Another novel opioid analgesic in development

[dokomo]

From the site:

NKTR-181 is a mu-opioid analgesic investigational drug candidate with a novel molecular structure designed to provide potent pain relief while reducing the serious side effects of respiratory depression, sedation and abuse potential associated with conventional opioids.

...

The unique molecular design of the polymer drug conjugate also prevents conversion of NKTR-181 into a rapid-acting abusable form of an opioid. As a result, NKTR-181 has the potential to be a highly effective analgesic with a highly favorable safety profile and reduced abuse potential.

Link

Press Release (PDF)

Research Poster (PDF)

 

[23536]

I think the conjugation of morphine with a PEG side chain is pretty brilliant, but:

: Analgesia was determined using the acetic acid writhing model in mice. Animals (n=5) were treated orally with saline or compounds (0.1 – 100 mg/kg range) 30 min prior to intraperitoneal injection of 0.5 % acetic acid, and writhes were counted over a 20 minute period.

really turns me off. It's one thing to euthanize animals, but quite another thing to torture them by injecting acid into their abdomens. There are many more-humane ways to determine analgesia, right?

 

[jaurk]

I think the conjugation of morphine with a PEG side chain is pretty brilliant, but:



really turns me off. It's one thing to euthanize animals, but quite another thing to torture them by injecting acid into their abdomens. There are many more-humane ways to determine analgesia, right?

I believe opiate ethunasia is the way to go, Terrence McKenna also appreciated that method, and suggested it over many others to a lady in a QandA.

 

[Midazle]

Sounds interesting from a pain patients point of view! I have pretty moderately severe chronic pain from an injury and a long term illness and since I'm so young my docs are ***holes with narcotics. Sure I would prefer to stay with OxyContin since in addition to pain relief, I get an elevated mood but this sounds interesting...

I believe opiate ethunasia is the way to go, Terrence McKenna also appreciated that method, and suggested it over many others to a lady in a QandA.

Agreed. I don't know why this isn't standard practice in areas where its legal...nodding out to death has got to be the most painless and blissful way to go...I mean think of how it feels to sleep on opiates...most of the time all you remember is being relaxed then nothing...

 

[skillet]

There are many more-humane ways to determine analgesia, right?

I don't think so, to measure a reduced response to pain you have to inflict pain... The most common ways I've read about are the hot-plate test and tail flick test.

About the thread topic, I think it's pointless. If someone's going to abuse something and can't do it with their medication, they'll probably just find something else.

 

[23536]

I don't think so, to measure a reduced response to pain you have to inflict pain... The most common ways I've read about are the hot-plate test and tail flick test.

Those sound much more humane than intraperitonial acetic acid injections.

 

[skillet]

Maybe, I guess it depends what concentration of acetic acid they use, I doubt it was neat. Glancing at this, it sounds like they mostly go for uncomfortable, rather than actually painful, which is kinda nice to know

Weaknesses are highlighted, including 1) that in most tests responses are monitored around a nociceptive threshold, whereas clinical pain is almost always more severe...