sibutramine

Action and Spectrum

Actions and spectrum: 

sibutramine works at the neural synapse by inhibiting norepinephrine (NE), serotonin (5-hydroxytryptamine, 5-HT), and to a lesser extent of dopamine reuptake. It induces satiety and decreases in appetite by lowering the reuptake of these neurotransmitters resulting in less food consumption. 

Drug Interaction

Adverse Reaction

Frequency defined 

Headache(30.3%) 

Constipation(11.5%) 

Dry mouth(17.2%) 

Depression(4.3%) 

Increase in blood pressure(2.1%) 

Anxiety(4.5%) 

abdominal pain(4.5) 

anorexia(13.0%) 

Frequency not defined 

Sleeping troubles 

Painful menstruation 

Indigestion 

Impatience 

Chills 

Black Box Warning

Black Box Warning 

None 

Contraindication / Caution

Contraindication/Caution: 

Cardiovascular disorders 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: C 

Lactation:  

Use of sibutramine is not recommended in case of lactation. 

Pregnancy category:  

• Category A: Studies that were well-controlled and met expectations revealed no risk to the foetus `in either the first or second trimester. 
• Category B: There were a 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 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: 

Pharmacodynamics: 

Sibutramine inhibits serotonin and norepinephrine reuptake in invivo but not in invitro. The metabolites M1 and M2 limits the neurotransmitter reuptake in both invitro and invivo. 

Pharmacokinetics: 

Absorption 

It is rapidly absorbed. 

Distribution 

Protein bound is 97%. 

Metabolism 

It is metabolised to two different metabolites by cytochrome P450 isozyme. 

Elimination and excretion 

It is eliminated through renal excretion with half life 1.1 hrs. 

Adminstartion

Administration: 

It is taken orally daily. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: sibutramine 

Pronounced: si- Bue-tra-meen  

Why do we use sibutramine? 

Sibutramine is an oral anorexiant that manages obesity and regulates brain neurotransmitters to control hunger and helps in weight management, but it is classified as a Schedule IV controlled substance in the US.