ULDNTX
observations
Hard to believe that it's been over 2 years since I've started using
naltrexone and I thought it might be usefull if I wrote down some of my
observations which may be usefull to people interested in
experimenting with naltrexone. I should note that people who
chose to play around with naltrexone do so entirely at their own risk
and any contemplated experimentation should be undertaken in
cooperation with your physician. Even though the doses of
naltrexone may seem miniscule, there are some very interesting things
that seem to happen with endogenous opiate systems when one uses
naltrexone in conjunction with opiates.
One of the primary goals I had in using naltrexone in my patients was
to see if I could slow the rate of development of opiate tolerance in
patients on chronic opiate therapy. When people are put on
opiates for pain, usually they get a dramatic response initially with
low doses of opiates, but in some people the dose required to produce
the same level of analgesia dramatically escalates. It may be
possible to use naltrexone to limit the development of opiate
tolerance, but unfortunately the patients in whom I was most interested
in decreasing opiate tolerance were the least likely to use the
naltrexone properly. All I can say is that none of them had
adverse effects, but I doubt very much whether naltrexone is the
solution in reducing their daily doses of opiates.
The most interesting effects of naltrexone were when it was used
alone. Thus far I have one patient in whom naltrexone was
effective in this manner and while the results may be secondary to the
placebo effect, I've seen enough ULDNTX effects to think
otherwise. This 80 year old woman had severe spinal stenosis and
eventually developed continuous pain in her low back and legs.
She sought me out because of my tolerance for "alternative" treatments
and was reluctant to take any opiates or COX-2 anti-inflammatories
which I initially suggested to her. When I saw her, my interest
in ULDNTX was near its peak and I suggested it to her. Somewhat
to my suprise, she was very receptive to the idea and I started her on
1 microgram of Naltrexone 3 times daily with instructions to increase
the dose by a factor of two daily until she got relief of pain. I
gave her some 1 mg Naltreone capsules which she dissolved in juice and
diluted appropriately to get the necessary doses. When I next saw
her, she was up to 10 micrograms 3 times daily and her pain was
gone. She was ecstatic that she finally had relief from her
unremitting spinal stenosis pain.
If the result was due to placebo effect, then one would expect pain
relief at the 1 microgram dose. This dose did absolutely nothing
for her and once she hit 10 micrograms good analgesia resulted.
Now the placebo effect is thought to be mediated by endorphins as
placebo analgesia can be blocked with intravenous naloxone and it could
be that my action of giving her the naltrexone resulted in increased
endorphin release and the ULDNTX potentiated these endorphin
effects. She continued to use the naltrexone with good results
until she finally had surgery for her spinal stenosis and thereafter
needed no further exogenous analgesics.
The manner in which I've used ULDNTX is to tell people to make up a 100
microgram/ml solution which can then be diluted further so that one can
start very low and work up. The dose/response curve of naltrexone
potentiation of analgesia appears to be parabolic; no response at too
low a dose, a maximum response at a higher dose and then decreasing
effectiveness as one continues to increase naltrexone dose.
At some point, the dose of naltrexone will be high enough and it will
be algesic; ie increase pain as it assumes its expected opiate receptor
blocking role. The dose of naltrexone that will antagonize
exogenous opiates and increase pain is quite variable among
individuals. The lowest dose I've seen put a chronic opiate user
into withdrawal has been 1 mg; naltrexone is a competative opiate
antagonist and so to treat this withdrawal one needs to merely take
more opiates. The standard 50 mg tablet that naltrexone is
marketed in will definately put someone on chronic opiates into
withdrawal and taking this high a dose of naltrexone is NOT recommended.
Generally I suggest to patients that they experiment with
combining microgram doses of naltrexone with opiate analgesics and I
have seen reductions of around 50% in opiate analgesic doses when this
approach has been used. One indication that a drug is doing
something is when patients ask for more of it. I've had patients
use opiates and naltrexone in combination and then come back asking for
more naltrexone as it seemed to be helping with analgesia. My
practice has been to give people about 5-10 1 mg capsules to start off
with and then write prescriptions for further supplies of
naltrexone. Doses that patients have been using range from 10
micrograms 2-4 times daily to 100-200 micrograms 2-4 times daily.
One interesting thing about naltrexone is that there appears to be a
tolerance to its effects. 10 micrograms might work very well
initially, but then the dose needs to be increased to 100 micrograms,
and then 1 mg. I've had some patients go from 30 micrograms daily
to 1-2 mg/day. How much of the naltrexone is getting into the
bloodstream is problematic since naltrexone has very extensive, but
very individually variable hepatic metabolism.
An application of naltrexone that has nothing to do with its analgesia
enhancing effects involves the blockade of opiate receptors in the
bowel with naltrexone. One major problem of using opiates on a
chronic basis is constipation and this can be severe in some
people. Oral naltrexone in the proper dose can relieve this
constipation. I generally start people on 1-2 mg of naltrexone
taken at bedtime and usually they have a bowel movement the next
morning. Several of my patients have been using naltrexone in
this manner over the last two years althought it works best if used
intermittently rather than on a daily basis.
Until I get around to compiling all of my naltrexone notes into some
systematic form, the above material recalled from memory will have to
do.
Getting naltrexone in the proper doseage form is problematic. One needs
a compounding pharmacy to produce low dose naltrexone or people can do
it on their own by crushing the standard 50 mg tablets of naltrexone
and dissolving them in acidic solutions (vineger or acidic fruit
juices). In Vancouver, Canada, I use Kripps pharmacy to compound
pure naltrexone powder into 1 mg capsules. The contents of these
capsules can then be dissolved in fruit juice at the appropriate
dilution. Diet pop keeps better in the refrigirator.
The only thing I haven't done thus far is to prescribe doses of
naltrexone above 3 mg daily. I consider the 50 mg tablets of
naltrexone to be overkill and don't recommend their use except for
research purposes where one wants to find out what it feels like to
totally block ones opiate receptors.
Last modified 21/4/2004 T:=00:53