Saturday, March 25, 2006

Minocycline for short-term neuroprotection.

Elewa HF, Hilali H, Hess DC, Machado LS, Fagan SC.1

Program in Clinical and Experimental Therapeutics, College of Pharmacy, University of Georgia, Athens, Georgia; Specialty Care Service Line, Veterans Administration Medical Center, Augusta, Georgia.

April 2006

Minocycline is a widely used tetracycline antibiotic. For decades, it has been used to treat various gram-positive and gram-negative infections. Minocycline was recently shown to have neuroprotective properties in animal models of acute neurologic injury. As a neuroprotective agent, the drug appears more effective than other treatment options. In addition to its high penetration of the blood-brain barrier, minocycline is a safe compound commonly used to treat chronic infections. Its several mechanisms of action in neuroprotection-antiinflammatory and antiapoptotic effects, and protease inhibition-make it a desirable candidate as therapy for acute neurologic injury, such as ischemic stroke. Minocycline is ready for clinical trials of acute neurologic injury.



Related Article:

The potential of minocycline for neuroprotection in human neurologic disease.

The potential of minocycline for neuroprotection in human neurologic disease.Zemke D, Majid A.Department of Neurology and Ophthalmology, Michigan State University, East Lansing, Michigan 48824, USA.

Minocycline is a member of the tetracycline class of molecules with broad-spectrum antibiotic activity. The unique properties of minocycline result in increased tissue distribution when compared with the other tetracyclines. Of particular interest is the ability of minocycline to diffuse into the central nervous system at clinically effective levels. Aside from its antimicrobial properties, minocycline has been found to have beneficial effects on inflammation, microglial activation, matrix metalloproteinases, nitric oxide production, and apoptotic cell death. Concordantly, minocycline has been found to have neuroprotective effects in animal models of a number of diseases including stroke, multiple sclerosis, and Parkinson disease. The proven safety of minocycline over decades of use as an antibiotic suggests that it may have potential for development into an effective treatment of multiple neurologic conditions in humans.

Publication Types:


PMID: 15613934 [PubMed - indexed for MEDLINE]




Take minocycline tablets or capsules by mouth. Follow the directions on the prescription label. Swallow tablets or capsules whole with a full glass of water; take tablets or capsules in an upright or sitting position. Taking a sip of water first, before taking the tablets or capsules, may help you swallow them. If possible take bedtime doses at least 10 minutes before lying down. It is best to take minocycline without food, but if it upsets your stomach take it with food. Take your doses at regular intervals. Do not take your medicine more often than directed. Finish the full course prescribed by your prescriber or health care professional even if you think your condition is better. Do not stop taking except on your prescriber's advice.
Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.


Side effects that you should report to your prescriber or health care professional as soon as possible: dark yellow or brown urine; difficulty breathing; fever; headache; increased sensitivity to the sun or ultraviolet light; itching in the rectal or genital area; pain on swallowing; redness, blistering, peeling or loosening of the skin, including inside the mouth; stomach pain or cramps; skin rash or itching; unusual bleeding or bruising; unusual tiredness or weakness; yellowing of eyes or skin.

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome): diarrhea; discolored tongue or teeth; drowsiness, dizziness; loss of appetite; nausea, vomiting; sore mouth.


Tell your prescriber or health care professional if your symptoms do not improve in 3 to 5 days. Sometimes it will take longer than this before you get better.

Do not take minocycline just before going to bed. It may not dissolve properly when you are lying down and can cause ulceration of your food pipe.

Keep out of the sun, or wear protective clothing outdoors and use a sunscreen. Do not use sun lamps or sun tanning beds or booths.

Birth control pills (contraceptive pills) may not work properly while you are taking this medicine. Use an extra method of birth control for at least one month.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how minocycline affects you. To reduce the risk of dizzy or fainting spells, do not sit or stand up quickly, especially if you are an older patient.

If you are being treated for a sexually transmitted disease, avoid sexual contact until you have finished your treatment. Your sexual partner may also need treatment.

If you are going to have surgery, tell your prescriber or health care professional that you are taking minocycline.

Antacid can stop minocycline working. If you get an upset stomach and want to take an antacid, make sure there is an interval of at least 2 hours since you last took minocycline, or 4 hours before your next dose.

Never take minocycline if it is past the expiration date; it can make you seriously ill.


Antacids; calcium salts; cholestyramine; colestipol; digoxin; female hormones, including contraceptive or birth control pills; ferrous sulfate; magnesium salts; other antibiotics; phenytoin; sodium bicarbonate; warfarin.

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.


Prescriber needs to know if you have any of these conditions: kidney disease; liver disease; long exposure to sunlight (working outdoors); an unusual or allergic reaction to minocycline, other tetracyclines; pregnant or trying to get pregnant; breast-feeding.


f you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses. There should be an interval of at least 4 to 6 hours between doses.


Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15-30 degrees C (59-86 degrees F). Protect from light and moisture. Throw away any unused medicine after the expiration date.