Chloroquine

Schizontocidal by interference with plasmodial DNA; killing of erythrocytic forms in all stages of development; no effect on tissue forms in the liver (malaria tertiana and quartana).

Anti-inflammatory by stabilizing lysosomal membrane, inhibiting chemotaxis of neutrophils and eosinophils.

Immunosuppressive, inhibition of DNA synthesis as well as formation of UV-induced thymidine dimers, accumulation in pigment-forming cells (cause of ophthalmological complications), inhibition of skin UV absorption.

In cutaneous lupus erythematosus, chloroquine leads to the reduction of HLA-DR+/CD1a+ cells in lesional skin!

• Malaria therapy: Initially 0.6 g chloroquin base/day p.o., then after 6, 24 and 48 hours 0.3 g chloroquin base each.
• Malaria prophylaxis: 0.3 g every 7 days during the risk of infection and 4-8 weeks afterwards.
• Lupus erythematosus and rheumatoid arthritis: 250 mg/day, reduction depending on the findings.
• Reticular erythematous mucinosis: 250 mg/day for 4 weeks, 125 mg/day for another 4 weeks, then further creeping.
• Porphyria cutanea tarda: 125 mg 3 times/week.

Remember! Before starting therapy, determine the glucose-6-phosphate dehydrogenase level. Women of childbearing age must have a negative pregnancy test before therapy and effective contraception protection must be provided during and up to 3 months after therapy (risk-benefit ratio in malaria prophylaxis and therapy, since malaria infection itself causes damage to the fetus)!

Accommodation disorders, irreversible retinopathy, blood count disorders, gastrointestinal disorders, allergic reactions, exacerbation of a psoriasis vulgaris or porphyria cutanea tarda, headache, dizziness, myopathy, leukopenia, agranulocytosis, stomach upset, headache, dizziness, exanthema, bluish discoloration of the skin, nail pigmentation, hearing loss, corneal damage.

Chloroquine can cause life-threatening torsade de poin arrhythmias.

Notice! With long-term therapy the risk of retinopathy is increased with 100 g Chloroquinbase and more, corresponding to a 2-year therapy with 250 mg/day. Therefore, regular ophthalmological check-ups in 3-month intervals are recommended!

Chloroquine is a substrate of CYP2C8 and CYPP3A4 and a medium strength inhibitor of CYP2D6. Leflunomide inhibits CYP2C8 via its teriflunomide, which allows chloroquine plasma levels to rise.

Notice! Patient information: The intake should take place after meals!

Significant interactions of chloroquine