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Tips for tapering off Neurontin (gabapentin)

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tezza

 

 

Admin note: Details about tapering techniques are here

 

 

IMPORTANT:  There is an interaction between gabapentin and magnesium, see http://www.webmd.com/drugs/2/drug-9845-8217/neurontin-oral/gabapentin-oral/details/list-interaction-details/dmid-1207/dmtitle-gabapentin-aluminum-magnesium-containing-compounds/intrtype-drug.

 

Taking magnesium at the same time as gabapentin decreases the absorption of gabapentin.

 

Avoid taking aluminum or magnesium containing products (such as antacids) for 2 hours before your gabapentin.

 

 


 


I'm trying to get info on water titrating gabapentin. Anyone that can offer advice, please help.

 

Edited by ChessieCat
added admin note

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Altostrata

Thanks, Gia.

 

Thanks for opening this thread on Neurontin, tezza. The rules of thumb for tapering Neurontin are the same as with other psychiatric drugs: 10% trial reduction per month, etc.

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Altostrata

Neurontin comes in liquid form, which could be handy for tapering.

 

This study below suggests a solution made from a Neurontin tablet mixed in water will last quite a while under refrigeration. (Personally, I would keep it for a week, then throw out.)

 

Pharm Res. 1992 May;9(5):595-600.

Stability studies of gabapentin in aqueous solutions.

Zour E, Lodhi SA, Nesbitt RU, Silbering SB, Chaturvedi PR.

 

Source

 

Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Morris Plains, New Jersey 07950.

 

Abstract at http://www.ncbi.nlm.nih.gov/pubmed/1608888

 

Gabapentin is a gamma-aminobutyric acid analogue, which has been shown to be an effective antiepileptic. The solution stability of gabapentin in buffered systems was studied in order to facilitate the formulation of a liquid product. The degradation of the drug was followed as a function of pH, buffer concentration, ionic strength, and temperature. The results indicated that the rate of degradation was proportional to the buffer concentration and temperature. The pH-rate profile of gabapentin degradation showed that the rate of degradation was minimum at an approximate pH of 6.0. Further, the data suggested a slower solvent-catalyzed degradation rate for the zwitterionic species compared to the cationic or anionic species in the pH range of 4.5 to 7.0. There was no influence of ionic strength on the rate of degradation. Arrhenius plots of the data indicated that a shelf life of 2 years or more at room temperature may be obtained in an aqueous solution at a pH value of 6.0.

 

 

[Word of the day: zwitterionic.]

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Altostrata

Aka Gralise, Neurontin, Aclonium, Novo-Gabapentin, Apo-Gabapentin (Canada), CO Gabapentin (Canada), Gen-Gabapentin (Canada), Novo-Gabapentin (Canada), PMS-Gabapentin (Canada), ratio-Gabapentin (Canada), Gabapentina, Gabapentine, Gabapentino, Gabapentinum

Gabapentin originally was intended to treat epilepsy. From http://www.drugbank.ca/drugs/DB00996


Gabapentin, an analog of GABA, is used as an anticonvulsant to treat partial seizures, amyotrophic lateral sclerosis (ALS), and painful neuropathies. Potential uses include monotherapy of refractory partial seizure disorders, and treatment of spasticity in multiple sclerosis, tremor. mood disorders, and attenuation of disruptive behaviors in dementia. Gabapentin has high lipid solubility, is not metabolized by the liver, has no protein binding, and doesn't possess the usual drug interactions.

 
Gabapentin has a half-life of about 5-7 hours.
 
Like other psychiatric drugs, going off gabapentin can incur a withdrawal syndrome http://www.medscape.com/viewarticle/722526
 

American Journal of Health-System Pharmacy
Am J Health Syst Pharm. 2010;67(11):910-912.
 
Withdrawal Symptoms after Gabapentin Discontinuation
Thaddaus R. Hellwig, Rhonda Hammerquist, Jill Termaat
 
Abstract
Purpose. A case of apparent gabapentin withdrawal symptoms after discontinuation of gabapentin therapy is reported.

Summary. A 53-year-old woman had coffee ground emesis, a two-day history of black tarry stools, and abdominal pain. ....On day 5, gabapentin was reinitiated, and the patient's confusion and agitation improved that evening. The next morning, the patient was calm, alert, and cooperative. Her symptoms resolved, and she was discharged on hospital day 7.

Conclusion. A patient developed apparent withdrawal symptoms beginning two days after gabapentin therapy was discontinued. The symptoms were unresponsive to treatment with benzodiazepines but completely resolved with the reinitiation of gabapentin therapy.
....
Patients who have abruptly discontinued gabapentin have reported symptoms of anxiety, diaphoresis, irritability, agitation, confusion, tachycardia, catatonia, and status epilepticus.[16–22] The symptoms that have been associated with gabapentin withdrawal tend to mimic some of the same withdrawal symptoms associated with ethanol and benzodiazepine withdrawal, possibly because gabapentin augments GABA levels, as does ethanol and benzodiazepines. We describe a case of withdrawal symptoms after discontinuation of gabapentin therapy.
....
Discussion
The temporal relationship between the development of symptoms about three days after gabapentin discontinuation and the absence of any improvements during the administration of benzodiazepines for presumed ethanol withdrawal suggest gabapentin withdrawal syndrome.

All of our patient's symptoms were typical of ethanol and benzodiazepine withdrawal syndromes. The patient received several doses of lorazepam, with no subsequent improvement in any of her symptoms. Once gabapentin was restarted, the patient's symptoms quickly improved and disappeared within a day.

Several case reports have described a possible gabapentin withdrawal syndrome, including symptoms such as irritability, agitation, anxiety, tachycardia, diaphoresis, confusion, disorientation, catatonia, and status epilepticus.[16–22] The symptoms of all of the patients described in these case reports resolved within one or two days after the reinitiation of gabapentin.
 
Gabapentin therapy may lead to increased levels of GABA synthesis.[3–5] Ethanol and benzodiazepines both augment GABA levels and are associated with a withdrawal syndrome upon abrupt discontinuation. Given the similarity of symptoms among ethanol, benzodiazepine, and gabapentin withdrawal syndromes, the common thread may be those agents' effects on GABA levels.
 
Pittenger and Desan%5B17%5D described two cases of patients suffering from gabapentin withdrawal treated with benzodiazepines without any improvement in symptoms. Both patients had a history of ethanol abuse, though they had no documented recent use of ethanol. One, a 33-year-old man, developed confusion, diaphoresis, disorientation, agitation, and tachycardia after discontinuing gabapentin 3600 mg daily. He received benzodiazepines without benefit, but his symptoms improved over two days after restarting gabapentin. The other patient, a 63-year-old man, had hallucinations, tachycardia, diaphoresis, and agitation after discontinuing gabapentin 4900 mg daily. Treatment with lorazepam 48 mg for two days produced limited improvement in symptoms, but the symptoms quickly improved once gabapentin was restarted.
 
These cases and the one we describe suggest that benzodiazepines may be an ineffective treatment option for gabapentin withdrawal. Of note, our patient was receiving a lower dose of gabapentin compared with patients described in other case reports.
 
The timing of ethanol ingestion in our patient raises the possibility that she actually experienced an ethanol withdrawal syndrome that was totally unresponsive to benzodiazepine therapy but was relieved by gabapentin. Although trials have examined the use of gabapentin for ethanol withdrawal,[10–15] we are unaware of studies that used gabapentin for benzodiazepine-resistant ethanol withdrawal symptoms.
 
Practitioners should be alert to the possibility of a withdrawal syndrome associated with gabapentin that mimics that of benzodiazepines and ethanol.
....

 
Reduce by 10% per month to start
The 10% rule holds for gabapentin, just like other psychiatric drugs: Reduce by 10% per month, calculated on the last dosage. (The amount of the reduction gets progressively smaller.)

See Why taper by 10% of my dosage?
 
Using tablets to taper
According to FDA information at http://www.drugs.com/ppa/gabapentin.html, gabapentin comes in the dosages below. Gabapentin is supplied as tablets or capsules.
 

Horizant
- Tablets, ER, oral 600 mg

Gabapentin (base)

Gralise
- Tablets, oral 300 mg
- Tablets, oral 600 mg

Neurontin
- Tablets, oral 600 mg
- Tablets, oral 800 mg
- Capsules, oral 100 mg
- Capsules, oral 300 mg
- Capsules, oral 400 mg
- Solution, oral 250 mg per 5 mL
Apo-Gabapentin (Canada)
CO Gabapentin (Canada)
Gen-Gabapentin (Canada)
Novo-Gabapentin (Canada)
PMS-Gabapentin (Canada)
ratio-Gabapentin (Canada)

 
When tablets are scored, they may be split. Cut them up with a pill cutter, available at any drug store. Capsules filled with powder may be opened for titration.

You may wish to precisely measure your dosage with an electronic scale that measures milligrams. These are available for under $30 US. See http://survivingantidepressants.org/index.php?/topic/1596-using-a-digital-scale-to-measure-doses/
 

Given the lack of low-dosage tablets to split and the dosage range of the capsules, the best method for a gradual, precise taper would be to use gabapentin liquid.

Using gabapentin liquid concentrate to taper
http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=c64c09c9-0567-4a4f-b2c6-8f667986c9af

HOW SUPPLIED

Gabapentin Oral Solution is supplied as follows:

250 mg/5 mL oral solution; Clear, colorless to slightly yellow solution; each 5 mL of oral solution contains 250 mg of gabapentin; available in: Bottles containing 470 mL: NDC 50383-311-47

Storage

Store refrigerated, 2°-8°C (36°-46°F)
....
The inactive ingredients for the oral solution are artificial cool strawberry anise flavor, d-xylitol, glacial acetic acid, glycerin, purified water, and sodium acetate. Glacial acetic acid and/or sodium acetate used to adjust pH.

 
As it is in a 50mg per mL concentration, this means using an oral syringe to measure out the proper amount. If you wish to take 50mg, you would take 1mL from the bottle.

If you are taking 500mg and wish to reduce by 10% (50mg), you would take 9mL (450mg) from the bottle.

Make your own liquid
According to the FDA, gabapentin "is freely soluble in water." Many people make their own liquid for tapering from tablets, or the powder from a capsule, and water. (A liquid made from gabapentin and water is quite stable, see http://survivingantidepressants.org/index.php?/topic/2309-tips-for-tapering-neurontin-gabapentin/?p=22919)

 

See How to make a liquid from tablets or capsules
 

Using a combination of tablets or capsules and liquid

Rather than switch directly to an all-liquid dose, you may wish to take part of your dose in liquid and part in lower-dose tablets or capsules, gradually converting to all liquid as you get to lower dosages. This can be very convenient and reduce any problems switching from one form of the drug to another.

If your doctor prescribes liquid and tablets or capsules at the same time, most likely, he or she will have to indicate "divided doses" in the prescriptions to get the drugs covered by insurance.

Have a compounding pharmacy make up capsules of smaller dosages
A compounding pharmacy will accurately weigh small doses and put them into capsules for you. See http://survivingantidepressants.org/index.php?/topic/235-tapering-techniques/page__p__3001#entry3001

 


 

NOTE There is an interaction between gabapentin and magnesium, see http://www.webmd.com/drugs/2/drug-9845-8217/neurontin-oral/gabapentin-oral/details/list-interaction-details/dmid-1207/dmtitle-gabapentin-aluminum-magnesium-containing-compounds/intrtype-drug. Taking magnesium at the same time as gabapentin decreases the absorption of gabapentin. Avoid taking aluminum or magnesium containing products (such as antacids) for 2 hours before your gabapentin.

Edited by Altostrata
updated

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Shanti

Somewhere along the line during my tapers, I tapered off of 1800 mg on Neurotin, kind of fast I recall. But I simply don't remember how in the world I did it. Everything is a blur. Well, I decided to try Neurontin again from my new doctor. I wanted to really pay attention to if it helped the nerve pain. I've been on 600 mg a day of it for about a month, and before that 300 mg for a month. I wonder if I can't do a quick taper. I mean, if I had bad symptoms from that 1800 mg taper then I'd surely remember. I'm such a space case from the last year. I need off the Neurontin. It's making me incredibally tired and I feel yucky, and it's not helping my pain.

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Altostrata

I would think you could back down to 300mg rather quickly, maybe in two steps over 10 days? Then a little slower off 300mg?

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Shanti

That sounds good. I have the capsules. Does that dilute in water well? That would be easy to just dilute it and then take half of it.

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RebelMaven

I'm doing a gabapentin taper as well and just wanted to mention that when I mix the contents of capsules in water it does not make a solution but a suspension. The drug may be water soluble and be in solution but it appears that the binders are not and they remain in suspension.

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Altostrata

Yes, that's the case with most of these drugs. It's not truly a solution unless all the particles are dissolved. So shake gently before drawing your dosage from a homemade liquid!

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tezza

I had the 300mg capsules also. I mixed with water and took 3/4 of suspension for about a week, then I took 1/2 for a week...then 1/3 for about a week and finally 1/4 for three or four days. At that point I forgot to take it one night so I left off there.

 

Thank you, Alto, for advising me to taper the neurontin as my next step. I'm so glad to be free from, at least, one med completely.

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elgee

Hi,

 

I am 9 months benzo free and have been feeling pretty good. I've decided to start a very conservative microtaper off of gabapentin today. I know that if things get rough I can always back off and try it again later. For those of you that have stepped off more than one drug, how long did you wait until you started another taper?

 

Thanks,

Elgee

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Shanti

Hi elgee. Congratulations on finishing your benzo taper! That is awesome. As for Gabapenten, (Neurontin, right?) I've tapered off it twice and had very little trouble. However, I was never on it that long. I think the longest was maybe 6 months or so. Both times I did quick tapers, so you might not want advice from me if you're sensitive to it or been on it long.

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Rhiannon

Elgee, I think if you've been feeling pretty good, that's a good time to start another taper. It sounds like you know to watch your body''s reaction and be conservative, especially at first. It's better to start small and slow and then gradually ramp up to tolerance.

 

Sounds like you know what you're doing. I'd say go for it!

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butterfly65

I have read much info on this site about using magnesium to help with gabapentin withdrawal. I am up to 700 mg of magnesium per day but am experiencing more withdrawal symptoms from gabapentin.  I am currently taking the magnesium

3x a day and noticing that when i take my afternoon dose of gabapentin at 3p.m. I feel worse, more nerve pain and anxiety. should i take the magnesium at diff times? Am I detoxing?

 

here is my schedule

 

magnesium 200 mg 6 am

gabapentin 200mg 8 30am

magnesium 200mg 1 00pm

gabapentin 300mg 3 pm

magnesium 200mg 6 pm

magnesium 100mg 7pm

gabapentin 300mg 11pm

 

 I also use epsom salts rinses with taper but only for a coupe of days until next taper. I am wondering if the magnesium is binding with the gabapentin and putting me into more withdrawal? Any help would be much appreciated.

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westcoast

I searched the web for: magnesium gabapentin interaction
 
There were pages of links that said there is an interaction. Few looked authoritative.
 
1. Medscape listed a study that found an interaction; I don't know if it's a good study though:

Once-daily Gastroretentive Gabapentin for the Management of Postherpetic Neuralgia
http://www.medscape.com/viewarticle/769493_6

"Aluminum and magnesium-based antacids taken immediately prior to gabapentin TID reduce its bioavailability by about 20%, but only by about 5% if gabapentin TID is taken 2 h after the antacid [Neurontin, 2010].

 

 

2. Drugs.com listed no interactions:

http://www.drugs.com/interactions-check.php?drug_list=1147-0,1511-0

 

 

3. Typical of the non-authoritative type (ie., no citations):

http://www.healthboards.com/boards/back-problems/369552-gabapentin-depletes-these-nutrients.html

 

"It did say not to take these supplements (the pharmacist said ANY really) within two hours of taking gabapentin. You shouldn't take any supplements within two hours of taking gabapentin, especially magnesium and calcium and folic acid. So be aware of that. That really goes for any med. He said the magnesium and calcium bind to the drug reducing its efficiency."

 

Search query:
https://www.google.com/search?q=magnesiusm+gabapentin+interaction#q=magnesium+gabapentin+interaction

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Altostrata

It helps to ask Dr. Google about things like this. Googling "magnesium gabapentin":
 
http://www.webmd.com/drugs/2/drug-9845-8217/neurontin-oral/gabapentin-oral/details/list-interaction-details/dmid-1207/dmtitle-gabapentin-aluminum-magnesium-containing-compounds/intrtype-drug
 

Neurontin Interactions Gabapentin/Aluminum; Magnesium-Containing Compounds

Medical warning:
Moderate.

These medicines may cause some risk when taken together....

How the interaction occurs:
Aluminum or magnesium containing products may decrease the amount of gabapentin your body absorbs.

 

What might happen:
The amount of gabapentin in your blood may decrease....

 

What you should do about this interaction:
Avoid taking aluminum or magnesium containing products (such as antacids) for 2 hours before your gabapentin.....

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butterfly65

Altostrata,

 

Thank you for this info. It seems that this could be happening, the magnesium is binding with the gabapentin and leaving me in protracted withdrawal continuously.

 

But now i am confused about the use of magnesium then to help with withdrawal. Should magnesium be used only after a taper to help with immediate withdrawal symptoms, then stop to allow body to adjust to new neurontin dose? I have read posts where some are taking magnesium all day, sipping it. Is that better? Better absorption and less interference perhaps? 

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Altostrata

Most people are not taking gabapentin. If magnesium is a problem for you, stop taking it.

 

Magnesium does not aid tapering. It helps reduce some symptoms. If you do not have those symptoms, or if magnesium does not help you, you don't have to take it.

 

Even if you are taking gabapentin, if you wish to also take magnesium, simply do this:

 

Avoid taking aluminum or magnesium containing products (such as antacids) for 2 hours before your gabapentin

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