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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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FDA advisories - Lariam, Lunelle
From American Family Physician, 11/15/02 by Carrie Morantz

* Mefloquine. The U.S. Food and Drug Administration (FDA) announced that it and Roche have strengthened the contraindications, warnings, precautions, and adverse reactions sections of the product label for mefloquine hydrochloride (Lariam). Mefloquine is indicated for the treatment of mild to moderate acute malaria caused by mefloquine-susceptible strains of Plasmodium falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax.

Mefloquine is also indicated for the prophylaxis of P. falciparum and P. vivax malaria infections, including prophylaxis of chloroquine-resistant strains of P. falciparum.

Mefloquine is contraindicated for prophylaxis in patients with active depression, a recent history of depression, generalized anxiety disorder, psychosis, schizophrenia, or other major psychiatric disorders, or with a history of convulsions. During prophylactic use, if psychiatric symptoms such as acute anxiety, depression, restlessness, or confusion occur, these may be considered prodromal to a more serious event. In these cases, the drug must be discontinued and an alternative medication should be substituted.

The MedWatch 2002 safety summary is available online at www.fda. gov. The text of a letter sent by Roche to physicians, and the full, revised label are also available.

* Lunelle. The FDA announced in October that Pharmacia is voluntarily recalling all Lunelle (medroxyprogesterone acetate and estradiol cypionate injectable suspension) prefilled syringe lots distributed in the United States, Puerto Rico, and the U.S. Virgin Islands during 2002, because of a lack of assurance of full potency and possible risk of contraceptive failure. A sub-potent dose of Lunelle may not be effective in preventing pregnancy. Lunelle packaged in vials is not affected by this recall, nor is any other Pharmacia contraceptive product.

Women who have been using Lunelle as their contraceptive are advised to seek the advice of their physician regarding alternative methods of birth control and to use an additional barrier method of birth control (such as male or female condoms, diaphragm, or spermicide) until beginning a new form of hormonal contraception.

Physicians may call the Pharmacia medical information service at 800-323-4204 for more information. Patients may call the Pharmacia patient information service at 888-691-6813.

COPYRIGHT 2002 American Academy of Family Physicians
COPYRIGHT 2002 Gale Group

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