introduction
Artemesia annua and it's derivatives
Whole herbs often have supporting chemicals in them that extractions don't. The U.S. strains of artemesia annua don't have nearly as high an artemesinin content as the Chinese. Not all Chinese A.a. have the same content either, but A.a. is being cultivated in China and possibly New Zealand/Austrailia for artemisinin content. Some strains are currently being bred for artemesinin content. Some stuff is grown organically- some is rumored to be grown with DDT, although the plant is very unlikely to have many insect problems... However, customs may irradate the stuff as it comes into the U.S.
Some of the extracts are sort of condensed "mini drugs". They are not synthesised but condensed and consistant; artemisuin is an example and available in the USA.
Large corporations are attempting synthesis of artemesinin because it is more profitable. There is no evidence that synthetic is more effective or less toxic- in fact the reverse may be true. The plain herb is used effectively as well in rural China for malaria, probably in combination with other herbs.
This is mostly cut and paste with links.
Beware, an allergy to artemisunin is not common but can affect the heart in a very scay way. I always start new things with a very small dose. Lucky I did- I had strong heart palpitations at 14mg artemesunin. I'm allergic to it. Too bad, it's an effective drug.
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START NOTES
MISC;
Artemether, Artesunin, Artemesinin are derivatives or extractions of Artemesia annua. They are stronger than the raw herb.
"Cure" rates do not always include later remissions.
Used to treat Babesia and Malaria, has shown effectiveness with Giardia and Cryptosporidium (sp?). Anti-protazoal, antibacterial, and supposedly anti-yeast.
Has shown some effectiveness with Leptospirosis (? 2 mentions- no details). May have some effectiveness with other spirochetes. Works with babesia by "exploding" oxygen molecules in the presence of malaria (& babesia- lives in RBC) & red blood cell iron molecules. See notes below- I don't completely understand this... Would it do the same with Lyme ????? with cyst forms ???? Would the whole herb do it?
Artemesia Annua (quing hao, ching hao, jing hao, quinghaosu (extract-artemisinin)) is different from other members of the Artemesia family as it seems to have nuero-toxins at extremely low levels. This is controversial. Artesunate- a semisynthetic, and Artemether- a product extracted with a methyl-ether compound, seem to have higher toxicity levels which possibly have been falsely attributed to Artemesinin In addition- some studies seem to have confused Artemesia families. In addition- there seems to be confusion some studies over the names of some of the compounds. Some studies show no toxicity with Artemesinin Artemesinin and Arteannuin are the primary active anti-malarials in Artemesinin annua. Other Artemesias don't have it, in addition some other Artemisias such as european wormwood- Artemesia abysinthia (abysinthe) are known to contain high levels of nuerotoxins.
People say they do herx with it. Some may be allergic to it as well. ***Heart may be effected with allergic or severe reactions. What effect when bbb is compromised?
there are 2 different treatment philosophies- treat high dose short term- & smaller dose long term. (Zhang actually uses 33mg arteannuin 3xday 4 months within a 500mg total herbal combo. It is possible part of that combo is dried powdered artemesia annua)
***VERY interesting study compares with abx &
differing compounds on bacteria, protozoa and fungus-
http://academic.iisc.ernet.in/~cursci/MAR25E1.html
"Inhibitory activities of artemesinin and its precursors were found
to be in the following order: artemesinin> arteannuin B > artemisinic
acid. " According to this study artemesinin is more efective than
arteannuin.
Artemesinin, extracts and semisynthetics are used both orally and parentally in Africa and Asia for malaria. It is not approved for this use in the US or Canada- but is legally obtainable at least for oral use. There are ancedotal reports from US citizens of successful Artemether txs for Babesia as well.
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http://www.naccca.org/news/200108/malaria.html
"Artemesinin acts like a bomb. It has two oxygen atoms that break apart in the presence of iron. The malaria parasite inhabits a person's red blood cells, which are rich in iron. When an artemisinin molecule encounters the parasite, it explodes, releasing lethal toxins that destroy the parasite. [*questionable how this would work with Lyme- works in red blood cells]"
http://www.itmonline.org/arts/chinghao.htm
Ching-hao is included in effective treatments for leptospirosis, a bacterial
disease that usually infects humans from animal waste contaminating water
supplies. [*leptospirosis is a spirochete, like Lyme]
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ANTI-MALARIAL PROPERTIES/ARTEMESIA FAMILY
""The confirmed structure, is reported only to have been isolated from Artemesia annua L. (Sweet wormwood) but not from Artemesia absinthium (wormwood)[...]The antimalarial activity of artemesinin, the chemistry of the compound, the pharmacology, the clinical applications and even the analysis have been well documented.3,16-26 Chinese researchers have reported, without giving specific details, that 30 other species of Artemesia extracts have been examined but that none of these extracts exhibited an antimalarial activity. Researchers in America also extracted A. dracunculus, A. pontica, A. abuscula and A. ludoviciana and none of these show the presence of artemesinin, nor an antimalarial activity.3,16-26 [*controversy on A. ludovinciana mexicana]""
http://www.nimh.btinternet.co.uk/ejhm/1_3_mm3.htm
"The antimalarial activity of qinghao was rediscovered in the Peoples Republic of China in 1971. During the 1970s an active crystalline compound named qinghaosu, arteannuin (literally, the active principle of qinghao or artemesinin) was isolated, characterized, and found to have an antimalarial activity. The Western name artemisinine was given to the compound and Chemical Abstract preferred artemisinin.6 This compound has been shown to have marked activity against malaria parasites, including chemo-resistant isolates of Plasmodium falciparum.7-1 3Artemesinin is not an alkaloid or an amine as the name suggests. This compound is a sesquiterpene lactone peroxide. The endoperoxide linkage is really unusual for an antimalarial compound. Structure activity studies carried out indicated that the presence of the peroxide bridge correlates with, and is essential for, the antimalarial activity.2,3,5,7,8,15,16,26
The confirmed structure, is reported only to have been isolated from Artemesia annua L. (Sweet wormwood) but not from Artemesia absinthium (wormwood).7,9 "
........http://www.itmonline.org/arts/chinghao.htm
"The primary fragrant component of Artemesia annua is the monoterpene artemesia ketone (see Figure 2), accompanied mainly by other monoterpenes (see Table 1). To retain these compounds in a decoction, it is recommended that the herb be decocted for no longer than 5 minutes [**powder or artemesinin may be more effective than tea??- these compounds not nessasarily anti-malarial, but may very well be supportive of those that are.]
...
The compound (see Figure 3) was later named artemesinin (alternatively: arteannuin). It is found in the leaves, making up a maximum of about 0.5-0.6% and is highest when the plant is in flower, which is the time traditionally recommended for collection of the herb. However, the amount in different plant samples varies markedly, with some specimens of Artemesia annua having little or no detectable amounts. For example, plants collected in the U.S. typically have very low levels (29). Most of the artemesinin is localized in the upper leaves (see Table 2). [**Chinese strains]Table 2. Artemesinin levels in different parts of the plant (29).
Plant Part Artemesinin as
% of total in plant [NOT % of plant- but % of total found]
Upper third 41.7
Middle third 25.0
Lower third 22.2
Side shoots 11.1
Stem, roots, and seeds 0.0 "
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ON-LINE RESOURCES/ORDERING
shipping charges not included
Artemesia Annua powder;4 oz; $12.25, 8 oz; $23.00, 1 lb; $37.75
http://herbalwise.com/bulklist.htm
[no indication of country grown in, or artemesinin content]
http://www.blessedherbs.com/printbulkbot.html
WILDCRAFTED in US_ NOT RECOMMENDED- may be poor artemesinin content;
Artemesia annua USA 1/4 LB; 6.00, 1 - 4 lbs; 11.50 per lb.
http://www.hepalin.com/products.htm
(Artemesinin 100MG) contains 60 capsules in a bottle $50
***BEST BET so far;
http://www.myvitanet.com/ar100mg60cap.html
Pure unadulterated Artemesinin powder. Artemesinin 100MG, 60 capsules
$39 - on sale; $30 May be less now- prices falling.
Zhang's http://www.dr-zhang.com/LD/LD2.htm
http://www.dr-zhang.com/LD/formulas/Artemesia.htm
to order;
Wellcare Pharmaceutical Co. (???)
http://www.yanjingsupply.com/bulkherbs/bulkherbsqt.htm
Good source of raw artemesia annua from China. Website may not be finished-
however, you can call and order from them by phone. US office.
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DOSAGES
there seem to be 2 philosophies of treatment- one- high dose- short term,
the other low dose long term. & also in combo with other herbs and
western drugs.
http://www.itmonline.org/arts/chinghao.htm
"Adult dosing at 500 mg/day (first day: 500 mg is given twice for a loading dose) for 5-7 days was tried (15). Parasite clearance usually occurred in the first two days. However, the disease returned with high frequency. In early Chinese clinical studies of artemesinin for malaria, the dosage given was 800-1,600 mg/day for three days, so the dose used in this study was probably too low to assure full clearance of the parasites.It has been suggested that high dose artemesinin (20 mg/kg body weight; typically more than 1 gram per day) for 2 days be followed up with quinine (30 mg/kg body weight) for 3 days to lower the recurrence rate, which appeared successful in one study (17). In another evaluation, artesunate was administered in cases of uncomplicated malaria using a dosage range from 400-800 mg by oral administration of tablets (14). As little as 400 mg in three days was sufficient to clear parasites and remove symptoms; parasite clearance took place in the first 16 hours. However, 39% of cases treated that way had recurrence within one month; at the highest dosage of 800 mg for 7 days, the recurrence rate was dropped by a factor of 10 to 3.9%. Therefore, high dose treatments, as well as a sufficient course of therapy, may be essential to avoiding recurrence as well as avoiding development of resistant strains (33). By combining artesunate with mefloquine, the recurrence rate can decline to 2% (18), though this level of effect has been claimed for high dose artesunate alone (31). Artesunate is available in injection form and in suppository for rectal administration in patients with advanced disease. One of the proposed uses of it is for treatment of severely debilitated patients in remote areas as an initial therapy before they can be treated by the modern drugs.
HERBAL TEA- Although ching-hao as a crude herb is not as often used today for treating malaria (being replaced by various preparations of the active components), there is information about the method for using it. The dosage of ching-hao recommended to treat malaria is 20-40 grams of the dried herb per day in decoction. In one trial, three days dosing at 24-29 grams per day was successful in curing malaria (recurrence rate not given). Based on a content of 0.5% artemesinin in the herb, these amounts provided about 120-145 mg of the compound, much less than used in the recent trials of the isolated compound or its synthetic derivatives. There may be a group of active compounds in the herb, leading to successful treatment in the dosage range cited; however, recurrence rates may be high.
There is no data on the safety of such prophylactic therapy over an extended period of use (e.g., several months). With its pro-oxidant effects, the high doses of ching-hao used in malarial treatments can only be recommended for about 3-6 months, a typical duration for administering ching-hao to treat lupus and other diseases
). Ching-hao is included in effective treatments for leptospirosis, a bacterial disease that usually infects humans from animal waste contaminating water supplies."
.....
Zhang's http://www.dr-zhang.com/LD/LD2.htm
Zhang's dosage (**33mg arteannuin** in a 500mg herbal combo 3x 4 months)
Zhang- 500mg, 3xday;
"D. Clinical Applications:
1) Malaria
Clinically, while used for treating malaria, a 100% cure rate was achieved in 485 cases of tertian malaria and 105 cases of subtertian malaria. These two groups were all treated with the tablet made from the dilute alcohol extract of the herb at a total dose of 72 or 86.4 grams of crude herb in divided doses spread over 3 days. In comparison with chloroquine, the herbal preparations and arteannuin had fast-acting antipyretic and anti-plamodial actions. It can also be used for treating systematic lupus erythematosus. [30]
2) Babesiosis,
In my clinical application, usually one treatment course is 40 days. Most patient will see their Babesiosis title turns to negative after one course treatment. Very few people need a second course.
3) SLE and lupus erythematosus discoides
Almost every case experienced remission in different degrees. At beginning of the treatment, the symptoms may worsen temporary. [31]
E. Package:
Each Capsule contains 500mg (contains 33mg arteannuin) of the extract of Artemisiae annua L. Herba, Astragalus membranaceus and Codonopsis pilosula.
Dose: take one capsule, three times a day."
.........
CRUDE HERB EXTRACT;
Zhang quotes study;
"D. Clinical Applications:
Clinically, while used for treating malaria, a 100% cure rate was achieved in 485 cases of tertian malaria and 105 cases of subtertian malaria. These two groups were all treated with the tablet made from the dilute alcohol extract of the herb at a total dose of 72 or 86.4 grams of crude herb in divided doses spread over 3 days. In comparison with chloroquine, the herbal preparations and arteannuin had fast-acting antipyretic and anti-plamodial actions. It can also be used for treating systematic lupus erythematosus. It has been used for:
1) Malaria
2) Babesiosis
3) SLE (systematic lupus erythematosus) "
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OTHER PARASITES AND INFECTIONS
"In addition to antimalarial effects, artemesinin was found to have promise in treating the parasitic diseases schistosomiasis and clonorchiasis (common in China and Africa, affecting over 200 million people each year) caused by trematodes (blood flukes). Artemether is now being used for prophylaxis against schistosomiasis; in combination therapy with praziquantel it is used to treat the disease (22). Ching-hao is included in effective treatments for *****leptospirosis******[SPIROCHETE], a bacterial disease that usually infects humans from animal waste contaminating water supplies."
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SIDE EFFECTS AND TOXICITY
"Side effects of ching-hao at normal to high therapeutic doses appear to be rare and mostly involve gastro-intestinal reactions such as nausea, vomiting, and diarrhea (with or without intestinal cramping). In a large study in Thailand comparing high-dose artemesinin derivatives (artemether and artesunate) alone versus in combination with mefloquine, the incidence of adverse effects with the artemesinin compounds was reported to be 34% for loss of appetite, 16% for nausea, 15% for dizziness, and 11% for vomiting; mefloquine greatly increased the incidence of side effects, doubling the rate (20). In a clinical trial comparing artesunate injection with chloroquine and with the combination of quinine and resorcin, no adverse effects of artesunate were reported, while dizziness was a common complaint with the drug therapies (35).
Animal studies with high-dose administration of artemesinin had revealed neurological damage, which was initially worrisome, but this appears to be highly species specific [***other species of artemesia ie- abysinthia, etc...] and does not affect humans in the dosage range normally used (21). Very high doses of the isolated artemesinin caused liver inflammation in animals and in humans; the human dosage causing this reaction was 10 times the therapeutic dose, given for 3 days (34). Published reports thus far agree that ching-hao, artemesinin, and its derivatives have low toxicity."
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http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9790421&dopt=Abstract
"Assessment of the neurotoxicity of parenteral artemesinin derivatives in mice."
WARNING- This study uses NOT artemesinin, but Artesunate; a semi-synthetic, and artemether; a compound processed with methyl-ether- a potentially damaging process.
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(????)
http://homepages.uel.ac.uk/4474p/qingh.htm
... Artemesinin potentiates [makes stronger] the effects of mefloquine,
primaquine and tetracycline. (Hien and White. 1993)
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OTHER SPECIES, Artemesia ludoviciana mexicana, reported to have anti-malarial
properties. Does not contain artemesinin No report of toxicity levels
(????). (Artemesia ludoviciana mexicana common name "big sage brush"
grows in US and Mexico. A US study disproved this, but people say they
used the wrong plant. Not A.L.mexicana)
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&dB=PubMed&list_uids=9419840&dopt=Abstract
Antimalaric effect of an alcoholic extract of Artemesia ludoviciana mexicana in a rodent malaria model. Malagon F, Vazquez J, Delgado G, Ruiz A.
Departamento de Microbiologia y Parasitologia, Facultad de Medicina,
UNAM, D.F., Mexico.
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http://www.geocities.com/nutriflip/Naturopathy/SweetAnnie.html
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http://www.hc-sc.gc.ca/hpb/lcdc/publicat/ccdr/00vol26/26s2/26s2j_e.html
c. Artemesinin Derivatives (Qinghaosu) for the Treatment of Drug-Resistant Malaria
"Artemesinin (qinghaosu) is a naturally occurring sesquiterpene lactone peroxide structurally unrelated to any known antimalarial. Qinghaosu, derived from cultivated Artemesia annua, is available as the parent compound artemesinin (oral, parenteral, and suppository formulations) and as three semi-synthetic derivatives: a water-soluble hemisuccinate salt (artesunate) for parenteral or oral administration; and two oil-soluble compounds (artemether and arteether) for intramuscular injection. All are metabolized to a biologically active metabolite, dihydroartemisinin. Artesunate is a prodrug for dihydroartemisinin and as such is the most rapidly active of the derivatives examined to date. All compounds have their antiparasitic effects on the younger ring-form parasites, thereby decreasing the numbers of late parasite forms that can obstruct the host’s microvasculature.
All artemesinin preparations have been studied and used only for treatment. They are recommended for treatment use only and not for prophylaxis. All compounds are at least as efficacious as quinine in the treatment of severe and complicated malaria. [*cerebral Qinghaosu and its derivatives lead to faster parasite (mean: 32% faster) and fever (mean: 17% faster) clearance times than do any other anti-malarials. In spite of the more rapid antiparasitic action of qinghaosu compounds, these agents have not been shown to decrease mortality compared with quinine.
Artemisinin-related compounds act rapidly against drug-resistant P. falciparum strains but have high recrudescence rates (about 10% to 50%) when used as monotherapy for less than 5 days. Recent studies have examined longer durations of therapy (7 days) and combinations of qinghaosu derivatives and mefloquine in order to prevent recrudescence. In vitro synergy has been demonstrated between artemesinin derivatives, mefloquine, and tetracycline. In Thailand, treatment with oral artesunate (over 3 to 5 days) combined with mefloquine (15 to 25 mg/kg) was more effective than mefloquine or artesunate alone. Combination therapy results in > 90% cure rates of primary and recrudescent P. falciparum infections.
Artemesinin derivatives have been used by over 1 million patients and are well tolerated. To date, there have been two human cases of complete heart block associated with their use, but most volunteer and clinical studies have found no evidence of cardiac or other toxicity. Neurologic lesions involving the brainstem have been seen in rats, dogs, and primates given repeated doses of artemesinin derivatives. [*See study above] To date, no clinical neurologic events have been observed in humans; however, studies addressing cumulative toxicity in humans have not been performed. The safety of qinghaosu derivatives in pregnancy has not been established. Because of their short half-life artemesinin and its derivatives should not be used for prophylaxis.
Artemesinin and its derivatives are now available and increasingly used in Southeast Asia and Africa; none is licensed in Canada. Combinations of artesunate and mefloquine appear to be the most active drug regimens for treatment of multidrug-resistant falciparum malaria in Southeast Asia. The quality of artemesinin derivatives available in developing countries is questionable, as they may not be produced in accordance with the good manufacturing production standards required in North America. Although there is good evidence that therapy with artemesinin compounds is safe, questions about cumulative neurologic toxicity require resolution."
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