Showing posts sorted by relevance for query gabapentin. Sort by date Show all posts
Showing posts sorted by relevance for query gabapentin. Sort by date Show all posts

Sunday, December 9, 2012

Severe morning sickness patients get relief from anti-seizure drug

 In continuation of my update on gabapentin

"The study showed that after two weeks of gabapentin therapy, the seven women experienced an average 80 percent reduction in their nausea and a 94 percent reduction in their vomiting and near normal levels of eating and drinking," Guttuso says. After this study was published, Guttuso knows of five more women with hyperemesis gravidarum that tried gabapentin and all experienced excellent relief.

The women needed to take gabapentin on average until about half way through their pregnancies before they could stop it without recurrent nausea and vomiting.

One of the potential concerns with gabapentin was that two of the babies born to patients in the UB study were found to have congenital defects. As a result, the Food and Drug Administration placed the study on clinical hold in April 2011 until further safety data was available on the use of gabapentin during pregnancy.

By May 2012 several pregnancy registries and other studies had reported that the rate of congenital defects among a total of 258 infants born to women taking gabapentin early in their pregnancies was about the same as the rate of congenital defects in the general population. After reviewing these findings, the FDA removed the clinical hold allowing Guttuso to resume his research on the effects of gabapentin on hyperemesis gravidarum. Although the results of the small pilot study were very encouraging, Guttuso emphasizes that a placebo-controlled study among many more patients needs to be conducted in order to know if gabapentin truly is effective for hyperemesis gravidarum. "The evidence right now is still very preliminary," he states.

Thursday, April 26, 2012

Gabapentin drug helps people to quit cannabis..

We know that, Gabapentin (see structure; brand names FanatrexGabaroneGraliseNeurontinNupentin) is a pharmaceutical drug, specifically a GABA analogue. It was originally developed for the treatment of epilepsy, and currently is also used to relieve neuropathic pain

Now Scientists at The Scripps Research Institute have found clinical evidence that the drug gabapentin, currently on the market to treat neuropathic pain and epilepsy, helps people to quit smoking marijuana (cannabis). Unlike traditional addiction treatments, gabapentin targets stress systems in the brain that are activated by drug withdrawal.

In a 12-week trial of 50 treatment-seeking cannabis users, those who took gabapentin used less cannabis, experienced fewer withdrawal symptoms such as sleeplessness, and scored higher on tests of attention, impulse-control, and other cognitive skills, compared to patients who received a placebo. If these results are confirmed by ongoing larger trials, gabapentin could become the first FDA-approved pharmaceutical treatment for cannabis dependence.

"A lot of other drugs have been tested for their ability to decrease cannabis use and withdrawal, but this is the first to show these key effects in a controlled treatment study," said Barbara J. Mason, the Pearson Family Chair and Co-Director of the Pearson Center for Alcoholism and Addiction Research at Scripps Research. "The other nice thing about gabapentin is that it is already widely prescribed, so its safety is less likely to be an issue."
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Tuesday, September 25, 2012

Once-daily Gralise significantly reduces pain intensity in PHN patients

Depomed, Inc. announced that a report of Phase 3 data published online this month, ahead of the print edition,  in the Clinical Journal of Pain showed that once-daily Gralise® (gabapentin) tablets (1,800 mg) formulation significantly reduces intensity of pain in patients with postherpetic neuralgia (PHN). The results showed that patients treated with Gralise experienced a significant reduction (- 2.12) in their average daily pain intensity compared with placebo treated patients (-1.63; P=0.013). This difference from placebo was statistically significant after one week and continued to be superior through the duration of the study. 

About Gralise (below structure-Gabapentin) : Gabapentin (brand names Fanatrex, Gabarone, Gralise, Neurontin, Nupentin) is a pharmaceutical drug, specifically a GABA analogue. It was originally developed for the treatment of epilepsy, and currently is also used to relieve neuropathic pain. There are, however, concerns regarding the quality of the trials conducted.

Depomed - Investor Relations - Press Releases

Tuesday, August 3, 2010

The Engineering of an Orally Active Conotoxin (Snail Spit) for the Treatment of Neuropathic Pain...

The mollusks use a deadly dose of conotoxins (peptide toxins, e.g., α/ω-conotoxin peptides) that disrupt myriad biological functions. The mollusks  inject into passing prey with hypodermic-needle-like teeth that shoot from their mouths like harpoons.

Within the conotoxin brew are several peptides that relieve tough-to-treat neuropathic pain just as well as morphine does but without its addictive properties. Although scientists have tried to turn such compounds into pain relievers, they've been hamstrung with problems administering such drugs. The pain reliever Prialt (see structure,  Ziconotide),  a synthetic version of ω-conotoxin MVIIA, but it must be injected directly into the spinal cord with a surgically implanted pump.

Now interestingly, scientists in Australia lead  by Prof. David Craik (Institute for Molecular Bioscience at the University of Queensland), have managed to engineer a conotoxin that can be taken orally. Researchers found that,  by linking the N-terminus of α-conotoxin Vc1.1—a compound derived from Conus victoriae—to its C-terminus, they could make the 16-residue peptide orally active.  In the cyclized peptide, which is known as α-conotoxin cVc1.1, the protein's head and tail are tethered by a string of six amino acids—two alanines flanked on each side by two glycines. Prof. Craik says he chose the linker because it was inexpensive, wouldn't add any functionality to the molecule, and would be easy to characterize with nuclear magnetic resonance. In tests with rats, the cyclized peptide proved to be as potent a painkiller as gabapentin, the most popular drug for neuropathic pain, even though the conotoxin-based peptide was administered at a dose that is less than 1% of the dose typically given for gabapentin (other orally prescribed peptide is Ciclosporin a immunosuppressant).

Craik's group has shown that cyclizing larger peptides can make them orally available. His team's analysis of the protein database shows that up to 25% of all proteins have their ends within 10 Å of one another a distance that could easily be spanned with linkers of six to 10 amino acids.

"All you need is for the ends to be roughly close to one another," Prof. Clark says.

Craik says the cyclization also enhances hydrogen bonding across the entire molecule, making it resistant to the endopeptidases that attack a protein's interior amino acids. He says it's sort of like a zipper: "A zipper can be regarded as a series of hydrogen bonds all interlocking together, and when you zip it all up, you've got a beautiful set of coordinated hydrogen bonds. But you've still got two ends, and when you pull apart those two ends of the zipper, then the first hydrogen bond goes, then the next, and then the next. Craik has discovered several other examples of cyclic peptides, which he calls cyclotides (C&EN, April 19, 2004, page 40). He's hoping to use their structural features to guide the engineering of other peptides, as he did with α-conotoxin cVc1.1 At the moment, Craik is trying to raise funds so enough preliminary experiments can be done to file an Investigational New Drug Application. "The most challenging aspect has been just raising the money to get it commercialized," he says. "Pharmaceutical companies are always a little nervous about peptides. We need more success stories so that they'll see peptides not only as fantastic leads but also as potential drugs."...

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Saturday, September 1, 2012

GSK and XenoPort receive FDA approval for Horizant® for postherpetic neuralgia

GlaxoSmithKline plc  and XenoPort, Inc. announced today that the United States (US) Food and Drug Administration (FDA) has approved Horizant® (gabapentin enacarbil see structure below) Extended-Release Tablets for the management of postherpetic neuralgia (PHN) in adults. 
 The efficacy and safety of Horizant for the management of PHN was evaluated in a single 12-week principal efficacy trial, plus two supportive studies that all met their respective primary endpoints. The three clinical studies involved 574 adult patients from the US, Canada and Germany. 

The recommended dosage for the management of PHN in adults is 600 mg twice daily. Treatment should be initiated at a dose of 600 mg in the morning for three days followed by 600 mg twice daily (1,200 mg/day) beginning on day four. Doses must be adjusted in patients with impaired renal function. In the 12-week, controlled study in patients with PHN, somnolence and dizziness were the most frequently reported side effects. Somnolence was reported in 10% of patients treated with 1,200 mg of Horizant per day compared with 8% of patients receiving placebo. Dizziness was reported in 17% of patients receiving 1,200 mg of Horizant per day compared with 15% of patients receiving placebo.