Inhibits protein synthesis in susceptible organisms by inhibiting DNA and RNA polymerase.
Active against chloroquine-sensitive strains of: Plasmodium falciparum, Plasmodium malariae, aPlasmodium ovale, and Plasmodium vivax.
Absorption: Highly variable (31–100%) following oral administation.
Distribution: Widely distributed; high concentrations in RBCs; crosses the placenta; excreted into breast milk.
Metabolism and Excretion: Partially metabolized by the liver to active metabolites; partially excreted unchanged by the kidneys.
Half-life: 40 days.
TIME/ACTION PROFILE (blood levels)
Use Cautiously in:
CV: HF, TORSADE DE POINTES, heart block, QT interval prolongation
Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), ERYTHEMA MULTIFORME, STEVENS-JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS, acute generalized exanthematous pustulosis, alopecia, hair color changes, hyperpigmentation, photosensitivity, pruritus, rash, urticaria
EENT: corneal deposits, nystagmus, retinopathy, tinnitus, vertigo, visual disturbances
GI: HEPATOTOXICITY, abdominal pain, anorexia, diarrhea, ↑ liver enzymes, nausea, vomiting
Hemat: AGRANULOCYTOSIS, APLASTIC ANEMIA, leukopenia, thrombocytopenia
Metabolic: ↓ weight
Neuro: ataxia, dyskinesia, dystonia, neuromyopathy, peripheral neuritis, tremor, SEIZURES, SUICIDAL THOUGHTS/BEHAVIORS, aggressiveness, anxiety, dizziness, fatigue, headache, irritability, nightmares, personality changes, psychoses
Resp: PULMONARY HYPERTENSION, bronchospasm
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
200 mg hydroxychloroquine sulfate = 155 mg of hydroxychloroquine base
PO (Adults): Prophylaxis– 400 mg sulfate (310 mg base) once weekly; start 2 wk prior to entering malarious area; continue for 4 wk after leaving area. Treatment– 800 mg sulfate (620 mg base), then 400 mg sulfate (310 mg base) at 6 hr, 24 hr, and 48 hr after initial dose.
PO (Children ≥31 kg): Prophylaxis– 6.5 mg/kg sulfate (5 mg/kg base) (not to exceed 400 mg sulfate [310 mg base]) once weekly; start 2 wk prior to entering malarious area; continue for 4 wk after leaving area. Treatment– 13 mg/kg sulfate (10 mg/kg base) (not to exceed 800 mg sulfate [620 mg base]) initially, then 6.5 mg/kg sulfate (5 mg/kg base) (not to exceed 400 mg sulfate [310 mg base]) at 6 hr, 24 hr, and 48 hr after initial dose.
PO (Adults): 400–600 mg sulfate (310–465 mg base) per day in 1–2 divided doses; once adequate response obtained, may ↓ dose to maintenance dose of 200–400 mg sulfate (155–310 mg base) per day in 1–2 divided doses.
PO (Adults): 200–400 mg sulfate (155–310 mg base) per day in 1–2 divided doses.
Tablets: 200 mg sulfate (155 mg base)
Assess deep tendon reflexes periodically to determine muscle weakness. Therapy may be discontinued should this occur.
Lab Test Considerations:
Monitor CBC and platelet count periodically throughout therapy. May cause decreased RBC, WBC, and platelet counts. If severe decreases occur that are not related to the disease process, hydroxychloroquine should be discontinued.
Administer with milk or meals to minimize GI distress.
Review methods of minimizing exposure to mosquitoes with patients receiving hydroxychloroquine prophylactically (use repellent, wear long-sleeved shirt and long trousers, use screen or netting).
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