The use of sibutramine (Meridia) in patients with obesity and ovarian dysfunction.

Sibutramine (Goldline)[edit | edit code]

Sibutramine is a derivative of the little-known dimethylamphetamine (metrotonin), whose psychic effects are further weakened by the addition of large structures on one side of the Reduxin Meridia
Sibutramine

(trade names
Goldline
,
Meridia
,
Reduxin
) is a pharmacological agent for suppressing appetite during weight loss. Sibutramine is also included in the Prohibited List of the World Anti-Doping Agency (2010) and is classified as a substance prohibited during competition.[1] The original drug and its analogues are available in Russia. Not to be confused with reduxin light.

Sibutramine is manufactured by Abbott Laboratories under the brands: Meridia, Reductil and Sibutrex. In the US, it is classified as a drug that can cause addiction, although it is not. The only reason for control is its abuse as an anorectic, receiving which for the first time as prescribed by a doctor, people then begin to continue unauthorized use for weight loss on their own.

Available in Russian pharmacies under the trademarks Goldline (price ≈ 900 rubles for 30 capsules of 10 mg) Reduxin (price ≈ 1,500 rubles for 30 capsules of 10 mg).

Legal status[edit | edit code]

Sibutramine, its salts, isomers, esters, all dosage forms and trade names are included in the list of potent substances on the basis of Decree of the Government of the Russian Federation of December 29, 2007 N 964. Criminal liability entails: illegal production, processing, acquisition, storage, transportation or forwarding for the purpose of sales, as well as illegal sale, or equipment for its production or processing.

Large size

Sibutramine is 0.5 g or more.[2]

Action of Sibutramine[edit | edit code]

Mechanism of action
Mechanism of action Goldline

Structurally, sibutramine is similar to the class of amphetamines, although it does not have their biological properties. Sibutramine, a centrally acting drug, is a reuptake inhibitor of serotonin (53%), norepinephrine (54%) and dopamine (16%), as a result of which it increases the level of these mediators in the intersynaptic space. By thus increasing the concentration of serotonin in the center of hunger and satiety, the drug suppresses appetite.[3]

The main effects of sibutramine:

1. inhibition of presynaptic reuptake of monoaminergic neurotransmitters in the central nervous system and suppression of appetite;
2. activation of the secretion of anorexigenic and decreased secretion of orexigenic neuropeptides;
3. increased energy expenditure and activation of the sympathetic effects of the peripheral nervous system.

Sibutramine may cause mood changes (improvement) because the control of energy homeostasis and mood often involves overlapping brain regions (eg, the serotonergic system)[4]. Sibutramine was approved by the FDA in 1997 as a weight loss drug only.

Contraindications[edit | edit code]

• Mental illness
• Addiction
• Hypersensitivity
• Heart and artery diseases
• Hypertonic disease
• Angle-closure glaucoma
• Prostate hyperplasia
• Pregnancy, lactation and childhood
• Concomitant use of MAO inhibitors (antidepressants)

Harm and side effects[edit | edit code]

Side effects from the cardiovascular system occur relatively often (about 10%): an increase in blood pressure by 2–20 mm Hg, an increase in heart rate by 3–20 beats/min [5]. In 2010, the FDA expressed concern about the high risk of heart disease and stroke when using Sibutramine in people with cardiovascular disease. [6] Side effects associated with its noradrenergic stimulation of the hypothalamic mechanisms that regulate appetite and sympathomimetic properties are also observed: dry mouth, nausea, taste changes, indigestion, constipation, insomnia, anxiety, algomenorrhea, muscle and joint pain, difficulty urination, blurred vision.

At a young age, in the absence of heart and vascular disease, Sibutramine is considered a safe drug. If side effects occur, after withdrawal all symptoms disappear without harm to health. Severe complications are rare.

Scientists believe that a person is at greater risk when being obese than when using Sibutramine. [7]

Sibutramine as a drug[edit | edit code]

The high level of drug control in the West gives rise to false rumors that Sibutramine is a drug. This drug does not cause addiction because it does not increase the release of dopamine from synapses, and a high level of control is associated with the unauthorized use of Sibutramine as a means of weight loss, which can only indicate high efficiency.

Doses of Sibutramine and method of use for weight loss[edit | edit code]

The average dose of Sibutramine is 10 mg once a day in the first half of the day; if this is not enough, after a few days of use the dose can be increased to 15 mg per day. As a rule, 6 months after the start of treatment and before stopping the drug, appetite normalizes, and body weight is set to a plateau[8]. Do not exceed the dose, as side effects and complications are often associated with this. Reception is carried out in combination with a low-calorie diet and exercise. After stopping the drug, weight gain is often observed. Sibutramine is an effective means of reducing body weight and food intake when treated for a short period of time (6-12 months), its effectiveness decreases with long-term use of the drug (> 1 year)[9].

pharmachologic effect

The effect of the drug is more anorexigenic, it suppresses hunger and at the same time increases a person’s body temperature, which leads to accelerated fat burning, as well as a decrease in the amount of food consumed and the formation of a fat layer. Treatment of obesity with sibutramine is really effective; weight goes off quite quickly. However, like any antidepressant, this drug has side effects.

The peculiarity of this substance is that it does not cause a psychostimulating effect, but activates beta-adrenergic receptors and inhibits the reuptake of brain neurotransmitters, in particular, serotonin and dopamine, “hormones of joy.” Weight loss is affected by lowering cholesterol and uric acid levels, as well as increasing lipoprotein levels.

A few facts: when consumed, blood pressure and pulse slightly increase, the medicine is absorbed by 78%, the maximum concentration occurs after 1.5-2 hours. Its processing is carried out mainly in the liver; breakdown products are found in the blood within 4 days.

How addiction treatment works:

• MOTIVATION Recommendations of a psychologist Visit of a specialist Guarantee of results
• DETOXIFICATION Home visit (in hospital) Cleansing of the body Diagnostics by a psychiatrist
• REHABILITATION Social program Standard program Individual program
• SOCIAL ADAPTATION Employment opportunity Job training Outpatient support
• SUPPORT FOR RELATIVES Self-help groups Webinars (online) Individual consultations

Legal status[edit | edit code]

Since January 24, 2008, sibutramine has been included in the government-approved list of potent drugs[11]. This means that its sale is allowed only in pharmacies with a prescription.

Despite the fact that in 2007 sibutramine was not included in this list, Svetlana Sukhorukova was sentenced for selling sibutramine in 2007 to 5 years under Art. 234 of the Criminal Code of the Russian Federation - illegal trafficking of potent substances. Sibutramine is also included in the Prohibited List of the World Anti-Doping Agency (2010) and is classified as a substance prohibited during competition.

Measures restricting the free sale of drugs containing sibutramine took place in 2008-2010 not only in Russia. Campaigns to suspend sales have taken place in the United States, a number of European Union countries and Ukraine. This measure was applied after receiving the results of a study where, with long-term use (several years) of 15 mg of sibutramine in patients with hypertension who had suffered a heart attack and stroke, a number of severe side effects were identified. The revocation of documents giving the right to trade in pharmacies, according to the wording of the regulatory authorities, is temporary, until special circumstances are clarified. In Ukraine, this ban does not apply to dietary supplements containing sibutramine in a higher dose (35-50 mg), due to the lack of legal procedures for proving the presence of this component in a weight loss product. There are studies suggesting that side effects are associated with the presence of the S-isomer in racemic sibutramine. On the contrary, R-sibutramine has a 2-fold lower risk of developing undesirable consequences. The presence of an optically pure dosage form containing R-sibutramine could, with a sufficient evidence base, have a positive impact on the current situation.

The Ministry of Health reports that drugs containing sibutramine as the only active ingredient are subject to registration and calls them “Slimia” (capsules), “Meridia” (capsules), “Goldline” (capsules) and “Lindaxa” (capsules). At the same time, the trademark “Reduxin” (capsules) is not subject to subject-quantitative accounting

, since it contains a combination of active substances: sibutramine + microcrystalline cellulose, and therefore does not belong to potent substances.[12]

Side effects

• thirst, dry mouth;
• headache;
• dizziness;
• tachycardia;
• increased blood pressure;
• insomnia;
• haemorrhoids;
• stool disorder.

However, quite often, in addition to these rather harmless consequences, it also causes quite serious health complications, if they occur, you should immediately stop taking this drug.

The most common side effects of sibutramine use are:

• hypertension;
• ischemia;
• bulimia;
• anorexia;
• mental disorders;
• disruption of the gastrointestinal tract:
• negative effect of sibutramine on potency;
• addiction and irresistible craving for capsules;
• depression, anxiety;
• fainting, loss of consciousness;
• anemia.

Quite often, people start taking the drug on their own, without a doctor’s prescription; uncontrolled use without taking into account contraindications leads to quite serious consequences for the body of a person who wants to lose weight. Only a doctor, after a series of examinations, can prescribe a patient a particular drug in a certain dosage and for a certain period.

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8 call our specialist

Links[edit | edit code]

1. "Top obesity drug sibutramine being suspended." 2010-01-22.
2. https://base.garant.ru/12158202/#block_3000
3. Heal, D.J.; Aspley; Prow; Jackson; Martin; Cheetham (1998). “Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine". International journal of obesity and related metabolic disorders : journal of the International Association for the Study of Obesity 22 Suppl 1: S18–28; discussion S29.
4. Colman E. Anorectics on trial: a half century of federal regulation of prescription appetite suppressants. Ann. Intern. Med. 2005;143(5):380-385.
5. Araujo JR, Martel F. Sibutramine effects on central mechanisms regulating energy homeostasis. Curr Neuropharmacol. 2012 Mar;10(1):49-52.
6. "Meridia (sibutramine hydrochloride): Follow-Up to an Early Communication about an Ongoing Safety Review"
7. Bruce Japsen (13 March 2005). “FDA weighs decision on Meridia; Health advisory likely for Abbott obesity drug." Chicago Tribune. Chicago, Illinois. pp. 1.
8. Padwal RS, Majumdar SR Drug treatments for obesity: orlistat, sibutramine, and rimonabant //The Lancet. – 2007. – T. 369. – No. 9555. – pp. 71-77.
9. Fernstrom JD, Choi SJ The development of tolerance to drugs that suppress food intake //Pharmacology & therapeutics. – 2008. – T. 117. – No. 1. – pp. 105-122.
10. price from 100 rub.
11. Decree of the Government of the Russian Federation of December 29, 2007 N 964. Moscow Retrieved August 2, 2012.
12. https://doctorpiter.ru/articles/10100/

What to do if an overdose occurs?

If a person does not follow the recommendations given by the doctor, independently extends the course of treatment and increases the daily dosage, the risk of overdose is quite high. To date, there is no antidote. An overdose of a drug causes a whole range of negative consequences. This includes a headache, a sharp increase in blood pressure, muscle weakness, and tachycardia.

If you or a loved one experience these symptoms, you should urgently call an ambulance to your home. If you want to get high-quality help from professionals in their field, call the doctors of the Center for Healthy Youth to your home; we work both in Moscow and the region, and have a network of centers throughout the country. You also have the opportunity to get a free anonymous consultation with a narcologist.

What to do before the specialist arrives:

• give the patient a lot of water, tea and coffee are not suitable;
• try to induce vomiting and empty the stomach;
• take activated carbon, smecta or other adsorbent.

After providing first aid, doctors hospitalize the victim in a hospital and do not carry out detoxification and therapeutic procedures until the health condition is completely normalized.

And finally...

So, if the problem of overweight or obesity is relevant to you, approach this problem with all responsibility. Since losing weight is not an easy process, it should be carried out exclusively under the supervision of qualified specialists. Firstly, it is necessary to develop a correct, balanced diet, which means you need to consult a qualified nutritionist, who, if necessary, can also select a truly effective and safe drug. The second important point is drawing up a correct physical activity program that suits you, so you can’t do it without a trainer either. And finally, since we are surrounded by many temptations and the process of losing weight can be accompanied by difficulties of a psychological nature, the help of a psychologist will also not be superfluous. And remember that the main thing is not only to effectively lose excess weight, but also not to harm your health. Otherwise, who wants a disastrous result?

Obesity: some statistics

WHO estimates that in 2008, about 1.5 billion people over 20 years of age worldwide were overweight, of whom more than 200 million men and 300 million women were obese.
In the United States, 54 million people are obese. In Europe the numbers are smaller, but still significant. And the saddest thing is that obesity rates are on the rise in most countries. WHO projections are also bleak: by 2015, approximately 2.3 billion adults will be overweight, and more than 700 million will be obese. As for Russia, according to the Ministry of Health and Social Development, in 2009 the incidence of obesity in our country was 789.3 per 100 thousand people. According to M. O. Apletaeva, a nutritionist at the Weight Control Clinic, today approximately 40–50% of the Russian population is overweight, and if earlier this problem was more relevant for middle-aged and older people, now a large percentage of people Those who are overweight are young people from 25 to 35 years old.

Who should not take the medicine?

Each medication has its own list of contraindications that must be studied. In this case, the drug is prohibited for people with severe diseases of internal organs: heart, kidneys, liver, genitourinary system. Among the main contraindications are:

• elderly age;
• minority;
• pregnancy and lactation period;
• hypertension;
• glaucoma;
• bulimia;
• addiction;
• alcoholism.

Sibutramine is completely incompatible with alcohol; this combination causes unpredictable side effects, as well as accelerating the development of addictions and depression of the nervous system.

When using medications, pay attention to the instructions; do not take pills without a doctor’s prescription!