The Risk of Drug-Drug Interactions with Paracetamol in a Population of Hospitalized Geriatric Patients

Aims. This study investigates the consumption of paracetamol and the risk of potential drug-drug interactions and assesses the clinical impact hereof in patients admitted to a department of geriatric medicine. Methods. A retrospective and longitudinal study was conducted in patients who had been receiving paracetamol upon or during hospitalization. The hospital files of the included patients were reviewed, including documentation of concomitant medications, diagnoses, biochemical values, and adverse incidents during admission. These parameters were used as a clinical follow-up when assessing a clinical probability impact of the identified drug-drug interactions. Results. In total, 104 patients were admitted during the study period. 91 (87.5%) of these (mean age 86 years) received a prescription or were treated with paracetamol. Of these, 10% were evaluated as being at risk of potential drug-drug interactions with paracetamol. Seven of the potential drug-drug interactions were related to treatments with warfarin, one with valsartan and one with phenytoin. Of the nine patients at risk, six did experience either abnormal biochemical values or potential related clinical incidents. Four patients experienced increased INR (range 3.2–4.6), of which one patient suffered from anaemia and one with hematemesis. Two patients experienced increased ALAT/ASAT (55/42 U/I and 87/51 U/I, both females). One experienced hypertension. Conclusion. A large majority of the patients in this study received treatment with paracetamol. Six patients were evaluated as having abnormal biochemical values or were experiencing clinical incidents during their hospitalization potentially related to the identified potential drug-drug interactions.

Over the Counter Sale of Antibiotics at Drug Stores Found in Mizan-Aman Town, Southwest Ethiopia: A Cross-Sectional Simulated Client Visit Study

Background. Antibiotics are crucial drugs, particularly in the developing world, where infectious diseases are a common cause of death. Misuse and overuse of antibiotics have driven the emergency of antibiotic-resistant bacteria, which in turn leads to a loss of efficacy of these drugs. This study aimed to assess the professional practice on OTC sale of antibiotics at community drug retail outlets found in Mizan-Aman town. Methods. A cross-sectional simulated client visit study was conducted among community drug retail outlets found in Mizan-Aman town, Southwest Ethiopia, from 14 to 28 March, 2018. Currently, there are 18 commercially licensed community drug retail outlets in Mizan-Aman town and the study was undertaken on all drug retail outlets. Each drug retail outlet was visited once by investigators who simulated inflicting clinical scenario according to simulated client method pharmacy surveys. Three different clinical scenarios were chosen and, in each of the three cases, three levels of demand were used to obtain the antibiotic. The findings of the study were entered, cleared, coded, and stored into Epi Info version 3.5.1 and exported to Statistical Package for Social Sciences (Windows version 21) and the collected data were compiled and presented as descriptive statistics using tables and figures. Results. Most, 17 (94.4%), of drug stores out of the total 18 in which all three clinical scenarios were allotted were issued antibiotics without a need of medical prescription with three different levels of demands. Antibiotics were sold without a prescription in most (94.4%) of drug stores in which a urinary tract infection clinical scenario was presented. Similarly, antibiotics were obtained without a prescription for acute diarrhea from 16 (88.9%) drug stores. With respect to sore throat simulation, antimicrobial drugs were obtained without a prescription from 14 (77.8%) drug stores. Commonly dispensed antibiotics were Metronidazole (50.0%), Ciprofloxacin (38.9%), and Amoxicillin (71.4%) for acute diarrhea, urinary tract infection, and sore throat case scenarios, respectively. Only 1 drug store (5.5%) refused to dispense any kind of antibiotics. Conclusion. The results of this study demonstrate that nonprescription sales of antibiotics were highly pronounced in contrary to national guidelines regarding this practice. Most of antibiotics were dispensed without a prescription when the simulator asked any medication to alleviate his/her symptoms.

The Challenges and Knowledge Gaps in Malaria Therapy: A Stakeholder Approach to Improving Oral Quinine Use in the Treatment of Childhood Malaria in Ghana

Background. The study was undertaken to elicit the knowledge, views, and perceptions of key stakeholders on malaria, its bioburden, and treatment options, in order to ascertain the knowledge gabs and challenges, especially in the use of oral quinine in childhood malaria. Methods. A cross-sectional survey was conducted using a well-structured Likert Scale and self-administered questionnaire. The principal site of the study was a government-run children’s hospital located in the Ashiedu Keteke Sub-Metro of Accra. The study population included health workers, parents, and guardians or care givers. The participants were 300, purposively selected, and consisted of both men (41%) and women (59%) who were twenty years and above, whether employed (42%), self-employed (37%), or unemployed (21%). Results. Majority of the participants (78%) demonstrated above average knowledge of malaria. However, their awareness of the causes, modes of transmission, signs, and symptoms as well as preventive mechanisms of malaria did not result in low incidence of malaria. About 77% of the respondents agreed they would seek treatment within 24 hours once signs and symptoms are detected. Though close to 50% undertook home treatment of malaria, majority eventually sought treatment at hospital or clinic. Above 92% of respondents knew that quinine is used to treat malaria and agreed its bitter taste greatly affects compliance, especially in children. Consequently, 95% of the respondents would be glad if its bitter taste is masked. Conclusion. The study demonstrated the availability of substantial knowledge of the devastating effects of malaria, especially in children. Therefore, there is the need to ensure the availability and utilization of effective paediatric formulations in the fight against malaria. From this study, fast dissolving oral thin film with a good mouth feel, would be the formulation of choice for quinine.

Antimicrobial Resistance Profile of Different Clinical Isolates against Third-Generation Cephalosporins

Background. Drug resistant microorganisms lead to an increase in morbidity and mortality as they boost the risk of inappropriate therapy. Hence, data on antimicrobial resistance help define the best possible treatment for individual patients. Therefore, this study aimed to screen the antimicrobial resistant profile of 3rd generation cephalosporin drugs in Jimma University Specialized Teaching Hospital. Methods. A hospital based prospective cross-sectional study was conducted in Jimma University Specialized Hospital (JUSH) from April to August 2016. The clinical samples such as wound swab, urine, sputum, and stool were collected from hospitalized patients. Then, bacterial species were isolated and identified as per the standard microbiological methods. Antimicrobial susceptibility tests were carried out using various antimicrobial discs by Kirby–Bauer disc diffusion method. Results. Totally, 248 bacterial isolates were obtained from 154 (62.1%) male and 94 (37.9%) female patients. Escherichia coli (25.4%) and Staphylococcus aureus (19.0 %) were the predominant organisms isolated from specimens. About 140 (56.5%) and 149 (60.1%) of the total bacterial isolates were found to be resistant to ceftriaxone and ceftazidime, respectively. The majority of Escherichia coli isolates 46 (73%) were resistant to ceftriaxone and 41 (65%) of them were resistant to ceftazidime. Staphylococcus aureus, which accounted 19% of the total bacterial isolates, showed 23.4% and 34% resistance to ceftriaxone and ceftazidime, respectively. Among the bacterial strains revealing resistant to ceftriazone and ceftazidime, about 109 (44%) and 108 (43.5%) of them were resistant to two, three, or four other drugs, respectively. Conclusion. Bacterial resistance towards third-generation cephalosporin (ceftriaxone and ceftazidime) is escalating as more than half of the isolated strains demonstrated resistance to these drugs. Moreover, these strains also revealed multidrug resistance mainly against clinically used drugs which could render therapy unsuccessful. Therefore, in clinical use appropriate medications should be selected based on the data obtained from antimicrobial susceptibility tests.

Evaluation between the Usability and Physicochemical Property of Acyclovir Ointments

A lot of prescription medicines have become switch over-the-counter (OTC) medicines. However, additives in brand-name drugs, generic drugs, and switch OTC drugs differ; therefore, the feelings associated with the use of these medicines vary for patients. The aim of this study was to compare the physicochemical properties and the feeling of use (assuming skin as an index of usability) of acyclovir (ACV) ointments. Five ACV ointments were used: ACV-A, a brand-name drug, ACV-B and ACV-C, generic drugs, and ACV-D and ACV-E, switch OTC drugs. The physicochemical properties were evaluated by determining the content uniformity, water content, flattening, viscosity and viscoelasticity, and near-infrared (NIR) absorption spectroscopy. Skin friction was measured to evaluate the feeling associated with use. Results of the content uniformity test indicated that the ACV content was uniform, and equivalence was observed. Measurement of moisture content indicated that this parameter differed in each ointment preparation. The yield value, which was calculated by measuring flattening, was 4416.7 dyne/cm2 for ACV-A, 1175.7 dyne/cm2 for ACV-B, 2114.9 dyne/cm2 for ACV-C, 4234.5 dyne/cm2 for ACV-D, and 3620.7 dyne/cm2 for ACV-E. Measurement of viscosity and viscoelasticity revealed that viscosity increased with time and the viscoelasticity of each ointment. The second derivative of the NIR spectrum revealed that ACV-B and ACV-C had a wider spectrum of absorption than the other ointments. ACV-B had lesser friction than other ointments. These findings suggest that differences in the type and content of additives (macrogol) result in differences in the physicochemical properties of individual ointments.

Self-Medication Practices among Community of Harar City and Its Surroundings, Eastern Ethiopia

Purpose. Self-medication practice is often associated with irrational medication use. The aim of this study was to assess self-medication practices among community of Harar City and its surroundings, Eastern Ethiopia. Methods. A cross-sectional study was conducted through exit interview in selected drug outlets of Harar City among 370 clients from March to April, 2017. The data was coded and entered into epi-data and processed and analyzed using SPSS version 20. Results. Many participants practiced self-medication to alleviate their headache (30.30%), to treat their respiratory disorders (29.50%), and to treat their gastrointestinal disorders (27%). More than half (57.8%) of study participants declared that they were practicing self-medication due to prior experience and seeking less expensive service (20.50%). Two-fifths of them (40.3%) reported pharmacy professionals as source of information while 18.9% of respondents were advised by neighbors, friends, or relatives. About one-third (31.9%) of them did not have any source of information for self-medication practice. The most common type of drug used for self-medication by the participants was analgesic (42.2%). Approximately one-third (31.1%) of the subjects were expecting to be counseled by the pharmacy professionals about the drug side effects and to be helped in selecting their self-medication drug (30.3%). Conclusion. Varieties of medications were used among study participants ranging from antipain to that of antibiotics for different complaints including headache, respiratory complaints, and gastrointestinal problems. Experience with drugs and diseases as well as affordability were frequently reported reasons for self-medication practice. Participants had different views toward the role of pharmacy professionals. Hence, it is very important to educate patients on responsible use of medications and create awareness on the role of pharmacist in self-selected medication use in community.

In Vitro and In Vivo Quality Evaluation of Glibenclamide Tablets Marketed in Addis Ababa, Ethiopia

Good quality drugs fulfilling the regulatory parameters and produced per the current good manufacturing (CGMP) standards are very critical for best therapeutic outcome in patient therapy. Hence, this study assesses quality as well as physicochemical bioequivalence of five brands of glibenclamide tablets marketed in Addis Ababa using in vitro and in vivo methods. Friability, disintegration, dissolution, and assay for the content of active ingredients were evaluated using the methods described in the British Pharmacopeia (2009) and United States Pharmacopeia (2007). All the brands of glibenclamide tablets complied with the official specification for hardness, friability, disintegration, and assay. Difference factor (f1) values were less than 15 and similarity factor (f2) values were greater than 50 for all products of glibenclamide. The hypoglycemic effect of different products of glibenclamide tablets was evaluated on normoglycemic mice. The in vivo studies indicated that there is no significant difference in percent reduction of blood glucose level between the brands of glibenclamide and the innovator product (p > 0.05). Hence, based on the in vivo results and in vitro dissolution studies, the brands might be substituted with the innovator product in clinical practice.

Association of PLGA Microspheres to Carrier Pellets by Fluid Bed Coating: A Novel Approach towards Improving the Flowability of Microparticles

Micro- and nanoparticles have been vastly studied due to their biopharmaceutical advantages. However, these particles generally display very weak packing and poor mechanical properties. Hereby, a new methodology is proposed to associate poorly flowing particles to macrostructures targeting the improvement of flowability and redispersibility of the particles. Cecropia glaziovii-loaded PLGA microspheres (4.59 ± 0.04 μm) were associated with carrier pellets by film coating in a top-spray fluid bed equipment. Optimal conditions were determined employing a IV-Optimal factorial design and RGB image analysis as 1% (w/v) Kollicoat® Protect as coating polymer (2:1 weight ratio of coating suspension to carrier pellets), containing 5 mg/mL microspheres (loading of 28.07 ± 1.01 mg/g). The method led to an improvement of the overall flowability. No relevant molecular interactions between PLGA microspheres and polymers were found. Microspheres detached rapidly from the surface of the pellets, without agglomeration, when exposed to hydrodynamic forces. In vitro release profiles, prior to and after fluid bed coating, showed no relevant changes in drug release rate and extent. The methodology developed is suitable for further applications when an improvement on the flow properties and redispersibility of the product is desired. We showed an easy-to-implement methodology that can be executed without significant increase in costs.

Effect of Skin Model on In Vitro Performance of an Adhesive Dermally Applied Microarray Coated with Zolmitriptan

Franz cell studies, utilizing different human skin and an artificial membrane, evaluating the influence of skin model on permeation of zolmitriptan coated on an array of titanium microprojections, were evaluated. Full thickness and dermatomed ex vivo human skin, as well as a synthetic hydrophobic membrane (Strat-M®), were assessed. It was found that the choice of model demonstrated different absorption kinetics for the permeation of zolmitriptan. For the synthetic membrane only 11% of the zolmitriptan coated dose permeated into the receptor media, whilst for the dermatomed skin 85% permeated into the receptor. The permeation of zolmitriptan through full thickness skin had a significantly different absorption profile and time to maximum flux in comparison to the dermatomed skin and synthetic model. On the basis of these results dermatomed skin may be a better estimate of in vivo performance of drug-coated metallic microprojections.

Cocoa Pod Husk Pectin Intended as a Pharmaceutical Excipient Has No Adverse Effects on Haematological Parameters in Sprague Dawley Rats

Natural polymer research has recently become the focus of intensive research in the quest for new enabling excipients for novel drugs in pharmaceutical formulation for optimal treatment outcomes. Evaluations of some excipients have shown deleterious haematological effects of varying extents on the safety profile of these excipients. A 90-day subchronic toxicity study was conducted to evaluate the influence of cocoa pod husk (CPH) pectin on indicators for haematotoxicity. Male and female Sprague Dawley rats (SDRs) were fed with CPH pectin in doses up to 71.4 mg/kg. The effects of CPH pectin on the haematological indices, direct and total bilirubin, and the spleen were determined. The results indicated that CPH pectin did not induce any untoward toxic effects on the haematological indices, bilirubin levels, and the spleen. There were, however, elevations in MCV at day 30, which was not sustained after the 90 days. The data obtained from this study did not reveal any remarkable findings of toxicological relevance to the haematopoietic system.