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Patient Education

Information about Quinacrine for Treating Lupus

Quinacrine Is Here Again!

Quinacrine is an anti-malarial drug that can benefit patients who especially have cutaneous lupus and fatigue as part of their systemic lupus. As discussed below, pleurisy, arthritis, and low blood counts can also improve. When production ceased, Many patients unexpectedly found themselves without one of their most important drugs. Many patients ended up with flares of their rashes, fatigue, and other problems because they had to turn to stronger immunosuppressants.

Quinacrine can be obtained from the compounding pharmacy called:

ChemistryRX, 829 Spruce St., Philadelphia, PA 19707 at 855-790-0100

I called the pharmacist myself at ChemistryRX and she confirmed that is is available.

Dr. Jun Kang, dermatologist at Johns Hopkins, told me that he has been able to get some insurance companies to cover the cost (personal communication June 2022).

If this is true, then this is a big change from prior to 2018. However, it makes sense. Quinacrine is much cheaper that anifrolumab (Saphnelo) and belimumab (Benlysta). 

Below, I share very practical information on how to prescribe quinacrine. I’ve used it in many patients for over 20 years and have found it helpful for many. My biggest concerns that I look out for are lichenoid drug reactions (in which case it should be stopped) and the yellow skin discoloration. I have had a few patients actually like the skin discoloration, comparing it to having a tan.

Atabrine or quinacrine vials used by soldiers in World War 2

Quinacrine (excerpt from The Lupus Encyclopedia)

Note: I discuss all lupus drugs in this manner in my book, The Lupus Encyclopedia, and I provide very practical advice for each medication.

Quinacrine is an antimalarial used to treat lupus (chloroquine and hydroxychloroquine are the other two). One of its major advantages is the lack of retina problems. Only two reported cases of retinopathy in medical literature have occurred out of millions of quinacrine prescriptions since the 1930s. In one case, the patient continued taking quinacrine since her problem was not severe enough to stop it; after an additional four more years, her eye condition did not worsen. Another study reported on twenty-six patients who took quinacrine over thirty years, and none developed retinopathy.

No major pharmaceutical companies have produced quinacrine since 1992, because it is not profitable for them to manufacture. There are not enough lupus patients taking it to offset the costs of production. However, compounding pharmacists can make it.

Comparison to HCQ

Lupus experts use quinacrine in patients because it works much faster than HCQ, and therefore it can be very useful to use along with HCQ initially to try to get quicker control of lupus, especially for severe rashes, mouth sores, hair loss, and arthritis. 

Since it does not affect the retina, it can be used in people who have eye problems that prevent them from being able to use  HCQ. Lastly, if someone is on  HCQ and has persistent mild lupus problems (such as fatigue, memory problems, mild rash, or mild arthritis), but is not sick enough to warrant strong immunosuppressant medicines or steroids, then quinacrine can be a better and safer alternative. It especially may be helpful for energy and memory in some people if those problems are directly due to lupus (instead of being due to depression, fibromyalgia, or other disorders). It can have rapid, impressive results when treating severe discoid lupus, mouth sores, and hair loss in some patients. Quinacrine can also help with swollen lymph nodes, fever, sun-sensitive rashes, and headaches.

Generic available

Yes, but it is not inexpensive since the compounding pharmacist must individually manufacture the capsules.

How quinacrine works

How it exactly works in lupus is not fully known. It may work like other antimalarials . For example, quinacrine has been shown to bind to DNA in the nuclei in cells and actually decrease the production of antinuclear antibodies (the hallmark lab finding in people who have SLE). Just like other antimalarial medicines, it also decreases the effects of ultraviolet light activity in the skin. Ultraviolet light is one of the best-known activators of lupus activity.

What benefits to expect from quinacrine

Like  HCQ and chloroquine, quinacrine is most helpful for mild lupus problems such as rashes, arthritis, serositis (pleurisy), fever, fatigue, and low blood counts. One of its biggest advantages is that it appears to stimulate the brain better, so energy levels and memory often improve better with quinacrine compared to the other antimalarial medications. It works a lot faster than  HCQ (which can take six to twelve months for its full effects). Quinacrine can start to work in a few weeks in some people. By three months, its full effect is noticeable. In fact, it can rapidly improve severe discoid lupus, hair loss, and mouth ulcers within 4 to 12 weeks.

Methods of taking quinacrine

It is usually provided as a yellow powder in capsule form. The usual prescribing dose is 50 mg to 100 mg a day. It is best to start with 50  mg a day first. If the desired effect is not achieved, the dose can be increased to 100 mg a day. When patients are doing well, we taper down the dose as needed. However, most patients do best if they continue to take it for a long time even if only taking it once or twice a week. Although it can be taken by itself, it works even better if taken along with  HCQ and/or chloroquine.

If you miss a dose of your medicine

If you miss a dose of your quinacrine, take your next dose as soon as you remember that you forgot it on the same day. For example, if you usually take it at 11:00 AM every day and you realize at 8:00 PM that you forgot to take your medicine, go ahead and take your tablet for that day. Resume taking your next dose of quinacrine at 11:00 AM the next day. However, if you do not remember until the next morning that you forgot your previous day’s dose, just wait until 11:00 AM, and take your usual dose for that day, totally missing the previous day’s dose. Consult with your prescribing doctor to double-check these instructions, but these guidelines will suffice for most people.

Alcohol/food/herbal interactions with quinacrine

Alcohol should be avoided if you get stomach upset. Quinacrine can be taken with or without food. However, taking it with food can decrease stomach upset. Also do not take Echinacea, which can increase immune system activity.

Potential side effects of quinacrine

The most significant potential side effect of quinacrine is that it can cause a severe blood problem called aplastic anemia. This is a condition where all the blood cell counts (red blood cells, white blood cells, and platelets) can become severely low, and unfortunately 50% of people who develop it can die from this complication.

However, aplastic anemia from quinacrine is very rare, only occurring in one out of 50,000 people. Eleven patients with lupus or rheumatoid arthritis have ever reported this complication. All but one were on much higher doses than 100 mg daily. In addition, these patients were not having their blood work monitored carefully (as recommended below). Fifty percent of the patients who developed this severe complication developed an itchy skin rash called lichen planus (or a lichenoid drug reaction) before they developed the blood problem. Today because doctors monitor patients much more closely and use much lower doses of the medicine, as long as people stop the medicine if they get a rash, this side effect should be very rare, and potentially may not even occur at all.

There are no reported cases of aplastic anemia in patients who take 100 mg a day and have their blood work monitored regularly. 

If the blood work does not show anemia, stopping the medicine will resolve it.

Other Side Effects

Quinacrine was initially developed as a yellow dye. Approximately 50% of people will develop discoloration of the skin, eyes, or gums. Half of these people will have black and blue areas, and half will have a yellow tone to the skin. Interestingly, sometimes the skin can appear tan, and some patients actually like the esthetics of the tanned look. If the discoloration occurs, it goes away and the skin returns to its normal color when the dose is decreased or the medicine is stopped.

Other unusual rashes can occur with the use of quinacrine, including hair loss. Fortunately, these only occur in one out of two thousand people who take quinacrine. All skin changes should be pointed out to your prescribing doctor if they occur.

What needs to be monitored while taking quinacrine

Blood work for complete blood cell counts should be done monthly for the first few months, then every two to three months after that. No eye exams are needed.

Reasons not to take quinacrine (contraindications or precautions)

Allergy to quinacrine.

While taking quinacrine

Discontinue use immediately if you develop a rash, and contact your doctor to a CBC blood test done.

Pregnancy and breast-feeding while taking quinacrine

Quinacrine crosses the placenta. No studies have been done on pregnant women. There have been reports of successful pregnancies in women who took quinacrine throughout pregnancy and no adverse effects. It is not recommended during pregnancy.

If you do get pregnant while taking quinacrine, consider contacting the Organization of Teratology Information Specialists (OTIS) who provide the MotherToBaby service and pregnancy studies at mothertobaby.org or 866-626-6847 or email MotherToBaby@health.ucsd.edu so that more can be learned about what happens when women on medications used in treating lupus become pregnant.

Adequate information is not available about breast-feeding while on this medication. It is not recommended while breast-feeding.

Geriatric use of quinacrine

No changes from the above information.

What to do with quinacrine at the time of surgery

It is always best to double-check with your rheumatologist and surgeon regarding specific instructions. However, quinacrine is probably safe to take up to the time you are told to stop taking medications by mouth before surgery.

Drug helpline for quinacrine

Unaware of any.

Website to learn more about quinacrine

Unaware of any. This appears to be some of the most practical information available.

Potential Side Effects of Quinacrine

Nuisance side effects

Headache or dizziness
Common
Contact your doctor. Resolves on lower doses or if medicine is stopped.

Insomnia, nervousness
Common
Contact your doctor. Usually resolves at lower doses.

Weight loss, loss of appetite
Uncommon
Resolves on lower doses or when stopped.

Decreased sweating
Uncommon
If bothersome, lower the dose

Stomach upset, nausea
Common
Try taking it with food or with Pepto Bismol. Usually resolves at lower doses.

Blue-black or yellow pigment changes of skin and gums
Very common
Resolves on lower doses or if the medicine is stopped.

Rash
Common
Stop the medicine immediately and contact your doctor to get a blood test done for complete blood count (CBC).

 

Serious side effects

Difficulty thinking, bizarre thoughts or behavior
Very rare
Resolves after stopping the medicine.

Aplastic anemia; 50% of the time preceded by an itchy rash
Very rare (if ever) at current doses and with getting a CBC done regularly
Contact your doctor immediately.

Side effect incidence key (approximations, as side effects can vary widely study to study): rare < 1% occurrence; uncommon 1%–5% occurrence; common > 5% occurrence

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