acipimox

Action and Spectrum

Actions and spectrum: 

acipimox is a medication that belongs to the class of drugs known as nicotinic acid derivatives. It is primarily used to treat dyslipidemia, which is characterized by abnormal levels of lipids. acipimox works by inhibiting the synthesis of triglycerides and decreasing VLDL the production in the liver. This results in a reduction of triglycerides and total cholesterol levels in the blood. 

The spectrum of acipimox’s action is focused on improving lipid profiles & decreasing the risk of cardiovascular diseases associated with dyslipidemia. It is particularly beneficial in conditions like hypertriglyceridemia, where elevated triglyceride levels are a significant concern. By addressing these lipid abnormalities, acipimox helps in managing and preventing complications related to high lipid levels, such as atherosclerosis and cardiovascular diseases. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Nausea 

abdominal discomfort 

Headache 

liver toxicity 

Dizziness 

itching 

skin rash 

swelling 

Black Box Warning

Black Box Warning: 

there is no specific black box warning associated with the use of acipimox. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals with known hypersensitivity or allergy to acipimox or any of its components should not use this medication. 
• Active Liver Disease: acipimox should not be used in active liver disease or severe hepatic impairment. 
• Severe Renal Impairment: The drug should be avoided in severe renal impairment as it can lead to accumulation of the drug and potential adverse effects. 
• Severe Gout: acipimox may exacerbate gout symptoms in patients with a history of severe gout. 
• Active Peptic Ulcer Disease: acipimox may worsen peptic ulcers and should be avoided in active peptic ulcer disease. 
• Active Bleeding Disorders: Due to its potential to impair platelet function, acipimox should not be used in individuals with active bleeding disorders. 

Caution: 

• Hepatic Impairment: acipimox should be used with caution with mild to moderate impairment, as the drug is metabolized in the liver. Dose adjustments may be necessary in these individuals. 
• Renal Impairment: In renal impairment, dosage adjustments may be required as acipimox and its metabolites are excreted through the kidneys. 
• Bleeding Disorders: acipimox has the potential to impair platelet function and may increase bleeding risk.  
• Gallstones: acipimox may affect cholesterol metabolism and increase the risk of gallstone formation. Caution is advised in patients with a history of gallstones. 
• Myopathy: acipimox may cause myopathy (muscle damage). Patients experiencing unexplained muscle pain or weakness should seek medical attention promptly. 
• Hypoglycemia: acipimox may cause a decrease in blood glucose levels. Diabetic patients should be monitored for signs of hypoglycemia during treatment.

Comorbidities: 

• Hypertriglyceridemia: acipimox is prescribed to reduce elevated triglyceride levels in patients with hypertriglyceridemia, a condition characterized by high levels of triglycerides in the blood. 
• Dyslipidemia: acipimox is used to manage dyslipidemia, which involves abnormal levels of lipids (cholesterol and triglycerides) in the blood. 
• Cardiovascular Diseases: Dyslipidemia and high triglycerides are risk factors for various cardiovascular diseases, including atherosclerosis, coronary artery disease, and heart attack. acipimox is sometimes prescribed to reduce these risks. 
• Metabolic Syndrome: It is a cluster of conditions, including high triglycerides, high blood pressure, obesity, and insulin resistance. acipimox may be used in patients with metabolic syndrome to address elevated triglycerides. 
• Diabetes: acipimox is sometimes prescribed to diabetic patients with high triglyceride levels as part of their overall management. 
• Obesity: Obesity is often associated with dyslipidemia and elevated triglycerides. acipimox may be used in obese individuals with high triglycerides as part of a comprehensive treatment plan. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• 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 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: 

acipimox is a hypolipidemic agent used to reduce elevated triglyceride levels in the blood. It belongs to the class of niacin derivatives known as nicotinic acid analogs. Acipimox works by inhibiting the enzyme diacylglycerol acyltransferase (DGAT), which plays a role in triglyceride synthesis. By blocking this enzyme, acipimox decreases triglyceride production and secretion, leading to a reduction in triglyceride levels.

Additionally, acipimox increases the breakdown of triglycerides, further contributing to its lipid-lowering effects. Unlike niacin, acipimox has minimal effects on raising high-density lipoprotein (HDL) cholesterol and does not cause significant flushing, making it a favourable option for patients who are intolerant to niacin. The pharmacology of acipimox highlights its role in managing dyslipidemia, particularly in cases of hypertriglyceridemia.  

Pharmacodynamics: 

• Triglyceride Reduction: acipimox primarily targets elevated triglyceride levels in the blood. It inhibits the enzyme diacylglycerol acyltransferase (DGAT), which is involved in triglyceride synthesis within the liver and adipose tissues. By blocking DGAT, acipimox reduces triglyceride production and secretion, leading to a decrease in circulating triglyceride levels. 
• Lipid Metabolism: acipimox influences lipid metabolism by increasing the breakdown of triglycerides through lipolysis. This process involves the hydrolysis of triglycerides into free fatty acids and glycerol. The increased lipolysis contributes to the overall reduction in triglyceride levels in the blood. 
• HDL Cholesterol: Unlike some other lipid-lowering agents, acipimox has minimal effects on raising high-density lipoprotein (HDL) cholesterol levels. It primarily focuses on lowering triglycerides and does not significantly impact HDL cholesterol levels. 
• Insulin Sensitivity: acipimox may have a favourable effect on insulin sensitivity in some individuals. It has shown to improve glucose metabolism & insulin sensitivity in certain patients, making it potentially beneficial for individuals with insulin resistance. 
• Vasodilation: acipimox has been reported to exert vasodilatory effects on blood vessels. This action may contribute to improved blood flow and cardiovascular function in patients with compromised vascular health. 
• Anti-Inflammatory Effects: acipimox has been found to possess anti-inflammatory properties, potentially exerting a protective effect on the cardiovascular system, and reducing inflammation-induced damage. 
• Platelet Function: Some studies suggest that acipimox may have mild antiplatelet effects, which could contribute to its potential cardiovascular benefits by reducing platelet aggregation and the risk of clot formation.

Pharmacokinetics: 

Absorption 

acipimox is rapidly and well absorbed from the gastrointestinal tract after oral administration. The presence of food will not affect the absorption. 

Distribution 

acipimox is extensively distributed throughout the body tissues and enters systemic circulation, where it reaches target organs like liver and adipose tissues to exert its pharmacological effects. 

Metabolism 

acipimox undergoes metabolism in the liver, primarily by hepatic glucuronidation, leading to the formation of acipimox glucuronide, which is a major metabolite. The liver enzyme uridine diphosphate-glucuronosyltransferase (UGT) is responsible for this conjugation. 

Elimination and excretion 

The main route of excretion for acipimox is through the urine, primarily as acipimox glucuronide. Only a small percentage of the drug is excreted unchanged in the urine. The elimination half-life of acipimox is short, leading to a rapid elimination from the body. 

Adminstartion

Administration: 

• Dosage: The recommended dosage of acipimox may vary depending on the patient’s medical condition, age, and response to treatment. The usual adult dose is around 250 to 500 mg, two to three times a day. 
• Timing: acipimox is usually taken with meals to improve its absorption. Taking the medication with food also helps reduce the likelihood of gastrointestinal side effects. 
• Duration: The duration of treatment with acipimox will be determined based on the individual’s response to therapy and the medical condition being treated. 
• Compliance: It is essential to take acipimox exactly as prescribed by the healthcare provider. Missing doses or taking it differently than directed may affect the effectiveness of the medication. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: acipimox 

Pronounced: (uh-SIP-uh-mox)  

Why do we use acipimox? 

acipimox is primarily used for the treatment of hypertriglyceridemia. It is particularly effective in reducing very low-density lipoprotein (VLDL) cholesterol and triglyceride levels. acipimox is often prescribed when lifestyle changes and other medications have not adequately controlled triglyceride levels. By reducing triglycerides, acipimox can help lower the risk of cardiovascular complications like heart disease, stroke, and pancreatitis.