lorcaserin

Action and Spectrum

Actions and Spectrum 

Activating the serotonin 2C receptor in the brain is how the prescription weight-loss medication lorcaserin works to suppress hunger and increase feelings of fullness. It works pharmacologically by selectively activating the serotonin 2C receptor. 

Regarding its range of applications, lorcaserin has been given the go-ahead for usage in people with a body mass index (BMI) of 30 or higher, which is considered obese, or in those with a BMI of 27 or higher who have at least one weight-related illness, such as type 2 diabetes, high blood pressure, or high cholesterol. 

Drug Interaction

Adverse Reaction

Frequency defined  

1-10% 

Fatigue (7.2%) 

Dry mouth (5.3%) 

Vomiting (3.8%) 

Diarrhea (6.5%) 

Urinary tract infection (6.5%) 

Musculoskeletal pain (2%) 

Back pain (6.3%) 

Constipation (5.8%) 

Rash (2.1%) 

Dizziness (8.5%) 

Nausea (8.3%) 

>10% 

Headache (16.8%) 

Nasopharyngitis (13%) 

Upper respiratory tract infection (13.7%) 

Post marketing reports 

Hypersensitivity 

Black Box Warning

Black Box Warning 

Regarding the possibility for cancer, the black box warning for lorcaserin details an elevated risk of tumours in rats given high dosages of the medication during research. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Because it might damage the fetus, lorcaserin should not be used while pregnant. 
• Patients who have a known allergy to the medication or any of its ingredients should not use lorcaserin. 

Caution: 

• Patients who have a history of valvular heart disease or congestive heart failure should use lorcaserin with care. 
• In individuals who have a history of mental illnesses, lorcaserin should be taken with caution since it might either create or exacerbate psychiatric disorders such depression or suicidal ideation. 
• lorcaserin should be taken with caution in individuals who need to be mentally aware, such as when driving or operating machinery, as it may produce cognitive impairment or somnolence. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excretion into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were 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 available 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 

The brain’s serotonin 2C receptors are activated by lorcaserin, a selective serotonin 2C receptor agonist. It is thought that activating these receptors decreases hunger and increases feelings of fullness, which can result in weight reduction. 

A neurotransmitter called serotonin is involved in the control of mood, hunger, and other bodily processes. 

Pharmacodynamics 

The selective agonism of the serotonin 2C receptor is a component of the pharmacodynamics of lorcaserin. 

Preclinical research has demonstrated that activating the serotonin 2C receptor in the hypothalamus and other regions of the brain reduces food intake while increasing energy expenditure. 

It has been demonstrated that lorcaserin, a selective agonist of this receptor, increases satiety and decreases food intake in people. 

Pharmacokinetics 

Absorption   

Following oral treatment, lorcaserin is readily absorbed, reaching peak plasma concentrations in 1 to 2 hours. The medication is taken orally and comes in the form of a tablet. 

Distribution 

The enormous volume of distribution of lorcaserin suggests that it is broadly dispersed throughout the body. Approximately 70% to 76% of the medicine is attached to plasma proteins, indicating that the drug is substantially protein-bound. 

Metabolism 

The liver substantially metabolises lorcaserin through a variety of mechanisms, such as oxidative and conjugative metabolism. The main metabolite, produced by the CYP3A4 and CYP2D6 enzymes, is the inactive N-desmethyl metabolite. Additionally, several insignificant metabolites have been found. 

Elimination and excretion 

Approximately 92% of lorcaserin and its metabolites are eliminated in the urine, with the remaining 2% ending up in the feces. It has a half-life of elimination of around 11 hours. 

Adminstartion

Administration:  

With or without food, lorcaserin is delivered orally as a tablet and suggested dosage is 10 mg administered twice a day. The pills must be taken whole; they should not be chewed, crushed or dissolved. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: lorcaserin 

Why do we use lorcaserin? 

An adult who is obese or overweight and has at least one weight-related comorbidity, such as hypertension, type 2 diabetes mellitus, or dyslipidaemia, may use the weight-loss drug lorcaserin.  

It is suggested for chronic weight control as an addition to a low-calorie diet and increased physical exercise.