The drugs quinacrine, chloroquine, and hydroxychloroquine were all developed as antimalarials but found new applications in treating chronic conditions. The conditions that benefit most from these drugs are those that involve inflammatory processes such as rheumatoid arthritis and lupus. While the exact mechanism of action is not known, many rheumatologists prescribe these medications because of their proven success in relieving symptoms like pain and swelling and preventing the recurrence of flares. Symptoms that may be improved with the use of quinacrine, chloroquine, and hydroxychloroquine include:

• Muscle and joint pain
• Rashes
• Fevers
• Fatigue
• Inflammation of the heart and lungs
• Damage to the kidneys and other organs

Quinacrine, Chloroquine, and Hydroxychloroquine

Drugs like quinacrine were initially used in preventing and treating malaria infections that are transmitted through mosquitoes. Quinine, which is derived from the cinchona plant and has been used for hundreds of years, was used before synthetics like quinacrine, chloroquine, and hydroxychloroquine were developed. Now, most antimalarial medications are synthetically produced.

While quinine was known to treat rheumatic conditions before WWII, it was not until its widespread use during the war that this application became more developed. It was discovered that soldiers being treated with antimalarials also had improvements in rheumatic symptoms like skin rashes and arthritis. Further research was then conducted and in the following years the synthetics that are still used now were developed.

When used to treat a chronic autoimmune condition, antimalarials are referred to as disease-modifying antirheumatic drugs or DMARDS. Quinine was one of the first DMARDS used for treating rheumatic diseases. A unique benefit of antimalarials is that they are capable of effectively modulating the immune response without suppressing the immune system. This is one of the main reasons they have been used consistently for so many years for rheumatic conditions.

Much of the recent research on antimalarials has focused on treating lupus and arthritis. It has been demonstrated that antimalarials reduce the severity of lupus and can prevent the cumulative damage that occurs over many years. If an antimalarial drug is started early, it may be able to reduce the damage to organs that starts as soon as three years after diagnosis.

Antimalarials and Compounding

Hydroxychlororquine is sold under the brand name Plaquenil as an antimalarial with no indication for treating rheumatic diseases. Quinacrine is no longer commercially available and can only be obtained from a compounding pharmacy. Chloroquine is commercially available but is usually more expensive than a compounded alternative. There are also combinations of antimalarials that are used when treatment with only one is not effective. A combination that is sometimes called “triquin” has quinacrine, chloroquine, and hydroxychloroquine in one capsule and is used to treat more severe symptoms. Multiple combinations and strengths are available from a compounding pharmacy since each prescription is made for an individual patient. Some common formulations available from our compounding pharmacy include:

• Quinacrine 50mg and 100mg Capsules
• Chloroquine 100mg, 250mg, and 500mg Capsules
• Hydroxychloroquine 200mg, 300mg, and 400mg Capsules
• Quinacrine 100mg, Chloroquine 250mg Capsules
• Quinacrine 100mg, Chloroquine 250mg, Hydroxychloroquine 200mg Capsules

Antimalarial Prescribing Information

These drugs are usually taken with food to prevent gastrointestinal upset and are prescribed to be taken either once or twice per day. They should be taken at the same time each day and if a dose is missed it should not be “doubled up” the next day. Since antimalarials are disease-modifying drugs that do not cure chronic conditions, they usually are prescribed to be taken indefinitely.  The full effects for autoimmune conditions may not be experienced for at least 6 months after starting treatment. It is important when taking these drugs to be aware of any pre-existing ophthalmic conditions as they may cause vision problems for certain patients.

While quinacrine, chloroquine, and hydroxychloroquine continue to be studied, they will also continue to be prescribed by healthcare practitioners who are familiar with their benefits. Some researchers have even commented that it may be unethical to conduct a placebo-controlled trial of these drugs given their well-documented success in treating rheumatic conditions. While certain antimalarials and combinations of these drugs are not commercially available, they can still be obtained from a compounding pharmacy at a reasonable price.

Research – External Links

• The Early Protective Effect of Hydroxychloroquine on the Risk of Cumulative Damage in Patients with Systemic Lupus Erythematosus. – Journal of Rheumatology
• Antimalarials—the ‘real‘ advance in lupus. – Lupus
• Hydroxychloroquine: the cornerstone of lupus therapy – Lupus