Author Ken Singleton, M.D.
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IV, or Intra-muscular?
Depending on the severity of a person’s symptoms, the method of administration of antibiotic drugs may vary. There are three basic methods of administration: orally (PO) in the form of pills or capsules, intravenously (IV) in which antibiotics are injected into the veins, and intramuscularly (IM) in which antibiotics are injected into the muscles. In some cases, a combination of these methods may also be necessary.
Types of Antibiotic Drugs for Treating Lyme Disease
I want to discuss the specific principles of antibiotic use for Lyme disease. There are five classes of antibiotics that we commonly use for Lyme disease.
The most commonly used antibiotics in this class are doxycycline and minocycline. To be effective, tetracyclines must be administered in dosages sufficient to produce high blood levels. To achieve this, high oral daily dosages may be required, and these dosages may need to be monitored by blood levels. If these dosages are not tolerated due to side effects, the drug may need to be administered intravenously. One of the advantages of tetracyclines is that they are able to penetrate the cell walls, making them a good choice when Bb and other bacteria have migrated inside the cells. The usual oral dosage of oral doxycycline is 100–300 mg twice a day with food (not with dairy products or mineral supplements). The dosage for minocycline is 100 mg twice a day. (One could use higher doses, but those doses tend to cause much more side effects.) Doxycycline can also be administered intravenously. The usual dosage for IV doxycycline is 300–400 mg once a day.
Precautions: Like all antibiotic drugs (as well as drugs in general), tetracyclines can cause adverse side effects and should not be used by pregnant and breastfeeding women. They are also not recommended for children aged eight and under because they can interfere with the growth and proper development of bones and cartilage and may also discolor teeth. Other side effects that need to be monitored include nausea (they should be taken with non-dairy food for this reason), yeast infections, gastrointestinal problems, rash (usually mild), and dizziness (especially minocycline). In some instances, tetracyclines can also cause eye, kidney, and liver problems. During the course of treatment, people using tetracyclines (especially doxycycline) should avoid exposure to sunlight, as the drugs can significantly increase the risk of “sun sensitivity.” This reaction can occur even through glass car windows and on overcast days and is not effectively prevented by sunblock. Additionally, antacids, dairy products, and iron supplements should also be avoided at the same time as tetracyclines (take an hour or more away from these substances), as these all interfere with tetracyclines’ ability to be absorbed. Finally, the medications in the tetracycline family (especially minocycline) may rarely cause a condition called “pseudotumor cerebri,” which is a serious complication for which the medication needs to be discontinued. The most common symptom of this condition is a severe and unrelenting headache after taking a dose of the medication. If this symptom occurs, I recommend notifying your Lyme-aware doctor promptly so that the proper evaluation may be done.
Antibiotic drugs in this class include oral amoxicillin and intramuscular (IM) benzathine penicillin (Bicillin LA). To be effective against Lyme, high blood and tissue levels of penicillins need to be sustained for 72 hours or more. Since blood levels of penicillins can significantly vary from patient to patient, the blood levels of amoxicillin are often measured during the course of treatment. The dose of amoxicillin commonly used for Lyme is 1,000–2,000 mg every eight hours, and it is at times combined with probenecid 500 mg, which helps to keep blood levels high. Amoxicillin combined with clavulanic acid (Augmentin) is also very effective.
Oral penicillin (such as Pen VK) is not effective. However, intramuscular penicillin, administered at a dose of 1,200,000 units two to three times a week, is highly useful. Although more painful when administered, the LA form of Bicillin is more effective than the CR form (which contains a local anesthetic.) As previously mentioned, the penicillin group should always be combined with other antibiotic classes that target the L-form (e.g., azithromycin) of Lyme and ideally the cystic form (e.g., metronidazole) of Lyme also.
Precautions: Penicillins are relatively safe. They should never be used if allergy to them is known or strongly suspected. Common side effects include fever, joint swelling, nausea, rash, and yeast overgrowth. Penicillins can also sometimes interfere with the body’s production of white blood cells known as neutrophils. In rare cases, they can also be fatal if administered to people who are allergic to them.
These medications are related to the penicillin group. Drugs in this class that are most commonly used to treat Lyme include two oral preparations and two intravenous drugs. Of the oral choices, cefuroxime (Ceftin) was the first drug approved by the Food and Drug Administration (FDA) for the treatment of early-stage Lyme disease. It is given orally at a dose of 500 mg twice a day while some patients may require higher doses. The other oral cephalosporin preparation is cefdinir (Omnicef ). It is very effective and can be taken as 600 mg once a day. Two other drugs in this class, ceftriaxone (Rocephin) and cefotaxime (Claforan) are usually administered intravenously. (Other IV medicines are also used, but these two are by far the most common ones used.) The dosages for the IV preparations are 1–2 grams every eight hours in the case of cefotaxime and 2 grams once per day in the case of ceftriaxone. (Some experts prefer to use this medication twice a day, four days on and three days off, per week.) These latter two drugs are later generations of this drug class and, overall, are more effective for treating Lyme disease. During treatment, high blood levels need to be achieved. Ideally, blood levels should be measured on a regular basis throughout the course of treatment. Finally, as with the penicillins, the medications in this class should ideally be combined with the oral antibiotic classes that target the L-form of Lyme and, ideally, the cystic form also.
Precautions: Cephalosporin drugs can cause liver toxicity and may lower the white blood count, especially the cell called neutrophil. For these reasons, routine and regular testing of blood should be done to detect any adverse reactions. Ceftriaxone can also cause gallstones, which can be prevented by using the medication, ursodiol. Other possible side effects of drugs in this class include diarrhea, rash, and yeast overgrowth, which at times can be serious. Additionally, some people who are allergic to penicillins are also allergic to cephalosporins, and therefore, great caution must be used in treating a patient who is allergic to penicillin with medications in this class.
Macrolides and Ketolides
Drugs in this class include azithromycin (Zithromax), clarithormycin (Biaxin), and the ketolide, telithromycin (Ketek). All these medicines are related to erythromycin, but erythromycin itself is not an effective treatment for Lyme disease and should not be used to treat LD. Like the tetracycline drugs, macrolides and ketolides are able to penetrate cell walls and tissues. Clarithormycin is given orally at a dose of 1,000 mg per day and is very effective for treating Lyme. But it is often difficult to tolerate due to its metallic aftertaste and the various gastrointestinal problems it can cause. Azithromycin is not as effective for Lyme as clarithromycin, but is better tolerated. The dose range for oral azithromycin is 250–600 mg daily. Azithromycin produces better results when given intravenously compared to oral administration. The IV dose of azithromycin is 500 mg per day.
Some experts feel that the drug of choice in this category is telithromycin, which is both better tolerated and more effective. The usual dose of telithromycin is 800 mg per day. This drug was engineered to prevent drug resistance, a phenomenon that occurs when bacteria, after prolonged drug exposure, mutate into forms that are resistant to drug therapy. However, if telithromycin is to be used, the patient’s electrocardiogram and liver function status need to be carefully evaluated, since this medication, in my experience, may have a greater chance of causing side effects involving the heart and liver than the macrolides. For this reason I rarely, if ever, use telithromycin.
Precautions: Macrolide drugs can cause cramping, diarrhea, and other gastrointestinal problems, as well as nausea, rashes, and vomiting. In some cases, they can also cause temporary hearing and vision problems (ringing in the ears, hearing loss, and blurry or double vision). They can also lead to unhealthy elevations of liver enzymes, which can be an early sign of liver damage. They may also cause reduction in white blood cell counts. Blood tests throughout the course of treatment with macrolides are necessary to monitor liver function and white blood cell (WBC) count. As mentioned, the macrolides can sometimes affect the electrical activity of the heart (called the Q-T interval), and this may need to be assessed prior to using these medications for an extended time. Additionally, macrolides can also interfere with a variety of other drugs by inhibiting the liver breakdown of other medicines. Therefore, be sure to mention to your doctor and your pharmacist any other medications you may be on prior to beginning macrolide treatment.
This antibiotic drug is increasingly being used to treat Lyme disease. Originally developed to treat harmful, single-cell bacteria and parasites, metronidazole (Flagyl) has since been shown to be useful in killing off Bb bacteria in their cystic form. This ability to destroy Lyme cystic form is something that the other classes of antibiotic drugs cannot do. For that reason, most Lyme-aware physicians utilize metronidazole in combination with one or more of the above classes of drugs for cases of chronic Lyme where there is a high likelihood of the presence of cystic forms. The dosage is 250–500 mg two to three times a day. (Tetracyclines, such as doxycycline, are not used with metronidazole because they can inhibit the latter’s effectiveness.) Precautions: Common, relatively minor, side effects of metronidazole include yeast overgrowth, headache, nausea, metallic taste, and rash. More serious side effects include nerve damage that can result in numbness and tingling of the extremities and, in rare cases, seizures. Metronidazole use should be immediately discontinued if these symptoms appear. It should also not be used for anyone on blood-thinning medications, such as coumadin, since metronidazole can increase the blood-thinning effects of these drugs, potentially leading to an increased risk of internal bleeding. Pregnant women should also avoid this medication. The drug should never be used with alcohol or alcohol-containing products (even cough syrups), since this combination can cause severe headache, nausea, skin flushing, vomiting, and other symptoms. (This effect is similar to the anti-alcoholism medication called Antabuse.)
In summary, there are several excellent Lyme disease antibiotic choices from which your Lyme-aware doctor has to choose. Each patient’s individual Lyme situation needs to be assessed to determine the precise antibiotic protocol that would be most effective. Because this type of antibiotic decision-making can be so complex, it is beyond the scope of this book to attempt to present all the possible scenarios in detail. It is advisable for a physician who is interested in becoming more Lyme-aware to visit the Web site of the International Lyme and Associated Diseases Society (www.ilads.org) for more information. On this site, one can also find excellent specific treatment guidelines for Lyme and the other TBDs by Dr. Joseph Burrascano, who truly is a pioneer in the field of Lyme medicine.
If you would like
to learn more about the book before ordering it, feel free to browse
these excerpts, which are available online, free of charge:
of Contents • Introduction
and Diagnosis • Natural
Killer (NK) Cells
Diet • Medical
History and Physical Exam
Dose Naltrexone (LDN) • Food,
Diet, and Omega Fatty Acids
and Positive Outlook • Index
"What I have accomplished with this 500+ page book, The Lyme Disease Solution, is to share my everyday knowledge and practical experience of 10 years as a Lyme-enlightened practitioner (who also is himself a Lyme-survivor). Although I hesitate to use the “cure” word in relation to chronic Lyme, the principles in this book have resulted in a greater than 90% response rate in my patients. At least 60% of my patients achieve long-term improvement that allows them to get off of antibiotics completely."
— Ken Singleton, M.D.
THE LYME DISEASE SOLUTION
By Ken Singleton, M.D.
Foreword by James A. Duke, Ph.D.
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