PHARMACOLOGY OF

OBESITY

Hernita T.,MD
Atas izin: Vivian Soetikno, MD, SpFK
Department of Pharmacology and Therapeutics
POTENTIAL STRATEGIES FOR ANTI-OBESITY
DRUG ACTION

 Reducing food intake. Either amplify effects of signals/factors

that inhibit food intake or block signals/factors that augment food intake
 Blocking nutrient absorption (especially fat or
carbohydrates) in the intestine.
 Increasing thermogenesis. Either increase metabolism and
dissipate food energy as heat or increase energy expenditure through the
enhancement of physical activity.
 Modulating fat metabolism/storage. Regulate fat
synthesis/breakdown by making appropriate adjustments to food intake or
energy expenditure.
 Modulating the central regulation of body
weight. Either alter the internal set point or modulate the signals
presented regarding fat stores.
INDICATIONS FOR USE OF OBESITY DRUGS

•A combined intervention of behavior therapy, dietary

changes and increased physical activity should be
maintained for at least 6 months before considering
pharmacotherapy.
INDICATIONS FOR USE OF OBESITY DRUGS
 BMI of 30 kg/m² or more or a BMI of 27 kg/m² or
more with comorbid condition
 Understand that drug therapy is adjunctive to
lifestyle intervention
 Have realistic expectations about weight loss goals
and outcomes
 Demonstrate readiness for change
 Are unable to lose/maintain weight with lifestyle
change alone
 Comply with medication use
 Have no medical or psychiatric contraindications
 ADDITIONAL CONSIDERATIONS WHEN USING
ANTI-OBESITY DRUGS

•Weight loss drugs should never be used without continued

concomitant lifestyle modifications and as part of a
comprehensive weight loss program.
•Continual assessment of drug therapy for efficacy and safety is
necessary.
•If the drug is efficacious in helping the patient to lose and/or
maintain weight loss and there are no serious adverse effects, it
can be continued.
•If not, it should be discontinued.
CONTRAINDICATIONS OR CAUTIONS TO THE USE OF
OBESITY DRUGS
 Pregnancy or lactation
 Unstable cardiac disease
 Uncontrolled hypertension (SBP >180, DBP > 110 mmHg)
 Unstable severe systemic illness
 Unstable psychiatric disorder or history of anorexia
 Other drug therapy, if incompatible (eg MAO inhibitors,
migraine drugs, adrenergic agents, arrhythmic potential)
 Closed angle glaucoma (caution)
 General anesthesia
ORLISTAT (XENICAL)
 Pancreatic lipase inhibitor that blocks the absorption of up to
one third of ingested fat.
 In addition to helping reduce weight, orlistat has been shown
to also:
 lower plasma low-density lipoprotein cholesterol (LDL)
cholesterol levels.
 The decline in LDL cholesterol is greater than that expected
due to weight loss alone.
 Lower HgbA1C in diabetic patients
INDICATIONS
Among obese patients who meet the criteria
for anti obesity drug therapy, orlistat is most likely
to benefit those who:
 Do not feel hungry
 Are not preoccupied with food
 Eat out or order-in often
 Have increased cardiovascular disease risk or multiple
cardiovascular risk factors
 Are older
 Take multiple medications

Orlistat is taken 3 times daily with meals

SIDE EFFECTS
 Because it blocks intestinal absorption of fat it can
result in diarrhea and steatorrhea
 This is minimized by maintaining a strict low fat diet
(<30% of diet)
 Another concern is the loss of fat soluble vitamins
with a potential for malnutrition.
 To prevent this, recommend a daily multivitamin for
all patients on this therapy
CONCLUSION
 PHARMACOTHERAPY OF OBESITY

 Diet/lifestyle changes remain the mainstay of the treatment

of obesity
 In patients not reaching goals, drugs can be an important
tool
 Expect only modest weight loss at best with current drugs

 Be aware of Rx indications and contraindications

 Off label use of non-indicated products is not recommended

 Investigational agents may offer hope for treatment of

obesity in the future