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Gabapentin and Cimetidine serum [GP]/clearance Q?

Posted by jmb2012 on May 7, 2011, at 14:07:40

Hi. I was hoping someone could shine some light on this: I've read that cimetidine (cimet) reduces clearance of gabapentin, (GP), by ~14%. Also Cimet increases serum levels of GP. Would taking GP with cimet increase the duration of it's active effects in the body? Would it synergize/potentiate and allow less to to be taken? Cimet inhibits certain cyp450 isoenzymes.Though GP is said not to be appreciably metabolized maybe there is a correlation. Also Cimet may have a stronger protein binding affinity than GP (prot bind= 3%).

I'm wondering if and how taking cimet with GP would increase it's active time in the body- reducing the need to dose every 4-5 hours. This up and down gets tiresome especially on long days. Ideally it would turn GP into a longer acting medication with a smoother, wider concentration/activity curve. IF possible, could this maybe even help with the development of inter-dose anxiety or with withdrawal?

Any takers? Any other ways to improve/extend GP effect in body? Don't think I can afford Lyrica at the dose I'd need. (Taking 4 X 300mg GP/day now)
Memantine perhaps?


Drug Interactions

Antacids: Antacids may reduce the bioavailability of gabapentin by ~20%; gabapentin should be taken at least 2 hours following antacid administration

Cimetidine: Cimetidine may increase gabapentin serum concentrations; clearance of gabapentin is decreased by 14%

Felbamate: Serum concentrations may be increased by gabapentin; monitor for increased felbamate effect/toxicity

Morphine: Serum concentrations of gabapentin may be increased during concurrent use.

Norethindrone: Gabapentin may increase Cmax of norethindrone by 13%

Phenytoin: Phenytoin serum concentrations may be increased by gabapentin; limited documentation; monitor. Note: Valproic acid, carbamazepine, and phenobarbital do not seem to be affected by gabapentin.




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