Action and Spectrum

Actions and Spectrum 

niacin slows down the breakdown of lipids that have been stored in adipose tissue, which slows down the flow of free fatty acids into the circulation. Triglyceride and LDL cholesterol synthesis is reduced as a result. 

It has been demonstrated that niacin raises HDL cholesterol levels, or “good” cholesterol. Heart disease risk is decreased by HDL cholesterol, which aids in the removal of LDL cholesterol from the bloodstream. 

niacin has a wide range of applications and is offered in a variety of formulations. It can be consumed orally in the form of a capsule, immediate-release tablet, or extended-release tablet. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Hepatotoxicity  

Postural hypotension 

Reversible increase in serum aminotransferase 

Diarrhea 

Headache 

Hepatic necrosis 

Nausea 

Vomiting 

Rhabdomyolysis 

Rash 

Abdominal pain 

Dyspepsia 

Flushing  

Pruritus  

Arrhythmias 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• niacin should not be used by people who are known to be allergic or hypersensitive to it or any of its ingredients. 
• Patients with active liver illness, such as hepatitis or severe liver malfunction, should not take niacin. 
• In people with extremely low blood pressure, niacin should be avoided. 
• niacin should be taken with caution or avoided in people who have active peptic ulcers since it can make them worse. 

Caution: 

• niacin may have an impact on insulin sensitivity and blood sugar levels. When using niacin, those with diabetes or prediabetes should closely check their blood glucose levels. 
• In people with a history of gout, niacin may raise uric acid levels and may cause gout episodes.  
• niacin can aggravate already existing gallbladder disease or raise the chance of gallstone development.  
• Patients who have a history of gallbladder issues should exercise caution. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: C 

Lactation: Excretion into human milk is known  

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology 

The main way that niacin is used to treat dyslipidemia (abnormal lipid levels) is as a lipid-modifying drug. It functions by lowering triglyceride and low-density lipoprotein (LDL) cholesterol levels while raising HDL (high-density lipoprotein) cholesterol levels. 

niacin prevents the breakdown of fat that has been accumulated in adipose tissue (lipolysis). As a result, there is a reduction in the amount of free fatty acids released into the blood, which lowers the formation of triglycerides and LDL cholesterol. 

niacin greatly raises HDL cholesterol, or “good” cholesterol, levels in the blood. Having higher levels of HDL cholesterol lowers the risk of cardiovascular illnesses by assisting in the removal of LDL cholesterol from the bloodstream. 

Pharmacodynamics 

niacin causes the activation of GPR109A, which inhibits lipolysis in adipose tissue. As a result, less free fatty acids are released into the bloodstream, which in turn results in less triglyceride and LDL cholesterol being produced. 

The liver produces and secretes less very-low-density lipoprotein (VLDL) particles when niacin is present. Triglyceride and LDL cholesterol levels in the blood are lowered as a result. 

Pharmacokinetics 

Absorption   

Following oral dosing, niacin is effectively absorbed from the gastrointestinal tract. The process of absorption is imperfect and incredibly individualistic. niacin’s bioavailability is influenced by things like the formulation, dosage, and food intake. In general, extended-release formulations take longer to absorb than immediate-release versions. 

Distribution 

niacin is found in large amounts throughout the body. It passes through a lot of binding to plasma proteins, mostly to albumin. niacin is present in breast milk and can penetrate the placenta and blood-brain barrier. It is found throughout the body and is not just found in certain organs or tissues. 

Metabolism 

The liver is where niacin is extensively metabolized. It is metabolized via several processes, such as methylation, glucuronidation, and hepatic dehydrogenation. niacin’s main active metabolite, nicotinamide, is created through dehydrogenation.  

Elimination and excretion 

niacin and its metabolites are mostly excreted by the kidneys. niacin is eliminated in the urine both in its unmodified form and as its metabolites. It is also minimally eliminated in feces. niacin has a 20-to-45-minute half-life in the body before it is eliminated. 

Adminstartion

Administration:  

Tablets or pills containing niacin are frequently taken orally. Usually, it is consumed along with a full glass of water.  

To lessen gastrointestinal adverse effects, immediate-release niacin formulations are often taken two to three times daily with meals. niacin can help lessen the flushing reaction when taken with food. 

niacin formulations for prolonged release are made to release the drug gradually over an extended period. They are typically taken once a day, ideally before night, to assist prevent flushing. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: niacin 

Why do we use niacin? 

The main medical application of niacin is to treat dyslipidemia, a disorder marked by abnormal blood lipid levels.  

High blood cholesterol levels are treated with niacin therapy. To get the best lipid control, it can be administered alone or in conjunction with other cholesterol-lowering drugs, such statins. 

It is beneficial in decreasing elevated levels of triglycerides, a type of fat found in the blood.