pharmacopeia
GET
/api/v1/drug/hydroxychloroquine
2D structure
2-[4-[(7-chloroquinolin-4-yl)amino]pentyl-ethylamino]ethanol
SMILES CCN(CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl)CCO
InChIKey XXSMGPRMXLTPCZ-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Malaria Hydroxychloroquine is a 4-aminoquinoline antimalarial [see Microbiology (12.4) ] and antirheumatic agent. Rheumatoid Arthritis, Systemic Lupus Erythematosus and Chronic Discoid Lupus Erythematosus The mechanisms underlying the anti-inflammatory and immunomodulatory effects of hydroxychloroquine sulfate tablets in the treatment of rheumatoid arthritis, chronic discoid lupus erythematosus and systemic lupus erythematosus are not fully known.

Enzyme

Indications

Sourced from openFDA
  • Hydroxychloroquine sulfate tablets are an antimalarial and antirheumatic indicated for the: Treatment of uncomplicated malaria due to Plasmodium falciparum, Plasmodium malariae, Plasmodium ovale, and Plasmodium vivax in adult and pediatric patients. ( 1.1 ) Prophylaxis of malaria in geographic areas where chloroquine resistance is not reported in adult and pediatric patients.ICD-10: B54

Contraindications

Sourced from openFDA
  • Hydroxychloroquine sulfate tablets are contraindicated in patients with known hypersensitivity to 4-aminoquinoline compounds.contraindicated

Dosage & administration

Sourced from openFDA

Malaria in Adult and Pediatric Patients ( 2.2 ): ● Prophylaxis: Begin weekly doses 2 weeks prior to travel to the endemic area, continue weekly doses while in the endemic area, and continue the weekly doses for 4 weeks after leaving the endemic area: - Adults: 400 mg once a week - Pediatric patients ≥ 31 kg: 6.5 mg/kg up to 400 mg, once a week ● Treatment of Uncomplicated Malaria: See Full Prescribing Information (FPI) for complete dosing information. Rheumatoid Arthritis in Adults ( 2.3 ): Initial dosage: 400 mg to 600 mg daily Chronic dosage: 200 mg once daily or 400 mg once daily (or in two divided doses) Systemic Lupus Erythematosus in Adults ( 2.4 ): 200 mg once daily or 400 mg once daily (or in two divided doses) Chronic Discoid Lupus Erythematosus in Adults ( 2.5 ): 200 mg once daily or 400 mg once daily (or in two divided doses) 2.1 Important Administration Instructions Administer hydroxychloroquine sulfate tablets orally with food or milk. Do not crush or divide the tablets. 2.2 Dosage for Malaria in Adult and Pediatric Patients Hydroxychloroquine sulfate tablets are not recommended in pediatric patients less than 31 kg because the lowest available strength (200 mg) exceeds the recommended dose for these patients and it cannot be divided. Prophylaxis Treatment must start 2 weeks before travel to an endemic area. Advise the patient to take the prophylaxis dosage once a week, staring 2 weeks prior to travel to the endemic area, on the same day every week, continuing the same weekly dose while in the endemic area, and for 4 weeks after leaving the endemic area.

Warnings & precautions

Sourced from openFDA

Cardiomyopathy and Ventricular Arrhythmias : Fatal or life-threatening cardiomyopathy and ventricular arrhythmias were reported. ( 5.1 ) Retinal Toxicity : Irreversible retinal damage is related to cumulative dosage and treatment duration. Baseline retinal exam and exams during treatment are recommended. ( 5.2 ) Serious Skin Reactions : Stevens Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms, acute generalized exanthematous pustulosis have been reported. ( 5.3 ) Worsening of Psoriasis : Avoid in patients with psoriasis. ( 5.4 ) Risks Associated with Use in Porphyria : Avoid in patients with porphyria. Hepatotoxicity was reported in patients with porphyria cutanea tarda ( 5.5 ). Hematologic Toxicity : Discontinue if myelosuppression occurs. ( 5.6 ) Renal Toxicity : Consider phospholipidosis as a possible cause of renal injury in patients with underlying connective tissue disorders. Discontinue hydroxychloroquine sulfate tablets if renal toxicity is suspected or demonstrated by tissue biopsy in any organ system. ( 5.1 , 5.8 , 5.11 ) 5.1 Cardiomypathy and Ventricular Arrhythmias Fatal and life-threatening cases of cardiotoxicity, including cardiomyopathy, have been reported in patients treated with hydroxychloroquine sulfate tablets. Signs and symptoms of cardiac compromise have occurred during acute and chronic hydroxychloroquine sulfate tablets treatment. In multiple cases, endomyocardial biopsy showed association of the cardiomyopathy with phospholipidosis in the absence of inflammation, infiltration, or necrosis.

Adverse reactions

Sourced from openFDA

The following adverse reactions are described in greater detail in other sections: Cardiomyopathy and Ventricular Arrhythmias [see Warnings and Precautions (5.1) ] Retinal Toxicity [see Warnings and Precautions (5.2) ] Serious Skin Reactions [see Warnings and Precautions (5.3) ] Worsening of Psoriasis [see Warnings and Precautions (5.4) ] Risks Associated with Use in Porphyria [see Warnings and Precautions (5.5) ] Hematologic Toxicity [see Warnings and Precautions (5.6) ] Hemolytic Anemia Associated with G6PD [see Warnings and Precautions (5.7) ] Skeletal Muscle Myopathy or Neuropathy [see Warnings and Precautions (5.8) ] Neuropsychiatric Reactions Including Suicidality [see Warnings and Precautions (5.9) ] Hypoglycemia [see Warnings and Precautions (5.10) ] Renal Toxicity [see Warnings and Precautions (5.11) ] The following adverse reactions have been identified during post-approval use of 4-aminoquinoline drugs, including hydroxychloroquine sulfate tablets.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to hydroxychloroquine sulfate tablets during pregnancy. Encourage patients to register by contacting 1-877-311-8972. Risk Summary Prolonged clinical experience over decades of use and available data from published epidemiologic and clinical studies with hydroxychloroquine sulfate tablets use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal, or fetal outcomes (see Data) . There are risks to the mother and fetus associated with untreated or increased disease activity from malaria, rheumatoid arthritis, and systemic lupus erythematosus in pregnancy (see Clinical Considerations) . Animal reproduction studies were not conducted with hydroxychloroquine. The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the US general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Pharmacokinetics

Sourced from openFDA
Metabolism
Following oral administration, the whole blood concentration of hydroxychloroquine at steady state is dose proportional over a dose range from 200 mg daily to 400 mg daily of hydroxychloroquine sulfate tablets in rheumatoid arthritis and lupus patients. Absorption Following a single 200 mg oral dose of hydroxychloroquine sulfate tablets to healthy male volunteers, whole blood hydroxychloroquine Cmax was 129.6 ng/mL (plasma C max was 50.3 ng/mL) with T max of 3.3 hours (plasma T max 3.7 hours).

Overdosage

Sourced from openFDA

Hydroxychloroquine sulfate tablets overdosage symptoms have an onset within 1–3 hours of ingestion. The following have been reported with hydroxychloroquine sulfate tablets overdosage: Cardiovascular toxicity, including QRS or QTc prolongation, ventricular tachycardia, ventricular fibrillation, torsade de pointes, atrioventricular block, cardiac arrest and death. Life-threatening hypotension is common. Severe hypokalemia secondary to an intracellular shift is common in severe toxicity. Central nervous system (CNS) depression, seizures, visual disturbances, transient blindness, and coma may occur. Gastrointestinal decontamination procedures warrant consideration in patients that present within the first hour post-ingestion. If the level of consciousness rapidly deteriorates in severe poisoning, consider intubation before gastrointestinal decontamination procedures. Monitor plasma potassium levels and manage accordingly. Hemofiltration, hemodialysis, and hemoperfusion are not of benefit. Consider contacting a poison center (1-800-221-2222) or a medical toxicologist for overdosage management recommendations.

Approval history

Sourced from openFDA
  • Apr 18, 1955NDANDA009768Advanz Pharma
  • Sep 30, 1994ANDAANDA040081Teva Pharms
  • Jan 27, 1996ANDAANDA040150Creekwood Pharms
  • May 29, 1998ANDAANDA040274Aurobindo Pharma Usa
  • Jun 14, 2007ANDAANDA040766Ipca Labs Ltd
  • Sep 21, 2007ANDAANDA040657Zydus Pharms Usa Inc
  • May 1, 2018ANDAANDA210441Appco
  • Jan 14, 2022NDANDA214581Novitium Pharma

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
149,343 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Ineffective41,30628%
  2. 2Rheumatoid Arthritis26,63018%
  3. 3Off Label Use22,12915%
  4. 4Pain21,70515%
  5. 5Fatigue18,43412%
  6. 6Arthralgia18,42112%
  7. 7Drug Intolerance16,45911%
  8. 8Joint Swelling15,85211%
  9. 9Rash13,9959.4%
  10. 10Nausea13,0028.7%
  11. 11Condition Aggravated12,1738.2%
  12. 12Abdominal Discomfort11,9018.0%
  13. 13Alopecia11,8497.9%
  14. 14Contraindicated Product Administered11,6507.8%
  15. 15Headache11,4617.7%

Literature

View JSON

Recent PubMed references pinned to Hydroxychloroquine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 618 ClinicalTrials.gov registrations naming Hydroxychloroquine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Hydroxychloroquine. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

  • G6PDCPIC CFDA label: Actionable PGx
    G6PD

Frequently asked questions

How does Hydroxychloroquine work?
Malaria Hydroxychloroquine is a 4-aminoquinoline antimalarial [see Microbiology (12.4) ] and antirheumatic agent. Rheumatoid Arthritis, Systemic Lupus Erythematosus and Chronic Discoid Lupus Erythematosus The mechanisms underlying the anti-inflammatory and immunomodulatory effects of hydroxychloroquine sulfate tablets in the treatment of rheumatoid arthritis, chronic discoid lupus erythematosus and systemic lupus erythematosus are not fully known.
What is Hydroxychloroquine used for?
According to FDA labeling, Hydroxychloroquine carries indications including: Hydroxychloroquine sulfate tablets are an antimalarial and antirheumatic indicated for the: Treatment of uncomplicated malaria due to Plasmodium falciparum, Plasmodium malariae, Plasmodium ovale, and Plasmodium vivax in adult and pediatric patients. ( 1.1 ) Prophylaxis of malaria in geographic areas where chloroquine resistance is not reported in adult and pediatric patients.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Hydroxychloroquine?
Hydroxychloroquine is classified as Aminoquinolines, Antimalarial, Antirheumatic Agent, Enzyme Inhibitors, Physiochemical Activity, Decreased Endocytosis, Decreased Immunologically Active Molecule Activity.
What are the brand names for Hydroxychloroquine?
Hydroxychloroquine is marketed under brand names including Plaquenil, Sovuna.
What are the contraindications for Hydroxychloroquine?
Hydroxychloroquine labeling lists contraindications including: Hydroxychloroquine sulfate tablets are contraindicated in patients with known hypersensitivity to 4-aminoquinoline compounds.. Always consult the full prescribing information and a clinician.
Note. Data for hydroxychloroquine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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