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.
1.1Malaria
Hydroxychloroquine sulfate tablets are indicated in adult and pediatric patients 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.
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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 Prevention 1 .
1.2Rheumatoid Arthritis
Hydroxychloroquine sulfate tablets are indicated for the treatment of acute and chronic rheumatoid arthritis in adults.
1.3Systemic Lupus Erythematosus
Hydroxychloroquine sulfate tablets are indicated for the treatment of systemic lupus erythematosus in adults.
1.4Chronic Discoid Lupus Erythematosus
Hydroxychloroquine sulfate tablets are indicated for the treatment of chronic discoid lupus erythematosus in adults.
Contraindications
Hydroxychloroquine sulfate tablets are contraindicated in patients with known hypersensitivity to 4-aminoquinoline compounds.
Patients with hypersensitivity to 4-aminoquinoline compounds ( 4 )
Warnings and precautions
Cardiomyopathy and Ventricular Arrhythmias : Fatal or life-threatening cardiomyopathy and ventricular arrhythmias were reported. ( 5.1 )
Retinal Toxicity : Irreversible retinal damage is related to cumulative dosage and treatment duration. Baseline retinal exam and exams during treatment are recommended. ( 5.2 )
Serious Skin Reactions : Stevens Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms, acute generalized exanthematous pustulosis have been reported. ( 5.3 )
Worsening of Psoriasis : Avoid in patients with psoriasis. ( 5.4 )
Risks Associated with Use in Porphyria : Avoid in patients with porphyria. Hepatotoxicity was reported in patients with porphyria cutanea tarda ( 5.5 ).
Hematologic Toxicity : Discontinue if myelosuppression occurs. ( 5.6 )
Renal Toxicity : Consider phospholipidosis as a possible cause of renal injury in patients with underlying connective tissue disorders. Discontinue hydroxychloroquine if renal toxicity is suspected or demonstrated by tissue biopsy in any organ system. ( 5.1 , 5.8 , 5.11 )
5.1Cardiomyopathy and Ventricular Arrhythmias Fatal
and life-threatening cases of cardiotoxicity, including cardiomyopathy, have been reported in patients treated with hydroxychloroquine. Signs and symptoms of cardiac compromise have occurred during acute and chronic hydroxychloroquine treatment. In multiple cases, endomyocardial biopsy showed association of the cardiomyopathy with phospholipidosis in the absence of inflammation, infiltration, or necrosis. Drug-induced phospholipidosis may occur in other organ systems [see Warnings and Precautions (5.8, 5.11) ] .
Patients may present with ventricular hypertrophy, pulmonary hypertension and conduction disorders including sick sinus syndrome. ECG findings include atrioventricular, right or left bundle branch block. Hydroxychloroquine has a potential to prolong the QT interval. Ventricular arrhythmias (including torsades de pointes) have been reported in hydroxychloroquine-treated patients. The magnitude of QT prolongation may increase with increasing concentrations of the drug.
Therefore, the recommended dose should not be exceeded [see Adverse Reactions (6) , Overdosage (10) ]. Avoid hydroxychloroquine administration in patients with congenital or documented acquired QT prolongation and/or known risk factors for prolongation of the QT interval such as:
Concomitant administration with QT interval prolonging agents as this may lead to an increased risk for ventricular arrhythmias [see Drug Interactions (7.1) ]. Therefore, hydroxychloroquine is not recommended in patients taking other drugs that have the potential to prolong the QT interval. Correct electrolyte imbalances prior to use. Monitor cardiac function as clinically indicated during hydroxychloroquine therapy. Discontinue hydroxychloroquine if cardiotoxicity is suspected or demonstrated by tissue biopsy.
5.2Retinal Toxicity
Irreversible retinal damage was observed in some patients treated with hydroxychloroquine sulfate and it is related to cumulative dosage and treatment duration. In patients of Asian descent, retinal toxicity may first be noticed outside the macula. Risk factors for retinal damage include daily hydroxychloroquine sulfate dosages ≥5 mg/kg of actual body weight, durations of use greater than five years, renal impairment, use of concomitant drug products such as tamoxifen citrate, and concurrent macular disease.
Within the first year of starting hydroxychloroquine, a baseline ocular examination is recommended including best corrected distance visual acuity (BCVA), an automated threshold visual field (VF) of the central 10 degrees (with retesting if an abnormality is noted), and spectral domain ocular coherence tomography (SD-OCT). For patients at higher risk of retinal damage, monitoring should include annual examinations which include BCVA, VF and SD-OCT.
For patients without significant risk factors, annual retinal exams can usually be deferred until five years of treatment. In patients of Asian descent, it is recommended that visual field testing be performed in the central 24 degrees instead of the central 10 degrees. If ocular toxicity is suspected, discontinue hydroxychloroquine and monitor the patient closely given that retinal changes and visual disturbances may progress even after cessation of therapy.
5.3Serious Skin Reactions
Serious adverse reactions have been reported with the use of hydroxychloroquine including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), drug reaction with eosinophilia and systemic symptoms (DRESS syndrome), acute generalized exanthematous pustulosis (AGEP). Monitor for serious skin reactions, especially in patients receiving a drug that may also induce dermatitis. Advise patients to seek medical attention promptly if they experience signs and symptoms of serious skin reactions such as blisters on the skin, eyes, lips or in the mouth, itching or burning, with or without fever [see Warnings and Precautions (5.4 , 5.5) , Adverse Reactions (6) ].
Discontinue hydroxychloroquine if these severe reactions occur.
5.4Worsening of Psoriasis Administration
of hydroxychloroquine to patients with psoriasis may precipitate a severe flare-up of psoriasis. Avoid hydroxychloroquine in patients with psoriasis, unless the benefit to the patient outweighs the possible risk.
5.5Risks Associated with Use in Porphyria Administration
of hydroxychloroquine to patients with porphyria may exacerbate porphyria. Avoid hydroxychloroquine in patients with porphyria. Hepatotoxicity Associated with Porphyria Cutanea Tarda Cases of hepatotoxicity have been reported when hydroxychloroquine was used in patients with porphyria cutanea tarda (PCT). Patients received dosages ranging from 200 mg twice weekly to 400 mg daily. Most of the PCT-related cases presented with marked elevations in transaminases (>20 times upper limit of the reference range) within days to a month of hydroxychloroquine initiation.
In some cases, PCT was diagnosed only after the occurrence of treatment-induced liver injury, when hydroxychloroquine was prescribed for an approved indication. Some of the cases were associated with other risk factors for hepatic injury (e.g., alcohol use, concomitant hepatotoxic medications). Measure liver tests promptly in patients who report symptoms that may indicate liver injury, such as fatigue, rash, nausea, dark urine, or jaundice.
In this clinical context, if the patient is found to have abnormal serum liver tests (e.g., ALT level greater than three times the upper limit of the reference range, total bilirubin greater than two times the upper limit of the reference range), interrupt treatment with hydroxychloroquine, and investigate further to establish the probable cause. The safety and effectiveness of hydroxychloroquine for the treatment of PCT have not been established and hydroxychloroquine is not approved for this use .
5.6Hematologic Toxicity
Hydroxychloroquine may cause myelosuppression including aplastic anemia, agranulocytosis, leukopenia, or thrombocytopenia. Monitor blood cell counts periodically in patients on prolonged hydroxychloroquine therapy. If the patient develops myelosuppression which cannot be attributable to the disease, discontinue the drug.
5.7Hemolytic Anemia Associated with G6PD Deficiency
Hemolysis has been reported in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency. Monitor for hemolytic anemia as this can occur, particularly in association with other drugs that cause hemolysis.
5.8Skeletal Muscle Myopathy or Neuropathy
Skeletal muscle myopathy or neuropathy leading to progressive weakness and atrophy of proximal muscle groups, depressed te
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Interactions
Drugs Prolonging QT Interval and Other Arrhythmogenic Drugs. ( 7.1 )
See FPI for more important drug interactions. ( 7 )
7.1Drugs Prolonging QT Interval and Other Arrhythmogenic Drugs
Hydroxychloroquine prolongs the QT interval. There may be an increased risk of inducing ventricular arrhythmias if hydroxychloroquine is used concomitantly with other arrhythmogenic drugs. Therefore, hydroxychloroquine is 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) ].
7.2Insulin or Other Antidiabetic Drugs
Hydroxychloroquine 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 can lower the seizure threshold. Co-administration of hydroxychloroquine with other antimalarials known to lower the seizure threshold (e.g., mefloquine) may increase the risk of seizures.
7.4Antiepileptics
The activity of antiepileptic drugs might be impaired if co-administered with hydroxychloroquine.
7.5Methotrexate
Concomitant use of hydroxychloroquine and methotrexate may increase the incidence of adverse reactions.
7.6Cyclosporine
An increased plasma cyclosporin level was reported when cyclosporin and hydroxychloroquine were co-administered. Monitor serum cyclosporine levels closely in patients receiving combined therapy.
7.7Digoxin
Concomitant hydroxychloroquine and digoxin therapy may result in increased serum digoxin levels. Monitor serum digoxin levels closely in patients receiving combined therapy.
7.8Cimetidine
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.
7.9Rifampicin Lack
of efficacy of hydroxychloroquine was reported when rifampicin was concomitantly administered. Avoid concomitant use of rifampicin.
7.10Praziquantel
Chloroquine has been reported to reduce the bioavailability of praziquantel. Interaction of praziquantel with hydroxychloroquine cannot be ruled out.
7.11Antacids
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.
Pregnancy and breastfeeding
8.1Pregnancy Pregnancy Exposure Registry
There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to hydroxychloroquine 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 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 to 4% and 15 to 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 2,500 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 outcomes, including spontaneous abortion, fetal death, preeclampsia, preterm birth, and intrauterine growth restriction. Passage of maternal auto-antibodies across the placenta may result in neonatal illness, including neonatal lupus and congenital heart block.
Data Human Data Data from published epidemiologic and clinical studies have not established an association with hydroxychloroquine use during pregnancy and major birth defects, miscarriage, or adverse maternal or fetal outcomes. Hydroxychloroquine readily crosses the placenta with cord blood levels corresponding to maternal plasma levels. No retinal toxicity, ototoxicity, cardiotoxicity, or growth and developmental abnormalities have been observed in children who were exposed to hydroxychloroquine in utero .
Available epidemiologic and clinical studies have methodological limitations including small sample size and study design.
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. 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 Laurus Generics Inc. at 1-833-3-LAURUS (1-833-352-8787) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Composition
Active ingredients
HYDROXYCHLOROQUINE SULFATE 200MG
Strengths and forms
The FDA lists each strength of a product separately; these pages share one label.
Prognia shows this product information for reference and learning. It is not treatment advice and can lag behind the official text. Always check the current product information and local protocols before prescribing.
