chloroquine (Rx)

Brand and Other Names:Aralen, Chloroquine phosphate
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 250mg
  • 500mg

Malaria

Prevention: 500 mg (300 mg base) PO once/week

Non-chloroquine-resistant

  • 1 g (600 mg base) PO, THEN
  • 500 mg (300 mg base) PO 6-8 hours later, THEN
  • 500 mg (300 mg base) PO at 24 hours & 48 hours after initial dose

Amebiasis, Extraintestinal

1 g (600 mg base) PO qDay for 2 days, THEN

500 mg (300 mg base) qDay for 14-21 days

Porphyria Cutanea Tarda (Off-label)

125-250 mg (75-150 mg base) PO twice weekly

Glioblastoma (Orphan)

Orphan designation for treatment of glioblastoma multiforme

Sponsor

  • DualTpharma B.V.; Boschstraat 111-D01; 6211 A W Maastricht; Netherlands

Dosage Forms & Strengths

tablet

  • 250mg
  • 500mg

Malaria

Prophylaxis: 5 mg/kg PO q1Week  

Treatment

  • 1st dose: 10 mg/kg PO x1 dose
  • 6 hours after 1st dose: 5 mg/kg PO qDay x2 days

Porphyria Cutanea Tarda (Off-label)

Dosing schedules not well established in children

Case reports describe dosage regimens that are effective yet tolerated, such as 12.5 mg PO twice weekly over 2 yr in a child aged 4-6 yr, and 100 mg PO twice weekly over 5 months in a child aged 12 yr; mg/kg dosing not reported

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Interactions

Interaction Checker

and chloroquine

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined

            Abnormal ECG

            Prolonged QT interval

            Amnesia

            Pruritus

            Diarrhea,

            Loss of appetite

            Nausea

            Stomach cramps

            Vomiting

            Methemoglobinemia (rare)

            Muscle weakness

            Retinopathy

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            Warnings

            Black Box Warnings

            Physicians should completely familiarize themselves with the complete contents of the package insert before prescribing chloroquine phosphate

            Contraindications

            Hypersensitivity to chloroquine, 4-aminoquinolones

            Psoriasis, porphyria, retinal or visual field changes

            Cautions

            For prevention, may use proguanil concomitantly

            Shown to cause severe hypoglycemia including loss of consciousness that could be life-threatening in patients treated with or without antidiabetic medications; patients should be warned about risk of hypoglycemia and associated clinical signs and symptoms; patients presenting with clinical symptoms suggestive of hypoglycemia during treatment with chloroquine should have blood glucose level checked and treatment reviewed as necessary

            Not effective in most areas; CDC recommends mefloquine or atovaquone/proguanil - check CDC traveler information for specific recommendations for region

            May cause hemolysis in glucose-6 phosphate dehydrogenase (G-6-PD) deficiency; blood monitoring may be needed as hemolytic anemia may occur, in particular in association with other drugs that cause hemolysis

            Monitor CBC periodically with prolonged therapy

            Caution with history of auditory damage

            Caution with hepatic disease, alcoholism, and coadministration with other hepatotoxic drugs

            May provoke seizures in patients with history of epilepsy

            Antacids and kaolin reduce chloroquine absorption; separate administration by at least 4 hr

            Irreversible retinal damage observed in some patients; significant risk factors for retinal damage include daily doses of chloroquine phosphate > 2.3 mg/kg of actual body weight, durations of use greater than five years, subnormal glomerular filtration, use of some concomitant drug products such as tamoxifen citrate, and concurrent macular disease

            A baseline ophthalmological examination should be performed within the first year of initiating therapy; for individuals with significant risk factors, monitoring should include annual examinations; discontinue if ocular toxicity is suspected; patient should be closely observed given that retinal changes (and visual disturbances) may progress even after cessation of therapy

            In individuals of Asian descent, retinal toxicity may first be noticed outside macula; it is recommended that visual field testing be performed in visual field of central 24 degrees instead of central 10 degrees

            May exacerbate heart failure

            Not effective against chloroquine- or hydroxychloroquine-resistant strains of Plasmodium species; information regarding geographic areas where resistance to chloroquine occurs, is available at the Centers for Disease Control and Prevention (www.cdc.gov/malaria)

            Does not treat hypnozoite liver stage forms of Plasmodium and will therefore not prevent relapses of malaria due to P. vivax or P. ovale; additional treatment with an anti-malarial agent active against these forms, such as an 8-aminoquinoline, is required for the treatment of infections with P. vivax and P. ovale

            Cases of cardiomyopathy resulting in cardiac failure, in some cases with fatal outcome, reported during long term therapy at high doses; monitor for signs and symptoms of cardiomyopathy and discontinue chloroquine if cardiomyopathy develops; chronic toxicity should be considered when conduction disorders (bundle branch block / atrio-ventricular heart block) diagnosed; if cardiotoxicity suspected, prompt therapy discontinuation may prevent life-threatening complications

            QT interval prolongation, torsades de pointes, and ventricular arrhythmias reported; risk is greater if chloroquine is administered at high doses; fatal cases reported; use with caution in patients with cardiac disease, a history of ventricular arrhythmias, uncorrected hypokalemia and/or hypomagnesemia, or bradycardia (<50 bpm), and during concomitant administration with QT interval prolonging agents due to potential for QT interval prolongation

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            Pregnancy & Lactation

            Pregnancy

            There are no adequate and well-controlled studies evaluating the safety and efficacy of chloroquine in pregnant women; usage during pregnancy should be avoided except in prophylaxis or treatment of malaria when benefit outweighs potential risk to fetus

            Lactation

            Because of the potential for serious adverse reactions in nursing infants from chloroquine, a decision should be made whether to discontinue nursing or to discontinue drug, taking into account potential clinical benefit of drug to mother

            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

            Active against erythrocytic forms of Plasmodium vivax & P. malariae and most strains of Plasmodium falciparum

            Precise mechanism not known

            Absorption

            Bioavailability: ~89%

            Peak plasma time: 1-2 hr

            Distribution

            Distributed widely in body tissues (eg, eyes, heart, kidneys, liver, lungs) where retention prolonged; crosses placenta; enters breast milk

            Metabolism

            Partially in liver

            Elimination

            Half-life: 3-5 days

            Excretion: urine (~70% as unchanged drug); acidification of urine increases elimination

            Small amounts may be present in urine months following discontinuation of therapy

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            Formulary

            FormularyPatient Discounts

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            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.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            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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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.