Prescription Drug Information: Hydroxychloroquine Sulfate

HYDROXYCHLOROQUINE SULFATE — hydroxychloroquine sulfate tablet, film coated
Quallent Pharmaceuticals Health LLC

1 INDICATIONS AND USAGE

1.1 Malaria

Hydroxychloroquine sulfate tablet in 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 tablet is 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 tablet is indicated for the treatment of acute and chronic rheumatoid arthritis in adults.

1.3 Systemic Lupus Erythematosus

Hydroxychloroquine sulfate tablet is indicated for the treatment of systemic lupus erythematosus in adults.

1.4 Chronic Discoid Lupus Erythematosus

Hydroxychloroquine sulfate tablet is indicated for the treatment of chronic discoid lupus erythematosus in adults.

2 DOSAGE AND ADMINISTRATION

2.1 Important Administration Instructions

Administer hydroxychloroquine sulfate tablet orally with food or milk. Do not crush or divide the tablets.

2.2 Dosage for Malaria in Adult and Pediatric Patients

Hydroxychloroquine sulfate is 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 = 2,000 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 2,000 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 concomitantly with hydroxychloroquine sulfate.

2.4 Dosage for Systemic Lupus Erythematosus in Adults

The recommended dosage is 200 mg given once daily, or 400 mg given once daily or in two divided doses.

2.5 Dosage for Chronic Discoid Lupus Erythematosus in Adults

The recommended dosage is 200 mg given once daily, or 400 mg given once daily or in two divided doses.

3 DOSAGE FORMS AND STRENGTHS

Tablets: 200 mg of hydroxychloroquine sulfate, white to off-white, capsule-shaped, biconvex, film-coated tablets debossed with “ZC38” on one side and plain on other side.

4 CONTRAINDICATIONS

Hydroxychloroquine sulfate is contraindicated in patients with known hypersensitivity to 4-aminoquinoline compounds.

5 WARNINGS AND PRECAUTIONS

5.1 Cardiomyopathy and Ventricular Arrhythmias

Fatal and life-threatening cases of cardiotoxicity, including cardiomyopathy, have been reported in patients treated with hydroxychloroquine sulfate. Signs and symptoms of cardiac compromise have occurred during acute and chronic hydroxychloroquine sulfate 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 (5.7, 5.10)].

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 sulfate has a potential to prolong the QT interval. Ventricular arrhythmias (including torsades de pointes) have been reported in hydroxychloroquine sulfate-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 sulfate administration in patients with congenital or documented acquired QT prolongation and/or known risk factors for prolongation of the QT interval such as:

  • Cardiac disease, e.g., heart failure, myocardial infarction.
  • Proarrhythmic conditions, e.g., bradycardia (< 50 bpm).
  • History of ventricular dysrhythmias
  • Uncorrected hypokalemia and/or hypomagnesemia.
  • 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 sulfate 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 sulfate therapy. Discontinue hydroxychloroquine sulfate if cardiotoxicity is suspected or demonstrated by tissue biopsy.

5.2 Retinal 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 sulfate, 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 sulfate and monitor the patient closely given that retinal changes and visual disturbances may progress even after cessation of therapy.

5.3 Serious Skin Reactions

Serious adverse reactions have been reported with the use of hydroxychloroquine sulfate 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), Adverse Reactions (6)]. Discontinue hydroxychloroquine sulfate if these severe reactions occur.

5.4 Worsening of Psoriasis and Porphyria

Administration of hydroxychloroquine sulfate in patients with psoriasis may precipitate a severe flare-up of psoriasis. Administration of hydroxychloroquine sulfate in patients with porphyria may exacerbate porphyria. Avoid hydroxychloroquine sulfate in patients with psoriasis or porphyria, unless the benefit to the patient outweighs the possible risk.

5.5 Hematologic Toxicity

Hydroxychloroquine sulfate may cause myelosuppression including aplastic anemia, agranulocytosis, leukopenia, or thrombocytopenia. Monitor blood cell counts periodically in patients on prolonged hydroxychloroquine sulfate therapy. If the patient develops myelosuppression which cannot be attributable to the disease, discontinue the drug.

5.6 Hemolytic 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.

5.7 Skeletal Muscle Myopathy or Neuropathy

Skeletal muscle myopathy or neuropathy leading to progressive weakness and atrophy of proximal muscle groups, depressed tendon reflexes, and abnormal nerve conduction, have been reported. Muscle and nerve biopsies have shown associated phospholipidosis. Drug-induced phospholipidosis may occur in other organ systems [see Warnings and Precautions (5.1, 5.10)].

Assess muscle strength and deep tendon reflexes periodically in patients on long-term therapy with hydroxychloroquine sulfate. Discontinue hydroxychloroquine sulfate if muscle or nerve toxicity is suspected or demonstrated by tissue biopsy.

5.8 Neuropsychiatric Reactions Including Suicidality

Suicidal behavior has been reported in patients treated with hydroxychloroquine sulfate [see Adverse Reactions (6)]. Alert patients to contact their healthcare provider if they experience new or worsening depression, suicidal thoughts or behavior, or mood changes. The risk and benefit of continued treatment with hydroxychloroquine sulfate should be assessed for patients who develop these symptoms.

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