Sibutramine


Concise Prescribing Info
Indications/Uses
Obesity.
Dosage/Direction for Use
Adult : PO Initial: 10 mg once daily, may increase to 15 mg once daily after 4 wk. Max: 15 mg/day.
Dosage Details
Oral
Obesity
Adult: Patients w/ BMI ≥30 kg/m2 or ≥27 kg/m2 in the presence of other risk factors: Initially, 10 mg once daily, may increase to 15 mg once daily after 4 wk; 5 mg dose may be given to patients who cannot tolerate the 10 mg dose. Max: 15 mg daily.
Elderly: >65 yr Contraindicated.
Renal Impairment
Severe: Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Administration
May be taken with or without food.
Contraindications
Major eating disorder (anorexia nervosa or bulimia nervosa), inadequately controlled HTN (>145/90 mmHg). History of coronary artery disease, CHF, arrhythmias, stroke. Patients >65 yr of age. Severe renal or hepatic impairment. Lactation. Concomitant use w/ MAOIs and other centrally acting wt loss drugs.
Special Precautions
Patient w/ narrow angle glaucoma, seizure disorder and those at risk of bleeding events. Mild to moderate renal or hepatic impairment. Pregnancy.
Adverse Reactions
Dry mouth, anorexia, insomnia, constipation, headache, back pain, flu syndrome, injury accident, asthenia; abdominal, chest and neck pain; allergic reaction, migraine, palpitation, nausea, dyspepsia, gastritis, vomiting, rectal disorder, thirst, generalised oedema, arthralgia, myalgia, tenosynovitis, joint disorder, dizziness, nervousness, anxiety, depression, paraesthesia, somnolence, CNS stimulation, emotional lability, rhinitis, pharyngitis, sinusitis, increased cough, laryngitis, rash, sweating, herpes simplex, acne, taste perversion, ear disorder and pain, dysmenorrhoea, UTI, vag monilia, metrorrhagia.
Potentially Fatal: Serious CV and cerebrovascular events (e.g. vasodilation, cardiac arrhythmias, HTN, MI, stroke).
Patient Counseling Information
May impair judgment, thinking or motor skills.
MonitoringParameters
Regularly monitor BP and pulse rate.
Overdosage
Symptoms: Tachycardia, HTN, headache, dizziness. Management: Symptomatic and supportive treatment. Establish a patent airway. β-blockers may be considered to control HTN or tachycardia, but caution is advised.
Drug Interactions
Increased plasma concentration w/ CYP3A4 inhibitors (e.g. ketoconazole, erythromycin).
Potentially Fatal: Risk of serotonin syndrome w/ MAOIs (e.g. phenelzine, selegiline). Increased risk of cardiac valve dysfunction w/ other centrally-acting wt loss agents.
Action
Description: Sibutramine inhibits the reuptake of norepinephrine and serotonin, and to a lesser extent, dopamine.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Time to peak plasma concentration: W/in 3-4 hr.
Distribution: Rapidly and extensively distributed into body tissues. Plasma protein binding: 97%.
Metabolism: Undergoes hepatic metabolism principally by CYP3A4 isoenzyme to desmethyl metabolites, M1 and M2, further metabolised via hydroxylation and conjugation to inactive metabolites.
Excretion: Mainly via urine (77%, as inactive metabolites). Elimination half-life: 14 hr (M1); 16 hr (M2).
Chemical Structure

Chemical Structure Image
Sibutramine

Source: National Center for Biotechnology Information. PubChem Database. Sibutramine, CID=5210, https://pubchem.ncbi.nlm.nih.gov/compound/Sibutramine (accessed on Jan. 23, 2020)

Storage
Store at 25°C.
MIMS Class
ATC Classification
A08AA10 - sibutramine ; Belongs to the class of centrally acting antiobesity products. Used in the treatment of obesity.
References
Buckingham R (ed). Sibutramine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 19/10/2015.

Meridia Capsule. U.S. FDA. https://www.fda.gov/. Accessed 19/10/2015.

Meridia Capsules (Abbott Laboratories, USA). U.S. FDA. https://www.fda.gov/. Accessed 19/10/2015.

Disclaimer: This information is independently developed by MIMS based on Sibutramine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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