Niacin 500mg ER Tablets
It is used to lower bad cholesterol, lower triglycerides, and raise good cholesterol (HDL).It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antihyperlipidemic, Vitamin B3
Pharmacologic Class
Nicotinic acid derivative, Lipid-modifying agent
Pregnancy Category
Category C
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Niacin is a B vitamin (B3) that, at higher doses, can help improve cholesterol levels by lowering 'bad' cholesterol (LDL and triglycerides) and raising 'good' cholesterol (HDL). The extended-release (ER) form helps 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 precisely. Take your medication with food, swallowing the tablet whole without chewing or crushing it. Avoid consuming alcohol, hot drinks, or spicy foods when taking your medication.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well. If you have any questions about breaking your tablet in half, consult with your doctor. Some products are designed to be taken at bedtime, while others can be taken at any time. Check with your pharmacist to confirm the best time to take your medication.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe 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. If you have questions about disposing of your medication, consult with your pharmacist. You may also want to check if there are 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. However, if it's close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses. If you stop taking your medication, consult with your doctor, as you may need to restart with 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 precisely. Take your medication with food, swallowing the tablet whole without chewing or crushing it. Avoid consuming alcohol, hot drinks, or spicy foods when taking your medication.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well. If you have any questions about breaking your tablet in half, consult with your doctor. Some products are designed to be taken at bedtime, while others can be taken at any time. Check with your pharmacist to confirm the best time to take your medication.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe 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. If you have questions about disposing of your medication, consult with your pharmacist. You may also want to check if there are 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. However, if it's close to the time for your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses. If you stop taking your medication, consult with your doctor, as you may need to restart with a lower dose and gradually increase it.
Lifestyle & Tips
- Take Niacin ER at bedtime after a low-fat snack to help reduce flushing and stomach upset.
- Avoid taking with hot beverages or alcohol, as these can worsen flushing.
- Consider taking a low-dose aspirin (e.g., 325 mg or 81 mg) 30 minutes before your niacin dose, as directed by your doctor, to help reduce flushing.
- Maintain a heart-healthy diet low in saturated and trans fats and cholesterol.
- Engage in regular physical activity.
- Quit smoking if applicable.
- Limit alcohol intake.
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 orally once daily at bedtime for 4 weeks; then 1000 mg orally once daily at bedtime for 4 weeks; then 1500 mg orally once daily at bedtime for 4 weeks; then 2000 mg orally once daily at bedtime. Titrate slowly to minimize flushing.
Dose Range:
500 - 2000 mg
Condition-Specific Dosing:
dyslipidemia:
As above, titrated to response and tolerability.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (Safety and efficacy not established for Niacin ER in pediatric patients.)
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment generally required, but monitor for adverse effects.
Moderate:
Use with caution; consider lower starting doses and slower titration. Monitor renal function and adverse effects closely.
Severe:
Contraindicated or not recommended due to increased risk of toxicity (e.g., rhabdomyolysis, hepatotoxicity).
Dialysis:
Not recommended; Niacin is not significantly removed by dialysis.
Hepatic Impairment:
Mild:
Use with caution; monitor liver function tests closely.
Moderate:
Contraindicated or not recommended due to increased risk of hepatotoxicity.
Severe:
Contraindicated due to increased risk of hepatotoxicity.
Pharmacology
Mechanism of Action
Niacin (nicotinic acid) reduces hepatic synthesis of very-low-density lipoprotein (VLDL), which in turn reduces LDL-C. It also reduces the catabolism of apoA-I, thereby increasing HDL-C levels. The exact mechanism for its lipid-modifying effects is not fully understood but involves binding to the GPR109A receptor (HM74A) on adipocytes, leading to reduced free fatty acid release, and inhibition of diacylglycerol acyltransferase-2 (DGAT2) in the liver, which reduces triglyceride synthesis.
Pharmacokinetics
Absorption:
Bioavailability:
Variable (ER formulation designed for sustained release)
Tmax:
Approximately 5 hours (for Niaspan ER)
FoodEffect:
Food significantly increases absorption and reduces flushing. Should be taken at bedtime after a low-fat snack.
Distribution:
Vd:
Not readily available for ER formulation, but generally distributes widely.
ProteinBinding:
Low (<20%)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2-3 hours (for Niaspan ER)
Clearance:
Not readily available
ExcretionRoute:
Renal (primarily as metabolites)
Unchanged:
Small percentage (typically <10%)
Pharmacodynamics
OnsetOfAction:
Lipid effects are gradual, typically seen over weeks to months.
PeakEffect:
Lipid-lowering effects peak after several weeks to months of consistent dosing.
DurationOfAction:
24 hours (due to ER formulation)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
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 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 high blood sugar, such as:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Passing urine more often
+ Flushing
+ Fast breathing
+ Breath that smells like fruit
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 either no side effects or only mild ones. However, if you notice any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Flushing (taking aspirin 30 minutes before taking this medication may help; if you wake up at night with flushing, get up slowly if you feel dizzy or lightheaded)
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 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 high blood sugar, such as:
+ Confusion
+ Feeling sleepy
+ Unusual thirst or hunger
+ Passing urine more often
+ Flushing
+ Fast breathing
+ Breath that smells like fruit
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 either no side effects or only mild ones. However, if you notice any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Flushing (taking aspirin 30 minutes before taking this medication may help; if you wake up at night with flushing, get up slowly if you feel dizzy or lightheaded)
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 rash.
- Unexplained muscle pain, tenderness, or weakness (especially with fever or dark urine) - could be rhabdomyolysis.
- Yellowing of skin or eyes (jaundice), dark urine, unusual fatigue, loss of appetite, or pain in the upper right abdomen - signs of liver problems.
- Severe stomach pain, nausea, or vomiting.
- Swelling of the face, lips, tongue, or throat; difficulty breathing (signs of allergic reaction).
- New or worsening joint pain (gout flare).
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 allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Bleeding problems
+ Liver problems or elevated liver enzymes
+ Ulcer disease
* If you are breast-feeding, as you should not breast-feed 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 problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change 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 allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Bleeding problems
+ Liver problems or elevated liver enzymes
+ Ulcer disease
* If you are breast-feeding, as you should not breast-feed 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 problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change 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 directed 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 and exacerbate flushing symptoms.
Be vigilant for signs of gout attacks while taking this medication. If you are 65 years or older, exercise caution when using this drug, 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 and exacerbate flushing symptoms.
Be vigilant for signs of gout attacks while taking this medication. If you are 65 years or older, exercise caution when using this drug, 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
- Hepatotoxicity
What to Do:
Seek immediate medical attention. Call 911 or Poison Control (1-800-222-1222). Treatment is supportive and symptomatic.
Drug Interactions
Contraindicated Interactions
- Statins (high doses of niacin with statins significantly increase risk of myopathy/rhabdomyolysis, especially with simvastatin >20mg/day)
- Alcohol (increases flushing and risk of hepatotoxicity)
- Anticoagulants (may increase bleeding risk)
Major Interactions
- Bile acid sequestrants (e.g., cholestyramine, colestipol - reduce niacin absorption; administer niacin 4-6 hours after or 1 hour before sequestrants)
- Antihypertensive agents (additive hypotensive effects)
- Aspirin (may potentiate flushing, but low-dose aspirin can be used to mitigate flushing)
- Insulin/Oral Hypoglycemics (may increase blood glucose, requiring dose adjustment of antidiabetic agents)
Moderate Interactions
- Allopurinol/Probenecid (niacin may increase uric acid levels, potentially counteracting gout medications)
- Herbal supplements (e.g., ginkgo biloba, garlic - may increase bleeding risk)
Minor Interactions
- Hot beverages/spicy foods (may exacerbate flushing)
Monitoring
Baseline Monitoring
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/HbA1c
Rationale: Niacin can increase blood glucose levels.
Timing: Prior to initiation of therapy.
Uric Acid
Rationale: Niacin can increase uric acid levels, potentially exacerbating gout.
Timing: Prior to initiation of therapy.
Routine Monitoring
Lipid Panel
Frequency: Every 6-12 weeks during titration, then every 6-12 months once stable.
Target: Individualized based on patient risk factors and guidelines (e.g., LDL-C <100 mg/dL, HDL-C >40-60 mg/dL, Triglycerides <150 mg/dL).
Action Threshold: Lack of desired lipid improvement, or significant adverse changes in lipid profile.
Liver Function Tests (ALT, AST)
Frequency: Every 6-12 weeks during the first year of therapy or during dose titration, then periodically (e.g., every 6-12 months) thereafter.
Target: Within normal limits.
Action Threshold: Persistent elevations >3 times the upper limit of normal (ULN) or any elevation accompanied by symptoms of liver injury (e.g., fatigue, nausea, dark urine, jaundice).
Fasting Glucose/HbA1c
Frequency: Periodically (e.g., every 6-12 months), more frequently in diabetic patients.
Target: Individualized.
Action Threshold: Significant or persistent increase in blood glucose levels.
Uric Acid
Frequency: Periodically (e.g., every 6-12 months), more frequently in patients with history of gout.
Target: Within normal limits.
Action Threshold: Significant or persistent increase in uric acid levels, or onset/exacerbation of gout symptoms.
Symptom Monitoring
- Flushing (redness, warmth, itching, tingling)
- Pruritus (itching)
- Gastrointestinal upset (nausea, vomiting, diarrhea, dyspepsia)
- Headache
- Dizziness
- Muscle pain or weakness (signs of myopathy/rhabdomyolysis)
- Symptoms of liver injury (unusual fatigue, anorexia, right upper quadrant pain, dark urine, jaundice)
- Symptoms of gout (joint pain, swelling, redness)
- Symptoms of hyperglycemia (increased thirst, urination, fatigue)
Special Patient Groups
Pregnancy
Niacin is Category C. Use only if the potential benefit justifies the potential risk to the fetus. High doses should be avoided.
Trimester-Specific Risks:
First Trimester:
Limited data, but generally avoided unless clearly needed.
Second Trimester:
Limited data, use with caution.
Third Trimester:
Limited data, use with caution.
Lactation
Niacin is excreted in breast milk. The American Academy of Pediatrics considers niacin compatible with breastfeeding. However, high doses should be used with caution due to potential for adverse effects in the infant (e.g., flushing, gastrointestinal upset). Monitor infant for adverse effects.
Infant Risk:
Low to Moderate (L3)
Pediatric Use
Safety and efficacy not established in pediatric patients. Generally not recommended for lipid modification in children.
Geriatric Use
Use with caution in elderly patients due to increased susceptibility to adverse effects (e.g., flushing, gastrointestinal upset, hepatotoxicity, myopathy). Start with lower doses and titrate slowly. Monitor closely for adverse reactions and drug interactions.
Clinical Information
Clinical Pearls
- Niacin ER is preferred over immediate-release (IR) niacin due to a significantly lower incidence of flushing and hepatotoxicity, allowing for higher, more effective doses.
- To minimize flushing, advise patients to take niacin ER at bedtime after a low-fat snack. Pre-treatment with aspirin (325 mg or 81 mg) 30 minutes before the niacin dose can also help.
- Educate patients that flushing is a common, usually harmless side effect that often diminishes over time with continued use.
- Monitor liver function tests (LFTs) closely, especially during the first year of therapy and with dose increases, as hepatotoxicity is a known risk.
- Caution patients about the increased risk of myopathy/rhabdomyolysis when niacin is co-administered with statins, particularly at higher doses of simvastatin.
- Niacin can increase blood glucose and uric acid levels; monitor these parameters, especially in patients with diabetes or gout.
Alternative Therapies
- Statins (e.g., atorvastatin, rosuvastatin, simvastatin)
- Fibrates (e.g., fenofibrate, gemfibrozil)
- Ezetimibe
- PCSK9 inhibitors (e.g., evolocumab, alirocumab)
- Bile acid sequestrants (e.g., cholestyramine, colestipol)
- Omega-3 fatty acid ethyl esters (e.g., icosapent ethyl, omega-3-acid ethyl esters)
Cost & Coverage
Average Cost:
Varies, typically $20-$100 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's 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 be sure to check with your pharmacist for more details. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider for clarification. 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 information about the medication taken, the amount, and the time it happened.