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Altostrata

Tips for tapering off amitriptyline

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Altostrata

Aka Vanatrip, Elavil, Endep, Saroten Retard

 

Official FDA information at http://www.drugs.com/pro/amitriptyline.html

 

Amitriptyline is a tricyclic antidepressants (TCA). Its half-life is highly variable, estimated at 10-26 hours, but it breaks down to an active metabolite, nortriptyline, with a half-life of 18-44 hours (see https://online.epocrates.com/u/10a136/amitriptyline

 

Nortriptyline has its own active metabolite, 10-hydroxynortriptyline, half-life of 8-10 hours (https://www.springerlink.com/index/P65310133707531P.pdf

 

The overlapping metabolism of amitriptyline and the 2 active metabolites nortriptyline and 10-hydroxynortriptyline is probably why it's so difficult to estimate the half-life of this medication: amitriptyline (10-26 hrs) ---> nortriptyline (18-44 hrs) ---> 10-hydroxynortriptyline (8-10 hrs)

 

(Nortriptyline, marketed on its own as another tricyclic antidepressant (ex. Pamelor), is metabolised by liver enzyme CYP2D6. See Official FDA Information for Nortriptyline http://www.drugs.com/pro/nortriptyline.html

 

From http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20(General%20Monographs-%20A)/AMITRIPTYLINE.html

Pharmacokinetics: Amitriptyline is well absorbed from the gastrointestinal tract with peak plasma concentrations occurring between 2 and 12 hours after administration. Bioavailability of the drug is between 30 and 60% due to extensive first pass metabolism of the drug in the liver. Amitriptyline is demethylated in the liver to its primary active metabolite, nortriptyline.

....

Its elimination half-life varies from 10 to 50 hours, with an average of 15 hours. Within 24 hours, approximately 25 to 50% of a dose of amitriptyline is excreted in the urine as inactive metabolites; small amounts are excreted in the bile.

....

Drug Interactions [see the page for full list]

....

Selective Serotonin Reuptake Inhibitors (SSRIs): Amitriptyline toxicity may occur if used concurrently with fluoxetine, because of inhibition of the hepatic mirosomal enzyme responsible for the metabolism of amitriptyline. Reduction of amitriptyline dose by as much as 75% may be necessary. The potential for this interaction occurring with other SSRIs must be considered. Because of the extremely long elimination half-life of fluoxetine, the potential for interacting with other drugs remains for several weeks after its discontinuation. Thyroid Medications: Concomitant use of amitriptyline and levothyroxine may potentiate the cardiovascular effects (e.g., arrhythmias) of both drugs. ....

 

Harm reduction: Taper by 10% As with other psychiatric drugs, a conservative taper of 10% per month, calculated on the last dosage (the amount of the decreases keeps getting smaller), is recommended to minimize withdrawal symptoms. See http://survivingantidepressants.org/index.php?/topic/1024-why-taper-by-10-of-my-dosage/

 

Tablet dosages

In the US, amitriptyline comes in 10mg, 25mg, 50mg, 75mg, 100mg, 150mg tablets. See FDA information at http://www.drugs.com/pro/amitriptyline.html Sometimes the tablets are taken in 3 to 4 divided doses per day or all at bedtime per http://www.drugs.com/dosage/amitriptyline.html

 

Sustained-release capsule dosages

In Europe, amitriptyline is available from Lundbeck as Saroten Retard (amitriptyline hydrochloride in a sustained release formulation) in 25mg and 50 mg capsules.

 

Here is the package insert from Lundbeck for Saroten Retard: http://home.intekom.com/pharm/lundbeck/saroten.html

Amitriptyline as such is rapidly absorbed but owing to the sustained release from SAROTEN RETARD capsules amitriptyline only becomes available for absorption slowly. This results in a rather flat serum concentration curve.

 

Probably, as in many extended-release formulations, the coating on the pellets inside the capsules is what delays the release of the entire dose at once.

 

Cutting up tablets

If you are taking the tablets, you can cut them up. For precise dosing, weigh the pieces with a digital scale.

 

Using amitryptyline liquid to taper

Amitryptyline is available as a liquid in the UK http://www.patient.co.uk/medicine/Amitriptyline.htm

The liquid needs refrigeration.

 

Order a liquid from a compounding pharmacy

Compounding pharmacies can make a liquid from medications that do not have special extended-release coatings or Cymbalta. Your doctor will have to write a prescription specifying how the drug is to be compounded.

 

Dissolving amitriptyline in water to make a liquid

About basic amitriptyline in tablets: Manzo 2006 Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Amitriptyline Hydrochloride http://www.fip.org/files/fip/BPS/BCS/Monographs/Manzo%202006.pdf

Amitriptyline hydrochloride is soluble 1:1 in water.11 The USP and the Ph. Eur. report this API to be ‘‘freely soluble in water’’.

 

How stable is this solution of amitriptyline in water? See Buckles 2008 The stability of amitriptyline hydrochloride in aqueous solution http://onlinelibrary.wiley.com/doi/10.1111/j.1365-2710.1976.tb00052.x/abstract

The present work, using thin layer chromatography and polarography, reports that solutions of amitriptyline hydrochloride in purified water at room temperature are stable for at least 8 weeks if protected from light.

 

Theoretically, you should be able to make a solution of amitriptyline in water, and use an oral syringe for precise dosing. See How to make a liquid from tablets or capsules

 

I haven't personally done this and I don't know of anyone who has, so if you do it, please post your experience in this topic.

 

Counting out pellets (sustained-release amitriptyline capsules)

As with Effexor XR, opening the capsule and counting out pellets is the only way to taper sustained-release amitriptyline by very small amounts. If you dissolve your sustained-release amitriptyline hydrochloride in water, my guess is you would get basic fast-release amitriptyline. We don't know how your nervous system would respond to this. I don't know anyone who's done it. If you try it, please post your experience in this topic.

 

Converting from sustained-release capsules to regular tablets

As with Effexor XR, to use the tablet cutting method, one might taper by converting from sustained-release amitriptyline capsules to regular amitriptyline in the same daily dosage amount. Keep in mind the sustained-release capsules gradually release the dosage over some number of hours, and amitriptyline's unpredictable half-life. Depending on how your nervous system interacts with the drug, converting to tablets may require taking the tablets in in 3 to 4 divided doses per day. You can then cut up the tablets to reduce the daily dosage. I don't know anyone who's done this. If you do it, please post your experience in this topic.

 

Use 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.

Edited by Altostrata
updated

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MrsGreen

Alto, I am amazed about all this information, thank you!

I think I will get another prescription and continue to take out the little balls.

I feel the ones I have left might have suffered in the light and I just can't risk worse nights right now!

 

I will keep returning to this post for reference.

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Altostrata

I suggest you save the little balls in a clean, airtight medicine container, you can use them later.

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MrsGreen

Good idea, you mean the sunlight hash't damaged them yet?

 

Take care,

Mrs. Green

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Altostrata

Discard the ones that have been exposed to light, heat, or moisture.

 

Keep any new ones you take out of the capsule. You can always discard them later if you don't use them.

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Danack

Hia,

 

Been put onto this funny old stuff for nerve pain. Now I missed a dose the Friday night and then on Saturday night I had a nightmare. (Whereas on  I normally just have really boring dreams on the stuff).

So, I know I've got to be a bit careful with this stuff and what I read here confirms that.

 

I'm taking 20mg per night at the moment and I want to taper it right down to the bare minimum to control the pain because I don't think it's doing my mental health any good. I'm not sleeping the same as I was.

 

. So if I look at doing the following:

- 20mg this week

- 15 mg next week

- 10 mg the week after that

 

Would this work or do I need to even more careful...?

 

Thanks,

Danack.

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Danack

I should mention that it's the tablets that I've been given, the little blue ones, so there's no little balls or anything like that, I will need to get a pill cutter.

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Rhiannon

Hia,

 

Been put onto this funny old stuff for nerve pain. Now I missed a dose the Friday night and then on Saturday night I had a nightmare. (Whereas on  I normally just have really boring dreams on the stuff).

So, I know I've got to be a bit careful with this stuff and what I read here confirms that.

 

I'm taking 20mg per night at the moment and I want to taper it right down to the bare minimum to control the pain because I don't think it's doing my mental health any good. I'm not sleeping the same as I was.

 

. So if I look at doing the following:

- 20mg this week

- 15 mg next week

- 10 mg the week after that

 

Would this work or do I need to even more careful...?

 

Thanks,

Danack.

 

As Alto says, if you've been taking it more than a month, this is MUCH too fast.

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ang

This site is so wonderfu!   My dear friend,  is on endep          Wants me to research it, and damn more information, instantly on this thread!  This person had  idea it is an SRNI.

 

I thought it was an old tricyclic,   this thread has put me straight.    

 

This person wanted was a sleeping tablet,   this doctor has written on the box  ""take one at night, as required""...................    with an SRNI!!!!!!!!!!!!!!!!

 

Advice, very welcome.    Please help me here, with my friend,  had to have 2 weeks off work, and not travelling well.               Hopefully, my friend, has only taken a few taqblets,  odd nights,   if so, my advice will be   STOP TAKING THEM!!!

 

Otherwise, I will be back here for advice...................................                   Alto, you are a lifesaver!              Seems gps put people on this stuff, with a damn take one tablet at night, as required?          OMG.

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Beary

Same story. I was told to take one tablet per night to help me sleep. I took 10 mg tablets, once a day for three nights then stopped. One month later I still have tingling and muscle jumps. My doc wants me to take a course of steroids and I am not sure how this will effect my symptoms. He has diagnosed me with whiplash.

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peng

Just been prescribed for my wife's, now-troubling, osteoarthritis.

 

First thing I read on two websites is that the drug is a tricyclic antidepressant and not SNRI as we see here on this thread.  ????

I am wary on my wife's behalf due to my own 15 years of trouble with Effexor.

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scallywag

Peng, prescription drug regulations allow prescribing amitriptyline to "treat" symptoms of "depression." Other uses are off-label. You may wish to check what the equivalent prescribing rules are in the U.K.:

 

MHRA - amitriptyline

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peng

Thanks for that s'wag!

Yes, probably offlabel for some pain problems.

Confirms it is a tricyclic ad.

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Altostrata

Yes, it's a tricyclic. Sorry for the error in #1, corrected.

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Melissa5000

I have some tablets of amitriptyline that have a coating. This might be a gastric juice resistant coating.  

 

Can I cut up those tablets or make a liquid from it in despite of the coating? 

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Altostrata

Look on the package and check with the manufacturer. Most likely, the coating doesn't do anything but protect the tablet, it has no timed-release properties, and the tablet can be split.

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