Hydroxychloroquine 100mg 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 (Historically, but often considered compatible with careful monitoring for autoimmune diseases)
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, in rare cases, it can affect your vision.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most out of your medication, follow these steps:
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 instructed 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're unsure, consult with your doctor.
Storing and Disposing of Your Medication
To keep your medication safe and effective:
Store your medication at room temperature in a dry place, away from the bathroom.
Keep all medications in a secure location, out of 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. You may also have access to drug take-back programs 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's 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 out of your medication, follow these steps:
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 instructed 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're unsure, consult with your doctor.
Storing and Disposing of Your Medication
To keep your medication safe and effective:
Store your medication at room temperature in a dry place, away from the bathroom.
Keep all medications in a secure location, out of 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. You may also have access to drug take-back programs 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's 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.
- Do not crush or chew tablets.
- Wear sunscreen and protective clothing when outdoors, as this medication can increase sun sensitivity.
- Avoid alcohol or limit intake, as it may increase the risk of liver problems.
- Attend all scheduled eye exams and blood tests as advised by your doctor.
- Report any changes in vision immediately.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Varies by indication. For Rheumatoid Arthritis: 200-400 mg daily (2-4 tablets of 100mg) in 1-2 divided doses. For Systemic Lupus Erythematosus: 200-400 mg daily (2-4 tablets of 100mg) in 1-2 divided doses. For Malaria Prophylaxis: 400 mg (4 tablets of 100mg) once weekly, starting 1-2 weeks before exposure and continuing for 4 weeks after leaving endemic area. For Acute Malaria Treatment: Initial dose of 800 mg (8 tablets of 100mg), then 400 mg (4 tablets of 100mg) at 6, 24, and 48 hours after the initial dose.
Dose Range:
200 - 800 mg
Condition-Specific Dosing:
Rheumatoid Arthritis:
200-400 mg daily, max 5 mg/kg/day or 400 mg/day, whichever is lower.
Systemic Lupus Erythematosus:
200-400 mg daily, max 5 mg/kg/day or 400 mg/day, whichever is lower.
Malaria Prophylaxis:
400 mg once weekly.
Acute Malaria Treatment:
Total 2000 mg over 3 days.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For Juvenile Idiopathic Arthritis/SLE: 3-7 mg/kg/day (max 400 mg/day or 5 mg/kg/day, whichever is lower). For Malaria Prophylaxis: 6.5 mg/kg (max 400 mg) once weekly. For Acute Malaria Treatment: 10 mg/kg initial dose (max 600 mg), then 5 mg/kg (max 300 mg) at 6, 24, and 48 hours after initial dose (total 25 mg/kg).
Adolescent:
Same as child dosing, generally not exceeding adult maximums.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, monitor for toxicity.
Moderate:
Consider dose reduction (e.g., 50%) or increased dosing interval; monitor for toxicity.
Severe:
Avoid use or significantly reduce dose (e.g., 50-75% reduction) and monitor closely; consider alternative therapies.
Dialysis:
Not significantly dialyzable; follow severe renal impairment guidelines.
Hepatic Impairment:
Mild:
No specific adjustment recommended, monitor for toxicity.
Moderate:
Consider dose reduction (e.g., 50%) and monitor for toxicity.
Severe:
Avoid use or significantly reduce dose and monitor closely; consider alternative therapies.
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 inflammatory response in lupus. In malaria, it concentrates in the parasite's food vacuole, inhibiting heme detoxification, leading to accumulation of toxic heme and parasite death.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 74%
Tmax:
3-4 hours (parent drug), 10-12 hours (major metabolite)
FoodEffect:
Food may increase absorption slightly and reduce GI upset.
Distribution:
Vd:
5800 L (extensive tissue distribution, especially in liver, spleen, kidney, lung, and retina)
ProteinBinding:
Approximately 45% (to plasma proteins)
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 from plasma), 40-50 days (whole blood)
Clearance:
Not readily available, but primarily renal and hepatic.
ExcretionRoute:
Renal (approximately 50% unchanged), hepatic/biliary.
Unchanged:
Approximately 50% (renal excretion)
Pharmacodynamics
OnsetOfAction:
Weeks to months for autoimmune conditions (e.g., 6-12 weeks for RA, up to 6 months for full effect). Rapid for malaria.
PeakEffect:
Not well-defined for chronic conditions due to slow onset; for malaria, within hours.
DurationOfAction:
Prolonged due to long half-life and tissue accumulation; effects can 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, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of kidney problems, such as:
+ Inability to pass urine
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Signs of low blood sugar, including:
+ Dizziness
+ Headache
+ Feeling sleepy
+ Feeling weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Seizures
New or worsening behavior or mood changes, such as depression or thoughts of suicide
Confusion
Hallucinations (seeing or hearing things that are not there)
Bad dreams
Ringing in the ears, hearing loss, or other changes in hearing
Balance problems
Trouble controlling body movements
Shakiness
Muscle weakness
Uncontrolled eye movements
Eye problems, including blurred or foggy vision, trouble focusing or reading, or difficulty seeing in dim light
Loss of vision, dark spots, or partial vision loss
Special Warnings:
This medication may increase the risk of severe eye problems, including lasting vision loss, especially if you have pre-existing eye or kidney problems, take high doses, or use the medication for an extended period (more than 5 years).
Heart problems, such as heart failure and abnormal heart rhythms (prolonged QT interval), have been reported, sometimes with fatal outcomes. Seek medical help immediately if you experience:
+ Fast or abnormal heartbeat
+ Severe dizziness or fainting
+ Shortness of breath
+ Sudden weight gain
+ Swelling in the arms or legs
Low blood cell counts may occur, increasing the risk of bleeding, infections, or anemia. Contact your doctor if you experience:
+ Fever
+ Chills
+ Sore throat
+ Unexplained bruising or bleeding
+ Extreme fatigue or weakness
Severe skin reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), may occur, sometimes affecting internal organs. Seek medical help immediately if you notice:
+ 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
+ Swollen glands
Other Possible Side Effects:
While many people may not experience any side effects or only mild ones, it's essential to report any concerns to your doctor. Common side effects include:
Dizziness
Tiredness
Weakness
Headache
Nervousness or excitability
Diarrhea
Stomach pain
Upset stomach
Vomiting
Decreased appetite
Weight loss
Skin color changes
Hair color changes
* Hair loss
If you have questions or concerns about side effects, contact your doctor or report them to the FDA at 1-800-332-1088 or 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, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Signs of kidney problems, such as:
+ Inability to pass urine
+ Changes in urine output
+ Blood in the urine
+ Sudden weight gain
Signs of low blood sugar, including:
+ Dizziness
+ Headache
+ Feeling sleepy
+ Feeling weak
+ Shaking
+ Fast heartbeat
+ Confusion
+ Hunger
+ Sweating
Seizures
New or worsening behavior or mood changes, such as depression or thoughts of suicide
Confusion
Hallucinations (seeing or hearing things that are not there)
Bad dreams
Ringing in the ears, hearing loss, or other changes in hearing
Balance problems
Trouble controlling body movements
Shakiness
Muscle weakness
Uncontrolled eye movements
Eye problems, including blurred or foggy vision, trouble focusing or reading, or difficulty seeing in dim light
Loss of vision, dark spots, or partial vision loss
Special Warnings:
This medication may increase the risk of severe eye problems, including lasting vision loss, especially if you have pre-existing eye or kidney problems, take high doses, or use the medication for an extended period (more than 5 years).
Heart problems, such as heart failure and abnormal heart rhythms (prolonged QT interval), have been reported, sometimes with fatal outcomes. Seek medical help immediately if you experience:
+ Fast or abnormal heartbeat
+ Severe dizziness or fainting
+ Shortness of breath
+ Sudden weight gain
+ Swelling in the arms or legs
Low blood cell counts may occur, increasing the risk of bleeding, infections, or anemia. Contact your doctor if you experience:
+ Fever
+ Chills
+ Sore throat
+ Unexplained bruising or bleeding
+ Extreme fatigue or weakness
Severe skin reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), may occur, sometimes affecting internal organs. Seek medical help immediately if you notice:
+ 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
+ Swollen glands
Other Possible Side Effects:
While many people may not experience any side effects or only mild ones, it's essential to report any concerns to your doctor. Common side effects include:
Dizziness
Tiredness
Weakness
Headache
Nervousness or excitability
Diarrhea
Stomach pain
Upset stomach
Vomiting
Decreased appetite
Weight loss
Skin color changes
Hair color changes
* Hair loss
If you have questions or concerns about side effects, contact your doctor or report them to the FDA at 1-800-332-1088 or https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Any changes in vision (blurred vision, difficulty reading, blind spots, halos, color changes)
- Unexplained muscle weakness or difficulty walking
- Unusual bleeding or bruising
- Persistent sore throat, fever, or signs of infection
- Severe skin rash or itching
- Severe nausea, vomiting, or diarrhea
- Ringing in the ears or hearing loss
- Yellowing of the skin or eyes (jaundice)
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, such as foods or drugs. 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 levels of magnesium or potassium in your blood
+ A slow heartbeat
+ Eye problems like retinopathy
+ Heart failure (a weakened heart) or a history of heart attack
+ Previous eye or vision changes caused by this medication or similar drugs
+ Porphyria or psoriasis
Concurrent use of specific medications, including:
+ Cimetidine or rifampicin
+ Drugs that can 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 medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information is crucial to avoid potential interactions.
To ensure your safety, it is vital to discuss all your medications and health conditions with your doctor and pharmacist. Do not start, stop, or modify the dosage of any medication without consulting your doctor first. This list is not exhaustive, and your doctor will help determine if it is safe for you to take this medication with your existing health conditions and medications.
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, such as foods or drugs. 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 levels of magnesium or potassium in your blood
+ A slow heartbeat
+ Eye problems like retinopathy
+ Heart failure (a weakened heart) or a history of heart attack
+ Previous eye or vision changes caused by this medication or similar drugs
+ Porphyria or psoriasis
Concurrent use of specific medications, including:
+ Cimetidine or rifampicin
+ Drugs that can 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 medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This information is crucial to avoid potential interactions.
To ensure your safety, it is vital to discuss all your medications and health conditions with your doctor and pharmacist. Do not start, stop, or modify the dosage of any medication without consulting your doctor first. This list is not exhaustive, and your doctor will help determine if it is safe for you to take this medication with your existing health conditions and medications.
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.
To ensure safe use, your doctor will recommend regular blood tests, eye exams, and an electrocardiogram (ECG) to monitor 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.
This medication can increase your sensitivity to sunlight, making you more prone to sunburn. Take necessary precautions when spending time outdoors, and notify your doctor if you experience excessive sunburn.
There is a risk of low blood sugar (hypoglycemia) associated with this medication, which can be severe and potentially life-threatening. Consult your doctor and monitor your blood sugar levels as advised.
Before consuming alcohol, discuss the potential risks with your doctor.
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.
If you are pregnant, planning to become pregnant, or breastfeeding, consult your doctor to discuss the benefits and risks of this medication to you and your baby.
Preventing Malaria
In addition to taking this medication, it is crucial to implement other preventive measures against malaria, including:
Using window screens and bed nets
Applying insect repellent (containing 10% to 35% DEET) to skin and clothing
Spraying permethrin on clothing and nets (avoid spraying insect repellents on children)
Reducing outdoor activities during evening and nighttime hours
If you experience a fever while in or after leaving a malaria-endemic area, contact your doctor immediately.
If you are pregnant and planning to travel to a malaria-infested region, consult your doctor to discuss the risks and necessary precautions before your trip.
When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, about your treatment.
To ensure safe use, your doctor will recommend regular blood tests, eye exams, and an electrocardiogram (ECG) to monitor 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.
This medication can increase your sensitivity to sunlight, making you more prone to sunburn. Take necessary precautions when spending time outdoors, and notify your doctor if you experience excessive sunburn.
There is a risk of low blood sugar (hypoglycemia) associated with this medication, which can be severe and potentially life-threatening. Consult your doctor and monitor your blood sugar levels as advised.
Before consuming alcohol, discuss the potential risks with your doctor.
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.
If you are pregnant, planning to become pregnant, or breastfeeding, consult your doctor to discuss the benefits and risks of this medication to you and your baby.
Preventing Malaria
In addition to taking this medication, it is crucial to implement other preventive measures against malaria, including:
Using window screens and bed nets
Applying insect repellent (containing 10% to 35% DEET) to skin and clothing
Spraying permethrin on clothing and nets (avoid spraying insect repellents on children)
Reducing outdoor activities during evening and nighttime hours
If you experience a fever while in or after leaving a malaria-endemic area, contact your doctor immediately.
If you are pregnant and planning to travel to a malaria-infested region, consult your doctor to discuss the risks and necessary precautions before your trip.
Overdose Information
Overdose Symptoms:
- Headache
- Drowsiness
- Blurred vision
- Cardiovascular collapse (hypotension, shock)
- Cardiac arrhythmias (e.g., QT prolongation, ventricular fibrillation, torsades de pointes)
- Seizures
- Hypokalemia
- Respiratory depression
- Coma
- Death
What to Do:
Seek immediate emergency medical attention. Call 911 or Poison Control at 1-800-222-1222. Management includes gastric lavage, activated charcoal, supportive care, and close monitoring of cardiac function (ECG), electrolytes (especially potassium), and respiratory status. Diazepam may be used for seizures. Intravenous potassium supplementation may be required for hypokalemia.
Drug Interactions
Major Interactions
- Amiodarone (increased risk of cardiac arrhythmias, especially QT prolongation)
- Digoxin (increased serum digoxin levels)
- Mefloquine (increased risk of seizures)
- Other QT-prolonging drugs (e.g., Class IA and III antiarrhythmics, antipsychotics, macrolide antibiotics, fluoroquinolones) - increased risk of torsades de pointes
- Insulin/Oral Hypoglycemics (enhanced hypoglycemic effect)
- Cyclosporine (increased cyclosporine levels)
- Tamoxifen (increased risk of retinopathy)
Moderate Interactions
- Antacids/Kaolin (decreased hydroxychloroquine absorption; separate administration by at least 4 hours)
- Cimetidine (may inhibit metabolism, increasing hydroxychloroquine levels)
- Neostigmine/Pyridostigmine (may antagonize effects of anticholinesterases)
- Praziquantel (decreased praziquantel levels)
- Vaccines (live attenuated vaccines: theoretical reduced immune response, though generally considered safe for most patients on HCQ)
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 maculopathy or risk factors for retinopathy.
Timing: Within the first year of starting therapy.
Complete Blood Count (CBC) with differential
Rationale: To check for baseline blood dyscrasias (e.g., anemia, leukopenia, thrombocytopenia).
Timing: Before starting therapy.
Liver Function Tests (LFTs)
Rationale: To assess baseline hepatic function, as drug is metabolized by the liver.
Timing: Before starting therapy.
Renal Function Tests (Creatinine, BUN)
Rationale: To assess baseline renal function, as drug is renally excreted.
Timing: Before starting therapy.
Glucose-6-Phosphate Dehydrogenase (G6PD) deficiency screen (if patient is of African, Mediterranean, or South Asian descent)
Rationale: To identify patients at risk of hemolytic anemia.
Timing: Before starting therapy.
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., renal impairment, concomitant tamoxifen, high cumulative dose, pre-existing retinal disease) are present. More frequent monitoring (e.g., every 6-12 months) for high-risk patients.
Target: Stable 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: Periodically (e.g., every 3-6 months initially, then annually) or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant drops in cell counts (e.g., leukopenia, thrombocytopenia, anemia) warrant investigation and potential drug discontinuation.
Liver Function Tests (LFTs)
Frequency: Periodically (e.g., every 3-6 months initially, then annually) or as clinically indicated.
Target: Within normal limits.
Action Threshold: Significant elevations in liver enzymes warrant investigation and potential drug discontinuation.
Renal Function Tests (Creatinine, BUN)
Frequency: Periodically (e.g., annually) or as clinically indicated, especially if renal impairment is present.
Target: Within normal limits or stable for patient's baseline.
Action Threshold: Significant worsening of renal function may necessitate dose adjustment or discontinuation.
Symptom Monitoring
- Visual disturbances (blurred vision, difficulty reading, light sensitivity, halos, blind spots, color vision changes)
- Muscle weakness or atrophy
- Unusual bleeding or bruising
- Persistent fever, sore throat, or signs of infection
- Skin rash or itching
- Nausea, vomiting, diarrhea, or abdominal pain
- Hair loss or changes in hair color
- Tinnitus or hearing loss
- Mood changes or psychiatric symptoms (rare)
Special Patient Groups
Pregnancy
Hydroxychloroquine is generally considered compatible with pregnancy for the treatment of autoimmune diseases like lupus and rheumatoid arthritis, as the benefits of controlling the disease often outweigh the potential risks. Untreated maternal autoimmune disease can pose greater risks to both mother and fetus. Close monitoring is recommended.
Trimester-Specific Risks:
First Trimester:
No increased risk of major congenital malformations observed in studies.
Second Trimester:
Generally considered safe; continued use is often recommended to maintain disease control.
Third Trimester:
Generally considered safe; continued use is often recommended to maintain disease control. No evidence of increased risk of retinopathy in the fetus/neonate.
Lactation
Hydroxychloroquine is excreted into breast milk in small amounts. It is generally considered compatible with breastfeeding, especially when the infant is healthy and full-term. Monitor the infant for adverse effects such as rash, diarrhea, or unusual drowsiness.
Infant Risk:
L2 (Safer - limited data suggest no increased risk)
Pediatric Use
Approved for use in pediatric patients for juvenile idiopathic arthritis, systemic lupus erythematosus, and malaria. Dosing is weight-based. Close 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 lead to increased drug accumulation and toxicity. Start with lower doses and monitor closely for adverse effects, especially visual changes.
Clinical Information
Clinical Pearls
- Hydroxychloroquine has a very long half-life, meaning it takes weeks to months to reach steady-state and for its full therapeutic effect to be observed. Patients should be counseled on this delay.
- The most serious adverse effect is retinopathy, which is rare but irreversible. Regular ophthalmologic screening is critical, especially after 5 years of use or if the cumulative dose exceeds 1000 grams (for 200mg/day, this is about 13.7 years). The current recommended maximum daily dose is 5 mg/kg of ideal body weight or 400 mg, whichever is lower, to minimize retinopathy risk.
- Take with food or milk to minimize gastrointestinal upset, which is a common side effect.
- Hydroxychloroquine can cause hypoglycemia, even in patients without diabetes. Monitor blood glucose, especially if co-administered with other hypoglycemic agents.
- It is generally considered safe and effective for long-term use in appropriate patients, with a good safety profile compared to other DMARDs.
- Patients should be advised to report any visual changes immediately, even subtle ones.
Alternative Therapies
- Methotrexate (for RA, SLE)
- Sulfasalazine (for RA)
- Leflunomide (for RA)
- Biologic DMARDs (e.g., TNF inhibitors, IL-6 inhibitors, B-cell depleters for RA, SLE)
- Corticosteroids (for acute flares in RA, SLE)
- Azathioprine (for SLE)
- Mycophenolate mofetil (for SLE)
- Chloroquine (another aminoquinoline antimalarial, but less commonly used for autoimmune diseases due to higher retinopathy risk)
Cost & Coverage
Average Cost:
$20 - $100 per 30 tablets (generic 200mg)
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 guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist. If you have any questions or concerns about this medication, don't 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.