Sea snail venom provides potent pain relief

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[size=+1]Sea snail venom provides potent pain relief[/size]
12:49 15 June 2010 by Jessica Hamzelou

Sea snail venom could become the gold standard for the relief of nerve-related pain following the development of a pill that is 100 times as potent as leading treatments.

Current treatments for neuropathic pain include morphine, which is highly addictive, and gabapentin, which both act on nerve receptors. Sea snail venom had been suggested as a good alternative because it consists of a cocktail of peptides, known as conotoxins. These act to immobilise prey by blocking nerve-cell conduction, but in mammals the peptides are an effective analgesic.

The only conotoxin-derived drug approved for human use is ziconotide. Unfortunately, the drug is susceptible to breakdown by enzymes in the saliva and gut, so it is administered by a pump surgically inserted into the abdominal wall, making it an invasive and expensive treatment.

Circle of strength
To solve this problem, David Craik and his team at the University of Queensland in Australia have developed the first "orally active" conotoxin drug.

They started with a synthetic version of conotoxin. Since the enzymes that break down the drug usually act at the ends of the conotoxin molecule, the team used a chain of amino acids to join up these ends to form a circular structure. They found this version to be resistant to enzymes in the body.

Craik's team tested the conotoxin in rats with neuropathic pain. They found that a single oral dose significantly reduced pain using a standard test – how much pressure the rat could withstand before withdrawing its paw. Compared with gabapentin, conotoxin was judged to be 100 times more potent.

Because the conotoxin is so powerful, only very small doses are needed, reducing the risk of side effects, says Craik. His team has applied for approval from the US Food and Drug Administration for a trial in humans.

Journal reference: Angewandte Chemie, DOI: 10.1002/anie.201000620


Link: http://www.newscientist.com/article/dn19044-sea-snail-venom-provides-potent-pain-relief.html
 
This has been studied for quite some time now. I was wondering when they were getting around to conducting tests on humans. This says they applied for approval for said tests, but i'm sure the FDA won't approve it since big pharma would take a huge dent in sales if this replaced some medications currently used to treat neuropathic pain.
 
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Tommyboy, I don't know how to break this to you, but Big Pharma wins either way. An established drug company will be responsible for releasing the drug, and everyone still gets to sell whatever else they are currently making. They lose most profits when drugs go off-patent, and they are kind of scraping the bottom of the "extended release" barrel as it is. I mean, just look at Darvocet. That is a worthless and dangerous painkiller that the FDA recommended removed from the market, but they still make it and docs write tons of scripts for it.
 
^2020 in the US possibly (if effective and safe). Most new drugs have to be tested in humans for close to a decade before FDA approval.
 
I would too like to try this.

I suffer from atypical trigeminal neuritis.
 
Because the conotoxin is so powerful, only very small doses are needed, reducing the risk of side effects, says Craik.
Click to expand...

I'm not expert on this class of drugs, but this statement seems flawed. Just because a smaller mass of drug is needed does not mean the therapeutic value goes up while the side-effects go down. That's silly to think that. It's all proportional.

By that logic, Fentanyl should be much safer that Codeine at similar therapeutic doses. However, we know this isn't true.
 
Still. People who suffer with chronic nerve pain like myself often have no other recourse but to become legitimate drug abusers or secretive drug importers, especially in the United States.

The only drug that legitimately helps my pain is Klonopin (approved for neuralgic pain) and to keep my doctor from thinking I'm a drug seeker I illegally import Xanax from foreign countries at a cost not much lower than street prices.

I'd give up getting high the rest of my life to end the chronic pain I experience.
 
di.ACE.tyl.rob said:
this statement seems flawed
Click to expand...

The authors are from the Queensland Brain Institute. They will break you.

NSFW:
ScannersExplodingHead.gif
 
Sarcasm? I have no clue what you're getting at.

It is a flawed statement. Just because something requires less physical mass to have an intended effect, does not mean that side-effects are reduced. Mass of material & physiological side-effects have no direct link (not even an indirect link AFAIK).

Maybe they were being specific to that drug, but it came off as a generalization.
 
^exploding head scene from SCANNERS is always sarcasm. I was making fun of the QBI's name

Pharmacological side effects are not necessarily a function of potency. Pharmacokinetic side effects, on the other hand, are usually inversely related to potency. Overall, the phrase "side effects" is not especially informative.
 
Ahh... I see hehe

We're all good then. I'm sure wikipedia could help me out, but for the hell of it do you think you could elaborate of the diff. between 'Pharmacologic' & 'Pharmacokinetic'?
 
When dealing with components of cigarette snail venom (one of the most powerful poisons in nature) you're right: priority one is keeping the patient's heart ticking. Same goes with fentanyl and cardiac or respiratory arrest. A very potent agent can do a lot of damage.

But when making a medicine for chronic pain, you're also designing a chemical that people will put into their bodies every day for the rest of their lives. A lot of thought and research has to go into what the body will do to absorb, distribute and eliminate it. This is the kinetics. This is where sometimes less drug = better drug.

Ethanol is good for illustration. As you know, once it's in the body, it's not just weight: it's a lot of individual molecules floating around (about 1,300,000,000,000,000,000,000,000 ethanol molecules in a 6 pack). Many of those will have a chance of hitting targets that produce drunkenness. They'll also hit some other targets because ethanol is versatile.

However, the body has to absorb, distribute, metabolize and eliminate each of those 1,300,000,000,000,000,000,000,000 ethanol molecules individually. This is the pharmacokinetic part. This is responsible for most of the unpleasant effects of hangover (primarily because acetaldehyde, the rate-limited intermediate, is toxic) because the body literally can't eliminate so many ethanols fast enough and has to invest some very necessary cofactors in doing so (e.g. two NAD+ for every ETOH). If ethanol were more potent, less of it would be needed and the body wouldn't have to devote so much work and resources to its elimination.
 
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