Each capsule contains sibutramine hydrochloride monohydrate 15 mg
Description
Sibutramine produces its therapeutic effect by norepinephrine, serotonin and dopamine reuptake inhibition. Sibutramine and its major pharmacologically active metabolites (M1 and M2) have low affinity for serotonin (5 HT1, 5 HT1A, 5 HT1B, 5 HT2A, 5 HT2C), norepinephrine (b1 and b3, a1 and a2), dopamine (D1 and D2) benzodiazepine and glutamate receptors as well as lack monoamine oxidase inhibitory activity.
Sibutramine produces its therapeutic effect by norepinephrine, serotonin and dopamine reuptake inhibition. Sibutramine and its major pharmacologically active metabolites (M1 and M2) have low affinity for serotonin (5 HT1, 5 HT1A, 5 HT1B, 5 HT2A, 5 HT2C), norepinephrine (b1 and b3, a1 and a2), dopamine (D1 and D2) benzodiazepine and glutamate receptors as well as lack monoamine oxidase inhibitory activity.
Indications
Sibutrex is indicated for the management of obesity, including weight loss and maintenance of weight loss, and should be used in conjunction with a reduced calorie diet. Sibutrex is recommended for obese patients with an initial body mass index > 30 kg/m2 or > 27 kg/m2 in the presence of other risk factors (e.g. hypertension, diabetes, dyslipidemia).
Sibutrex is indicated for the management of obesity, including weight loss and maintenance of weight loss, and should be used in conjunction with a reduced calorie diet. Sibutrex is recommended for obese patients with an initial body mass index > 30 kg/m2 or > 27 kg/m2 in the presence of other risk factors (e.g. hypertension, diabetes, dyslipidemia).
Body mass index is calculated by taking the patient's weight, in kg, and dividing by the square of the height of the patient, in metres.
Dosage and administration
The recommended starting dose of Sibutrex is 2 x 5mg once daily with or without food. If there is inadequate weight loss, the dose may be titrated after four weeks to a total of 15 mg once daily. Doses above 15 mg daily are not recommended. The 5 mg dose should be reserved for patients who do not tolerate the 10 mg dose. Blood pressure and heart rate changes should be taken into account when making decisions regarding dose titration.
The recommended starting dose of Sibutrex is 2 x 5mg once daily with or without food. If there is inadequate weight loss, the dose may be titrated after four weeks to a total of 15 mg once daily. Doses above 15 mg daily are not recommended. The 5 mg dose should be reserved for patients who do not tolerate the 10 mg dose. Blood pressure and heart rate changes should be taken into account when making decisions regarding dose titration.
Contraindications
Hypersensitivity to sibutramine
Patients receiving monoamine oxidase inhibitors
Patients taking other centrally acting appetite suppressant drugs
Anorexia nervosa
Warnings and precautions
DRUG INTERACTIONS
CNS active drugs: Sibutramine should not be used concomitantly with monoamine oxidase inhibitors (MAOI) and serotonergic drugs (selective serotonin reuptake inhibitors) since rare, but serious, constellation of symptoms termed β€˜serotonin syndrome’ have been reported. At least two weeks should elapse between discontinuation of an MAOI and initiation of treatment with sibutramine. Similarly, at least two weeks should elapse between discontinuation of sibutramine and an MAOI.
CNS active drugs: Sibutramine should not be used concomitantly with monoamine oxidase inhibitors (MAOI) and serotonergic drugs (selective serotonin reuptake inhibitors) since rare, but serious, constellation of symptoms termed β€˜serotonin syndrome’ have been reported. At least two weeks should elapse between discontinuation of an MAOI and initiation of treatment with sibutramine. Similarly, at least two weeks should elapse between discontinuation of sibutramine and an MAOI.
Drugs that may raise blood pressure and/or heart rate: Concomitant use of sibutramine and other agents that may raise blood pressure or heart rate (e.g. certain decongestants, cough, cold and allergy medications that contain agents such as phenylpropanolamine, ephedrine or pseudoephedrine) have not been evaluated. Caution should be used when prescribing sibutramine to patients who use these medications.
Drugs that inhibit cytochrome P450 (3A4) metabolism: In vitro studies have shown that ketoconazole, erythromycin and cimetidine inhibit the cytochrome P450 (3A4) mediated metabolism of sibutramine but the magnitude of such an interaction appears to be small and not of clinical significance.
Alcohol: The concomitant use of sibutramine and excess alcohol is not recommended.
BLOOD PRESSURE AND PULSE
Sibutramine substantially increases blood pressure in some patients. Hence regular monitoring of blood pressure is required when prescribing sibutramine. For patients who experience a sustained increase in blood pressure or pulse rate while receiving sibutramine, either dose reduction or discontinuation should be considered. Sibutramine should be given with caution to those patients with a history of hypertension and should not be given to patients with uncontrolled or poorly controlled hypertension.
Sibutramine substantially increases blood pressure in some patients. Hence regular monitoring of blood pressure is required when prescribing sibutramine. For patients who experience a sustained increase in blood pressure or pulse rate while receiving sibutramine, either dose reduction or discontinuation should be considered. Sibutramine should be given with caution to those patients with a history of hypertension and should not be given to patients with uncontrolled or poorly controlled hypertension.
CONCOMITANT CARDIOVASCULAR DISEASE
Treatment with sibutramine has been associated with increases in heart rate and/or blood pressure. Therefore, sibutramine should not be used in patients with a history of coronary artery disease, congestive heart failure, arrhythmias or stroke.
Treatment with sibutramine has been associated with increases in heart rate and/or blood pressure. Therefore, sibutramine should not be used in patients with a history of coronary artery disease, congestive heart failure, arrhythmias or stroke.
GLAUCOMA
Because sibutramine can cause mydriasis, it should be used with caution in patients with narrow angle glaucoma.
Because sibutramine can cause mydriasis, it should be used with caution in patients with narrow angle glaucoma.
PULMONARY HYPERTENSION
Certain centrally-acting weight loss agents that cause release of serotonin from nerve terminals have been associated with pulmonary hypertension (PPH), a rare but lethal disease. In pre-marketing clinical studies, no cases of PPH have been reported with sibutramine. Because of the low incidence of this disease in the underlying population, however, it is not known whether or not sibutramine may cause this disease.
Certain centrally-acting weight loss agents that cause release of serotonin from nerve terminals have been associated with pulmonary hypertension (PPH), a rare but lethal disease. In pre-marketing clinical studies, no cases of PPH have been reported with sibutramine. Because of the low incidence of this disease in the underlying population, however, it is not known whether or not sibutramine may cause this disease.
SEIZURES
During premarketing testing, seizures were reported in Packs of 30 x 5mg Sibutramine 5mg.
During premarketing testing, seizures were reported in Packs of 30 x 5mg Sibutramine 5mg.
Too Fat? Pop a Pill
Article by Women'€™s Fitness
Your dietician is lying if she tells you that there is no magic pill to knock off a few kilos. There is. In fact, there are a variety of them. Walk into any chemist shop and ask for allopathic anti-obesity pills. Chances are, you will be dazed by the assortment and the accompanying guarantees.
Roughly, these pills can be categorized into two groups-ones that suppress hunger, and other that reduce fat absorption. The first chemical name sibutramine €“ sold under brand names Obestat, Sibutrex, Sibutrim and Slenfig-work by interfering with chemical messages in the central nervous system so as to produce a feeling of fullness. The other pills, available under the brand name Xenical (chemical name orlisatat), decrease absorption of fat by about 30 per cent. While sibutramine pills are freely available in India, Xenical can be bought on the Internet or at select chemist shops, under the counter.
Though technically, sibutramine and orlistat pills are meant for obese people, in reality, teenagers and others who are slightly overweight are popping these pills to avoid getting on to the stepper for a few minutes.
Manufacturers admit that though these are prescription drugs, their unregulated, self-referring market is expanding rapidly. Already, India's monthly consumption of anti-obesity pills is worth Rs. 1.1 crore.
But can a pill really make you lose your appetite and turn your body into a calorie-burning machine? Well, opinion is divided.
Dr. R.K.Suri, A Delhi-based diabetologist says, "Though these drugs are made for people with obesity-related diseases, most can't take them because their side effects far outweigh the risk of being mildly overweight." About 40 to 50 per cent of his patients, who were prescribed sibutramine, complained of high blood pressure.
Dr. Rakesh Gupta, a senior consultant with Apollo Hospital, who has been prescribing sibutramine pills for over a year-and-a-half, however, finds them very effective. "When taken along with a controlled diet and regular exercise, they help in reducing 8 to 10 per cent body weight in six months. And frankly, I have not seen any side effects," he said.
"Sibutramine acts on the brain's satiety centres and kills hunger. As, for some, feeling satisfied with less food is a major barrier to weight loss, medication is necessary to control their appetite." Dr. Gupta said.
But if you are tempted to knock off a few kilos by popping these pills, be warned. Sibutramine pills have a long list of side effects, the most common being insomnia. "People who take sibutramine often return to buy sleeping pills," a chemist said. More serious, though, are depression, visual disorders and impotence. Slimming pills have also been known to lead to addiction, blood disorders, psychosis and even death.
The Duchess of York is one of the most famous victims of slimming pills. The pills fogged Fergie`s brain and she became "hysterical" and had to be weaned off the pills.
Dr. Manish Chawla, who works at Cipla and is happy that their Obestat (Sibutrex) is doing "great business" said, "These medicines have been tested internationally. All drugs have side effects and so do these. But compared to the benefits, the side effects are negligible." Obestat, he says, can be taken once daily for up to two years, and helps in shedding 5-10 per cent body weight.
Dr. Sanghi, who runs Delhi's Pulse Impulse health clinic, however, rejects the sales pitch. "If these pills are so wonderful, why do drug companies restrict their use to two years?" Because, she explains, long term use of these pills will result in complications similar to those of starving and anemia: Vitamin deficiency that may affect eyes, hair, skin, and other body parts.
Dr. Makhija, a well-known Delhi dietician says," These drugs help initially-by motivating you and reducing your food intake. But you have to get off them soon. You have to learn to manage your food and not fool your brain into thinking that you have eaten.
The bottom line is; these pills are handy in curing obesity-caused by a sedentary lifestyle, abundance of high-calorie foods and ever-expanding portion sizes – when taken under supervision, along with controlled diet and exercise. They get the initial push and motivation with these pills," Dr. Sangh said. But remember, these will only suppress your appetite. Not greed.
DO THEY WORK?
Sibutramine: If we have chocolate or milk at night, serotonin is released in our body, giving us a sense of satisfaction. Sibutramine (brand names, Obestat, Sibutrex, Sibutrim, Slenfig) releases serotonin without our eating anything.
Side effects: Can cause headache, dry mouth, anorexia, insomnia, constipation, convulsions, increased blood pressure, dizziness, anxiety, depression.
Below are some of the details of Sibutrex 15
Sibutramine, usually available as sibutramine hydrochloride monohydrate, is an orally administered agent for the treatment of obesity, as an appetite suppressant. It is a centrally-acting serotonin-norepinephrine reuptake inhibitor structurally related to amphetamines, although its mechanism of action is distinct. Sibutramine is manufactured by Abbott Laboratories, under brand names such as Reductil, Meridia and Sibutrex.
P - Contraindicated in pregnancy
L - Contraindicated in lactation
L - Contraindicated in lactation
Page Contents
Pharmacodynamics
Sibutramine is a neurotransmitter reuptake inhibitor that reduces the reuptake of serotonin (by 53%), norepinephrine (by 54%), and dopamine (by 16%), thereby increasing the levels of these substances in synaptic clefts and helping enhance satiety; the serotonergic action, in particular, is thought to influence appetite. Older anorectic agents such as amphetamine and fenfluramine force the release of these neurotransmitters rather than affecting their reuptake. Despite having a mechanism of action similar to tricyclic antidepressants, sibutramine has failed to demonstrate antidepressant properties in animal studies.
Pharmacokinetics
Sibutramine acts by inhibiting the reuptake of norepinephrine and serotonin, and to a lesser extent, dopamine.
Absorption
Well absorbed from the GI tract (oral).
Distribution
Protein-binding: 97%
Metabolism
Extensive first-pass metabolism by CYP3A4. .
Excretion
Mainly in urine (as inactive metabolites). Plasma elimination half-life: About 14-16 hours.
Absorption
Well absorbed from the GI tract (oral).
Distribution
Protein-binding: 97%
Metabolism
Extensive first-pass metabolism by CYP3A4. .
Excretion
Mainly in urine (as inactive metabolites). Plasma elimination half-life: About 14-16 hours.
Clinical Efficacy
Information Not Available
Adverse Reactions
Dry mouth, drowsiness, dizziness, rhinitis, depression, emotional lability, migraine, skin rash, mydriasis, insomnia, constipation, diarrhoea, peripheral oedema, menstrual disorders.
Precautions
Overdosage
Symptoms include: Tachycardia, hypertension, headache and dizziness. Treatment is supportive and symptomatic. Ξ²-blockers may be used to control elevated BP and tachycardia.
Symptoms include: Tachycardia, hypertension, headache and dizziness. Treatment is supportive and symptomatic. Ξ²-blockers may be used to control elevated BP and tachycardia.
Special Precautions
Hypertension; narrow-angle glaucoma; seizures; history of gallstones; family history of motor or verbal tics. Should not drive or operate machinery. Mild-moderate renal impairment. History of depression. History of hypertension, coronary artery disease, congestive heart failure, arrhythmias or stroke. Monitor BP and heart rate.
Other Drug Interactions
Avoid concurrent admin with or within 2 wk of stopping MAOIs. Care should be taken with drugs that may raise BP or heart rate e.g. phenylpropanolamine, ephedrine or pseudoephedrine. Increased serum levels when used with drugs that inhibit CYP3A4 e.g. ketoconazole and erythromycin. Decreased serum levels when used with rifampicin, phenytoin, carbamazepine and phenobarbital. Increased risk of serotonin syndrome when used with serotonergics such as SSRIs, sumatriptan, lithium and pethidine.
Other Interactions
Information Not Available
Dosage
Oral
Obesity
Adult: Initially, 10 mg daily in the morning. Re-evaluate treatment in patients whose weight loss is <2 kg in the 1st 4 weeks of treatment. May increase dose to 15 mg daily. Reassess 4 weeks later. Discontinue treatment if weight loss is still <2 kg. Max: 15 mg daily.
Obesity
Adult: Initially, 10 mg daily in the morning. Re-evaluate treatment in patients whose weight loss is <2 kg in the 1st 4 weeks of treatment. May increase dose to 15 mg daily. Reassess 4 weeks later. Discontinue treatment if weight loss is still <2 kg. Max: 15 mg daily.
Food (before/after)
May be taken with or without food.
List of Contraindications
Sibutramine and Pregnancy
Contraindicated in pregnancy
Sibutramine and Lactation
Contraindicated in lactation
Sibutramine and Children
Safety and efficacy in children younger than 16 years of age not established.
Sibutramine and Geriatic
Use with caution in patients older than 65 years of age.
Sibutramine and Other Contraindications
History of cerebrovascular disease or CV disorder; uncontrolled or poorly controlled hypertension; history of eating disorders (e.g. anorexia nervosa and bulimia nervosa); bipolar disorder, Tourette's syndrome, hyperthyroidism, phaeochromocytoma, benign prostatic hyperplasia; history of drug or alcohol abuse. Pregnancy, lactation. Severe renal or hepatic impairment.
Storage
Oral
Store at 15-30Β°C
Store at 15-30Β°C
Lab interference
Information Not Available
Source: http://www.drugsupdate.com/
