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Hydroxychloroquine

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Hydroxychloroquine
Plaquenil; mostly prescribed generically

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Summary
Common uses
Rheumatoid arthritis0, Systemic lupus erythematosus0, Discoid and subacute cutaneous lupus0, Sjögren's syndrome0, Malaria treatment and prophylaxis (chloroquine-sensitive areas)0
Pharmacy
Starting dose
200-400 mg PO daily; dose by actual body weight ≤5 mg/kg/d to reduce retinopathy risk (AAO 2016 guideline)
Preparations
200 mg tablets; 100 mg/5 mL suspension
US FDA Max
400 mg/d typical maintenance; weight-adjusted ceiling per ophthalmology guidance
Pharmacology
Routes
Oral
Onset
Rheumatologic effect at 6-12 weeks
Duration
Weeks (long half-life)
Half-life
~40 days (terminal; reflects extensive tissue distribution)[1]
Bioavailability
70-75% (oral)[1]
Pregnancy
Long-considered safe in pregnancy for lupus and other rheumatologic indications; benefits typically outweigh.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Hydroxychloroquine accumulates in lysosomes (lysosomotropic weak base), raising lysosomal pH and impairing endolysosomal antigen processing and TLR7/9 endosomal signaling; the net effect dampens innate immune activation and reduces autoantibody production in lupus and inflammation in rheumatoid arthritis.0 Retinal toxicity is the dose- and duration-limiting adverse effect (bull's eye maculopathy with photoreceptor damage); the 2016 American Academy of Ophthalmology guideline established the ≤5 mg/kg actual-body-weight ceiling and baseline + annual screening starting at year 5[1]. QT prolongation and rare cardiomyopathy are recognized cardiac risks. The 2020 COVID-19 controversy is documented separately; HCQ does not have established benefit in COVID-19 and was eventually withdrawn from active recommendation.

References

  1. 1.0 1.1 1.2 FDA Prescribing Information, Plaquenil (hydroxychloroquine sulfate), Sanofi-Aventis, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/009768s048lbl.pdf