Hydroxychloroquine

Hydroxychloroquine comes as a tablet to take by mouth. For prevention of malaria in adults, two tablets are usually taken once a week on exactly the same day of each week. The first dose is taken 1 to 2 weeks before traveling to an area where malaria is common, and then doses are continued for 8 weeks after exposure. For treatment of acute attacks of malaria in adults, four tablets are usually taken right away, followed by two tablets 6 to 8 hours later and then two tablets on each of the next 2 days.

For prevention or treatment of malaria in infants and children, the amount of hydroxychloroquine is based on the child's weight. Your doctor will calculate this amount and tell you how much hydroxychloroquine your child should receive.

For lupus erythematosus, one or two tablets are usually taken once or twice daily. For rheumatoid arthritis, one to three tablets are usually taken once a day.

Hydroxychloroquine can be taken with a glass of milk or a meal to decrease nausea. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take hydroxychloroquine exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

If you are taking hydroxychloroquine for symptoms of rheumatoid arthritis, your symptoms should improve within 6 months. If your rheumatoid arthritis symptoms do not improve, or if they worsen, stop taking the drug and call your doctor. Once you and your doctor are sure the drug works for you, do not stop taking hydroxychloroquine without talking to your doctor. Symptoms of rheumatoid arthritis will return if you stop taking hydroxychloroquine.

Children can be especially sensitive to an overdose, so keep the medication out of the reach of children. Children should not take hydroxychloroquine for long-term therapy.

Keep all appointments with your doctor and the laboratory. Your doctor may order certain lab tests to check your response to hydroxychloroquine.

If you are taking hydroxychloroquine for a long period of time, your doctor will recommend frequent eye exams. It is very important that you keep these appointments. Hydroxychloroquine can cause serious vision problems. If you experience any changes in vision, stop taking hydroxychloroquine and call your doctor immediately.

Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.

No information provided. Please refer to the WARNINGS and PRECAUTIONS sections.

Hydroxychloroquine is a prescription medication used to reduce pain and swelling caused by diseases of the immune system such as rheumatoid arthritis, juvenile arthritis, and systemic lupus erythematosus (SLE). This medication belongs to a group of drugs called DMARDs (disease modifying antirheumatic drugs) which work by suppressing the excessive activity of the immune system.

Hydroxychloroquine is also used to prevent and treat malaria. For this reason, it is sometimes classified as an antimalarial drug. The exact way it works for this condition is unknown.

Hydroxychloroquine comes in tablet form. It is taken once or twice a day, unless it is used for the prevention of malaria, in which case it is taken once a week beginning 1 to 2 weeks prior to traveling to an area where malaria is common. Take this medication with a meal or a glass of milk to prevent stomach upset.

Common side effects include nausea, loss of appetite, headache, and diarrhea. Hydroxychloroquine can cause blurred vision and dizziness. Do not drive or operate heavy machinery until you know how it affects you.

Serious side effects have been reported with hydroxychloroquine including the following:

• Heart failure. Hydroxychloroquine can cause weakening of the heart muscle, resulting in heart failure.Tell your healthcare provider right away if you have some or all of the following symptoms of heart failure.
  • breathlessness
  • swelling of the legs
  • irregular heart beat
  • fatigue
  • dizziness
• Retinal damage. Hydroxychloroquine may cause irreversible damage to the retina (the back of the eye where vision is created). You are required to have an eye exam before taking hydroxychloroquine, then a follow-up as often as needed while taking hydroxychloroquine. Tell your healthcare provider right away if you have some or all of the following symptoms.
  • blurred vision
  • seeing halos around lights (especially at night)
  • seeing light flashes and streaks
  • visual field loss
  • change in eye color
  • difficulty focusing eye
  • difficulty reading (skipped words)
  • night blindness
• Hypoglycemia (low blood sugar). Tell your healthcare provider right away if you have some or all of the following symptoms.
  • sweating
  • shakiness
  • weakness
  • dizziness
  • fast heartbeat
• Muscular weakness. All patients on long term therapy should be questioned and examined periodically, including the examination of skeletal muscle function and tendon reflexes, testing of knee and ankle reflexes, to detect any evidence of muscular weakness. If weakness occurs, your doctor may need to discontinue the drug.
• Low blood counts. Your doctor will monitor your blood counts and may have to discontinue medication depending on the results.

Hydroxychloroquine can cause blurred vision and dizziness. Do not drive or operate heavy machinery until you know how hydroxychloroquine affects you.

Do not take hydroxychloroquine if you:

• are allergic to hydroxychloroquine or to any of its ingredients 
• pre-existing retinopathy of the eye
• use in children below 6 years of age (200 mg tablets not adapted for weight < 35kg)

Before taking hydroxychloroquine, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

• are allergic to hydroxychloroquine, allergic to any of its ingredients, or allergic to chloroquine
• liver or kidney disease
• blood disease, including a rare blood disease called porphyria
• nervous system disease
• a skin disease called psoriasis
• a genetic condition known as “glucose-6-phosphate dehydrogenase deficiency”

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Hydroxychloroquine can cause serious liver or heart problems, especially if you use certain medicines at the same time, including:

• other medicines to treat malaria;

• an antibiotic or antifungal medicine;

• antiviral medicine to treat hepatitis or HIV/AIDS;

• antidepressants or antipsychotic medicines;

• birth control pills or hormone replacement therapy;

• cancer medication;

• cholesterol-lowering medication;

• heart or blood pressure medicine;

• pain or arthritis medicines (including aspirin, Tylenol, Advil, and Aleve);

• seizure medication;

• stomach acid reducers; or

• tuberculosis medicine.

This list is not complete and many other drugs can interact with hydroxychloroquine. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide. Tell your doctor about all medicines you use, and those you start or stop using during your treatment with hydroxychloroquine. Give a list of all your medicines to any healthcare provider who treats you.

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For hydroxychloroquine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to hydroxychloroquine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of hydroxychloroquine to prevent and treat malaria in children. However, children are more sensitive to the effects of hydroxychloroquine than adults. Safety and efficacy of hydroxychloroquine to treat lupus and arthritis have not been established in children.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of hydroxychloroquine in the elderly. However, elderly patients are more likely to have age-related kidney problems, which may require caution and an adjustment in the dose for patients receiving hydroxychloroquine.

Breast Feeding

Studies in women suggest that this medication poses minimal risk to the infant when used during breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking hydroxychloroquine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using hydroxychloroquine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Amifampridine
• Amisulpride
• Aurothioglucose
• Bepridil
• Cisapride
• Dronedarone
• Mesoridazine
• Pimozide
• Piperaquine
• Saquinavir
• Sparfloxacin
• Terfenadine
• Thioridazine
• Ziprasidone

Using hydroxychloroquine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Alfuzosin
• Amiodarone
• Amitriptyline
• Anagrelide
• Apomorphine
• Aripiprazole
• Aripiprazole Lauroxil
• Arsenic Trioxide
• Asenapine
• Astemizole
• Atazanavir
• Azithromycin
• Bedaquiline
• Buserelin
• Chloroquine
• Chlorpromazine
• Ciprofloxacin
• Citalopram
• Clarithromycin
• Clomipramine
• Clozapine
• Crizotinib
• Cyclobenzaprine
• Dabrafenib
• Dasatinib
• Degarelix
• Delamanid
• Desipramine
• Deslorelin
• Deutetrabenazine
• Disopyramide
• Dofetilide
• Dolasetron
• Domperidone
• Donepezil
• Doxepin
• Droperidol
• Ebastine
• Efavirenz
• Eribulin
• Erythromycin
• Escitalopram
• Famotidine
• Felbamate
• Fingolimod
• Flecainide
• Fluconazole
• Fluoxetine
• Formoterol
• Foscarnet
• Fosphenytoin
• Galantamine
• Gatifloxacin
• Gemifloxacin
• Gonadorelin
• Goserelin
• Granisetron
• Halofantrine
• Haloperidol
• Histrelin
• Hydroquinidine
• Hydroxyzine
• Ibutilide
• Iloperidone
• Imipramine
• Itraconazole
• Ivabradine
• Ketoconazole
• Lapatinib
• Leuprolide
• Levofloxacin
• Lumefantrine
• Mefloquine
• Methadone
• Methotrimeprazine
• Metronidazole
• Mifepristone
• Mizolastine
• Moricizine
• Moxifloxacin
• Nafarelin
• Nelfinavir
• Nilotinib
• Norfloxacin
• Octreotide
• Ofloxacin
• Olanzapine
• Ondansetron
• Paliperidone
• Panobinostat
• Paroxetine
• Pasireotide
• Pazopanib
• Pentamidine
• Perphenazine
• Pimavanserin
• Pipamperone
• Pitolisant
• Posaconazole
• Probucol
• Procainamide
• Prochlorperazine
• Promethazine
• Propafenone
• Protriptyline
• Quetiapine
• Quinidine
• Quinine
• Ranolazine
• Ribociclib
• Rilpivirine
• Risperidone
• Ritonavir
• Sertindole
• Sevoflurane
• Sodium Phosphate
• Sodium Phosphate, Dibasic
• Sodium Phosphate, Monobasic
• Solifenacin
• Sorafenib
• Sotalol
• Sulpiride
• Sultopride
• Sunitinib
• Tacrolimus
• Tamoxifen
• Telaprevir
• Telavancin
• Telithromycin
• Tetrabenazine
• Tizanidine
• Tolterodine
• Toremifene
• Trazodone
• Trimipramine
• Triptorelin
• Vandetanib
• Vardenafil
• Vemurafenib
• Venlafaxine
• Vilanterol
• Vinflunine
• Voriconazole
• Vorinostat
• Zotepine
• Zuclopenthixol

Using hydroxychloroquine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Digoxin

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of hydroxychloroquine. Make sure you tell your doctor if you have any other medical problems, especially:

• Allergy to 4-aminoquinoline compounds (eg, chloroquine)—Should not be used in patients with this condition.

• Blood or bone marrow problems or
• Diabetes or
• Eye or vision problems or
• Muscle problems or
• Nerve problems or
• Porphyria (blood disorder) or
• Psoriasis (skin disease) or
• Stomach or bowel problems–Use with caution. May make these conditions worse.

• Glucose-6-phosphate dehydrogenase (G6PD) deficiency—May cause hemolytic anemia in patients with this condition.

• Kidney disease or
• Liver disease—Use with caution. The effects may be increased because of the slower removal of the medicine from the body.

Use hydroxychloroquine as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take this medicine with food or milk.
• If antacids are used, they may need to be taken at some other time than hydroxychloroquine. Talk with your doctor or pharmacist.
• To gain the most benefit, do not miss doses.
• Keep taking this medicine as you have been told by your doctor or other health care provider, even if you feel well.

What do I do if I miss a dose?

• Take a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

Administer with food or milk. Do not crush or divide film-coated tablets.

CBC at baseline and periodically; liver function; renal function (in patients at risk for ocular toxicity); blood glucose (if symptoms of hypoglycemia occur); muscle strength (especially proximal, as a symptom of neuromyopathy) during long-term therapy

Ophthalmologic exam at baseline (fundus examination within the first year plus visual fields and spectral-domain optical coherence tomography [SD OCT] if maculopathy is present) to screen for retinal toxicity, followed by annual screening beginning after 5 years of use (or sooner if major risk factors are present) (Marmor [AAO 2016]). Additionally, the manufacturer recommends an ocular exam include best corrected distance visual acuity and an automated threshold visual field of the central 10 degrees (24 degrees in patients of Asian ancestry as retinal toxicity may appear outside of the macula). Consider annual exams (without deferring 5 years) in patients with significant risk factors.

Hydroxychloroquine can be detected in the cord blood at delivery in concentrations similar to those in the maternal serum (Costedoat-Chalumeau 2002). In animal reproduction studies with chloroquine, accumulation in fetal ocular tissues was observed and remained for several months following drug elimination from the rest of the body. Based on available human data, an increased risk of fetal ocular toxicity has not been observed following maternal use of hydroxychloroquine, but additional studies are needed to confirm (Osadchy 2011).

Maternal lupus is associated with adverse maternal and fetal events; however, pregnancy outcomes may be improved if conception does not occur until the disease has been inactive for ≥6 months. Hydroxychloroquine is one of the medications recommended for the management of lupus and lupus nephritis in pregnant women. If pregnancy is detected during therapy, it should not be stopped (could precipitate a flare in maternal disease and exposure to the fetus will still continue for 6 to 8 weeks due to tissue binding) (Baer 2011; Bertsias 2012; Hahn 2012; Levy 2001). Maternal use of hydroxychloroquine may also decrease the incidence of cardiac malformations associated with neonatal lupus (Izmirly 2012).

Malaria infection in pregnant women may be more severe than in nonpregnant women and has a high risk of maternal and perinatal morbidity and mortality. Therefore, pregnant women and women who are likely to become pregnant are advised to avoid travel to malaria-risk areas. Hydroxychloroquine is recommended as an alternative treatment of pregnant women for uncomplicated malaria in chloroquine-sensitive regions (refer to current guidelines) (CDC 2011).

Women exposed to hydroxychloroquine for the treatment of rheumatoid arthritis or systemic lupus erythematosus during pregnancy may be enrolled in the Organization of Teratology Information Specialists (OTIS) Autoimmune Diseases Study pregnancy registry (877-311-8972).

Consult your pharmacist.

How to use Hydroxychloroquine Powder

Consult your pharmacist.

Get emergency medical help if you have signs of an allergic reaction to hydroxychloroquine: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Taking hydroxychloroquine long-term or at high doses may cause irreversible damage to the retina of your eye. Stop taking this medicine and call your doctor at once if you have trouble focusing, if you see light streaks or flashes in your vision, or if you notice any swelling or color changes in your eyes.

Call your doctor at once if you have:

• headache with chest pain and severe dizziness, fainting, fast or pounding heartbeats;

• very slow heart rate, weak pulse;

• muscle weakness, numbness or tingling;

• low blood sugar - headache, hunger, sweating, irritability, dizziness, nausea, fast heart rate, and feeling anxious or shaky; or

• low blood cell counts - fever, chills, sore throat, weakness or ill feeling, swollen gums, mouth sores, skin sores, rapid heart rate, pale skin, easy bruising, unusual bleeding, feeling light-headed.

Common hydroxychloroquine side effects may include:

• headache, dizziness, ringing in your ears;

• nausea, vomiting, stomach pain;

• loss of appetite, weight loss;

• mood changes, feeling nervous or irritable;

• skin rash or itching; or

• hair loss.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

-Initial dose: 400 to 600 mg (310 to 465 mg base) orally once a day to optimum response (usually 4 to 12 weeks)
-Maintenance dose: 200 to 400 mg (155 to 310 mg base) orally once a day
Dose adjustment: The dose may need to be reduced temporarily if adverse side effects occur; after 5 to 10 days the dose may gradually be increased to the optimum response level

Maintenance dose: 200 to 400 mg (155 mg to 310 mg base) orally daily

Comments:
-This drug should be taken with a meal or a glass of milk.
-Side effects may require reduction in the initial dose for 5 to 10 days; the dose may then gradually be increased to the optimum response level.
-The compound is cumulative in action and will require several weeks to exert its beneficial therapeutic effects, whereas minor side effects may occur relatively early.
-Several months of therapy may be required before maximum effects can be obtained.
-If objective improvement (such as reduced joint swelling, increased mobility) does not occur within 6 months, therapy should be discontinued.
-Safe use of this drug in the treatment of juvenile rheumatoid arthritis has not been established.
-Retinopathy has been reported to be higher when the maintenance dose is exceeded.
-Should a relapse occur after medication is withdrawn, therapy may be resumed or continued on an intermittent schedule if there are no ocular contraindications.
-Corticosteroids and salicylates may be used in conjunction with this drug, and they can generally be decreased gradually in dosage or eliminated after the drug has been used for several weeks. When gradual reduction of steroid dosage is indicated, it may be done by reducing every 4 to 5 days: the dose of cortisone by no more than from 5 mg to 15 mg; of hydrocortisone from 5 mg to 10 mg; of prednisolone and prednisone from 1 mg to 2.5 mg; of methylprednisolone and triamcinolone from 1 mg to 2 mg; and of dexamethasone from 0.25 mg to 0.5 mg.

Use: For acute or chronic rheumatoid arthritis in patients who have not responded satisfactorily to drugs with less potential for serious side effects

Substance Name

Hydroxychloroquine

CAS Registry Number

118-42-3

Drug Class

Antimalarials