Comment · Fri, September 6, 2013 · Ceretropic
Is it necessary to maintain a piracetam blood serum level?
Original post in this thread
Damderiam · 20 points
With a half life of 4-5 hours it would require measuring and taking exact doses 3-4 times a day, and that's just not feasible all the time. However, there are plenty of medicines that continue to act, indirectly, after they've been eliminated. Am I getting any effect at all by taking it prior to bedtime, or would a morning dose be necessary as well? Since we don't know exactly how piracetam works I'll have to go by anecdotes and experimental evidence, but it's better than winging it. I figure it may, for example, increase the efficiency of sleep, or have lingering effects.
What they were answering
alan2102 · 1 points
1. Is it possible that the long half-life is responsible (partly or wholly) for the increased passage through the BBB? Perhaps a critical concentration in blood, above which BBB transport is disproportionately increased, which happens only briefly with piracetam, and much more with oxi? Mere speculation, but... [whoops! ignored the "edit"; well, that's a surprise; if LOWER brain levels, then...?]
2. Bioavailability: why not add the universal absorption-booster, piperine? Black pepper.
3. Bioavailability 2: MYASD: you may want to check this out as a potential aid in your formulations (why not liquid formulations?):
http://www.ncbi.nlm.nih.gov/pubmed/16948563
Expert Opin Drug Deliv. 2006 Sep;3(5):685-92.
Promoting absorption of drugs in humans using medium-chain
fatty acid-based solid dosage forms: GIPET.
u/MisterYouAreSoDumb · Ceretropic
It's possible the greater effects are peripherally mediated by the adrenals. The longer half life would not make a difference to peak CSF concentrations, as both reach peak effects in about the same time.
Piperine would do nothing, as neither are metabolized by CYP3A4. It's not a universal absorption booster. It only affects certain substances. It mainly inhibits CYP3A4 and the P-glycoprotein transporter. This study showed that another P-glycoprotein inhibitor, Morin, did not alter the pharmacodynamics of piracetam. That means piperine is not likely to have any effect on either piracetam or oxiracetam.
Medium-chain fatty acids will not really help with any of the substances we are using. Most have a very high intestinal bioavailability as it is. We are more concerned with BBB permeability, which is more complicated than enteric coating. We need to reduce the polarity of the molecule to make it more lipid soluble. However, that's hard to do without completely changing the molecule.