Obestat
Obestat Uses, Dosage, Side Effects, Food Interaction and all others data.
Obestat produces its therapeutic effect by norepinephrine, serotonin and dopamine reuptake inhibition. Obestat exerts its pharmacological actions predominantly via its secondary (M1) and primary (M2) amine metabolites. The parent compound Obestat is a potent inhibitor of serotonin and norepinephrine reuptake in vivo. However metabolites M1 and M2 inhibit the reuptake of these neurotransmitters both in vivo and in vitro.
Obestat is an orally administered agent for the treatment of obesity. Obestat exerts its pharmacological actions predominantly via its secondary (M1) and primary (M2) amine metabolites. The parent compound, sibutramine, is a potent inhibitor of serotonin and norepinephrine reuptake in vivo, but not in vitro. However, metabolites M1 and M2 inhibit the reuptake of these neurotransmitters both in vitro and in vivo. In human brain tissue, M1 and M2 also inhibit dopamine reuptake in vitro, but with ~3-fold lower potency than for the reuptake inhibition of serotonin or norepinephrine. Obestat, M1 and M2 exhibit no evidence of anticholinergic or antihistaminergic actions. In addition, receptor binding profiles show that sibutramine, M1 and M2 have low affinity for serotonin (5-HT1, 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C), norepinephrine (b, b1, b3, a1 and a2), dopamine (D1 and D2), benzodiazepine, and glutamate (NMDA) receptors. These compounds also lack monoamine oxidase inhibitory activity in vitro and in vivo.
Trade Name | Obestat |
Availability | Discontinued |
Generic | Sibutramine |
Sibutramine Other Names | Sibutramina, Sibutramine, Sibutraminum |
Related Drugs | phentermine, semaglutide, Wegovy, Saxenda, liraglutide, Alli |
Weight | 120mg |
Type | Capsule |
Formula | C17H26ClN |
Weight | Average: 279.848 Monoisotopic: 279.175377544 |
Protein binding | 97% (to human plasma proteins) |
Groups | Approved, Illicit, Investigational, Withdrawn |
Therapeutic Class | Appetite suppressant drugs/Anti-obesity drugs |
Manufacturer | Cipla Limited, Panacea Pharmaceuticals |
Available Country | India, Pakistan |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Obestat is used in the management of obesity, including weight loss and management of weight loss. It should be used in conjunction with a reduced caloric diet. Obestat is recommended for obese patients with an initial body mass index (BMI) ≥30 kg/m2 or ≥27 kg/m2 in the presence of other risk factors (e.g., hypertension, diabetes, dyslipidemia)
Obestat is also used to associated treatment for these conditions: BMI >30 kg/m2
How Obestat works
Obestat produces its therapeutic effects by inhibition of norepinephrine (NE), serotonin (5-hydroxytryptamine, 5-HT), and to a lesser extent, dopamine reuptake at the neuronal synapse. By inhibiting the reuptake of these neurotransmitters, sibutramine promotes a sense of satiety and decrease in appetite, thereby reducing food intake. Data from animal studies also suggest that sibutramine may also increase energy expenditure through thermogenic effects in both the basal and fed states, but this has not been confirmed in humans. Obestat and its major pharmacologically active metabolites (M1 and M2) do not act via release of monoamines.
Dosage
Obestat dosage
The recommended starting dose is 10 mg administered once daily with or without food. If there is inadequate weight loss, the dose may be titrated after 4 weeks to a total of 15 mg once daily. 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. Analysis of numerous variables has indicated that ≈ 60% of patients who lose at least 4 lbs in the first 4 weeks of treatment with a given dose of Obestat in combination with a reduced-calorie diet lose at least 5% (placebo-subtracted) of their initial body weight by the end of 6 months to 1 year of treatment on that dose. Conversely, ≈ 80% of patients who do not lose at least 4 lbs in the first 4 weeks of treatment with a given dose do not lose at least 5% (placebo-subtracted) of their initial body weight by the end of 6 months to 1 year of treatment on that dose. If a patient has not lost at least 4 lbs in the first 4 weeks of treatment, consider reevaluation of therapy which may include increasing the dose or discontinuing Obestat. The safety and efficacy of Obestat have not been determined beyond 1 year at this time.
Side Effects
Commonly reported side-effects of Obestat are dry mouth, headache, insomnia and constipation; diarrhoea, dizziness, drowsiness and rhinitis have also occurred. Less frequently reported side-effects include dysmenorrhoea, oedema, influenza-like symptoms, and depression. Abnormal bleeding, acute interstitial nephritis, emotional lability, migraine, seizures and skin rashes have been reported rarely. Clinically significant increases in heart rate and blood pressure may occur. Obestat may decrease salivary flow and therefore increase the risk of dental caries, periodontal disease, or other oral disorders. It may also produce mydriasis. Increases in liver enzyme have been reported.
Toxicity
Side effects include dry mouth, anorexia, insomnia, constipation and headache.
Precaution
Use caution when prescribing Obestat with other agents that may raise blood pressure or heart rate including certain decongestant, cough, cold and allergy medications that contain agents such as phenylpropanolamine, ephedrine or pseudoephedrine.
Interaction
Obestat should not be given concurrently with, or within at least two weeks of stopping an MAOI; at least two weeks should elapse between discontinuation of Obestat and starting therapy with an MAOI. There is a risk of the serotonin syndrome developing if Obestat is administered together with other serotonergic drug such as selective serotonin reuptake inhibitors (SSRIs), sumatriptan, lithium, pethidine, fentanyl, dextromethorphan and pentazocine. Obestat should not be used with other drugs that may increase heart rate or blood pressure such as ephedrine, phenylpropanolamine, and pseudoephedrine (which may be ingredients of some cough and cold remedies). Alcohol should be avoided. Inhibitors of the cytochrome P450 isoenzyme CYP3A4, such as ketoconazole and erythromycin, may increase plasma concentrations of Obestat.
Food Interaction
[Moderate] GENERALLY AVOID: Alcohol may potentiate the central nervous system and cardiovascular effects of centrally-acting appetite suppressants.
In one study, concurrent administration of methamphetamine (30 mg intravenously) and ethanol (1 gm This increases cardiac work and myocardial oxygen consumption, which may lead to more adverse cardiovascular effects than either agent alone. Subjective effects of ethanol were diminished in the eight study subjects, but those of methamphetamine were not affected. The pharmacokinetics of methamphetamine were also unaffected except for a decrease in the apparent volume of distribution at steady state. Patients should be counselled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
MANAGEMENT: Concomitant use of centrally-acting appetite suppressants and alcohol should be avoided if possible, especially in patients with a history of cardiovascular disease.
Obestat Drug Interaction
Major: escitalopram, fluoxetine, bupropionModerate: aspirin, contained in alcoholic beverages , zolpidem, lorazepam, pregabalin, quetiapine, alprazolam, cetirizineUnknown: amoxicillin, sulfamethoxazole / trimethoprim, celecoxib, acetaminophen, methylphenidate, levothyroxine, sildenafil, ascorbic acid, orlistat
Obestat Disease Interaction
Major: anorexia nervosa, cardiovascular, glaucoma, renal/liver diseaseModerate: diabetics, seizures, substance abuse
Elimination Route
Rapid absorption following oral administration. Absolute bioavailability is not known, but at least 77% of a single oral dose of sibutramine is absorbed.
Half Life
1.1 hours
Clearance
- Oral cl=1750 L/h [oral administration]
Elimination Route
Obestat is metabolized in the liver principally by the cytochrome P450 (3A4) isoenzyme, to desmethyl metabolites, M1 and M2. These active metabolites are further metabolized by hydroxylation and conjugation to pharmacologically inactive metabolites, M5 and M6. Approximately 85% (range 68-95%) of a single orally administered radiolabeled dose was excreted in urine and feces over a 15-day collection period with the majority of the dose (77%) excreted in the urine. The primary route of excretion for M1 and M2 is hepatic metabolism and for M5 and M6 is renal excretion.
Pregnancy & Breastfeeding use
The use of Obestat is not recommended during pregnancy. Women of child-bearing potential should use adequate contraception while taking this drug. Patients should be advised to notify their physician if they become pregnant or intend to become pregnant during therapy. It is not known whether Obestat or its active metabolites are excreted in breast milk. It is not recommended for use in nursing mothers. Patients should be advised to notify their physician if they are breast-feeding.
Contraindication
Patients receiving monoamine oxidase inhibitors (MAOIs), hypersensitivity to Obestat or any of the active ingredients of Obestat; patients with anorexia nervosa, patients taking other centrally acting appetite-suppressant drugs. Give with caution to those patients with a history of hypertension and do not give to patients with uncontrolled or poorly controlled hypertension.
Storage Condition
Should be protected from light. Store in a dry place and between 15˚ to 30˚C temperature.
Innovators Monograph
You find simplified version here Obestat
Obestat contains Sibutramine see full prescribing information from innovator Obestat Monograph, Obestat MSDS, Obestat FDA label
FAQ
What is Obestat used for?
Obestat is used together with diet and exercise to treat obesity that may be related to diabetes, high cholesterol, or high blood pressure.Obestat may also be used for other purposes not listed in this medication guide.
How safe is Obestat?
Obestat is safe, well tolerated, and produces statistically and clinically significant body weight loss in obese patients whose hypertension is well controlled with an ACE inhibitor.
What are the common side effects of Obestat?
The common side effects of Obestat are include:
- A Stuffy And Runny Nose
- Dry Mouth
- Constipation
- Dizziness
- Difficulty Sleeping
- Decreased Appetite
- Headache
- Nervousness
- Irritability
- Anxious Feelings
How does Obestat work in the body?
Obestat blocks the reuptake of the neurotransmitters dopamine, norepinephrine, and serotonin.
Is Obestat safe during pregnancy?
The use of Obestat is considered contraindicated during pregnancy. It is recommended that women of child bearing potential use adequate contraception while on Obestat therapy. Patients should be advised to notify their physician if they become pregnant or intend to become pregnant during therapy.
Is Obestat safe during breastfeeding?
Obestat is considered contraindicated during breast-feeding by the manufacturer. Patients should be advised to notify their physician if they are breast-feeding.
Can I drink alcohol with Obestat?
Using Obestat with alcohol can increase the risk of cardiovascular side effects such as increased heart rate, chest pain, or blood pressure changes.
How long does Obestat stay in my system?
Obestat is metabolized stay in your system half-lives of 14 and 16 hours, respectively.
Does Obestat give mecenergy?
it reduces energy intake by increasing satiety and it increases energy expenditure.
Does sibutramine get me high?
Obestat has no abuse potential since it does not enhance dopamine release at the synapse.
Does Obestat affect fertility?
Obestat is associated with decreases in sperm transit time, quantity and quality, leading to reduced fertility.
Is Obestat a stimulant?
It is a centrally acting stimulant chemically.
Can Obestat cause heart problems?
Obestat is one such agent and potentially causes cardiac arrest even in subjects without pre-existing cardiovascular disease, particularly when combined with drugs that lead to QT prolongation.
Is Obestat an antidepressant?
Obestat was initially developed as an antidepressant.
Can I take Obestat long time?
Obestat should not be taken for longer than 2 years.
When is the best time to take Obestat?
Obestat is taken once daily, generally in the morning.
What happens if I miss a dose of Obestat?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
What happens if I overdose of Obestat?
Seek emergency medical attention.
Overdose symptoms may include headache, dizziness, and fast heart rate.