ABSTRACT

The aim of this systematic review is to analyze after that is the ‘unlicensed ’ and ‘off labelled ’drugs prescribed for children are being used safely in pediatric after population. A systematic search was made in Medline PubMed, CINAHL and Cochrane Library from 1998 to 2014 addressing the use of unlicensed and off labelled drugs in pediatric population. After that process of identification 29 studies fulfilled the criteria to be included . Total number of pediatric patients covered in the review of 29 selected publications is 3589061. Data from 16 countries are included. Unlicensed use of drug in pediatric age group starting from neonates were found to be from 1.26% - 16.8% with a maximum of 90% use of off-label use of drug in the age group of 23-36 weeks. Almost 34-36% off-label use of these drugs and 62.3% for unlicensed or off-label use of the drugs were found in critical care areas. A range of 3.3% to 76% off-label and 1.26-33%  unlicensed or unapproved drugs usage was found in the OPD and Clinical settings. The drug categories found to be used mostly are analgesic drugs 26.9% and antispasmodic drugs (31.5%). Paracetamol had 25-49% off-label use. A considerable off- label and unlicensed use is observed in pediatric population. The increase in number of studies and awareness is also evident through this review. The regulatory agencies apart from stringent rules to control unapproved use of drugs have to ensure pharmacovigilance of existing drugs. Healthcare providers should be prudent in the use of drugs weighing the risk-benefit analysis and practice informing the parents about the off- label use and start after their consent.

Keywords: Healthcare providers, Pediatric, drugs

ABSTRACT

Our aim in the present study was to evaluate the anti-obesity activity of Centella asiatica in high fat diet (HFD), Triton-X and Progesterone induced obesity in rats and mice. Ethanolic extract of Centella asiatica (EECA) was prepared and the extract is tested with different doses (100, 200 and 400mg/kg) and the efficiency of EECA is comparable to that of standard anti-obesity drug Orlistat (20mg/kg). Although food consumption was moderately increased in high fat diet fed rats, EECA administration significantly reduces weight gain in them. Serum total cholesterol (TC), triglycerides (TG), low density lipoproteins (LDL) and very low density lipoproteins (VLDL) levels were significantly (P< 0.05) lowered, while high density lipoproteins (HDL) increased in EECA administered rats. Based on our results, we find that the EECA has potential anti-obesity activity.

Keywords: Centella asiatica, HFD (high fat diet), progesterone, Triton-X, lipid levels.

ABSTRACT

The aim of the present study was to investigate the potential toxic effects of bioallethrin-based Mosquito-Repellents (MR) in non-adult rats as well as to ascertain whether the antioxidant substances such as Vitamin C and Vitamin E + Selenium  have any roles in preventing such toxic effects or not. 100 rat pups were divided into four study groups (each group consists of 25 rat pups) as Group I (control), Group II (bioallethrin), Group III (Vit C+ bioallethrin) and Group IV (Vit E+selenium+bioallethrin).  The animals in Group II, III, IV were exposed to the vapor of heated tablets including 4.2% bioallethrin 8 hours/day for a period of ninety days in a room with a volume of 23 m³. Vit C was added at a concentration of 500 mg/L to the fresh drinking water of animals in Group III. Vit E+Selenium combination was administered intraperitonally to the animals in Group IV once weekly at a dose of 50 mg/kg. According to the results, it was determined that antioxidants, particularly combination of Vitamin E+selenium administration, may be beneficial at preventing toxic effects of bioalletrin in rat pups. As a conclusion, when bioallethrin based- MR is used, Vit E+Selenium combination can be advised to prevent the effects of bioallethrin.

Keywords : Mosquito repellent, Bioallethrin, Toxicity, Vitamin C, Vitamin E, Selenium

ABSTRACT

Self-medication is an issue of great concern particularly in developing countries like Nigeria where there is unrestricted access to drugs, including prescription only medicines. There is paucity of data on self-medication among pharmacy undergraduates in Nigeria. The aim of this descriptive cross sectional study was to assess the prevalence of self-medication among undergraduate pharmacy students of the University of Uyo, Nigeria. The study was carried out between October and November, 2015, using self-administered questionnaires, which were collected in the various classes after completion. Data were analyzed using Statistical Product and Service Solutions (SPSS) Version 16.0.  The prevalence of self-medication in this study was 82.0% with most frequently reported illness being fever/malaria (33.2%). The major reasons for self-medication were mildness of the disease (48.2%) and being knowledgeable about drugs (22.5%). Analgesics (70.2%) and antibiotics (61.9%) were the two most frequently used classes of medications, most of which were obtained from pharmacy outlets (60.9%). Academic knowledge (24.7%) was the most frequently reported source of drug information for self-medication in this study. The prevalence of self-medication among undergraduate Pharmacy students of the University of Uyo was high. No demographic characteristic was found to affect self-medication practice. In other to reduce the practice of self-medication among Pharmacy undergraduates and hence minimize its attendant negative effects, efforts to promote responsible self-medication and rational drug use should be intensified in Schools of Pharmacy.

Keywords: Self-medication, Prevalence, Pharmacy undergraduates, University, Prescription.

ABSTRACT

Vital tooth bleaching is a widespread and conservative treatment for the majority of superficial extrinsic or intrinsic stains, compared to composite resin and porcelain veneers, metal and all ceramic crowns. It refers to a process that changes the tooth color without the use of restorative materials. It is a technique of proven safety, as long as certain prerequisites are met by both dentist and patient. Nowadays, a worldwide increase in the desire for whiter teeth is recorded. As part of this increased demand, tooth bleaching is usually incorporated or at least proposed in almost every therapeutic plan, at least of the anterior dental region, under the scope of minimal invasive dental procedures. In vitro and in vivo studies propose different protocols for at-home and in-office bleaching, discussing different degrees of color change and affectivity of the current bleaching products. The aim of this paper is the collection of contemporary evidence-based data concerning tooth bleaching, focusing especially on materials and techniques. Furthermore suggestions on the interpretation of the relevant research data are given. Finally, contemporary evidence-based bleaching protocols based on current bibliography are described.

Keywords: Tooth bleaching, peroxides, OTC products, protocols

ABSTRACT

Alzheimer's disease affects cognitive function through formation of ß- secretase mediated extracellular cerebral protein plaques and intracellular neurofibrillary tangles, thus its antagonism could mitigate disease progression. This project aims to identify newly obtained and optimized molecules which decrease the formation of ß -amyloid plaques through inhibition of the ß- secretase enzyme. Protein databank (PDB) depositions describing the bound coordinates of 6 lead structures complexed with ß- secretase were identified (PDB ID- 2VKM, 4B05, 4IVS, 3U6A, 3IGB, 2Q11) as leads for in silico ligand based and de novo design of novel antagonist molecules. For the first part of this study, ligands extracted from the protein were used as templates for screening ViCi Hamburg’s database. Protomols were generated for each of the ligands using the Surflex Dock suite in SYBYL-X. The molecules received through ViCi were then used as ligand sources. For the second part of the study the ligand binding affinity (LBA) of each small molecule for its cognate receptor was calculated in X-Score for baseline affinity establishment. 2D topology maps highlighting the important interactions between ligand and receptor were generated using Poseview, and noncritical moieties were computationally removed in the process of creating seed structures (n=3, 2, 3,2,2,2 respectively) on to which novel moieties were computationally introduced using the GROW module of LigBuilder. Protomol and Keysite volumes were then compared using UCSF Chimera. 1636 novel structures were generated with 253 structures being Lipinski Rule compliant. The highest ranking molecules from each pharmacophoric family were identified for optimization and in vitro validation.

Keywords: Beta- Secretase, BACE1, Alzheimer’s Disease, de novo drug design, in silico ligand- based drug design.

ABSTRACT

This project utilised abiraterone as a lead molecule for further iterative design of novel anti-prostate cancer drugs which modulate the CYP17A1 receptor. The protein data bank crystallographic deposition describing the bound co-ordinates of abiraterone and the CYP17A1 enzyme was selected. Abiraterone and the CYP17A1 were examined using structure activity relationship studies; Sybyl^®-X was used to generate the apo-receptor and abiraterone extract. For in silico ligand based drug design, ViCi^® Hamburg screened for molecules similar to abiraterone. A protomol for CYP17A1 was generated, usingSybyl^®-X, in order to probe areas of instability, within the active site region. Both abiraterone extract and the apo-receptor were later imported into X-SCORE^® to calculate the ligand binding affinity and the ligand binding energy (kcal mol^-1). A total of three seeds was generated using Sybyl^®-X, from which de novo molecules were generated, using LigBuilder^®. Novel structures divided into various families were generated having different pharmacophores and filtered in accordance to Lipinski’s rule of five. The protomol and the keysite volumes were then compared using UCSF^® Chimera.1000 molecules were generated using in silico based drug design, of which 756 were Lipinski rule compliant; 99 molecules exhibited a total score of 6 or higher, when docked into the protomol. 727 de novo molecules were generated; 465 were found to be Lipinski rule compliant and hence further used in the study for pharmacophoric evaluation. Some of the de novo molecules exhibit a pKd higher than the baseline value of 7.04, for abiraterone molecule.

Keywords: 3RUK, Abiraterone, CYP17A1, Malta, prostate cancer, protomol.

ABSTRACT

Leak from Gastrointestinal anastomosis following resection is associated with morbidity.  To address this issue, we conducted a randomized trial comparing "hand-sewn" with "stapled " anastomosis. The cases were randomly allocated depending on the affordability and availability of instrument for the procedure .A detailed history and the routine and specified investigations were carried out and the details about operation were recorded. Proper post operative  care and careful observations done. Two group made (i) Stapled and (ii) Hand Sewan 25 patients in each group. The primary outcome measure was anastomotic leak rate. Secondary outcome were duration of surgery, hospital stay and wound infection. The overall anastomotic leak rate was 14%. The leak rate was higher in hand sewn group(hand-sewn: 5/25, stapled: 2/25; p=<0.005). The stapled anastomotic technique was faster (8.5 ±.5 min vs. 25.4 ± 1.8 min; p=<0.05). In stapled bowel surgery the mean return of G.I. function occurred on 4.32th day and in hand sewn it was 5.32th or 1 day (24 hours) earlier when stapling technique was used (p. Value 0.0217) There were significant differences in the leak rates and postoperative outcome between the two techniques. The only concern is the financial issues specifically in India.

ABSTRACT

High performance liquid chromatography for estimation of Sulbactam Sodium and Ampicillin Trihydrate in their combine dosage form was developed and validated. The method was performed on Younglin Instrument  with Autochro-3000 Operation software using Varian C-18 (250 Χ 4.6 mm i.d, 5 μm particle size column and Ammonium acetate Buffer : Acetonitrile: Water (75:17:08, %v/v/v)  as mobile phase at ambient temperature. Detection was carried out at 228 nm in the concentration range 25-125 µg/ml for Sulbactam Sodium and 50-250 µg/ml for Ampicillin Trihydrate. The percentage recovery of Sulbactam Sodium and Ampicillin Trihydrate was found to be 99.15 -100.16 and 98.91-103.48 respectively.. Correlation coefficient for Sulbactam Sodium and Ampicillin Trihydrate was found 0.997 and 0.999 respectively. The Rt values for Sulbactam Sodium and Ampicillin Trihydrate were found to be 4.0 min ±0.02 and 5.97 min ±0.03 respectively. The method can successfully applicable to routine analysis.  And under Statistical analysis, Paired t-test is applied for comparison between developed method and reported method where, we reject the null hypothesis, because value of t is less than 0.05 so we can conclude that there is significance difference between the developed method and reported method for Sulbactam Sodium and Ampicillin Trihydrate.

Keywords: Sulbactam Sodium, Ampicillin Trihydrate, HPLC, Mobile phase, Column.

ABSTRACT

RP-HPLC method has been developed for the simultaneous determination of Metformin hydrochloride and Miglitol in pharmaceutical dosage form. The method is simple, precise and accurate. RP-HPLC method is based on the separation eluted using a mobile phase mixture of methanol and phosphate buffer (adjusted to pH 4.5 using ortho phosphoric acid) in a ratio of 60:40 %v/v at a flow rate of 1.0ml/min. The detection was made at 218 nm. The retention times were 3.84 for MET and 5.07min for MIG. Calibration curve was linear over the concentration range of 50-150μg/ml for Metformin hydrochloride and 5-15 μg/ml for Miglitol. The accuracy of the method was assessed by recovery studies and was found to be 99.69% for Metformin hydrochloride and 99.80% for Miglitol. The developed method was validated as per the ICH guidelines parameters like Linearity, precision, accuracy, robustness, LOD and LOQ. The results were validated as per ICH Q2 R1 guideline and were satisfactory.

Keywords: Metformin hydrochloride, Miglitol, RP-HPLC.