Lorcaserin

Lorcaserin is an sympathomimetic amines belonging to anorectic agent

Lorcaserin is used in the treatment for short-term of Weight management.

Lorcaserin has a peak plasma concentration of about 1.5 – 2 hours, but the bioavailability was not determined. The volume of distribution was not determined, but lorcaserin distributes to the central nervous system and cerebrospinal fluid. Lorcaserin hydrochloride has a plasma protein binding of approximately 70%.Lorcaserin has extensive hepatic metabolism producing inactive compounds. Lorcaserin sulfamate (M1) is the major metabolite circulating in the plasma, and N-carbamoyl glucuronide lorcaserin (M5) is the major metabolite in urine. Other minor metabolites that are both excreted in urine are glucuronide or sulfate conjugates.Lorcaserin is eliminated by hepatic metabolism, and the metabolites are eliminated mostly in the urine (92.3%) and some through feces (2.2%).

The Tmax of Lorcaserin is approximately 1-4 hours.

Lorcaserin shows common side effects like Insomnia, Dizziness, Headache, Dry mouth, Nervousness, Restlessness, Diarrhea, Constipation, Increased heart rate, High blood pressure.

Lorcaserin is available in the form of tablets.

Lorcaserin is available in India, Germany, Canada, Italy, USA

Although the exact mechanism is unknown, it is believed to involve the selective activation of 5-HT2C receptors in the anorexigenic pro-opiomelanocortin neurons in the arcuate nucleus of the hypothalamus. This results in decreased food intake and satiety by promoting the release of alpha-melanocortin stimulating hormone, which acts on melanocortin-4 receptors.

Lorcaserin is available in the form of tablets.

Immediate release: Administer 1 hour before meals; may also administer 1 tablet midevening (to overcome night hunger).

Controlled release: Swallow whole; administer at midmorning.

Bariatric surgery: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. Do not cut, crush, or chew. Switch to IR tablet.

Lorcaserin is used in the treatment for short-term of Weight management.

Lorcaserin is a serotonin 2C receptor agonist used in conjunction with physical activity and calorie restriction for weight loss in obese patients with a body mass index (BMI) of 30 and above, and in overweight patients with weight-related comorbidities.

Lorcaserin is approved for use in the following clinical indications

Weight management, short-term: Short-term (few weeks) in the management of exogenous obesity. Therapy should be used in conjunction with a comprehensive weight management program.

Obesity

Indicated as an adjunct to a reduced-calorie diet and exercise for chronic weight management with initial BMI ≥30 kg/m² (obese) or ≥27 kg/m² (overweight) with 1 weight-related comorbid condition (eg, hypertension, dyslipidemia, type 2 diabetes mellitus).

Lorcaserin is available in various strengths as25 mg, 75 mg.

Lorcaserin is available in the form of tablets.

• Dosage Adjustment in Kidney Patient

Mild (CrCl >50 mL/min): No dosage adjustment required

Moderate (CrCl 30-50 mL/min): Use caution

Severe (CrCl <30 mL/min) or ESRD: Not recommended

• Dosage Adjustment in Hepatic impairment Patient

Mild-to-moderate (Child-Pugh score 5-9): No dosage adjustment required

Severe (Child-Pugh score >9): Use caution

• Dosage Adjustment for Pediatric Patients

Adolescents >16 years: Refer to adult dosing.

Hypersensitivity or idiosyncrasy to Lorcaserin or other sympathomimetic amines; advanced arteriosclerosis, severe hypertension; pulmonary hypertension; hyperthyroidism; glaucoma; agitated states, history of drug abuse; during or within 14 days following MAO inhibitor therapy, concurrent use with other anorectic agents.

Serotonin Syndrome or Neuroleptic Malignant Syndrome (NMS)-like Reactions

Lorcaserin is contraindicated during pregnancy, because weight loss offers no potential benefit to a pregnant woman and may result in fetal harm. Maternal exposure to lorcaserin in late pregnancy in rats resulted in lower Body weight in offspring which persisted to adulthood. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard of maternal Weight loss to the fetus.

• Common Adverse effects:

Dizziness ,Headache ,Dry mouth, Nervousness ,Restlessness, Diarrhea ,Constipation, Increased heart rate, High blood pressure, Palpitations, Tremors ,Sweating, Dizziness

• Less Common Adverse effects:

Mood changes, Hallucinations ,Blurred vision ,Difficulty urinating, Rash, Itching, Swelling, Difficulty breathing, Chest pain, Fainting ,Seizures, Abdominal pain, Yellowing of the skin or eyes (jaundice)

• Rare Common Adverse effects:

Allergic reactions such as anaphylaxis or angioedema, Psychotic reactions such as delusions or paranoia, Suicidal thoughts or behavior ,Stroke ,Heart attack, Pulmonary hypertension, Primary pulmonary hypertension, Cardiac valvulopathy ,Neuroleptic malignant syndrome ,Stevens-Johnson syndrome

• Use with Other Agents that Affect Serotonin Pathways

Based on the mechanism of action of Lorcaserin and the theoretical potential for serotonin syndrome, use with extreme caution in combination with other drugs that may affect the serotonergic neurotransmitter systems, Including, but not limited to, triptans, monoamine oxidase inhibitors (MAOIs, including linezolid, an antibiotic which is a reversible non-selective MAOI), selective serotonin reuptake inhibitors (SSRIs), selective serotonin-Norepinephrine reuptake inhibitors (SNRIs), dextromethorphan, tricyclic antidepressants (TCAs), bupropion, Lithium, tramadol, tryptophan, and St. John’s Wort.

• Cytochrome P450 (2D6) substrates

Use caution when administering Lorcaserin together with drugs that are CYP 2D6 substrates, as LORCASERIN can Increase exposure of these drugs.

The common side effects of Lorcaserin include the following Insomnia, Dizziness, Headache, Dry mouth, Nervousness, Restlessness, Diarrhea, Constipation, Increased heart rate, High blood pressure.

Most common adverse reactions include hypoglycemia (diabetic patients), headache, back pain, fatigue, decrease in lymphocytes, upper respiratory tract infection, and nasopharyngitis. Moreover, the safety and efficacy of co-administration with other weight loss products has not been established, and cardiovascular effects on mortality and morbidity have not been established.

Pharmacodynamic

Lorcaserin is a sympathomimetic stimulant drug marketed as an appetite suppressant. Chemically, it is the N,N-diethyl analog of cathinone. Its mechanism of action is similar to other appetite suppressants such as sibutramine, phentermine and dextroamphetamine.

Pharmacokinetics

• https://www.rxlist.com/dopram-drug.htm
• https://www.mims.com/india/drug/info/Lorcaserin ?type=full&mtype=generic
• https://go.drugbank.com/drugs/DB00561
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7003846/