Hydroxychloroquine 400mg Tablets
It is used to treat or prevent malaria. It is used to treat lupus.It is used to treat rheumatoid arthritis.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antimalarial, Disease-Modifying Antirheumatic Drug (DMARD)
Pharmacologic Class
Aminoquinoline
Pregnancy Category
Category C
FDA Approved
Mar 1955
DEA Schedule
Not Controlled
Overview
What is this medicine?
Hydroxychloroquine is a medication used to treat certain autoimmune diseases like lupus and rheumatoid arthritis, and also to prevent or treat malaria. It works by calming down the overactive immune system in autoimmune conditions and by killing the malaria parasite. It's important to take it exactly as prescribed and to have regular eye exams because it can, in rare cases, affect your vision.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow these guidelines:
Take your medication exactly as directed by your doctor. Read all the information provided with your prescription and follow the instructions carefully.
For all uses of this medication:
+ Take your dose with food or milk to help your body absorb the medication.
+ Swallow the tablet whole; do not chew, break, or crush it.
+ Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
+ Avoid taking antacids or kaolin within 4 hours of taking this medication, as they may interfere with its effectiveness.
If you are taking this medication to prevent malaria:
+ Make sure you understand when to start taking your medication. If you are unsure, consult with your doctor.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store your medication at room temperature in a dry place, away from the bathroom.
Keep all medications in a secure location, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. Check with your pharmacist for guidance on the best way to dispose of your medication, and consider participating in a drug take-back program in your area.
What to Do If You Miss a Dose
If you miss a dose of your medication:
Take the missed dose as soon as you remember.
If it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule.
* Do not take two doses at the same time or take extra doses to make up for a missed dose.
To ensure you get the most benefit from your medication, follow these guidelines:
Take your medication exactly as directed by your doctor. Read all the information provided with your prescription and follow the instructions carefully.
For all uses of this medication:
+ Take your dose with food or milk to help your body absorb the medication.
+ Swallow the tablet whole; do not chew, break, or crush it.
+ Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
+ Avoid taking antacids or kaolin within 4 hours of taking this medication, as they may interfere with its effectiveness.
If you are taking this medication to prevent malaria:
+ Make sure you understand when to start taking your medication. If you are unsure, consult with your doctor.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store your medication at room temperature in a dry place, away from the bathroom.
Keep all medications in a secure location, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. Check with your pharmacist for guidance on the best way to dispose of your medication, and consider participating in a drug take-back program in your area.
What to Do If You Miss a Dose
If you miss a dose of your medication:
Take the missed dose as soon as you remember.
If it is close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule.
* Do not take two doses at the same time or take extra doses to make up for a missed dose.
Lifestyle & Tips
- Take with food or milk to reduce stomach upset.
- Take at the same time each day for consistent levels.
- Do not stop taking this medication without consulting your doctor, even if you feel better.
- Protect your skin from the sun, as this medication can increase sun sensitivity.
- Attend all scheduled eye examinations and blood tests as advised by your doctor.
- Report any new or worsening vision changes immediately to your doctor.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Varies by indication. For Rheumatoid Arthritis/Lupus: Initial 400-600 mg daily, maintenance 200-400 mg daily. For Malaria Prophylaxis: 400 mg once weekly. For Acute Malaria: Initial 800 mg, then 400 mg at 6, 24, and 48 hours.
Dose Range:
200 - 800 mg
Condition-Specific Dosing:
Rheumatoid Arthritis:
Initial 400-600 mg daily (single or divided doses) for 4-12 weeks, then 200-400 mg daily for maintenance. Max 6.5 mg/kg/day or 400 mg/day, whichever is lower.
Systemic Lupus Erythematosus:
Initial 400 mg daily (single or divided doses) for several weeks or months, then 200-400 mg daily for maintenance. Max 6.5 mg/kg/day or 400 mg/day, whichever is lower.
Malaria Prophylaxis:
400 mg (310 mg base) once weekly on the same day of the week, starting 2 weeks before exposure and continuing for 4 weeks after leaving the endemic area.
Acute Malaria (non-falciparum or chloroquine-sensitive falciparum):
Initial 800 mg (620 mg base), followed by 400 mg (310 mg base) at 6 hours, 24 hours, and 48 hours after the initial dose (total 2000 mg over 3 days).
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For Rheumatoid Arthritis/Lupus: Max 6.5 mg/kg/day or 400 mg/day, whichever is lower. For Malaria Prophylaxis: 6.5 mg/kg (base) once weekly, not to exceed adult dose. For Acute Malaria: Initial 13 mg/kg (base), then 6.5 mg/kg (base) at 6, 24, and 48 hours after initial dose (total 31 mg/kg base).
Adolescent:
Dosing similar to adult, based on weight (max 6.5 mg/kg/day or 400 mg/day).
Dose Adjustments
Renal Impairment:
Mild:
Consider dose reduction or increased monitoring, especially with long-term use.
Moderate:
Dose reduction (e.g., 50%) or increased dosing interval recommended. Monitor for toxicity.
Severe:
Contraindicated or significant dose reduction (e.g., 50-75%) and careful monitoring. Avoid if possible.
Dialysis:
Hydroxychloroquine is not significantly removed by dialysis. Dose adjustments based on residual renal function.
Hepatic Impairment:
Mild:
Use with caution; monitor for adverse effects.
Moderate:
Use with caution; consider dose reduction and close monitoring.
Severe:
Use with extreme caution or avoid; significant dose reduction likely required. Monitor for toxicity.
Pharmacology
Mechanism of Action
Hydroxychloroquine is an antimalarial and immunomodulatory agent. Its exact mechanism in autoimmune diseases is not fully understood but is thought to involve interference with lysosomal activity, leading to altered antigen presentation and reduced cytokine production (e.g., IL-1, IL-6, TNF-alpha). It also inhibits toll-like receptor (TLR) signaling, particularly TLR9, which is involved in the immune response to DNA/RNA. In malaria, it concentrates in the parasite's food vacuole, inhibiting heme detoxification and leading to accumulation of toxic heme, which kills the parasite.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 74%
Tmax:
3-4 hours (for parent drug), 8-12 hours (for active metabolite)
FoodEffect:
Food may increase bioavailability and reduce GI upset.
Distribution:
Vd:
High (5800 L), indicating extensive tissue distribution
ProteinBinding:
Approximately 50%
CnssPenetration:
Limited, but can cross the blood-brain barrier and accumulate in CNS tissues over time.
Elimination:
HalfLife:
Approximately 32-50 days (terminal elimination half-life)
Clearance:
Not available (highly variable)
ExcretionRoute:
Renal (approximately 50% unchanged), hepatic/biliary
Unchanged:
Approximately 50%
Pharmacodynamics
OnsetOfAction:
Weeks to months for autoimmune conditions (e.g., 6-12 weeks for RA, longer for SLE). Rapid for acute malaria.
PeakEffect:
Months for autoimmune conditions.
DurationOfAction:
Due to long half-life, effects persist for weeks after discontinuation.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin with or without fever, wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes.
Signs of kidney problems: inability to pass urine, changes in urine output, blood in the urine, or significant weight gain.
Signs of low blood sugar: dizziness, headache, feeling sleepy, feeling weak, shaking, rapid heartbeat, confusion, hunger, or sweating.
Seizures.
New or worsening behavioral or mood changes, such as depression or suicidal thoughts.
Confusion.
Hallucinations (seeing or hearing things that are not there).
Bad dreams.
Ringing in the ears, hearing loss, or changes in hearing.
Balance problems.
Difficulty controlling body movements.
Shakiness.
Muscle weakness.
Inability to control eye movements.
Severe eye problems, which may lead to lasting vision problems. This risk may be higher if you have pre-existing eye or kidney problems, take high doses of this medication, use it for more than 5 years, or take certain other medications like tamoxifen. If you experience any changes in vision, such as blurred or foggy vision, trouble focusing or reading, or difficulty seeing in low light, contact your doctor immediately.
Heart problems, including heart failure and abnormal heart rhythms (prolonged QT interval), which can be life-threatening. If you experience a rapid or irregular heartbeat, severe dizziness or fainting, shortness of breath, significant weight gain, or swelling in the arms or legs, seek medical help right away.
Low blood cell counts, which can increase the risk of bleeding, infections, or anemia. If you experience signs of infection, such as fever, chills, or sore throat, unexplained bruising or bleeding, or feel extremely tired or weak, contact your doctor immediately.
Severe skin reactions, including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and other serious reactions, which can be life-threatening. If you experience symptoms such as red, swollen, blistered, or peeling skin, red or irritated eyes, sores in the mouth, throat, nose, eyes, genitals, or skin, fever, chills, body aches, shortness of breath, or swollen glands, seek medical help right away.
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you experience any of the following side effects and they bother you or do not go away, contact your doctor:
Dizziness, tiredness, or weakness.
Headache.
Feeling nervous or excitable.
Diarrhea, stomach pain, upset stomach, vomiting, or decreased appetite.
Weight loss.
Changes in skin color.
Changes in hair color.
* Hair loss.
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin with or without fever, wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes.
Signs of kidney problems: inability to pass urine, changes in urine output, blood in the urine, or significant weight gain.
Signs of low blood sugar: dizziness, headache, feeling sleepy, feeling weak, shaking, rapid heartbeat, confusion, hunger, or sweating.
Seizures.
New or worsening behavioral or mood changes, such as depression or suicidal thoughts.
Confusion.
Hallucinations (seeing or hearing things that are not there).
Bad dreams.
Ringing in the ears, hearing loss, or changes in hearing.
Balance problems.
Difficulty controlling body movements.
Shakiness.
Muscle weakness.
Inability to control eye movements.
Severe eye problems, which may lead to lasting vision problems. This risk may be higher if you have pre-existing eye or kidney problems, take high doses of this medication, use it for more than 5 years, or take certain other medications like tamoxifen. If you experience any changes in vision, such as blurred or foggy vision, trouble focusing or reading, or difficulty seeing in low light, contact your doctor immediately.
Heart problems, including heart failure and abnormal heart rhythms (prolonged QT interval), which can be life-threatening. If you experience a rapid or irregular heartbeat, severe dizziness or fainting, shortness of breath, significant weight gain, or swelling in the arms or legs, seek medical help right away.
Low blood cell counts, which can increase the risk of bleeding, infections, or anemia. If you experience signs of infection, such as fever, chills, or sore throat, unexplained bruising or bleeding, or feel extremely tired or weak, contact your doctor immediately.
Severe skin reactions, including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and other serious reactions, which can be life-threatening. If you experience symptoms such as red, swollen, blistered, or peeling skin, red or irritated eyes, sores in the mouth, throat, nose, eyes, genitals, or skin, fever, chills, body aches, shortness of breath, or swollen glands, seek medical help right away.
Other Possible Side Effects
Most people do not experience significant side effects, but some may occur. If you experience any of the following side effects and they bother you or do not go away, contact your doctor:
Dizziness, tiredness, or weakness.
Headache.
Feeling nervous or excitable.
Diarrhea, stomach pain, upset stomach, vomiting, or decreased appetite.
Weight loss.
Changes in skin color.
Changes in hair color.
* Hair loss.
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Any changes in vision (blurred vision, difficulty reading, blind spots, halos around lights, changes in color vision)
- Muscle weakness or difficulty moving
- Unexplained bruising or bleeding
- Fever, chills, or persistent sore throat (signs of infection)
- Severe stomach pain, nausea, vomiting, or diarrhea
- Skin rash or itching
- Dizziness, lightheadedness, or fainting
- New or worsening shortness of breath or chest pain
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
A history of abnormal heart rhythms, including a prolonged QT interval on an electrocardiogram (ECG).
Certain health conditions, such as:
+ Low magnesium or potassium levels
+ Slow heartbeat
+ Eye problems like retinopathy
+ Heart failure (weak heart) or a history of heart attack
+ Previous eye or vision changes caused by this medication or similar drugs
+ Porphyria or psoriasis
Current medications, including:
+ Cimetidine or rifampicin
+ Any drugs that may cause abnormal heart rhythms (prolonged QT interval). There are many medications that can have this effect, so consult your doctor or pharmacist if you are unsure.
* All prescription and over-the-counter medications, natural products, and vitamins you are taking. This information is crucial to avoid potential interactions and ensure safe treatment.
Remember to consult your doctor before starting, stopping, or changing the dose of any medication. It is your responsibility to verify that it is safe to take this medication with all your other medications and health conditions.
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
A history of abnormal heart rhythms, including a prolonged QT interval on an electrocardiogram (ECG).
Certain health conditions, such as:
+ Low magnesium or potassium levels
+ Slow heartbeat
+ Eye problems like retinopathy
+ Heart failure (weak heart) or a history of heart attack
+ Previous eye or vision changes caused by this medication or similar drugs
+ Porphyria or psoriasis
Current medications, including:
+ Cimetidine or rifampicin
+ Any drugs that may cause abnormal heart rhythms (prolonged QT interval). There are many medications that can have this effect, so consult your doctor or pharmacist if you are unsure.
* All prescription and over-the-counter medications, natural products, and vitamins you are taking. This information is crucial to avoid potential interactions and ensure safe treatment.
Remember to consult your doctor before starting, stopping, or changing the dose of any medication. It is your responsibility to verify that it is safe to take this medication with all your other medications and health conditions.
Precautions & Cautions
Important Warnings and Cautions
When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, about your treatment. Regular monitoring is crucial, so be sure to undergo blood tests, eye exams, and electrocardiograms (ECGs) as directed by your doctor to assess your heart rhythm.
If you have a deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD), you may be at increased risk of developing anemia. This deficiency is more common in individuals of African, South Asian, Middle Eastern, and Mediterranean descent. Your doctor will closely monitor your condition to prevent any potential complications.
This medication can increase your sensitivity to the sun, making you more prone to sunburn. Take necessary precautions when exposed to sunlight, and inform your doctor if you experience any unusual sunburn or skin reactions.
There is a risk of hypoglycemia (low blood sugar) associated with this medication, which can be severe and potentially life-threatening. It is crucial to monitor your blood sugar levels regularly, as advised by your doctor, and to discuss any concerns or symptoms with your healthcare provider.
Before consuming alcohol, consult with your doctor to understand any potential risks or interactions. Additionally, keep this medication out of reach of children, as accidental ingestion can be fatal. If a child accidentally takes this medication, seek immediate medical attention.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects. Pregnant or breastfeeding women should discuss the benefits and risks of this medication with their doctor before starting treatment.
Preventing Malaria
When using this medication to prevent malaria, it is essential to combine it with other preventive measures, including:
Using window screens and bed netting to prevent insect bites
Applying insect repellents containing 10% to 35% DEET
Spraying permethrin on clothing and nets
Avoiding the use of most insect repellents on children
* Reducing outdoor activities during evening and nighttime hours when mosquitoes are most active
If you experience a fever while in or after leaving a malaria-infested area, contact your doctor immediately. Pregnant women traveling to areas with malaria should consult their doctor before starting treatment to discuss the potential risks and benefits.
When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, about your treatment. Regular monitoring is crucial, so be sure to undergo blood tests, eye exams, and electrocardiograms (ECGs) as directed by your doctor to assess your heart rhythm.
If you have a deficiency of the enzyme glucose-6-phosphate dehydrogenase (G6PD), you may be at increased risk of developing anemia. This deficiency is more common in individuals of African, South Asian, Middle Eastern, and Mediterranean descent. Your doctor will closely monitor your condition to prevent any potential complications.
This medication can increase your sensitivity to the sun, making you more prone to sunburn. Take necessary precautions when exposed to sunlight, and inform your doctor if you experience any unusual sunburn or skin reactions.
There is a risk of hypoglycemia (low blood sugar) associated with this medication, which can be severe and potentially life-threatening. It is crucial to monitor your blood sugar levels regularly, as advised by your doctor, and to discuss any concerns or symptoms with your healthcare provider.
Before consuming alcohol, consult with your doctor to understand any potential risks or interactions. Additionally, keep this medication out of reach of children, as accidental ingestion can be fatal. If a child accidentally takes this medication, seek immediate medical attention.
If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects. Pregnant or breastfeeding women should discuss the benefits and risks of this medication with their doctor before starting treatment.
Preventing Malaria
When using this medication to prevent malaria, it is essential to combine it with other preventive measures, including:
Using window screens and bed netting to prevent insect bites
Applying insect repellents containing 10% to 35% DEET
Spraying permethrin on clothing and nets
Avoiding the use of most insect repellents on children
* Reducing outdoor activities during evening and nighttime hours when mosquitoes are most active
If you experience a fever while in or after leaving a malaria-infested area, contact your doctor immediately. Pregnant women traveling to areas with malaria should consult their doctor before starting treatment to discuss the potential risks and benefits.
Overdose Information
Overdose Symptoms:
- Headache
- Drowsiness
- Blurred vision
- Cardiovascular collapse (hypotension, shock)
- Cardiac arrhythmias (e.g., QTc prolongation, ventricular fibrillation, torsades de pointes)
- Seizures
- Respiratory depression
- Hypokalemia
- Hypoglycemia
- Coma
- Death
What to Do:
Call 1-800-222-1222 (Poison Control Center) immediately. Seek emergency medical attention. Treatment may include gastric lavage, activated charcoal, supportive care, and management of arrhythmias and seizures. Close cardiac monitoring is essential.
Drug Interactions
Major Interactions
- Amiodarone (increased risk of cardiac arrhythmias, especially QTc prolongation)
- Digoxin (increased digoxin levels)
- Mefloquine (increased risk of seizures)
- Other QTc-prolonging drugs (e.g., Class IA and III antiarrhythmics, antipsychotics, tricyclic antidepressants, macrolide antibiotics, fluoroquinolones) - increased risk of torsades de pointes
- Insulin and oral hypoglycemics (enhanced hypoglycemic effect)
- Methotrexate (potential for increased adverse effects, though often co-administered with careful monitoring)
- Cyclosporine (increased cyclosporine levels)
Moderate Interactions
- Antacids/Kaolin (decreased hydroxychloroquine absorption - separate administration by at least 4 hours)
- Cimetidine (may inhibit metabolism, increasing hydroxychloroquine levels)
- Praziquantel (may decrease praziquantel levels)
- Vaccines (live attenuated vaccines may have reduced efficacy in immunosuppressed patients, though HCQ is generally considered safe with most vaccines)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Ophthalmologic examination (visual acuity, fundoscopy, automated visual fields, spectral domain optical coherence tomography (SD-OCT))
Rationale: To establish baseline and detect pre-existing retinopathy or maculopathy, and to monitor for drug-induced retinopathy.
Timing: Before starting therapy
Complete Blood Count (CBC) with differential
Rationale: To establish baseline and monitor for hematologic abnormalities (e.g., agranulocytosis, aplastic anemia, thrombocytopenia) which are rare but serious adverse effects.
Timing: Before starting therapy
Liver Function Tests (LFTs)
Rationale: To establish baseline and monitor for hepatic toxicity.
Timing: Before starting therapy
Renal Function Tests (Creatinine, BUN)
Rationale: To establish baseline and guide dose adjustments in renal impairment.
Timing: Before starting therapy
Electrocardiogram (ECG)
Rationale: To establish baseline QTc interval, especially in patients with pre-existing cardiac conditions or those on other QTc-prolonging drugs.
Timing: Before starting therapy, if clinically indicated
Routine Monitoring
Ophthalmologic examination (visual acuity, fundoscopy, automated visual fields, SD-OCT)
Frequency: Annually after 5 years of therapy, or sooner if high-risk factors (e.g., daily dose > 5 mg/kg actual body weight, renal impairment, concomitant tamoxifen, pre-existing macular disease) are present.
Target: Normal visual fields and retinal appearance
Action Threshold: Any new visual changes, scotomas, or retinal abnormalities (e.g., bull's eye maculopathy) warrant immediate discontinuation and referral to ophthalmologist.
Complete Blood Count (CBC) with differential
Frequency: Every 3-6 months, or as clinically indicated.
Target: Within normal limits
Action Threshold: Significant decrease in cell counts (e.g., leukopenia, thrombocytopenia) warrants investigation and potential discontinuation.
Liver Function Tests (LFTs)
Frequency: Every 3-6 months, or as clinically indicated.
Target: Within normal limits
Action Threshold: Significant elevation in liver enzymes warrants investigation and potential discontinuation.
Electrocardiogram (ECG)
Frequency: Periodically, especially if new cardiac symptoms develop or if patient is on other QTc-prolonging drugs.
Target: Normal QTc interval
Action Threshold: Significant QTc prolongation (>500 ms or >60 ms increase from baseline) warrants investigation and potential discontinuation.
Symptom Monitoring
- Visual changes (blurred vision, difficulty reading, light sensitivity, halos, blind spots, color vision changes)
- Muscle weakness or atrophy
- Hearing loss or tinnitus
- Skin rash, itching, or pigmentation changes
- Gastrointestinal upset (nausea, vomiting, diarrhea, abdominal pain)
- Neurological symptoms (headache, dizziness, nervousness, psychosis, seizures)
- Signs of infection (fever, sore throat, unusual bruising or bleeding)
Special Patient Groups
Pregnancy
Generally considered compatible with pregnancy for the treatment of autoimmune diseases (e.g., lupus) where the benefits of controlling the disease outweigh potential risks. Untreated lupus can lead to worse maternal and fetal outcomes. Data suggest low risk of congenital malformations.
Trimester-Specific Risks:
First Trimester:
Low risk of teratogenicity based on available data.
Second Trimester:
Generally considered safe and continued for disease control.
Third Trimester:
Generally considered safe and continued for disease control.
Lactation
Considered compatible with breastfeeding. Hydroxychloroquine is excreted into breast milk in small amounts, but infant exposure is low and adverse effects are rare. Monitor infant for signs of toxicity (e.g., rash, diarrhea).
Infant Risk:
L2 (Safer)
Pediatric Use
Used in pediatric patients for juvenile idiopathic arthritis, systemic lupus erythematosus, and malaria. Dosing is weight-based. Long-term monitoring for retinopathy is crucial, similar to adults.
Geriatric Use
Use with caution in elderly patients due to potential for age-related decreases in renal and hepatic function, which may alter drug clearance and increase risk of toxicity. Increased susceptibility to ocular toxicity may also be a concern. Start with lower doses and monitor closely.
Clinical Information
Clinical Pearls
- Hydroxychloroquine has a very long half-life, meaning it takes weeks to months to reach steady state and for its effects to fully manifest or dissipate.
- The most critical long-term adverse effect is irreversible retinopathy. Regular ophthalmologic screening is paramount, especially after 5 years of use or if high-risk factors are present.
- Dosing should ideally be based on actual body weight (ABW) for retinopathy risk assessment, with a maximum daily dose of 5 mg/kg ABW (or 400 mg/day, whichever is lower) to minimize ocular toxicity.
- Take with food to minimize gastrointestinal side effects.
- Patients should be educated on the importance of adherence to monitoring schedules and reporting any visual changes immediately.
- Hydroxychloroquine is generally well-tolerated compared to other DMARDs, making it a first-line agent for many patients with lupus and mild RA.
Alternative Therapies
- For Rheumatoid Arthritis: Methotrexate, Sulfasalazine, Leflunomide, Biologic DMARDs (e.g., TNF inhibitors, IL-6 inhibitors, T-cell costimulation modulators)
- For Systemic Lupus Erythematosus: Belimumab, Anifrolumab, Mycophenolate mofetil, Azathioprine, Cyclophosphamide, Corticosteroids
- For Malaria: Chloroquine (if sensitive), Mefloquine, Atovaquone/Proguanil, Doxycycline, Primaquine (for P. vivax/ovale radical cure)
Cost & Coverage
Average Cost:
$20 - $100 per 30 tablets (400mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (preferred generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further evaluation and guidance. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may have additional patient information leaflets, so it is a good idea to consult with your pharmacist for more information. If you have any questions or concerns about this medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.