LORCASERIN

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Created Sep 2019 | Updated Oct 2020

LORCASERIN

  • [BELVIQ]
  • [LORQUESS]
  • [EISAI]

DEA CODE 1625: Schedule 4

Belviq is the brand name of the drug lorcaserin, which is used along with diet and exercise to treat obesity. The medicine is sometimes given to treat obesity associated with high cholesterol, high blood pressure, or type 2 diabetes. Belviq is in a class of drugs known as serotonin receptor agonists. It works by targeting chemicals in the brain that affect appetite. The Food and Drug Administration (FDA) approved Belviq in 2012. The drug is manufactured by Arena Pharmaceuticals.

Belviq (lorcaserin hydrochloride) is a serotonin 2C receptor agonist. It has been shown to decrease food consumption and promote satiety by selectively activating serotonin 2C receptors in the brain. Belviq is specifically indicated as an adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in clinically obese adults (BMI of 30 kg/m2 or greater) and overweight adults (BMI of 27 kg/m2 or greater) with at least one weight-related comorbid condition. Belviq is supplied as a tablet designed for oral administration. The recommended dose is one 10mg tablet twice daily. Use of Belviq should be discontinued if 5% weight loss is not achieved by week 12 of treatment.

The drug works by controlling appetite - specifically by activating brain receptors for serotonin, a neurotransmitter that triggers feelings of satiety and satisfaction. Serotonin is also involved in mood; many antidepressant drugs work by preventing the reuptake of serotonin and keeping brain receptors bathed in the chemical. Researchers at Arena say their drug is designed to seek out only the serotonin receptors that affect appetite. According to clinical trial data submitted by Arena to the FDA, nearly half of dieters without Type 2 diabetes who used the medication lost at least 5% of their starting weight - or an average of 12 lbs. - over a year. For best results, dieters are advised to use the medication together with a healthy diet and exercise program. The approved labeling for Belviq also recommends that people discontinue the drug if they fail to lose 5% of their body weight after 12 weeks; longer treatment is unlikely to lead to meaningful weight loss.

The FDA approved the medication for people who are obese (with a body mass index, or BMI, of 30 or higher) or who are overweight (with a BMI of 27 or above) and also have at least one weight-related health condition such as Type 2 diabetes, high blood pressure or high cholesterol.

The most common side effects of Belviq in non-diabetic patients are headache, dizziness, fatigue, nausea, dry mouth and constipation; in patients with diabetes, side effects include low blood sugar, headache, back pain, cough and fatigue.

History of Belviq (Lorcaserin)
The FDA approved the commercialization of Belviq in the United States in 2012, making it the first weight loss medication to receive authorization in over a decade. Arena Pharmaceuticals filed a New Drug Application (NDA) for Locarserin at the end of 2009. Within the two-year-process, the FDA analyzed the data provided by both Arena and Eisai, and issued positive recommendations based on the clinical studies. While Eisai holds the rights to commercialize Belviq worldwide, with the exception of South Korea, Taiwan, Australia, Israel and New Zealand, Arena is responsible for the sales in all other regions.

Lorcaserin, combined with diet and exercise, can be used to produce additional weight loss, although the effect on morbidity and mortality is not known. It should be discontinued in patients who do not lose at least 5% of their body weight in the first 12 weeks because they are unlikely to have any additional weight loss. Initial two-year studies did not demonstrate cardiac valvulopathy, but these studies excluded patients with significant cardiac disease. Euphoric effects at supratherapeutic dosages make the potential for recreational drug abuse a valid concern.

Abuse Potential?
The concern is that lorcaserin has the potential to cause mind-altering effects that might lead to diversion of the prescription drug for recreational purposes. According to researchers, a small proportion of the patients who received supratherapeutic [higher than recommended] doses of lorcaserin in clinical trials have reported altered perception, abnormal dreams, sedation, or feelings of euphoria.

The reason lies in the difficulty in finding drugs that bind to only one subtype of 5-HT2 receptors (bear with me, there are only three - just remember that 5-HT2C receptor stimulation is most desirable here). Classic drugs that cause hallucinations - LSD and mescaline - act by stimulating the 5-HT2A receptor. Drugs that stimulate the next subtype, the 5-HT2B receptor, have been associated with heart valve disease, the major reason for withdrawal of the fenfluramine part of the fen-phen weight loss combination drug. Stimulating the 5-HT2C receptor alone does not appear to cause hallucinations or heart valvular problems.

Frankly, I'm surprised that the DEA chose to classify lorcaserin as Schedule IV. In my mind, Schedule V would have been more appropriate. But I believe that concerns about the widespread prescribing of lorcaserin played into the more stringent classification.


Lorcaserin, currently marketed under the trade name Belviq and previously Lorqess during development, is a weight-loss drug developed by Arena Pharmaceuticals. Lorcaserin is a selective 5-HT2C receptor agonist, and in vitro testing of the drug showed reasonable selectivity for 5-HT2C over other related targets. 5-HT2C receptors are located almost exclusively in the brain, and can be found in the choroid plexus, cortex, hippocampus, cerebellum, amygdala, thalamus, and hypothalamus. The activation of 5-HT2C receptors in the hypothalamus is supposed to activate proopiomelanocortin (POMC) production and consequently promote weight loss through satiety. This hypothesis is supported by clinical trials and other studies. While it is generally thought that 5-HT2C receptors help to regulate appetite as well as mood, and endocrine secretion, the exact mechanism of appetite regulation is not yet known. Lorcaserin has shown 100x selectivity for 5-HT2C versus the closely related 5-HT2B receptor, and 17x selectivity over the 5-HT2A receptor

  • How it works: According to the National Institutes of Health, lorcaserin, which is available by the brand name Belviq, works as a serotonin receptor agonist. Translation: It makes you feel full faster. When paired with a low-calorie diet and exercise, it generally helps people lose weight within three months.
  • Side effects: While you take it, you may deal with headaches, dizziness, and fatigue, says Rader. Another downside is that the medication helps with weight control only if you continue to take it. So once you cut it out, you could see the pounds creep back on.
  • Who could take it: Though lorcaserin is a derivative of the appetite suppressant fenfluramine, which was banned for causing heart problems, it doesn't cause cardiac issues. So it's a good choice for people who can't tolerate the stimulant side effects of other meds, like a racing heartbeat and jitters, says Rader.

Liver:
Lorcaserin was in clinical use for eight years when it was withdrawn because of concerns regarding an excess in cancer risk after long term use. In prelicensure studies and while in clinical use, lorcaserin was not found to be associated with serum enzyme elevations during therapy or to instances of clinically apparent liver injury.

Lorcaserin Hepatotoxicity:
In premarketing clinical trials, serum aminotransferase elevations were no more common among patients receiving lorcaserin than placebo. Clinically apparent liver injury due to lorcaserin has not been reported, but the numbers of patients treated has been limited.

E Likelihood score: E (unlikely cause of clinically apparent liver injury).


Cardio Vascular:
Treatment with the serotonin receptor agonist lorcaserin yielded sustained weight loss over a median follow-up of 3 years without an excess risk for major adverse CV events in adults with overweight or obesity at high CV risk, according to new data from the CAMELLIA-TIMI 61 study. Randomized, double-blind, placebo-controlled trial of more than 12,000 patients in eight countries with atherosclerotic CVD or multiple CV risk factors, researchers also found no increased risk for new or worsening valvulopathy in patients assigned lorcaserin (Belviq, Eisai) compared with placebo, which has been a concern with other weight-loss drugs.

Cardio Vascular:
In the past, several promising weight loss medications have been pulled from the market because of cardiovascular side effects. Eisai's weight loss drug lorcaserin does not increase people's risk of major cardiovascular events, according to data from a study of 12,000 overweight or obese patients. Everyone in the study, which was funded by Eisai, had atherosclerotic cardiovascular disease or multiple risk factors for heart disease. With half the study participants tracked for at least three years, there was no difference in the combined risk of heart attack, stroke or any type of cardiovascular death between people taking lorcaserin and people taking a dummy pill.

Epilepsy:
Lorcaserin, a selective serotonin receptor agonist commonly used for weight loss, is a potentially effective anti-seizure medication for patients with severe epilepsy of childhood onset, according to a study in Neurology. These promising preliminary findings support the need for randomized, controlled trials of lorcaserin for treatment-resistant epilepsies, the researchers concluded.

Pregnancy:
Contraindicated during pregnancy, because weight loss offers no benefit to a pregnant woman and may result in fetal harm; limited data on lorcaserin use in pregnant women are not sufficient to determine drug-associated risk of major congenital malformations or miscarriage; appropriate weight gain based on pre-pregnancy weight is currently recommended for all pregnant women, including those who are already overweight or obese, due to the obligatory weight gain that occurs in maternal tissues during pregnancy; in rats, maternal exposure to lorcaserin in late pregnancy resulted in lower body weight in offspring which persisted to adulthood; advise pregnant women of potential risk to a fetus.

Diabetes:
If you have diabetes, this product may affect your blood sugar. Check your blood sugar regularly as directed and share the results with your doctor. Tell your doctor right away if you have symptoms of low blood sugar. Your doctor may need to adjust your diabetes medication, exercise program, or diet.

Lorcaserin will not treat any underlying health condition (such as heart disease, diabetes, high blood pressure). Keep taking any other medications your doctor has prescribed to treat these conditions.

Important Information:

Do not use lorcaserin if you are pregnant. Weight loss during pregnancy can harm an unborn baby.

Serious drug interactions can occur when certain medicines are used together with lorcaserin. Tell each of your healthcare providers about all medicines you use now, and any medicine you start or stop using.

Avoid driving or hazardous activity until you know how lorcaserin will affect you. Your reactions could be impaired.

Avoid taking cough and cold or allergy medications while taking lorcaserin.

Do not take any other prescription or over-the-counter weight-loss products without your doctor's advice.

Interactions:

Drug Interactions (188) Alcohol/Food Interactions (1) Disease Interactions (10)


What other drugs will affect Lorcaserin?
Tell your doctor about all your current medicines. Many drugs can affect lorcaserin, especially:
  • cabergoline
  • linezolid
  • lithium
  • St. John's wort
  • tramadol
  • tryptophan (also called L-tryptophan)
  • any type of antidepressant
  • cold or cough medicine that contains dextromethorphan (a cough suppressant)
  • erectile dysfunction medicine:
    • avanafil
    • sildenafil
    • tadalafil
    • Cialis
    • Levitra
    • Viagra
    • others
  • medicine to treat mental illness, anxiety, or a mood disorder
  • a "triptan" migraine headache medicine:
    • almotriptan
    • frovatriptan
    • rizatriptan
    • sumatriptan
    • zolmitriptan
    • Imitrex
    • Maxalt
    • Zomig
    • others
This list is not complete and many other drugs may affect lorcaserin. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

A total of 188 drugs are known to interact with Lorcaserin.

  • 80 major drug interactions
  • 105 moderate drug interactions
  • 3 minor drug interactions

Lorcaserin affects chemical signals in the brain that control appetite. Lorcaserin works by helping you feel full with smaller meals. Lorcaserin is used together with diet and exercise to treat obesity. Lorcaserin will not treat any underlying health condition (such as heart disease, diabetes, high blood pressure). Keep taking any other medications your doctor has prescribed to treat these conditions. Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

What is the most important information I should know about Lorcaserin?
You should not use lorcaserin if you are allergic to it, or if you are pregnant. Before you take lorcaserin, tell your doctor if you have diabetes, congestive heart failure, a heart valve disorder, sickle cell anemia, leukemia or myeloma, kidney or liver disease, or a physical deformity of the penis (such as Peyronie's disease). Do not use lorcaserin if you are pregnant. Do not use lorcaserin if you are pregnant. Lorcaserin may be habit-forming. Do not take this medication in larger or smaller amounts or for longer than recommended. There are many other drugs that can interact with lorcaserin. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products.

Belviq (lorcaserin hydrochloride)
Maximum Dosage:
Prescribers Digital Reference
Adults:20 mg/day PO
Geriactric:20 mg/day PO
Adolescents:Safety and efficacy have not been established.
Children:Safety and efficacy have not been established.
Infants:Safety and efficacy have not been established.
Neonates:Safety and efficacy have not been established.

Belviq (lorcaserin hydrochloride)
Side Effects:
Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.
RxList
Stop using lorcaserin and call your doctor at once if you have:
  • unusual changes in mood or behavior, thoughts of suicide or hurting yourself
  • dry eyes, blurred vision
  • feelings of standing next to yourself or being outside of your body
  • memory problems, trouble concentrating
  • breast swelling (in women or men), nipple discharge
  • penis erection that is painful or lasts longer than 4 hours
  • heart problems - fast heart rate, trouble breathing, dizziness, ongoing weakness, or swelling in your arms, hands, legs, or feet
  • high levels of serotonin in the body - agitation, hallucinations, fever, fast heart rate, overactive reflexes, nausea, vomiting, diarrhea, loss of coordination, fainting
  • severe nervous system reaction - very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, feeling like you might pass out
Common side effects may include:
  • headache, dizziness, feeling tired
  • dry mouth, cough
  • nausea, constipation
  • back pain
  • low blood sugar (in people with diabetes)
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Pediatric:
Appropriate studies have not been performed on the relationship of age to the effects of lorcaserin in the pediatric population.

Safety and efficacy have not been established.

Geriatric:
Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of lorcaserin in the elderly. However, elderly patients are more likely to have kidney problems, which may require caution and an adjustment in the dose for patients receiving lorcaserin.

Other Medical Problems:
Make sure you tell your doctor if you have any other medical problems, especially:

  • Bradycardia (slow heartbeat)
  • Congestive heart failure
  • Depression
  • Diabetes
  • Heart block, history of
  • Heart valvular disease
  • Hyperprolactinemia (high prolactin in the blood)
  • Hypoglycemia (low blood sugar)
  • Mental illness, history of
  • Pulmonary hypertension, history of - Use with caution. May make these conditions worse
  • Kidney disease, moderate
  • Liver disease, severe - Use with caution. The effects may be increased because of slower removal of the medicine from the body
  • Kidney disease, severe or end-stage - Use is not recommended in patients with this condition
  • Abnormal penis, including curved penis, birth defects of the penis, and Peyronie's disease
  • Leukemia (blood related cancer)
  • Multiple myeloma (blood related cancer)
  • Sickle-cell anemia (blood disorder) - Lorcaserin should be used with caution in these patients as problems with prolonged erection of the penis may occur

VA PDF Lorcaserin

Caymanchem PDF Lorcaserin

Lorcaserin:

It was removed from the market in the United States in 2020 due to an increased risk of cancer detected in users of Belviq.

  • A weight-loss drug
  • Used long term for weight loss in those who are obese.
  • It reduces appetite by activating a type of serotonin receptor known as the 5-HT2C receptor in a region of the brain called the hypothalamus, which is known to control appetite.

In December 2012, the US Drug Enforcement Administration proposed classifying lorcaserin as a Schedule IV drug because it has hallucinogenic properties at higher than approved doses and users could develop psychiatric dependencies on the drug. On 7 May 2013, the US Drug Enforcement Administration classified lorcaserin as a Schedule IV drug

In February 2020, the FDA requested that the manufacturer lorcaserin voluntarily withdraw the drug from the US market because a safety clinical trial showed an increased occurrence of cancer. The drug manufacturer, Eisai, has submitted a request to voluntarily withdraw the drug.

  
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