Posted 3/10/2018 11:53 AM (GMT -7)
It's confusing to me too. I bought the 5-MTHF version, but it's only 300 mCg (not even MG).
My plan is to do testing in a week, and find what dosage works for me.
Horowitz suggests at least 30mg, but I find that a bit high to start of with.
This is from his book:
For my most resistant patients I now use several different combinations of intracellular drugs, including combinations of tetracyclines (minocycline and/or doxycycline), rifampin, macrolides (Zithromax or Biaxin), and Dapsone (two to three intracellular drugs, occasionally four), combined with Plaquenil and grapefruit seed extract (two cyst-busters), pulsed cell-wall drugs (Ceftin, Omnicef, penicillins or IV Rocephin), nystatin (for preventing yeast), biofilm busters (like Serrapeptase, Stevia, and monolaurin, which is a coconut oil extract), with extra folic acid to help prevent side effects of Dapsone. I use Leucovorin, a pharmaceutical folic acid, and a nutraceutical high-strength activated folic acid from Xymogen called 5-MTHF-ES (5-methyltetrahydrofolate extra-strength) or Folify-ER. A total of at least 30 mg of folic acid a day must be used (sometimes higher, i.e., 45 to 60 mg/day) to minimize the anemia associated with Dapsone. Average decreases in hemoglobin of about 2 to 3 grams can be expected with Dapsone using the above doses of folic acid, which stabilizes over time. Deplin (L-methyl folate) can also be included in the protocol.
Although Dapsone can be effective, it is not a benign drug without side effects, and the risks/benefits must be discussed with the patient. There are four main potential side effects—Herxheimer reactions, Anemia, Rashes and Methemoglobinemia—that can be remembered with the acronym, Do No “HARM.”
Herxheimer (JH) reactions are seen in the majority of patients using Dapsone, and they can be severe, in which case the dose will need to be temporarily decreased or held for several days, especially if the JH reactions persist despite using LDN, high-dose glutathione with NAC, alpha-lipoic acid, alkalizing the body and drainage remedies. Some patients take months to get to the full Dapsone dose secondary to severe JH reactions, but they still improve significantly over time. Although the full dose (100 mg per day) was the most effective dose in our studies to date, severe Herxheimer reactions with other intracellular medications may require starting at a low initial dose (25 mg every other day), and slowly increasing the dose (i.e., 25 mg/day for one to two weeks, then 50 mg alternating with 25 mg for one to two weeks, then 50 mg/day for one to two weeks (the minimum effective dose), until slowly getting to the full dose.
Another side effect is anemia, secondary to Dapsone interfering with folic acid synthesis. This will cause the size of red blood cells to increase, causing a macrocytic (large cell) anemia, which is the most common form of anemia seen with the drug. Rarely, Dapsone can cause a hemolytic anemia (where the red blood cells burst). You will need to initially have blood drawn every two to three weeks on the protocol (CBC, CMP, occasionally checking a Coombs direct antibody for hemolytic anemia) and consider getting checked for G6PD (glucose 6 phosphate dehydrogenase) deficiency, which can be an overlapping cause of hemolytic anemia. Certain antibiotic/antimalarial medications as well as ingestion of fava beans can cause anemia in people who are G6PD-deficient. Even though hemolytic anemia is possible with Dapsone, we have not witnessed it in over four hundred patients on the protocol. Once patients stop Dapsone, the anemia usually reverses and goes back to baseline levels within a month, as long as folic acid supplementation continues and there are no overlapping causes of anemia.
I also suggest treating iron deficiency anemia before starting Dapsone, and following iron levels (iron, TIBC [total iron binding capacity], and ferritin) in women of childbearing age, since heavy menstrual periods and iron loss will worsen anemia. Any woman prone to heavy menses must be on iron and contact her healthcare provider if there is any heavy bleeding, which may require stopping Dapsone, increasing folic acid, and increasing iron intake. Since Dapsone will cause on the average a 2 to 3 gram drop in hemoglobin (rarely more), women should aim to have an initial starting hemoglobin of at least 13 grams/dL, so as to not drop below 10 grams/dL. Despite the anemia, many women report that their energy level is significantly better!
Another side effect of Dapsone is rashes. It is a sulfa drug, and may cause a rash in those who are sulfa sensitive, although we have seen patients who can’t tolerate Bactrim, another sulfa drug, who can take Dapsone without any side effects. If you are sulfa sensitive, and the risk/benefit ratio requires doing a trial of Dapsone due to having failed multiple other antibiotic protocols, discuss with your healthcare provider using an H1 blocker (Zyrtec and/or Benadryl) with an H2 blocker (Zantac) prior to starting treatment, which may keep down side effects of rashes and itching. If, however, there is a history of severe sulfa allergies, it may be best to avoid the drug.
The last, significant side effect of Dapsone is methemoglobinemia. This is where the hemoglobin in our red blood cells, which carries oxygen, is exposed to increased oxidative stress and oxidizes the iron molecules so that they can’t effectively release oxygen to the tissues. This can rarely cause a “blue man/woman syndrome” where the lips and extremities turn blue due to low oxygen levels (hypoxia), with shortness of breath. This will usually not happen with methemoglobin levels below 10 percent, although levels between 5 and 10 percent can occasionally cause symptoms of fatigue, dizziness and shortness of breath. Levels below 5 percent are usually asymptomatic. Methemoglobinemia can resolve rapidly within twenty-four hours of stopping the drug and increasing folic acid with antioxidants. A pulse oximetry checking oxygen levels is a good screening test, and methemoglobin levels should be checked periodically during treatment. I therefore recommend high-dose antioxidants (like resveratrol, and/or curcumin), with liposomal glutathione, NAC and alpha-lipoic acid, since glutathione has been shown to be an alternative pathway to reverse methemoglobin. In severe cases, supplemental oxygen with a methylene blue 1 percent solution (10 mg/ml, at 1 to 2 mg/kg intravenously slowly over five minutes) can be used to quickly reverse methemoglobinemia. Tagamet (yes, the H2 blocker) can also be used to treat elevated methemoglobin levels. We have fortunately only seen high methemoglobin levels in a handful of patients (especially if they were using oxidant therapies on their own, such as ozone), and stopping Dapsone and reintroducing it at lower levels when the methemoglobin returns to normal, while avoiding pro-oxidant therapies with more glutathione support, has generally prevented a recurrence.
Despite the potential side effects, we have found Dapsone to be safe and effective. We don’t yet know if 50 mg versus 100 mg of Dapsone per day is superior when used in long-term combination therapy (higher doses of Dapsone usually have greater efficacy in our clinical studies), or the length of time of treatment required to effect a “cure” (if it is possible), or which combination of meds will produce the best long-term results. We are also not sure about the success rate once the drug is stopped at twelve months (which is the time frame of our ongoing study). This is the same length of time required to treat other persister bacteria like leprosy with rifampin and Dapsone. Why did we choose twelve months? We tried stopping Dapsone at two months, but symptoms relapsed. We tried again at four and six months, but the same thing happened, although symptoms were clearly better than when they started, with some patients getting neurological improvements not seen with other drugs. One woman could text and use her thumbs, which had been almost paralyzed from Lyme and Bartonella; another had been sick for twelve years, and her brain fog, joint, and muscle pain improved as she went from 20 percent to 80 percent of normal within a few months. One man with severe neuropsychiatric symptoms (psychosis) who failed all antibiotics and antipsychotic medications after taking Dapsone at 25 mg QOD for two weeks, woke up and started speaking normally after a severe Herxheimer reaction. Unfortunately, the beneficial effect didn’t last when the drug was stopped, and we are re-evaluating using Dapsone at higher doses with more detox support. Clearly, mycobacterium “persister” drugs like Dapsone are acting differently than other intracellular antibiotics I have used.
We have had some patients relapse at six months using lower dosages, and others who took it for seven months with other intracellular drugs who remained symptom-free. Some patients had greater clinical improvements with the Dapsone protocol than with any other drug regimen, but had PCR evidence of Lyme and Bartonella midway during therapy. We are therefore evaluating different dosages, combinations, and lengths of therapy. The combinations that seem to be the most effective usually involve taking Dapsone with a tetracycline and macrolide (Zithromax or Biaxin) or a tetracycline with rifampin, but there are some severely ill patients who failed multiple protocols who are on four-drug intracellular regimens (pulsing rifampin and Zithromax, with regular use of minocycline or doxycycline with Dapsone) who are doing extremely well. All of these patients were on Plaquenil and grapefruit seed extract (GSE) for cyst forms, pulsed cell-wall drugs (Ceftin or Omnicef) three days a week (Monday, Wednesday, Saturday) with nystatin BID (for yeast), and biofilm busters (Serrapeptase, Stevia, and/or Lauricidin).
By following this protocol, many of my sickest patients, as well as my Herx kings and queens, have started to improve. We have enrolled over four hundred patients on the Horowitz Dapsone protocol, and the vast majority are improving. Patients who have been sick for many years (five to forty) have reported that this was the best regimen they had ever taken. If you have failed classical protocols and you are disabled from tick-borne disorders, with chronic fatigue, pain, neuropathy, and memory/concentration problems, as well as sweats and chills (chronic babesiosis), then have an informed conversation with your healthcare provider. If you follow the above recommendations, Dapsone may help you.