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Q: Getting Pacerone out of my system ( Answered 5 out of 5 stars,   1 Comment )
Subject: Getting Pacerone out of my system
Category: Health > Medicine
Asked by: lja-ga
List Price: $25.00
Posted: 11 Nov 2005 17:01 PST
Expires: 11 Dec 2005 17:01 PST
Question ID: 592082
Can a patient whose doctor has taken him off Pacerone do anything to
speed up the time it takes for that drug to leave his system? (The
doctor has said the side effects of Pacerone may last for months after
one stops taking it. I'd like to know whether drinking, eating or
doing something may speed that process.)
Subject: Re: Getting Pacerone out of my system
Answered By: crabcakes-ga on 11 Nov 2005 21:30 PST
Rated:5 out of 5 stars
Hello Lja,

     Your doctor is correct about Pacerone (amiodarone) lingering in
the body for a long while. Amiodarone is stored in fatty tissue, heart
and skeletal muscle, and the thyroid. The half life is 100 days,
meaning that after 100 days, half of the drug is eliminated from the
body. In another hundred days, half of what remained is gone, and this
pattern continues till the drug is eliminated. You can see it would
easily take over a year to eliminate the majority of the drug.

Example: Suppose you had 300mg stored in your body at the time of
discontinuation. In 100 days, you would have 150mg remaining. In
another 100 days, you would have 75mg remaining. In another 100 days
the level would be down to 37.5 mg.

I found nothing you could take to promote elimination. However, since
Pacerone is eliminated by the liver, take good care of your liver!
Don?t drink alcohol or take any unnecessary drugs or medications.

?There is no specific antidote for amiodarone intoxication. Amiodarone
is not dialysable.? Even having your blood cleansed by having dialysis
would eliminate the drug from your body.

If you are very concerned about your thyroid, you can ask your doctor
to order some TFTs (Thyroid Function Tests), including PBI, iodine
uptake, serum thyroxine (T4), reverse triiodothyronine (rT3) and free
thyroxine index (FTI) serum triiodothyronine (T3). Liver function
tests (LFTs) would be a good idea too, to get a picture of your
thyroid and liver health.

  Several drugs can inhibit the liver enzymes that metabolize
Pacerone, so don?t take the following drugs unless necessary, or drink
grapefruit juice.:

Protease inhibitors: 
?Protease inhibitors are known to inhibit CYP3A4 to varying degrees.
Inhibition of CYP3A4 by indinavir has been reported to result in
increased serum concentrations of amiodarone. Monitoring for
amiodarone toxicity and serial measurement of amiodarone serum
concentration during concomitant protease inhibitor therapy should be

Here is a list of protease inhibitors: 

Histamine H 2 antagonists: 
Cimetidine (Tagamet) inhibits CYP3A4 and can increase serum amiodarone levels. 

Other substances: 
Grapefruit juice inhibits CYP3A4-mediated metabolism of oral
amiodarone in the intestinal mucosa, resulting in increased plasma
levels of amiodarone; therefore, grapefruit juice should not be taken
during treatment with oral amiodarone?

?Amiodarone contains two iodine atoms. It is estimated that amiodarone
metabolism in the liver releases approximately 3 mg of inorganic
iodine per 100 mg of amiodarone into the systemic circulation. The
average iodine content in a typical American diet is about 0.3 mg/day.
Thus, 6 mg of iodine associated with a 200 mg dose of amiodarone
markedly increases the daily iodine load [6].
Amiodarone is very lipophilic and is concentrated in adipose tissue,
cardiac and skeletal muscle, and the thyroid. Elimination from the
body occurs with a half-life of about 100 days [7]. Amiodarone
toxicity can therefore occur well after drug withdrawal.?

Another report gives the half life of Pacerone as a mean of  53 days!
?In patients on long-term oral therapy, amiodarone has a biphasic
elimination pattern, with an initial decline in plasma levels observed
from 2.5 to 10 days after discontinuation of therapy. This initial
phase is followed by a marked rebound in plasma levels at 12 to 20
days post-dosing, before settling into a slower terminal elimination
phase. In one study (n=8), the plasma elimination half-life of the
parent compound ranged from 26 to 107 days (mean: 53 days).?

Pacerone is metabolized by the liver and excreted into the stool
through the biliary tract, in bile.
 ?The major enzyme responsible for the N-deethylation to DEA is
believed to be cytochrome P-450 3A4.?

?There is negligible excretion of amiodarone or DEA in urine. Neither
amiodarone nor DEA is dialyzable. Amiodarone and DEA cross the
placenta and both appear in breast milk.?

?The metabolite desethylamiodarone exhibited a distribution pattern
comparable to the parent drug. However, its maximum concentrations in
serum and tissues were consistently lower than the corresponding
amiodarone concentrations and varied from 18 to 55% (mean 27%),
depending on the acute oral dose applied and on the kind of tissue.
The amiodarone tissue/serum concentration ratios were high in lung
tissue (60-100) and moderate to high in the other tissues except brain
(3-60), and indicate an extensive distribution of the drug with the
lung as an organ with specific binding sites or uptake mechanisms and
adipose tissue as a reservoir with a large storage capacity. The
metabolite tissue/serum concentration ratios were very high in lung
tissue (500-800), high in renal, thyroid, liver and adipose tissue
(80-200) and moderate in the other tissues except for brain (20-60)?

General Information on Pacerone:

Other than pampering your liver for the next year, there is nothing
you can do to accelerate the elimination of the Pacerone. I urge you
to discuss this concern with your doctor, and not to fall for any
quack schemes.

Chelation therapy will not work.

I hope this had helped you out. If any part of my answer is unclear,
please request an Answer Clarification, before you rate. This will
allow me to assist you further, if possible.

Sincerely, Crabcakes

Search Terms

Amiodarone  +  half life
Amiodarone  elimination from body
Amiodarone + potentiate
Amiodarone absorbents
Amiodarone + antidotes
Amiodarone + chelation
lja-ga rated this answer:5 out of 5 stars
Thanks much, Crabcakes. A very thorough and understandable, albeit
substantively disappointing, answer. I'm pretty good with search
engines but surfaced nothing relevant myself, because I lacked the
medical expertise and/or skilled researcher expertise to hit the right
keywords. You did it -- and in record time. lja

Subject: Re: Getting Pacerone out of my system
From: crabcakes-ga on 11 Nov 2005 23:20 PST
Thank you for the 5 stars. I wish you the best!
Sincerely, Crabcakes

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