Hydroxychloroquine Compounded

Hydroxychloroquine is an aminoquinoline/antimalarial agent used to treat Lupus, Rheumatoid Arthritis, and Malaria. It has off-label uses for dermatomyositis, porphyria cutanea tarda, primary Sjögren syndrome, Q fever, sarcoidosis, and most recently, COVID-19. With commercial dosage forms in short supply, compounding pharmacies can make hydroxychloroquine in a strength and dosage form that is appropriate for you.

🔬 Mechanism of Action

Hydroxychloroquine's mechanism of action is not fully understood, however, it has been shown to increase intracellular pH and inhibit lysosomal activity in immune cells, which is key in reducing T cell activation, differentiation, and expression of costimulatory proteins and cytokines. Furthermore, it alters the pH of endosomes and interrupts binding between toll-like receptors and their RNA/DNA ligand, suppressing TLR signaling. In the cytoplasm, it can interfere with interactions between cytosolic DNA and the nucleic acid sensory cyclic GMP-AMP synthase — cumulatively reducing pro-inflammatory signaling and cytokine production.

📊 Administration & Dosing

• Systemic Lupus / Rheumatoid Arthritis: 200–400 mg daily as a single dose or in 2 divided doses. Do not exceed >5 mg/kg/day using actual body weight.
• Malaria Treatment: 800 mg once, followed by 400 mg at 6, 24, and 48 hours after initial dose.
• Malaria Chemoprophylaxis: 400 mg once weekly on the same day; begin 1–2 weeks before travel and continue for 4 weeks after leaving the malarious area.

⚠️ Drug Interactions

Hydroxychloroquine can interact with many medications. Consult your physician if you are taking artemether, dapsone, lumefantrine, or mefloquine.

📋 Talk to Your Doctor If You Have

Gastrointestinal disorders, hepatic impairment, porphyria, psoriasis, or renal impairment.

🚨 Adverse Effects — Tell Your Doctor If You Experience

🤰 Pregnancy & Breastfeeding

Hydroxychloroquine does not appear to pose significant risk to a fetus at lower doses. The CDC has stated that the malarial prophylactic dose of 400 mg/week is safe. At higher doses for prolonged periods, there is increased fetal risk, though the magnitude is unknown. Daily amounts should be taken cautiously in breastfeeding women because of the slow elimination rate and potential for toxic accumulation in the infant.

📚 References

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2. Centers for Disease Control and Prevention (CDC). Guidelines for treatment of malaria in the United States. Updated April 1, 2019.
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5. Hydroxychloroquine: from Lexicomp.com. Accessed 4/6/2020.
6. Plaquenil (hydroxychloroquine) [prescribing information]. St. Michael, Barbados: Concordia Pharmaceuticals Inc; September 2019.
7. Singh JA, et al. 2015 American College of Rheumatology guideline for the treatment of rheumatoid arthritis. Arthritis Rheumatol. 2016;68(1):1–26.
8. Zhou D, et al. Journal of Antimicrobial Chemotherapy. 2020 Mar.