probucol

Action and Spectrum

Actions and spectrum: 

Action: 

• Hypocholesterolemic Action: probucol acts by reducing the levels of cholesterol, specifically low-density lipoprotein (LDL) cholesterol, in the bloodstream. It does this by altering the metabolism and transport of lipids (fats) in the body. 
• Antioxidant Properties: probucol also possesses antioxidant properties. It can help protect cells and lipoproteins from oxidative damage. Oxidative stress and the formation of oxidized lipoproteins are associated with the development of atherosclerosis (hardening of the arteries). 

Spectrum of Use: 

• Hypercholesterolemia: probucol is used to lower elevated levels of cholesterol in individuals with hypercholesterolemia, particularly elevated LDL cholesterol. It can be beneficial for those who do not respond adequately to dietary and lifestyle modifications or other cholesterol-lowering medications. 
• Atherosclerosis Prevention: By reducing LDL cholesterol and possessing antioxidant properties, probucol is used to help prevent or slow down the progression of atherosclerosis in which fatty deposits build up on inner walls of arteries, potentially leading to cardiovascular events such as heart attacks and strokes. 

Drug Interaction

Adverse Reaction

Frequency not defined 

GI upset 

flatulence 

nausea 

angioedema 

Diarrhoea 

abdominal pain 

vomiting 

Fatal cardiac arrhythmias 

Black Box Warning

Black Box Warning: 

There were no specific black box warnings associated with probucol. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals with a known hypersensitivity or allergy to probucol or any of its components should not use the medication. 
• Pregnancy and Lactation: The use of probucol during pregnancy and breastfeeding should be carefully considered. Women of childbearing age should use effective contraception while taking probucol. 
• Renal Impairment: probucol is excreted primarily through the kidneys, and individuals with renal impairment may require dose adjustments. It should be used with caution in this population. 
• Hepatic Impairment: Individuals with liver impairment should be monitored closely while taking probucol, as hepatic metabolism of the drug may be affected. Dose adjustments may be necessary. 
• Gallbladder Disease: probucol can increase the risk of gallstone formation, and it is contraindicated in individuals with a history of gallbladder disease. 

Caution: 

• Gastrointestinal Disorders: probucol may cause gastrointestinal side effects, including diarrhea and abdominal discomfort. It should be used with caution in individuals with pre-existing gastrointestinal disorders. 
• Hypercholesterolemia: probucol is specifically indicated for the management of high cholesterol levels, and its use in other conditions or for prevention purposes should be carefully considered. 
• Elderly Population: Elderly individuals may be more susceptible to certain side effects of probucol. Monitoring and lower initial doses may be required. 
• Concurrent Medications: There may be interactions between probucol and other medications, so its use should be carefully considered in individuals taking medications that may interact with probucol.

Comorbidities: 

• Hypercholesterolemia: Elevated cholesterol levels, particularly elevated levels of low-density lipoprotein (LDL) cholesterol, are the primary indication for probucol. Individuals with hypercholesterolemia may have comorbid conditions that increase their risk of cardiovascular disease. 
• Atherosclerosis: Atherosclerosis is characterized by buildup of fatty deposits on inner walls of arteries. Individuals with atherosclerosis may benefit from probucol as part of their management plan. 
• Diabetes: Diabetes, particularly type 2 diabetes, is associated with an increased risk of cardiovascular disease. Some individuals with diabetes may require cholesterol-lowering medications like probucol to reduce their cardiovascular risk. 
• Hypertension: It is a risk factor for heart disease and stroke. Individuals with hypertension may use probucol as part of their risk reduction strategy. 

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. 
• 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: 

probucol is a medication primarily used to lower elevated cholesterol levels and prevent atherosclerosis, a condition characterized by buildup of fatty deposits in arteries. Its pharmacology is centered on its ability to reduce cholesterol levels in the bloodstream. It does this by increasing the uptake of LDL (low-density lipoprotein) cholesterol by the liver, thereby decreasing the amount of LDL cholesterol circulating in the blood. probucol also has antioxidant properties, which help protect cells and lipoproteins from oxidative damage.  

Pharmacodynamics: 

• Cholesterol-Lowering Effects: probucol primarily acts as a hypolipidemic (cholesterol-lowering) agent. It reduces elevated levels of low-density lipoprotein (LDL) cholesterol in the bloodstream, which is commonly referred to as “bad cholesterol.” This action is achieved by enhancing the uptake of LDL cholesterol by the liver, leading to its removal from the circulation. By reducing LDL cholesterol, probucol helps lower the risk of atherosclerosis and related cardiovascular events. 
• Increase in High-Density Lipoprotein (HDL) Cholesterol: In addition to lowering LDL cholesterol, probucol has been shown to increase levels of HDL cholesterol, often referred to as “good cholesterol.” HDL cholesterol plays a protective role in cardiovascular health by helping transport excess cholesterol away from arterial walls. 
• Antioxidant Properties: probucol possesses antioxidant properties, which means it can help protect cells and lipoproteins from oxidative damage caused by free radicals. By reducing oxidative stress, probucol contributes to the prevention of atherosclerosis. 
• Anti-Inflammatory Effects: Some research suggests that probucol may have anti-inflammatory properties, which can further contribute to its cardiovascular benefits. Inflammation is associated with atherosclerosis.

Pharmacokinetics: 

Absorption 

probucol is administered orally in the form of tablets or capsules. It is absorbed from gastrointestinal tract after oral ingestion. Its absorption may be influenced by the presence of food in the stomach. 

Distribution 

probucol is distributed throughout the body, including various tissues. It crosses blood-brain barrier and enter the central nervous system. 

Metabolism 

probucol undergoes hepatic (liver) metabolism primarily through conjugation with glucuronic acid. This metabolic process leads to the formation of metabolites. 

Elimination and excretion 

The primary route of excretion for probucol and its metabolites is through the kidneys, where they are eliminated in the urine. 

Adminstartion

Administration: 

• Dosage: The dosage of probucol is determined by the healthcare provider based on the individual’s specific condition, cholesterol levels, and cardiovascular risk factors. 
• Oral Administration: probucol is taken by mouth, and the tablets or capsules should be swallowed whole with a glass of water. 
• Duration: The duration of probucol treatment depends on the individual’s condition and cardiovascular risk factors. It may be prescribed for the long term to reduce the risk of atherosclerosis. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: probucol 

Pronounced: (PROE-bue-kol)  

Why do we use probucol? 

probucol is prescribed to lower elevated cholesterol levels in individuals with hypercholesterolemia, particularly elevated levels of LDL cholesterol. It is often used when dietary and lifestyle modifications alone are insufficient to manage cholesterol levels.

probucol may be used as part of the treatment plan for individuals with established coronary artery disease, helping to lower the risk of recurrent cardiovascular events. In some cases, probucol may be prescribed to manage elevated levels of triglycerides and total cholesterol.