benfluorex

Action and Spectrum

Actions and spectrum: 

Action:  

benfluorex acts as an appetite suppressant, which means it reduces feelings of hunger. It achieves this by affecting neurotransmitters in the brain, particularly serotonin and norepinephrine, which play roles in regulating appetite. 

Spectrum of Use: 

• Weight Management: benfluorex was primarily prescribed for weight management and obesity treatment. It was used in cases where lifestyle changes (such as diet and exercise) alone were insufficient in achieving weight loss goals. 
• Appetite Suppression: Due to its ability to suppress appetite, benfluorex was used to help individuals control their food intake, which, in turn, could aid in weight reduction. 

Drug Interaction

Adverse Reaction

Frequency not defined 

nausea 

asthenia 

dizziness 

Loose stools 

epigastric discomfort 

drowsiness 

Black Box Warning

Black Box Warning: 

benfluorex carries a black box warning due to its association with serious cardiovascular and pulmonary risks. It has been linked to heart valve disorders, pulmonary arterial hypertension (PAH), and other potentially life-threatening cardiovascular complications. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Known Hypersensitivity: Individuals with a known hypersensitivity or allergy to benfluorex or any of its components should not use this medication. 
• Pulmonary Hypertension: benfluorex is contraindicated in individuals with a history of pulmonary hypertension due to its association with exacerbating this condition. 
• Heart Valve Disorders: It is contraindicated in individuals with a history of heart valve disorders, as benfluorex has been linked to heart valve abnormalities. 
• Cardiovascular Disease: Patients with existing cardiovascular diseases, such as coronary artery disease or heart failure, should avoid benfluorex due to its potential to worsen these conditions. 
• Renal Impairment: Individuals with severe renal impairment (kidney dysfunction) may need to avoid benfluorex, as its elimination from the body may be impaired in these cases. 

Caution: 

• Cardiovascular Risk: benfluorex has been associated with an increased risk of heart valve disorders and pulmonary arterial hypertension (PAH). Individuals with a history of heart disease or risk factors for cardiovascular problems should exercise extreme caution when considering benfluorex. 
• Pulmonary Hypertension: Individuals with a history of or predisposition to pulmonary hypertension (high blood pressure in the arteries of the lungs) should use benfluorex with caution, as it can exacerbate this condition. 
• Regular Monitoring: Patients taking benfluorex should be closely monitored for signs and symptoms of heart valve disorders, PAH, and other cardiovascular issues. Regular medical check-ups are essential to detect and manage these potential side effects. 
• Liver and Kidney Function: Patients with impaired liver or kidney function may need dose adjustments or careful monitoring while taking benfluorex, as the drug’s elimination from the body may be affected. 
• Pregnancy and Lactation: benfluorex should not be used during pregnancy & breastfeeding due to potential risks to the fetus and infant. Safer alternatives for weight management should be considered.

Comorbidities: 

• Cardiovascular Disorders: benfluorex has been linked to an increased risk of heart valve disorders, such as valvular regurgitation. These conditions can lead to symptoms like shortness of breath, chest pain, and heart palpitations. 
• Pulmonary Arterial Hypertension (PAH): benfluorex has been associated with an elevated risk of developing pulmonary arterial hypertension, a severe and life-threatening condition characterized by high blood pressure in the arteries of the lungs. 
• Cardiovascular Events: Some individuals taking benfluorex have experienced heart attacks and strokes. 
• Valvular Heart Disease: Long-term use of benfluorex has been linked to damage to heart valves, which can impair the heart’s function and lead to heart failure. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into breast 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: 

benfluorex is a centrally acting anorectic agent that was used for weight management and appetite suppression. Its pharmacology involved primarily affecting the levels of neurotransmitters in brain, particularly serotonin and norepinephrine. By increasing the availability of these neurotransmitters, benfluorex was believed to reduce appetite and induce a feeling of fullness, thus promoting weight loss.

However, it was withdrawn from the market in many countries due to safety concerns, particularly its association with heart valve disorders and pulmonary arterial hypertension. Consequently, its use is highly discouraged, and safer alternatives for weight management are recommended.  

Pharmacodynamics: 

• Serotonin and Norepinephrine Modulation: benfluorex is thought to enhance the activity of serotonin and norepinephrine, two neurotransmitters involved in regulating mood, appetite, and satiety. By increasing these neurotransmitters in the brain, benfluorex may reduce the feelings of hunger and increases the feelings of fullness. 
• Appetite Suppression: The enhanced serotonin and norepinephrine activity is believed to influence the hypothalamus, a brain region responsible for appetite control. This influence can result in a reduced appetite, leading to decreased food intake. 
• Thermogenic Effect: benfluorex may also have a thermogenic effect, increasing the body’s energy expenditure and promoting weight loss.

Pharmacokinetics: 

Absorption 

benfluorex is orally administered and typically taken in tablet form. It is absorbed from gastrointestinal tract into the bloodstream, where it can exert its effects. 

Distribution 

Once absorbed, benfluorex is distributed throughout the body, including the brain, where it interacts with neurotransmitters involved in appetite regulation. 

Metabolism 

benfluorex undergoes metabolism in the liver. The exact metabolic pathways are not extensively studied or well-documented. 

Elimination and excretion 

benfluorex and its metabolites are excreted from the body primarily through urine and feces. 

Adminstartion

Administration: 

The administration of benfluorex, a medication that was once used for weight management and appetite suppression but is now withdrawn in many countries due to safety concerns, typically involved oral ingestion in tablet form.

However, it is important to emphasize that the use of benfluorex is strongly discouraged due to its association with serious cardiovascular and pulmonary risks, including heart valve disorders and pulmonary arterial hypertension. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: benfluorex 

Pronounced: (ben-floo-rex)  

Why do we use benfluorex? 

benfluorex was initially used for weight management and appetite suppression. It was prescribed to individuals with obesity or those seeking to lose weight. The drug works by affecting neurotransmitters in brain, such as serotonin and norepinephrine, to reduce appetite and induce a feeling of fullness.