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Sibutramine information from DrugsUpdate  

1
See Available Brands of Sibutramine in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation

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.

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 inhibitng 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.

Sibutramine Indications / Sibutramine Uses

Information Not Available

Sibutramine Adverse Reactions / Sibutramine Side Effects

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. β-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.

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 15-30°C

Lab interference

Oral
Store at 15-30°C

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