Pharmacogenomics: Applications in Drug Discovery and Pharmacotherapy

Pharmacogenomics is the scientific study which explains individual variability of drug targets and to explore the genetic basis for such changes. With the completion of human genomic study, clear relation could now be established between the drug response in relation to a person’s genome. Pharmacogenomics, also known as personalized medicine, uses the person’s genome to determine the dose and dosage regimen, so that therapy could be optimized. As with the techniques like DNA microarray technologies person’s response to a therapy can be predicted and new therapies could be assigned. In the present review, the current technologies, and past significance has been discussed

Phytoalexins: Sources and Their Pharmacological Potential

Background: Plants are easily prone towards microbial infections on exposure to microorganisms and pathogens. In order to defense, plants produce low molecular weight secondary metabolites which were later known as “Phytoalexins”. These molecules have vast therapeutic potential also. Purpose: The purpose of this review is to explore the phytoalexins and their pharmacological effects.Methods: The data included from the articles were published from Web of Science, PubMed, Medline, Scopus, and Embase by using relevant keywords including plants possessing phytoalexins and their specific biological applications.Results: The review insights the potential of phytoalexins in various diseases and to explore phytoalexins applications in human health and disease control. Conclusions: On the basis of this review it may be concluded that phytoalexins have tremendous potential in the treatment and prevention of various life-threatening diseases like diabetes mellitus, cancer, brain damage, and heart attack

Mannich Bases of 2-Substituted Benzimidazoles - A Review

Mannich bases are the end products of mannich reaction and are known as beta amino ketone carrying compounds. Mannich reaction is a carbon carbon bond forming nucleophilic addition reaction which helps in synthesizing N-methyl derivatives and many other drug molecules. Mannich base derivatives of benzimidazoles possess many pharmacological properties such as anti-oxidant, anti-inflammatory, anticancer, antiviral, anthelmintic and play an important role in medical field. As these drugs are clinically useful in treatment of microbial infections and exhibit other therapeutic activities also, so this encouraged the development of more potent, novel and clinically significant compounds. In this review synthesis and various biological activities of new mannich bases of benzimidazole derivatives reported is discussed

Synthesis,Characterization and Biological studies on Mannich Bases of 2-Substituted Benzimidazole Derivatives

In the present study novel derivatives of 2-substituted benzimidazoles were prepared via Mannich reaction and evaluated for their in vitro antimicrobial activity against two gram negative strains (Escherichia coli and Pseudomonas aeruginosa), two gram positive strains (Bacillus subtilis and Staphylococcus aureus) and fungal strains (Candida albicans and Aspergillus niger).The synthesized compounds were also screened for antioxidant activity.The newly synthesized compounds were characterized by spectral and analytical techniques.The results revealed that all the synthesized compounds have a significant antioxidant and biological activity against the tested microorganisms

A Comprehensive Review on Therapeutic Potential of Benzimidazole: A Miracle Scaffold

Background: Benzimidazole is a category of heterocyclic aromatic compounds formed from the fusion of six membered benzene with five membered imidazolering. The moiety possesses diverse biological and clinical applications. A number of studies have shown that a varied substituent around the benzimidazole nucleus results in pharmacologically active compounds of therapeutic interest. Purpose: Owing to its number of pharmacological properties, this moiety is of choice of interest in designing and synthesis of new therapeutic compounds. The existence of the benzimidazole core in numerous groups of biological agents like antimicrobial, antiviral, antiparasitic, antihypertensive, anticancer, CNS stimulant as well as depressants has made important scaffold for development of many newer therapeutic agents. There is utmost need to understand the synthesis and associated role of benzimidazole derived compounds in different diseases. Therefore, in the present review, we attempt to discuss various derivatives of benzimidazole nucleus with different pharmacological activities. Conclusion: Benzimidazoles have played a great role in discovery of drug and development. Huge attempt has been made towards benzimidazole heterocyclic-based organic compounds with great excellence that resulted in drugs with enormous biological activity. Therapeutic drugs containing benzimidazole nucleus are used in building drugs that serve to be an active area of research. This article becomes a source that will lead to discovery of new opportunities for all researchers interested in benzimidazole-based heterocyclic medicinal chemistry

Development and Optimization of Fast Dissolving Tablets of Losartan Potassium Using Natural Gum Mucilage

Current research work involves preparation of fast dissolving tablets of Losartan Potassium by direct compression method using different concentrations of Plantago ovata and Lepidium sativum mucilage as natural superdisintegrants. A two factor three level (32) factorial design is being used to optimize the formulation. Nine formulation batches (A1-A9) were prepared by taking two factors as independent variables (X1- amount of Plantago ovata mucilage and X2- amount of Lepidium sativum mucilage)were taken with three levels (+1, 0, -1). All the active blends were evaluated for precompression parameters (angle of repose, bulk density, carr’s index, hausner’s ratio) and formulated tablets were evaluated for post compression parameters (hardness, friability, weight variation, wetting time, disintegration time, water absorption ratio). In vitro drug release studies were carried out using USP II dissolution apparatus for 30 min. The software Design Expert (8.0.7.1) was used for generating experimental design, modeling the response surface and calculating the statistical evaluation. Tablet parametric tests of formulation batches (A1-A9) of FDT were found within prescribed limits.DT was observed in the range from 12±2 to 58.7±2.52 sec and WT from 10.3±1.52 to 49.7±5.13 sec for formulation batches (A1-A9). More than 87% drug release was observed in all formulation batches (A1-A9) within 15 minutes. Polynomial mathematical models, generated for various response variables using multiple linear regression analysis, were found to be statistically significant (P < 0.05). Formulation A7 was selected by the design expert software which exhibited DT (22.15sec), WT (17.31sec) and in vitrodrug release (100%) within 15 minutes

Receptor Identification: Advances in Ligands and Transmitters Discovery

Receptor identification is an integral part of drug discovery and development. By the beginning of the next millennium, the search for the natural ligands of the orphan G-protein-coupled receptors will lead to the discovery of so many new peptides that it may well double their present number. It has recently become evident that all types of chemical messengers, hormones and transmitters act through membrane receptors which constitute our largest superfamily of proteins, i.e. the G protein-coupled receptors. The development of targeted therapies has revolutionized the treatment of various chronic diseases. Receptors have well-conserved regions that are recognized and activated by hormones and neurotransmitters. These ligands are peptides, lipids or biogenic amines, and act as transmitter molecules. Identification of orphan receptors include screening, binding and reverse engineering that help to find out cysteinyl leukotriene CysLT1 and Cys T2, hepatointestinal leukotriene B4, motilin, Ghrelin, Growth hormone-releasing peptide and growth hormone secretagogue receptor and many more. Techniques involved in screening of receptors include low stringency hybridization followed by PCR-derived approaches helps to discover various orphan g protein couple recptors (oGPCR). The discovery of the oGPCR represents a hallmark in neuroscience research, and the exploitation of its numerous physiological and pathophysiological functions is a promising avenue for therapeutic applications

Preparation and Characterization of Phytosomal-Phospholipid Complex of P. Amarus and its Tablet Formulation

Present investigation was aimed at formulation, characterization and evaluation of phytosomal complex tablets for sustained delivery of Phyllanthus amarus complex. Phyllanthin, one of the active lignin present in this plant species was isolated from the aerial parts, by silica gel column chromatography employing gradient elution with hexane −ethyl acetate solvent mixture. It was obtained in high yields (1.23%), compared to reported procedures and the purity was ascertained by HPTLC analysis. Phyllanthin was characterized for M.P, UV −Visible spectrophotometry, FT-IR, 1H NMR, 13C and NMR analysis. Release kinetics was evaluated by using United States Pharmacopeia (USP)-22 type I dissolution apparatus. Scanning electron microscopy was used to visualize the effect of dissolution medium on matrix tablet surface. HPTLC was carried out for quantitative and qualitative estimation of Phyllanthin in Phyllanthus amarus and Rf of phyllanthin was found to be about 0.25. The content was found to be maximum for phytosomal complex of phyllanthus formed by vaccum drying of 1:1 drug excipient ratio. The in-vitro drug release study revealed that optimized formulation sustained the drug release for 12 hr (88.1% ± 4.1% release). Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism of drug release

A Review on Medication Errors

Role of clinical pharmacist is to provide optimal pharmaceutical care for individual patients and optimal pharmaceutical care is attained when the right drug in the correct dosage and quality reaches the right patients at the right point in time with the right information. Any preventable event that may cause or lead to inappropriate medication use or patient harm during medication to user is called medicational error and is in the control of the health care professional, patient and consumer. In this review on medication errors, prescr-ibing errors (67 %), administration errors (25%), dispensing errors (08%) were found on the basis of review of literature.Prescribing errors are the prime cause of MEs that further leads to subsequent dispensing and administration errors. Medication errors are common cause of adverse drug events or subtherapeutic outcomes of pharmaceutical care