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Journal of Chromatographic Science Jan 2016Two accurate and sensitive chromatographic methods have been developed and validated for simultaneous determination of cinnarizine (CIN) and dimenhydrinate (DIM). The...
Two accurate and sensitive chromatographic methods have been developed and validated for simultaneous determination of cinnarizine (CIN) and dimenhydrinate (DIM). The first method uses simultaneous quantitative thin layer chromatography (TLC) spectrodensitometric evaluation of them, using ethyl acetate:methylene chloride (8 : 2 by volume) as a mobile phase. Chromatograms are scanned at 254 nm. This method analyzes CIN in a concentration range of 0.5-6 µg per band with mean percentage recovery of 99.78 ± 1.001 and DIM in a concentration range of 1-6 µg per band with mean percentage recovery of 99.87 ± 1.319. The second method is high-performance liquid chromatography using methanol:acetonitrile:water [85 : 10 : 5, by volume +0.5% tri ethyl amine (TEA)] as a mobile phase. The linearity was found to be in the range of 10-60 and 5-60 µg mL(-1) for CIN and DIM, respectively. The methods were successfully applied to the simultaneous determination of CIN and DIM in bulk powder, laboratory-prepared mixtures and pharmaceutical dosage forms. The validity of results was assessed by applying standard addition techniques. The results obtained are found to agree statistically with those obtained by a reported method, showing no significant difference with respect to accuracy and precision.
Topics: Chromatography, High Pressure Liquid; Chromatography, Thin Layer; Cinnarizine; Complex Mixtures; Dimenhydrinate
PubMed: 26354946
DOI: 10.1093/chromsci/bmv103 -
Neurological Sciences : Official... Oct 2015Vestibular migraine (VM) is one of the most frequent causes of episodic vertigo, with a lifetime prevalence of 0.98%. Prophylactic therapy includes calcium channel... (Observational Study)
Observational Study
Vestibular migraine (VM) is one of the most frequent causes of episodic vertigo, with a lifetime prevalence of 0.98%. Prophylactic therapy includes calcium channel blockers, beta-blockers, antiepileptic drugs and antidepressants. We studied the association of cinnarizine 20 mg and dimenhydrinate 40 mg (Arlevertan) in a group of 22 patients affected by definite VM. Proposed therapy included one tablet twice a day for 1 month, which was repeated three times with 1 month of interval between drug intake; results were compared with those of a control group of 11 VM patients who asked to observe only lifestyle measures for migraine. The main outcome was the number of vertigo and headache crises in the 6 months before therapy and in the 6 months of follow-up. Subjects performing Arlevertan presented during the 6 months of therapy a decrease of vertigo attacks from 5.3 to 2.1 and of headaches from 4.3 to 1.7 (p < 0.0001); 68% of these subjects reported a decrease of at least 50% of vertigo attacks, while 63% of headaches. Conversely, vertigo attacks decreased from 3.5 to 2.2 and headaches from 2.6 to 2 in patients observing only lifestyle; 18% of these subjects reported a decrease of at least 50% of vertigo crises and 27% of headaches. Our data do not differ from those of previous works assessing efficacy of different prophylactic therapies for VM and reporting consistent reduction of vertigo spells in a rate of patients ranging from 60 and 80%.
Topics: Adult; Calcium Channel Blockers; Cinnarizine; Dimenhydrinate; Drug Combinations; Female; Follow-Up Studies; Histamine H1 Antagonists; Humans; Male; Migraine Disorders; Time Factors; Treatment Outcome; Vertigo; Vestibular Diseases
PubMed: 26037548
DOI: 10.1007/s10072-015-2270-6 -
Medycyna Pracy May 2017The phenomenon of stupefying by the use of available over-the-counter drugs (OTC) among adolescents is an essential problem in both Poland and throughout the world.... (Review)
Review
The phenomenon of stupefying by the use of available over-the-counter drugs (OTC) among adolescents is an essential problem in both Poland and throughout the world. Popular analgesics, cold medicine and antihistamines contain psychedelic substances, such as dextromethorphan (DXM), pseudoephedrine/ephedrine, codeine (methylmorphine), dimenhydrinate, paracetamol (acetaminophren) and others. Cases of fatal addiction to dextromethorphan, one of the active substances contained in medicines, e.g., the common cold, have been reported. The test results cited by the authors clearly indicate that the use of OTC drugs, whose turnover is not controlled is a domain of females. The extent of use of drugs not prescribed by a doctor has remained for many years at a constant level. The most common poisonings with OTC drugs are caused by those that affect the respiratory system or exert analgesic or antipyretic effects. They are also used in attempted suicides, especially among females. Analyzing poisonings caused by OTC medications their seasonality has been observed. Their number increases during spring-autumn. A territorial differentiation in areas of OTC drug trade in terms of their quantities, with the predominance of southern regions is also noted. Intoxication with psychoactive substances causes the deterioration of relations between young people. In the reviewed studies there is no detailed information on the composition of non-prescription medicines. Moreover, young people have easy access to mushroom fungi, growing in nearby forests and meadows that may have hallucinogenic effects and are available in pharmacies and on the Internet. Med Pr 2017;68(3):413-422.
Topics: Adolescent; Agaricales; Female; Humans; Male; Nonprescription Drugs; Poland; Substance-Related Disorders
PubMed: 28512368
DOI: 10.13075/mp.5893.00245 -
Drug Design, Development and Therapy 2019Chemotherapy-induced nausea and vomiting (CINV) are a major burden for patients undergoing emetogenic chemotherapy. International guidelines recommend an antiemetic... (Observational Study)
Observational Study
BACKGROUND
Chemotherapy-induced nausea and vomiting (CINV) are a major burden for patients undergoing emetogenic chemotherapy. International guidelines recommend an antiemetic prophylaxis with corticosteroids, 5-HTR-antagonists and NKR-antagonists. The NKR-antagonist fosaprepitant has shown favorable results in pediatric and adult patients. There is little pediatric experience with fosaprepitant.
METHODS
This non-interventional observation study analyzed 303 chemotherapy courses administered to 83 pediatric patients with a median age of 9 years (2-17 years), who received antiemetic prophylaxis either with fosaprepitant and granisetron with or without dexamethasone (fosaprepitant group/FG; n=41), or granisetron with or without dexamethasone (control group/CG; n=42), during moderately (CINV risk 30-90%) or highly (CINV risk>90%) emetogenic chemotherapy. The two groups' results were compared with respect to the safety and efficacy of the antiemetic prophylaxis during the acute (0-24hrs after chemotherapy), delayed (>24-120hrs after chemotherapy) and both CINV phases. Laboratory and clinical adverse events were compared between the two cohorts.
RESULTS
Adverse events were not significantly different in the two groups (p>0.05). Significantly fewer vomiting events occurred during antiemetic prophylaxis with fosaprepitant in the acute (23 vs 142 events; p<0.0001) and the delayed (71 vs 255 events; p<0.0001) CINV phase. In the control group, the percentage of chemotherapy courses with vomiting was significantly higher during the acute (24%/FG vs 45%/CG; p<0.0001) and delayed CINV phase (28%/FG vs 47%/CG; p=0.0004). Dimenhydrinate (rescue medication) was administered significantly more often in the CG, compared to the FG (114/FG vs 320/CG doses; p<0.0001). Likewise, in the control group, dimenhydrinate was administered in significantly more (p<0.0001) chemotherapy courses during the acute and delayed CINV phases (79 of 150; 52.7%), compared to the fosaprepitant group (45 of 153; 29.4%).
CONCLUSION
Antiemetic prophylaxis with fosaprepitant and granisetron with or without dexamethasone was well tolerated, safe and effective in pediatric patients. However, larger prospective trials are needed to evaluate these findings.
Topics: Adolescent; Antiemetics; Antineoplastic Combined Chemotherapy Protocols; Child; Child, Preschool; Cohort Studies; Dexamethasone; Drug Therapy, Combination; Female; Granisetron; Humans; Male; Morpholines; Nausea; Vomiting
PubMed: 31686784
DOI: 10.2147/DDDT.S214264 -
Drug Delivery and Translational Research Oct 2019The objective of the study was the development and in vitro characterization of a self-emulsifying drug delivery system (SEDDS) for the nasal application of...
The objective of the study was the development and in vitro characterization of a self-emulsifying drug delivery system (SEDDS) for the nasal application of dimenhydrinate. Final composition of SEDDS was established based on drug solubility and stability studies. Dimenhydrinate was loaded into the SEDDS pre-concentrates to 7.5% (m/v). The droplet size of the final SEDDS formulations was in a range between 60 and 220 nm. Permeability, as well as tissue toxicity, of the formulations was investigated using bovine nasal mucosa. Enhancement in permeation up to 2.8-fold compared to pure dimenhydrinate was confirmed. Furthermore, toxicity studies did not reveal any serious tissue damages related to the SEDDS. Additionally, irritation potential of SEDDS was evaluated in ciliary beat frequency measurements. Incorporation of dimenhydrinate into SEDDS might therefore be considered as a promising approach within the field of nasal delivery of antiemetics by utilizing permeation enhancement strategy.
Topics: Administration, Intranasal; Animals; Antiemetics; Cattle; Cilia; Dimenhydrinate; Drug Delivery Systems; Drug Liberation; Emulsions; In Vitro Techniques; Nasal Mucosa; Permeability; Solubility
PubMed: 30877627
DOI: 10.1007/s13346-019-00634-1 -
Biomolecules & Biomedicine May 2024Dimenhydrinate (DMH), used to alleviate motion sickness symptoms such as nausea, vomiting, dizziness, and vertigo, encounters limitations in oral pharmaceutical...
Dimenhydrinate (DMH), used to alleviate motion sickness symptoms such as nausea, vomiting, dizziness, and vertigo, encounters limitations in oral pharmaceutical formulations due to its poor water solubility and bitter taste. Our research hypothesized that inclusion complexation with β-cyclodextrin (β-CD) might address these drawbacks while ensuring that the newly formed complexes exhibit no cytotoxic or genotoxic effects on peripheral blood mononuclear cells (PBMCs). Inclusion complexes were prepared using the kneading method and the solvent evaporation method. The phase solubility analysis, attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR), and differential scanning calorimetry (DSC) were conducted to evaluate the complexation efficacy and stability constant of the new binary systems. The results demonstrated that both methods provided complete and efficient complexation. Cytogenotoxic analysis, including the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT) assay, alkaline comet assay, and cytokinesis-block micronucleus cytome (CBMN-cyt) assay, was conducted to assess the cytogenotoxic potential of DMH-β-CD inclusion complexes, a topic previously unexamined. No cytotoxic or genotoxic effects were observed within the concentration range of 36.36 to 109.09 ng/mL. Cell viability of treated PBMCs exceeded 85% for all tested concentrations. No significant increases in DNA strand breaks were observed at any dose, and tail intensity of all complexes remained lower or up to 2.2% higher than the negative control. Parameters indicating genotoxic effects, as well as cytotoxic and cytostatic potential in the CBMN-cyt assay, did not significantly differ from untreated controls. These results suggest that inclusion complexation with β-CD might be a safe and promising solution to overcome the limitations of poor solubility and unpleasant taste of DMH, potentially providing opportunities for new and improved oral pharmaceutical dosage forms.
PubMed: 38819319
DOI: 10.17305/bb.2024.10507 -
Oman Medical Journal Jan 2016One of the major causes of mortality in children is acute gastroenteritis. Vomiting is common in early stages of the disease. The aim of this study was to determine the...
OBJECTIVES
One of the major causes of mortality in children is acute gastroenteritis. Vomiting is common in early stages of the disease. The aim of this study was to determine the effect of oral dimenhydrinate (DH) in the control of vomiting in cases of acute gastroenteritis in children.
METHODS
This double-blind, randomized, clinical trial was conducted in a university-affiliated hospital in a western province of Iran. Two hundred children aged one to 12 years old were randomly assigned to either drug or placebo groups. Children in the drug group received oral DH as four doses of 1 mg/kg every six hours (maximum 200 mg), and children in the placebo group received a placebo drug. The patients variables were compared 24 hours after receiving the first dose and at seven and 14 days after discharge.
RESULTS
The mean number of episodes of vomiting was 4.4±2.5 in the drug group versus 4.4±2.1 in the placebo group, which was not statistically significant (p<0.050). The mean number of episodes of diarrhea was 7.4±3.2 and 10.1±2.8 in the drug and placebo groups, respectively, (p<0.050). The duration of diarrhea, side effects, need to revisit, and parent's satisfaction in both groups were also significantly different (p>0.050).
CONCLUSIONS
Oral DH in children with acute gastroenteritis does not reduce the number and duration of vomiting. However, our results showed that consumption of DH in acute gastroenteritis patients was effective in reducing the frequency and duration of diarrhea and further investigation into this is warranted.
PubMed: 26813018
DOI: 10.5001/omj.2016.04 -
Journal of Clinical Psychopharmacology Feb 2015
Topics: Adult; Chronic Disease; Dimenhydrinate; Female; Humans; Psychotic Disorders; Substance-Related Disorders
PubMed: 25392935
DOI: 10.1097/JCP.0000000000000238 -
International Journal of Pharmaceutics Aug 2014The first interlaboratory testing of electronic taste sensing systems was performed within five participating centers, each working with the Insent (Insent Inc.,...
The first interlaboratory testing of electronic taste sensing systems was performed within five participating centers, each working with the Insent (Insent Inc., Atsugi-Shi, Japan) e-tongue. Preparation of the samples for the comprised four experiments, shipping of the samples and evaluation of the results was performed at the University of Duesseldorf. The sensitivity (in this case the difference between lowest and highest sensor response) and slope of the regression line values, obtained within Experiment 1 and 2, have been found to serve as applicable evaluation criterions for interlaboratory comparability. Modified sensor responses could be attributed to aged sensors, but did not influence the results of either Experiment 3, dealing with the evaluation of film formulations, or Experiment 4, dealing with the evaluation of minitablet formulations, in a great amount. Presented PCA Score and Loading Scatter Plots as well as Euclidean distance patterns based on the raw sensor responses confirmed the comparable performance of Insent e-tongues of the participating centers.
Topics: Dimenhydrinate; Electrical Equipment and Supplies; Excipients; Laboratories; Potassium Chloride; Tablets; Taste; Technology, Pharmaceutical; Tongue
PubMed: 24560640
DOI: 10.1016/j.ijpharm.2014.02.036 -
Cancer Medicine Mar 2020Previous studies have shown that forkhead box P4 antisense RNA 1 (FOXP4-AS1) is dysregulated in tumor tissues and can serve as a prognostic indicator for multiple...
Previous studies have shown that forkhead box P4 antisense RNA 1 (FOXP4-AS1) is dysregulated in tumor tissues and can serve as a prognostic indicator for multiple cancers. However, the clinical significance of FOXP4-AS1 in pancreatic ductal adenocarcinoma (PDAC) remains unclear. The goal of this study is to recognize the possible clinical significance of long noncoding RNA FOXP4-AS1 in patients with early stage PDAC. A total of 112 patients from The Cancer Genome Atlas (TCGA) PDAC cohort, receiving RNA sequencing, were involved in the study. Survival analysis, functional mechanism, and potential small molecule drugs of target therapy of FOXP4-AS1 were performed in this study. Survival analysis in TCGA PDAC cohort suggested that patients with high FOXP4-AS1 expression had significantly augmented possibility of death than in PDAC patients with lower FOXP4-AS1 expression (adjusted P = .008; adjusted HR = 2.143, 95% CI = 1.221-3.760). In this study, a genome-wide RNA sequencing dataset was used to identify 927 genes co-expressing with FOXP4-AS1 in PDAC tumor tissues. A total of 676 differentially expressed genes were identified between different FOXP4-AS1 expression groups. Functional enrichment analysis of these genes and gene set enrichment analysis for PDAC genome-wide RNA sequencing dataset was done. We have found that FOXP4-AS1 may function in PDAC by participating in biological processes and pathways including oxidative phosphorylation, tricarboxylic acid cycle, classical tumor-related pathways such as NF-kappaB as well as Janus kinase/signal transducers in addition to activators of transcription, cell proliferation, and adhesion. In addition, we also screened two potential targeted therapeutic small molecule drugs (dimenhydrinate and metanephrine) for FOXP4-AS1 in PDAC. In conclusion, our present study demonstrated that higher expression of FOXP4-AS1 in PDAC tumor tissues were related with an inferior medical outcome. Through multiple genome-wide approaches, we identified the potential molecular mechanisms of FOXP4-AS1 in PDAC and two targeted therapeutic drugs for it.
Topics: Antineoplastic Agents; Biomarkers, Tumor; Carcinoma, Pancreatic Ductal; Cell Proliferation; Citric Acid Cycle; Cohort Studies; Datasets as Topic; Female; Gene Expression Regulation, Neoplastic; Humans; Male; Middle Aged; Neoplasm Staging; Nomograms; Oxidative Phosphorylation; Pancreas; Pancreatic Neoplasms; Pancreaticoduodenectomy; RNA, Long Noncoding; RNA-Seq; Survival Analysis
PubMed: 31991068
DOI: 10.1002/cam4.2818