Sibutramine, formerly sold under the brand name Meridia among others, is an appetite suppressant which has been discontinued in many countries. It works as a serotonin–norepinephrine reuptake inhibitor similar to a tricyclic antidepressant. Until 2010, it was widely marketed and prescribed as an adjunct in the treatment of obesity along with diet and exercise. However, the drug remains available in some countries.buy sibutramine hydrochloride 20 mg
As of 2018, the FDA still found sibutramine in over 700 diet supplements marketed as “natural”, “traditional” or “herbal remedies”
Medical uses
Sibutramine has been used to produce appetite suppression for the purpose of attaining weight loss in the treatment of patients with obesity.
Pharmacokinetics
Sibutramine is well absorbed from the gastrointestinal tract (77%), but undergoes considerable first-pass metabolism, reducing its bioavailability. The drug itself reaches its peak plasma level after 1 hour and has also a half-life of 1 hour. Sibutramine is metabolized by cytochrome P450 isozyme CYP3A4 into two pharmacologically active primary and secondary amines (called active metabolites 1 and 2) with half-lives of 14 and 16 hours, respectively. Peak plasma concentrations of active metabolites 1 and 2 are reached after three to four hours. The following metabolic pathway mainly results in two inactive conjugated and hydroxylated metabolites (called metabolites 5 and 6). Metabolites 5 and 6 are mainly excreted in the urine.sibutramine hydrochloride monohydrate
Chemistry
Sibutramine has usually been used in the form of the hydrochloride monohydrate salt.
Detection in body fluids
Sibutramine and its two active N-demethylated metabolites may be measured in biofluids by liquid chromatography-mass spectrometry. Plasma levels of these three species are usually in the 1–10 μg/L range in persons undergoing therapy with the drug. The parent compound and norsibutramine are often not detectable in urine, but dinorsibutramine is generally present at concentrations of >200 μg/L.
Weight loss pills
what is Sibutramine hydrochloride is a weight loss drug, it is hydrochloride salt form of sibutramine , and the pharmacological effects are fully consistent with of sibutramine , but the stability and solubility are better than sibutramine.
Sibutramine hydrochloride is firstly used to treat depression, in their clinical application process , people find that the effect of weight loss is significantly stronger than the effect of the antidepressant . On one hand ,by inhibiting the reuptake of serotonin, which makes the body reduce hunger, it can suppress appetite and control caloric intake effectively ; on the other hand, by activating the adrenergic receptors, which increases adipose tissue consumption, it can increase metabolism and energy consumption;it has obvious weight loss effect, but it may cause endangering serious side effects such as high blood pressure, high heart rate, anorexia, insomnia, abnormal liver function.
The above information is edited by the chemicalbook of Tian Ye.
Precautions
Sibutramine hydrochloride belongs to the serotonin and norepinephrine reuptake inhibitors, it has the dual role of inhibiting appetite and enhancing metabolism, it can be used for the treatment of obesity which diet and exercise can not control.
There are many taboos in clinical practice of sibutramine hydrochloride , for example, patients with severe hypertension or patients with severe liver and kidney dysfunction, or patients with angle-closure glaucoma and women after childbirth, should not use it . Because the physiological effects of 16 years old or younger minors have not yet been confirmed, use of it should be prohibited. Also doses should be strictly controlled by users, the recommended starting dose is 10 mg per day for adults, the maximum should not exceed 15 mg. If there is overdose, patients should go to hospital for treatment, there is no specific antidote, only symptomatic treatment can be taken in clinic.
Uses
It is used as an antidepressant.sibutramine hydrochloride side effects
Uses
Sibutramine Hydrochloride is a 5-HT and noradrenaline reuptake inhibitor.
Uses
Sibutramine hydrochloride monohydrate was used as standard to screen dietary supplements for sibutramine using ion mobility spectrometer.1
Uses
Anorexic; antidepressant.
English name:Sibutramine hydrochloride
CAS:84485-00-7 CBNumber:CB3783665 MF:C17H27Cl2N MW:316.31
Melting point 190-200°C
storage temp. room temp
solubility Soluble to 5 mM in water and to 100 mM in DMSO
form Powder
CAS DataBase Reference 84485-00-7(CAS DataBase Reference)
FDA UNII 9GG866ZP1E
More Introduction:https://en.wikipedia.org/wiki/Sibutramine
