Niacin 250mg TR 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 B3
Pharmacologic Class
Nicotinic acid derivative; Vitamin
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) in your blood. This controlled-release form is designed to 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 taking your medication, as they may interfere with its absorption.
Swallow the medication 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.
Long-Acting Tablets
Some long-acting tablets can be broken in half, but check with your doctor first to confirm.
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. Consult with your pharmacist to determine the best schedule for 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 and secure location, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. Check with your pharmacist for guidance on the best way to dispose of your medication, and consider participating in a local drug take-back program.
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 resume your regular schedule.
Do not take two doses at the same time or take extra doses to make up for a missed dose.
* If you stop taking your medication, consult with your doctor before restarting. You may need to begin with a lower dose and gradually increase it to minimize potential side effects.
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 taking your medication, as they may interfere with its absorption.
Swallow the medication 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.
Long-Acting Tablets
Some long-acting tablets can be broken in half, but check with your doctor first to confirm.
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. Consult with your pharmacist to determine the best schedule for 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 and secure location, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. Check with your pharmacist for guidance on the best way to dispose of your medication, and consider participating in a local drug take-back program.
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 resume your regular schedule.
Do not take two doses at the same time or take extra doses to make up for a missed dose.
* If you stop taking your medication, consult with your doctor before restarting. You may need to begin with a lower dose and gradually increase it to minimize potential side effects.
Lifestyle & Tips
- Take exactly as prescribed, usually at bedtime with a low-fat snack to help reduce flushing and stomach upset.
- Avoid taking with hot beverages or alcohol, as these can worsen flushing.
- Do not crush, chew, or break the capsules; swallow them whole.
- Maintain a heart-healthy diet low in saturated and trans fats and cholesterol.
- Engage in regular physical activity as recommended by your doctor.
- Inform your doctor about all other medications, supplements, and herbal products you are taking.
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: 250 mg orally once daily at bedtime with a low-fat snack. Titrate gradually. Maintenance: 1000-2000 mg/day, typically divided into 1-2 doses.
Dose Range:
250 - 2000 mg
Condition-Specific Dosing:
hyperlipidemia:
Initial: 250 mg at bedtime. Increase by 250-500 mg every 4-7 days as tolerated, up to 1000-2000 mg/day. Max 2000 mg/day for controlled-release formulations due to hepatotoxicity risk.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established for hyperlipidemia; use only under specialist supervision for specific metabolic disorders.
Adolescent:
Not established for hyperlipidemia; use only under specialist supervision for specific metabolic disorders.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment, monitor for adverse effects.
Moderate:
Use with caution, consider lower doses and increased monitoring.
Severe:
Use with extreme caution; contraindicated in end-stage renal disease due to potential for accumulation and toxicity.
Dialysis:
Not recommended; Niacin is not significantly dialyzable.
Hepatic Impairment:
Mild:
Use with caution, monitor LFTs closely.
Moderate:
Contraindicated 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 plasma concentrations of triglycerides and LDL-C. It also reduces the catabolism of apolipoprotein A-I, thereby increasing HDL-C levels. The exact mechanism for HDL-C elevation is not fully understood but involves reduced hepatic uptake of apoA-I and HDL particles.
Pharmacokinetics
Absorption:
Bioavailability:
Variable, generally good. Controlled-release formulations have slower, more sustained absorption.
Tmax:
Controlled-release: 4-5 hours (range 3-12 hours)
FoodEffect:
Absorption is enhanced and flushing reduced when taken with food, especially a low-fat snack.
Distribution:
Vd:
Not precisely quantified for humans, widely distributed.
ProteinBinding:
Low (<20%)
CnssPenetration:
Limited
Elimination:
HalfLife:
Controlled-release: Approximately 2-4 hours (terminal half-life, but effective half-life for lipid effects is longer due to metabolic pathways)
Clearance:
Not precisely quantified, primarily hepatic metabolism.
ExcretionRoute:
Renal excretion of metabolites (primarily nicotinuric acid and nicotinamide).
Unchanged:
Small percentage (<10%)
Pharmacodynamics
OnsetOfAction:
Lipid-lowering effects are gradual, typically observed within weeks to months.
PeakEffect:
Maximum lipid-lowering effects usually seen after 3-6 weeks of stable dosing.
DurationOfAction:
Effects persist as long as therapy is continued.
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 immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes
Signs of high blood sugar: confusion, feeling sleepy, unusual 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 severe 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 or seek medical help:
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 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 or seek immediate medical attention:
Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat
Signs of liver problems: dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, vomiting, or yellow skin or eyes
Signs of high blood sugar: confusion, feeling sleepy, unusual 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 severe 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 or seek medical help:
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 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.
- Yellowing of the skin or eyes (jaundice), dark urine, or light-colored stools (signs of liver problems).
- Severe stomach pain, nausea, vomiting, or diarrhea.
- Swelling in your hands or feet.
- Sudden joint pain and swelling (signs of gout).
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, it is crucial 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 vital to notify all your healthcare providers and laboratory personnel that you are taking this drug.
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 this drug.
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.
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.
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 vital to notify all your healthcare providers and laboratory personnel that you are taking this drug.
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 this drug.
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.
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, itching, rash
- Gastrointestinal upset (nausea, vomiting, diarrhea)
- Dizziness, fainting
- Hypotension
- Liver dysfunction (elevated LFTs, jaundice)
- Hyperglycemia
- Hyperuricemia
What to Do:
Seek immediate medical attention or call a poison control center (1-800-222-1222). Treatment is supportive and symptomatic. Gastric lavage or activated charcoal may be considered if ingestion is recent.
Drug Interactions
Contraindicated Interactions
- Statins (HMG-CoA reductase inhibitors) - increased risk of myopathy/rhabdomyolysis, especially with controlled-release niacin. Co-administration generally not recommended unless benefits outweigh risks and patient is closely monitored.
- Alcohol (ethanol) - may exacerbate flushing and increase risk of hepatotoxicity.
Major Interactions
- 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, beta-blockers, calcium channel blockers) - may cause additive hypotensive effects.
- Antidiabetic agents (e.g., insulin, oral hypoglycemics) - niacin may increase blood glucose levels, requiring adjustment of antidiabetic therapy.
- Other hepatotoxic drugs (e.g., amiodarone, methotrexate) - increased risk of liver injury.
Moderate Interactions
- Aspirin - may reduce niacin-induced flushing, but high doses of aspirin may increase niacin levels and toxicity.
- Allopurinol - niacin may increase uric acid levels, potentially counteracting allopurinol's effect.
- Warfarin - theoretical risk of increased bleeding due to niacin's effect on platelet aggregation, monitor INR.
Minor Interactions
- Herbal supplements (e.g., red yeast rice) - potential for additive lipid effects or adverse reactions.
Monitoring
Baseline Monitoring
Liver Function Tests (LFTs): AST, ALT, alkaline phosphatase, bilirubin
Rationale: To establish baseline liver health and detect pre-existing hepatic impairment, as niacin can cause hepatotoxicity.
Timing: Prior to initiation of therapy.
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.
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 precipitating gout.
Timing: Prior to initiation of therapy.
Routine Monitoring
Liver Function Tests (LFTs): AST, ALT
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 or stable from baseline.
Action Threshold: Discontinue if ALT or AST persistently exceed 3 times the upper limit of normal (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: Adjust dose or consider alternative therapy if goals not met or adverse effects occur.
Fasting Glucose
Frequency: Periodically (e.g., every 3-6 months), especially in diabetic or pre-diabetic patients.
Target: Individualized.
Action Threshold: Adjust antidiabetic therapy or discontinue niacin if hyperglycemia is significant and persistent.
Uric Acid
Frequency: Periodically (e.g., every 3-6 months), especially in patients with a history of gout.
Target: Within normal limits or stable from baseline.
Action Threshold: Consider allopurinol or discontinue niacin if hyperuricemia is significant or gout flares occur.
Creatine Kinase (CK)
Frequency: If muscle pain, tenderness, or weakness occurs.
Target: Within normal limits.
Action Threshold: Discontinue niacin if CK levels are significantly elevated (e.g., >10x ULN) or if rhabdomyolysis is suspected.
Symptom Monitoring
- Severe flushing (redness, warmth, itching, tingling)
- Persistent or severe gastrointestinal upset (nausea, vomiting, diarrhea, abdominal pain)
- Unexplained muscle pain, tenderness, or weakness (signs of myopathy/rhabdomyolysis)
- Dark urine, yellowing of skin or eyes (jaundice), light-colored stools (signs of liver injury)
- Swelling of ankles or feet
- Shortness of breath, chest pain
- Signs of gout (joint pain, swelling, redness)
Special Patient Groups
Pregnancy
Generally not recommended for the treatment of hyperlipidemia during pregnancy due to lack of sufficient safety data and the availability of safer alternatives (e.g., diet and lifestyle modifications). Niacin is a vitamin, but doses used for lipid modification are pharmacological. Use only if clearly needed and benefits outweigh risks.
Trimester-Specific Risks:
First Trimester:
Potential for teratogenicity not well-established at pharmacological doses; generally avoided.
Second Trimester:
Limited data; generally avoided.
Third Trimester:
Limited data; generally avoided.
Lactation
Niacin is excreted in breast milk. While it is a vitamin, pharmacological doses may pose a risk to the infant. Use with caution; monitor infant for adverse effects. Consider alternative lipid-lowering therapies or temporary discontinuation of breastfeeding.
Infant Risk:
Low to moderate risk. Potential for flushing, gastrointestinal upset in infant. Long-term effects unknown.
Pediatric Use
Not generally recommended for routine treatment of hyperlipidemia in children due to limited safety and efficacy data. Use only in severe cases under the guidance of a lipid specialist or pediatric endocrinologist.
Geriatric Use
Use with caution. Start with lower doses and titrate slowly due to increased susceptibility to adverse effects (e.g., flushing, gastrointestinal upset, hepatotoxicity) and potential for polypharmacy. Monitor liver function, glucose, and uric acid closely.
Clinical Information
Clinical Pearls
- Controlled-release niacin formulations are designed to reduce flushing compared to immediate-release, but they may carry a higher risk of hepatotoxicity.
- To minimize flushing, advise patients to take niacin with a low-fat snack at bedtime and avoid hot beverages or alcohol around dosing time.
- Aspirin (325 mg) taken 30 minutes before niacin can help reduce flushing, but discuss this with the patient's physician due to potential for increased bleeding or other interactions.
- Emphasize the importance of regular monitoring of liver function tests, blood glucose, and uric acid, especially during dose titration.
- Educate patients on the signs and symptoms of serious adverse effects, particularly liver injury and muscle pain/weakness, and when to seek medical attention.
- Niacin's lipid-lowering effects are dose-dependent and require consistent adherence for optimal results.
Alternative Therapies
- Statins (HMG-CoA reductase inhibitors - e.g., atorvastatin, rosuvastatin, simvastatin)
- Fibrates (e.g., fenofibrate, gemfibrozil)
- Ezetimibe
- PCSK9 inhibitors (e.g., evolocumab, alirocumab)
- Bile acid sequestrants (e.g., cholestyramine, colesevelam)
- Omega-3 fatty acid ethyl esters (e.g., icosapent ethyl, omega-3-acid ethyl esters)
Cost & Coverage
Average Cost:
Varies widely by brand/generic and quantity per 30 capsules
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 for generic; Tier 3 or higher for brand-name if available.
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 for more information. 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. 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 taken, the amount, and the time it happened.