Entereg - The End of Constipation From Opiates

[Paregoric Kid]

This pharm. company called Adolor is waiting for FDA approval of a drug called alvimopan, planned to be market under the trade name Entereg. it is a "peripherally-acting mu opioid receptor (PAM-OR) antagonist designed to block the adverse side effects of opioid analgesics on the GI tract without blocking their beneficial analgesic effects." kind of like the loperamide of antagonists. I used to think "wouldn't it be great if there was an antagonist that didn't cross the BBB? well they beat me to it lol

wanted to add that they are also working on combining entereg with opioids.

edit: pharm. companies wyeth and progenics are in collaboration trying to get approval for a similar drug, methylnaltrexone. they are seeking approval for treatments in: Subcutaneous for opioid-induced constipation in advanced medical illness, I.V. postoperative ileus, Oral opioid-induced constipation.

it's likely these drugs may also reverse some other side effects of opiates.

[nick]

Nice-if a little late for me.

Kid,there will be other chances-just remember where the patent office is.How's about fudge flavoured junk-we could make a fortune.I always wanted to see my name on a medicine label.

[Paregoric Kid]

the FDA has approved methylnaltrexone, brand name Relistor, and alvimopan, brand name Entereg. Entereg has only been approved for in hospital use and not to be given more than 15 times. entereg can cause diarrhea and probably other GI wd symptoms if taken after you've been using agonists for at least a few days. relistor is only available in SC injection but they are coming out with an oral version for chronic pain patients in 2009-2011.

[resorcinol]

I really like the idea of methylnaltrexone.

It does pose problems for those of us who are already physically dependent the old fashioned way though. You'll be in the bathroom for ages with precipitated peripheral w/d shitting water out of your ass. On the bright side, you could be nodding at the same time. Gotta love the BBB.

whatever keeps methylnaltrexone out of the CNS... anyone who uses this must take care not to tamper with whatever keeps it out of the CNS. If it's Pgp, don't take any Pgp inhibitors! If it's just because it's extremely hydrophilic than we're pretty safe.

I tend to think of withdrawal symptoms:

These are associated with peripheral mu receptors: diarrhea, cramps, abdominal pain, nausea, vomiting

associated with CNS mu receptors: everything else... anxiety, akathisia, goosebumps, lacrimation, rhinorrhea, hot and cold flashes, chills, etc

[Narkotikon]

I know this stuff could be useful to people on MMT or other strong opiates for long times like CP patients, but honestly I'd still be afraid to use it. When not on opaites, I eat Immodium like crazy to have normal movement down there. It's like all the opiates have fucked up by GI tract, and now I need the Immodium to have a normal bowel movement. It doesn't really constipate me anymore, it just makes things normal again. I have a feeling if I used something like this, even while on opiates, it would fuck it up and be very very uncomfortable. I don't think this stuff should be used by the average junkie looking to use the bathroom, rather maybe only for those who are on maintenance or are CP patients.

Plus, in another thread, someone said one of these drugs was $50 a dose. That's ridiculous. I'd rather use an OTC laxative or a coffee enema. Plus the idea of putting any antagonist, even if it doesn't cross the BBB, into my body scares me. So it doesn't cross the BBB, what if it antagonizes the receptors in the other parts of the body that are responsible for causing leg aches? Does that mean you'd get leg aches / jerks from taking this just so you can use the bathroom? I mean, does this really only work on the GI tract? Just because it's not lipid soluble and can't cross the BBB, doesn't mean it can't affect other receptors outside the brain.

[Duckfeet]

Yeah, I kind of see all of this as kind of fitting into my "no free lunch" theory of longterm opiate use: me, w/methadone, or any daily, consistent use of opiates, the constipation is one of worst side effects, and I could hardly bear it anymore...just made me sick, physically and mentally, and when I finally got down around 15mg daily, and began to have regular bms again, I almost wept, I was so fucking happy...

But I still take a daily 100mg docusate (stool softener), but eventually will probably give it up...and I too, thought I would be that way even after getting off opiates, but no, it got normal again...was just the methadone, in my case...