Hydroxychloroquine

Indication

It is indicated for the treatment of uncomplicated malaria due to Plasmodium fatciparum, Plasmodium malariae, Plasmodium ovale and Plasmodium vivax; and for the prophylaxis of malaria in geographic area where chloroquine resistance is not reported. It is also indicated in the treatment of rheumatoid...read more

Limitations of Use in Malaria: It is not recommended for the treatment of complicated malaria. It is not effective against chloroquine or hydroxychloroquine-resistant strains of Plasmodium. It is not recommended for the treatment of malaria acquired in geographic areas where chloroquine resistance o...read more

Dosage and Administration

The action of hydroxychloroquine is cumulative and may require weeks to months to achieve the maximum therap­eutic effect. HCQShin film-coated tablets cannot be divi­ded, therefore they should not be used to treat patients who weigh less than 31 kg. Take with a meal or a glass of milk.

Prophylaxis of Malaria:

Adult: 400 mg once weekly on the same day of each week starting 2 weeks prior to exposure and continued for 4 weeks after leaving the endemic area.

Weight-based dosing in adults and pediatric patients: 6.5 mg/kg, not to exceed 400 mg, once weekly on the same day of the week starting 2 weeks prior to exposure and continued for 4 weeks after leaving the endemic area.

Treatment of Uncomplicated Malaria:

Adult: 800 mg followed by 400 mg at 6 hours, 24 hours and 48 hours after the initial dose (total 2,000 mg hy­droxychloroquine sulfate).

Weight based dosage in adults and pediatric patients: 13 mg/kg, not to exceed 800 mg followed by 6.5 mg/kg, not to exceed 400 mg, at 6 hours, 24 hours and 48 hours after the initial dose.

For radical cure of P. vivax and P. malariae infections, concomitant therapy with an 8-aminoquinoline compound is necessary.

Rheumatoid Arthritis:

Adult: Initially 400 to 600 mg daily in single or divided dose. (Temporary reduction of the initial dosage may require in some patients.) When good response is obtained, continued at maintenance level of200 to 400 mg daily in single or divided dose. Do not exceed 600 mg or 6.5 mg/kg per day. Treatme...read more

Lupus Erythematosus

Adult: 200 to 400 mg daily in single or divided dose. Doses above 400 mg a day are not recommended.

Composition

Each film-coated tablet contains:

Hydroxychloroquine Sulfate USP ... 200 mg.

Description

Hydroxychloroquine Sulfate is a synthetic derivative of quinolyl with chemotherapeutic and antibiotic properties. Chemically, it is (±)-2-[4]-[(7-Chloro-4-quinolyl)amino] pentyl]ethylamino] ethanol sulfate (I: 1) (salt). Its molecular formula is C18H26ClN3O.H2SO4 and molecular weight is 433.95.

Clinical Pharmacology

Hydroxychloroquine Sulfate is an aminoquinoline like chloroquine but its mechanism is unknown. It may inhibit hemozoin biocrystallization, which facilitates the aggregation of cytotoxic heme. Free cytotoxic heme accumulates in parasites, causing death. It acts against erythrocytic Plasmodium parasit...read more

Pharmacokinetics

Hydroxychloroquine is almost completely and rapidly absorbed after oral administration and has large distribution volume. About 50% of the Hydroxychloroquine is bound to plasma proteins. It is metabolized in the liver into three active metabolites: desethylchloroquine (DCQ), desethyl­ hydroxychloroq...read more

Contraindication

It is contraindicated in patients with known hypersensitivity to 4-aminoquinoline compounds, children under 6 years of age (increased risk of overdose) and pre-existing retinopathy of eye.

Precautions

Use with caution in patients with G6PD deficiency, psoriasis, alcoholism, severe gastrointestinal, neurological or blood disorders and in those with a sensitivity to quinine. Dose adjustment is necessary in severely compromised hepatic or renal function.

Adverse Effects

Common adverse effects are abdominal pain, nausea, diarrhea, vomiting, skin rash, pruritus, anorexia, headache and blurring of vision (reversible).

Other adverse effects reported are vertigo, tinnitus, urticaria, angioedema, bronchospasm, hypoglycaemia, bone marrow depression, anaemia, aplastic anaemia, agranulocytosis, leukopenia, thrombocytopenia, retinopathy (at very high dose), hypoglycaemia, hemolysis in patients with G6PD deficiency, pote...read more

Overdose

Overdose with 4-aminoquinolines is dangerous particularly in infants, as little as 1 - 2 g having proved fatal. Symptoms of toxic symptoms may occur within 30 minutes and include headache, drowsiness, visual disturbances, cardiovascular collapse, convulsions, hypokalaemia, rhythm and conduction diso...read more

Drug Interaction

Digoxin: Increased serum digoxin levels.

Insulin or Antidiabetic drugs: enhanced the effects of a hypoglycemic treatment.

Drugs that prolong QT interval and other arrhythmogenic drugs: Increased risk of inducing ventricular arrhythmias Cyclosporine: Increased plasma cyclosporine level.

Other anti-malarials: Both Hydroxychloroquine and other anti-malarial (e.g mefloquine) can lower the convulsive threshold, thus may increase the risk of convulsions. So, the activity of antiepileptic drugs may be impaired when administered with anti-malarials.

Praziquantel: Chloroquine has been reported to reduce the bioavailability of praziquantel.

Antacids and kaolin: Antacids and kaolin can reduce absorption of hydroxychloroquine; an interval of at least 4 hours between intake of these agents and hydroxychloroquine should be observed.

Methotrexate: may increase the incidence of adverse effects. Cimetidine: Cimetidine can inhibit the metabolism of chloroquine, increasing its plasma level.

Ampicillin: Chloroquine significantly reduced the bioavailability of ampicillin.

Storage

Store below 30°C in cool, dry place. Protect from light and moisture. Keep out of reach and sight of children.

Presentation

10 x 10's Blisters.