Thursday, August 13, 2015

Dexamethasone May Help Prevent Severe Kidney Injury Following Heart Surgery

In continuation of my update on dexamethasone....Skeletal formula of dexamethasone

The anti-inflammatory drug dexamethasone helps prevent serious kidney complications that can arise following heart surgery, according to the results of a randomized clinical trial. The findings, which appear in an upcoming issue of the Journal of the American Society of Nephrology (JASN), could lead to a change in care for patients during cardiac operations.

Acute kidney injury (AKI) is one of the most devastating complications following cardiac surgery. Approximately 1% of patients undergoing cardiac surgery require dialysis to treat severe AKI that arises after surgery, and the incidence is higher among patients with pre-operative chronic kidney disease. These patients experience strikingly high death rates while in the hospital that exceed 40%. "One percent sounds like a small percentage, however given the fact that each year, over half a million people undergo heart surgery in the United States alone, this means that an estimated 5000 patients develop renal failure and of those about 2500 die as a result of this complication," said Kirolos Jacob, MD (University Medical Center, Utrecht, The Netherlands). He noted that these figures are rising due to the aging population.

Because heart surgery initiates an inflammatory reaction in the body that can have negative effects on the kidneys, Dr. Jacob and his colleagues wondered whether giving patients dexamethasone, an anti-inflammatory drug, could decrease the risk of severe AKI following cardiac surgery. The team analyzed the results of a large randomized controlled trial called the Dutch Dexamethasone for Cardiac Surgery (DECS) trial, which included 4465 patients undergoing cardiac surgery who were randomized to receive placebo or dexamethasone during surgery. The original trial tested whether dexamethasone could reduce the risk of a variety of major postoperative complications. In this analysis, the investigators specifically examined kidney failure and focused on the most severe form: AKI requiring dialysis.

Dexamethasone appeared to protect against the development of severe AKI. Patients who received the drug had about a 2.5-times lower risk of developing AKI requiring dialysis compared with those receiving a placebo.

"The beneficial effects of dexamethasone were particularly present in those who already had pre-existing kidney disease before heart surgery," said Dr. Jacob. "This reinforces the fact that this drug could be of major importance for the increasing elderly population with pre-existing kidney disease undergoing a heart operation."

Read more at : http://dx.doi.org/10.1681/ASN.2014080840

Wednesday, August 12, 2015

Potential new painkiller provides longer lasting effects ..........



Medications have long been used to treat pain caused by injury or chronic conditions. Unfortunately, most are short-term fixes or cause side effects that limit their use. Researchers at the University of Missouri have discovered a new compound that offers longer lasting painkilling effects, and shows promise as an alternative to current anesthetics.

"Because of its versatility and effectiveness at quickly numbing pain in targeted areas, lidocaine has been the gold standard in local anesthetics for more than 50 years," said George Kracke, Ph.D., associate professor of anesthesiology and perioperative medicine at the MU School of Medicine and lead author of the study. "While lidocaine is effective as a short-term painkiller, its effects wear off quickly. We developed a new compound that can quickly provide longer lasting relief. This type of painkiller could be beneficial in treating sports injuries or in joint replacement procedures."

Painkillers work by interfering with the nervous system's transmission of nerve signals that the body perceives as pain. Lidocaine is used as an injectable pain reliever in minor surgical or dental procedures, or as a topical ointment or spray to relieve itching, burning and pain from shingles, sunburns, jellyfish stings and insect bites. The new compound developed at MU, boronicaine, could potentially serve many of those same functions as an injectable or topical painkiller.
National Academy of Sciences member M. Frederick Hawthorne, Ph.D., director of MU's International Institute of Nano and Molecular Medicine and a pioneer in the field of boron chemistry, synthesized boronicaine as a derivative of lidocaine. By changing aspects of the chemical structure of lidocaine, the researchers found that the new compound provided pain relief that lasted five times longer than lidocaine. In pre-clinical, early stage studies, boronicaine provided about 25 minutes of relief, compared to about five minutes of pain relief with lidocaine.

"Although some conditions may warrant the use of a short-lasting painkiller, in many cases a longer lasting anesthetic is a better option," Kracke said. "Having a longer lasting anesthetic reduces the dosage or number of doses needed, limiting the potential for adverse side effects." While other types of painkillers can provide longer pain relief than lidocaine, they can cause heart toxicity, gastrointestinal issues and other side effects. Preliminary findings show no toxicity in single-dose studies of boronicaine, though more studies are needed.
"Boronicaine could have distinct advantages over existing painkilling medications," said Hawthorne, who also serves as the Curators' Distinguished Professor of Chemistry and Radiology at MU. "We're conducting more research into the side effects of the compound, but in time it could very well become a useful material to use as an anesthetic."

Ref : http://onlinelibrary.wiley.com/doi/10.1002/cmdc.201402369/pdf

Tuesday, August 11, 2015

Viagra to prevent transmission of the malaria parasite?



By increasing the stiffness of erythrocytes infected by the causal agent of malaria, Viagra favors their elimination from the blood circulation and may therefore reduce transmission of the parasite from humans to mosquitoes. This astonishing discovery, made by scientists from the CNRS, INSERM, Université Paris Descartes -- at the Institut Cochin -- and the Institut Pasteur, working in collaboration with a team from the London School of Hygiene and Tropical Medicine, could lead to a treatment to reduce the spread of malaria within a population. Their work is published in PLOS Pathogens on 7 May 2015.


More : http://journals.plos.org/plospathogens/article?id=10.1371/journal.ppat.1004815



Viagra to prevent transmission of the malaria parasite? 

Monday, August 10, 2015

Plant-derived compound targets cancer stem cells

In continuation of my updates on cauliflower, cabbage, broccoli

A compound and an enzyme that occur naturally in cruciferous vegetables--cauliflower, cabbage, broccoli and Brussels sprouts--may help prevent recurrence and spread of some cancers, according to researchers. When they treated human cervical cancer stem cells with phenethyl isothiocyanate (PEITC) in a Petri dish, about 75 percent died within 24 hours using a 20-micromolar concentration of the compound.  
Phenethyl isothiocyanate.svg

A compound and an enzyme that occur naturally in cruciferous vegetables -- cauliflower, cabbage, broccoli and Brussels sprouts -- may help prevent recurrence and spread of some cancers, according to associate professor Moul Dey of the South Dakota State University Department of Health and Nutritional Sciences. She has been doing research on phenethyl isothiocyanate (PEITC) through a five-year grant from the National Institutes of Health for more than $875,000 and support from the South Dakota Agricultural Experiment Station.
The precursor compound and enzyme in cruciferous vegetables combine during the chewing process to produce PEITC within the body, Dey explained. Though PEITC is a good candidate to develop as a dietary supplement, studies have also shown that sufficient cancer-preventing levels of PEITC can be achieved through diet alone.
Role of cancer stem cells
When cancer is treated with chemotherapy or radiation, the tumor disappears but the cancer stem cells live on. "These cells are frequently resistant to conventional therapies," Dey said.
Though cancer stem cells make up less than 5 percent of a tumor, they can regenerate the original tumor and migrate through the blood vessels spreading cancer to secondary locations.
"These tiny cells are very difficult to detect in a tumor," Dey pointed, adding that for a long time scientists did not even know they existed. "It's like finding a needle in a haystack."

Promising Results
When Dey and her team treated human cervical cancer stem cells with PEITC in a Petri dish, about 75 percent died within 24 hours using a 20-micromolar concentration of the compound.
In other experiments, Dey and her team have found that lower concentrations of PEITC are still very effective. Working with SDSU veterinary pathologist David Knudsen, Dey and her team found that 10-micromolar concentrations of PEITC can dramatically prevent the spread of cancer in mouse lung tissue.

"Preliminary evidence has shown a quite dramatic difference between the lung sections from the PEITC-treated and untreated mice," Dey said. However, she cautioned, although mice provide a model for human diseases, further testing is necessary to determine whether outcomes will be similar in humans.

Based on information from scientific literature, the concentrations of PEITC that Dey and her team typically use in their research -- 5 to 15 micromolars -- may be achieved through diets rich in certain types of cruciferous vegetables, particularly land and watercress.

Next, she and her team will examine how PEITC is able to overcome the resistance mechanisms that protect these stem cells from other drugs. "That's the second piece of this work," Dey added.

Friday, August 7, 2015

FDA Expands Uses of Vyvanse to Treat Binge-Eating Disorder



Lisdexamfetamine-Structural Formula V.1.svg


Lisdexamfetamine (contracted from L-lysine-dextroamphetamine) is a central nervous system (CNS) stimulant prodrug of thephenethylamine and amphetamine chemical classes. Its chemical structure consists of dextroamphetamine coupled with the essential amino acid L-lysine. Lisdexamfetamine itself is inactive and acts as a prodrug to dextroamphetamine upon cleavage of the lysine portion of the molecule.

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The U.S. Food and Drug Administration today expanded the approved uses of Vyvanse (lisdexamfetamine dimesylate) to treat binge-eating disorder in adults. The drug is the first FDA-approved medication to treat this condition.

In binge-eating disorder, patients have recurrent episodes of compulsive overeating during which they consume larger amounts of food than normal and experience the sense that they lack control. Patients with this condition eat when they are not hungry and often eat to the point of being uncomfortably full. Patients may feel ashamed and embarrassed by how much they are eating, which can result in social isolation. Binge-eating disorder may lead to weight gain and to health problems related to obesity.

FDA Expands Uses of Vyvanse to Treat Binge-Eating Disorder

Thursday, August 6, 2015

FDA Approves Prezcobix (darunavir and cobicistat) for HIV-1 Infection in Adults

Darunavir2DCSD.svg

In continuation of my update on darunavir  


Janssen Therapeutics, Division   of    Janssen    Products, LP     (Janssen), today announced the U.S. Food and Drug Administration (FDA)    has approved Prezcobix   (darunavir 800 mg/cobicistat 150 mg) tablets, an HIV-1  protease inhibitor combined with a CYP3A4 inhibitor, for the treatment of human immunodeficiency virus (HIV-1) in combination with other antiretroviral agents for treatment-naive and treatment-experienced adults with no darunavir resistance-associated substitutions.




FDA Approves Prezcobix (darunavir and cobicistat) for HIV-1 Infection in Adults

Wednesday, August 5, 2015

FDA Approves Glyxambi (empagliflozin and linagliptin) for Type 2 Diabetes



Empagliflozin.svg



In continuation of my update on empagliflozin



The U.S. Food and Drug Administration (FDA) has approved Glyxambi (empagliflozin/linagliptin) tablets, from Boehringer Ingelheim Pharmaceuticals, Inc. (BIPI) and Eli Lilly and Company (NYSE: LLY), as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes (T2D) when both empagliflozin and linagliptin are appropriate treatments. Glyxambi is not recommended in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis. Glyxambi has not been studied in patients with a history of pancreatitis, and it is unknown if using Glyxambi increases the risk of developing pancreatitis in these patients.

Glyxambi is not recommended in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis. Glyxambi has not been studied in patients with a history of pancreatitis, and it is unknown if using Glyxambi increases the risk of developing pancreatitis in these patients.

Tuesday, August 4, 2015

FDA Approves Ibrance (palbociclib) for Postmenopausal Women with Advanced Breast Cancer



Palbociclib.svg


In continuation of my update on palbociclib

The U.S. Food and Drug Administration today granted accelerated approval to Ibrance (palbociclib) to treat advanced (metastatic) breast cancer.

Breast cancer in women is the second most common type of cancer in the United States. It forms in the breast tissue and in advanced cases, spreads to surrounding normal tissue. The National Cancer Institute estimates that 232,670 American women were diagnosed with breast cancer and 40,000 died from the disease in 2014.
Ibrance works by inhibiting molecules, known as cyclin-dependent kinases (CDKs) 4 and 6, involved in promoting the growth of cancer cells. Ibrance is intended for postmenopausal women with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer who have not yet received an endocrine-based therapy. It is to be used in combination with letrozole, another FDA-approved product used to treat certain kinds of breast cancer in postmenopausal women.

FDA Approves Dutrebis (lamivudine and raltegravir) for HIV-1 Infection



Lamivudine structure.svg   Raltegravir structure.svg


The United States Food and Drug Administration (FDA) has approved Dutrebis, a fixed dose combination tablet containing 150 mg of lamivudine and 300 mg of raltegravir. Dutrebis tablet is approved for use in combination with other antiretroviral products for the treatment of HIV-1 infection in adults and pediatric patients greater than or equal to 6 years of age weighing at least 30 kg. The recommended dosage of Dutrebis is one tablet taken twice daily with or without food.

Dutrebis approval was based on an open-label, single dose, randomized, two-period, crossover study in healthy subjects (n=108). One Dutrebis fixed dose combination table was shown to provide comparable lamivudine and raltegravir exposures to one Epivir 150 mg tablet plus on Isentress 400 mg tablet. Due to the higher bioavailability of raltegravir contained in Dutrebis, the exposures provided by the 300 mg dose of raltegravir are comparable to 400 mg of ralegravir given as the raltegravir poloxamer formulation (Isentress), which accounts for the difference in raltegravir dose.


Monday, August 3, 2015

FDA Approves Lenvima (lenvatinib) for Differentiated Thyroid Cancer


LENVIMA (lenvatinib) Structural Formula Illustration



LENVIMA, a kinase inhibitor, is the mesylate salt of lenvatinib. Its chemical name is 4- [3chloro-4-(N’-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carbox- amide methanesulfonate. The molecular formula is C21H19ClN4O4•CH4O3S, and the molecular weight of the mesylate salt is 522.96. The chemical structure of lenvatinib mesylate is:

The U.S. Food and Drug Administration today granted approval to Lenvima(lenvatinib) to treat patients with progressive, differentiated thyroid cancer (DTC) whose disease progressed despite receiving radioactive iodine therapy (radioactive iodine refractory disease).

FDA Approves Lenvima (lenvatinib) for Differentiated Thyroid Cancer