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Hydroxychloroquine
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800 mg (620 mg base) PO, then 400 mg (310 mg base)/dose PO at 6, 24, and 48 hours after the initial dose for a total dose of 2,000 mg (1,550 mg base). For P. vivax or P. ovale, add primaquine phosphate or tafenoquine.[41806] [68403] [68436]
13 mg (10 mg base)/kg/dose [Max: 800 mg (620 mg base)/dose] PO, then 6.5 mg (5 mg base)/kg/dose [Max: 400 mg (310 mg base)/dose] PO at 6, 24, and 48 hours after the initial dose for a total dose of 32.5 mg (25 mg base)/kg [Max: 2,000 mg (1,550 mg base)]. For P. vivax or P. ovale, add primaquine phosphate or tafenoquine (16 years and older).[41806] [68403] [68436]
13 mg (10 mg base)/kg/dose [Max: 800 mg (620 mg base)/dose] PO, then 6.5 mg (5 mg base)/kg/dose [Max: 400 mg (310 mg base)/dose] PO at 6, 24, and 48 hours after the initial dose for a total dose of 32.5 mg (25 mg base)/kg [Max: 2,000 mg (1,550 mg base)]. For P. vivax or P. ovale, add primaquine phosphate.[41806] [68403]
400 mg (310 mg base)/dose PO once weekly, starting 1 to 2 weeks prior to entry into endemic area and continuing for 4 weeks after leaving the area.[41806] [68402]
6.5 mg (5 mg base)/kg/dose [Max: 400 mg (310 mg base)/dose] PO once weekly, starting 1 to 2 weeks prior to entry into endemic area and continuing for 4 weeks after leaving the area.[41806] [68402] [68436] [70821]
6.5 mg (5 mg base)/kg/dose [Max: 400 mg (310 mg base)/dose] PO once weekly, starting 1 to 2 weeks prior to entry into endemic area and continuing for 4 weeks after leaving the area. Guidelines suggest hydroxychloroquine as an alternative to chloroquine.[68402] [70821]
400 to 600 mg (310 to 465 mg base) PO once daily or in 2 divided doses as monotherapy or part of combination therapy. After a clinical response is obtained, reduce dose to 200mg/day (155 mg base/day), 300 mg/day (232 mg base/day), or 400 mg/day (310 mg base/day) in 1 or 2 divided doses.[41806] [65215] [68436]
200 to 400 mg (155 to 310 mg base) PO once daily or in 2 divided doses.[41806] [68436] Target dose: 5 mg/kg/day. Max: 400 mg/day (310 mg base/day). Individualize dose based on risk for flare and retinal toxicity. Consider tapering dose to 200 mg/day (155 mg base/day) in persons in remission.[70847]
4 to 5 mg (3.1 to 3.8 mg base)/kg/day PO. Target dose: 5 mg/kg/day. Max: 400 mg/day (310 mg base/day). Individualize dose based on risk for flare and retinal toxicity.[65218] [65219] [65220] [69026] [70847]
200 mg (155 mg base) PO once daily or 400 mg (310 mg base) PO once daily or in 2 divided doses.[41806] May add quinacrine if a patient fails monotherapy.[62154] [65216]
200 to 400 mg/day (155 to 310 mg/day base) or 5 mg/kg/day PO.[52522] [65217] [70847] [71743] Doses less than 3 mg/kg/day may not achieve adequate serum concentrations and may be associated with higher flare rates.[71743]
200 to 400 mg (155 to 310 mg base) PO once daily or in 2 divided doses.[61732]
200 to 400 mg (155 to 310 mg base) PO once daily.[69854]
200 mg (155 mg base) PO once or twice daily or 400 mg (310 mg base) PO once daily.[68344] [68345]
5 mg (3.875 mg base)/kg/dose (Max: 400 mg/dose or 310 mg base/dose) PO once daily.[68313] [68314] [68320]
200 to 600 mg (155 to 465 mg base) PO once daily plus doxycycline for at least 18 months.[70594]
5 to 6.5 mg (3.875 to 5 mg base)/kg/dose (Max: 600 mg (465 mg base) PO once daily for 6 to 12 weeks.[71725] [71726] [71727] [71728] [71729] [71731]
5 to 6.5 mg (3.875 to 5 mg base)/kg/dose (Max: 600 mg (465 mg base) PO once daily for 6 to 12 weeks.[71725] [71726] [71727] [71728] [71729] [71731]
800 mg/dose (620 mg base/dose) PO for malaria up to a total of 2,000 mg (1,550 mg base) PO in 48 hours; 400 mg/week (310 mg base/week) PO for malaria prophylaxis; 600 mg/day (465 mg base/day) PO for rheumatoid arthritis; 400 mg/day (310 mg base/day) PO for systemic lupus erythematosus and chronic discoid lupus erythematosus
800 mg/dose (620 mg base/dose) PO for malaria up to a total of 2,000 mg (1,550 mg base) PO in 48 hours; 400 mg/week (310 mg base/week) PO for malaria prophylaxis; 600 mg/day (465 mg base/day) PO for rheumatoid arthritis; 400 mg/day (310 mg base/day) PO for systemic lupus erythematosus and chronic discoid lupus erythematosus
weighing 31 kg or more: 13 mg/kg/dose (10 mg base/kg/dose) [Max: 800 mg (620 mg base)] PO for malaria up to a total of 32.5 mg/kg (25 mg base/kg) [Max: 2,000 mg (1,550 mg base)] PO in 48 hours; 6.5 mg/kg/week (5 mg base/kg/week) [Max: 400 mg/week (310 mg base/week)] PO for malaria prophylaxis.
weighing less than 31 kg: 13 mg/kg/dose (10 mg base/kg/dose) PO for malaria up to a total of 32.5 mg/kg (25 mg base/kg) PO in 48 hours has been used off-label; 6.5 mg/kg/week (5 mg base/kg/week) PO for malaria prophylaxis has been used off-label.
weighing 31 kg or more: 13 mg/kg/dose (10 mg base/kg/dose) [Max: 800 mg (620 mg base)] PO for malaria up to a total of 32.5 mg/kg (25 mg base/kg) [Max: 2,000 mg (1,550 mg base)] PO in 48 hours; 6.5 mg/kg/week (5 mg base/kg/week) [Max: 400 mg/week (310 mg base/week)] PO for malaria prophylaxis.
weighing less than 31 kg: 13 mg/kg/dose (10 mg base/kg/dose) PO for malaria up to a total of 32.5 mg/kg (25 mg base/kg) PO in 48 hours has been used off-label; 6.5 mg/kg/week (5 mg base/kg/week) PO for malaria prophylaxis has been used off-label.
13 mg/kg/dose (10 mg base/kg/dose) PO for malaria up to a total of 32.5 mg/kg (25 mg base/kg) PO in 48 hours has been used off-label; 6.5 mg/kg/week (5 mg base/kg/week) PO for malaria prophylaxis has been used off-label.
Safety and efficacy have not been established.
A dosage reduction may be necessary in patients with hepatic disease or those taking concomitant medications known to affect the liver. However, no specific dosage adjustment guidelines are available for patients with hepatic impairment.[41806]
A dosage adjustment is not required in patients with renal impairment. However, a dosage reduction may be necessary in patients with renal disease or those taking concomitant medications known to affect the kidney. No specific dosage adjustment guidelines are available for patients with renal impairment.[41806]
† Off-label indicationHydroxychloroquine is an oral disease-modifying antirheumatic drug (DMARD) used to treat rheumatoid arthritis and systemic lupus erythematosus. It also is used to prevent and treat malaria. Irreversible retinal damage has been observed with use, and cases of life-threatening and fatal cardiomyopathy, including ventricular arrhythmias and torsade de pointes, have been reported.[41806]
For storage information, see the specific product information within the How Supplied section.
Extemporaneous 25 mg/mL oral suspension (using tablets)†
NOTE: Extemporaneous compounding is not FDA-approved.[41806]
Hydroxychloroquine can cause ocular toxicity including irreversible retinal damage related to cumulative dose and treatment duration. A baseline ocular exam should be performed within the first year of hydroxychloroquine treatment. This baseline exam should include best corrected distance visual acuity (BCVA), an automated threshold visual field (VF) of the central 10 degrees (with retesting if an abnormality is noted), and spectral domain ocular coherence tomography (SD-OCT). Annual exams are recommended for patients at higher risk of retinal damage. For patients without significant risk factors, annual exams may be deferred until 5 years of treatment. In Asian patients, retinal toxicity may first be noticed outside the macula; therefore, visual field testing should be performed in the central 24 degrees instead of the central 10 degrees. Discontinue hydroxychloroquine if ocular toxicity is suspected and monitor the patient closely for ocular disease (i.e., retinal changes) and visual disturbance which may progress even after discontinuation of therapy. Other ocular adverse events include retinopathy, retinal pigment changes (bull's eye appearance), visual field defects/visual impairment (paracentral scotomata), macular degeneration, decreased dark adaptation, corneal edema, and corneal opacification.[41806]
Serious adverse reactions reported with hydroxychloroquine include Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), drug reaction with eosinophilia and systemic symptoms (DRESS), and acute generalized exanthematous pustulosis (AGEP). Monitor for serious skin reactions, especially in individuals receiving a medication that may also induce dermatitis. Advise individuals to seek medical attention promptly if they experience signs and symptoms of serious rash or skin reactions such as blisters on the skin, eyes, lips or in the mouth, itching or burning, with or without fever. Discontinue hydroxychloroquine if these severe reactions occur. Other allergic or dermatologic reactions reported with hydroxychloroquine include alopecia, hair color changes (hair discoloration), rash, pruritus, photosensitivity, hyperpigmentation (skin discoloration), exfoliative dermatitis, erythema multiforme, urticaria, angioedema, and bronchospasm.[41806]
Hydroxychloroquine may precipitate a severe attack of psoriasis that may be associated with pyrexia and hyperleukocytosis. Monitor patients with known psoriasis for a flare-up of the psoriasis.[41806]
Skeletal muscle myopathy or peripheral neuropathy leading to progressive weakness and atrophy of proximal muscle groups, depression of tendon reflexes, and abnormal nerve conduction has been reported. Muscle and nerve biopsies have been associated with curvilinear bodies and muscle fiber atrophy with vacuolar changes. Muscle and nerve biopsies have showed associated phospholipidosis. Drug-induced phospholipidosis may occur in other organ systems. Assess muscle strength and deep tendon reflexes periodically in patients on long-term therapy with hydroxychloroquine. If muscle or nerve toxicity is suspected or demonstrated by tissue biopsy, discontinue hydroxychloroquine therapy.[41806]
Hematological adverse reactions of hydroxychloroquine include myelosuppression (bone marrow suppression), including anemia, aplastic anemia, agranulocytosis, leukopenia, and thrombocytopenia. Hemolysis/hemolytic anemia has been reported in individuals with glucose-6-phosphate dehydrogenase (G-6-PD) deficiency. Monitor blood cell counts periodically if patients are given prolonged hydroxychloroquine therapy. If myelosuppression develops which is not attributable to the disease under treatment occurs, discontinue hydroxychloroquine.[41806]
Sensorineural hearing loss and tinnitus have been reported with hydroxychloroquine or other 4-aminoquinolines.[41806]
Fatal and life-threatening cases of cardiotoxicity, including cardiomyopathy, have been reported in patients treated with hydroxychloroquine. Signs and symptoms of cardiac compromise have occurred during acute and chronic treatment with the drug. Patients may present with ventricular hypertrophy, pulmonary hypertension, and conduction disorders including sick sinus syndrome. ECG findings include AV block or right or left bundle-branch block. In multiple cases, endomyocardial biopsy revealed an association of cardiomyopathy with phospholipidosis in absence of inflammation, infiltration, or necrosis. Drug-induced phospholipidosis may occur with other organs. Chronic toxicity should be considered when conduction disorders or biventricular hypertrophy are diagnosed. If cardiotoxicity is suspected or demonstrated by tissue biopsy, prompt discontinuation of hydroxychloroquine may prevent life-threatening cardiac complications. Additionally, hydroxychloroquine causes QT prolongation. The magnitude of QT prolongation may increase with increasing drug concentrations. Ventricular arrhythmias (i.e., ventricular fibrillation, ventricular tachycardia) and torsade de pointes have been reported in patients taking hydroxychloroquine. Monitor the ECG and cardiac function as indicated during hydroxychloroquine therapy. Cardiac disorders reported with the class of 4-aminoquinoline drugs postmarketing have included cardiomyopathy, heart failure, QT-interval prolongation, ventricular tachycardia, torsade de pointes, AV block, bundle-branch block, sick sinus syndrome, and pulmonary hypertension.[41806]
Adverse gastrointestinal (GI) effects reported with hydroxychloroquine or other 4-aminoquinolines include nausea, vomiting, abdominal pain, diarrhea, and anorexia. These effects are associated with oral administration and can be minimized by taking hydroxychloroquine with food. Abnormal liver function tests and fulminant hepatic failure have also been reported.[41806]
Suicidal behavior, suicidal ideation, and other neuropsychiatric adverse events have been reported in patients treated with hydroxychlorquine. Neuropsychiatric adverse events typically occur within the first month after starting hydroxychloroquine and have been reported in patients with and without prior history of psychiatric disorders. Psychiatric and CNS adverse events reported with hydroxychloroquine or other 4-aminoquinolines include headache, dizziness, affect/emotional lability, irritability, psychosis, nervousness, depression, hallucinations, anxiety, agitation, confusion, delusions, paranoia, mania, sleep disorders (insomnia, night terrors, nightmares), vertigo, nystagmus, ataxia, seizures, and extrapyramidal disorders such as dystonic reaction, dyskinesia, and tremor. Assess the risk and benefit of continued treatment in patients who develop neuropsychiatric reactions, including new or worsening depression, suicidal thoughts or behavior, or mood changes. Given the long half-life of the drug, it may take several weeks for the symptoms to partially or fully abate after stopping hydroxychlorquine.[41806]
Weight loss and fatigue have been reported with the use of hydroxychloroquine or other 4-aminoquinolines.[41806]
Hydroxychloroquine has been shown to cause severe hypoglycemia including loss of consciousness that could be life threatening in patients treated with or without antidiabetic medications. Monitor blood glucose and adjust treatment as necessary in patients presenting with clinical symptoms of hypoglycemia during hydroxychloroquine treatment.[41806]
Hydroxychloroquine may cause nephrotoxicity. Cases of proteinuria with or without a moderate reduction in glomerular filtration rate have been reported with hydroxychloroquine therapy. Renal biopsy revealed phospholipidosis without immune deposits, inflammation, and/or increased cellularity. Phospholipidosis may be considered as a potential cause of renal injury in patients receiving hydroxychloroquine with underlying connective tissue disorders. Drug-induced phospholipidosis may occur in other organ systems. If renal toxicity is suspected or demonstrated by tissue biopsy, discontinue hydroxychloroquine.[41806] [68436]
Use of hydroxychloroquine in individuals with porphyria has been shown to exacerbate porphyria. Additionally, in individuals with porphyria cutanea tarda (PCT), cases of hepatotoxicity have developed after administration of hydroxychloroquine at doses ranging from 200 mg twice weekly to 400 mg daily. For most PCT-related cases, individuals presented with markedly elevated hepatic enzymes [more than 20-times upper limit of normal (ULN)] within days to months of starting hydroxychloroquine. Some of the cases were associated with other risk factors for hepatic injury (e.g., alcohol use, concomitant hepatotoxic medications). Measure liver tests promptly in individuals who report symptoms that may indicate liver injury, such as fatigue, rash, nausea, dark urine, or jaundice. If an individual is found to have an abnormal liver function test (e.g., ALT more than 3-times ULN, total bilirubin greater than 2-times ULN), interrupt treatment with hydroxychloroquine and investigate for the probable cause.[41806] [68584]
The coadministration of certain medications may lead to harm and require avoidance or therapy modification; review all drug interactions prior to concomitant use of other medications.
This medication is contraindicated in patients with a history of hypersensitivity to it or any of its components. Hydroxychloroquine is also contraindicated in individuals with known hypersensitivity to 4-aminoquinoline compounds.[41806]
Irreversible retinal damage was observed in some individuals treated with hydroxychloroquine. Risk factors for retinal damage include hydroxychloroquine dosages of 6.5 mg/kg/day (5 mg/kg/day base) or more of actual body weight, durations of use longer than 5 years, renal impairment, use of concomitant medications such as tamoxifen, and concurrent macular disease. Perform a baseline ocular exam, including best corrected distance visual acuity (BCVA), automated threshold visual field (VF) of the central 10 degrees (with retesting if an abnormality is noted), and spectral domain optical coherence tomography (SD-OCT), within the first year of hydroxychloroquine treatment. In Asian patients, retinal toxicity may first be noticed outside the macula; perform VF testing in the central 24 degrees instead of the central 10 degrees in Asians. For individuals at higher risk of retinal damage, monitoring should include annual examinations which include BCVA, VF, and SD-OCT. For individuals without significant risk factors, annual exams can usually be deferred until 5 years of treatment.[41806]
Avoid use of hydroxychloroquine in people with baseline QT prolongation or who have conditions that may increase the risk of QT prolongation or torsade de pointes, including bradycardia, congenital long QT syndrome, hypocalcemia, hypokalemia, hypomagnesemia, geriatric adults, females, structural abnormalities that interfere with electrical conduction (e.g., cardiomyopathy, coronary artery disease, ischemic heart disease), or in those who have other additional risk factors for QT prolongation or torsade de pointes. The use of other medications that have been associated with QT prolongation or torsade de pointes may further increase risk.[41806] [65180] [67452] [72115] [72116] [72117] [72118] Also avoid hydroxychloroquine in individuals with cardiac disease or a history of ventricular arrhythmias. Correct electrolyte imbalances prior to hydroxychloroquine use.[41806]
A hydroxychloroquine dose reduction may be necessary in individuals with hepatic disease.[41806]
A hydroxychloroquine dose reduction may be necessary in individuals with renal disease. Irreversible retinal damage was observed in some individuals treated with hydroxychloroquine. Risk factors for retinal damage include renal impairment.[41806]
Avoid hydroxychloroquine in individuals with porphyria, as it may exacerbate the condition.[41806]
Avoid hydroxychloroquine in individuals with psoriasis unless the benefit outweighs the possible risk, as it may precipitate a severe exacerbation of the disease.[41806]
Hemolysis has been reported with hydroxychloroquine in individuals with glucose-6-phosphate dehydrogenase deficiency (G6PD deficiency). Monitor for hemolytic anemia as this can occur, particularly in association with other medications that cause hemolysis.[41806]
Advise individuals with a major psychiatric disorder to contact their health care provider promptly if they experience worsening neuropsychiatric symptoms, such as depression, mood changes, or suicidal thoughts or behavior. Suicidal behavior, suicidal ideation, and other neuropsychiatric adverse reactions have been reported with hydroxychloroquine.[41806]
Monitor blood sugar concentrations in individuals with diabetes mellitus or individuals presenting with clinical symptoms suggestive of hypoglycemia who are receiving hydroxychloroquine. Hydroxychloroquine can cause severe, life-threatening hypoglycemia in the presence or absence of antidiabetic medications. Adjust antidiabetic medication as necessary.[41806]
Use cautious dose selection for hydroxychloroquine in geriatric adults, starting with the lowest recommended dose and taking into consideration the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.[41806]
Prolonged clinical experience over decades of use and available data from published epidemiologic and clinical studies with hydroxychloroquine use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Hydroxychloroquine readily crosses the placenta with cord blood levels corresponding to maternal plasma levels. No retinal toxicity, ototoxicity, cardiotoxicity, or growth and developmental abnormalities have been observed in children who were exposed to hydroxychloroquine in utero. Available epidemiologic and clinical studies have methodological limitations including small sample size and study design. There are risks to the mother and fetus associated with untreated or increased maternal disease activity from malaria, rheumatoid arthritis, and systemic lupus erythematosus (SLE) during pregnancy that should be considered. There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to hydroxychloroquine during pregnancy. Encourage patients to register by contacting 1-877-311-8972.[41806] Hydroxychloroquine is considered to be compatible for use during pregnancy in some anti-rheumatic guidelines, and may be continued in pregnancy for maintenance of remission or treatment of a disease flare.[62180] [64661] [64662] Hydroxychloroquine may also be appropriate for pregnancies complicated by lupus.[34349] [34358] Guidelines also recommend hydroxychloroquine as an alternative to chloroquine as a treatment option for acute malaria and for prophylaxis in pregnant women during all trimesters.[68402] [68403] Animal reproductive studies have not been conducted.[41806]
Data regarding the use of hydroxychloroquine during breast-feeding report that hydroxychloroquine is present in human milk at low levels. No adverse reactions have been reported in breastfed infants. No retinal toxicity, ototoxicity, cardiotoxicity, or growth and developmental abnormalities have been observed in children who were exposed to hydroxychloroquine through breastmilk. There is no information on the effect of hydroxychloroquine on milk production.[41806] Hydroxychloroquine is considered to be compatible for use during breast-feeding in some anti-rheumatic guidelines, and may be continued during lactation for maintenance of remission or treatment of a disease flare.[62180] [64661] [64662] During lactation studies, breast milk concentrations ranged from 10.6 to 1,392 mcg/L and breast-fed infants would likely receive 0.2 mg/kg or less of hydroxychloroquine.[48476] [48477] [48478] [48479] In infants monitored for up to at least 1 year of age, careful follow-up found no adverse effects on growth, vision, or hearing.[48474] [48475] The developmental and health benefits of breast-feeding should be considered along with the mother's clinical need for the medication and any potential adverse effects on the breastfed child from hydroxychloroquine exposure or from the underlying maternal condition.[41806]
Hydroxychloroquine, a 4-aminoquinoline antimalarial, is a weak base and may exert its antimalarial effect by concentrating in the acid vesicles of the plasmodia and by inhibiting the polymerization of heme. It can also inhibit certain enzymes by its interaction with DNA. Organisms with reduced susceptibilities to chloroquine also show reduced susceptibilities to hydroxychloroquine.[41806]
Although the mechanisms underlying the antiinflammatory and immunomodulatory effects of hydroxychloroquine in the treatment of rheumatoid arthritis, chronic discoid lupus erythematous, and systemic lupus erythematosus are not fully known, several possible mechanisms of action have been proposed. It is unclear if these mechanisms work similarly for rheumatic and autoimmune diseases. Potential mechanisms include reduced cytokine production, inhibition of immune effector cells, inhibition of platelet function, protection of the cell surface from external disturbances, competitive binding to nucleic acid ligands or toll-like receptors (TLRs), interference with lysosomal function, reduction of leakage of lysosomal enzymes, and interference with endosomal NADPH oxidase (NOX).[41806] [61727] [61728] [61729]
Revision Date: 09/29/2025, 03:24:13 PMHydroxychloroquine is administered orally. It is approximately 50% bound to plasma proteins and is widely distributed into body tissues, with high concentrations in the bone marrow, liver, kidneys, lungs, adrenal gland, and pituitary gland. Hydroxychloroquine has a high affinity for melanin and thus is concentrated in the choroid and ciliary body of the eye, which may account for the retinal toxicity. Cellular concentrations have been shown to be higher in mononuclear cells than in polymorphonuclear leukocytes.[41806][61731][61732] Hydroxychloroquine is primarily metabolized by CYP2C8, CYP3A4, and CYP2D6 as well as by flavin-containing monooxygenase 1 (FMO-1) and monoamine oxidase A (MAO-A). Three metabolites have been identified, including the major metabolite, desethylhydroxychloroquine (DHCQ), as well as desethylchloroquine (DCQ) and bidesethylhydroxychloroquine (BDCQ). Renal clearance of unchanged drug ranges from 16% to 30% and does not change with chronic dosing. The half-life of a single 200 mg oral dose is approximately 40 days. After chronic administration, the absorption half-life is approximately 3 to 4 hours and the terminal half-life in whole blood ranges from 40 to 50 days. In rheumatoid arthritis (RA) patients, the effective half-life is likely to be shorter.[41806]
Affected cytochrome P450 isoenzymes and drug transporters: CYP2C8, CYP2D6, CYP3A4, P-gp, MATE1, MATE2-K
In vitro data suggest that hydroxychloroquine is metabolized primarily by CYP2C8 and CYP3A4, and to a much lesser extent, by CYP2D6.[65236][65239] It has also been shown to be an inhibitor of the drug transporter P-glycoprotein (P-gp).[65237] An in vitro study suggests that hydroxychloroquine also has the potential to inhibit CYP2D6, CYP3A4, and multidrug and toxin extrusion transporters MATE1 and MATE2-K.[41806] In vitro data suggest that hydroxychloroquine does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, OATP1B1, OATP1B3, OAT1, OAT3, OCT1, and OCT2. In vitro data suggest that hydroxychloroquine has no significant potential to induce CYP1A2, CYP2B6, and CYP3A4.[68436]
The mean absolute oral bioavailability of hydroxychloroquine is 79% under fasting conditions. In rheumatoid arthritis (RA) patients, there is a large variability in absorption (30% to 100%) with mean concentrations significantly higher in patients with less disease activity. After a singe 200 mg dose to healthy volunteers, the peak whole blood concentration (Cmax) was 129.6 ng/mL (plasma Cmax was 50.3 ng/mL) and the time to reach peak blood concentration (Tmax) was 3.3 hours (plasma Tmax was 3.7 hours). Peak blood concentrations of the metabolites were observed at the same time as peak hydroxychloroquine concentrations. Steady state concentrations are achieved by 6 weeks after oral administration of 400 mg daily in RA patients. At steady state, the whole blood concentration of hydroxychloroquine is dose proportional over a range of 200 to 400 mg daily in patients with RA and lupus.[41806]
After a single 155 mg intravenous infusion of hydroxychloroquine in healthy volunteers, peak blood concentrations (Cmax) ranged from 1,161 ng/mL to 2,436 ng/mL (mean 1,918 ng/mL). The Cmax range after a single 310 mg infusion was 2,290 ng/mL and 4,211 ng/mL; thus, indicating linear pharmacokinetics.[41806]
Prolonged clinical experience over decades of use and available data from published epidemiologic and clinical studies with hydroxychloroquine use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Hydroxychloroquine readily crosses the placenta with cord blood levels corresponding to maternal plasma levels. No retinal toxicity, ototoxicity, cardiotoxicity, or growth and developmental abnormalities have been observed in children who were exposed to hydroxychloroquine in utero. Available epidemiologic and clinical studies have methodological limitations including small sample size and study design. There are risks to the mother and fetus associated with untreated or increased maternal disease activity from malaria, rheumatoid arthritis, and systemic lupus erythematosus (SLE) during pregnancy that should be considered. There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to hydroxychloroquine during pregnancy. Encourage patients to register by contacting 1-877-311-8972.[41806] Hydroxychloroquine is considered to be compatible for use during pregnancy in some anti-rheumatic guidelines, and may be continued in pregnancy for maintenance of remission or treatment of a disease flare.[62180] [64661] [64662] Hydroxychloroquine may also be appropriate for pregnancies complicated by lupus.[34349] [34358] Guidelines also recommend hydroxychloroquine as an alternative to chloroquine as a treatment option for acute malaria and for prophylaxis in pregnant women during all trimesters.[68402] [68403] Animal reproductive studies have not been conducted.[41806]
Data regarding the use of hydroxychloroquine during breast-feeding report that hydroxychloroquine is present in human milk at low levels. No adverse reactions have been reported in breastfed infants. No retinal toxicity, ototoxicity, cardiotoxicity, or growth and developmental abnormalities have been observed in children who were exposed to hydroxychloroquine through breastmilk. There is no information on the effect of hydroxychloroquine on milk production.[41806] Hydroxychloroquine is considered to be compatible for use during breast-feeding in some anti-rheumatic guidelines, and may be continued during lactation for maintenance of remission or treatment of a disease flare.[62180] [64661] [64662] During lactation studies, breast milk concentrations ranged from 10.6 to 1,392 mcg/L and breast-fed infants would likely receive 0.2 mg/kg or less of hydroxychloroquine.[48476] [48477] [48478] [48479] In infants monitored for up to at least 1 year of age, careful follow-up found no adverse effects on growth, vision, or hearing.[48474] [48475] The developmental and health benefits of breast-feeding should be considered along with the mother's clinical need for the medication and any potential adverse effects on the breastfed child from hydroxychloroquine exposure or from the underlying maternal condition.[41806]
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