Generic Aralen (Chloroquine)

Aralen (Chloroquine) has selective toxicity to plasmodia infection in the erythrocyte phase. It binds to nucleic acids, interrupting DNA synthesis. It contributes to the death of parasites that cause malaria, as well as tissue forms of amoeba. It has an immunosuppressive and anti-inflammatory effect in autoimmune processes. It has an antiarrhythmic effect reducing the myocardium excitability.

Indications

Aralen is used for the prevention and treatment of malaria, systemic lupus erythematosus, porphyria, amoebiasis. This drug is used as a part of the combination therapy of systemic lupus erythematosus, scleroderma, rheumatoid arthritis, and photodermatosis.

Contraindications

The most common contraindications of Aralen are:

  • inhibition of cerebral circulation;
  • renal and hepatic insufficiency;
  • psoriasis;
  • neutropenia;
  • cardiac muscle rhythm disturbances;
  • individual intolerance;
  • children’s age up to 12 months.

With caution:

  • epilepsy;
  • glucose-6-phosphate dehydrogenase deficiency;
  • retinopathy;
  • myasthenia gravis;
  • diseases of the gastrointestinal tract;
  • hypersensitivity.

Pregnancy and lactation

According to FDA, this drug belongs to Category C. Use with caution during pregnancy and lactation in cases when the intended benefit outweighs the risk to the fetus and newborn.

Dosage and administration

Use in children

Oral administration, depending on age:

  • 1-6 years old: 1st day – 125 mg, 2-3 days – 50 mg each;
  • 6-10 years old: 1st day – 250 mg, 2-3 days – 125 mg each;
  • 10-15 years old: 1st day – 500 mg, 2-3 days – 250 mg each.
  • For the treatment of extraintestinal amebiasis: 6 mg/kg per day for 2 weeks, followed by a halving of the dose.

Adults

  • Oral administration, for the prevention of malaria – 500 mg 2 times a week, then 500 mg 1 time on the same day of the week.
  • The treatment of malaria – 1 g on the 1st day once, then after 6-8 hours – 500 mg, on the 2nd and 3rd day 750 mg at a time.
  • The treatment of amoebiasis: oral, 500 mg 3 times a day for a week, then 250 mg 3 times a day for the second week, after which – 750 mg 2 times a week for 2-6 months.
  • Rheumatoid arthritis: 259 mg 2 times a day for a week. Then 250 mg daily for 12 months.
  • Systemic lupus erythematosus: 250-500 mg once a day.
  • Treatment of photodermatosis: 250 mg per day for a week, then 500-750 mg per week.
  • The highest daily dose: 1.5 g.
  • The highest single dose: 1 g.

Side effects

  • Central and peripheral nervous system: dizziness, headache, seizures, sleep disorders, acute psychosis.
  • Hematopoietic system: thrombocytopenia, agranulocytosis, leukopenia.
  • Cardiovascular system: arterial hypotension, toxic myocarditis.
  • Digestive system: anorexia, gastralgia, nausea, vomiting.
  • Musculoskeletal system: arthralgia, muscle weakness, myalgia, muscle spasms.
  • Dermatological reactions: itching, hyperpigmentation of the mucous membranes and skin, dermatitis, hair discoloration (depigmentation).
  • Sensory organs: ringing in the ears, hearing impairment, damage to the retina, clouding of the cornea, visual impairment.
  • Allergic reactions.

Overdose

The symptoms of an overdose are nausea and vomiting, a sharp decrease in blood pressure, quickly passing into a coma and apnea.

The treatment is symptomatic.

Interaction

  • Aralen increases glycosidic intoxication of cardiac glycosides.
  • With simultaneous use with penicillamine, gold preparations, levamisole, phenylbutazone and cytostatics, neurotoxicity increases.
  • Ethanol increases the hepatotoxicity of Aralen.
  • With simultaneous use with glucocorticoids, the risk of developing cardiomyopathy and myopathy increases.
  • Cimetidine increases the concentration of chloroquine in blood plasma.
  • Antacids reduce Aralen absorption.
  • Monoamine oxidase inhibitors increase toxicity.