Sibutramine was a medication that was primarily used to help
overweight individuals lose weight, but was also sometimes
prescribed to help people keep the weight off. This drug belonged
to a class of medications known as appetite suppressants, which are
said to aid in curbing hunger by altering the appetite control
centers in the brain.
1. Quick Details:
|Water Solubility :||2.9 mg/mL|
|Appearance:||White crystal powder|
|Storage:||Shading, confined preservation|
2. Sibutramine Description:
Sibutramine is a medication that assists with weight-loss by
altering neurotransmitters within the brain. Neurotransmitters are
chemicals that are produced and released by nerves in order to
communicate with other nerves. Released neurotransmitters may
attach to other nerves or they may be taken up again by the nerves
that release them, a process termed reuptake. Sibutramine blocks
the reuptake of the neurotransmitters dopamine, norepinephrine, and
serotonin. Blocking the reuptake of neurotransmitters alters the
balance of neurotransmitters within the nerve cells and thereby
affect nerve function and interaction.
Patients taking sibutramine may achieve a 5-10% reduction from
their baseline weight. Additionally, sibutramine-assisted weight
loss has been accompanied by improvement in blood lipids (e.g,
cholesterol). Sibutramine was approved by the FDA in 1997.
Neurotransmitters are chemicals that the nerves of the body create
and release in order to communicate with other nerves. Sometimes
these released chemicals become attached to other nerves, while at
other times they become reattached to the same nerve that released
them. Sibutramine worked by preventing these chemicals - which
included norepinephrine, serotonin, and dopamine - from reattaching
to the same nerves that produced them. This process allowed for an
increase of neurotransmitters in the synaptic clefts, which was
thought to help decrease hunger in the patient.
Sibutramine is used together with diet and exercise to treat
obesity that may be related to diabetes, high cholesterol, or high
4. Mechanism of Action and Effect:
Sibutramine is a serotonin (5-hydroxytryptamine, 5-HT) and
norepinephrine (NE) reuptake inhibitor (SNRI).In vitro testing
found sibutramine to be much less potent than its primary and
secondary amine metabolites in inhibiting monoamine reuptake.
Therefore, the pharmacological actions of sibutramine are thought
to be due predominantly to its active metabolites. The metabolites
of sibutramine inhibit 5-HT and NE reuptake with potencies
comparable to those of fluoxetine and desipramine, respectively.
Combined NE and 5-HT reuptake inhibition is thought to promote a
sense of satiety, leading to a decrease in energy intake, and,
possibly, to increase resting metabolic rate. Randomized,
placebo-controlled, double-blind studies in obese and in nonobese
subjects have shown significant reductions in self-rated premeal
hunger and in energy intake with sibutramine use, even in the
absence of an imposed reduced-calorie diet. One study found no
difference in the decrease in resting energy expenditure associated
with weight loss between subjects receiving sibutramine and
subjects receiving placebo, in spite of significantly greater
weight loss in the sibutramine group. In another study, basal
metabolic rate, as measured by indirect calorimetry, increased more
in sibutramine-treated patients than in patients receiving placebo;
however, this finding has not been consistent.
5. Sibutramine Dosage:
Take exactly as prescribed by your doctor. Do not take in larger or
smaller amounts or for longer than recommended. Follow the
directions on your prescription label.Sibutramine is usually taken
once daily. Follow your doctor's instructions.Your doctor may
occasionally change your dose to make sure you get the best
results.Sibutramine can be taken with or without food.
You should lose at least 4 pounds during the first 4 weeks of
taking sibutramine and eating a low calorie diet. Tell your doctor
if you do not lose at least 4 pounds after taking the medication
for 4 weeks.Your blood pressure and pulse will need to be checked
often. Visit your doctor regularly.Sibutramine should not be taken
for longer than 2 years.
|Description||white crystal powder||Conforms|
|Identification||The reaction is positive||The reaction is postitive|
|Assay||98.5 ~ 102%||99.90%|
|Loss on drying||<0.5%||0.20%|
|Residuc on ignition||<0.1%||0.07%|
|PH||5.0 ~ 7.5||6.9|
|Specific rotation||+18.5 ~ +20 °||+19.6°|
|Related substances||The any secondary spot <0.5%||<0.5%|
|Crystallinity||Meets the requirements||Conforms|
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