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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 study has been done to know the changes of BGL after administration of low-dose nicorandil with sulfonylureas in Diabetic as well as normal rabbits. The study has been done on normal and alloxan induced diabetic rabbits by keeping them 12 hrs fasting & water ad lib. Glibenclamide was given in a dose of 50μg/kg body weight & Nicorandil was administered in a dose of 10,20,40,80 and160μg/kg body weight concurrently. The drugs were given by oral route. Normal saline treated rabbits were used as control. Blood samples were collected from marginal ear vein & BGL was estimated in the process described by Hultmann. The statistical significance was calculated by employing student “t” test. Glibenclamide per se in a dose of 50 μg/kg produced significant hypoglycemia, Nicorandil in in doses of 20μg/kg abolishes the hypoglycemic effect of glibenclamide, & in dose of 40μg/kg produced significant hyperglycemia. Nicorandil, a k+ channel opener can increase blood glucose level by its action probably on ATP sensitive k+ channel of β cells of pancreas only at a certain dose range (20 to40 μg/kg body weight doses) for 2 to 3 hours., but no change in BGL in 80 and 160 μg/kg body weight doses which are also relatively low doses than conventional dose. The sensitivity of low dose nicorandil is more than sulfonylureas on β cells of pancreas & the response is dose dependent. In alloxan induced diabetic rabbit, the change in BGL is not so marked probably due to lack of β cells of pancreas (Anupam Gupta et al. The concurrent use of sulfonylureas & nicorandil, risk or benefit. Drug discovery, 2013, 3(8), 24-26).

DRUG DISCOVERY OF THE MONTH

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Role of Aleglitazar in T2DM: a bench-to-bedside

Balasubramanian J, Narayanan N

PPARγ and PPARα are nuclear receptors mainly involved in the regulation of glucose homeostasis and lipid levels, respectively. Aleglitazar, is a dual agonist for PPARγ and PPARα for the potential simultaneous treatment of hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus (T2DM).

Drug Discovery, 2013, 3(7), 3-4

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FDA APPROVED DRUGS

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FDA approved drugs - November 2012

Brithvi V

Cometriq (cabozantinib) is a pan-tyrosine kinase inhibitor. It is specifically approved for the treatment of progressive, metastatic medullary thyroid cancer.

Drug Discovery, 2013, 3(7), 5-6

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RESEARCH

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An investigation and comparison of natural polymers as barrier Layers in predictable pulsatile drug release

Kanaka Durga Devi N, Narasimha Rao N, Sai Mrudula B, Abhinaya M

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.

Drug Discovery, 2013, 3(7), 7-12

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DRUG DISCOVERY OF THE MONTH

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A View on the first dipeptidyl peptidase 4 inhibitor - Sitagliptin

Balasubramanian J, Narayanan N

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).

Drug Discovery, 2013, 3(8), 15-16

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FDA APPROVED DRUGS

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FDA approved drugs - December 2012

Brithvi V

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

Drug Discovery, 2013, 3(8), 17-19

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DATABASE

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APMP - a web database for Active Principles in Indian Medicinal Plants

Udayakumar Mani, Raguraman R, Rajagopalan SK

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

Drug Discovery, 2013, 3(8), 20-23

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RESEARCH

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The concurrent use of sulfonylureas & nicorandil: risk or benefit

Anupam Gupta, Paras Nath

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.

Drug Discovery, 2013, 3(8), 24-26

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Antimycobacterial Drug Design: Homology Modeling and Docking Studies on Mycobacterium tuberculosis Alanine Racemase

Maruthi Prasad Palthur, Suresh Kumar Chitta

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.

Drug Discovery, 2013, 3(8), 27-36

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DRUG DISCOVERY OF THE MONTH

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Maraviroc CCR5 antagonist for HIV

Balasubramanian J, Narayanan N

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.

Drug Discovery, 2013, 3(9), 39-40

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FDA APPROVED DRUGS

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FDA approved drugs - January 2013

Brithvi V

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.

Drug Discovery, 2013, 3(9), 41-42

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PERSPECTIVE

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Grapefruit: A Nutritional Fruit Fraught with Danger of Severe Drug Interactions

Shashi K. Agarwal

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.

Drug Discovery, 2013, 3(9), 43-44

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