Posted by admin on Sep 30, 2017 in |
The renin-angiotensin system (RAS) plays an important role in pathogenesis of hypertension, congestive heart failure, and chronic renal failure. In addition to a discussion of the current understanding of the chemical structures and the modes of action of angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor (ATR) antagonists, review includes their SAR analysis and chemical modification for improving their activity. Nowadays different modeling strategies are underway to develop tailor made molecules with the best of properties among nonpeptide renin inhibitors, dual action receptor antagonists (e.g. angiotensin and endothelin antagonists, ACE/NEP inhibitors, AT1/TxA2 antagonists, balanced AT1/AT2 antagonists), triple inhibitors. In the first part is given an overview of various ACE inhibitors. The second part is devoted to overview of angiotensin receptor antagonists. The advances that have been made, new opportunities, and future directions of design and development of these classes have been...
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Posted by admin on Sep 30, 2017 in |
The skin has been used as a medium for systemic delivery of therapeutic agents. The resistance provided by the stratum corneum is the major barrier in delivering of the agents through skin. Due to this the number of drug molecules used under this category is limited. Iontophoresis is an efficient technique for physically enhancing conveyance of molecules across skin for local and systemic effects. The main feature offered by iontophoresis is the control offered by it in dose modulation by adjustment of current applied to undergo the process. It is suitable as an alternative for parenteral route as it is pain free and cost effective technique. The flux associated with iontophoretic treatment is described along with its applications in the article. The future aspects of iontophoretic treatment and the medications currently available are included in this article. Iontophoresis as a treatment regimen has gained popularity in relatively less treatment methodology but the concept should be well popularized as it offers enhancement to transdermal drug delivery system. This system being...
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Posted by admin on Sep 30, 2017 in |
Contraceptive agents are drugs or devices used by women and men in the reproductive age group, to prevent unintended pregnancies. Although various contraceptive agents are available for women and men, they are associated with health risks or lack of efficacy, and thus are insufficient to cater to the needs of the diverse target population with varying contraceptive requirements according to their socio-cultural background and individual preferences. Thus, there is a need to develop newer contraceptive agents with better risk benefit profile and greater acceptability. Thorough understanding of the complex reproductive physiology would help us in identifying various targets for developing efficacious and safe contraceptive agents. Agents with contraceptive potential need to be evaluated for its efficacy and safety in various preclinical and clinical studies before it could be granted marketing authorization. This review discusses in brief about the various in vitro tests and in vivo methods (animal models) used for evaluation of the contraceptive agents. Contraceptive agents for women can be screened for their estrogenic, anti-estrogenic, progestational, anti-progestational, anti-ovulatory...
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Posted by admin on Sep 30, 2017 in |
Hypertension is a major risk factor in the development of cardiovascular diseases and has emerged as one of the largest death causing diseases for mankind. There are number of medicines useful for treatment of high blood pressure but the main obstacle for the oral delivery of antihypertensive drugs is low bioavailability due to first pass metabolism. Also, if there is sudden increase in blood pressure, rapid onset of pharmacological action becomes necessary to enable the patients to resume their functional activities. The drug absorbed via sublingual blood vessels bypasses the hepatic first pass metabolism processes giving acceptable bioavailability with low doses and hence decreases the side effects. As sublingual area is more permeable than cheeks and palatal area of mouth, delivery by this route leads to rapid onset of action of drug. It is also convenient for patients having difficulty in swallowing. The present article gives a brief view on various research studies undertaken in the areas of sublingual delivery of antihypertensive drugs to improve the bioavailability and patient...
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Posted by admin on Aug 31, 2017 in |
In the Philippines, about 11 million suffer from arthritis. Jatropha curcas is being widely used by traditional users for treating arthritis. The study evaluated the anti-arthritic claims of J. curcas leaf extract in male albino mice with collagen type II-induced arthritis by assessing two parameters; the reduction of paw thickness due to inflammation and analysis of histopathological parameters (e.g., inflammatory cell invasion, cartilage destruction, bone erosion, synovial hyperplasia, and pannus formation). Three doses of the leaf extract were used: 250mg, 500mg and 750mg per kilogram body weight while Indomethacin and water were used as positive and negative controls respectively. Post hoc analysis showed significant reduction in the paw thickness and histopathological parameters in comparison to the positive, untreated and negative controls. The median effective dose (ED50) is 963.86 mg. The anti-arthritic activity was dose dependent. The J. curcas leaf extract is an anti-arthritic agent in male albino...
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