Sibutramine

Severe: Contraindicated.

Severe: Contraindicated.

May be taken with or without food.

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.

Patient w/ narrow angle glaucoma, seizure disorder and those at risk of bleeding events. Mild to moderate renal or hepatic impairment. Pregnancy.

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).

May impair judgment, thinking or motor skills.

Regularly monitor BP and pulse rate.

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.

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.

Description:
Mechanism of Action: 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).

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

Store at 25°C.

Thuốc chống béo phì

A08AA10 - sibutramine ; Belongs to the class of centrally acting antiobesity products. Used in the treatment of obesity.

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.