Metronidazole
Mobile spirochetes:
"For both microaerobic and aerobic incubation the normal mobile spirochetes were resistant to this antibiotic with an MBC > or = 512 microg/ml."
Cystic forms:
"When they were incubated under microaerobic conditions, the biologically active cystic forms had an MBC > or = 4 microg/ml, but the MBC was > or = 32 microg/ml with aerobic incubation at 37 degrees C."
Hydroxychloroquine
Mobile spirochetes:
"The minimal bactericidal concentration (MBC) of HCQ against the mobile spirochetes was > 32 microg/ml at 37 degrees C, and > 128 microg/ml at 30 degrees C"
Cystic forms:
"When incubated at 37 degrees C, the MBC for young biologically active cysts (1-day old) was > 8 microg/ml, but it was > 32 microg/ml for old cysts (1-week old)."
Tinidazole
Mobile spirochetes:
"The minimal bactericidal concentration (MBC) of TZ against the mobile spirochetes was >128 microg/ml at 37 degrees C in micro-oxic atmosphere when incubated for 14 days."
Cystic forms:
"The MBC for older (10-months-old) cysts at 37 degrees C in a micro-oxic atmosphere was >0.5 microg/ml, but >0.125 microg/ml for young (1-day-old) cysts."
* Note that these are all in vitro studies; it is uncertain what the activity of these drugs in vivo is.
* There is the hypothesis that hydroxychloroquine can also increase the clinical activity of macrolide antibiotics in the treatment of Lyme disease. [2]
Metronidazole versus tinidazole
The studies of Brorson & Brorson show in vitro a higher activity of tinidazole over metronidazole against the cystic forms. Furthermore tinidazole has less side effects, and has a few other advantages [1]:
From the full text:
"In 1999, we published a study on the treatment of cystic forms of B. burgdorferi with metronidazole (MZ) However, this drug may not be tolerated by all patients. Therefore, the second generation 5-nitroimidazole tinidazole, which is better tolerated by most patients and may also be more efficient than MZ was tested."
"When the cysts were incubated with a high concentration of TZ (32 μg/ml), no blebs originated. In contrast, incubation with MZ produced a few blebs. Therefore, TZ may have more adverse effects on the DNA in the blebs than MZ. As the content of the blebs is of great pathogenic importance, TZ may be better suited for the treatment of Lyme disease."
"In addition, tinidazole is also an effective eradicator of Clostridium difficile and may prevent yeast infection, which may be troublesome during long-term treatment of Lyme disease. Another advantage of TZ compared to MZ is its higher accumulation in the cerebrospinal fluid.,,
Citrosept oraz inne ziola
Grapefruit seed extract
In vitro evaluation showed that grapefruit seed extract (GSE) can be a powerful agent against spirochetes and the cysts of Borrelia afzelii ACA-1 when applied in the range of concentration between 0.165% and 0.00032%. Susceptibility testing of mobile spirochetes exposed to GSE for 1 h revealed lack of motile bacteria at concentrations of 0.041%, and at concentration of 0.165%, they either completely dissolved or displayed a degenerated shape. When the mobile spirochetes were exposed to GSE for 1 week, the estimated minimal inhibitory concentration (MIC) value was ⩽0.00032%, and the minimal bactericidal concentration (MBC) value was 0.0052%. Moreover, visible breaking of cysts incubated for 1 h with GSE in a concentration range from 0.165% to 0.021% was noticed, and rupturing of cysts was observed after treatment with GSE diluted from 0.01% to 0.00064% with efficacy from 90% to 5%. The MBC value was established to be 0.0013%. Interestingly, the authors observed the abnormal protrusion of membranes and their eventual disruption with the contents leaking at lower applied concentrations of GSE, while the highest GSE concentrations made the bacteria and cysts disappear completely. The MBC was strongly dependent on the length of the incubation, but even short incubation with GSE showed to be very effective against active and latent rounded forms of Borrelia afzelii [Brorson and Brorson, 2007]. Effect of GSE on biofilm was not performed in the study. However, we noticed that GSE was ineffective at the MIC and MBC concentrations that were used in testing against spirochetes for 1 week, and with 30–40% efficacy at the highest MBC concentrations tested against spirochetes and cysts for 1 h [Goc et al. unpublished]. The study corroborates with results of Heggers et al., who demonstrated that mechanism of GSE’s antibacterial activity manifests by disruption of the bacterial membrane and liberating the cytoplasmic contents within 15 min after its application [Heggers et al. 2002]. However, it has also been shown that GSE is an efflux inhibitor; thus, the anti-borreliae activity of this agent can express itself using this mechanism as well [Abulrob et al. 2004; Fraser et al. 1997]. Interestingly, GSE showed to be effective against many pathogenic strains but not against intestinal microflora [Ionescu et al.1990; Reagor et al. 2002]. One study indicated that antimicrobial activity of GSE can be attributed to just the synthetic preservative agents contained within [Von Woedtke et al. 1999]. Also contradictory studies are published in regard to its cytotoxicity. One study showed GSE to be gastro-protective and anti-inflammatory [Zayachkivska et al. 2005]. Another study reported about cytotoxicity of GSE on fibroblasts and severely damaging inflammatory effect to the connective tissue just after 24 h of incubation, leading to greater toxicity at higher GSE concentrations [Guedes et al. 2013],,
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4971593/
References
1: Brorson O, Brorson SH.
An in vitro study of the susceptibility of mobile and cystic forms of Borrelia
burgdorferi to tinidazole.
Int Microbiol. 2004 Jun;7(2):139-42.
PMID: 15248163 [PubMed - indexed for MEDLINE]
Full text: http://www.im.microbios.org/26june04/09%20Brorson.pdf
2: Donta ST.
Macrolide therapy of chronic Lyme Disease.
Med Sci Monit. 2003 Nov;9(11):PI136-42.
PMID: 14586290 [PubMed - indexed for MEDLINE]
Full text: http://www.medscimonit.com/pub/vol_9/no_11/3706.pdf
3: Brorson O, Brorson SH.
An in vitro study of the susceptibility of mobile and cystic forms of Borrelia
burgdorferi to hydroxychloroquine.
Int Microbiol. 2002 Mar;5(1):25-31.
PMID: 12102233 [PubMed - indexed for MEDLINE]
Full text: http://www.im.microbios.org/articles020 ... rorson.pdf
4: Brorson O, Brorson SH.
Susceptibility of motile and cystic forms of Borrelia burgdorferi to ranitidine
bismuth citrate.
Int Microbiol. 2001 Dec;4(4):209-15.
PMID: 12051564 [PubMed - indexed for MEDLINE]
Full text: http://www.im.microbios.org/16december0 ... rorson.pdf
5: Brorson O, Brorson SH.
An in vitro study of the susceptibility of mobile and cystic forms of Borrelia
burgdorferi to metronidazole.
APMIS. 1999 Jun;107(6):566-76.
PMID: 10379684 [PubMed - indexed for MEDLINE]
6: Brorson O, Brorson SH.
Grapefruit seed extract is a powerful in vitro agent against motile and cystic forms of Borrelia burgdorferi sensu lato.
Infection. 2007 Jun;35(3):206-8. No abstract available.
PMID: 17565468 [PubMed - in process]
https://www.ncbi.nlm.nih.gov/pubmed/17565468
Grapefruit Seed Extract is a Powerful in vitro Agent Against Motile and Cystic Forms of Borrelia burgdorferi sensu lato.
MEDLINE ABSTRACT NOT AVAILABLE - FREE ARTICLE PREVIEW BELOW
Lyme borreliosis [1], caused by Borrelia burgdorferi sensulato, may lead to long-term tissue infection, which may be difficult to cure. The outcome of Lyme borreliosis is highly dependent on the antibiotic treatment [2]. The observation of the ability of B. burgdorferi sensu lato to convert (and reconvert) to cystic forms [3–5] may explain why the infection sometimes is persistent and reactivating. Therefore, it might be important to eradicate all germative forms (not only the motile form) of the bacterium to obtain a proper treatment for Lyme borreliosis. Grapefruit-seed extract (GSE) contains bioactive flavenoids (e.g., hesperitin, resveratrol, and naringenin) and has been shown to possess anti-microbiological effect against bacteria and fungus [6, 7]. Many studies indicate that GSE is a substance whose therapeutic effect ranks equal to or better than other known anti-bacterial agents. Positive effects of GSE are decreased levels of TNF-α, Nuclear factor Kb, NO, protection of the gastrointestinal tract against mechanical stress, and has anti-allergic and other antioxidative properties [8, 9]. Naringenin, hesperidin and other citrus flavones have been found in plasma and tissue after ingestion [10]. Lactobacillus and bifidobacteria in the gut seems to be insignificantly affected by GSE [6], and no severe side effects have been observed. B. burgdorferi sensu lato has a gene for efflux mechanism which may be responsible for antibiotic resistance [11]. GSE is an efflux inhibitor, which can be used to enhance the activity of antibacterial agents [12]. For the reasons mentioned above it is reasonable to test the hypothesis that motile and cystic forms of B. burgdorferi sensu lato will be susceptible to GSE, and this is the aimof our study
http://www.greenmedinfo.com/article/grapefruit-seed-extract-powerful-vitro-agent-against-motile-and-cystic-forms-borelia
http://www.mdjunction.com/forums/lyme-disease-support-forums/studies-research/368910-grapefruit-seed-extract-naturally-kill-lyme-cysts
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Citrosept jest środkiem w 100% naturalnym i nie jest niebezpieczny dla zdrowia, mimo to ostrożność przy jego stosowaniu powinny zachować poniżej wymienione osoby:
- uczulone na cytrusy - powinny zacząć stosować ekstrakt w bardzo małych dawkach porcjach np. 1 kropla na szklankę płynu dziennie. Jeżeli nie wystąpi reakcja alergiczna należy przyjmować taką porcję przez ok. 5 dni i stopniowo zwiększać ją o 1 kroplę dziennie, aż do porcji jaką chce się uzyskać.
- przyjmujące leki nasercowe lub na nadciśnienie - przyjmowanie tych leków nie wyklucza stosowania Citroseptu. Jednak należy zachować przynajmniej 2 godziny odstępu pomiędzy przyjmowaniem leków i Citroseptu. Ekstrakt z grejpfruta (także owoc grejpfruta i sok grejpfrutowy) wpływa na wchłanianie i metabolizm niektórych leków, nie powinien więc być z nimi stosowany bez modyfikacji ich dawki przez leczącego nas lekarza. Spożycie leku jednocześnie z Citroseptem (lub z sokiem grejpfrutowym) może spowodować, że precyzyjnie dobrana przez lekarza dawka leku zostanie przekroczona. Może to spowodować zaburzenia rytmu serca, skoki ciśnienia krwi czy inne dolegliwości ze strony układu krążenia. Odstęp 2 godzin pomiędzy przyjmowaniem leków i Citroseptu zmniejsza ryzyko takich powikłań, ale prosimy o obserwację swego organizmu, zwłaszcza na początku przyjmowania ekstraktu. W razie wątpliwości polecamy konsultację u swego lekarza.
- przyjmujące leki zapobiegające odrzutom przeszczepów - w takich przypadkach w ogóle odradzamy stosowanie ekstraktu.
- przyjmujące leki w związku z chorobami wątroby - dotyczy to m.in. leków stosowanych przy wirusowych zapaleniach wątroby. Proponujemy w tym przypadku konsultację z lekarzem - wprawdzie badania potwierdziły hepatoprotekcyjne (działające ochronnie na wątrobę) właściwości ekstraktu, jednak jego działanie może nałożyć się na działanie leków. Poza tym wiele leków jest metabolizowanych w wątrobie, a przy zaburzeniu jej funkcji zmienia się tempo przemian, co może prowadzić do zmian stężenia substancji aktywnych w organizmie i nieprzewidzianych skutków.
- kobiety w ciąży - nie przeprowadzano badań nad wpływem ekstraktu na płód, więc mimo tego, że nie wydaje się aby ekstrakt powodował zagrożenie, polecamy zastosowanie zasady „masz wątpliwości - nie bierz". Wiele kobiet przyjmuje ekstrakt w ciąży, jednak z pewnością nie powinny zaczynać jego stosowania od dużych porcji (czytaj: REAKCJA HERXHEIMERA).
- chore na cukrzycę - poziom cukru we krwi może ulec nieznacznemu obniżeniu.
http://citrosept.pl/ostroznosc-w-stosowaniu/
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