Chloroquine (7-chloride-4-[4'-diethyleamino-1'-methyle-butylamino]-chinoline; molecular weight 319.89; chloroquine diphosphate molecular weight 515.9) is a white, crystalline, bitter-tasting powder. It is easily soluble in water and nearly unsoluble in ethanol and chloroform. Hydroxychloroquine is a derivative of chloroquine. As the latter does not significantly differ from chloroquine with respect to mode of action, pharmacokinetics, toxicology, side effects, and indications, both medicaments are discussed together.
One hundred fifty milligrams of the pure chloroquine base corresponds to approximately 250 mg of the commercially available chloroquine diphosphate, and 155 mg of hydroxychloroquine base corresponds to 200 mg of hydroxychloroquine sulfate. The conversion factor from chloroquine diphosphate to the base is approximately 0.6, and from the base to the salt is approximately 1.6. The factors for hydroxychloroquine are 0.77 and 1.29, respectively. The dosages in the text relate to the clinically relevant dosages of the salts.
Quinacrine (Atabrine, mepacrine, atebrin) (6-chloro-9-[1-methyl-4-diethyl-amine]butylamino-2-methoxyacridine) is available as the dihydrochloride. It is a
Table 26.1. Indications for chloroquine and hydroxychloroquine for the treatment of noninfectious diseases (according to Arneal et al. 2002, Barthel et al. 1996, Dereure and Guilhou 2002, Erhan et al. 2002, Khoury et al. 2003, Nguyen et al. 2002, Reeves et al. 2004, Wallace 1996, Ziering et al. 1993)
Strong indications for effectivity
Indication for effectivity in individual cases
Effectivity may evolve
Case records with positive effects
Porphyria cutanea tarda Sarcoidosis (of the skin)
Hyperlipidemia (mainly during corticosteroid therapy)
Thromboembolic prophylaxis in case of antiphospholipid antibodies or intraopera-tively
Skin manifestations of dermatomyositis
Primary Sjögren's syndrome
Polymorphous light eruption
REM syndrome Lymphocytic infiltration Interstitial or alveolear lung diseases in children Hypercalcemia Autoimmune thrombocyto-penia (with steroids)
Nonrheumatoid forms of inflammatory arthritis Prevention of acute GvHD
Prospective controlled double-blind studies Prospective controlled double-blind studies Clinical studies Controlled clinical studies, partially double blind Controlled clinical studies
Controlled clinical studies
Large series of patients
Controlled double-blind study Controlled double-blind study (only laboratory improvement) Prospective double-blind study
Large series of patients Large series of patients Large series of patients
Large series of patients Patient series
Case reports Open clinical studies Large series of patients Open study Open study
Controlled clinical studies Large series of patients
Sideroblastic anemia, chronic ulcerative stomatitis, epidermolysis bullosa, erythema anlare centrifugum, granuloma anulare, granulomatosis disciformis, light urticaria, Lyme disease, morphea, cutaneous mucinoses, panniculitis (Pfeiffer-Weber-Christian), pemphigus, polymyal-gia rheumatica, pseudolymphoma, pseudopelade Broq, chronic sinusitis, urticarial vasculitis, Well's syndrome, autoimmune urticaria, necrobiosis lipoidica
GvHD, graft versus host disease; REM, reticular erythematous mucinosis.
bright yellow, odorless, bitter crystalline, water-soluble powder that contains an approximately 80% quinacrine base. Tablets contain 100 mg of the dihydrochloride.
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