This is topic Pulsing Artemisinin? in forum Medical Questions at LymeNet Flash.


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Posted by JT's Mom (Member # 24553) on :
 
My son's LLMD has him pulsing Artemisinin. I just read in another post that this is not a good idea.

Why is pulsing for Babesia a bad idea?? Resistance?

We've only done 2 cycles so far... 10 days on, then 10 days off. Perhaps I should hold off on any more cycles. We meet with a new LLMD in February.
 
Posted by ang (Member # 29459) on :
 
My LLMD has me pulse 10 days on and 20 days off of Artemsia.
 
Posted by DeniseNM (Member # 11182) on :
 
My LLMDs have me pulsing 4 days on, 3 off.
 
Posted by jkmom (Member # 14004) on :
 
My LLMD said to pulse 4 days on, 3 days off. Supposedly, artemsia loses its effectiveness over time. Pulsing it keeps it working.

I do not pulse my abx for babs.
 
Posted by TF (Member # 14183) on :
 
My lyme doc had me pulse art 3 days on and 4 days off each week. It worked for me. It is now almost 6 years since I completed my lyme treatment.

This topic has been discussed before. There have been studies that determined the art must be pulsed.

Here are excerpts from previous posts explaining why it must be pulsed:

Per Dr. K.: Artemisinin provokes the intestinal wall to secrete an enzyme which destroys the medication before it can be absorbed. This process builds up over 3 weeks. After a one week pause the enzyme has disappeared and takes another 3 weeks to reemerge. Grapefruit juice prevents formation of this enzyme.


Eur J Clin Pharmacol. 2008 Mar;64(3):283-92. Epub 2007 Dec 7.
Artemisinin and CYP2A6 activity in healthy subjects.

Asimus S, Hai TN, Van Huong N, Ashton M.

Unit for Pharmacokinetics and Drug Metabolism, Department of Pharmacology, Sahlgrenska Academy at G�teborg University, P.O. Box 431, 405 30, G�teborg, Sweden.
Abstract

OBJECTIVE: To investigate whether the antimalarial drug artemisinin affects CYP2A6 activity in healthy subjects and to compare the utility of coumarin and nicotine as in vivo probe compounds for CYP2A6. METHODS: Twelve healthy male Vietnamese subjects were given coumarin or nicotine in randomized sequence before and after 5 days of a repeated oral administration of artemisinin during two different treatment periods 1 month apart. Sequential blood samples were drawn at baseline 7 days prior to artemisinin treatment and on the first and fifth day of artemisinin treatment during both treatment periods. Plasma concentrations of 7-hydroxycoumarin glucuronide (7-OHCG), nicotine, cotinine and artemisinin were analysed by high-performance liquid chromatography and those of coumarin and 7-hydroxycoumarin (7-OHC) were determined by liquid chromatography-tandem mass spectrometry. Urine, collected in two time intervals on the days of coumarin intake, was treated with beta-glucuronidase and analysed for 7-OHC levels.

RESULTS: Artemisinin AUC(0-infinity) values decreased significantly to 23% [95% confidence interval (CI) 18%-28%] on the fifth day of artemisinin administration as compared with the first. The sum of renally excreted 7-OHC and 7-OHCG increased by 1.55-fold (adjusted 95% CI 1.08-2.23) in the 3- to 8-h interval compared to baseline 7 days before. The 7-OHCG/7-OHC plasma AUC(0-infinity) ratio increased by 1.72-fold (adjusted 95% CI 1.16-2.54) following 5 days of artemisinin intake. There was no significant change in the cotinine/nicotine AUC(0-11 hr) ratio between study days.

CONCLUSION: Artemisinin significantly increased the sum of renally excreted 7-OHC and 7-OHCG in one of the two collection intervals, suggesting an induction of CYP2A6. A significant increase in the 7-OHCG to 7-OHC AUC(0-infinity) ratio indicates artemisinin to be an inducer of glucuronidation.

PMID: 18064444

The poster of this article writes:

Artemisinin induces enzymes which accelerate its clearance, as you can see you would need to take a five times larger dose on the fifth day to achieve the same concentration as the first day. Impractical and probably unhealthy.

Hence, pulsing.

So, to summarize, the intestines will stop absorbing artemesinin if you take it continuously. So, you have to take breaks from it.
 
Posted by ktkdommer (Member # 29020) on :
 
The 3 of us take artemesia for 10 days a month. This month will be our first time taking the full dose of 3 pills per day. Merry Christmas to us!
 


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