Neurontin

US Brand Name: Neurontin
A link here will take you to the official website for the drug.

Other Brand Names: Gantin (Australia)
Kaptin (Colombia)Generic Name: gabapentin

Other Forms: tablets, oral solution

What is Neurontin: Neurontin is an anticonvulsant
Read up on these sections if you haven’t done so already, because they cover a lot of information about multiple medications that I’m not going to repeat on many pages.  I’m just autistic that way about not repeating myself.

What are Neurontin’s FDA Approved Uses: Adjunctive treatment (i.e. you must use another drug along with it) for  partial epileptic seizures in adults and children.

These include:

  • Simple partial seizures – you’re still awake (more or less), with symptoms such as one or two limbs spazzing out or wacky visual or other sensory distortions.  Think Alice in Wonderland, as Lewis Carroll must have had some serious temporal lobe issues.  The fist link will take you to a better explanation.  For a really detailed explanation of what a simple partial seizure is, click here.
  • Complex partial seziures – the people around you think you’re just acting out to get attention.  In reality you have no control over what’s happening.  Again, click there for the basics, click here for what neurologists think about

Neurontin (gabapentin) is also approved for postherpetic neuralgia (the physical pain from shingles) in adults.

What are Neurontin’s Off-Label Uses: What isn’t Neurontin used for? It’s the late-20th century’s most successful snake oil! Monotherapy Treatment for Epilepsy (used all by its lonesome).  Bipolar Disorder – basically useful only if bad anxiety or substance abuse is also present, or nothing else has worked. And then usually only as an add-on med.  Migraines.  Neuropathic pain. Depression.  PTSD.  Alcoholism (one study has it working well on mild-to-moderate alcohol withdrawal, another showed it to be insignificant for acute withdrawal). Anxiety (including panic and social phobia, but Parke-Davis’ data are suspect, and public speaking).  Sleep Disorders.  Restless Leg Syndrome/PLMS, MS, Chronic Fatigue.  Menopausal Symptoms.  Treating HIV/AIDS-related Neuropathy.   Phantom Limb Pain.   Cocaine Abuse.  And probably a bunch of stuff I don’t even know about.  Sometimes it’s quite useful in these applications, sometimes it’s prescribed first just because it’s an anticonvulsant with a very low side effect profile and doctors are sick and tired of people whining about how medication sensitive they are.

Neurontin’s Pros and Cons: 

Pros: It has a very low side effect profile. Given that what you take is what works on your brain there are few drug-drug interactions (but they are wacky). Neurontin (gabapentin) is a proven pain reliever that doesn’t mess with you as much as the other anticonvulsants do, and works better for non-migraine pain better than most of the others.

Cons: It doesn’t work for a lot of people, mostly because of bioavailabilty issues. Because of Parke-Davis’ allegedly sleazy marketing practices you can’t get samples from your doctor anymore.

Neurontin’s Typical Side Effects: The usual for anticonvulsants, albeit to a lesser degree for most people. Although at the higher dosages Mouse and I, especially Mouse, experience memory problems. The main problems with Neurontin are dizziness, cloudy thinking, fatigue and klutziness.

Neurontin’s Not So Common Side Effects: Edema. Really goofy thinking – one person taking it calls the med, “Morontin.”  If being treated for bipolar disorder, don’t be surprised if it results in hypomania instead of working as a mood stabilizer – as that has been reported in the clinical trials for epilepsy, in at least one of the studies on Neurontin (gabapentin) as a treatment for bipolar, and several times in the online support groups. I haven’t found any studies to back this up, but my doctor tells me that at the higher dosages Neurontin (gabapentin) does start to hit the dopamine receptors. The combination of GABA and dopamine may be just the thing for depression, but can get some people really goofy, and not necessarily in a good way.

These may or may not happen to you don’t, so don’t be surprised one way or the other.

Neurontin’s Freaky Rare Side Effects: Taste perversion, abnormal accommodation, libido increased, baby you are coming over to my house right now! I’ve got plenty of Neurontin on hand!

Interesting Stuff Your Doctor Probably Won’t Tell You: Neurontin (gabapentin) is a prime example of the Law of Diminishing Returns in that the more you take the less you get. Seriously. It’s right there in the PI sheet. “As dose is increased, bioavailability decreases. Bioavailability of gabapentin is approximately 60%, 47%, 34%, 33%, and 27% following 900, 1200, 2400, 3600, and 4800 mg/day given in 3 divided doses, respectively.” You can try to squeeze out a little more absorption by taking it with food, but you buy a whopping 14% increase, on average, in the bioavailability. Sometimes every little bit helps.

Neurontin (gabapentin) is basically a neurotransmitter in a pill. Rather, it’s close to the neurotransmitter GABA. GABA can’t cross the blood-brain barrier. True synthesized GABA would have to be injected straight into your noggin. Sorry to make you cringe. The point is, unlike most psychiatric drugs, what you take in the capsule (or tablet or oral solution) is what more-or-less what works in your brain. Neurontin (gabapentin) doesn’t need your liver to make what really does the job. That means it will play well with practically every other medication there is, right? For us crazies and spazzes, that’s right. The only thing we have to be careful with is stuff like Maalox. As a lot of meds cause tummy troubles, a lot of us use OTC remedies like Maalox. Maalox interferes a bit with Neurontin (gabapentin). You just have to wait a couple hours after taking antacids to take Neurontin (gabapentin).

But people who take Neurontin (gabapentin) for pain, and that includes a lot of us crazies, as fibromyalgia is far too common in the bipolar community, Neurontin (gabapentin) has a weird drug-drug interaction with opiates. The opiates make Neurontin (gabapentin) work better, but the Neurontin (gabapentin) makes the opiates less efficient! It’s weird, and since Neurontin (gabapentin) isn’t really metabolized, who the hell knows what the deal is with that. This is spelled out in the PI sheet, but who reads those, right?  When you take Neurontin (gabapentin) along with hydrocodone (a.k.a. Vicodin), it decreases the bioavailability of the hydrocodone by up to 22%!  While the bioavailability of Neurontin (gabapentin) is increased by 14%.  It’s even odder when combined with morphine.  As Mouse points out there’s an element of timing involved, as the one article on the interaction has morphine administered two hours before the Neurontin (gabapentin).   The morphine was unaffected, having pretty much been on its way towards peak plasma, but the Neurontin (gabapentin) bioavailability was increased by a whopping 44%!  We have no idea if this effect carries over to the artificial opiods, like Demerol or buprenorphine.

Meanwhile taking naproxen (a.k.a. Aleve) increases Neurontin’s bioavailability by 12-15%, while there is no apparent affect on naproxen’s bioavailability.

Neurontin’s Dosage and How to Take Neurontin: Given all the different things for which Neurontin (gabapentin) is used, I’m not about to cover all the possible dosages. I’m just going to cover the FDA-approved applications in adults and bipolar disorder. For everything else it’s between you and your doctor.

For shingles start with 1 300mg dose. On day 2 take your 300mg dose two times a day. On day 3 take it three times a day. Then work your way up as required to a dosage range of 1,800 to 3,600mg a day divided over three to four doses a day.

For epilepsy Parke-Davis recommends you start right out with the therapeutic dosage of 900mg a day, divided over 3 300mg doses. What the hell? This is an add-on medication folks, how about a little titration? My advice is to follow the schedule for shingles. Give your body a chance to get used to this stuff. The effective therapeutic range is 900 to 2,400mg a day, in doses taken three to four times a day. You shouldn’t let 12 hours pass between doses.

For bipolar, remember everything is off-label, experimental and, frankly, Neurontin (gabapentin) is not a first-line bipolar medication. Follow the schedule for shingles, although you may allow yourself twice as long to get used to the med – two days at each dosage. Don’t expect to feel much until you get to 900mg a day. Like epilepsy, once you get up to 900mg a day, don’t let more than 12 hours pass between each dose. If you don’t feel anything by the time you get up to 1800mg a day, just give up. If Neurontin (gabapentin) is doing something for you, that’s one thing, but if it’s not doing anything at all, don’t just throw more at it.

Parke-Davis is all about taking it three times a day. My experience, my doctor’s and the various studies I’ve looked at indicate that mileage always varies. There has even been one study on taking Neurontin (gabapentin) three or four times a day. I found that taking it four times a day works better for me than three times a day.

As for how much you can take, the sky is the limit. There is no known lethal dosage for Neurontin (gabapentin). The tablets are more likely to be a choking hazard than the risk of poisoning yourself from several bottles of the stuff. However, between the diminishing returns of bioavailability and the side effects of getting all that stuff in you it’s just a pointless exercise to be taking megadosages of Neurontin (gabapentin). The real harm of a lot of Neurontin, from a psychiatric standpoint, is that it gets in the way of taking the right medications.  If it works for you, fine.  But if Neurontin (gabapentin) isn’t doing squat at the normal therapeutic range, just give up and move on.

Days to Reach a Steady State: Two days after you’re taking it at least three times a day.

When you’re fully saturated with the medication and less prone to peaks and valleys of effects. You still might have peaks of effect after taking many meds, but with a lot of the meds you’ll have fewer valleys after this point. In theory anyway.

How Long Neurontin Takes to Work: It should start to do something for you a couple days after you reach 900mg a day. But because of the whole bioavailability issue it may not be until you’re somewhere in the range of 900-1800mg a day, presuming it will do anything at all for you.

 Neurontin’s Half-Life: 5-7 hours.

Average Time for Neurontin to Clear Out of Your System:   It’s out of your system in 2 days.

How to Stop Taking Neurontin: Your doctor should be recommending that you reduce your dosage by 100-300mg a day every two days, 5-7 hour half-life, if not more slowly than that.

Like any anticonvulsant, if you’ve been taking Neurontin (gabapentin) for more than a couple months and you’re up to or above 900mg a day you just can’t stop cold turkey if you’re not at the therapeutic dosage for another anticonvulsant that you know works for you, otherwise you risk  partial-complex, absence seizures or even tonic-clonic grand mals, despite your never having had a seizure disorder before!   The risk is worse if you’re taking a lithium variant, and/or any antidepressant, especially Wellbutrin (bupropion hydrochloride).  Anyone with a history of a seizure disorder who needs to stop taking an anticonvulsant cold turkey needs to be discussing that with two neurologists and not getting your information from some stupid web site. Get off your computer and start making appointments!

If you’ve worked your way up to a particular dosage, it’s usually best to spend this many days at the next lowest dosage before going down the next lowest dosage before that and so forth. This is the least sucky way to avoid problems when stopping any psychiatric medication. Presuming you have the option of slowly tapering off them.

Comments: Be sure to read the section on anticonvulsants if you haven’t done so already.

Approved by the FDA to treat epilepsy in December 1993 Neurontin (gabapentin) is the weakest of the semi-official mood stabilizers,  but it works for me! Yet I am a known freak. Neurontin’s main problem is in the digestive tract, and that is allegedly going to be solved with the new and improved version, pregabalin, which might be on the market by the time you read this. As you can see from the data above, Neurontin’s bioavailability tends to be an issue as you take more of it. I’ve seen other figures indicating even lower bioavailability of Neurontin (gabapentin).  Maybe it’s because Neurontin (gabapentin) pretty much bypasses your liver and gets to your brain through the L-amino acid pathways.  Thus because Mouse and I are total freaks with food allergies and quite sensitive to those sorts of things, we probably get way more Neurontin (gabapentin) absorption than most people.  This is just a wild-ass guess on our parts.

Neurontin (gabapentin) has helped Mouse with her restless leg syndrome, and may be providing her with some mood stabilization.

The whole question comes up, is Neurontin (gabapentin) worth a damn as a mood stabilizer? Well it certainly shouldn’t be used first without some good reason, such as a comorbid chronic pain ailment or partial onset seizures. Basically the existing data show that Neurontin (gabapentin) isn’t that good of a mood stabilizer. At least, not if other stuff seems to work. However, if nothing else is working, adding Neurontin to the mix can sometimes help, although apparently not if rapid cycling is involved. It has helped me. How can I tell? First I tried to see what life would be like without Neurontin (gabapentin). Boy was that a bad time. Since then I switched from 300mg four times a day to 400mg three times a day, and found it to be less effective. If I missed a dose I was more susceptible to breakthrough hypomanias or depressions. At 400mg four times a day my memory is a bit worse, but if I forget a dose (which is now more likely since my memory is worse; like, duh) I don’t have a breakthrough event. The reports at Remedy Find and on the bipolar support groups follow the studies – generally useless for most people, but the one missing piece or the one drug that worked when all else failed for a small number of people.

Neurontin (gabapentin) can also be effective in treating panic/anxiety disorders. It’s not as good as the benzodiazepines or the antipsychotics in that regard, but if you’re not able to tolerate any medication from either of those classes, Neurontin (gabapentin) is certainly better than nothing. I’ve found it most helpful in dealing with my agoraphobia. It doesn’t do squat for Mouse’s anxiety. Like people in the one study referenced, Mouse found Neurontin (gabapentin) to aggravate her OCD.

It did start to work on my epilepsy once I got up to the 900mg a day level. Mouse told me the absence seizures were fewer (but they didn’t vanish completely until Topamax (topiramate) was added to the cocktail) and the partial-complex events also decreased in frequency and severity. Again it took the addition of Topamax (topiramate) to finally deal with all of my epileptic symptoms. But Neurontin (gabapentin) is quite the helpful medication for me.

As for all the pain stuff, it has helped Mouse with her fibromyalgia, with both the pain and the quality of her sleep, but she hits a wall of side effects. Above 1,200mg a day her memory becomes too bad for her to function. At 1,200mg a day Neurontin (gabapentin) helps a lot, but it could help more were it not for the memory issues. Other people we know taking it for chronic pain have reported a mixed bag of results, some positive some where nothing happened. The people posting at Remedy Find report along similar lines, with a few noting intolerable side effects.

Additionally Neurontin (gabapentin) has been studied and used for things like agitation in dementia patients, cocaine dependency and cravings, and alcohol withdrawal.

It all comes down to being literally able to stomach this stuff. Neurontin (gabapentin) is an effective medication for some people, a worthless sugar pill for others, and an evil source of side effects for a small unfortunate few. The real problem seems to have been Parke-Davis’ allegedly sleazy marketing practices, which prevented people from getting the correct medications and has led to an anti-anticonvulsant backlash. They took a good thing and oversold it, screwing it up for everyone else.  Expect the backlash to be worse now that Pfizer has settled for over 400 million dollars.

Now the Pfizer has acquired Parke-Davis and Neurontin (gabapentin) is to be superseded by pregablin, who knows what things will be like? Will pregablin be used for as many off-label applications? Will it be more or even less effective in some applications? Neurontin (gabapentin) will still be on the market, but things will be different after 2003.

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