The main aim of the study was to determine the prescribing patterns of antibiotics with an emphasis on fluoroquinolones in the private health sector of South Africa. The empirical study followed a quantitative, descriptive, observational method using retrospective, longitudinal medicine claims data provided by a nationally representative Pharmaceutical Benefit Management company (PBM) from 1 January 2005 to 31 December 2012. Penicillins, cephalosporins, carbapenems, aminoglycosides, chloramphenicol, fluoroquinolones, macrolides, tetracyclines, sulphonamides and trimethoprim were considered in the study. A total of 5 155 262 (44.8%) patients received at least one antibiotic prescription out of the total number of registered beneficiaries included in the database. The average number of antibiotic prescriptions per patient per year ranged from 2.22 ± 1.89 (95% CI 2.22-2.22) in 2005 to 1.98 ± 1.62 (95% CI 1.98-1.99) in 2012. The number of antibiotics per prescription per year remained fairly constant at 1.05 ± 0.19 (95% CI 1.05-1.05) in 2005 to 1.06 ± 0.21 (95% CI 1.06-1.06) in 2012. The prevalence of patients receiving antibiotic prescriptions decreased from 46.1% (n = 789 247) in 2005 to 38.2% (n = 480 159) in 2012. Antibiotics were mostly prescribed for females (54.9%, n = 2 831 686) and in patients aged 0 to 18 years (26.5%, n = 1 366 824) and least in patients above 65 years (9.5%, n = 490 496). The prevalence of patients receiving antibiotic prescriptions was highest in Gauteng (41.9%, n = 2 159 360) and lowest in the Northern Cape (1.7%, n = 87 720). Antibiotics were mostly prescribed during the winter period. Penicillins were the most prescribed antibiotics (43%) and carbapenem the least (0.1%) out of the total number of antibiotics claimed. No practically significant association was found between antibiotic prescribing and gender, age, province and season. A total of 1 983 622 prescriptions for fluoroquinolones were claimed in patients older than 18 years. The average number of fluoroquinolone prescriptions per patient per year ranged from 1.45 ± 0.92 (95% CI 1.44-1.45) in 2005 to 1.31 ± 0.71 (95% CI 1.31-1.32) in 2012. The highest prevalence of fluoroquinolone prescribing was observed in females (64.1%, n = 850 253) and in patients between 45 and 65 years (38.6%, n = 511 542). The total fluoroquinolone use by the study population decreased from 2.85 DID in 2005 to 2.41 DID in 2012. Norfloxacin was the only first-generation fluoroquinolone prescribed. The second-generation fluoroquinolones accounted for more than 50% of the total DID, with ciprofloxacin being the most used active ingredient in this generation. Moxifloxacin was the most prescribed third-generation fluoroquinolone; its use ranging from 0.51 DID in 2005 to 0.44 DID in 2012. Between 2005 and 2012, a total of 57 325 prescriptions for fluoroquinolones were claimed by patients 18 years and younger. The prevalence of patients receiving fluoroquinolone prescriptions decreased from 3.6% (n = 8 329) in 2005 to 2.9% (n = 3 310) in 2012. Fluoroquinolones were mostly prescribed to females and in patients between 12 and 18 years. In all age groups, prescribing was mainly done by general medical practitioners. Ciprofloxacin was the most prescribed fluoroquinolone, followed by levofloxacin. In conclusion, this study established estimates on the prevalence of antibiotic prescribing covering an eight-year period. Secondly, baseline estimates for fluoroquinolone prescribing in adults using the ATC/DDD methodology were determined. Fluoroquinolone prescribing patterns in children and adolescents were determined, with specific reference to the comparison between the prescribed daily and recommended daily dosages in the different age groups and by prescribers’ specialties. / MPharm (Pharmacy Practice), North-West University, Potchefstroom Campus, 2015

The Gram-negative bacterium Pseudomonas aeruginosa is a life-threatening nosocomial pathogen due to its generally low susceptibility toward antibiotics. Furthermore, many strains have acquired resistance mechanisms requiring new antimicrobials with novel mechanisms to enhance treatment options. Proline-rich antimicrobial peptides, such as the apidaecin analog Api137, are highly efficient against various Enterobacteriaceae infections in mice, but less active against P. aeruginosa in vitro. Here, we extended our recent work by optimizing lead peptides Api755 (gu-OIORPVYOPRPRPPHPRL-OH; gu = N,N,N′,N′-tetramethylguanidino, O = L-ornithine) and Api760 (gu-OWORPVYOPRPRPPHPRL-OH) by incorporation of Ile-Orn- and Trp-Orn-motifs, respectively. Api795 (gu-O(IO)2RPVYOPRPRPPHPRL-OH) and Api794 (gu-O(WO)3RPVYOPRPRPPHPRL-OH) were highly active against P. aeruginosa with minimal inhibitory concentrations of 8–16 and 8–32 μg/mL against Escherichia coli and Klebsiella pneumoniae. Assessed using a quartz crystal microbalance, these peptides inserted into a membrane layer and the surface activity increased gradually from Api137, over Api795, to Api794. This mode of action was confirmed by transmission electron microscopy indicating some membrane damage only at the high peptide concentrations. Api794 and Api795 were highly stable against serum proteases (half-life times >5 h) and non-hemolytic to human erythrocytes at peptide concentrations of 0.6 g/L. At this concentration, Api795 reduced the cell viability of HeLa cells only slightly, whereas the IC50 of Api794 was 0.23 ± 0.09 g/L. Confocal fluorescence microscopy revealed no colocalization of 5(6)-carboxyfluorescein-labeled Api794 or Api795 with the mitochondria, excluding interactions with the mitochondrial membrane. Interestingly, Api795 was localized in endosomes, whereas Api794 was present in endosomes and the cytosol. This was verified using flow cytometry showing a 50% higher uptake of Api794 in HeLa cells compared with Api795. The uptake was reduced for both peptides by 50 and 80%, respectively, after inhibiting endocytotic uptake with dynasore. In summary, Api794 and Api795 were highly active against P. aeruginosa in vitro. Both peptides passed across the bacterial membrane efficiently, most likely then disturbing the ribosome assembly, and resulting in further intracellular damage. Api795 with its IOIO-motif, which was particularly active and only slightly toxic in vitro, appears to represent a promising third generation lead compound for the development of novel antibiotics against P. aeruginosa.

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Hintergrund: Zahlreiche Studien haben den therapeutischen Nutzen von systemischem Antibiotika in der Behandlung schwerer Parodontitis gezeigt. Bisher ist allerdings noch nicht geklärt, welches antibiotische Behandlungkonzept das Geeignetste ist. Daher sollen in einer randomisierten, klinischen Blindstudie zwei verschiedene, systemische Antibiotika adjuvant zur konventionellen, instrumentellen Behandlung von Patienten mit rapid progressiver Parodontitis (RPP) miteinander verglichen werden. Material und Methode: 33 Patienten mit klinisch und radiologisch gesicherter RPP-Diagnose wurden auf 2 Gruppen verteilt: (1) AM-Gruppe (n=17): 500 mg Amoxicillin und 250 mg Metronidazol (3*/ Tag - 10 Tage), (2) D-Gruppe (=16) 200mg Doxycyclin am 1.Tag und 100mg Doxycyclin 13 Tage. Zu Beginn erhielten alle Patienten 3* eine professionelle Zahnreinigung, und anschlie§end Scaling und Wurzelglättung unter Lokalanästhesie in 2 Sitzungen. 3 Monate später wurde ein Recall und die Antibiose durchgeführt. Im Abstand von jeweils 3 Monaten erfolgten 2 weitere Recallsitzungen. Nach erfolgreicher Mundhygieneinstruktion und zu allen Recallsitzungen wurden alle klinischen Parameter wie Taschentiefe, relatives Attachmentlevel und das Bluten bzw. Pus nach Sondieren mit der Florida probe eruiert. Die Bestimmung 8 verschiedener Parodontalpathogene wurde mit dem DNS-Sondentest von Meridol durchgeführt. Die mikrobiologischen Proben wurden mit sterilen Papierspitzen an den vier tiefsten Taschen vor der Antibiose und zu den anschlie§enden Recalls entnommen und mit der Gensondentechnik im Labor der Wybert GmbH elmex Forschung, Lörrach, analysiert. Zur Bestimmung des IL-1-Genpolymorphismus wurde venöses Blut in der 1. Sitzung abgenommen. Die Auswertung erfolgte mit dem GenoType(R) PRTest (Hain Diagnostika GmbH). Ergebnisse: Die klinischen Parameter zeigen sowohl durch die konservative als auch durch die antibiotisch adjuvante Therapie eine signifikante klinische Verbesserung (p / Background: Several studies have shown a therapeutical benefit from systemic antibiotics in the treatment of severe periodontitis. However, it has not yet been layed down which concept of antibiotic treatment is the best. Therefore the purpose of this study is to compare two different systemic antibiotics adjunctive to a conventional, mechanical treatment of patients with rapidly progressive periodontitis (RPP) in a randomised, blinded, clinical trial. Material and methods: 33 patients with a clinically and radiographically confirmed diagnosis of RPP were distributed in two groups: (1) AM-group (n=17): 500 mg amoxicillin and 250 mg metronidazole (3*/ d - 10days), (2) D-group (=16) 200mg doxycyclin on the 1st day and 100mg doxycyclin for 13days. In the beginning the patients received 3* professional tooth cleaning, and subsequently scaling and root planning under local anaesthesia in two sessions. 3 months later a recall visit and the antibiotic regimen were carried out. In 3 months-intervals another 2 recall visits were performed. After successfull oral hygiene instructions and during all recall visits all clinical parameters like pocket depths, relative attachment level, and bleeding and pus on probing were evaluated with the Florida probe. The determination of 8 different periodontal pathogens was performed with the DNS-Sondentest of Meridol. Before the antibiotic treatment and during the following recall visits the microbiological samples were taken from the 4 deepest pockets with sterile paper points and analysed by PCR-technique in the laboratory of Wybert GmbH elmex Forschung, Lörrach. To determine the IL-1 genetic polymorphism venous blood samples were taken in the first session. The analysis was done by GenoType(R), PRTest (Hain Diagnostika GmbH). Results: The clinical parameters show a significant clinical improve by the conservative as well as by the adjunctive antibiotic treatment (p

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