dopetalk does not endorse any advertised product nor does it accept any liability for it's use or misuse

This website has run out of funding so feel free to contribute if you can afford it (see footer)

Author Topic: The absorption of gabapentin following high dose escalation  (Read 2000 times)

Offline Chip (OP)

  • Server Admin
  • Hero Member
  • *****
  • Administrator
  • *****
  • Join Date: Dec 2014
  • Location: Australia
  • Posts: 6493
  • Reputation Power: 0
  • Chip has hidden their reputation power
  • Gender: Male
  • Last Login:Yesterday at 05:37:04 PM
  • Deeply Confused Learner
  • Profession: IT Engineer
source restriction disclosure: https://www.sciencedirect.com/science/article/pii/S1059131102001425

Abstract

Gabapentins (GBP) are structurally similar to GABA yet its mode of action remains uncertain. It is water-soluble and GI tract absorption occurs via the l-amino acid transport system in the proximal small bowel. It has been suggested that this transportation is capacity limited, thus decreasing GBP bioavailability at higher doses. GBP is not protein bound, therefore, salivary levels might be expected to be similar to those in serum; also the drug does not induce hepatic enzymes and is excreted unmetabolised by the kidney. Within the dose-range normally prescribed, it is devoid of pharmacokinetic (PK) drug interactions with all other anti-epileptic drugs.

This study assesses two things in patients with epilepsy: (a) bioavailability of higher doses of GBP (1200–4800 mg per day), and (b) the influence of high dose GBP on between-dose serum concentrations of co-prescribed anti-epileptic drugs. After stabilising at each dosage, a sequence of serum and saliva samples were collected within the dosage interval; GBP and co-medication concentrations were determined and the results subjected to PK modelling.

Meaned results from 10 patients indicate that GBP continues to be absorbed in a reasonably linear manner relative to dose up to 4800 mg per day. The study also shows that GBP is transported into saliva, however, salivary concentrations are only 5–10% of those in plasma. Furthermore, the results indicate that GBP, in higher than recommended doses, did not change plasma concentrations of lamotrigine, carbamazepine, carbamazepine-epoxide, vigabatrin, primidone, phenobarbitone or phenytoin when added to treatment.

It is concluded that larger than recommended doses of GBP can be efficiently absorbed by some patients and also that GBP plasma levels do not fluctuate greatly between dosage intervals, therefore, twice daily dosage is a possibility.
I do not condone or support any illegal activities. All information is for theoretical discussion and wonder.
All activities discussed are considered fictional and hypothetical. Information of all discussion has been derived from online research and in the spirit of personal Freedom.

Tags:
 

Related Topics

  Subject / Started by Replies Last post
7 Replies
4698 Views
Last post August 03, 2016, 09:22:50 PM
by MoeMentim
47 Replies
22835 Views
Last post December 31, 2017, 06:59:51 PM
by Chip
37 Replies
16766 Views
Last post January 25, 2018, 02:52:59 PM
by Chip
7 Replies
4935 Views
Last post January 12, 2016, 07:27:19 PM
by Strapped420
0 Replies
2760 Views
Last post March 08, 2016, 06:16:13 AM
by Chip
0 Replies
2369 Views
Last post September 12, 2017, 06:03:21 AM
by Chip
8 Replies
4370 Views
Last post March 30, 2018, 11:41:47 AM
by limerence
1 Replies
2645 Views
Last post February 13, 2018, 02:43:47 PM
by Mr.pooper
0 Replies
1358 Views
Last post July 02, 2019, 02:26:46 PM
by Chip
1 Replies
1535 Views
Last post November 08, 2019, 11:40:32 AM
by limerence


dopetalk does not endorse any advertised product nor does it accept any liability for it's use or misuse





TERMS AND CONDITIONS

In no event will d&u or any person involved in creating, producing, or distributing site information be liable for any direct, indirect, incidental, punitive, special or consequential damages arising out of the use of or inability to use d&u. You agree to indemnify and hold harmless d&u, its domain founders, sponsors, maintainers, server administrators, volunteers and contributors from and against all liability, claims, damages, costs and expenses, including legal fees, that arise directly or indirectly from the use of any part of the d&u site.


TO USE THIS WEBSITE YOU MUST AGREE TO THE TERMS AND CONDITIONS ABOVE


Founded December 2014
SimplePortal 2.3.6 © 2008-2014, SimplePortal