The emergence of drug resistant strains of Mycobacterium tuberculosis necessitates the discovery of new molecular scaffolds a priority, and the current situation even necessitates the re-engineering and repositioning of some old drug families to achieve effective control. Due to its essential nature and coupled with the absence of a human homolog, an essential and uniquely prokaryotic enzyme alanine racemase has been pursued as a target for antimycobacterial drug discovery. Biological assembly of obligatory dimer functional unit is modeled. D-Cycloserine is a rigid analog of D-alanine is chosen as scaffold for the rational design of new analogs. In this study, we present a unified approach involving homology modeling and molecular docking studies. Collectively, the results demonstrate the feasibility of using homology modeling and molecular docking studies to obtain novel alanine racemase inhibitor lead compounds that are potentially useful for development as antimycobacterial agents.
Cometriq (cabozantinib) is a pan-tyrosine kinase inhibitor. It is specifically approved for the treatment of progressive, metastatic medullary thyroid cancer.
Many drugs have disadvantages like first pass metabolism, peak and valley absorptions at different absorption sites and drug instability problems. Pulsatile drug delivery systems (PDDS) are gaining interest as they can curtail most of the above mentioned disadvantages. Besides that, we can deliver the drug based on time dependent or site dependent theories as per requirement of the therapy.
Sitagliptin is a dipeptidyl-peptidase inhibitor (DPP-4 inhibitor) that has recently been approved for the therapy of type 2 diabetes. Like other DPP-4 inhibitors its action is mediated by increasing levels of the incretin hormones glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP).
Iclusig (ponatinib) is a small-molecule dual Abl/Src protein inhibitor. It is specifically indicated for the treatment of adult patients with chronic phase, accelerated phase, or blast phase chronic myeloid leukemia (CML) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy or Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ALL) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy
Plants represent the eternal kindness of nature by all means which is really expressed in varied human culture from time immemorial. Many of the modern medicines are produced indirectly from medicinal plants, for example aspirin. Medicinal plants can provide biologically active molecules and lead structures for the development of modified derivatives with enhanced activity and /or reduced toxicity
Nicorandil, a k+ channel opener is frequently used in ischaemic heart disease (IHD). Diabetes mellitus is often associated with IHD. There is a possibility of alteration of blood glucose level (BGL) by nicorandil when used with sulfonylureas by influencing insulin release as it’s a k+ channel opener.
The emergence of drug resistant strains of Mycobacterium tuberculosis necessitates the discovery of new molecular scaffolds a priority, and the current situation even necessitates the re-engineering and repositioning of some old drug families to achieve effective control. Due to its essential nature and coupled with the absence of a human homolog, an essential and uniquely prokaryotic enzyme alanine racemase has been pursued as a target for antimycobacterial drug discovery.
Maraviroc (UK-427,857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity and favorable pharmacological properties. Maraviroc is the product of a medicinal chemistry effort initiated following identification of an imidazopyridine CCR5 ligand from a high-throughput screen of the Pfizer compound file.
Kynamro (mipomersen sodium) inhibits the ApoB-100 molecule, a protein that plays a pivotal role in the production of low-density lipoprotein (LDL). It reduces LDL-C by preventing the formation of atherogenic lipoproteins, the particles that carry cholesterol through the bloodstream.
Grapefruit is a common breakfast item, eaten cut up or imbibed as a juice. It is rich in vitamin C and a variety of other vitamins and minerals. It is cardioprotective. However, it also contains which can inhibit the cytochrome P450 3A4 in the liver and the small intestine, allowing increased bioavailability of many commonly used drugs.
Stivarga (regorafenib) is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment.
study was conducted to check the efficacy of certain herbal medicinal plants against opportunistic pathogenic bacteria. Plant extracts of Allium sativum, Zingiber officinale, Curcuma longa, Syzigium aromaticum, Trigonella foenam graeaum were extracted out by solvent extraction method .
Osphena (ospemifene) is an estrogen agonist/antagonist with tissue selective effects. It binds to estrogen receptors, resulting in the activation of estrogenic pathways in some tissues and the blockade of estrogenic pathways in other tissues.
Gongronema latifolium is an important and highly medicinal plant commonly called utazi in Nigeria. It is commonly used as spice, ad vegetable and traditional folk medicine. The kidney by the way is an essential organ and part of the urinary system and serves as natural filter of blood and removal of wastes, among other functions.
Sitavig (acyclovir) is an antiviral buccal tablet formulated on the company's proprietary Lauriad muco-adhesive technology. It is specifically indicated for the treatment of recurrent herpes labialis in immunocompetent adults. It is supplied as a tablet for oral administration.
Liptruzet (ezetimibe and atorvastatin) treats two sources of cholesterol by inhibiting both the absorption of cholesterol in the digestive tract - through ezetimibe - and the production of cholesterol in the liver - through atorvastatin.
Revlimid (lenalidomide), a thalidomide analogue, is an immunomodulatory agent specifically indicated for the treatment of patients with mantle cell lymphoma (MCL) whose disease has relapsed or progressed after two prior therapies, one of which included bortezomib.
Pneumonia is an inflammatory condition affecting the lung alveoli. Approximately 450 million people around the world were infected with pneumonia with an estimated mortality of 4 million. Chlamydophila pneumoniae is an obligate intracellular bacterium that infects humans and is a major cause of pneumonia.
Zubsolv is a sublingual tablet formulation of buprenorphine, an opioid analgesic, and naloxone, an opioid antagonist. It was designed to counteract the high effect that may arise following the intravenous injection of a disolved tablet. Combining buprenorphine and naloxone in a single tablet reduces the risk of intravenous abuse. It is specifically indicated for the maintenance treatment of opioid dependence and should be used as part of a complete treatment plan to include counseling and psychosocial support. It is supplied as a tablet for sublingual administration. The recommended target dosage of Zubsolv sublingual tablet is 11.4 mg/2.8 mg buprenorphine/naloxone/day (two 5.7/1.4 mg tablets) as a single daily dose. The dosage of Zubsolv should be progressively adjusted in increments/decrements of 1.4 mg/0.36 mg or 2.8 mg/0.72 mg buprenorphine/naloxone to a level that holds the patient in treatment and suppresses opioid withdrawal signs and symptoms.
Aim of study: The aim of this study was to establish the anti-inflammatory activity of the methanolic extract of Ocimum sanctum leaves (MEOS) with its fractions and to delineate the possible mechanism of action for MEOS. Materials and methods: The anti-inflammatory activities of MEOS along with its petroleum ether and chloroform fractions were evaluated in a Carrageenan induced model of acute inflammation. The effect of MEOS on lipopolysaccharide induced production of nitric oxide (NO) in macrophages was also studied. Results: MEOS (100, 200 and 400 mg/kg body weight) significantly reduced Carrageenan induced paw edema; chloroform fraction was most potent (66%, p < 0.001). MEOS was non-toxic up to 125 microgm/ml in mouse peritoneal macrophages wherein it (0–100 microgm/ml) reduced lipopolysaccharide induced NO production. Conclusion: MEOS possesses significant anti-inflammatory activity. Chloroform fraction of MEOS showed best anti-inflammatory activity.
Tivicay is specifically indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and children aged 12 years and older and weighing at least 40 kg. It is supplied as a tablet for oral administration.
In the present study as the methanolic extract of Lantana camara showed significant toxicity,that extract was selected for the study of invivo action of Lantana camara extract on the total protein and free aminoacid content in the Culex mosquito larvae.In the laboratory condition, 85mg/100ml was found to be very effective in creating 100% mortality of the mosquito larvae. Fourth instar mosquito larvae was put in a lethal concentration of the extract and kept them for time periods such as 2,4 and 6 hours. The LD50 of methanolic extract of Lantana camara,with respect to the larvae and was almost found to be 40mg/100ml. Within this period, the larvae showed visible symptoms of toxicity such as lack of co-ordination of movements, incapability of surfacing to take oxygen and poor response to stimuli such as touching with glass rods. A very simple observation on the pH of the larval homogenate of control and drug treated larvae showed that the homogenate of normal larvae was alkaline (pH 7.1 to 7.2) but in treated and intoxicated larvae the pH of homogenate was slightly acidic (pH 6.8 to 6.9). The protein content of whole body on wet weight basis was more than 3%.On incubating mosquito larvae in lethal concentration of Lantana camara extract,there was a gradual increase of total free amino acid together with gradual decrease in protein content.The study indicated that at the sixth hour of incubation almost 1/3rd of protein was depleted and there was a 50% increase of aminoacid that together resulted in the death of the larvae.Thus the findings proved to suggest the use of the above information in future for the formulation of effective antilarvicidal agent from the invasive weed Lantana camara, that prevents the spreading of dreadful mosquito borne diseases.
Piper betel plants and 5 strains of medically important fungi were selected for this study. Antifungal susceptibility test was performed to screen the antifungal activity of this plant against the selected fungi. Piper betel showed to possess antifungal property against 4 out of 5 strains of the fungus. Solid Phase extraction (SPE) technique was applied to Piper betel to achieve initial separation of active antifungal compound in the form of methanol fractions. These fractions were tested for their antifungal property. Piper betel showed the best antifungal activity against A. flavus.
BRINTELLIX
Generic Name : Vortioxetine;
Company : Lundbeck and Takeda Pharmaceuticals America, Inc. Approved by September 2013
Treatment for Major Depressive Disorder
Blood pressure is generally measured on in one arm – usually the non-dominant arm. However, increasing data suggests that arm to arm difference in blood pressure is common and may indicate atherosclerotic peripheral vascular disease. Other causes of inter-arm blood pressure difference include vasculitis, fibromuscular hyperplasia, connective tissue disorders, radiation arteritis, thoracic outlet compression, dissecting aortic aneurysm, and congenital abnormalities. Its presence is therefore not benign. The common etiology of this abnormality has been attributed to atherosclerosis involving the subclavian arteries. It also is a proxy for generalized atherosclerotic disease. A recent meta-analysis of 20 studies revealed that a systolic blood pressure difference of more than 15 mm Hg between the right and left arm was associated with a 2.5 greater risk of peripheral vascular disease, a 1.7 fold increase in cardiovascular mortality, and a 1.6 higher risk of all-cause death. Atherosclerosis is associated with vascular inflammation. CRP is a sensitive and reliable biomarker of this phenomenon and is frequently found elevated in patients with systolic inter-arm blood pressure difference.
Multidrug resistance is one of the serious problems faced by public health at the beginning of twenty first century. It is usually associated with significant morbidity, longer hospitalization, excess costs and mortality. Staphylococcus aureus is a common pathogen in hospital and community acquired disease that causes a wide range of infection such as skin and soft tissue infection to life threatening disease like respiratory tract infection, meningitis, endocarditis, bacteraemia, musculoskeletal infection and urinary tract infection. Approximately 90% of Staphylococcus strains are resistant to penicillin.
