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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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Drug problem: the Lariam debate
From Evening Standard (London), 9/17/02

Controversy has surrounded Lariam since it was launched in 1989, and has been linked to several suicides around the world. Its maker, Hoffman-La Roche estimates that only one in 10,000 users will become so ill from side-effects as to require hospital treatment - although other studies have suggested that as many as one in 140 users may suffer temporarily disabling side-effects.

Malaria kills over two million people every year, making it one of the world's deadliest diseases.

Over 30,000 European and American travellers are infected every year with the disease, which spreads from person to person by mosquitos. Early symptoms are often mistaken for flu (a mild fever, chills, headaches, general malaise). Later symptoms include fever, delirium and confusion.

Cerebral malaria is fatal in 20 per cent of cases.

Lariam is 97 per cent effective in preventing malaria, and is recommended for most African countries, all around the Amazon basin, some parts of Central Asia, and South East Asia.

Doctors point out that contracting malaria could be worse than the side effects of Lariam. But in most cases, there are other anti- malarial drugs available.

Possible side-effects of Lariam include convulsions, depression, hallucinations, dizziness, psychosis, loss of balance, headaches, insomnia, abnormal dreams, anxiety, depression, panic attacks, agitation, fatigue, muscle weakness and loss of appetite. The drug is not recommended for anyone with epilepsy, who is pregnant, for scuba divers, or for anyone who has a history of psychological problems or depression.

Psychological effects are known to occur after stopping taking the drug.

Before being licensed, drug trials were conducted largely on soldiers - who were young, male and healthy. Eight out of 10 adults who experienced the most serious sideeffects were women, who tend to weigh less, but take the same dose as men.

A study by Peter Barrett from the Medical Advisory Service Travellers Abroad found that 40 per cent of people experience some kind of side-effect such as nausea, dizziness, strange or vivid dreams, anxiety, depression or seizures.

While most of these effects are short-term, the way the drug works is not fully understood, and in some people the symptoms may last for months or years.

Copyright 2002
Provided by ProQuest Information and Learning Company. All rights Reserved.

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