| SIBUTRAMINE HYDROCHLORIDE MONOHYDRATE
Classifications: cns stimulant, anorexiant; Therapeutic:appetite suppressant
Pregnancy Category: C
Controlled Substance: Schedule IV
5 mg, 10 mg, 15 mg capsules
Inhibits central reuptake of serotonin (5-HT3), monoamine reuptake, as well as norepinephrine and dopamine reuptake, by blocking their receptors.
Appetite suppression by enhancing satiety and raising the metabolic rate. Indicated by a loss of at least 4 lb during the
first 4 wk of therapy.
Management of obesity, including weight loss and maintenance of weight loss, in patients with BMI of at least 30 kg/m2 or BMI of at least 27 kg/m2 and other risk factors (hypertension, diabetes, dyslipidemia).
Major eating disorders; anorexia nervosa, bulimia; arrhythmias; concurrent administration with other serotonin reuptake
inhibitors (e.g., fluoxetine), MAOIs, lithium, tryptophan; severe hepatic or renal impairment; ESRD, dialysis; CHF, stroke, CAD; uncontrolled or poorly controlled
hypertension; seizures; pregnancy (category C), lactation.
History of hypertension; older adults; narrow-angle glaucoma; mild or moderate hepatic disease; renal impairment. Safety
and efficacy in patients <16 y are not established.
Route & Dosage
Adult: PO 10 mg once daily, preferably in morning, may be increased to 15 mg if inadequate weight loss (<4 lb) in 4 wk
- Note: Doses above 15 mg/d are not recommended.
- Allow at least 2 wk to elapse between discontinuing an MAOI and starting sibutramine.
- Store at 15°30° C (59°86° F) in a tightly closed container; protect from light.
Adverse Effects (≥1%)Body as a Whole:
Back pain, flu-like syndrome, asthenia, arthralgia. CNS: Headache, insomnia
, migraine headache, dizziness, nervousness, anxiety, depression
, paresthesias, seizures (rare). CV:
Increase in BP, tachycardia, vasodilation, palpitations. GI: Dry mouth,
, abdominal pain, increased appetite, nausea, dyspepsia, taste perversion. Respiratory:
Rhinitis, pharyngitis, sinusitis
, cough. Skin:
Rash, sweating. Urogenital:
Interactions Drug: decongestants
, cough and allergy medications
may cause additional increase in BP; maoi
s, ergot derivatives
, sumatriptan, naratriptan, rizatriptan, zolmitriptan, dextromethorphan, meperidine, pentazocine, fentanyl, lithium; ssri
s may predispose to serotonin
syndrome (see Appendix F); ketoconazole, erythromycin
may inhibit metabolism of sibutramine. Herbal: St. John's wort
may cause serotonin
syndrome (headache, dizziness, sweating, agitation).
Rapidly from GI tract. Peak:
1.2 h. Distribution:
97% protein bound; concentrates in liver and kidneys. Metabolism:
In liver by cytochrome P450 3A4 to 2 active metabolites. Elimination:
Primarily in kidneys. Half-Life:
1416 h (active metabolites).
Assessment & Drug Effects
- Monitor weight changes carefully to determine therapeutic effect.
- Lab tests: Periodic liver function, bilirubin, alkaline phosphatases, lipid profile.
- Monitor BR and HR regularly; report sustained increases in BP or HR immediately.
- Monitor for and immediately report S&S of serotonin syndrome (see Appendix F).
- Monitor persons with narrow-angle glaucoma closely for worsening intraocular pressure.
Patient & Family Education
- Notify physician if any of the following develop: Rash, hives, or other S&S of an allergic reaction; signs of hyperstimulation
such as restlessness, shivering, profuse sweating, irritability, and tremor.
- Take in the morning; causes less interference with sleep.
- Check with physician before taking any OTC cough, cold, allergy, or weight-loss drugs.
- Maintain strict adherence to prescribed antihypertensives.
- Inform physician of all drugs being taken. Serious adverse effects may be experienced with concomitant use of some drugs
used to treat depression.