Increasing gabapentin absorption via loperamide

[dexamine]

So, the biggest issue about taking gabapentin is its limited absorption efficiency. We know the typical and common ways of increasing absorption: taking it in staggered doses, taking it with food, etc.

I’ve been searching and have not been able to find any information about lowered gut mobility and gabapentin increased absorption.

Below I have taken a paragraph from an article that I read about lowered gut mobility and that it may increase gabapentin absorption. My theory is that loperamide being an anti-diarrheal lowers gut mobility, and can increase the absorption of gabapentin by slowing down it’s pass through the small bowel, which would increase the time it is there, thereby increasing absorption.

URL: http://www.pharmacytimes.com/contri...015/09/how-gabapentin-differs-from-pregabalin

Renal excretion is the major method of both drugs’ elimination from the body. Agents that decrease small bowel motility can theoretically cause an increase in the absorption of gabapentin, because it is not completely absorbed. However, as pregabalin is more than 90% absorbed, its absorption is not affected by changes in small bowel motility.**

** Bockbrader HN, Wesche D, Miller R, Chapel S, Janiczek N, Burger P. A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin. Clin Pharmacokinetics. 2010;49(10):661-9.

If anybody has any thoughts on this I would greatly appreciate it.

 

[clubcard]

Don't mix them, it will kill you - https://academic.oup.com/jat/article/40/8/677/2445880

 

[atara]

clubcard: I'm pretty sure those deaths are all loperamide overdoses -- gabapentin levels were high in two cases but loperamide levels were not abnormally low for a decedent.

I'm pretty sure absorption happens mostly in the small intestine, whereas loperamide inhibits clearing of the large intestine. The large intestine only absorbs water pretty much. Residence time in the large intestine is generally ~20 hours whereas residence time in the small intestine is maybe one hour so most anti-diarrheals target the large intestine. I'm not sure inhibiting peristalsis in the small intestine would be healthy anyway...

 

[Kittycat5]

For example, both drugs are structurally similar to the amino acid leucine. Because of this, they can both undergo facilitated transport across cellular membranes through system L-amino acid transporters.3 This is the major form of absorption for gabapentin and pregabalin, with the exception of an extended-release gabapentin prodrug to be discussed later.

This is more important. Find something to maximize those amino acid transporters.

 

[clubcard]

You refer to Seizure. 2003 Jan;12(1):28-36? GP is absorbed by the duodenum digitorum?

 

[MyExcuse]

http://m.ajpendo.physiology.org/content/298/5/E1011.short

Eat more amino acids.