bifemelane

Action and Spectrum

Actions and Spectrum 

Actions: 

• Inhibition of MAO-B: bifemelane inhibits MAO-B, which helps maintain higher dopamine levels in the brain. 
• Neuroprotective: It is believed to have neuroprotective properties, potentially protecting neurons from damage. 
• Antidepressant: bifemelane treats depression, as increased dopamine levels can have mood-enhancing effects. 
• Cognitive Enhancement: Some studies suggest it may improve cognitive function, particularly in elderly individuals with cognitive impairment. 
• Anti-Parkinsonian Potential: It has been investigated for its potential use in Parkinson’s disease to improve motor symptoms and delay disease progression. 

Spectrum: 

bifemelane primarily affects neurotransmitter levels in the brain, particularly dopamine. Like some other psychiatric medications, it does not have a broad spectrum of activity on various neurotransmitter systems. 

Drug Interaction

Adverse Reaction

Frequency not Defined 

Nausea 

Drowsiness 

Diarrhea 

Anorexia 

Constipation 

Anxiety 

Chest Pain  

Heart Burn 

Taste disturbance 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 

Cautions: 

• Medical conditions 
• Drug interactions  
• Renal impairment 
• Hepatic impairment 
• Concomitant medications 
• Psychiatric disorders 
• Elderly population 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

The drug is contraindicated during pregnancy. 

Breastfeeding warnings:  

The excretion of the drug in breast milk is unknown.   

Pregnancy category: 

Category A: Well-controlled and satisfactory studies show no risk to the fetus in the initial 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: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

• Monoamine Oxidase B (MAO-B) Inhibition: bifemelane acts as a reversible and selective inhibitor of MAO-B. MAO-B breaks down neurotransmitters such as dopamine in the brain. By inhibiting MAO-B, bifemelane increases dopamine levels available in the synaptic cleft, potentially enhancing dopaminergic neurotransmission. This action may contribute to its therapeutic effects in conditions where dopamine imbalance exists. 
• Dopaminergic Effects: The elevation of dopamine levels in the brain is thought to be the primary pharmacological action of bifemelane. Dopamine is a neurotransmitter in mood regulation, motor control, and various cognitive functions. The increase in dopamine can have mood-enhancing and potentially neuroprotective effects. 

Pharmacodynamics: 

• Mood Enhancement: The increased dopaminergic activity may contribute to mood-enhancing effects. In conditions such as depression, where dopamine levels may be imbalanced, the elevation of dopamine levels by bifemelane can have an antidepressant effect. 
• Neuroprotection: bifemelane is believed to have neuroprotective properties, potentially related to its ability to increase dopamine levels. This neuroprotection may help safeguard neurons from damage and degeneration, making it a subject of interest for neurodegenerative disorders like Parkinson’s. 
• Cognitive Enhancement: Some studies have suggested that bifemelane may improve cognitive function, especially in elderly individuals with cognitive impairment. The increased dopamine availability may support cognitive processes. 

Pharmacokinetics: 

Absorption 

Oral absorption is 47.5% ± 47.5 

Distribution 

The volume of distribution is 8L/kg 

Plasma protein binding is 95% 

Metabolism 

Presystemic metabolism is 45% ± 45 

Elimination and Excretion 

The elimination half-life is 3.3 hours 

The rate of renal excretion is 0.023% 

Adminstartion

Administration: 

The specific dosage of bifemelane can vary depending on the patient’s medical condition, age, and the medication formulation. It’s essential to follow the prescribed dosage instructions provided by your healthcare provider. 

bifemelane is usually taken with meals. Taking it with food can help improve absorption and minimize the risk of stomach upset. Follow your healthcare provider’s recommendations regarding the timing of doses. Most bifemelane tablets or capsules should be swallowed whole with a full glass of water.

Patient Information Leaflet

Patient information leaflet 

Generic Name: bifemelane 

Why do we use bifemelane? 

bifemelane is a medication primarily used for the following purposes: 

• Treatment of Depression: bifemelane is prescribed to alleviate depressive symptoms by increasing dopamine levels in the brain. 
• Improving Cognitive Function: It may enhance cognitive function, especially in elderly individuals with cognitive impairment. 
• Neuroprotection: bifemelane is believed to have neuroprotective properties, potentially safeguarding neurons from damage and degeneration. 
• Potential in Parkinson’s Disease: It has been investigated for its use in Parkinson’s disease, which may help improve motor symptoms and delay disease progression. 
• Management of Mixed Hyperlipidemia: In some cases, bifemelane has been used to treat mixed hyperlipidemia.