Hypertension is a diverse illness interlinked with cerebral, cardiovascular (CVS) and renal abnormalities. Presently, the malady is being treated by focusing on Renin-angiotensin system (RAS), voltage-gated calcium channels, peripheral vasodilators, renal and sympathetic nervous systems. Cardiovascular and renal abnormalities are associated with the overactivation of RAS, which can be constrained by angiotensin-converting enzyme inhibitors (ACEIs), angiotensin II (Ang-II) -AT1 receptor blockers (ARBs) and renin inhibitors. The latter is a new player in the old system. The renin catalyzes the conversion of angiotensinogen to Angiotensin I (Ang-I). This can be overcome by inhibiting renin, a preliminary step, eventually hinders the occurrence of the cascade of events in the RAS. Various peptidomimetics, the first-generation renin inhibitors developed six decades ago have limited drug-like properties as they suffered from poor intestinal absorption, high liver first-pass metabolism and low oral bioavailability. The development of chemically diverse molecules from peptides to nonpeptides expanded the horizon to achieving direct renin inhibition. Aliskiren, a blockbuster drug that emerged as a clinical candidate and got approved by the US FDA in 2007 was developed by molecular modeling studies. Aliskiren indicated superior to average efficacy and with minor adverse effects relative to other RAS inhibitors. However, its therapeutic use is limited by poor oral bioavailability of less than 2% that is similar to first-generation peptidic compounds. In this review, we present the development of direct renin inhibitors (DRIs) from peptidic to nonpeptidics that lead to the birth of aliskiren, its place in the treatment of cardiovascular diseases and its limitations.
Floating drug delivery system (FDDS) helps to improve the buoyancy property of the drug over the gastric fluids and hence maintain the longer duration of action. It is helpful in minimizing the dosing frequency. The density of dosage form must be less than the density of gastric contents (1.004 gm/ml) in FDDS. It may effervescent or non-effervescent system. The drugs having narrow absorption window in GIT is good candidate for the floating drug delivery system. The main objective of writing this review article is to compile the recent literature with special focus on classification, method of preparation, mechanism of action advantages and disadvantages. Keywords: Floating drug delivery system, Sustained release, controlled release, Floating tablet, Evaluation, Application, Gastro-retentive drug delivery system.
Introduction: Tobacco has been traditionally used in many parts of India which was known to be associated with many oral mucosal lesions which has higher chance for morbidity and mortality. A cross sectional study was conducted in Chidambaram population to find the prevalence of oral mucosal lesion in association with tobacco and alcohol related habits. Methods: A descriptive cross-sectional study was conducted among 2246 participants from in and around Chidambaram who attended the outpatient department, during the period of 2months (December 2019 to January 2020). Data collected using questionnaire adapted from global adult tobacco survey questionnaire followed by oral examination. Result: Among the 2246, 161 participants has the habit of using smoking, chewing tobacco and alcohol consumption. This study has the predominance of participants who have combination habits such as smoking tobacco and alcohol consumption. Among the participants with oral mucosal lesion leukoplakia has higher predominance followed by tobacco pouch keratosis and smoker’s palate. Most of the lesions were present in the buccal mucosa. Conclusion: Prevalence of premalignant lesions in association with adverse habits was significant in our study. This shows necessity for early diagnosis and Awareness should be created to the public through anti-tobacco campaign by the government and private agencies. Tobacco cessation clinics should be opened in all primary health care centre and more knowledge should be created about premalignant lesion to prevent the morbidity and mortality rate.
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