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The Treatment of Lupus - Antimalarials

The bark of certain trees has, for many centuries, been known to have healing powers. Aspirin, for example, from the bark of the willow tree - long known for its pain relieving properties - has also come into it's own as a protection against blood clotting such as heart attacks & strokes.

Similarly, the bark of the cinchona tree has been known for centuries by the South Americans as a treatment for fever. The essential ingredients of this particular bark were quinines (found in small amounts in tonic water). Quinines were found to have a variety of healing powers; in fever, aches & pains, cramp and more widely, in treating malaria. In the quinine family, chloroquine became used world wide, not only for malaria but also for a variety of skin diseases. One of the recognised skin diseases was lupus and during the nineteenth century chloroquine became widely used for cutaneous lupus.

In 1895, Dr Thomas Payne, a physician in St. Thomas' Hospital London, recognised that chloroquine might have more general healing powers in lupus, for example healing joint pain & fatigue. This discovery paved the way for a century of 'antimalarial' use in various forms of lupus.

Hydroxychloroquine (Plaquenil)
The 'older' drug chloroquine, whilst very effective, had a number of serious side effects including nausea, and in high doses, retinal damage in the eye. The move to the 'son of chloroquine' - hydroxychloroquine - trade name Plaquenil, has changed all this. Plaquenil has a very high degree of safety (particularly regarding the eyes) and in most countries in the world (sadly not all) has replaced chloroquine.

What does it do?
Plaquenil has beneficial effects on 3 major aspects of lupus; skin rashes, aches & pains and fatigue. It has also been found to help in a number of other features of the disease, though less predictably.

It is very effective in the treatment of a whole variety of lupus skin rashes, particularly those found to be worsened by sunlight. Thus it is widely used as first choice (or 'first line') treatment in lupus. As well as helping the skin itself, it is often helpful in treating hair loss in lupus. It helps the muscle & joint pains, though in cases where these are severe, its effects may be too mild. One of the most successful uses is in fatigue, many patients showing improvement after several weeks' treatment.

How does Plaquenil work?
Surprisingly, the reason for its success in lupus still remains somewhat mysterious. It has a wide variety of known effects - aspirin-like anti-inflammatory, mild immunosuppressive and (mild) cholesterol lowering amongst others. Perhaps an important property is that of sun-protection. This may contribute to its success in treating many sun-sensitive rashes in lupus. It is the practice of some patients from sunnier countries, such as Greece, to take Plaquenil in the summer months, coming off for winter.

Dose
The normal dose of Plaquenil is 1 tablet a day (200mg/day). Some doctors recommend 2 a day (400mg/day) but we find that 1 a day suits most people - the dose can always be increased for a flare. One of the attractions of this medication is its long 'half-life' - it stays in the system for days & weeks. Thus many patients find they can gradually lower the dose - for example to 3 tablets a week - Monday, Wednesday & Friday.

For how long?
The answer is 'for years', if necessary. There are no firm rules about duration, though many lupus patients find they benefit by staying on a 'long term - low dose regime'. An interesting study from Canada found that there were more flares of lupus if the drug was stopped, suggesting it was keeping the disease at bay.

Side effects
Hydroxychloroquine (Plaquenil) is one of the safest drugs in medicine. Serious side effects are rare & routine blood tests are not required. Allergy (new skin rashes) is unusual but it means ruling our future use. Commoner, usually mild, side effects are indigestion, 'gurgly tummy', diarrhoea & headache. A rare, but important, side effect, usually on higher doses (2-3 tablets a day) is of 'lazy eye' - slight difficulty in focussing. Although harmless, it is important as it causes patients to worry about blindness - and needlessly stop the drug.

Pregnancy
Another reason for wrongly stopping the drug is pregnancy. Hydroxychloroquine is safe in pregnancy and is in routine use in our own lupus pregnancy clinic at St. Thomas' Hospital.

The Eye
The older drug, chloroquine, in higher doses, was found to cause damage to the retina of the eye - in extreme cases, blindness. Fortunately, Plaquenil is considered safe. A few years ago we published a careful study, with our eye colleagues, of patients taking Plaquenil daily for 5 years. No eye toxicity was seen.

Other anti-malarials
Another drug with similar properties to Plaquenil is Mepacrine (in some countries Atabrine). It is very much a second choice for 2 reasons. Firstly, it can cause yellowing of the skin. Secondly, it is very bitter & most unpleasant to take. Nevertheless, it is an extremely effective medicine in patients with severe skin rashes.

Some 20 years ago we introduced a 'combination regime' of Plaquenil & Mepacrine for patients with severe skin lupus - Plaquenil 1 or 2 a day plus Mepacrine (100mg) or alternate days. This regime is now widely used in lupus clinics around the world.
Note: Patients often find difficulty in obtaining Mepacrine from pharmacies. The drug is available. Some years ago, Boots, the makers & distributors of Mepacrine in the UK gave an assurance that although demand for the drug was low, the company would undertake to continue to make it available for lupus sufferers.

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