Sibutramine

Sibutramine is an active ingredient that is used to treat overweight (obesity). The active ingredient is used in combination with diet, behavioral changes and exercise. It belongs to the anorectic group and is a serotonin-norepinephrine reuptake inhibitor and is therefore closely related to antidepressants. In 2010, the European Medicines Agency (EMA) decided to withdraw the active ingredient from the market due to severe side effects affecting the cardiovascular system. Sibutramine causes an increased risk of suffering a heart attack or stroke and can therefore have fatal side effects. In addition, the EMA reassessed the benefit-risk profile and came to the conclusion that patients who took sibutramine only lost 2-4 kg more weight. This effect was too small for the EMA to keep the drug on the market. In addition, the effect stops when you stop taking sibutramine.

Sibutramine is usually present as sibutramine hydrochloride. It inhibits the appetite and causes a feeling of satiety. The active ingredient works by preventing the reuptake of norepinephrine and serotonin into the nerve cell. This increases the concentration in the synaptic cleft, which causes the feeling of satiety. As a result of this effect, patients are less hungry and eat less. Animal studies have also shown that sibutramine increases energy levels. However, this could not be confirmed in human studies. Sibutramine was originally intended to be developed as an antidepressant, but was never studied or approved for this purpose. The two antidepressants venlafaxine and duloxetine are available as antidepressants and also have an appetite-suppressing effect.

Sibutramine is broken down in the liver, mainly via the CYP3A4 isoenzymes. The bioavailability of sibutramine, i.e. the percentage of the active substance that is available in the blood, is 77%. The half-life, i.e. the time the body needs to excrete half of the active ingredient, is around 1 hour.

Always take sibutramine exactly as described in the package leaflet or as advised by your doctor.

The usual recommended starting dose is 10 mg daily in the morning. After 4 weeks, the dose can be increased to 15 mg daily if 10 mg is not enough to lose weight.

The following side effects may occur:

Very common:

• Constipation
• sleep disturbances
• Dry mouth

Frequent:

• Palpitations
• palpitations
• cardiac arrhythmia
• Increased blood pressure
• hot flushes
• malaise
• worsening of hemorrhoids
• sweating
• unusual taste
• drowsiness
• tingling
• headache
• anxiety

Occasionally:

• Kidney problems
• elevated liver enzyme levels
• skin rash
• bruising
• diarrhea
• vomiting
• Bleeding in the digestive system
• seizures
• blurred vision
• depression
• suicidal thoughts
• restlessness
• hair loss
• Loss of short-term memory
• impotence
• Disorders of the menstrual cycle

Interactions may occur if the following medicines are taken at the same time:

• Antibiotics such as rifampicin, erythromycin, troleandomycin, clarithromycin
• Medication containing the substances ephedrine, pseudoephedrine or xylometazoline
• carbamazepine
• phenobarbital
• phenytoin
• ketoconazole
• itraconazole
• warfarin
• Acetylsalicylic acid
• clopidogrel
• Sumatriptan
• Dihydroergotamine
• fentanyl
• pentazocine
• pethidine
• Dextromethorphan
• Ciclosporin
• dexamethasone
• MAO inhibitors
• Selective serotonin uptake inhibitors (SSRI)
• tricyclic antidepressants
• Alcoholic beverages can reduce the weight-lowering effect of sibutramine.

Sibutramine must NOT be taken in the following cases:

• in case of hypersensitivity or allergy to sibutramine
• if an illness is the reason for the weight problem
• in the case of eating disorders
• when taking medication for the treatment of depression
• in Tourette's syndrome
• if you have taken tryptophan, phentermine or diethylpropion in the last 2 weeks
• with a blood pressure above 140 mmHg
• with heart problems, now or in the past
• with hardening of the arteries, now or in the past
• after a stroke
• severe liver or kidney problems
• problems with the prostate, thyroid or an adrenal tumor
• with eye diseases
• drugs, medication or alcohol abuse, now or in the past

Sibutramine is listed as a stimulant in the doping list!

Sibutramine can affect judgment, thinking or reaction time .

Sibutramine should NOT be used under the age of 18 or over the age of 65.

Sibutramine should NOT be used during pregnancy and breastfeeding.

In the past, sibutramine was often illegally added to food supplements. The doses contained in these supplements were significantly higher than the recommended daily doses.

In 2010, sibutramine was withdrawn from both the European market and the US market. The CHMP (Committee for Medicinal Products for Human Use) of the European Medicines Agency (EMA) based its decision on the results of the SCOUT study (Sibutramine Cardiovascular Outcome Trial). The active substance has severe side effects on the cardiovascular system. In Europe, there were 2 deaths caused by sibutramine. In the USA, 34 deaths are reported to have been caused by sibutramine.