Hydroxychloroquine Sulphate
Indications
Hydroxychloroquine Sulphate is used for:
Acute and chronic rheumatoid arthritis, Systemic Lupus Erythematosus (SLE), Malaria
Adult Dose
Oral
Malaria
Acute treatment
800 mg PO, then 400 mg PO 6-8 hours later, then 400 mg PO at 24 and 48 hours
Prophylaxis
400 mg PO weekly, starting 2 weeks before exposure and continued for 4 weeks after departure from area
Rheumatoid Arthritis
400-600 mg PO daily for 4-12 weeks; maintenance: 200-400 mg PO daily
Systemic Lupus Erythematosus
400 mg PO once or twice daily; maintenance: 200-400 mg PO daily
Hepatic impairment: Estimation of plasma hydroxychloroquine levels to be undertaken in patients with severely compromised function and dosage adjusted accordingly.
Child Dose
Malaria
Acute treatment
13 mg/kg base PO, then 6.5 mg/kg base PO 6 hr later, then 6.5 mg/kg base PO at 24 and 48 hours; not to exceed 400 mg/day base
Prophylaxis
6.5 mg/kg base (not to exceed 400 mg [310 mg base]) PO weekly, starting 2 weeks before exposure and continued for 4 weeks after departure from area
Renal Dose
Renal impairment: Estimation of plasma hydroxychloroquine levels to be undertaken in patients with severely compromised function and dosage adjusted accordingly.
Administration
Should be taken with food.
Contra Indications
The presence of retinal or visual field changes attributable to any 4-aminoquinoline compound, patients with known hypersensitivity to 4-aminoquinoline compounds, long term therapy in children.
Precautions
Impaired liver or renal function, severe GI disorders, porphyria, psoriasis, neurological disorders especially a history of epilepsy, myasthenia gravis, G6PD deficiency, pregnancy, lactation. Monitor CBC in patients receiving prolonged therapy. Perform baseline and periodic 6-mth eye exams, test periodically for muscle weakness.
Lactation: Drug is concentrated in breast milk (American Academy of Pediatrics committee states that it is compatible with nursing)
Pregnancy-Lactation
Interactions
Cimetidine may increase serum levels of hydroxychloroquine. Its absorption may be decreased by kaolin or Mg trisilicate. Avoid digoxin and alcohol. Increased risk of ventricular arrhythmias when used with halofantrine. Concurrent use with mefloquine may increase the risk of convulsions.
Adverse Effects
Side effects of Hydroxychloroquine Sulphate :
Retinopathy, hair loss, photosensitivity, tinnitus, myopathy (long-term therapy). Psychosis, seizures, leucopenia and rarely aplastic anaemia, hepatitis, GI upsets, dizziness, hypokalaemia, headache, pruritus, urticaria, difficulty in visual accommodation. Loss of hair, bleaching of hair pigment, bluish-black pigmentation of the mucous membranes and skin, photosensitivity, tinnitus, reduced hearing, nerve deafness, neuromyopathy, and myopathy, including cardiomyopathy.
Mechanism of Action
Hydroxychloroquine is a 4-aminoquinoline antimalarial with actions similar to those of chloroquine but is mainly used in the treatment of SLE and rheumatoid arthritis. It interferes with digestive vacuole function within susceptible malarial parasites by increasing pH and interrupting with lysosomal degradation of Hb thus impeding normal cell function of sensitive parasites.