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» LymeNet Flash » Questions and Discussion » Medical Questions » The secret is in the dose--Artemisinin.

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Author Topic: The secret is in the dose--Artemisinin.
Dave6002
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Artemisinin and other Artemnisia derivatives have become popular among LLMD and Lymies for lyme treatment especially Babasia treatment and seems are effective.

However, the dramatic cure seen in malaria has never happened in Babesia.

Why?

The secret probably is in the dose.

3X100mg of Artemisinin daily did nothing for me.

3X100mg of Artemether (6 times stronger than Artemisinin) daily quieted my heart immeadiately whithin a day, giving me severe fatigue.

Quite a few people here have the similar experience.

Some even suspected if Artemisinin has anything good for Lyme treatment.

The secret is in the dose.

I am going to ramp up the doses of artemether to the doses as high as possible.

People used Artemisinin for malaria up to 1600mg per day for three days.

Could I double it to 3200mg for Babesia?

For Artemether, it could be 600mg=3x200mg per day for three days then off 4 days.

Very high dose (5000mg) of Artemisinin caused liver inflammation, which resolved upon discontinuing of the herb.

The idea is to use Artemisinin doses high enough to kill the bugs but not cause big damage to the hosts.

This could be achievable as Artemisinin has mild side effects.

Believe me, I don't want to suicide. [lol]

So I publish my plan.

Any comments or suggestions?


Thanks.


Dave

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LYMESCIENCE
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GREAT NEWS MAN. Publish the pain. Clinical trials, clinical trials!!1
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LYMESCIENCE
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Artemether??

Where did you obtain this?

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5dana8
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Be careful

--------------------
5dana8

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mag
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hi dave

thanks for the info on artemesia
here are some questions

got some z max 2000 mg x 5 doses over 5 weeks
but did not get mepron approval for the babesia-
so i want to combo z max and artemesia with astralagus

I have been dosin the art for 3 to 4 days then off for a week or two - MY lfts (liver) are elevated already and have some valve problems - It makes me very ill

Most people say there is no herx - Are you sick for several days after dosing?
Did you order it or buy at a health food store?
Appreciate you sharing the good info

mags

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SForsgren
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1600 mg sounds reasonable for 3 days. Doubling that does not. Dr. K mentions in high doses in his teachings at about 1500mg per day for 3 days.

--------------------
Be well,
Scott

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GiGi
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Want to follow Scott's post:

Yes, that's what Dr. K. uses for three days. Then repeated two weeks later, etc. until symptoms resolved.

Take care.

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treepatrol
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quote:
Originally posted by LYMESCIENCE:
Artemether??

Where did you obtain this?

( �-Artemether/ Artemisinin / Artusenate)

--------------------
Do unto others as you would have them do unto you.
Remember Iam not a Doctor Just someone struggling like you with Tick Borne Diseases.

Newbie Links

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pq
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teh excellent site Tree provided says that there various fractions are fat, alc., and water soluble.
knowing these would suggest that, for example, that mixing it with a household fat should maximize absorption and effectiveness of the fat sol. fractions of artem.

one question would be which fat is best, saturated or unsat.? i'd think a sat. fat would be best; e.g.: coconut oil, or lard. But ask the company.

doing this would negate the need for increasing the dose beyond that prescribed, because you've maximized the chances of getting at least the fat-sol. fractions into the system.

i don't know for sure, but, even though some effective fractions are alc.-sol., i'd guess (w/o proof) that adding alcohol to the mix might destroy the fat and water sol. fractions.


best to write or call the company.

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Dave6002
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Thanks guys for your input.


Tree's link is especially useful: Grapefruit juice concentrate increases the bioavailability of artemether by over two times.

I'll make some Grapefruit juice concentrate and try it out.

Mags:
quote:
Are you sick for several days after dosing?
I was bedriden for a couple days after one week of Artemether at 3X100mg when I first time took it. (Now I didn't have much of that. Just getting better. I was taking 2X50mg of Iron)

The main symptoms were severe fatigue and weekness. I am not sue this is a herx or side effects of the drug.

quote:
Most people say there is no herx -


I was wondering if it was due to that the doses were not high enough.

quote:
Did you order it or buy at a health food store?
I ordered form the web.

Take care.

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8man12
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good info page on ART


http://www.drlam.com/A3R_brief_in_doc_format/Artemisinin.cfm#7

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Jon
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When should one take the fatty foods and grapfruit juice?? I take 2 100mg pills spread across the day... Should i take it before I take each dose?

A 2 week break sounds rather long, why is it 2 weeks, and not one week?

(from that link)

"When ART is tested with monkeys, they showed no toxicity when they received up to 292 mg/kg of artemether over 1 to 3 months. This is equal to a human dose of 20,000 mg for a 70 kg male"

WOW!!!!!!!!!!!! I dont know how reliable this website is though.

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Jon
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Another question. I live in Canada and Artemisinin for some #%@#$@#$ reason is illegal to sell here. I found one Canadian website and ordered the Artemisinin but it was really PRICEY.
It came to 50 Dollars CAD after tax and shipping.
Artemisinin

1st Question- Does anyone know if I can buy this stuff at a cheaper price?

2nd Question- The are selling art made by NUTRICOLOGY. By reading the description (see the provided link) it seems like its HIGH quality stuff! Can anyone comment on that and if its worth 50 dollars?


Thanks so much. [kiss]

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8man12
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http://www.1stchineseherbs.com/


1 POUND is 7.99 us.It will last 4.5 months at a high dose.

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oxygenbabe
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Malaria separates heme in the hemoglobin with hemezoin, and then there is free iron, and artemisinin is a free radical that in the presence of iron sort of explodes everything in its presence.

I've never been able to determine if babesia--which does not have hemezoin--works in a similar fashion, creating free iron in the blood cell.

It may work well for babesia, or only marginally so.

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Jon
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That website only has Artemesia not Artemisinin.
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Dave6002
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quote:
Unlike quinoline-based antimalarials (e.g., chloroquine) which have only one mechanism of action, trioxanes (artemisinin and its derivatives) kill malaria parasites probably by generating more than one type of cytotoxic intermediate. Thus, trioxanes are versatile prodrugs, triggered by ferrous iron, to produce several different types of highly reactive intermediates (e.g., oxy radicals, carbon radicals, high-valent iron-oxo species) as well as several different kinds of longer-lived neutral electrophiles (e.g., epoxides, aldehydes, and dicarbonyl compounds). This fundamental characteristic of trioxanes to act as prodrugs for generating such a wide variety of different harmful species suggests that it will be difficult for malaria parasites to develop resistance to this promising class of new antimalarial agents.

Acc Chem Res. 2004 Jun;37(6):397-404.


Knowledge of the proposed chemical mechanism of action and cytochrome p450 metabolism of antimalarial trioxanes like artemisinin allows rational design of new antimalarial peroxides.

* Posner GH,
* O'Neill PM.

Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA. [email protected]

Evidence is reviewed elucidating the mechanism of iron-induced triggering of antimalarial trioxanes. As prodrugs, trioxanes undergo homolytic, inner-sphere, reductive cleavage by ferrous iron to form sequentially oxy radicals, carbon radicals, high-valent iron-oxo species, epoxides, aldehydes, and dicarbonyl compounds. One or more of these reactive intermediates and neutral alkylating agents likely kill the malaria parasites. Several new, orally active antimalarial peroxides have been designed rationally based on this fundamental mechanistic paradigm. Incorporating metabolism-blocking substituents also provides some new, potent, semi-synthetic artemisinin derivatives.


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Dave6002
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quote:
Mechanism of action

The specific mechanism of action of artemisinin is not well understood, and there is ongoing research directed at elucidating it. When the parasite that causes malaria infects a red blood cell, it consumes hemoglobin and liberates free heme, an iron-porphyrin complex. The iron reduces the peroxide bond in artemisinin generating high-valent iron-oxo species, resulting in a cascade of reactions that produce reactive oxygen radicals which damage the parasite leading to its death.[2]

Numerous studies have investigated the type of damage that these oxygen radicals may induce. For example, Pandey et al. have observed inhibition of digestive vacuole cysteine protease activity of malarial parasite by artemisinin.[3] These observations were further confirmed by ex vivo experiments showing accumulation of hemoglobin in the parasites treated with artemisinin, suggesting inhibition of hemoglobin degradation. They found artemisinin to be a potent inhibitor of hemeozoin formation activity of malaria parasite.

A 2005 study investigating the mode of action of artemisinin using a yeast model demonstrated that the drug acts on the electron transport chain, generates local reactive oxygen species, and causes the depolarization of the mitochondrial membrane. [4]

The oxygen radicals have also been shown to inhibit PfATP6, a SERCA-type enzyme (calcium transporter) and artemisinin has been shown to compete with thapsigargin for SERCA binding, though artemesinin is much less toxic to mammalian cells.

Resistance is conferred by a single mutation in the calcium transporter (PfATP6). This mutation has been studied in the laboratory but recently a study from French Guiana in field isolates of malaria parasites has identified a different mutation in the calcium transporter (PfATP6) that is associated with resistance to artemether.[5]
[edit]

from Wikipedia


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liz28
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Hi, Dave. Always love your posts, but hope to throw in an alternative explanation on this one.

Supposedly, artemisinin works well because it immediately lowers the amount of active malaria in the body, but only on a temporary basis.

In drugs like Riamet, two malaria drugs are taken at once, artemether and lumefantrine. The artemether lowers the malaria levels right away, so you don't die before the second drug has a chance to kick in. It also has an effect on malaria strains that have developed resistance to chloroquine. However, it has a short elimination half life, which limits the ability of malaria to develop resistance to it, but also doesn't allow it to stay in your body very long. Here's a Novartis website on Riamet:

http://www.malariaandhealth.com/professional/riamet_coartem/02_anewoption.htm

"Combining antimalarials - the advantages

Artemisinin derivatives have a short elimination half-life (2-3 hours), which means that they carry a smaller risk of developing resistance. The main drawback of the short half-life is that it results in substantial recrudescence if artemisinin derivatives are used alone for less than 5 days. Therefore, artemisinins are commonly used in free combination with other antimalarials.

Furthermore, a fixed combination of two antimalarials offers significant advantages over the free combination of such drugs. Firstly, it facilitates compliance, and secondly, by preventing the patients from taking either drug alone, it helps to prevent the development of resistant Plasmodium strains.

Riamet�/Coartem� - a highly effective combination

Riamet�/Coartem� is such a fixed combination antimalarial. The tablet contains artemether (20mg), a synthetic derivative of artemisinin, and lumefantrine (120mg), a highly lipophilic aryl amino alcohol. Lumefantrine has a much longer elimination half-life (several days) than artemether, and is associated with a low recruduscence rate, but has a slower onset of action. However, when used together, the complementary properties of artemether and lumefantrine result in a highly effective combination."

The form of malaria that Riamet combats, plasmodium falciparum, does not have the capacity to go into dormancy, so one course of Riamet is usually all you need to get better. There are two other forms of plasmodium, p. vivax and p. ovale, that are able to evade drug treatment by hiding in the liver. They can reactivate years after a malaria sufferer becomes symptom-free. The only drug regularly prescribed for the dormant form of malaria is primaquine.

If you check with the Bill and Melinda Gates Foundation, you will find that they are running African drug trials on primaquine. The World Health Organization is also considering wider distribution of this drug. The reason you don't hear more about it is that it can cause severe side effects in people with a genetic variation called G6PD deficiency, which is prevalent in Africa and the Middle East.

People with G6PD deficiency can still take primaquine, but in lower doses. The lowest dosage is frequently listed as 30mg "base" (that's two 15mg base tablets) per WEEK for 30 weeks.

I took it on a 15mg "base" per day, four-day-on, two-day-off pulse for three months, and probably could have stopped after two months. I took a G6PD deficiency test before starting this medication. The first two months, it caused intense side effects and a massive Lyme relapse. It should also be taken with lots of liver support, since dormant malaria hides in the liver and you are really going to stir things up.

It no longer has any effect, and I have not had babesia/malaria/whatever symptoms for three months. I also took three courses of chloroquine, spaced a MINIMUM of one week apart (it's very easy to overdose on chloroquine, since it stays in the body a long time and builds up). Children take a much lower dosage of chloroquine than adults.

Prior to taking this chloroquine/primaquine treatment, I had babesia/malaria/whatever for over five years. I took mepron and artemisinin for over a year. Artemisinin is a wonderful herb, but it really does not stay in your body long enough to cure you, no matter how high a dose you take.

And mepron was only a stopgap measure. It did suppress the babesia symptoms, but I relapsed every time I stopped taking it, despite taking two teaspoons twice a day and getting liver and kidney damage in the process. Each time I stopped mepron and then started again, it worked less well.

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NP40
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Art is normally given in 100mg doses three times per-day. However, this is normally given in conjunction with mepron or malarone.

I'd doubt seriously about trying 3200mg p-day. The herx's alone would knock you on your butt.
Do a Google search for Organic Pharmacy as their Art works well also.

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Dave6002
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Liz, thank you for sharing your experience on Babesia treatment, which is the most excited one I ever heard of.

You have cured your babesia by primaquine and Riamet�.

I'll collect more information about them.

Thanks again for providing your successful story on babesia treatment.


Dave.

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Dave6002
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Thanks Dana and Np,

I'll be very carefull about the dosing-up of Art.

Dave

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liz28
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Dave, thanks, it really is wonderful to read your increasingly enthusiastic and educated posts. Glad to see you are going to be getting out of here!

Just want to say, if you decided to explore either chloroquine or quinine, you shouldn't have to take as much primaquine. I took a lot more than was probably necessary because I heard about it first, then added in the chloroquine.

Also, chloroquine and plaquenil (i.e. hydroxychloroquine) are related, if you want to check it out in your research. Chloroquine is the much stronger version. That's probably one reason so many babesia sufferers feel better taking plaquenil, but rarely are cured by it.

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psano2
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Wanted to add to this post as I'm taking 1200mg twice a day. I've been on this for about 10 days so far w/o any problems.

My LLMD specified Zhang's artemesiae.

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CD57
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A thought -- maybe pulsing at high doses is better too? I didn't read the entire thread so sorry if there's a repeat in here.....just wanted to add that my LLMD pulses 1000 mg/artemesinin 4 days on, 3 days off...along with Mepron and Zith. 1000 mg seems a lot higher than most folks here have been doing. I don't know his success rate.

He recommends the Allergy Research Group artemesinin or Zhang's.

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Bugg
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Hey guys--

I took Mepron (2x a day), zith (2x a day) and Art two times a day. The half-life of Art is very short (2-5 hours). Mepron is anywhere from 2-4 days on average. Zith is about 68 hours. I, too have read a great deal about malaria and saw where they had the best eradication successes by combining a drug with a short life (art) with other combination therapies such as different anti-protozoals. In my personal regimen for babs, I would take my dosage at dinner and then 4 hours later (right before bed) take my next dose. Yes, this was very hardcore and did not allow my body to detoxify very well. I first started taking the Mepron and the zith. Then, in the next couple of weeks I added in the Art, 5 days on and 2 days off. The art definitely increased the herxes. If I tried to go 3x a day with the art (which my LLMD did NOT recommend) I was sweating like crazy and my heart would race. So, I reduced back to 2x a day. Anyway, I too, have wondered if higher doses of art might assist in babesial eradication. However, I'm pleased to report I've made MAJOR progress on just 4 months of 2x a day mep, 2x a day zith, and 2x a day art. (I'm on my way to see my LLMD to see what's next.) On the other side of the coin, I also remember reading that longer duration of combination therapies and perhaps switching combination therapies was what really eradicates chronic babesia. You guys may want to check out the Dec. 2007 Scientific Publication posted on chronic babs in this forum. It's by Peter Krause and it's entitled: Persistent and Relapsing Babesiosis in Immunocompromised Patients.

Hang in there!!

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adamm
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http://www.springerlink.com/content/18x05p746026470x/


Art. is NOT a benign substance;

it can damage neurons in the same way it damages the parasites.

Google toovey artemisinin neurotoxic to read more about this, and

DO NOT go up to that dose without a doctor's approval

(and then, if you get that, possibly seek a second opinion.) It is

not even known if Babs is curable, or, like Falciparum malaria,

it becomes sequestered in the tissue and thus impossible to

wipe out.


As for what that website said about taking 20 grams of the

stuff-- I would not believe that for a second. That much

of any drug is almost always bad news.

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doc
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this might be a stupid ? but has anyone ever used artemisia vulgaris (mugwort) or artmisia absinthium (wormwood) in there natural form ,(plant). I only ask because i have it in my store and its very inexpencive in this form. If so wondering what amount would u use?. going back to llmd next week and will ask him about it (2nd vist for wife, clinical dx lyme bab) just wondering as she is on 3 antibotics and worried ins co will not pay for long term treatment. just wondering ,but not going expeiment with them . just trying to get as much info as possible any 1 have any input thanks Doc (nickname)
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adamm
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No, but I've known some absinth-drinkers, and they

seemed pretty neurotox-ified at times [Wink]

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Looking
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Hi Doc:

Artemisia Annua, also known as Sweet Annie or Sweet Wormwood is the one to use for lyme or malaria.

Although it is in the same genus as both wormwood (absinthe, Artemisia absinthium) and mugwort (Artemisia vulgaris), each of these herbs has different uses and should not be confused. (A. absinthium & A. vulgaris are not the ones to use for lyme.)

Botanist Dr. James A. Duke reports that some research has shown that the whole herb is more active than artemisinin, that gelatin capsules of the herb are 3.5 times more effective than artemisinin for clearing parasitemia in mice.

"The whole-herb capsules are better than chloroquine for fever and malarial symptoms," he says. "When it comes to malaria, I personally believe that whole extracts of Artemisia annua, with all their synergens, could be better and cheaper than the isolated silver bullet, or derivatives thereof, at preventing as well as treating malaria. It could have fewer side effects and would be less likely to lead to multidrug resistance.

http://www.northeastherbal.org/article-artemisinin.asp

I am using Artemisia by Nutricology. Dosage and length of use determined by muscle testing.

Looking

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doc
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thanks much for the post and link, Doc
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Limping Lily
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i have used mugwort and wormwood together in a para-cleanse with a number of other herbs, and gotten a herx, so maybe it's the combo that does the job. right now, after doing several cleanses,i am feeling a little better than before,even though i still have fibro,edema,and mild joint pain which might be bart. i'm afraid to try stuff like levaquin, i hear such bad stories from people about that, but herbs do a lot of good for me. i'm still trying to find a combo that will relieve most of my sx (i can live with that.)for even a short time.

--------------------
~*~ Carole ~*~
 - Young at Heart Grandmother of 4

Posts: 140 | From Morristown, NJ, USA | Registered: Jan 2004  |  IP: Logged | Report this post to a Moderator
Hides1
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LIZ28- I too have gone through the gammet of Babs protocols including a long stint with Mepron. I still have the Babs on my IGM Test but now it is negative on Ignex FSH finally. SInce I still have the IGM of 320 my docs continues to do Malarone with me. He has brought up Riamet but we can't get it over here. Do you know of a reliable place to get Riamet? How did you get yours? Please PM me. Thanks
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psano2
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Adamm,

It would be interesting to know what kind of patients the study you posted were involved. Is it a coincidence that the neurologic symptoms they say is caused by artemesia are also the same as symptoms caused by Lyme dz and/or the coinfections?

I just started artemesia recently and I already had all of those symptoms before I started. In fact, those are the symptoms I'm hoping to get rid of.

If the patients they used in the study were Lyme patients, maybe what they were seeing were Lyme symptoms? At least that thought crossed my mind when I read the study.

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psano2
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I just saw my LLMD today and learned that I should be pulsing my artemesia. His nurse had called me with the initial order and hadn't told me that. So just to clarify, I'm to take 1200mg twice a day for 5 days on then 5 days off or 7 days on and 3 weeks off.
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adamm
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Specifically, they were problems with the cells of the brainstem,

and were observed in vitro.

A while back, I posted some research which you may be able to

find in a search. I'll track down some more stuff tomorrow and

put it up for you (or, if you don't want to wait, you

could google a fellow named toovey and the studies he's done)


I hope the art works for you--I know it's helped a lot of people.

It just has its risks, like every drug.

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adamm
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here's one:

http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6TCR-4K4DH5F-1&_user=443835&_rdoc=1&_fmt=&_orig=search&_sort=d&view=c&_acct=C000020958&_version=1&_urlVersion=0&_userid=44 3835&md5=2caadb1a5fb32fd74c9e788229fcee1c

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HaplyCarlessdave
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In my fight with babesia, I started out taking a couple grams
of raw artimesia anua every day or 400mg of artimisin,
and I also took copious amounts of garlic, as well as grapefruitseed
extract and olive leaf extract. My doc had me taking the
atovaquone, too, though (as well as 'biaxin' and doxy). I did
"ramp up" the artimesia at the beginning. I think I have read
that, malaria
does not seem to develop resistance to artimesia; thus nothing is
lost by "ramping up"; babesia is probably similar.

This combi, in these amounts, did the trick for me; was the
key to success. I had been fighting lyme-etcetera for a couple
years, but once I nailed the babesia, it was only a matter of
months before was off the drugs.
DaveS

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lymie tony z
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Although I have never come up positive for Babesia whenever tested....

I believe I have this disease...or at least one of the 13 species of this disease as noted symptomatically.

I started using zithromax, mepron and artimisinin about six or so months ago. I have

not kept up with it for this amount of time due to other symptoms needing different abx.

However, I am back to taking the above treatments for Babs.

I read lynn's post with some appreciation and some apprehension. These symptoms are the most

troublesome left that I present. I wish to rid myself of them of course. The only bummer is

that the three species of malaria she mentions are species of malaria, correct? I understand

the similarities of the babesial parasite but am not sure they would be exactly the same nor

would the remedy for malaria necessarily work against an unknown thus unnamed species of


babesia. There are, of course you know, 13 suspected species of babesia, of which only

three have been named. So, what if I have one of the, as yet, unamed species. Furthermore, if the

missdiagnosis of my condition, which prompted steroidal prescriptions early on and made my Bb

infection disseminate and then weaken my immune system. Who is to say, the same is not true, for

any of the species of Babesia I may have swimming around in my liver or other organs?

I will, none the less, give lynn's theoretical regimen some thought.

As far as Adams decisions to ramp up medications...I believe this to be a dangerous

move and one that I feel is an unnecessary risk. I believe that a decent dose over longer

periods of time are more appropriate then overdosing in an attempt to erradicate much of these diseases associated with TBD's.

Of course a doctor of some sort would be the most likely candidate to prescribe the amount of

any medication, due to perhaps the largeness or slightness of any patient.

zman

--------------------
I am not a doctor...opinions expressed are from personal experiences only and should never be viewed as coming from a healthcare provider. zman

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