What Is the Connection Between Niacin and Triglycerides?

Nicotinic acid sustained-release tablets, the indication is that for patients at high risk of cardiovascular disease due to hypercholesterolemia, the use of lipid-lowering drugs is just one of many interventions. Nicotinic acid treatment can be used when diet therapy and other non-drug methods that limit saturated fatty acid and cholesterol intake alone do not work. Prior to niacin treatment, secondary causes of hypercholesterolemia (such as difficult-to-control diabetes, hypothyroidism, nephrotic syndrome, dysproteinemia, obstructive liver disease, cholesterol levels caused by other drugs should be ruled out Elevated, alcoholism), and total blood cholesterol, HDL-C and triglycerides should be measured.

Nicotinic acid sustained-release tablets, the indication is that for patients at high risk of cardiovascular disease due to hypercholesterolemia, the use of lipid-lowering drugs is just one of many interventions. Nicotinic acid treatment can be used when diet therapy and other non-drug methods that limit saturated fatty acid and cholesterol intake alone do not work. Prior to niacin treatment, secondary causes of hypercholesterolemia (such as difficult-to-control diabetes, hypothyroidism, nephrotic syndrome, dysproteinemia, obstructive liver disease, cholesterol levels caused by other drugs should be ruled out Elevated, alcoholism), and total blood cholesterol, HDL-C and triglycerides should be measured.

Drug Name

Niacin Sustained Release Tablets

Drug type

Prescription drugs, medicines for medical workers' injuries

Use classification

Other vitamin supplements

Niacin sustained release tablets ingredients

The main ingredients and chemical names of this product are:
Main ingredients: Nicotinic acid Chemical name: Pyridine-3-carboxylic acid Chemical structural formula:

Molecular formula: C ₆ H ₅ NO ₂
Molecular weight: 123.11

Properties of Niacin Sustained Release Tablets

It is a special-shaped film-coated tablet. After removing the coating, it is white or off-white.

Niacin sustained-release tablets

For patients at high risk of cardiovascular disease due to hypercholesterolemia, treatment with lipid-lowering drugs is just one of many interventions. Nicotinic acid treatment can be used when diet therapy and other non-drug methods that limit saturated fatty acid and cholesterol intake alone do not work. Prior to niacin treatment, secondary causes of hypercholesterolemia (such as difficult-to-control diabetes, hypothyroidism, nephrotic syndrome, dysproteinemia, obstructive liver disease, cholesterol levels caused by other drugs should be ruled out Elevated, alcoholism), and total blood cholesterol, HDL-C and triglycerides should be measured.
1. If the diet therapy does not work, patients with primary hypercholesterolemia and mixed dyslipidemia (type a, b, see table) can use this product as an adjuvant to reduce elevated total cholesterol and low-density lipids. Protein cholesterol, apolipoprotein B and triglyceride levels, and increase high density lipoprotein levels.
2. In adult patients with primary hypercholesterolemia (type a, see table), when the diet or diet plus monotherapy is not effective, this product can be combined with bile acid binding resin, as an adjuvant treatment of diet, to Reduce elevated total cholesterol and low-density lipoprotein cholesterol levels.
3. This product can also be used as an adjuvant therapy for adult patients who are at high risk of pancreatitis and whose serum triglyceride levels are not ideal for diet therapy (types IV and V hyperlipidemia, see table). . Typical patients have serum triglyceride levels in excess of 2000 mg / dL and elevated low-density lipoprotein cholesterol and fasting chylomicrons (V-type hyperlipidemia, see table). Patients with serum or plasma total triglyceride levels consistently below 1000 mg / dL are unlikely to develop pancreatitis. For patients with a history of pancreatitis or recurrence of typical abdominal pain typical of pancreatitis, if triglyceride levels are between 1000-2000 mg / dL, niacin treatment may need to be considered. Some type IV patients with triglyceride levels below 1000 mg / dL can be converted to type V patients with significantly increased triglycerides and chylomicrons due to poor diet control or alcohol abuse. In this case, use niacin Whether the risk of pancreatitis can be reduced has not been fully studied. This product is not suitable for type I hyperlipoproteinemia (elevated chylomicrons, plasma triglycerides, but normal low-density lipoprotein cholesterol levels). Plasma refrigerated for 14 hours can help distinguish between type I, type IV, and type V hyperlipidemia.
4. For patients with a history of myocardial infarction and hypercholesterolemia, niacin can reduce the risk of non-fatal myocardial infarction recurrence.

5. For patients with a history of coronary artery disease (CAD) and hypercholesterolemia, the combined use of niacin and bile acid resin can delay the progression of atherosclerosis or promote the regression of atherosclerotic lesions.
Table Types of Hyperlipidemia Types of Elevated Lipoprotein Components Elevated Lipids Major Secondary I (Rare) Chyle Microparticles TG , TC
IIa LDL TC-
IIb LDL, VLDL TC TG
III (rare) IDL TC / TG-
IV VLDL TG , TC
V (rare) chylomicrons, VLDL TG , TC
TC: total cholesterol; TG: triglycerides; LDL: low density lipoprotein VLDL: very low density lipoprotein IDL: medium density lipoprotein : increased : no change.

Niacin sustained release tablets specifications

0.5g

Niacin sustained-release tablets

This product must be swallowed whole, not split or chewed.
This product should be taken before going to bed after a low-fat diet.
Oral, the recommended dosage is 1 tablet (0.5g) once a week for 1-4 weeks, once a day; the dosage is 2 tablets (1g) once a day for 5-8 weeks. After 8 weeks, depending on the patient's efficacy and tolerance, the maximum dose can be increased to a maximum of 4 tablets (2g) per day if necessary.
Maintenance dose The recommended maintenance dose is 1g-2g (2-4 tablets) daily before bedtime. It is not recommended that daily doses exceed 2 g (4 tablets), and female patients have lower doses than male patients.
If a single treatment of this product is not effective or tolerates higher doses of this product, these patients can be treated with this product in combination with bile acid resin or HMG-COA reductase inhibitor.
Taking aspirin or other non-steroidal anti-inflammatory drugs 30 minutes before taking this product can reduce the frequency or severity of skin flushing (see Adverse Reactions). After a few weeks, the patient quickly tolerated flushing of the skin. Increasing the dose of niacin and avoiding fasting can also greatly reduce side effects such as skin flushing, itching, and gastrointestinal discomfort.
Patients already taking other nicotinic acid preparations should start taking the doses in the recommended starting dose table, and the dose depends on the individual patient's efficacy. If this product is discontinued for a longer period of time, recovery therapy should include the initial phase.

Nicotinic acid sustained-release tablets adverse reactions

General tolerance to this product is good, side effects are mild and transient. Common side effects are skin flushing (such as feeling warm, redness, itching, or tingling), which can be accompanied by dizziness, tachycardia, palpitations, shortness of breath, sweating, chills, and / or edema. May cause syncope. Other adverse reactions include abdominal pain, diarrhea, indigestion and rash, occasionally nausea, vomiting and rhinitis. The incidence of adverse reactions is generally higher in female patients than in males.
During clinical research or routine treatment, the following adverse reactions have also been reported in the application of niacin preparations:
Systemic symptoms: edema, general weakness, chills;
Cardiovascular: Atrial fibrillation and other arrhythmias, tachycardia, palpitations, orthostatic hypotension;
Eyes: toxic amblyopia, cystic plaque edema;
Gastrointestinal tract: active peptic ulcer, jaundice;
Metabolism: impaired glucose tolerance, gout;
Musculoskeletal: myalgia;
Nerves: dizziness, insomnia;
Skin: hyperpigmentation, black acanthosis, maculopapular urticaria, dry skin, sweating;
Other: Migraine.
[u] Clinical laboratory abnormalities [/ u]
Blood biochemistry: serum transaminase (see [u] precautions [/ u]), low-density lipoprotein, fasting blood glucose, uric acid, total bilirubin, elevated amylase, and decreased blood phosphorus;
Blood: Decreased platelet count, prolonged prothrombin time (see [u] Precautions [/ u]).

Taboo of Niacin Sustained Release Tablets

People who are allergic to niacin or any other ingredient in this product; patients with severe or unexplained liver dysfunction; patients with active peptic ulcer or arterial bleeding.

Notes on Niacin Sustained Release Tablets

1. This product cannot be replaced with an equivalent dose of a fast-acting niacin formulation. For patients who switched from taking immediate-release niacin to this product, they should start with a low dose and then gradually increase the dose to produce a better effect. Severe liver toxicity, including explosive hepatic necrosis, has occurred in patients with equivalent-dose immediate-release niacin preparations replacing niacin extended-release preparations.
Patients who drink a lot of alcohol and / or have a history of liver disease should use this product with caution. Patients with active liver disease or an elevated aminotransferase of unknown cause should not use this product.
During the treatment of this product, pay attention to liver function tests. Serum transaminase should be checked regularly (about 6 months) before treatment, every 6-12 weeks in the first year, and after 1 year. Special attention needs to be paid to patients with elevated aminotransferases, which should be reviewed immediately and the frequency of examinations should be increased. This product should be discontinued if the performance continues to increase, especially if it has risen to 3 times the upper limit of normal values and persists, or accompanied by vomiting, fever and / or physical discomfort.
2. A few cases of rhabdomyolysis are related to the combined application of niacin (1g / day) and HMG-COA reductase inhibitors. Doctors should carefully weigh the pros and cons when using this product in combination with HMG-COA reductase inhibitors, and closely monitor patients for signs or symptoms of muscle pain, tenderness, weakness, especially during the first few months of administration and increase During a drug dose. In the meantime, doctors should consider regular monitoring of serum creatine phosphokinase and potassium, but there is no guarantee that it will prevent severe myopathy.
3. Patients with jaundice hepatitis, hepatobiliary disease, diabetes or peptic ulcer should strictly monitor liver function and blood sugar during taking nicotinic acid sustained-release tablets to avoid serious adverse reactions.
If patients have unstable angina pectoris or are in the acute phase of myocardial infarction, especially when these patients are also taking cardiovascular drugs (such as nitrates, calcium channel blockers, epinephrine blockers), they should be used with caution Niacin extended release tablets.
4. Nicotinic acid has been used in patients with elevated uric acid, and patients with gout tendency should be used with caution.
5. Nicotinic acid sustained-release tablets showed statistically significant dose-dependent reductions in platelet counts (average 11% reduction in platelet counts at a dose of 2g) and prolonged prothrombin time (approximately 4%). Therefore, patients who are preparing for surgery should be carefully evaluated. When nicotinic acid sustained-release tablets are used in combination with anticoagulants, attention should be paid to closely monitoring prothrombin time and platelet count.
6. Placebo-controlled studies have shown that nicotinic acid sustained-release tablets are associated with dose-related reductions in blood phosphorus. Although the reduction is temporary, patients at risk of developing hypophosphatemia should regularly monitor blood phosphorus levels.
7. Nicotinic acid is mainly metabolized in the liver and excreted mainly by the kidneys, so patients with liver or kidney disease should take medication under the guidance of a physician.
8. After taking a low-fat meal, take this product before bedtime, generally do not take this product on an empty stomach.
9. This product should be taken strictly in accordance with the medication and dosage requirements to avoid serious adverse reactions.
10. After stopping niacin sustained-release tablets for a period of time, the treatment plan should be re-determined under the guidance of a physician.
11. If the patient is taking a nutritional supplement containing niacin or nicotinamide, the physician should be informed to determine the dosage.
12. Niacin sustained-release tablets should be swallowed whole, not crushed or broken apart.

Niacin sustained-release tablets for pregnant and lactating women

Animal reproduction experiments on niacin or this product have not been studied. If women with primary hypercholesterolemia (type I or II) become pregnant while taking niacin, this product should be stopped.
It is reported that niacin can be secreted through human milk. Because the therapeutic dose of niacin may cause serious adverse reactions in infants, the decision to stop breastfeeding or to stop medication should be based on the importance of the drug to breast milk.

Niacin sustained-release tablets for children

The safety and effectiveness of niacin in pediatric patients ( 16 years of age) have not been established. Studies of niacin sustained-release tablets have not been performed in patients under the age of 21. Therefore, this product is not recommended for patients under 21 years of age.

Niacin sustained-release tablets drug interactions

HMG-COA reductase inhibitors: see notes and effects on skeletal muscle.
Antihypertensive drugs: Niacin may enhance the effects of nerve block drugs and vasoactive drugs and cause orthostatic hypotension.
Aspirin: Co-administration with aspirin may reduce the metabolic clearance of niacin in vivo, and the clinical relevance of this finding is unknown.
Cholate Multivalent Chelators: An in vitro study observed the binding of colestipol and cholesyramine to niacin, respectively. About 98% of nicotinic acid can be combined with colestipol and 10% -30% can be combined with colestipol. The results show that there should be 4-6 hours or as much as possible between taking bile acid binding resin and taking this product Long intervals.
Others: Ingestion of alcohol or hot drinks may increase the occurrence of side effects such as flushing and itching. Therefore, when taking this product, avoid drinking and hot drinks. Vitamin preparations or other nutritional supplements containing large amounts of niacin or related compounds such as nicotinamide may increase the adverse effects of this product.
Niacin may cause false positive increases in catechol in plasma or urine. Niacin may also cause false positive reactions with copper sulfate reagents in urine glucose tests.

Nicotinic acid sustained-release tablets overdose

In case of overdose, appropriate first aid or treatment measures should be taken immediately.

Pharmacology and Toxicology of Niacin Sustained-release Tablets

Nicotinic acid exerts a lipid-lowering effect after being converted to NAD in the nicotinamide adenine dinucleotide (NAD) coenzyme system in the body. Niacin can reduce total cholesterol (TC), low density lipoprotein (LDL-C), and triglyceride (TG) levels, and increase high density lipoprotein (HDL-C) levels. Niacin also lowers serum levels of apolipoprotein B-100 (ApoB), most very low density lipoprotein (VLDL), some LDL, and lipoprotein a [Lp (a)].
Mice taking 1% niacin solution for life had no carcinogenic effect; Ames test showed that niacin had no teratogenicity; the reproductive toxicity of niacin had not been studied. Carcinogenic, teratogenic, or reproductive toxicity of niacin sustained-release tablets has not been studied.

Pharmacokinetics of Niacin Sustained-release Tablets

According to foreign data, the pharmacokinetics of nicotinic acid sustained-release tablets are as follows:
Absorption: Niacin is quickly and fully absorbed after oral administration (at least 60% -76% of oral dose). To improve bioavailability and reduce gastrointestinal discomfort, it is recommended to take it before bedtime after a small, low-fat diet.
Distribution: An isotope radiolabeled nicotinic acid experimental study in rats shows that nicotinic acid and its metabolites are concentrated in the liver, kidney, and adipose tissue.
Metabolism: The pharmacokinetic parameters of nicotinic acid are complex because of the rapid and extensive first-pass metabolism of nicotinic acid that is race-specific and dose-rate specific.

After a person takes niacin, they metabolize in two ways:
(1) Niacinylglycine (NUA) is formed by simple combination with glycine, which is excreted in the urine and may be converted into niacin with a small amount of reversible metabolism.
(2) Nicotinamide adenine dinucleotide (NAD) is formed. When the dose of hyperlipidemia is treated, the two metabolic pathways are saturated. Therefore, when niacin sustained-release tablets are used repeatedly, there is a non-linear relationship between the niacin dose and the plasma niacin concentration.

Excretion: After taking single-dose or multiple-dose niacin sustained-release tablets, about 60% -76% of the dose is excreted in the form of niacin and its metabolites through the urine. After taking multiple doses, up to 12% of the administered dose is excreted as it is. The ratio of metabolites in urine depends on the dose administered.

Niacin extended release tablets storage

Protected from light and sealed.

Niacin sustained release tablets packaging

7 pieces per board, two boards per box; aluminum-plastic composite packaging.
10 pieces per plate, one plate per box; aluminum-plastic composite packaging.
10 sheets per board, two boards per box; aluminum-plastic composite packaging.

Validity of Niacin Sustained Release Tablets

Tentative 24 months.

Nicotinic acid sustained release tablets

YBH04092003 ^[1]