hydroxychloroquine sulfate (Rx)

Brand and Other Names:Plaquenil
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 200mg

Malaria

Prophylaxis

  • Indicated for prophylaxis of malaria in geographic areas where chloroquine resistance is not reported
  • 400 mg (310 mg base) PO weekly, starting 2 weeks before exposure and continued for 4 weeks after departure from endemic area OR
  • Weight-based dosing: 6.5 mg/kg (5 mg/kg base) PO once weekly, not to exceed 400 mg (310 mg base), starting 2 weeks before exposure and continued for 4 weeks after leaving the endemic area  

Acute treatment

  • Indicated for treatment of uncomplicated malaria due to P falciparum, P malariae, P ovale, and P vivax
  • 800 mg (620 mg base) PO, then 400 mg (310 mg base) PO at 6 hr, 24 hr, and 48 hr after initial dose
  • Weight-based dosing: 13 mg/kg (10 mg/kg base), not to exceed 800 mg (620 mg base) followed by 6.5 mg/kg (5 mg/kg base), not to exceed 400 mg (310 mg base), PO at 6 hr, 24 hr, and 48 hr after initial dose  

Rheumatoid Arthritis

Indicated for treatment of acute and chronic rheumatoid arthritis

400-600 mg/day (310-465 mg base/day) PO as a qDay or in BID

When a good response is obtained, reduce dosage by 50% and continue maintenance dose of 200-400 mg/day (155-310 mg base/day) PO as a qDay or in BID; not exceed 600 mg or 6.5 mg/kg (5 mg/kg base) per day, whichever is lower, as the incidence of retinopathy has been reported to be higher when this maintenance dose is exceeded

Use corticosteroids and salicylates in conjunction with hydroxychloroquine; gradually decrease dosage or eliminate after a maintenance dose has been achieved

Systemic Lupus Erythematosus

Indicated for treatment of chronic discoid lupus erythematosus and systemic lupus erythematosus

200-400 mg/day (155-310 mg base/day) PO as a single daily dose or in two divided doses

Doses >400 mg/day are not recommended

Incidence of retinopathy has been reported to be higher when this maintenance dose is exceeded

Coronavirus Disease 2019 (COVID-19) (Off-label)

Data available as of June 15, 2020

FDA revoked the emergency use authorization (EUA) that hydroxychloroquine donated to the Strategic National Stockpile to be used to treat certain hospitalized patients with COVID-19 when a clinical trial was unavailable, or participation in a clinical trial was not feasible

Based on its ongoing analysis of the EUA and emerging scientific data, the FDA determined that hydroxychloroquine is unlikely to be effective in treating COVID-19 for the authorized uses in the EUA; additionally, in light of ongoing serious cardiac adverse events and other potential serious side effects, the known and potential benefits of hydroxychloroquine no longer outweigh the known and potential risks for the EUA

While additional clinical trials may continue to evaluate potential benefit, the FDA determined the EUA was no longer appropriate

For more information, see the FDA news release: FDA Revokes Emergency Use Authorization for Chloroquine and Hydroxychloroquine

Additional Medscape COVID-19 references are available

Porphyria Cutanea Tarda (Off-label)

100-200 mg (77.5-155 mg base) PO 2-3 times/wk

Dosing Considerations

Before prescribing hydroxychloroquine for treatment or prophylaxis of malaria, consult the Centers for Disease Control and Prevention (CDC) Malaria website (link http://www.cdc.gov/malaria)

Limitations of use in malaria

  • Not recommended for treatment of complicated malaria
  • Not effective against chloroquine or hydroxychloroquine-resistant strains of Plasmodium species
  • Not recommended for treatment of malaria acquired in geographic areas where chloroquine resistance occurs or when the Plasmodium species has not been identified
  • Not recommended for malaria prophylaxis in geographic areas where chloroquine resistance occurs
  • Does not prevent relapses of P vivax or P ovale because it is not active against the hypnozoite forms of these parasites
  • For radical cure of P vivax and P ovale infections, concomitant therapy with an 8-aminoquinoline compound is necessary

Dosage Forms & Strengths

tablet

  • 200mg

Malaria

Prophylaxis

  • Indicated for prophylaxis of malaria in geographic areas where chloroquine resistance is not reported.
  • 6.5 mg/kg (5 mg/kg base) PO once weekly, not to exceed 400 mg (310 mg base), starting 2 weeks before exposure and continued for 4 weeks after leaving the endemic area  

Acute treatment

  • Indicated for treatment of uncomplicated malaria due to P falciparum, P malariae, P ovale, and P vivax
  • 13 mg/kg (10 mg/kg base), not to exceed 800 mg (620 mg base) followed by 6.5 mg/kg (5 mg/kg base), not to exceed 400 mg (310 mg base), PO at 6 hr, 24 hr, and 48 hr after initial dose  

Porphyria Cutanea Tarda (Off-label)

Dosing schedules not well established in children

A case report describes 3 mg/kg PO twice weekly over 14 months reported as safe and effective in a child aged 4 yr

Dosing Considerations

Before to prescribing hydroxychloroquine for treatment or prophylaxis of malaria, consult the Centers for Disease Control and Prevention (CDC) Malaria website (link http://www.cdc.gov/malaria)

Limitations of use in malaria

  • Not recommended for treatment of complicated malaria
  • Not effective against chloroquine or hydroxychloroquine-resistant strains of Plasmodium species
  • Not recommended for treatment of malaria acquired in geographic areas where chloroquine resistance occurs or when the Plasmodium species has not been identified
  • Not recommended for malaria prophylaxis in geographic areas where chloroquine resistance occurs
  • Does not prevent relapses of P vivax or P ovale because it is not active against the hypnozoite forms of these parasites
  • For radical cure of P vivax and P ovale infections, concomitant therapy with an 8-aminoquinoline compound is necessary
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Interactions

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            Adverse Effects

            Frequency Not Defined

            Blood and lymphatic system disorders: Bone marrow failure, anemia, aplastic anemia, agranulocytosis, leukopenia, and thrombocytopenia; hemolysis reported in individuals with glucose-6-phosphate dehydrogenase (G-6-PD) deficiency

            Cardiac disorders: Cardiomyopathy, QT interval prolongation, and ventricular arrhythmias and torsade de pointes

            Ear and labyrinth disorders: Vertigo, tinnitus, nystagmus, nerve deafness, deafness

            Eye disorders: Irreversible retinopathy with retinal pigmentation changes (bull’s eye appearance), visual field defects (paracentral scotomas) and visual disturbances (visual acuity), maculopathies (macular degeneration), decreased dark adaptation, color vision abnormalities, corneal changes (edema and opacities) including corneal deposition of drug with or without accompanying symptoms (halo around lights, photophobia, blurred vision)

            Gastrointestinal disorders: Nausea, vomiting, diarrhea, abdominal pain

            General disorders and administration site conditions: Fatigue

            Hepatobiliary disorders: Liver function tests abnormal, hepatic failure acute

            Immune system disorders: Urticaria, angioedema, bronchospasm

            Metabolism and nutrition disorders: Decreased appetite, hypoglycemia, porphyria, weight decreased

            Musculoskeletal and connective tissue disorders: Sensorimotor disorder, skeletal muscle myopathy or neuromyopathy leading to progressive weakness and atrophy of proximal muscle groups, depression of tendon reflexes and abnormal nerve conduction

            Nervous system disorders: Headache, dizziness, seizure, ataxia and extrapyramidal disorders such as dystonia, dyskinesia, tremor

            Psychiatric disorders: Affect/emotional lability, nervousness, irritability, nightmares, psychosis, suicidal behavior

            Skin and subcutaneous tissue disorders: Rash, pruritus, pigmentation disorders in skin and mucous membranes, hair color changes, alopecia; dermatitis bullous eruptions including erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms (DRESS syndrome), photosensitivity, dermatitis exfoliative, acute generalized exanthematous pustulosis (AGEP)

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            Warnings

            Contraindications

            Hypersensitivity to 4-aminoquinoline derivatives

            Cautions

            Not effective against chloroquine-resistant strains of P falciparum

            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

            Rare suicidal behavior has been reported

            May cause severe hypoglycemia including loss of consciousness that could be life-threatening in patients treated with or without antidiabetic medications; check blood glucose and adjust treatment if necessary

            Exercise caution in patients with hepatic disease or alcoholism or in conjunction with known hepatotoxic drugs; a dosage reduction may be necessary in patients with hepatic or renal disease, as well as in those taking medicines known to affect these organs

            Antimalarial compounds should be used with caution in patients with hepatic disease or alcoholism or in conjunction with known hepatotoxic drugs; perform periodic blood cell counts if patients are given prolonged therapy; if any severe blood disorder (eg, aplastic anemia, agranulocytosis, leukopenia, thrombocytopenia) appears which is not attributable to the disease under treatment, consider discontinuing treatment

            Use with caution in patients having glucose-6-phosphate dehydrogenase (G-6-PD) deficiency

            Dermatologic reactions may occur

            Cardiac effects

            • Postmarketing cases of life-threatening and fatal cardiomyopathy have been reported
            • May present with AV block, pulmonary hypertension, sick sinus syndrome or with cardiac complications
            • ECG findings include atrioventricular, right or left bundle branch block
            • Monitor for signs and symptoms of cardiomyopathy is advised
            • If cardiotoxicity is suspected, promptly discontinue treatment

            Ocular toxicity

            • Irreversible retinal damage observed; significant risk factors for retinal damage include daily doses of hydroxychloroquine sulfate >6.5 mg/kg (5 mg/kg base) of actual body weight, durations of use >5 years, subnormal glomerular filtration, use of some concomitant drug products such as tamoxifen citrate and concurrent macular disease
            • Recommend an ocular exam within first year of therapy; baseline exam should include: 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)
            • In individuals of Asian descent, retinal toxicity may first be noticed outside macula; in patients of Asian descent, perform visual field testing in central 24 degrees instead of central 10 degrees
            • Discontinue if ocular toxicity is suspected and closely observe any retinal changes (and visual disturbances) even after cessation of therapy

            Drug interaction overview

            • Avoid use with other drugs that have potential to prolong QT interval; hydroxychloroquine prolongs QT interval; ventricular arrhythmias and torsades de pointes reported in patients taking hydroxychloroquine
            • Concomitant use with hydroxychloroquine and digoxin therapy may result in increased serum digoxin levels: closely monitor serum digoxin levels in patients receiving combined therapy
            • May enhance the effects of a hypoglycemic treatment, a decrease in doses of insulin or antidiabetic drugs may be required
            • Coadministration with other antimalarials known to lower the convulsion threshold (eg, mefloquine) may increase the risk of convulsions
            • Activity of antiepileptic drugs might be impaired if coadministered with hydroxychloroquine
            • An increased plasma cyclosporine level was reported when cyclosporine and hydroxychloroquine were coadministered
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            Pregnancy & Lactation

            Pregnancy

            • Human pregnancies resulting in live births have been reported in the literature and no increase in the rate of birth defects has been demonstrated
            • Embryonic deaths and malformations of anophthalmia and microphthalmia in the offspring have been reported when pregnant rats received large doses of chloroquine

            Lactation

            • Exercise caution when administering hydroxychloroquine to nursing women
            • When administered to nursing women, hydroxychloroquine is excreted in human milk and it is known that infants are extremely sensitive to the toxic effects of 4-aminoquinolines

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Malaria

            • Precise mechanism of action against Plasmodium is unknown
            • Hydroxychloroquine, like chloroquine, is a weak base and may exert its effect by concentrating in the acid vesicles of the parasite and by inhibiting polymerization of heme
            • It can also inhibit certain enzymes by its interaction with DNA

            Rheumatoid arthritis and systemic lupus erythematosus

            • Mechanisms underlying the anti-inflammatory and immunomodulatory effects of hydroxychloroquine are unknown

            Absorption

            Peak plasma concentration: 129.6 ng/mL (single 200-mg dose)

            Peak plasma time: 3.26 hr (single 200-mg dose); 3-4 hr (chronic PO administration)

            Metabolism

            Metabolites: Desethylhydroxychloroquine, desethylchloroquine

            Elimination

            Half-life: 40-50 days

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            Administration

            Oral Administration

            Take with a meal or a glass of milk

            Do not crush or split tablets

            Storage

            Dispense in a tight, light-resistant container

            Keep out of the reach of children

            Store at room temperature (20-25ºC [68-77ºF]), allows excursions at 15-30ºC (59-86ºF)

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
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            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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