Find information on thousands of medical conditions and prescription drugs.

Mefloquine

Mefloquine is an orally administered antimalarial drug used as a prophylaxis against and treatment for malaria. It also goes by the trade name Lariam^TM (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...

Home

Marinol

Marplan

Matulane

Maxair

Maxalt

Maxolon

MDMA

Medrol

Mobic

Modicon

Motrin

Mucinex

Muse

Mykacet

Mykinac

Myleran

Mylotarg

Mysoline

Phentermine

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

• [List your site here Free!]

Change of dosing regimen for malaria prophylaxis with mefloquine - drug to prevent Plasmodium falciparum malaria
From Morbidity and Mortality Weekly Report, 2/1/91

Change of Dosing Regimen for Malaria Prophylaxis with Mefloquine

CDC recommends mefloquine (Lariam[R!) alone as the drug of choice for malaria prevention for travelers to areas with drug-resistant Plasmodium falciparum malaria [1-4!. (*1) Based on accumulating experience with this drug, the prophylactic dosing regimen has been revised to a single dose of mefloquine to be taken every week [3!. The first dose should be taken 1 week before travel. It should be continued weekly during the entire period of travel in malarious areas and for 4 week after departure from such areas.

The previous dosing regimen (in which one dose was taken each week for 4 weeks, followed by one dose every other week) compromises the effectiveness of mefloquine. Malaria prophylaxis with this dosing regimen among Peace Corps volunteers in West Africa was less effective than expected [5!. The relatively low effectiveness was due to the every-other-week dosing regimen because all mefloquine prophylaxis failures occurred during the second week of the alternate-week dosing regimen in volunteers who had used mefloquine 2 months. Mean mefloquine blood concentrations were substantially lower during the second week of the every-2-weeks dosing regimen than during the first week, suggesting that during the second week blood levels are too low to suppress parasitemia [5!.

All studies confirm that mefloquine is well tolerated when used for prophylaxis. No serious adverse reactions to mefloquine prophylaxis (i.e., psychoses and convulsions) have been observed among Peace Corps volunteers or among 18,462 persons enrolled in prophylactic drug trials and surveys of travelers who were taking mefloquine weekly [5!. However, serious adverse reactions have been reported, especially when mefloquine was used for treatment of patients with malaria. Because mefloquine has been used in the United States for only 18 months, monitoring of adverse reactions remains important. Physicians are encouraged to report serious adverse reactions in persons using mefloquine to CDC's Malaria Branch, Division of Parasitic Diseases, Center for Infectious Diseases telephone (404) 488-4046.

Consistent with previous guidelines, mefloquine is not recommended for use by travelers with known hypersensitivity to mefloquine children 15 kg (30 lbs) pregnant women travelers using beta blockers travelers involved in tasks requiring fine coordination and spatial discrimination, such as airplane pilots and travelers with histories of epilepsy or psychiatric disorder [1,2!.

Travelers to areas of risk where chloroquine-resistant P. falciparum is endemic and for whom mefloquine is contraindicated may elect to use daily doxycycline alone or chloroquine alone. If chloroquine is used, the traveler needs to be aware of the need to seek medical attention for febrile episodes and to carry a treatment dose of pyrimethamine-sulfadoxine (Fansidar[R!)to be used if medical care is not available within 24 hours [1,2!.

The CDC publication Health Information for International Travel [2! provides detailed information for each country on the risk for malaria to travelers and on the presence of drug-resistant P. falciparum [1!. Health information for travelers is available 24 hours a day from the CDC automated telephone system at (404) 332-4555.

Periodic shortages of mefloquine have occurred in the United States. Travelers who cannot obtain mefloquine before departure may be able to purchase it in Europe while in transit to countries with endemic malaria. Prescriptions written in the United States are accepted at airport pharmacies in Frankfurt and Paris (both Charles de Gaulle and Orly airports). The pharmacy at Heathrow Airport in London requires prescriptions written in Great Britain. At the airport pharmacy in Brussels, a prescription from the airport physician is required. Mefloquine is not available at the airports in Amsterdam and Rome and at Gatwick (London).

In some countries, a fixed combination of mefloquine and pyrimethamine-sulfadoxine is marketed under the name Fansimef[R!. Fansimef[R! should not be confused with mefloquine, and it is not recommended for prophylaxis of malaria.

(*1) This revision replaces the recommended mefloquine dosing regimen in reference 1, page 4 and figure 2, and reference 2, page 98.

References

[1.! CDC. Recommendations for the prevention of malaria among travelers. MMWR 1990 39 (no. RR-3).

[2.! CDC. Health information for international travel, 1990. Atlanta: US Department of Health and Human Services, Public Health Service, 1990 DHHS publication no. (CDC)90-8280.

[3.! CDC. Revised dosing regimen for malaria prophylaxis with mefloquine. MMWR 1990 39:630.

[4.! Lackritz EM, Lobel HO, Howell J, Bloland P, Campbell CC. Imported Plasmodium falciparum malaria in American travelers to Africa. JAMA 1991 265:383-5.

[5.! Lobel HO, Bernard KW, Williams SL, Hightower AW, Patchen L, Campbell CC. Effectiveness and tolerance of long-term malaria prophylaxis with mefloquine: need for a better dosing regimen. JAMA 1991 265:361-4.

Return to Mefloquine

Home

Contact

Resources

Exchange Links

ebay