Talk:Difenoxin

unsourced 1

The following is unsourced. Moved here til it can be reliably sourced.

Related compounds

Loperamide (Imodium) is also closely related to difenoxin in chemical structure but does not cross the blood–brain barrier as does difenoxin, and the combination drug diphenoxylate hydrochloride with atropine sulfate (Lomotil) is the prototype of this four-member subfamily of the synthetic opioid receptor agonists and sub-category of opioid anti-diarrhoeals. Diphenoxylate is the ethyl ester of difenoxin and about 50 per cent the potency of difenoxin. The parent of the three above-mentioned pethidine-related anti-diarrhoeals is diphenoxylic acid, which can also be manufactured and used pharmaceutically.

Pethidine was serendipitously discovered in research during the 1930s on gastrointestinal drugs to serve as alternatives to belladonna and opium derivatives, but the anti-diarrhoeal effects of pethidine are less than those of this subclass and equivalent constipating doses of pethidine have prominent central actions. A notable close relative of difenoxin is the strong analgesic alphaprodine (Nisentil, Prisilidine).

Another opioid with a somewhat more distant structural relationship to difenoxin &c is piritramide (Dipidolor), which is the prototype of its own small family of agents, rather than a 4-phenylpiperidine like pethidine; piritramide was also invented by Dr Janssen at Janssen Pharmaceutica along with a large number of other drugs including fentanyl and haloperidol.

Therefore, with difenoxin and related drugs, the ratio of GI effects to central narcotic effects is particularly high, which makes it an attractive alternative in the minds of many to the other opioids used for diarrhoea, viz. codeine, morphine, dihydrocodeine, paregoric, laudanum and opium .

- Jytdog (talk) 23:09, 3 April 2016 (UTC)

Approved before it was introduced? (Possible conflict of fact between sources)

The last sentence in the article reads:

"It was introduced by Cilag in 1980 in the former West Germany.[6]:485 It was first approved in the US in 1978.[7]"

This seems to say that USFDA approved difenoxin before it was introduced. Another possible interpretation is that difenoxin was introduced in (the former) West Germany two years after it gained USFDA approval, which is sort of the opposite sequence for new drug approvals in general - NDAs are generally granted in Europe before they are in the US.

I"m going to examine the source documents to allow that sentence to be changed to be less confusing, but hoping Jytdog (who has edited this article in the past with a view toward sourcing of facts) knows what really happened, has already read the relevant sources, and can write a less confusing but still accurate version of this sentence before I get around to it. loupgarous (talk) 13:40, 6 October 2016 (UTC)

Thanks, fixed it as well I could. Those two sources say what they say and are the only two sources I have found so far that give dates. Jytdog (talk) 16:34, 6 October 2016 (UTC)

Thank you. loupgarous (talk) 02:22, 9 October 2016 (UTC)