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Lariam

Mefloquine is an orally administered antimalarial drug used as a prophylaxis against and treatment for malaria. It also goes by the trade name LariamTM (manufactured by Roche Pharmaceuticals) and chemical name mefloquine hydrochloride (forumulated with HCl). Mefloquine was developed in the 1970s at the Walter Reed Army Institute of Research in the U.S. as a chemical synthetic similar to quinine. more...

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Side-effects

Like many other drugs, mefloquine has adverse side-effects. It is known to cause severe depression, anxiety, paranoia, nightmares, insomnia, vestibular (balance) damage and central nervous system problems. For a complete list of adverse physical and psychological effects — including suicidal ideation — see the most recent product information. In 2002 the word "suicide" was added to the official product label, though proof of causation has not been established. Since 2003, the FDA has required that patients be screened before mefloquine is prescribed. Anyone taking antidepressants or with a history of psychiatric illness should not take mefloquine. The latest Consumer Medication Guide to Lariam has more complete information.

In the 1990s there were reports in the media that the drug may have played a role in the Somalia Affair, the misbehaviour of Canadian peacekeeping troops on duty in Somalia. There has been similar controversy since three murder-suicides involving Special Forces soldiers at Fort Bragg, N.C., in the summer of 2002. To date more than 19 cases of vestibular damage following the use of mefloquine have been diagnosed by military physicians. The same damage has been diagnosed among business travelers and tourists.

Neurological activity

In 2004, researchers found that mefloquine in adult mice blocks connexins called Cx36 and Cx50. Cx36 is found in the brain and Cx50 is located in the eye lens. Connexins in the brain are believed to play a role in movement, vision and memory.

Chirality and its implications

Mefloquine is a chiral molecule. It contains two asymmetric carbons, which means there are a total of four different enantiomers of the molecule. Mefloquine is currently manufactured and sold as a racemate of the (+/-) R*,S* enantiomers by Hoffman-LaRoche, a Swiss pharmaceutical company. According to some research, the (+) enantiomer is more effective in treating malaria, and the (-) enantiomer specifically binds to adenosine receptors in the central nervous system, which may explain some of its psychotropic effects. Some believe that it is irresponsible for a pharmaceutical company to sell mefloquine as a racemic mixture. It is not known whether mefloquine goes through stereoisomeric switching in vivo.

Advice to travelers

Mefloquine is one of the antimalarial drugs which the August 2005 issue of the CDC Travel Health Yellow Sheet advises travelers in areas with malaria risk — Africa, South America, the Indian subcontinent, Asia, and the South Pacific — to take.

There are virulent strains of malaria that are resistant to one or more anti-malarial drugs; for example, there are mefloquine-resistant strains in Thailand. Travelers are advised to compare current recommendations before selecting an antimalarial drug as the occurrence of drug-resistant strains changes.

Read more at Wikipedia.org


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The malaria medication controversy
From International Travel News, 2/1/05 by Alan M. Spira

Is its prevention worse than the disease?

This theme has run wild lately with regard to malaria, and it is time to set the record straight. Let's look at the facts and calm the excitement with some common sense.

To understand why we need protection against malaria, let's understand what we are fighting. Malaria is a potentially fatal disease spread by mosquito bites. It's found through much of the world but primarily in the tropics. It infects 300 million to 550 million people (yes, that is one-third to one-half billion people, about seven times the number of those suffering from AIDS) and kills between one and three million annually.

There are four species of this parasite which affect mankind. The most dangerous is called Falciparum, but the most common form is called Vivax, which can hibernate for months to years in the liver.

Travelers visiting areas where malaria exists can avoid this disease with just two tools: personal protective measures against mosquito bites and appropriate malaria preventive medication, officially known as "chemoprophylaxis."

The medication is taken to avoid dying from malaria and to reduce serious infection; no medication confers 100% protection against infection. Because of the life cycle of the parasite, any antimalarial medication must be taken for a set period of time after leaving the risk area.

In the United States, we have four medications available to us for prevention (it is a different story for the treatment of malaria as a disease): chloroquine, mefloquine, doxycycline and atovaquone-proguanil. Let's dissect each of these in turn and learn about them.

Chloroquine (Aralen[R]) has been around for over half a century and was once the standard drug for preventing malaria. Unfortunately, it now only works in a few regions of the world such as Central America and parts of the Middle East.

It is taken weekly, beginning two weeks before arrival in the malarious area and continued throughout the trip until four weeks after having left the risk area. It is generally safe and can be used in pregnancy but can be fatal in overdosages, particularly with children.

Mefloquine (Lariam[R]) has also been around for decades and is a highly effective antimalarial, but resistance to this drug is now recognized, particularly in Southeast Asia.

It is the most convenient of the four, being taken only once a week, starting two weeks before arrival in the malarious area and continued throughout the trip until four weeks after having left the risk area.

This medication has an unfortunately bad reputation because of its potential side effects. Approximately one in 200 users develop sleep disturbances or emotional instability. It is forbidden in those who have a seizure disorder or psychiatric problems.

Doxycycline (Vibramycin[R]) is an antibiotic, often used by dermatologists for acne control. It is a very good medication to prevent malaria and can be started fight at the beginning of the trip instead of two weeks in advance. It must be taken daily throughout the exposure period and continued for four additional weeks after leaving the risk area.

The potential problems with this medication are the risk of yeast infection in women, ulcers and photo-toxicity from sun exposure, plus it cannot be taken by pregnant women nor children.

Atovaquone-Proguanil (Malarone[R]) is the newest antimalarial but is actually two old drugs which when combined is very effective.

Like doxycycline it is taken daily, but instead of having to continue for four weeks after leaving the risk area you merely take it for one week after. The shorter course leads to a higher likelihood that a traveler will actually take the medication correctly and fully. It is very safe and very gentle and has become the medication of choice in my full-time travel and tropical medicine clinic, especially for short-term travel.

In other parts of the world, such as Great Britain, a drug called Paludrine (proguanil + chloroquine) is used, but, while very safe, it is not very effective and they have a higher death rate from malaria because of this.

Amazingly, travelers have been told by other travelers on the road not to take malaria medication and have been infected or have died as a result. This is not worth it!

There is a place for each of these, but thought and time is necessary to figure out which is best for you when you travel. Please consult with a specialist in travel or tropical medicine before your journey.

Healthy Travels!

Dr. Spira is medical director of the Travel Medicine Center (131 N. Robertson Blvd., Beverly Hils, CA 90211; visit www.healthytravel.com) and you may reach him at travelmed@ earthlink.net.

Next month in this column--a few words on Economy Class Syndrome from Dr. Larry G. Baratta.

COPYRIGHT 2005 Martin Publications, Inc.
COPYRIGHT 2005 Gale Group

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