Hydroxychloroquine
FDA Drug Information • Also known as: Hydroxychloroquine
- Brand Names
- Hydroxychloroquine
- Route
- ORAL
- Dosage Form
- TABLET
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
11 DESCRIPTION Hydroxychloroquine sulfate tablets, USP is an antimalarial and antirheumatic drug, chemically described as 2-[[4-[(7-Chloro-4-quinolyl)amino]pentyl]ethylamino] ethanol sulfate (1:1) with the molecular formula C 18 H 26 ClN 3 O
What Is Hydroxychloroquine Used For?
1 INDICATIONS AND USAGE Hydroxychloroquine sulfate tablets are an antimalarial and antirheumatic indicated for the: Treatment of uncomplicated malaria due to Plasmodium falciparum, Plasmodium malariae, Plasmodium ovale, and Plasmodium vivax in adult and pediatric patients. ( 1.1 ) Prophylaxis of malaria in geographic areas where chloroquine resistance is not reported in adult and pediatric patients. ( 1.1 ) Treatment of rheumatoid arthritis in adults. ( 1.2 ) Treatment of systemic lupus erythematosus in adults. ( 1.3 ) Treatment of chronic discoid lupus erythematosus in adults. ( 1.4 ) Limitations of Use ( 1.1 ): Hydroxychloroquine sulfate tablets are not recommended for the: Treatment of complicated malaria. Treatment of chloroquine or hydroxychloroquine-resistant strains of Plasmodium species. Treatment of malaria acquired in geographic areas where chloroquine resistance occurs or when the Plasmodium species has not been identified. Prophylaxis of malaria in geographic areas where chloroquine resistance occurs. Prevention of relapses of P. vivax or P. ovale because it is not active against the hypnozoite liver stage forms of these parasites. For radical cure of P. vivax and P. ovale infections, concomitant therapy with an 8-aminoquinoline drug is necessary. 1.1 Malaria Hydroxychloroquine sulfate tablets are indicated in adult and pediatric patient for the: Treatment of uncomplicated malaria due to Plasmodium falciparum, Plasmodium malariae, Plasmodium vivax, and Plasmodium ovale. Prophylaxis of malaria in geographic areas where chloroquine resistance is not reported. Limitations of Use : Hydroxychloroquine sulfate tablets are not recommended for: Treatment of complicated malaria. Treatment of malaria by chloroquine or hydroxychloroquine-resistant strains of Plasmodium species [see Microbiology (12.4) ]. Treatment of malaria acquired in geographic areas where chloroquine resistance occurs or when the Plasmodium species has not been identified. Prophylaxis of malaria in geographic areas where chloroquine resistance occurs. Prevention of relapses of P. vivax or P. ovale because it is not active against the hypnozoite liver stage forms of these parasites. For radical cure of P. vivax and P. ovale infections, concomitant therapy with an 8-aminoquinoline drug is necessary [see Microbiology (12.4) ]. For the most current information about drug resistance, refer to the latest recommendations from the Center for Disease Control and Prevention1. 1.2 Rheumatoid Arthritis Hydroxychloroquine sulfate tablets are indicated for the treatment of acute and chronic rheumatoid arthritis in adults. 1.3 Systemic Lupus Erythematosus Hydroxychloroquine sulfate tablets are indicated for the treatment of systemic lupus erythematosus in adults. 1.4 Chronic Discoid Lupus Erythematosus Hydroxychloroquine sulfate tablets are indicated for the treatment of chronic discoid lupus erythematosus in adults.
Dosage and Administration
2 DOSAGE AND ADMINISTRATION Malaria in Adult and Pediatric Patients ( 2.2 ): ● Prophylaxis: Begin weekly doses 2 weeks prior to travel to the endemic area, continue weekly doses while in the endemic area, and continue the weekly doses for 4 weeks after leaving the endemic area: - Adults: 400 mg once a week - Pediatric patients ≥ 31 kg: 6.5 mg/kg up to 400 mg, once a week ● Treatment of Uncomplicated Malaria: See Full Prescribing Information (FPI) for complete dosing information. Rheumatoid Arthritis in Adults ( 2.3 ): Initial dosage: 400 mg to 600 mg daily Chronic dosage: 200 mg once daily or 400 mg once daily (or in two divided doses) Systemic Lupus Erythematosus in Adults ( 2.4 ): 200 mg once daily or 400 mg once daily (or in two divided doses) Chronic Discoid Lupus Erythematosus in Adults ( 2.5 ): 200 mg once daily or 400 mg once daily (or in two divided doses) 2.1 Important Administration Instructions Administer hydroxychloroquine sulfate tablets orally with food or milk. Do not crush or divide the tablets. 2.2 Dosage for Malaria in Adult and Pediatric Patients Hydroxychloroquine sulfate tablets are not recommended in pediatric patients less than 31 kg because the lowest available strength (200 mg) exceeds the recommended dose for these patients and it cannot be divided. Prophylaxis Treatment must start 2 weeks before travel to an endemic area. Advise the patient to take the prophylaxis dosage once a week, staring 2 weeks prior to travel to the endemic area, on the same day every week, continuing the same weekly dose while in the endemic area, and for 4 weeks after leaving the endemic area. The recommended prophylaxis dosage is: Adult patients: 400 mg once a week Pediatric patients ≥ 31kg: 6.5 mg/kg actual body weight (up to 400 mg) once a week Treatment of Uncomplicated Malaria The dosages for the treatment of uncomplicated malaria are: Adult patients: Administer 800 mg initially; subsequently administer 400 mg at 6 hours, 24 hours, and 48 hours after the initial dose (total dosage = 2000 mg). Pediatric patients ≥ 31 kg: Administer 13 mg/kg (up to 800 mg) initially; subsequently administer 6.5 mg/kg (up to 400 mg) at 6 hours, 24 hours, and 48 hours after the initial dose (total dosage = 31 mg/kg - up to 2000 mg). For radical cure of P. vivax and P. ovale infections, concomitant therapy with an 8-aminoquinoline drug is necessary [see Microbiology (12.4) ]. 2.3 Dosage for Rheumatoid Arthritis in Adults The recommended dosage is: Initial dosage: 400 mg to 600 mg daily as a single daily dose or two divided doses. The action of hydroxychloroquine is cumulative and may require weeks to months for maximum therapeutic effect. Daily doses exceeding 5 mg/kg (actual weight) of hydroxychloroquine sulfate increase the incidence of retinopathy [see Warnings and Precautions (5.2) ]. Chronic dosage: 200 mg once daily to 400 mg daily, as a single dose or two divided doses. Corticosteroids, salicylates, and other antirheumatic agents may be used...
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS The following adverse reactions are described in greater detail in other sections: Cardiomyopathy and Ventricular Arrhythmias [see Warnings and Precautions (5.1) ] Retinal Toxicity [see Warnings and Precautions (5.2) ] Serious Skin Reactions [see Warnings and Precautions (5.3) ] Worsening of Psoriasis [see Warnings and Precautions (5.4) ] Risks Associated with Use in Porphyria [see Warnings and Precautions (5.5) ] Hematologic Toxicity [see Warnings and Precautions (5.6) ] Hemolytic Anemia Associated with G6PD [see Warnings and Precautions (5.7) ] Skeletal Muscle Myopathy or Neuropathy [see Warnings and Precautions (5.8) ] Neuropsychiatric Reactions Including Suicidality [see Warnings and Precautions (5.9) ] Hypoglycemia [see Warnings and Precautions (5.10) ] Renal Toxicity [see Warnings and Precautions (5.11) ] The following adverse reactions have been identified during post-approval use of 4-aminoquinoline drugs, including hydroxychloroquine sulfate tablets. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure: Blood and lymphatic system disorders : Bone marrow depression, anemia, aplastic anemia, agranulocytosis, leukopenia, thrombocytopenia Cardiac disorders : Cardiomyopathy, cardiac failure, QT-interval prolongation, ventricular tachycardia, torsades de pointes, atrioventricular block, bundle branch block, sick sinus syndrome, pulmonary hypertension Ear and labyrinth disorders : Vertigo, tinnitus, nystagmus, sensorineural hearing loss Eye disorders : Retinopathy, retinal pigmentation changes (typically bull's eye appearance), visual field defects (paracentral scotomas), macular degeneration, corneal edema, corneal opacities, decreased dark adaptation Gastrointestinal disorders : Nausea, vomiting, diarrhea, abdominal pain General disorders : Fatigue Hepatobiliary disorders : Abnormal liver function tests, fulminant hepatic failure Immune system disorders : Urticaria, angioedema, bronchospasm Metabolism and nutrition disorders : Anorexia, hypoglycemia, weight loss Musculoskeletal and connective tissue disorders : Proximal myopathy, depressed tendon reflexes, abnormal nerve conduction Nervous system disorders : Ataxia, dizziness, headache, seizure, extrapyramidal disorders (dystonia, dyskinesia, tremor) Neuropsychiatric disorders : Affect/emotional lability, irritability, nervousness, psychosis, suicidal ideation, suicidal behavior, depression, hallucinations, anxiety, agitation, confusion, delusions, paranoia, mania and sleep disorders (insomnia, night terrors, nightmares) Skin and subcutaneous tissue disorders : Alopecia, hair color changes, rash, pruritus, photosensitivity, psoriasis exacerbation, hyperpigmentation, exfoliative dermatitis, erythema multiforme, acute generalized exanthematous pustulosis, Drug Rash with Eosinophilia and Systemic Symptoms (DRESS syndrome), Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN) The most common adverse reactions reported are: nausea, vomiting, diarrhea, and abdominal pain. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Creekwood Pharmaceuticals LLC. at 1-732-344-0220 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
Drug Interactions
7 DRUG INTERACTIONS Drugs Prolonging QT Interval and Other Arrhythmogenic Drugs. ( 7.1 ) See FPI for more important drug interactions. ( 7 ) 7.1 Drugs Prolonging QT Interval and Other Arrhythmogenic Drugs Hydroxychloroquine sulfate tablets prolongs the QT interval. There may be an increased risk of inducing ventricular arrhythmias if hydroxychloroquine sulfate tablets are used concomitantly with other arrhythmogenic drugs. Therefore, hydroxychloroquine sulfate tablets are not recommended in patients taking other drugs that have the potential to prolong the QT interval or are arrhythmogenic [see Warnings and Precautions (5.1) ]. 7.2 Insulin or Other Antidiabetic Drugs Hydroxychloroquine sulfate tablets may enhance the effects of insulin and antidiabetic drugs, and consequently increase the hypoglycemic risk. Therefore, a decrease in dosage of insulin and other antidiabetic drugs may be necessary [see Warnings and Precautions (5.10) ]. 7.3 Drugs that Lower the Seizure Threshold Hydroxychloroquine sulfate tablets can lower the seizure threshold. Co-administration of hydroxychloroquine sulfate tablets with other antimalarials known to lower the seizure threshold (e.g., mefloquine) may increase the risk of seizures. 7.4 Antiepileptics The activity of antiepileptic drugs might be impaired if co-administered with hydroxychloroquine sulfate tablets. 7.5 Methotrexate Concomitant use of hydroxychloroquine sulfate tablets and methotrexate may increase the incidence of adverse reactions. 7.6 Cyclosporine An increased plasma cyclosporine level was reported when cyclosporine and hydroxychloroquine sulfate tablets were co-administered. Monitor serum cyclosporine levels closely in patients receiving combined therapy. 7.7 Digoxin Concomitant hydroxychloroquine sulfate tablets and digoxin therapy may result in increased serum digoxin levels. Monitor serum digoxin levels closely in patients receiving combined therapy. 7.8 Cimetidine Concomitant use of cimetidine resulted in a 2-fold increase of exposure of chloroquine, which is structurally related to hydroxychloroquine. Interaction of cimetidine with hydroxychloroquine cannot be ruled out. Avoid concomitant use of cimetidine. 7.9 Rifampicin Lack of efficacy of hydroxychloroquine was reported when rifampicin was concomitantly administered. Avoid concomitant use of rifampicin. 7.10 Praziquantel Chloroquine has been reported to reduce the bioavailability of praziquantel. Interaction of praziquantel with hydroxychloroquine cannot be ruled out. 7.11 Antacids and kaolin Antacids and kaolin can reduce absorption of chloroquine; an interval of at least 4 hours between intake of these agents and chloroquine should be observed. Interaction of antacids and kaolin with hydroxychloroquine cannot be ruled out. 7.12 Ampicillin In a study of healthy volunteers, chloroquine significantly reduced the bioavailability of ampicillin. Interaction of ampicillin with hydroxychloroquine cannot be ruled out.
Contraindications
4 CONTRAINDICATIONS Hydroxychloroquine sulfate tablets are contraindicated in patients with known hypersensitivity to 4-aminoquinoline compounds. Patients with hypersensitivity to 4-aminoquinoline compounds ( 4 )
Pregnancy and Breastfeeding
8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to hydroxychloroquine sulfate tablets during pregnancy. Encourage patients to register by contacting 1-877-311-8972. Risk Summary Prolonged clinical experience over decades of use and available data from published epidemiologic and clinical studies with hydroxychloroquine sulfate tablets use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal, or fetal outcomes (see Data) . There are risks to the mother and fetus associated with untreated or increased disease activity from malaria, rheumatoid arthritis, and systemic lupus erythematosus in pregnancy (see Clinical Considerations) . Animal reproduction studies were not conducted with hydroxychloroquine. The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the US general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo-Fetal Risk Malaria : Malaria during pregnancy increases the risk for adverse pregnancy outcomes, including maternal anemia, prematurity, spontaneous abortion, and stillbirth. Rheumatoid Arthritis : Published data suggest that increased disease activity is associated with the risk of developing adverse pregnancy outcomes in women with rheumatoid arthritis Adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2500 g) infants, and small for gestational age at birth. Systemic Lupus Erythematosus : Pregnant women with systemic lupus erythematosus, especially those with increased disease activity, are at increased risk of adverse pregnancy...
Overdosage
10 OVERDOSAGE Hydroxychloroquine sulfate tablets overdosage symptoms have an onset within 1–3 hours of ingestion. The following have been reported with hydroxychloroquine sulfate tablets overdosage: Cardiovascular toxicity, including QRS or QTc prolongation, ventricular tachycardia, ventricular fibrillation, torsade de pointes, atrioventricular block, cardiac arrest and death. Life-threatening hypotension is common. Severe hypokalemia secondary to an intracellular shift is common in severe toxicity. Central nervous system (CNS) depression, seizures, visual disturbances, transient blindness, and coma may occur. Gastrointestinal decontamination procedures warrant consideration in patients that present within the first hour post-ingestion. If the level of consciousness rapidly deteriorates in severe poisoning, consider intubation before gastrointestinal decontamination procedures. Monitor plasma potassium levels and manage accordingly. Hemofiltration, hemodialysis, and hemoperfusion are not of benefit. Consider contacting a poison center (1-800-221-2222) or a medical toxicologist for overdosage management recommendations.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING 16.1 How Supplied Hydroxychloroquine sulfate tablets, USP 200 mg is white, capsule shaped film-coated tablets debossed with "ꓲꓲꓲ" on one side and plain on other side. The tablets are available in bottles of: 100 tablets - NDC 82619-131-01 500 tablets - NDC 82619-131-02 1000 tablets - NDC 82619-131-03 16.2 Storage Dispense in a tight, light-resistant container as defined in the USP/NF. Store at 20° to 25°C (68° to 77°F), excursions permitted between 15° and 30°C (59° and 86°F) [See USP Controlled Room Temperature]. 16.1 How Supplied Hydroxychloroquine sulfate tablets, USP 200 mg is white, capsule shaped film-coated tablets debossed with "ꓲꓲꓲ" on one side and plain on other side. The tablets are available in bottles of: 100 tablets - NDC 82619-131-01 500 tablets - NDC 82619-131-02 1000 tablets - NDC 82619-131-03
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.