Artemisinin - to pulse or not to pulse for babesia?

[sianrecovery]

Hi Guys

My LLMD has suggested 100mg x 2 daily dose of artemisinin, taken as a steady dose, over the long term. I am treating for babesia microti and duncani. I am already on mepron 1500 mg daily, and 500mg azith. I have read so many conflicting ideas on the best form and method for dosing artemisinin...any one have any suggestions?

Thanks in advance for your responses.

 

[heapsreal]

Its all confusing?????
I've been reading that some drs say not to use a bacteriostatic abx like doxy with a bactericidal abx like amoxicillin or bicillin etc.
Last night read that shouldn't take doxy with flagyl as it renders flagyl useless? I'm not sure thats right as i have had some brutal die off from flagyl and been on doxycycline .

Have u tried bactrim or plaquinil for babs?

 

[sianrecovery]

Yeah, clear as mud eh? And some people say only use artensuate, or liposomal arteminisin...

Bactrim I am allergic too - properly, severe reaction - plaquenil I took for four days a few years back, and then ended up with a frozen shoulder which took months to remit. I can only call this an associative relationship, but it still leaves me reluctant to try it again.

 

[heapsreal]

I do Ok on bactrim for sinusitis which im guessing maybe babesia. Started bicillin with first shot a few days ago. Sinuses are clearing up but getting die off symptoms . I dont know what that really means. Sinuses may not be babesia ? ?

Clear as mud for sure.

 

[Mesurfer]

I can't instruct on dosing but be careful with artemisinin. Maybe start slow. That really threw me for a loop when i took it a bunch of years back. It made me feel like I was dying so I had to come off it.

 

[sianrecovery]

I did a nasal swab a few months back and found a real variety of abs resistant bacterial, and some fungi. The resistant bugs synchronised with the antibiotics I've had the most. Sinus stuff is difficult eh, both structurally and in terms of biofilm. I think I've resigned myself to control rather than eradication. The BEGi spray helped for a while.

 

[aquariusgirl]

Omg where can I find doctors who will treat like this?

 

[sianrecovery]

I think there's a few around - kind of standard Burrascano (cuse spelling) stuff really. Think a lot more LLMD's are aware of problems with mold and sinuses etc now.

 

[Dufresne]

The LLMD's don't seem to be in agreement on how artemisinin should be taken. There is a study showing it's only a fifth as effective on day five as it was on day one. So the three days on, four days off pulsing fits this reasoning. However I've read the enzyme that deactivates the artemisinin can be offset with grapefruit juice. That might be the way to go if you end up taking it longer.

 

[heapsreal]

Omg where can I find doctors who will treat like this?

Lots of research and the deep dark internet.

 

[sianrecovery]

I read a Dr Marty Ross saying that Dufrene....he said three days on, high dose, eleven days off. My Lyme prac is more conservative, 'steady state' dosing. Any idea of where I might find that paper? Haven't turned it up yet. Just opinion. Schaller is dead against Arteminisinin full stop - his editorials always come up first in my searches...

 

[Dufresne]

http://www.ncbi.nlm.nih.gov/pubmed/18064444

Artemisinin and CYP2A6 activity in healthy subjects.
Asimus S1, Hai TN, Van Huong N, Ashton M.
Author information
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.

 

[sianrecovery]

Help out a brain fogged lyme...what is this really saying?

 

[Dufresne]

Help out a brain fogged lyme...what is this really saying?

I hear ya. It's pretty much Greek to me too. My take is that within a few days of taking artemisinin your body releases various P-450 enzymes that metabolize it.

These are the lines that jump out at me:

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.

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.

Here's another bit you can pick through.

Artemisinin and derivatives
Artemisinin and its derivatives are drugs used to fight malaria infection [Articles:19851082, 19926036]. Recombinant CYP2A6 metabolizes artemisinin and CYP2A6 inhibition attenuates the rate of drug disappearance in human microsomes in vitro [Article:10583023]. However, CYP2B6 and CYP3A4 enzymes are thought to have a greater role in artemisinin metabolism [Article:10583023] (see the PharmGKB Artemisinin and Derivatives Pathway, Pharmacokinetics). Artemisinin derivatives (arteether, artemether, artesunate) were developed to enhance drug bioavailability, and are used in combination with a second unrelated slower acting drug, in order to initially rapidly eradicate malaria parasites within red blood cells, and then kill any residual parasites [Articles:19851082, 19926036]. CYP2A6 is the major CYP450 enzyme involved in artesunate metabolism, forming dihydro-artemisinin, which is then inactivated by UGT enzymes (see the PharmGKB Artemisinin and Derivatives Pathway, Pharmacokinetics) [Articles:12920490, 19926036]. Therefore, CYP2A6 alleles which confer loss-of-function or decreased function may affect metabolism of these anti-malarial drugs. However, studies investigating urinary metabolites after dosing with artemisinin or derivatives, and use concurrent coumarin or nicotine probe drugs, see no clear correlation between CYP2A6 genotype and an effect on PK or enzyme activity [Articles:18064444, 18979093]. Artemisinin and derivatives induce CYP2B6 expression [Article:18350255; 12844133], further complicating CYP2A6 association studies. Studies controlling for CYP2B6 status and with larger numbers are therefore required to investigate the clinical implications of CYP2A6 genotype on the metabolism of artemisinin and its derivatives.