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Frontiers in Pharmacology 2023Self-medication is a part of the self-care practices carried out by the elderly in their environment. The aim of this case report is to show how the self-medication of...
Self-medication is a part of the self-care practices carried out by the elderly in their environment. The aim of this case report is to show how the self-medication of fluoxetine and dimenhydrinate in an older adult can induce serotoninergic and cholinergic syndromes, showing symptoms such as nausea, tachycardia, tremor, loss of appetite, memory loss, decreased vision, falls, and increased urination. An older adult who has been diagnosed with arterial hypertension, dyslipidemia, diabetes mellitus, and a recent diagnosis of essential thrombosis is the subject of this case report. After the analysis of the case, cessation of fluoxetine was recommended to avoid withdrawal symptoms, therefore decreasing the need for dimenhydrinate and the medicines used for dyspepsia. After the recommendation, the patient showed an improvement in the symptoms. Finally, the comprehensive evaluation process of the medication in the Medicines Optimization Unit achieved the detection of the problem and improved the patient's health condition.
PubMed: 36874029
DOI: 10.3389/fphar.2023.1080249 -
Experimental & Molecular Medicine Apr 2024Sarcopenia, the progressive decline in skeletal muscle mass and function, is observed in various conditions, including cancer and aging. The complex molecular biology of...
Sarcopenia, the progressive decline in skeletal muscle mass and function, is observed in various conditions, including cancer and aging. The complex molecular biology of sarcopenia has posed challenges for the development of FDA-approved medications, which have mainly focused on dietary supplementation. Targeting a single gene may not be sufficient to address the broad range of processes involved in muscle loss. This study analyzed the gene expression signatures associated with cancer formation and 5-FU chemotherapy-induced muscle wasting. Our findings suggest that dimenhydrinate, a combination of 8-chlorotheophylline and diphenhydramine, is a potential therapeutic for sarcopenia. In vitro experiments demonstrated that dimenhydrinate promotes muscle progenitor cell proliferation through the phosphorylation of Nrf2 by 8-chlorotheophylline and promotes myotube formation through diphenhydramine-induced autophagy. Furthermore, in various in vivo sarcopenia models, dimenhydrinate induced rapid muscle tissue regeneration. It improved muscle regeneration in animals with Duchenne muscular dystrophy (DMD) and facilitated muscle and fat recovery in animals with chemotherapy-induced sarcopenia. As an FDA-approved drug, dimenhydrinate could be applied for sarcopenia treatment after a relatively short development period, providing hope for individuals suffering from this debilitating condition.
Topics: Animals; Autophagy; Mice; Transcriptome; Humans; Protein Biosynthesis; Disease Models, Animal; Muscle, Skeletal; Gene Expression Profiling; Sarcopenia; Muscular Dystrophy, Duchenne
PubMed: 38556548
DOI: 10.1038/s12276-024-01189-z -
The Medical Letter on Drugs and... Oct 2019
Review
Topics: Acetazolamide; Altitude Sickness; Antiemetics; Carbonic Anhydrase Inhibitors; Central Nervous System Stimulants; Dexamethasone; Humans; Jet Lag Syndrome; Modafinil; Motion Sickness
PubMed: 31599874
DOI: No ID Found -
BMC Cancer Nov 2019Chemotherapy-induced nausea and vomiting (CINV) belong among the most burdensome side effects in hemato-oncology. Mostly, a combination of ondansetron and dexamethasone... (Observational Study)
Observational Study
Efficacy, safety and feasibility of fosaprepitant for the prevention of chemotherapy-induced nausea and vomiting in pediatric patients receiving moderately and highly emetogenic chemotherapy - results of a non-interventional observation study.
BACKGROUND
Chemotherapy-induced nausea and vomiting (CINV) belong among the most burdensome side effects in hemato-oncology. Mostly, a combination of ondansetron and dexamethasone is used as antiemetic prophylaxis in pediatric patients undergoing emetogenic chemotherapy. However, dexamethasone is prohibited in different pediatric chemotherapy protocols. Currently, data on the use of ondansetron with the new antiemetic agent fosaprepitant without dexamethasone is not available for pediatric patients.
METHODS
In this non-interventional observation study, 79 pediatric patients with a median age of 8.0 years (range 0.5-17.9 years) who received a CINV prophylaxis regimen with either fosaprepitant (4 mg/kg; maximum 150 mg) and ondansetron (as 24-h continuous infusion) (n = 40; fosaprepitant group/FG) or ondansetron only (n = 39; control group/CG) during moderately or highly emetogenic chemotherapy were analyzed. The groups were analyzed and compared for frequency of vomiting, administered doses of on-demand antiemetic dimenhydrinate and adverse events during the acute (0-24 h after chemotherapy administration) and delayed (> 24 h-120 h) CINV phases.
RESULTS
A total of 112 and 116 chemotherapy blocks were analyzed in the fosaprepitant and the control group, respectively. The emetogenic potential of the administered chemotherapy did not significantly differ (p = 0.8812) between the two cohorts. In the acute CINV phase, the percentage of patients experiencing vomiting (n = 26 patients) and the vomiting events were significantly higher (p = 0.0005 and p < 0.0001, respectively) in the CG (n = 26 patients (66.7%); 88 events) compared with the FG (n = 10 patients (25.0%); 37 events). In the delayed CINV phase, the percentage of patients experiencing vomiting and the vomiting events were also significantly higher (p = 0.0017 and p < 0.0001, respectively) in the CG (n = 31 patients (79.5%); 164 events) compared with the FG (n = 17 patients (42.5%); 103 events). Additionally, significantly more dimenhydrinate doses were administered in the CG compared with the FG patients (n = 322/n = 198; p < 0.0001). The occurrence of adverse events did not significantly differ between the two groups (p > 0.05).
CONCLUSION
Fosaprepitant (4.0 mg/kg) in addition to ondansetron, without application of dexamethasone, was well tolerated, safe, effective and superior to ondansetron only as CINV prophylaxis in pediatric patients during moderately and highly emetogenic chemotherapy.
Topics: Adolescent; Antiemetics; Antineoplastic Agents; Case-Control Studies; Child; Child, Preschool; Feasibility Studies; Female; Humans; Infant; Male; Morpholines; Nausea; Neoplasms; Ondansetron; Patient Safety; Treatment Outcome; Vomiting
PubMed: 31730451
DOI: 10.1186/s12885-019-6252-6 -
Journal of AOAC International Jun 2022Reverse phase liquid chromatography (RP-LC) is considered the most extensively used chromatographic technique in drug separation and quantification, yet its routine use...
Simple Eco-Friendly RP-LC Method for the Synchronous Separation of Six Widely Used Drugs in the Treatment of Cerebrovascular and Vestibular Disorders: Application for Analysis in Their Single and Combined Drug Products.
BACKGROUND
Reverse phase liquid chromatography (RP-LC) is considered the most extensively used chromatographic technique in drug separation and quantification, yet its routine use shows increasing environmental challenges about energy consumption, solvent used, and waste engendered. From this perception, efforts for greening the developed RP-LC methods are focused on using green solvents and reducing the amount of solvent used and waste produced.
OBJECTIVE
The target of this work is to develop an eco-friendly RP-LC method for the synchronous separation of six widely used drugs in the treatment of cerebrovascular and vestibular disorders, namely neurotropic piracetam, antihistamines dimenhydrinate, cinnarizine, and fluranizine, and vasodilators vincamine and vinpocetine.
METHOD
Separation and quantification are accomplished at ambient temperature by isocratic elution mode using acetonitrile-0.2% triethylamine (85:15 by volume) as a mobile phase at a flow rate of 1.5 mL/min on a Hypersil C18 column. UV detection and quantification are carried out at 225 nm.
RESULTS
The method is fully validated per ICH guidelines, where all analytical parameters are within the acceptable range (r > 0.9999), accuracy (≥99.55%), and precision (0.02-0.97%).
CONCLUSIONS
The method is applied for the routine analysis of the cited drugs in their single and combined drug products, and it is considered excellent in terms of greenness with respect to Eco-Scale assessment.
HIGHLIGHTS
As the routine use of the RP-LC technique shows increasing environmental challenges, efforts for greening are attempted focusing on the use of green solvents and reducing the amount of solvent used and waste produced. A simple eco-friendly RP-LC method for the synchronous separation of six widely used drugs in the treatment of cerebrovascular and vestibular disorders is developed. The method is fully validated per ICH guidelines, where all analytical parameters are within the acceptable range. The method is applied for the routine analysis of the cited drugs in their single and combined drug products.
Topics: Chromatography, High Pressure Liquid; Chromatography, Reverse-Phase; Solvents
PubMed: 35167683
DOI: 10.1093/jaoacint/qsac021 -
Pakistan Journal of Pharmaceutical... Jan 2021Development of dimenhydrinate (DMN) emulgel formulation has been described in this work with enhanced permeation for transdermal delivery of DMN for effective management...
Development of dimenhydrinate (DMN) emulgel formulation has been described in this work with enhanced permeation for transdermal delivery of DMN for effective management of motion sickness. Various DMN emulgel formulations were prepared using central composite design in response surface methodology. Propylene glycol and olive oil were used in varying ratios as permeation enhancers along-with carbopol-934 as gelling agent. Prepared formulations were evaluated by physico-chemical properties, stability and Fourier transform infrared spectroscopy (FTIR) studies. In-vitro drug release was studied using cellophane membrane. Formulation F2 showed maximum drug permeation following diffusion-based release mechanism and was used in further studies. Rat skin was used in Franz cell for ex-vivo studies to determine various permeation kinetic parameters. FTIR studies provided no evidence of chemical interaction between DMN and polymers used, whereas molecular docking revealed formation of a stable complex in the presence of aqueous environment with stable intermolecular binding and the complex was well hydrated. No evidence of skin irritation was observed in human volunteers following application of the optimized formulation. Histopathology data of the rat skin showed a decreased proliferation of the lymphocytes whereas monocytes were induced. In conclusion, combination of propylene glycol and olive oil was successfully employed for delivery of DMN through transdermal route with good permeability and prolonged release time that can be highly beneficial in treating motion sickness in unusual circumstances.
Topics: Administration, Cutaneous; Animals; Antiemetics; Dimenhydrinate; Drug Delivery Systems; Emulsions; Gels; Molecular Docking Simulation; Motion Sickness; Olive Oil; Propylene Glycol; Rats; Skin; Skin Absorption; Spectroscopy, Fourier Transform Infrared
PubMed: 34275848
DOI: No ID Found -
Brazilian Journal of Biology = Revista... 2022Chrozophora tinctoria (L.) A.Juss. is herbaceous, monecious annual plant used traditionally to cure gastrointestinal disorders. The present study was carried out to find...
Chrozophora tinctoria (L.) A.Juss. is herbaceous, monecious annual plant used traditionally to cure gastrointestinal disorders. The present study was carried out to find the bioactive compounds by Gas Chromatography-Mass Spectrometry, the acetylcholinesterase inhibitory potential acute toxicity, and emetic activity present in the ethyl acetate fraction of Chrozophora tinctoria (EAFCT) and dichloromethane fraction of Chrozophora tinctoria (DCMFCT). The compounds detected in both fractions were mostly fatty acids, with about seven compounds in EAFCT and 10 in DCMFCT. These included pharmacologically active compounds such as imipramine, used to treat depression, or hexadecanoic acid methyl ester, an antioxidant, nematicide, pesticide, hypocholesterolemic, 9,12,15-Octadecatrienoic acid, ethyl ester, (Z,Z,Z)- is used as a cancer preventive, antiarthritic, antihistaminic, hepatoprotective, insectifuge, nematicide, Pentadecanoic acid, 14-methyl-, methyl ester have antifungal, antimicrobial and antioxidant activities, 10-Octadecanoic acid, methyl ester have the property to decrease blood cholesterol, Antioxidant and antimicrobial, 1-Eicosanol is used as an antibacterial, 1-Hexadecene has antibacterial, antioxidant, and antifungal activities. Both DCMFCT and EAFCT fractions inhibited acetylcholinesterase (AChE) activity with IC50 values of 10 µg and 130 µg, respectively. Both the fractions were found to be toxic in a dose-dependent manner, inducing emesis at 0.5g onward and lethargy and mortality from 3-5 g upwards. Both the fractions combined with distilled water showed highly emetic activity. The significant increase in the number of vomits was shown by EAFCT plus distilled water which are 7.50±1.29, 7.25±3.10, and 11.75±2.22 number of vomits at 1g, 2g, and 3g/kg concentration respectively, while DCMFCT plus distilled water showed 5.25±2.22, 7.50±2.52 and 10.25±2.22 number of vomits at 1g, 2, and 3g/kg correspondingly. The antiemetic standard drug metoclopramide has a higher impact against the emesis induced by both the fractions than dimenhydrinate. Metoclopramide decreases the number of vomits caused by EAFCT to 1.00±0.00, 2.00±0.00, 4.00±1.00 at 1g, 2, and 3g/kg sequentially, while dimenhydrinate decreases the number of vomits to 1.33±0.58, 2.33±1.15, 4.33±0.58 at 1g, 2, and 3g respectively. In the same way, Metochloprimide decreases the number of emesis caused by DcmCt from 5.25±2.22, 7.50±2.52, 10.25±2.22 to 1.33±0.58, 2.33±1.1, 4.33±0.58 at 1g, 2, and 3g/kg concentrations. The present study is the first documented report that scientifically validates the folkloric use of Chrozophora tinctoria as an emetic agent.
Topics: Acetylcholinesterase; Animals; Anti-Bacterial Agents; Antifungal Agents; Antioxidants; Dimenhydrinate; Emetics; Esters; Euphorbiaceae; Gas Chromatography-Mass Spectrometry; Metoclopramide; Models, Animal; Plant Extracts; Vomiting; Water
PubMed: 35613215
DOI: 10.1590/1519-6984.260566 -
European Journal of Hospital Pharmacy :... Mar 2023Patients in the acute phase of agitation can require the administration of multiple drugs by intramuscular injection in order to temporarily stabilise their condition....
BACKGROUND
Patients in the acute phase of agitation can require the administration of multiple drugs by intramuscular injection in order to temporarily stabilise their condition. Administration of multiple psychotropic medications in a single syringe can be beneficial to both the patient and healthcare professionals. However, there are very little data in the literature regarding psychotropic drug compatibility in syringes for acute agitation.
OBJECTIVE
The aim of this study was to assess the visual compatibility of various combinations of 12 intramuscular psychotropic medications in syringes, and to validate compatibility with the use of a particle counter. The medications evaluated were benztropine mesylate, diazepam, dimenhydrinate, diphenhydramine hydrochloride, haloperidol lactate, hydroxyzine, lorazepam, loxapine, methotrimeprazine, midazolam, olanzapine and zuclopenthixol acetate.
METHODS
Compounded solutions of medication combinations underwent visual inspection initially and after 0.25, 0.5, 1, 2 and 4 hours using a white background and a black background. In order to validate the compatibility results, the presence of particulate matter was determined by light obscuration.
RESULTS
This study identified 35 combinations that were visually compatible and 35 that were visually incompatible. We chose eight highly clinically relevant combinations to test using the requirements of the United States Pharmacopoeia (USP) chapter 788 (Particulate Matter in Injections). Of those eight, six were physically compatible, including the triple combinations of lorazepam and haloperidol with either benztropine or diphenhydramine.
CONCLUSION
These physical compatibility results will give healthcare professionals an idea of the possible compatible combinations of psychotropic drugs in syringes, and thus complete some of the missing data in the literature.
Topics: Humans; Haloperidol; Lorazepam; Syringes; Psychotropic Drugs; Diphenhydramine
PubMed: 36002244
DOI: 10.1136/ejhpharm-2022-003378 -
BMJ Quality & Safety Dec 2019Benzodiazepines and sedative hypnotics (BSH) have numerous adverse effects that can lead to negative outcomes, particularly in vulnerable hospitalised older adults. At... (Comparative Study)
Comparative Study
BACKGROUND
Benzodiazepines and sedative hypnotics (BSH) have numerous adverse effects that can lead to negative outcomes, particularly in vulnerable hospitalised older adults. At our institution, over 15% of hospitalised older adults are prescribed sedative-hypnotics inappropriately. Of these prescriptions, 87% occurred at night to treat insomnia and almost 20% came from standard admission order sets.
METHODS
We conducted a time-series study from January 2015 to August 2016 among medical and cardiology inpatients following the implementation in August 2015 of a sedative reduction bundle (education, removal of BSH from available admission order sets and non-pharmacological strategies to improve sleep). Preintervention period was January-July 2015 and postintervention period was August 2015-August 2016. A surgical ward served as control. Primary outcome was the proportion of BSH-naive (not on BSH prior to admission) patients 65 years or older discharged from medical and cardiology wards who were prescribed any new BSH for sleep in hospital. Data were analysed on statistical process control (SPC) p-charts with upper and lower limits set at 3δ using standard rules. Secondary measures included Patient-reported Median Sleep Quality scores and rates of fall and sedating drug prescriptions that may be used for sleep (dimenhydrinate).
RESULTS
During the study period, there were 5805 and 1115 discharges from the intervention and control units, respectively. From the mean baseline BSH prescription rate of 15.8%, the postintervention period saw an absolute reduction of 8.0% (95% CI 5.6% to 10.3%; p<0.001). Adjusted for temporal trends, the intervention produced a 5.3% absolute reduction in the proportion of patients newly prescribed BSH (95% CI 5.6% to 10.3%; p=0.002). BSH prescription rates remained stable on the control ward. Patient-reported measure of sleep quality, falls and use of other sedating medications remained unchanged throughout the study duration.
CONCLUSION
A comprehensive intervention bundle was associated with a reduction in inappropriate BSH prescriptions among older inpatients.
Topics: Aged; Aged, 80 and over; Drug Utilization; Female; Health Education; Health Personnel; Hospitalization; Hospitals, University; Humans; Hypnotics and Sedatives; Inpatients; Male; Ontario; Prescription Drug Misuse; Sleep Initiation and Maintenance Disorders
PubMed: 31270252
DOI: 10.1136/bmjqs-2018-009241