COMPARATION OF EFFICACY OF DIFFERENT PERIOPERATIVE MEDICAL PREPARATION SCHEMES FOR TRANSPAPILLAR ENDOSCOPIC INTERVENTIONS

The intensity of peristaltic activity has significant impact on the duration of transpapillar endoscopic interventions and in some cases (juxtapapillary diverticulum, stenotising papillitis or severe oedema of papilla) can impede operations. Therefore, proper inhibition of duodenal peristalsis is one of the important preconditions for successful fulfilment of such procedures. The aim of the study was to carry out comparative analysis of impact of antispasmodic medications used through the perioperative period on the quality of transpapillar endoscopic interventions. Case histories of patients, who were treated at the Surgical Department of Municipal Enterprise “Sklifosovskiy Poltava Regional Clinical Hospital” for 2017-2019, were investigated, and 75 cases were chosen for further analysis. We divided our cohort in two groups depending on medications used for duodenal peristalsis inhibition: I group – hyoscine butyl bromide (1 ml 2% solution intramuscular injection); II – hyoscine butyl bromide (1 ml 2% solution intramuscular injection), and atropine (1ml 0,1% solution intramuscular injection). Time needed for selective cannulation, total procedure length, number and type of adverse events during manipulation and in early postoperative period were compared between the groups. After statistical data processing the following conclusions were made: 1) proper medical preparation significantly facilitates the implementation of transpapillar endoscopic interventions; 2) combined scheme to reduce duodenal peristalsis, which includes hyoscine butyl bromide and atropine, is not superior to hyoscine butyl bromide alone.

Palliative Sedation in COVID-19 End-of-Life Care. Retrospective Cohort Study

Background and Objectives: Descriptions of end-of-life in COVID-19 are limited to small cross-sectional studies. We aimed to assess end-of-life care in inpatients with COVID-19 at Alicante General University Hospital (ALC) and compare differences according to palliative and non-palliative sedation. Material and Methods: This was a retrospective cohort study in inpatients included in the ALC COVID-19 Registry (PCR-RT or antigen-confirmed cases) who died during conventional admission from 1 March to 15 December 2020. We evaluated differences among deceased cases according to administration of palliative sedation. Results: Of 747 patients evaluated, 101 died (13.5%). Sixty-eight (67.3%) died in acute medical wards, and 30 (44.1%) received palliative sedation. The median age of patients with palliative sedation was 85 years; 44% were women, and 30% of cases were nosocomial. Patients with nosocomial acquisition received more palliative sedation than those infected in the community (81.8% [9/11] vs 36.8% [21/57], p = 0.006), and patients admitted with an altered mental state received it less (20% [6/23] vs. 53.3% [24/45], p = 0.032). The median time from admission to starting palliative sedation was 8.5 days (interquartile range [IQR] 3.0–14.5). The main symptoms leading to palliative sedation were dyspnea at rest (90%), pain (60%), and delirium/agitation (36.7%). The median time from palliative sedation to death was 21.8 h (IQR 10.4–41.1). Morphine was used in all palliative sedation perfusions: the main regimen was morphine + hyoscine butyl bromide + midazolam (43.3%). Conclusions: End-of-life palliative sedation in patients with COVID-19 was initiated quite late. Clinicians should anticipate the need for palliative sedation in these patients and recognize the breathlessness, pain, and agitation/delirium that foreshadow death.

Scopolamine fatal outcome in an inmate after buscopan® smoking

Scopolamine is an alkaloid which acts as competitive antagonists to acetylcholine at central and peripheral muscarinic receptors. We report the case of a 41-year-old male convict with a 27-year history of cannabis abuse who suddenly died in the bed of his cell after having smoked buscopan® tablets. Since both abuse of substances and recent physical assaults had been reported, we opted for a comprehensive approach (post-mortem computed tomography CT (PMCT), full forensic autopsy, and toxicology testing) to determine which was the cause of the death. Virtopsy found significant cerebral edema and lungs edema that were confirmed at the autopsy and at the histopathological examination. Scopolamine was detected in peripheral blood at the toxic concentration of 14 ng/mL in blood and at 263 ng/mL in urine, and scopolamine butyl bromide at 17 ng/mL in blood and 90 ng/mL in urine. Quetiapine, mirtazapine, lorazepam, diazepam, and metabolites and valproate were also detected (at therapeutic concentrations). Inmates, especially when they have a history of drug abuse, are at risk to use any substance they can find for recreational purposes. In prisons, active surveillance on the management and assumption of prescribed drugs could avoid fatal acute intoxication.

Medication use and deprescribing in older patients in the last 14 days of life

Introduction Older patients may continue to receive potential inappropriate medications (PIMs) at the end of life. Application of consensus-based tools to identify PIMs may result in the identification of candidate medications for deprescribing, with the aim of overcoming the harm of inappropriate medication and improving clinical outcomes. This study aims to describe medication use and deprescribing patterns, and to assess prescribing appropriateness for older people in the last 14 days of life in the hospice setting. Methods Longitudinal, retrospective cohort study of deceased patients (≥65 years) who died between 1 January 2018 and 31 December 2018 in three hospices in a region of the United Kingdom. We identified prescribed and deprescribed medications and assessed medication appropriateness using consensus-based criteria, namely STOPPFrail[1] and criteria developed by Morin et al.[2] Unexpected/sudden deaths were excluded. Statistical analysis was conducted using SPSS statistics 26.0. Preliminary results Data collection is currently ongoing. To date, data from 69 deceased patients have been collected (mean age 76.1 years). Of these decedents, 62.3% were female and the majority (just under 90%) had cancer reported as the cause of death. During the last 14 days of life, each patient was prescribed a mean of 17 ± 5 different medications. The mean number of medications decreased significantly between day 14 and the day of death from 13.2 ± 4.4 to 9.4 ± 3.7 (P < 0.01). Six hundred and thirty-nine medications were discontinued, with just under 70% stopped in the last seven days before death. 34.9% of those discontinued were prescribed for chronic conditions and 22% were proton pump inhibitors. In most decedents, swallowing difficulty was the reason for medication discontinuation. According to the STOPPFrail criteria [1], 42 (60.1%) of decedents received at least one PIM between day 14 and the day of death. There were 59 PIMs in total for these patients; of these 20.3% were hyoscine butyl-bromide and 16.9% were gliclazide. Using the criteria developed by Morin et al [2], 103 medications were assessed as being of questionable (81.6%) or inadequate (18.4%) clinical benefit. Of these, 64.1% were initiated during hospice admission. There was a statistically significant association between medications of questionable clinical benefit and medication number during the last 14 days of life (P < 0.01). Three of the PIMs were vitamins, considered inappropriate by both sets of criteria. Prescribing of PIMs reduced as patients neared death. Conclusion A substantial proportion of older patients with life-limiting diseases receive PIMs during their last days of life. No systematic discontinuation of inappropriate medications was observed thus guidelines and resources are needed to facilitate rationalisation and deprescribing of drug treatments for older patients in the last days of life. The small sample size makes the relationship between most variables insignificant; however, data extraction is still ongoing in hospices. References 1. Lavan H, Gallagher P, Parsons C, Mahony O. STOPPFrail (Screening Tool of Older Persons’ Prescriptions in Frail adults with a limited life expectancy): Consensus validation. Age and ageing. 2017; 46 (4): 600–607. 2. Morin L, Laroche M L, Vetrano D L, Fastbom J, Johnell K. Adequate, questionable, and inadequate drug prescribing for older adults at the end of life: A European expert consensus. European Journal of Clinical Pharmacology. 2018; 74(10): 1333–1342.

Comparative study of four greenness assessment tools for selection of greenest analytical method for assay of hyoscine N-butyl bromide

The competencies of four greenness assessment tools were tested. AGREE is the best greenness tool while NEMI is the poorest one. AGREE, GAPI, and ESA are reliable greenness tools.

Survey to assess management of abdominal pain and cramping in South African pharmacy chains

Background: Most consumers with abdominal cramps and pain choose to treat them with over-the-counter (OTC) medication. Currently there are no data evaluating the approach of South African pharmacy staff to abdominal cramps and pain. The purpose of this survey was to evaluate the approach of pharmacy healthcare providers (HCPs) to abdominal pain and cramping and attitudes towards Buscopan (hyoscine butyl bromide) for treatment of abdominal cramps. Method: An online and face-to-face survey was conducted with 142 pharmacists and 82 pharmacist’s assistants from two major retail pharmacy chains. The study was commissioned by an independent research company. Results: Pharmacists and pharmacist’s assistants reported providing advice to an average of 13 patients with abdominal cramps weekly. The majority of HCPs recommended treatment based on symptoms, potential for drug interactions and safety. Only approximately half of consumers always followed the advice of the HCP. HCPs commonly saw patients who had taken inappropriate medication for their abdominal pain and cramping, including nonsteroidal anti-inflammatory drugs (NSAIDs), paracetamol and codeine-containing preparations. Overall, 85% of pharmacists recommended Buscopan for the treatment of abdominal pain and cramping, based on perceptions of efficacy, tolerability and improvement in quality of life. Conclusions: Consumers don’t always select an appropriate medication for abdominal pain and cramping, and require advice from a pharmacy HCP. Fostering trust and confidence is essential to ensure that the patient follows the advice given. Most South African pharmacy HCPs within these two major retail chain pharmacies recommend Buscopan as first line for treatment of abdominal cramps.

2-Butyl-6-phenyl-4,5-dihydropyridazin-3(2H)-one: Synthesis, In Silico Studies and In Vitro Cyclooxygenase-2 Inhibitory Activity

Pyridazinone derivatives are a great template for developing cyclooxygenase-2 (COX-2) inhibitors. The 2-butyl-6-phenyl-4,5-dihydropyridazin-3(2H)-one was prepared by reacting 6-phenyl-4,5-dihydropyridazin-3(2H)-one with n-butyl bromide in the presence of potassium carbonate. The structure of the compound was confirmed based on its FTIR, 1H-NMR, 13C-NMR, and Mass data. The molecular docking studies assessed the COX-2 binding capability of the synthesized compound. The in silico physicochemical and pharmacokinetic parameters of this compound concerning selected drugs were also calculated. The COX-2/COX-1 analysis revealed the synthesized compound as a novel potent COX-2 inhibitor, in comparison to indomethacin, with a promising physicochemical and pharmacokinetic profile.

Facile Synthesis of Propranolol and Novel Derivatives

Propranolol is one of the first medications of the beta-blocker used for antihypertensive drugs. This study reports the facile route for the synthesis of propranolol and its novel derivatives. Herein, propranolol synthesis proceeded from 1-naphthol and isopropylamine under mild and less toxic conditions. Novel propranolol derivatives were designed by reactions of propranolol with benzoyl chloride, pyridinium chlorochromate, and n-butyl bromide through esterification, oxidation reduction, and alkylation, respectively. The isolation and purity of compounds were conducted using column chromatography and thin-layer chromatography. Mass spectrometry and 1H-NMR spectroscopy were applied to identify new compounds structure. Propranolol derivatives from 2-chlorobenzoyl chloride (compound 3), 2-fluorobenzoyl chloride (compound 5), and especially acetic anhydride (compound 6) manifested high yields and significantly increased water solubility. Six semisynthetic propranolol derivatives promise to improve antioxidative and biological activities.