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Pronunciation: high-drox-ee-KLOR-oh-kwin SULL-fate
Class: 4–aminoquinoline compound, Antirheumatic
- Tablets 200 mg (equivalent to 155 mg base)
May interfere with parasitic nucleoprotein (DNA/RNA) synthesis and parasite growth or cause lysis of parasite or infected erythrocytes. In rheumatoid arthritis, may suppress formation of antigens responsible for symptom-producing hypersensitivity reactions.
Hydroxychloroquine is readily absorbed from the GI tract. T max is 1 to 3 h.
Hydroxychloroquine concentrates in the liver, spleen, kidney, heart, lungs, and brain.
It is partially hepatic to active de-ethylated metabolites.
Approximately 50% of the unchanged drug is excreted in urine. Elimination in urine is very slow and may persist for months or years after discontinuation. Renal excretion is increased by acidification and decreased by alkalinization of the urine. The plasma t ½ is approximately 32 days.
Special PopulationsRenal Function Impairment
Use with caution.Hepatic Function Impairment
Use with caution.Children
Use with caution. A number of fatalities have been reported following ingestion of chloroquines.
Indications and Usage
Prophylaxis and treatment of acute attacks of malaria caused by Plasmodium vivax , Plasmodium malariae , Plasmodium ovale , and susceptible strains of Plasmodium falciparum . Treatment of chronic discoid and systemic lupus erythematosus (SLE) and acute or chronic rheumatoid arthritis in patients not responding to other therapies.
Retinal or visual field changes caused by any 4-aminoquinoline compound; hypersensitivity to 4-aminoquinoline compounds; long-term therapy in children.
Dosage and AdministrationAcute Attack of Malaria
PO 800 mg (620 mg of base) followed by 400 mg in 6 to 8 h and 400 mg on each of 2 consecutive days. Alternatively, a single 800 mg dose (620 mg of base) has proved effective.Children
PO 10 mg/kg (base), up to adult dose; followed by 5 mg/kg (base), not exceeding 310 mg of base, 6 h after first dose; followed in 18 h after the second dose by 5 mg/kg (base). A fourth dose of 5 mg/kg (base) is given 24 h after third dose.Lupus Erythematosus
PO Initially 400 mg/day or twice daily. For prolonged therapy, reduce to 200 to 400 mg/day (155 to 310 mg of base).Rheumatoid Arthritis
Adults Initial dose
PO 400 to 600 mg/day (310 to 465 mg of base) with food or milk.Maintenance
PO After good response (usually 4 to 12 wk), reduce dosage 50% and continue at 200 to 400 mg/day (155 to 310 mg of base).Suppression of Malaria
Begin 2 wk prior to exposure; continue for 8 wk after leaving area.Adults
PO 400 mg (310 mg of base) weekly on same day each week.Children
PO 5 mg/kg of base weekly on same day each week, up to max 400 mg (310 mg of base).
- Administer prescribed dose with food or milk to minimize GI side effects.
- Disease-modifying antirheumatic drugs, glucocorticoids, salicylates, NSAIDs, and analgesics may be continued during treatment of rheumatoid arthritis with hydroxychloroquine.
Store tablets at controlled room temperature (up to 86°F).
Drug InteractionsBeta-blockers (eg, metoprolol)
Plasma levels and CV effects of certain beta-blockers may be increased.Cimetidine
Pharmacologic effect of hydroxychloroquine may be increased.Cyclosporine
Serum levels may be increased by hydroxychloroquine, increasing the risk of nephrotoxicity.Digoxin
May increase serum digoxin levels.Hepatotoxic drugs
May increase potential for hepatotoxicity.Magnesium sulfate
Absorption of hydroxychloroquine may be reduced, decreasing the pharmacologic effect; antacid activity of magnesium sulfate may be decreased.Mefloquine
Coadministration may increase risk of seizures.
Laboratory Test Interactions
None well documented.
Hypotension; ECG changes; cardiomyopathy (rare).
Headache; irritability; nervousness; emotional changes; nightmares; psychosis; dizziness; vertigo; nystagmus; nerve deafness; convulsions; ataxia.
Bleaching of hair; alopecia; pruritus; skin and mucosal pigmentation; skin eruptions; exacerbation of psoriasis.
Disturbance of accommodation with blurred vision; transient corneal edema; corneal opacities; decreased corneal sensitivity; retinal edema; retinal atrophy; abnormal retinal pigmentation; loss of retinal reflexes; optic disc pallor and atrophy; scotoma; retinopathy; tinnitus.
Anorexia; nausea; vomiting; diarrhea; abdominal cramps.
Aplastic anemia; agranulocytosis; leukopenia; thrombocytopenia; hemolysis in G-6-PD deficiency; exacerbation of porphyria.
Immunoblastic lymphadenopathy; extraocular muscle palsies; skeletal muscle weakness; absent or hypoactive deep tendon reflexes.
MonitorBaseline disease activity
Document baseline disease state activity in patient being treated for rheumatoid arthritis or lupus erythematosus. Reassess periodically to document response to therapy.CBC
Ensure CBC with differential and platelet count is evaluated before starting therapy and periodically thereafter during prolonged therapy.Muscular weakness
Ensure patient on long term therapy is periodically evaluated for development of muscular weakness.
Category C . Avoid use in pregnancy, except in suppression of malaria when benefit outweighs the possible hazard.
Excreted in breast milk.
Deaths have occurred following accidental ingestion of relatively small doses. Do not exceed recommended doses for children with malaria. Not indicated for juvenile rheumatoid arthritis.
Use with caution.
Use with caution. May increase risk of hepatotoxicity.
Special Risk Patients
May exacerbate psoriasis, porphyria, or other dermatitis; may cause hemolysis in patients with glucose-6-phosphate dehydrogenase (G-6-PD) deficiency.
May increase risk of hepatotoxicity.
If weakness occurs, discontinue.
Irreversible retinal damage with long-term hydroxychloroquine therapy has been observed. Retinal changes and visual disturbances may progress after cessation of therapy. Ensure that ophthalmologic exam is obtained before starting therapy and periodically (eg, every 3 mo) thereafter during prolonged therapy.
Headache, drowsiness, visual disturbances, CV collapse, convulsions, respiratory and cardiac arrest, bradycardia, ventricular fibrillation.
- Advise patient to take each dose with milk or food to minimize stomach upset.
- Advise patient to continue other medications for arthritis or lupus as recommended by health care provider.
- Advise patient with arthritis that it may take several months of treatment before max benefit is seen. Advise patient to notify health care provider if symptoms have not improved after 6 mo of treatment or if symptoms appear to be getting worse.
- Instruct patient to take medication once weekly for malaria prophylaxis, beginning 2 wk prior to arrival in malaria-infected area, while in the malaria-infected area, and for 8 wk after leaving the malaria-infected area.
- Advise patient that protective clothing, insect repellants, and bednets are important components of malaria prophylaxis.
- Advise patient to immediately report any of the following to health care provider: any visual changes; muscle weakness; ringing in the ears or hearing loss; fever; sore throat; unusual bleeding or bruising; unusual pigmentation (eg, blue-black) of the skin; bleaching or loss of hair; mood or mental changes.
- Advise patient to notify health care provider if persistent or bothersome nausea, vomiting, diarrhea, stomach pain, or other symptoms develop.
- Advise patient that drug may cause dizziness and to use caution while driving or performing other tasks requiring mental alertness, coordination, or physical dexterity until tolerance is determined.
- Advise patient medication may cause photosensitivity (sensitivity to sunlight) and to avoid unnecessary exposure to sunlight or tanning lamps, and to use sunscreens and wear protective clothing to avoid photosensitivity reactions.
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