Niacin 500mg Tablets
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; B Vitamin
Pregnancy Category
Category C
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
Niacin, also known as Vitamin B3 or nicotinic acid, is a medication primarily used to help lower 'bad' cholesterol (LDL and triglycerides) and raise 'good' cholesterol (HDL) in your blood. It works by affecting how your body makes and processes fats. It can also be used to treat a condition called pellagra, which is caused by a lack of Vitamin B3.
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. Take your medication with food to help your body absorb it properly. When it's time to take your dose, avoid consuming alcohol, hot drinks, or spicy foods. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
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 location, out of the reach of children and pets. When your medication is no longer needed or has expired, dispose of it properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. If you have questions about disposing of your medication, ask your pharmacist for guidance. 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. 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 need to stop taking your medication, consult with your doctor first. You may need to restart your medication at a lower dose and gradually increase it to your previous dose.
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. Take your medication with food to help your body absorb it properly. When it's time to take your dose, avoid consuming alcohol, hot drinks, or spicy foods. Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
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 location, out of the reach of children and pets. When your medication is no longer needed or has expired, dispose of it properly. Do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist. If you have questions about disposing of your medication, ask your pharmacist for guidance. 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. 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 need to stop taking your medication, consult with your doctor first. You may need to restart your medication at a lower dose and gradually increase it to your previous dose.
Lifestyle & Tips
- Take niacin with a low-fat snack or meal to help reduce stomach upset and flushing.
- Avoid hot drinks, hot showers/baths, and alcohol around the time you take your dose, as these can worsen flushing.
- Taking a non-enteric coated aspirin (325 mg) about 30 minutes before your niacin dose may help reduce flushing. Consult your doctor first.
- Start with a low dose and gradually increase as directed by your doctor to minimize side effects.
- Do not crush, chew, or break extended-release or sustained-release tablets; swallow them whole.
- Maintain a healthy diet low in saturated and trans fats, and engage in regular physical activity as part of your cholesterol management plan.
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:
For dyslipidemia: Initial 250 mg once daily at bedtime, titrated gradually. Common maintenance doses range from 1000 mg to 2000 mg daily, divided.
Dose Range:
250 - 3000 mg
Condition-Specific Dosing:
dyslipidemia:
Initial 250 mg once daily at bedtime, increased by 250-500 mg every 4-7 days, not exceeding 2000 mg/day for immediate-release (IR) or 2000 mg/day for extended-release (ER). Max dose for some formulations can be 3000 mg/day.
pellagra:
50-100 mg three to six times daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not generally recommended for dyslipidemia; for pellagra, 100-300 mg/day in divided doses.
Adolescent:
Not generally recommended for dyslipidemia; for pellagra, 100-300 mg/day in divided doses.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment, but use with caution.
Moderate:
Use with caution; consider lower doses and closer monitoring.
Severe:
Use with caution; consider lower doses and closer monitoring. Contraindicated in end-stage renal disease.
Dialysis:
Not recommended in patients on dialysis due to potential for accumulation and toxicity.
Hepatic Impairment:
Mild:
Use with caution; monitor liver function closely.
Moderate:
Use with caution; consider lower doses and closer monitoring. Increased risk of hepatotoxicity.
Severe:
Contraindicated in patients with active liver disease or unexplained persistent elevations of serum transaminases.
Pharmacology
Mechanism of Action
Niacin (nicotinic acid) reduces hepatic synthesis of very-low-density lipoprotein (VLDL), which in turn reduces plasma concentrations of VLDL and low-density lipoprotein (LDL). It also reduces the catabolism of high-density lipoprotein (HDL) apolipoprotein A-I, thereby increasing HDL cholesterol concentrations. Additionally, it inhibits the mobilization of free fatty acids from adipose tissue, reducing the substrate for hepatic triglyceride synthesis.
Pharmacokinetics
Absorption:
Bioavailability:
Highly variable (30-70%) depending on formulation and dose.
Tmax:
Immediate-release (IR): 0.5-2 hours; Extended-release (ER): 4-5 hours.
FoodEffect:
Food can delay absorption and reduce peak concentrations, but may reduce flushing. Taking with a low-fat meal is often recommended.
Distribution:
Vd:
Not widely reported, but distributes into most body tissues.
ProteinBinding:
Low (<20%)
CnssPenetration:
Limited
Elimination:
HalfLife:
Immediate-release (IR): 0.9-1.4 hours; Extended-release (ER): 2-4.5 hours.
Clearance:
Highly variable, dose-dependent.
ExcretionRoute:
Renal (primarily as metabolites, small amount as unchanged drug).
Unchanged:
Varies with dose and formulation; typically <30% for IR, <12% for ER.
Pharmacodynamics
OnsetOfAction:
Lipid-lowering effects are gradual, typically seen within weeks to months.
PeakEffect:
Peak lipid-lowering effects usually observed after several weeks to months of consistent dosing.
DurationOfAction:
Dependent on formulation; IR has a shorter duration of effect on flushing, while lipid effects persist with regular dosing.
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 immediately or seek emergency medical attention:
Signs of an allergic reaction: rash, hives, itching, redness, swelling, blistering, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems: dark urine, fatigue, decreased appetite, stomach upset or pain, light-colored stools, vomiting, or yellowing of the skin or eyes
Signs of high blood sugar: confusion, drowsiness, excessive thirst or hunger, frequent urination, flushing, rapid breathing, or 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 may lead to kidney problems and can be life-threatening, especially when used with certain cholesterol-lowering medications like atorvastatin and simvastatin
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
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, stomach upset, or vomiting
Cough
Dry skin
Headache
Reporting Side Effects
This list is not exhaustive, and you may experience other 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 immediately or seek emergency medical attention:
Signs of an allergic reaction: rash, hives, itching, redness, swelling, blistering, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems: dark urine, fatigue, decreased appetite, stomach upset or pain, light-colored stools, vomiting, or yellowing of the skin or eyes
Signs of high blood sugar: confusion, drowsiness, excessive thirst or hunger, frequent urination, flushing, rapid breathing, or 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 may lead to kidney problems and can be life-threatening, especially when used with certain cholesterol-lowering medications like atorvastatin and simvastatin
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor:
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, stomach upset, or vomiting
Cough
Dry skin
Headache
Reporting Side Effects
This list is not exhaustive, and you may experience other 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 skin flushing, itching, or tingling.
- Unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or dark urine (signs of muscle damage).
- Yellowing of the skin or eyes (jaundice), dark urine, pale stools, or severe stomach pain (signs of liver problems).
- Severe nausea, vomiting, or diarrhea.
- Dizziness or lightheadedness.
- Signs of bleeding or unusual bruising (if also taking blood thinners).
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 medications and health conditions. Never start, stop, or adjust the dosage 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 medications and health conditions. Never start, stop, or adjust the dosage 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, it is crucial 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 notify all your healthcare providers and laboratory personnel that you are taking this drug.
To maximize the benefits 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 liver disease and exacerbate flushing symptoms. Be vigilant for signs of gout attacks, which may be triggered by 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 benefits 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 liver disease and exacerbate flushing symptoms. Be vigilant for signs of gout attacks, which may be triggered by 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 upset (nausea, vomiting, diarrhea)
- Dizziness
- Headache
- Itching
- Hypotension (low blood pressure)
What to Do:
In case of suspected overdose, seek immediate medical attention or call a poison control center. In the US, call 1-800-222-1222. Treatment is supportive and symptomatic.
Drug Interactions
Contraindicated Interactions
- Active liver disease
- Active peptic ulcer disease
- Arterial hemorrhage
Major Interactions
- Statins (HMG-CoA reductase inhibitors): Increased risk of myopathy/rhabdomyolysis. Co-administration should be done with caution and close monitoring, especially with higher doses of both agents.
- 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 bile acid sequestrants.
- Antihypertensive agents (e.g., ACE inhibitors, calcium channel blockers): May cause additive hypotensive effects, especially with initial niacin doses or dose increases.
- Alcohol: May exacerbate flushing and increase risk of hepatotoxicity.
Moderate Interactions
- Aspirin: May exacerbate niacin-induced flushing, but low-dose aspirin (325 mg) taken 30 minutes before niacin can reduce flushing.
- Antidiabetic agents (e.g., Insulin, oral hypoglycemics): Niacin may increase blood glucose levels, requiring adjustment of antidiabetic therapy.
- Gout medications (e.g., Allopurinol, Probenecid): Niacin may increase uric acid levels, potentially reducing the effectiveness of these agents or precipitating gout attacks.
- Warfarin: Niacin may prolong prothrombin time (PT) and increase INR, increasing bleeding risk. Monitor INR closely.
Minor Interactions
- Herbal supplements (e.g., Guggul, Red Yeast Rice): May have additive lipid-lowering effects or increase risk of adverse effects.
Monitoring
Baseline Monitoring
Fasting Lipid Panel (Total Cholesterol, LDL-C, HDL-C, Triglycerides)
Rationale: To establish baseline lipid levels and assess the need for therapy.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST, Alkaline Phosphatase, Bilirubin)
Rationale: To assess baseline liver function and identify pre-existing hepatic impairment, as niacin can cause hepatotoxicity.
Timing: Prior to initiation of therapy.
Fasting Blood Glucose (FBG) or HbA1c
Rationale: Niacin can increase blood glucose levels.
Timing: Prior to initiation of therapy.
Uric Acid
Rationale: Niacin can increase uric acid levels, potentially precipitating gout.
Timing: Prior to initiation of therapy.
Routine Monitoring
Liver Function Tests (ALT, AST)
Frequency: Every 6-12 weeks for the first year of therapy, then periodically (e.g., every 6-12 months) or as clinically indicated.
Target: Within normal limits or stable from baseline.
Action Threshold: Discontinue if persistent elevations >3 times the upper limit of normal (ULN) occur, or if accompanied by symptoms of liver injury.
Fasting Lipid Panel
Frequency: Every 6-12 weeks after dose stabilization, then periodically (e.g., every 6-12 months) to assess therapeutic response.
Target: Achieve target lipid levels based on patient risk assessment.
Action Threshold: Re-evaluate therapy if target lipid levels are not achieved or if adverse effects outweigh benefits.
Fasting Blood Glucose or HbA1c
Frequency: Periodically (e.g., every 6-12 months) or more frequently in diabetic patients.
Target: Maintain within target range for glycemic control.
Action Threshold: Adjust antidiabetic therapy or re-evaluate niacin if glucose levels become uncontrolled.
Uric Acid
Frequency: Periodically (e.g., every 6-12 months) or if symptoms of gout develop.
Target: Within normal limits.
Action Threshold: Consider dose reduction or discontinuation if uric acid levels are significantly elevated or if gout attacks occur.
Symptom Monitoring
- Severe flushing (redness, warmth, itching, tingling)
- Persistent or severe gastrointestinal upset (nausea, vomiting, diarrhea, abdominal pain)
- Unexplained muscle pain, tenderness, or weakness (especially if accompanied by fever or malaise)
- Dark urine, yellowing of skin or eyes (jaundice)
- Loss of appetite
- Unusual fatigue
- Dizziness or lightheadedness
- Signs of bleeding or bruising (if on anticoagulants)
Special Patient Groups
Pregnancy
Niacin is classified as Pregnancy Category C. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. While niacin is a vitamin, high pharmacological doses used for dyslipidemia are not typically recommended unless clearly indicated and benefits outweigh risks.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm not definitively established at pharmacological doses; use with caution.
Second Trimester:
Use with caution; monitor for maternal adverse effects.
Third Trimester:
Use with caution; monitor for maternal adverse effects.
Lactation
Niacin is excreted into breast milk. While normal dietary amounts are safe, pharmacological doses used for dyslipidemia should be used with caution. The American Academy of Pediatrics considers niacin compatible with breastfeeding, but monitoring for infant side effects is prudent.
Infant Risk:
Low risk at typical doses, but potential for adverse effects in the infant at high pharmacological doses. Monitor for flushing, gastrointestinal upset.
Pediatric Use
Safety and efficacy for dyslipidemia in pediatric patients have not been established. Use is generally not recommended for lipid-lowering in children, except in specific cases of severe familial dyslipidemia under specialist supervision. For pellagra, specific pediatric dosing exists.
Geriatric Use
Elderly patients may be more susceptible to the adverse effects of niacin, particularly flushing, gastrointestinal upset, and hepatotoxicity. Start with lower doses and titrate more slowly. Close monitoring of liver function, glucose, and uric acid is recommended.
Clinical Information
Clinical Pearls
- Flushing is the most common side effect and can be significantly reduced by starting with a low dose and titrating slowly, taking aspirin 30 minutes before the dose, taking niacin with food, and avoiding hot beverages or alcohol around dosing.
- Sustained-release (SR) and extended-release (ER) formulations generally cause less flushing but may have a higher risk of hepatotoxicity compared to immediate-release (IR) niacin, especially at higher doses. Liver function tests must be monitored regularly.
- Niacin can increase blood glucose and uric acid levels, requiring careful monitoring in patients with diabetes or gout.
- Patients should be educated on the importance of adherence to the titration schedule and reporting any severe or persistent side effects.
- Niacin's primary role in dyslipidemia management has shifted with the advent of more effective and safer agents like statins. It is often considered for patients who cannot tolerate statins or as an add-on therapy for specific lipid abnormalities (e.g., very high triglycerides, low HDL) after statin therapy is optimized.
Alternative Therapies
- Statins (e.g., Atorvastatin, Rosuvastatin, Simvastatin, Pravastatin, Lovastatin, Fluvastatin, Pitavastatin)
- Fibrates (e.g., Fenofibrate, Gemfibrozil)
- PCSK9 Inhibitors (e.g., Alirocumab, Evolocumab)
- Ezetimibe
- Bile Acid Sequestrants (e.g., Cholestyramine, Colestipol, Colesevelam)
- Omega-3 Fatty Acid Esters (e.g., Icosapent ethyl, Omega-3-acid ethyl esters)
Cost & Coverage
Average Cost:
Varies widely, typically $10-$50 per 30 tablets (generic 500mg IR)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or 2 for generic formulations; higher tiers for brand-name extended-release formulations.
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 information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to ensure you receive the best possible care.