Endocrinology Book



Aka: Orlistat, Xenical
  1. See Also
    1. Medications Associated with Weight Gain
    2. Lorcaserin (Belviq)
    3. Phentermine (Ionamin, Fastin)
    4. Phentermine and Topiramate (Qsymia, Qnexa)
    5. Obesity
    6. Obesity in Children
    7. Obesity Evaluation
    8. Obesity Measurement (or Obesity Screening)
    9. Obesity Risk (or Obesity Comorbid Conditions)
    10. Obesity Management
    11. Obesity Medication
    12. Dietary Supplements in Obesity
    13. Exercise in Obesity
    14. Obesity Resources
  2. Indication: Obesity Management
    1. Body Mass Index over 30 kg/m2
    2. Body Mass Index over 27 kg/m2 with comorbidity
      1. Diabetes Mellitus
      2. Hypertension
      3. Dyslipidemia
  3. Mechanism
    1. Pentanoic acid ester binds gastric, pancreatic Lipase
    2. Lipase Inhibitor (Blocks Fat absorption)
      1. Decreased Triglyceride absorption
      2. Decreased Cholesterol absorption
  4. Pharmacokinetics
    1. Minimal systemic absorption
  5. Efficacy
    1. Weight loss is greater with 120 mg (7.5 lb or 3.4 kg) than with 60 mg (5.5 lb or 2.5 kg)
    2. Combined results of two large Placebo controlled trials
      1. Year one
        1. Orlistat: 9-10 kg loss (10% of baseline weight)
        2. Placebo: 6 kg (6% of baseline weight)
      2. Year two
        1. Orlistat: 1.5-3 kg regained weight
        2. Placebo: 4-6 kg regained weight
    3. References
      1. Sjostrom (1998) Lancet 352:167 [PubMed]
      2. Davidson (1999) JAMA 281:235 [PubMed]
  6. Adverse effects
    1. Gastrointestinal side effects (40%)
      1. Flatus with discharge
      2. Oily stool with spotting
      3. Fecal urgency
      4. Fecal Incontinence
      5. Abdominal Pain
    2. Fat soluble Carotenoid (fruit, vegetable) malabsorption
    3. Fat soluble Vitamin malabsorption (daily MVI recommended in package insert)
      1. Vitamin A
      2. Vitamin D
      3. Vitamin E
      4. Vitamin K
  7. Drug Interactions
    1. Does not interfere with absorption of other medications
      1. Coumadin
      2. Oral Contraceptives
      3. Antihypertensives
  8. Dosing
    1. Take three times daily with each meal containing fat
    2. Prescription dose: 120 mg orally three times daily
    3. OTC dose: 60 mg orally three time daily
  9. Precautions
    1. Avoid fat-soluble Vitamins within 2 hours of Orlistat
    2. Maintain Dietary Fat intake <30% of calories
  10. References
    1. (1999) Med Lett Drugs Ther 41(1055):55-6 [PubMed]
    2. Erlandson (2016) Am Fam Physician 94(5): 361-8 [PubMed]
Medication Costs
xenical (on 2/22/2017 at Medicaid.Gov Pharmacy Drug pricing)
XENICAL 120 MG CAPSULE $6.18 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

orlistat (C0076275)

Definition (NCI) A reversible active-site inhibitor of gastrointestinal lipases. Orlistat forms a covalent bond with the active serine site in gastric and pancreatic lipases, thereby inhibiting their activity and preventing dietary fat from being hydrolyzed and absorbed. (NCI04)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C055122
SnomedCT 116093009, 387007000
English 1-((3-hexyl-4-oxo-2-oxetanyl)methyl)dodecyl-2-formamido-4-methylvalerate, L-Leucine, N-formyl-, 1-((3-hexyl-4-oxo-2-oxetanyl)methyl)dodecyl ester, (2S-(2alpha(R*),3beta))-, tetrahydrolipstatin, THLP, orlistat, orlistat (medication), ORLISTAT, orlistat [Chemical/Ingredient], tetrahydrolipastatin, Orlistat, Orlistat (product), Orlistat (substance)
Spanish orlistat (producto), orlistat (sustancia), orlistat
Derived from the NIH UMLS (Unified Medical Language System)

Xenical (C0732649)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C055122
English xenical, Hoffmann-La Roche brand of orlistat, Roche brand of orlistat, Xenical
Derived from the NIH UMLS (Unified Medical Language System)

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