Niacin 500mg SR Capsules
It is used to lower bad cholesterol, lower triglycerides, and raise good cholesterol (HDL).Some products are used to treat niacin deficiency.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antilipemic agent; Vitamin
Pharmacologic Class
Nicotinic acid derivative; Vitamin B3
Pregnancy Category
Category C
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Niacin is a form of Vitamin B3 that helps lower 'bad' cholesterol (LDL and triglycerides) and raise 'good' cholesterol (HDL). The 'SR' or 'Controlled-Release' form is designed to release the medicine slowly over time, which can help reduce common side effects like flushing.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely.
Special Instructions for Long-Acting Products
Take your medication with food to help your body absorb it properly.
Avoid consuming alcohol, hot drinks, or spicy foods when it's time to take your medication.
Swallow the tablet whole - do not chew or crush it.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel well.
Important Notes for Long-Acting Tablets
Some long-acting tablets can be broken in half, but check with your doctor first to make sure.
The timing of when to take your medication may vary depending on the specific product. Some products should be taken at bedtime, while others can be taken at any time. Check with your pharmacist for specific guidance on when to take your medication.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom.
Keep all medications in a safe place, 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. Check with your pharmacist for guidance on the best way to dispose of your medication. You may also want to check if there are any drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember.
If it's close to the time for your next dose, skip the missed dose and return to your regular schedule.
Do not take two doses at the same time or take extra doses.
* If you stop taking your medication, be sure to talk to your doctor. You may need to restart at a lower dose and gradually increase it.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely.
Special Instructions for Long-Acting Products
Take your medication with food to help your body absorb it properly.
Avoid consuming alcohol, hot drinks, or spicy foods when it's time to take your medication.
Swallow the tablet whole - do not chew or crush it.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel well.
Important Notes for Long-Acting Tablets
Some long-acting tablets can be broken in half, but check with your doctor first to make sure.
The timing of when to take your medication may vary depending on the specific product. Some products should be taken at bedtime, while others can be taken at any time. Check with your pharmacist for specific guidance on when to take your medication.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom.
Keep all medications in a safe place, 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. Check with your pharmacist for guidance on the best way to dispose of your medication. You may also want to check if there are any drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember.
If it's close to the time for your next dose, skip the missed dose and return to your regular schedule.
Do not take two doses at the same time or take extra doses.
* If you stop taking your medication, be sure to talk to your doctor. You may need to restart at a lower dose and gradually increase it.
Lifestyle & Tips
- Take with a low-fat snack at bedtime to help reduce flushing.
- Avoid hot beverages, spicy foods, and alcohol around the time of dosing, as these can worsen flushing.
- Taking a low-dose aspirin (e.g., 325 mg) 30 minutes before niacin may help reduce flushing, but consult your doctor first.
- Maintain a heart-healthy diet and regular exercise as recommended by your doctor.
- Report any unusual muscle pain, weakness, dark urine, or yellowing of skin/eyes immediately.
Available Forms & Alternatives
Available Strengths:
- Niacin 250mg Tablets
- Niacin TR 1000mg Tablets
- Niacin 500mg Tablets
- Niacin 100mg Tablets
- Niacin 500mg SR Capsules
- Niacin ER 1000mg Tablets
- Niacin 750mg ER Tablets
- Niacin 500mg ER Tablets
- Niacin ER 1000mg Tablets
- Niacin 500mg ER Tablets
- Niacin 750mg ER Tablets
- Niacin 250mg TR Capsules
- Niacin 500mg TR Tablets
- Niacin 500mg TR Tablets
Dosing & Administration
Adult Dosing
Standard Dose:
Initial: 500 mg once daily at bedtime for 4 weeks; then increase to 1000 mg once daily at bedtime. Max: 2000 mg/day.
Dose Range:
500 - 2000 mg
Condition-Specific Dosing:
dyslipidemia:
Initial: 500 mg once daily at bedtime for 4 weeks; then increase to 1000 mg once daily at bedtime. May increase to 1500 mg/day after 4 weeks, then to 2000 mg/day after another 4 weeks, if tolerated and indicated. Administer with a low-fat snack at bedtime to reduce flushing.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not routinely recommended for dyslipidemia; specific dosing for deficiency states varies.
Adolescent:
Not routinely recommended for dyslipidemia; specific dosing for deficiency states varies.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment, but use with caution.
Moderate:
Use with caution; consider lower doses and increased monitoring of renal function and adverse effects.
Severe:
Contraindicated or use with extreme caution; significant risk of accumulation and toxicity.
Dialysis:
Not recommended; Niacin is not significantly removed by dialysis.
Hepatic Impairment:
Mild:
Use with caution; monitor liver function tests closely.
Moderate:
Contraindicated due to increased risk of hepatotoxicity.
Severe:
Contraindicated due to increased risk of hepatotoxicity.
Pharmacology
Mechanism of Action
Niacin (nicotinic acid) exerts its lipid-modifying effects primarily by inhibiting hepatic synthesis of very-low-density lipoproteins (VLDL), which leads to a reduction in plasma triglycerides and LDL-C. It also reduces the catabolism of apolipoprotein A-I, thereby increasing HDL-C levels. The controlled-release formulation aims to reduce the flushing side effect by providing a slower, more sustained release of niacin.
Pharmacokinetics
Absorption:
Bioavailability:
Highly variable (30-70%) due to first-pass metabolism; controlled-release formulations aim for more consistent absorption.
Tmax:
Approximately 4-5 hours for controlled-release formulations.
FoodEffect:
Food generally delays absorption and can reduce the severity of flushing.
Distribution:
Vd:
Not precisely quantified, but widely distributed.
ProteinBinding:
Low (<20%).
CnssPenetration:
Limited.
Elimination:
HalfLife:
Approximately 2-3 hours (variable, depends on dose and formulation).
Clearance:
Primarily hepatic metabolism and renal excretion.
ExcretionRoute:
Renal (as metabolites and unchanged drug).
Unchanged:
Small percentage (10-30%) excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Lipid-modifying effects are gradual, typically observed within weeks of initiating therapy.
PeakEffect:
Maximum lipid-modifying effects usually seen after several weeks to months of consistent dosing.
DurationOfAction:
Effects persist as long as therapy is continued.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Immediately
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:
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 high blood sugar, such as:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Frequent urination
+ Flushing
+ Rapid breathing
+ Fruity-smelling breath
Chest pain or pressure
Abnormal heartbeat
Dizziness or fainting
Shortness of breath
Excessive sweating
Black, tarry, or bloody stools
Muscle pain, tenderness, or weakness (with or without fever or feeling unwell), which can be a sign of a rare but serious muscle problem (rhabdomyolysis) that can lead to kidney problems and be life-threatening, especially when used with certain cholesterol-lowering medications like atorvastatin and simvastatin
Other Possible Side Effects
Most people experience no side effects or only mild side effects when taking this medication. However, if you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention:
Flushing (taking aspirin 30 minutes before taking this medication may help; if you experience flushing at night, get up slowly to avoid dizziness or fainting)
Itching
Diarrhea
Upset stomach or vomiting
Cough
Dry skin
* Headache
Reporting Side Effects
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.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:
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 high blood sugar, such as:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Frequent urination
+ Flushing
+ Rapid breathing
+ Fruity-smelling breath
Chest pain or pressure
Abnormal heartbeat
Dizziness or fainting
Shortness of breath
Excessive sweating
Black, tarry, or bloody stools
Muscle pain, tenderness, or weakness (with or without fever or feeling unwell), which can be a sign of a rare but serious muscle problem (rhabdomyolysis) that can lead to kidney problems and be life-threatening, especially when used with certain cholesterol-lowering medications like atorvastatin and simvastatin
Other Possible Side Effects
Most people experience no side effects or only mild side effects when taking this medication. However, if you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention:
Flushing (taking aspirin 30 minutes before taking this medication may help; if you experience flushing at night, get up slowly to avoid dizziness or fainting)
Itching
Diarrhea
Upset stomach or vomiting
Cough
Dry skin
* Headache
Reporting Side Effects
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:
- Severe or persistent flushing, itching, or tingling.
- Unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or dark urine.
- Yellowing of the skin or eyes (jaundice), dark urine, pale stools, or persistent nausea/vomiting (signs of liver problems).
- Severe stomach pain or persistent diarrhea.
- Swelling in the ankles or feet.
- Symptoms of gout (sudden, severe joint pain, redness, swelling).
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:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Bleeding problems
+ Liver problems or elevated liver enzymes
+ Ulcer disease
* If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other drugs and health conditions. Never start, stop, or adjust the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
Certain health conditions, including:
+ Bleeding problems
+ Liver problems or elevated liver enzymes
+ Ulcer disease
* If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other drugs and health conditions. Never start, stop, or adjust the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you have diabetes, you will need to closely monitor your blood sugar levels. Regularly undergo blood work and other laboratory tests as instructed by your doctor. Be aware that this medication may interfere with certain lab tests, so it is crucial to notify all your healthcare providers and laboratory personnel that you are taking this drug.
To maximize the effectiveness of this medication, adhere to the diet and exercise plan recommended by your doctor. When taking this medication, avoid taking colesevelam, colestipol, or cholestyramine within a 4-hour window before or after taking your dose.
Limit your alcohol consumption to fewer than 3 drinks per day, as excessive alcohol intake may increase your risk of developing liver disease. Additionally, be aware that alcohol may exacerbate flushing symptoms. Be vigilant for signs of gout attacks, which can be a potential side effect of this medication.
If you are 65 years or older, exercise caution when using this medication, as you may be more susceptible to side effects. If you are pregnant or planning to become pregnant, consult your doctor to discuss the potential benefits and risks of using this medication during pregnancy.
To maximize the effectiveness of this medication, adhere to the diet and exercise plan recommended by your doctor. When taking this medication, avoid taking colesevelam, colestipol, or cholestyramine within a 4-hour window before or after taking your dose.
Limit your alcohol consumption to fewer than 3 drinks per day, as excessive alcohol intake may increase your risk of developing liver disease. Additionally, be aware that alcohol may exacerbate flushing symptoms. Be vigilant for signs of gout attacks, which can be a potential side effect of this medication.
If you are 65 years or older, exercise caution when using this medication, as you may be more susceptible to side effects. If you are pregnant or planning to become pregnant, consult your doctor to discuss the potential benefits and risks of using this medication during pregnancy.
Overdose Information
Overdose Symptoms:
- Severe flushing
- Gastrointestinal distress (nausea, vomiting, diarrhea)
- Dizziness
- Hypotension
- Tachycardia
- Liver damage (in severe cases)
What to Do:
Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is supportive and symptomatic.
Drug Interactions
Contraindicated Interactions
- Active peptic ulcer disease
- Active hepatic disease or unexplained persistent elevations in liver function tests
Major Interactions
- Statins (HMG-CoA reductase inhibitors): Increased risk of myopathy/rhabdomyolysis, especially with higher doses of niacin (>1g/day) and potent statins.
- Bile acid sequestrants (e.g., cholestyramine, colestipol): May bind niacin and reduce its absorption. Administer niacin at least 4-6 hours after or 1 hour before sequestrants.
- Antihypertensive agents (e.g., ACE inhibitors, calcium channel blockers): May potentiate hypotensive effects, leading to orthostatic hypotension.
- Alcohol: May exacerbate flushing and increase risk of hepatotoxicity.
Moderate Interactions
- Aspirin: May exacerbate niacin-induced flushing.
- Anticoagulants/Antiplatelets (e.g., warfarin, clopidogrel): Niacin may prolong prothrombin time; monitor INR.
- Diabetes medications (e.g., insulin, oral hypoglycemics): Niacin can increase blood glucose levels, requiring adjustment of antidiabetic therapy.
- Allopurinol/Probenecid: Niacin can increase uric acid levels, potentially counteracting effects of uricosuric agents.
Minor Interactions
- Herbal supplements (e.g., ginkgo biloba, garlic): Potential for additive effects on bleeding or blood pressure.
Monitoring
Baseline Monitoring
Fasting Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Rationale: To establish baseline lipid levels and assess treatment efficacy.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST, Alkaline Phosphatase, Bilirubin)
Rationale: To assess baseline hepatic function due to risk of hepatotoxicity.
Timing: Prior to initiation of therapy.
Fasting Glucose
Rationale: Niacin can increase blood glucose levels.
Timing: Prior to initiation of therapy.
Uric Acid
Rationale: Niacin can increase uric acid levels, potentially leading to gout.
Timing: Prior to initiation of therapy.
Routine Monitoring
Liver Function Tests (ALT, AST)
Frequency: Every 6-12 weeks for the first year, then periodically (e.g., every 6-12 months) or as clinically indicated.
Target: Within normal limits (typically <3 times upper limit of normal).
Action Threshold: Discontinue if ALT/AST >3 times ULN or if accompanied by symptoms of liver injury.
Fasting Lipid Panel
Frequency: Every 6-12 weeks until desired lipid levels are achieved, then every 6-12 months.
Target: Individualized based on patient risk factors and treatment goals.
Action Threshold: Re-evaluate therapy if lipid goals are not met or if adverse effects occur.
Fasting Glucose
Frequency: Periodically (e.g., every 6-12 months) or as clinically indicated, especially in diabetic patients.
Target: Individualized based on patient's diabetic status.
Action Threshold: Adjust antidiabetic therapy if glucose levels become uncontrolled.
Uric Acid
Frequency: Periodically (e.g., every 6-12 months) or as clinically indicated, especially in patients with a history of gout.
Target: Within normal limits or individualized for gout patients.
Action Threshold: Consider allopurinol or discontinuation if symptomatic hyperuricemia or gout flares occur.
Symptom Monitoring
- Severe flushing (redness, warmth, itching, tingling)
- Gastrointestinal upset (nausea, vomiting, diarrhea, abdominal pain)
- Muscle pain, tenderness, or weakness (especially if co-administered with statins)
- Dark urine, yellowing of skin/eyes (jaundice) - signs of liver injury
- Unusual fatigue or weakness
- Swelling of ankles or feet
- Symptoms of gout (joint pain, swelling, redness)
Special Patient Groups
Pregnancy
Generally not recommended for the treatment of dyslipidemia during pregnancy due to limited data and the availability of safer alternatives. Niacin is a vitamin, but high doses for lipid-lowering are not typically indicated. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Limited data; potential for unknown risks.
Second Trimester:
Limited data; potential for unknown risks.
Third Trimester:
Limited data; potential for unknown risks.
Lactation
Niacin is excreted into breast milk. While generally considered compatible with breastfeeding at typical vitamin doses, high doses used for dyslipidemia may pose a risk to the infant. Monitor the infant for adverse effects. Use with caution, or consider alternative lipid-lowering therapies.
Infant Risk:
Low to moderate risk; potential for flushing, gastrointestinal upset in infant, or theoretical risk of liver effects at high maternal doses.
Pediatric Use
Safety and efficacy for lipid-lowering in pediatric patients are not well-established. Use is generally not recommended for dyslipidemia unless under specialist guidance for specific conditions (e.g., familial hypercholesterolemia) and when benefits outweigh risks. Dosing for niacin deficiency is different.
Geriatric Use
Elderly patients may be more susceptible to the adverse effects of niacin, particularly flushing, gastrointestinal upset, and hepatotoxicity. Initiate therapy at lower doses and titrate slowly with close monitoring of liver function and other adverse effects.
Clinical Information
Clinical Pearls
- Controlled-release niacin formulations are designed to reduce flushing compared to immediate-release, but hepatotoxicity risk may be higher with some SR formulations. Extended-release (ER) niacin (e.g., Niaspan) generally has a better tolerability and safety profile than generic SR forms.
- Always advise patients to take niacin with a low-fat snack at bedtime to minimize flushing and improve tolerability.
- Pre-treatment with a low-dose aspirin (e.g., 325 mg) 30 minutes before niacin can significantly reduce flushing for many patients.
- Strict adherence to liver function monitoring is crucial, especially during dose titration and the first year of therapy.
- Educate patients about the difference between niacin (nicotinic acid) and niacinamide (nicotinamide); niacinamide does not have lipid-lowering effects.
- Niacin can worsen glycemic control in diabetic patients and increase uric acid levels, potentially precipitating gout attacks. Monitor these parameters closely.
Alternative Therapies
- Statins (e.g., atorvastatin, rosuvastatin, simvastatin)
- Ezetimibe
- PCSK9 inhibitors (e.g., evolocumab, alirocumab)
- Fibrates (e.g., fenofibrate, gemfibrozil)
- Omega-3 fatty acid ethyl esters (e.g., icosapent ethyl, omega-3-acid ethyl esters)
- Bile acid sequestrants (e.g., cholestyramine, colesevelam)
- Adenosine triphosphate-citrate lyase (ACL) inhibitors (e.g., bempedoic acid)
Cost & Coverage
Average Cost:
$20 - $100+ per 30 capsules
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it is a good idea to consult with your pharmacist. 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 reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount consumed, and the time it occurred.