nursing home care in Malaysia as defined by Screening Tool of Older Peoples Prescriptions (STOPP) and Beers criteria. Setting : Four Nursing Homes situated in Penang, Malaysia. Methods : A multicenter and cross-sectional study was conducted over 2 months period at four large non-governmental organizations nursing homes in Penang, Malaysia. The study population included older residents (≥65 years old) taking at least one medication. Residents who had been diagnosed with dementia or taking anti dementia drugs, delirium, too frail or refused to give consent were excluded. Demographic, clinical data and concurrent medications were collected through direct interview and also by reviewing medical records. STOPP and Beers criteria were applied in the medical review to screen for PIMs. Main Outcome measure : Potentially Inappropriate Medication using STOPP and Beers criteria. Results : Two hundred eleven residents were included in the study with the median age of 77 (inter quartile range (IQR) 72-82) years. Median number of prescription medicines was 4 (IQR 1-14). STOPP identified less residents (50 residents, 23.7 %) being prescribed on PIMs compared with Beers criteria (69 residents, 32.7 %) ( p < 0.001). There was a significant difference in the number of residents with PIMs detected by STOPP (23.7 %) and by Beers criteria (32.7 %), p < 0.001. The common identified PIMs by Beers criteria included nifedipine short acting, chlorpheniramine and diphenhydramine. The STOPP identified first generation antihistamines, duplication of drug classes, glibenclamide and anticholinergic agents. Higher number of medications (OR = 1.405 [1.193-1.654]; OR = 1.447 [1.215-1.723]) and longer stay at nursing home (OR = 1.132 [1.045-1.226]; OR = 1.133 [1.034-1.241]) were identified as predictors for both Beers and STOPP PIMs. Conclusion: Potentially inappropriate medications are highly prevalent among older residents living in the nursing homes and are associated with number of medications and longer nursing home stay. Further research is warranted to study the impact of PIMs towards health related outcomes in these elderly. [ABSTRACT FROM AUTHOR]

Rationale: The traditional antihistamine chlorpheniramine ameliorates panic attacks, phobias, and lowered mood, and this therapeutic effect is independent of the blockade of histamine H receptors. Since chlorpheniramine inhibits the reuptake of serotonin (5-HT), the anxiolytic-like effect of chlorpheniramine may be produced by an increase in serotonergic function. Objective: To elucidate the mechanisms underlying the anxiolytic-like effects of chlorpheniramine in mice, we examined the involvement of 5-HT systems in the prefrontal cortex that is a crucial region in the regulation of emotional function. Results: Chlorpheniramine (0.05-5 mg/kg, i.p.) dose-dependently and significantly decreased the duration of freezing behavior in both the elevated open-platform and conditioned fear tests. The anti-freezing effects of chlorpheniramine (5 mg/kg, i.p.) in these tests were inhibited by pretreatment with the non-selective antagonist at 5-HT receptors, methiothepin (0.01 mg/kg, s.c.). In addition, the local injection of chlorpheniramine (10-100 ng/mouse) and 5-HT (1-10 μg/mouse) into the medial part of the prefrontal cortex (mPFC) dose-dependently and significantly decreased the duration of freezing behavior in the elevated open-platform test. In a microdialysis study, chlorpheniramine (0.5 and 5 mg/kg, i.p.) dose-dependently and significantly increased the extracellular 5-HT level in the mPFC. In addition, the local perfusion of chlorpheniramine (10 and 30 μM), but not of the selective H1 receptor antagonist, cetirizine, into the mPFC markedly increased the extracellular 5-HT level in the mPFC. Conclusion: The anxiolytic-like effect of chlorpheniramine is produced, at least in part, by the facilitation of serotonergic neurotransmission in the PFC. [ABSTRACT FROM AUTHOR]

sensitive and selective high performance liquid chromatography-peroxyoxalate chemiluminescence (PO-CL) method has been developed for the simultaneous determination of chlorpheniramine (CPA) and monodesmethyl chlorpheniramine (MDCPA) in human serum. The method combines fluorescent labeling with 4-(4,5-diphenyl-1 H-imidazole-2-yl)phenyl boronic acid using Suzuki coupling reaction with PO-CL detection. CPA and MDCPA were extracted from human serum by liquid–liquid extraction with n-hexane. Excess labeling reagent, which interfered with trace level determination of analytes, was removed by solid-phase extraction using a C18 cartridge. Separation of derivatives of both analytes was achieved isocratically on a silica column with a mixture of acetonitrile and 60 mM imidazole-HNO buffer (pH 7.2; 85:15, v/ v) containing 0.015% triethylamine. The proposed method exhibited a good linearity with a correlation coefficient of 0.999 for CPA and MDCPA within the concentration range of 0.5–100 ng/mL. The limits of detection (S/N = 3) were 0.14 and 0.16 ng/mL for CPA and MDCPA, respectively. Using the proposed method, CPA could be selectively determined in human serum after oral administration. [ABSTRACT FROM AUTHOR]

A chiral mobile phase HPLC method is described for chiral separation and determination of chlorpheniramine (CP) enantiomers in various commercial preparations. Chromatographic separation was achieved on a conventional ODS column with a mixture of aqueous sodium phosphate (5 mM) containing 0.5 mM carboxymethyl-β-cyclodextrin, methanol and triethylamine (73:25:2, v/v/v, pH 4.3) as the mobile phase. The flow rate of isocratic elution was 0.24 mL/min and peaks were detected at 224 nm. The method was applied to nine commercial CP preparations in six dosage forms and CP enantiomers were well separated without any disturbance of other ingredients or impurities present. The results showed that only one preparation was d-CP and the others were dl-CP preparations. The contents of all the preparations were found to be in the range of 97%–104% of labeled contents. This method was economical and convenient, affording sufficient accuracy, precision and reproducibility, as well as sensitivity and selectivity. [ABSTRACT FROM AUTHOR]

A high performance liquid chromatographic method has been developed for the simultaneous determination of chlorpheniramine maleate (CPM), methscoplamine nitrate (MSN) and phenylephrine hydrochloride (PEH) in sustained release capsules. The separation was carried out on a reverse-phase CN-column with use of a mobile phase consisting of 70% ( v/v) solution of acetonitrile in water containing 2% ( v/v) acetic acid and 0.005M sodium 1-hepatane sulfonate at a flow rate of 2 mL min−1. The eluted peaks were detected at 262 nm. The method is sensitive, accurate and rapid and can be used in the routine analysis of the mixture of the three compounds. [ABSTRACT FROM AUTHOR]

Chlorpheniramine (CPA) is an antihistaminic that changes the conformation of DNA and inhibits polyamine biosynthesis in mammalian cells. In the present work, we tested the effect of CPA on four genera of fungi species ( Altemaria alternata, Botrytis cinerea, Cladosporium cladosporioides and three Penicillium spp.) grown in vitro. Similar growth inhibitions of these genera were produced by 0.5 raM iprodione, CPA and histidinol, but CPA was the most effective. The CPA sensitivities of the two B. cinerea strains were different. Putrescine did not restore the fungal growth inhibited by CPA. [ABSTRACT FROM AUTHOR]

Drug interactions in reinforcing effects of over-the-counter cough syrups were investigated by utilizing place preference conditioning in rats. Dihydrocodeine (2 mg/kg, IP) induced a small, non-significant place preference. On the other hand, concurrent dosing of dihydrocodeine (2 mg/kg, IP) and a mixture (SC) of methylephedrine (4 mg/kg), caffeine (4 mg/kg) and chlorpheniramine (0.8 mg/kg) produced a significant place preference, the mean conditioning score in this group being about 3 times higher than that in the dihydrocodeine alone group. The potentiation of dihydrocodeine-conditioned place preference was observed by combination with chlorpheniramine (0.8 mg/kg, SC) alone as well as with the mixture, but neither with methylephedrine (4 mg/kg, SC) nor with caffeine (4 mg/kg, SC). Chronic infusion of the dopamine D receptor antagonist SCH23390 (1.0 mg/kg/day, SC) during conditioning abolished the appetitive effects of dihydrocodeine combined with chlorpheniramine. In conclusion, it is suggested that the potentiation of appetitive effects of dihydrocodeine is mostly due to chlorpheniramine among three ingredients in the cough syrups, and that the dopaminergic system, especially D receptor, may play an important role in the potentiation effect of chlorpheniramine on the reinforcing effects of dihydrocodeine. [ABSTRACT FROM AUTHOR]

Purpose. The effects of concomitant administration of the H-receptor antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H-receptor antagonists chlorpheniramine and diphenhydramine were studied in rabbits. Methods. A single dose of chlorpheniramine 10 mg (Group A) or diphenhydramine 10 mg (Group B) was given intravenously on three different study days as follows: 2 weeks before cimetidine administration, after giving cimetidine 100 mg/kg intravenously every 12 hours for one week, and two weeks after discontinuing the cimetidine. Serum chlorpheniramine and diphenhydramine concentrations were measured by HPLC. Histamine H-blockade was assessed by measuring suppression of the histamine-induced wheals in the skin. Results. The chlorpheniramine and diphenhydramine terminal elimination half-life values and area under the curve values were significantly increased, and the systemic clearance rates were significantly decreased, during concomitant administration of cimetidine. For each H-receptor antagonist, pharmacokinetic parameters were similar before cimetidine was co-administered and two weeks after cimetidine was discontinued. Wheal suppression produced by chlorpheniramine or diphenhydramine was increased and prolonged when cimetidine was administered concomitantly. Conclusions. Any enhanced peripheral H-blockade observed could be attributed, at least in part, to a pharmacokinetic interaction. [ABSTRACT FROM AUTHOR]

The antihistaminic effect of loratadine (160 mg) was compared in twenty-four normal male volunteers to chlorpheniramine maleate (4 mg) and placebo in a double blinded 3-way cross-over study of latin square design. After receiving single oral doses of each medication, the wheal response to serial 0.1 ml intradermal histamine (2 µg) and saline (control) injections were recorded over a 24-h period. The calculated wheal areas were compared to baseline measurements. The results were analyzed by analysis of variance. Loratadine exhibited a more pronounced inhibition of histamine wheal formation than placebo or chlorpheniramine maleate ( p<0.003). In contrast to chlorpheniramine maleate which had a duration of action of only 3 h, loratadine inhibited the response for the entire observation period between 1 and 24 h post-dose. Although sedation was observed less frequently with loratadine (Placebo, n=2; chlorpheniramine, n=3; and loratadine, n=1), the relative incidence were not statistically significant. [ABSTRACT FROM AUTHOR]

Plasma and urinary levels of chlorpheniramine (CPM) and its 2 demethylated metabolites were measured by HPLC after i.v. and oral dosing. In 5 mg (maleate) i.v. bolus studies in 2 subjects, plasma CPM levels were fitted to triexponential equations with terminal half-lives ( t) of 23 and 22 h and area of 3.6 and 3.21/kg, respectively. Intravenous data predicted hepatic blood extraction ratios for the 2 subjects to be 0.06 and 0.07, respectively. Absolute bioavailability from oral solution (10 mg) was 59 and 34%, and from tablets (8 mg) 44 and 25%, respectively, indicating extensive gut first-pass metabolism. Mean t from 7 oral fasting studies in 5 subjects was 28 h (19-43 h). Mean absorption lag time was 0.7 h (0.4-1.3 h), and mean peak time was 2.8 h (2-4 h). In 2 subjects, 6 mg solutions were given every 12 h for 9 doses; good correlation between single and multiple dose kinetics was found. Significant accumulation was demonstrated in simulation studies with frequent daily dosing. Estimated accumulation ratios vary from 4.1 to 9.4 (mean 6.5). The t from urinary data (collected for 12 days) was consistent with plasma data. The above results suggest the need to reexamine the current practice of frequent daily dosing and the use of sustained or controlled release dosage forms of this drug. The possible cause of reduced plasma clearance of CPM in renal patients is discussed. [ABSTRACT FROM AUTHOR]

The addition of the stimulant, ephedrine hydrochloride (15 mg), to the antihistamine, chlorpheniramine maleate (10 mg) is shown significantly to reduce the adverse drowsy effects of the latter upon various components of human performance. Auditory vigilance - a test of long-term attentiveness - is shown particularly to benefit from the addition of ephedrine. Whilst ephedrine does not aid simple reaction speed, it does reduce the pausing in serialchoice performance, indicative of a drowsy state, which otherwise occurs under chlorpheniramine alone. [ABSTRACT FROM AUTHOR]

The behavioral effects of the histamine H antagonists d- and l-chlorpheniramine and of the H antagonist zolantidine were determined in squirrel monkeys responding under a fixed-interval (FI) 3-min schedule of stimulus-shock termination. Although d-chlorpheniramine is known to be much more potent than l-chlorpheniramine for antagonizing H receptor-mediated effects of histamine or displacing [H]-mepyramine from histamine H receptors, similar doses of racemic chlorpheniramine and the d- and l-isomers (3.0-10.0 mg/kg) produced comparable increases in rates of responding. Zolantidine (1.0-17.0 mg/kg) did not alter or, at the highest dose, markedly decreased responding. These findings suggest that the psychomotor stimulant effects of chlorpheniramine involve actions other than the blockade of histamine H or H receptors. Selected H antagonists and cocaine are known to have comparable rateincreasing, reinforcing, and discriminative stimulus effects and, recently, the enantiomers of chlorpheniramine have been shown to displace [H]-cocaine from binding sites in CNS with approximately equal potency. Possibly, such actions mediate behavioral effects common to H antagonists and cocaine. [ABSTRACT FROM AUTHOR]