Niacin ER 1000mg 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
Pharmacologic Class
Vitamin (B3); Lipid-modifying agent
Pregnancy Category
Category C
FDA Approved
Apr 1997
DEA Schedule
Not Controlled
Overview
What is this medicine?
Niacin ER is a vitamin B3 medication used to help lower 'bad' cholesterol (LDL and triglycerides) and raise 'good' cholesterol (HDL) in your blood. It's an extended-release tablet, meaning it releases the medicine slowly over time to help reduce side effects like flushing.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, it's essential to follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication with food, and swallow the tablets whole without chewing or crushing them. Avoid consuming alcohol, hot drinks, or spicy foods when it's time to take your medication.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well. If you're unsure whether your medication can be broken 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 by your pharmacist. If you have questions about disposing of your medication, consult with your pharmacist, who may be aware of 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 extra doses. If you need to stop taking your medication, consult with your doctor, as you may need to restart at a lower dose and gradually increase it.
To get the most benefit from your medication, it's essential to follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. Take your medication with food, and swallow the tablets whole without chewing or crushing them. Avoid consuming alcohol, hot drinks, or spicy foods when it's time to take your medication.
Continue taking your medication as directed by your doctor or healthcare provider, even if you start feeling well. If you're unsure whether your medication can be broken 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 by your pharmacist. If you have questions about disposing of your medication, consult with your pharmacist, who may be aware of 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 extra doses. If you need to stop taking your medication, consult with your doctor, as you may need to restart at a lower dose and gradually increase it.
Lifestyle & Tips
- Take the tablet whole, do not crush, chew, or break it.
- Take at bedtime with a low-fat snack to minimize flushing and stomach upset.
- Avoid taking with hot beverages or alcohol, as this can worsen flushing.
- Avoid sudden changes in posture to prevent dizziness from potential blood pressure drop.
- Maintain a heart-healthy diet (low in saturated and trans fats, cholesterol).
- Engage in regular physical activity as advised by your doctor.
- Quit smoking if you smoke.
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 once daily at bedtime for 4 weeks. Maintenance: 1000-2000 mg once daily at bedtime. Max: 2000 mg/day.
Dose Range:
500 - 2000 mg
Condition-Specific Dosing:
Dyslipidemia:
Titrate dose gradually to minimize flushing and other side effects. Take with a low-fat snack at bedtime.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (Safety and efficacy not established in pediatric patients)
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, but use with caution.
Moderate:
Use with caution; monitor for adverse effects. Consider lower doses.
Severe:
Contraindicated in severe renal impairment (CrCl < 30 mL/min) due to increased risk of toxicity.
Dialysis:
Not recommended; Niacin is not significantly removed by dialysis.
Hepatic Impairment:
Mild:
Use with caution; monitor liver function closely.
Moderate:
Contraindicated in active liver disease or unexplained persistent elevations of serum transaminases.
Severe:
Contraindicated in active liver disease or unexplained persistent elevations of serum transaminases.
Pharmacology
Mechanism of Action
Niacin (nicotinic acid) exerts its lipid-modifying effects primarily by inhibiting the synthesis of VLDL (very-low-density lipoprotein) in the liver, which in turn reduces the synthesis of LDL (low-density lipoprotein). It also reduces the catabolism of HDL (high-density lipoprotein) apolipoprotein A-I, leading to increased HDL cholesterol levels. Additionally, it inhibits the release of free fatty acids from adipose tissue, reducing the substrate for hepatic triglyceride synthesis.
Pharmacokinetics
Absorption:
Bioavailability:
Highly variable (30-70%) due to first-pass metabolism; ER formulation improves consistency.
Tmax:
Approximately 4-5 hours for ER formulation.
FoodEffect:
Absorption is enhanced and flushing is reduced when taken with a low-fat snack at bedtime. Taking on an empty stomach or with hot beverages can increase 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 (typically <10%)
Pharmacodynamics
OnsetOfAction:
Lipid-lowering effects are gradual, typically observed within weeks.
PeakEffect:
Maximal lipid-lowering effects usually seen after several weeks to months of consistent dosing.
DurationOfAction:
Extended-release formulation provides sustained release over 8-12 hours.
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: 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, fast 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, although many people may not experience any or may only have mild symptoms. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
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.
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: 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, fast 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, although many people may not experience any or may only have mild symptoms. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
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 flushing, itching, or rash.
- Unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or dark urine (could be rhabdomyolysis).
- Yellowing of skin or eyes (jaundice), dark urine, light-colored stools, persistent nausea/vomiting, severe fatigue (signs of liver problems).
- Severe stomach pain, black or tarry stools (signs of peptic ulcer).
- Swelling in ankles or feet.
- New or worsening joint pain (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 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 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 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 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 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 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 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 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 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, alcohol may exacerbate flushing symptoms.
Be vigilant for signs of gout attacks, and if you experience any, seek medical attention promptly.
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 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, alcohol may exacerbate flushing symptoms.
Be vigilant for signs of gout attacks, and if you experience any, seek medical attention promptly.
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
- Hypotension
- Tachycardia
- Pruritus
- Burning sensation
- Headache
What to Do:
Seek immediate medical attention. There is no specific antidote. Treatment is supportive and symptomatic. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Contraindicated Interactions
- Active liver disease
- Active peptic ulcer disease
Major Interactions
- Statins (HMG-CoA reductase inhibitors): Increased risk of myopathy/rhabdomyolysis, especially with higher doses of niacin or statins.
- Bile acid sequestrants (e.g., cholestyramine, colestipol): May bind niacin and reduce its absorption. Administer niacin at least 4-6 hours after sequestrants.
- Alcohol: May exacerbate flushing and increase risk of hepatotoxicity.
Moderate Interactions
- Antihypertensive agents: May cause additive hypotensive effects.
- Aspirin: May reduce niacin-induced flushing, but high doses of aspirin may increase niacin levels.
- Allopurinol/Probenecid: Niacin may increase serum uric acid, potentially counteracting effects of uricosuric agents.
- Insulin/Oral hypoglycemic agents: Niacin may increase blood glucose levels, requiring adjustment of antidiabetic therapy.
Minor Interactions
- Herbal supplements (e.g., ginkgo biloba, garlic): Potential for additive antiplatelet effects.
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 and monitor for niacin-induced 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 precipitating gout.
Timing: Prior to initiation of therapy.
Routine Monitoring
Fasting Lipid Panel
Frequency: Every 6-12 weeks during titration, then every 6-12 months once stable.
Target: Individualized based on treatment goals (e.g., LDL-C < 100 mg/dL, HDL-C > 40 mg/dL, Triglycerides < 150 mg/dL).
Action Threshold: Lack of therapeutic response or worsening lipid profile.
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.
Action Threshold: Persistent elevations > 3 times the upper limit of normal (ULN) or any elevation accompanied by symptoms of liver injury (e.g., jaundice, fatigue, nausea).
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: Significant or persistent elevation requiring intervention.
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.
Action Threshold: Significant or persistent elevation, or onset of gout symptoms.
Symptom Monitoring
- Flushing (redness, warmth, itching, tingling)
- Pruritus (itching)
- Gastrointestinal upset (nausea, vomiting, diarrhea, dyspepsia)
- Myalgia (muscle pain), weakness, dark urine (rhabdomyolysis symptoms)
- Fatigue, jaundice, dark urine, light-colored stools (signs of liver injury)
- Dizziness, lightheadedness (hypotension)
- New onset or worsening of gout symptoms (joint pain, swelling)
Special Patient Groups
Pregnancy
Category C. Niacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. High doses may be associated with fetal abnormalities in animal studies.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm, use only if clearly needed.
Second Trimester:
Use with caution, monitor for maternal adverse effects.
Third Trimester:
Use with caution, monitor for maternal adverse effects.
Lactation
Niacin is excreted in breast milk. While generally considered compatible with breastfeeding at typical dietary intake levels, therapeutic doses for dyslipidemia may pose a risk to the infant. Use with caution; monitor infant for adverse effects (e.g., flushing, GI upset). Consider alternative lipid-lowering agents or temporary discontinuation of breastfeeding.
Infant Risk:
L3 (Moderately safe - possible mild adverse effects or insufficient data to rule out risk).
Pediatric Use
Safety and efficacy have not been established in pediatric patients. Use is generally not recommended.
Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Start with lower doses and titrate carefully due to potential for increased sensitivity to adverse effects (e.g., flushing, GI upset, hepatotoxicity). Monitor renal and hepatic function closely.
Clinical Information
Clinical Pearls
- To minimize flushing, advise patients to take niacin ER at bedtime with a low-fat snack. Avoid hot beverages or alcohol around the time of dosing.
- Pre-treatment with 325 mg (or 81 mg) of aspirin 30 minutes before the niacin dose can help reduce flushing, but this should be discussed with a healthcare provider due to bleeding risk.
- Patients should be advised that flushing is a common and usually transient side effect, often decreasing with continued use.
- Emphasize the importance of adherence to the gradual titration schedule to improve tolerability.
- Niacin ER should not be substituted for immediate-release or sustained-release niacin products on a milligram-for-milligram basis due to differences in absorption and potential for increased toxicity.
- Monitor for signs of liver toxicity (e.g., jaundice, dark urine, persistent nausea/vomiting) and muscle pain/weakness, especially when co-administered with statins.
Alternative Therapies
- Statins (e.g., Atorvastatin, Rosuvastatin, Simvastatin)
- Fibrates (e.g., Fenofibrate, Gemfibrozil)
- Ezetimibe
- PCSK9 inhibitors (e.g., Alirocumab, Evolocumab)
- 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, typically $50-$200+ per 30 tablets (1000mg ER)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 for generic; Tier 3 or higher for brand.
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 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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.