Sibutramine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe (d)

Austria: Reductil, Sibutramin; Bulgaria: Reductil, Lindaxa; Czech Republic: Lindaxa, Meridia, Sibutramin; Denmark: Reductil; Estonia: Lindaxa, Reductil, Sibutramine, Sibutril; Finland: Reductil; France: Sibutral; Germany: Reductil, Reduxade, Sibutramin, Zelium; Greece: Reductil, Sibutramine; Hungary: Lindaxa, Minimectil, Reductil; Ireland: Reductil, Sibutramine, Sitrane; Italy: Ectiva, Reductil; Latvia: Reductil, Sibutril; Lithuania: Lindaxa, Reductil, Sibutramine, Sibutril; Luxembourg: Reductil; Malta: Reductil; Netherlands: Reductil, Sibutramine; Poland: Afibron, Lindaxa, Meridia, Obesan, Sibutramine, Zelixa; Portugal: Reductil, Sibutramina, Zelium; Romania: Lindaxa, Minimacin, Reductil, Sibutramina, Siluton; Slovakia: Lindaxa, Reductil, Sibutramin; Slovenia: Reductil, Sibutramin; Sweden: Reductil, Sibutramin, Sibutramine; UK: Reductil.

North America (d)

Canada: Meridia, Sibutramine; USA: Meridia.

Latin America (d)

Argentina: Aderan, Downtrat, Fagolip, Ipomex, Restrical, Sacietyl, Sertinal, Sibu-Estirol, Sibutramina; Brazil: Plenty, Reductil, Sibutramina, Vazi; Mexico: Adelseril, Adelvag, Ectiva, Gea, Ifa-Certez, Raductil, Randism, Serotramin, Siruton, Tramentel.

Drug combinations

Chemistry

Sibutramine Hydrochloride: C~17~H~26~ClN HCl H~2~O. Mw: 334.32. (1) Cyclobutanemethanamine, 1-(4-chlorophenyl)-N,N-dimethyl-α-(2-methylpropyl)-, hydrochloride, monohydrate, (±)-; (2)(±)-1-(p-Chlorophenyl)-α-isobutyl-N,N-dimethylcyclobutanemethylamine hydrochloride monohydrate. CAS-125494-59-9 (monohydrate); CAS-84485-00-7 (anhydrous); CAS-106650-56-0 (sibutramine)(1990).

Pharmacologic Category

Anorexigenic Agents and Respiratory and Cerebral Stimulants, Miscellaneous. (ATC-Code: A08AA10).

Mechanism of action

Anorectic effects principally due to active metabolites (M~1~ and M~2~) which inhibit reuptake (but not release) of serotonin, norepinephrine, and, to a lesser extent, dopamine at neuronal synapse, thus promoting sense of satiety. No monoamine-releasing (or depleting) activity. Increases energy expenditure through thermogenic effects in animals (not confirmed in humans).

Therapeutic use

Obesity.

Pregnancy and lactiation implications

Teratogenic effects not observed in animals except at doses also causing maternal toxicity. There are no adequate studies in pregnant women. Use in pregnancy not recommended. Excretion in breast milk unknown (not recommended in nursing women).

Unlabeled use

Contraindications

In 2010 EMEA and FDA recommended against the continued use of sibutramine or sibutramine-containing medicines due to unnecessary cardiovascular risks to patients. Hypersensitivity to sibutramine or any component of the formulation. During or within 2 weeks of MAOIs or concomitant centrally-acting appetite suppressants. Anorexia nervosa, bulimia nervosa. Poorly-controlled or uncontrolled hypertension, coronary artery disease, congestive heart failure, arrhythmia. Stroke.

Warnings and precautions

May impair ability to engage in potentially hazardous activities. May cause increase in blood pressure (should not be used in coronary artery disease, heart failure, arrhythmia, or stroke). May cause increased heart rate (should not be used in coronary artery disease, congestive heart failure, arrhythmia, or stroke). Use of some anorexigens associated with development of valvular heart disease (avoid stimulants in known serious structural cardiac abnormalities, cardiomyopathy, serious heart rhythm abnormalities, or other serious cardiac problems which could increase risk of sudden death that these conditions alone carry). Use with caution in bleeding disorders, in diabetes mellitus (antidiabetic agent requirements may be altered with anorexigens and concomitant dietary restrictions), in history of gallstones (weight loss may precipitate or exacerbate gallstone formation), in narrow-angle glaucoma (risk of mydriasis), and in mild-moderate hepatic or renal impairment (avoid use in severe impairment). Use with caution in history of psychiatric symptoms (rare reports of depression, suicide and suicidal ideation documented in patients on sibutramine), in history of seizure disorder (seizures reported), and in Tourette’s syndrome (stimulants may unmask tics). Risk for development of serotonin syndrome if used with other serotonergic agents.

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