Drugs & Supplements Therapy in
Obesity Management
Dhani Isti - Ikhsan

Why using drugs?
I : BMI > 30 kg/m2 or BMI >27 kg/m2 w/
additional complicating factor(s)
I : Sudden weight gain 10-15 kg
• Reduced BW Maintained for 1-2 years at
minimum
• Reduce <10% of BW  reducing 25% risk of
comorbidities

Role of drugs
• Reduce appetite
• Reduce fat absorption
• Increase energy expenditure
 Reduction of comorbidities

General Precaution
Contraindication
Pregnancy, breast-feeding
Unstable cardiac disease
Uncontrolled hypertension (SBP > 180
mmHg, DBP > 110 mmHg)
Unstable severe systemic illness
History of anorexia nervosa
Active severe psychiatric disorder
Other drug therapy, if incompatible (e.g.
monoamine oxidase inhibitors,
antimigraine
drugs, adrenergic agents, drugs with
arrhythmia potential)
Caution
Presence of any severe systemic illness
History of severe psychiatric disorder
Other drug therapy
Closed angle glaucoma
Age < 18 years or > 65 years
Atkinson RL. Management of obesity:pharmacotherapy. In: Kopelman PG, Caterson ID,
Dietz WH (ed.). Clinical obesity in adults and children. 2nd ed. Oxford: Blackwell
Publishing Ltd; 2005. p.380-9

Type of drugs
• Lipase inhibitor
– Orlistat
– Cetilistat (under development) : fewer adverse
effect
• Amylase inhibitor
– α-glucosidase inhibitor (Acarbose) : only
significant in type 2 diabetes patient
• Biguanid : Metformin

Type of drugs
• Hormones
– HGH :mostly reduce visceral fat (!)cardiac changes
– Testosterone: reduce visceral fat
• Adrenergic agonist
– methamphetamin
• Serotonin agonist
– Sibutramin

Orlistat
• Approved by U.S. FDA : 60 mg in package,
3x/day, may be used for BMI >25kg/m2 (WHO
std)
• Mechanism of action :
– Blocks the action of pancreatic lipase, reducing
tryglyceride digestion and absorption
• Benefit :
– LDL reduction

Coutinho W. The first decade of sibutramine and orlistat: a reappraisal of their expanding roles
in the treatment of obesity and associated conditions. Arq Bras Endocrinol Metab. 2009;53/2

Side effects
Blockage of triglyceride digestion
• Fecal fat loss & GI symptomps
• Small-significant ↓ fat-soluble vitamins (Only
statistically significant for Vit. E
Contraindication
• Pregnancy
• Breastfeeding
• Cholestasis

Pharmacological interaction
• Safe w/ oral contraceptive in healthy women
• Reduce cyclosporin absorpstion

?Sibutramin?
• Mech. Of action: katekolaminergik &
serotoninergik
– Noradrenaline & 5-hydroxyttryptamine reuptake
inhibitor  increase satiety
• activation of sympathetic nervous system
trough β3-adrenergic receptors  increasing
metabolic rates & energy expenditures

Disadvantage
• Increase heart rate, blood pressure &
cardiovascular events
• Common effects:
– Insomnia, headache, dry mouth, constipation
• Serious effects : Seizure, gallstone, manic
episode in bipolar pts.
• Banned by FDA since 2010

References
1. Bray GA, Van Gaal LF. Drugs that modify fat absorption and
alter metabolism. In: Bray GA, Bouchard C (ed.). Handbook
of obesity: clinical applications. 3rd ed. New York: Informa
Healthcare; 2008. p.315-29
2. Atkinson RL. Management of obesity:pharmacotherapy. In:
Kopelman PG, Caterson ID, Dietz WH (ed.). Clinical obesity in
adults and children. 2nd ed. Oxford: Blackwell Publishing Ltd;
2005. p.380-9
3. Coutinho W. The first decade of sibutramine and orlistat: a
reappraisal of their expanding roles in the treatment of
obesity and associated conditions. Arq Bras Endocrinol
Metab. 2009;53/2
4. Sibutramine. [online] 10 Jan 2010. Diunduh dari:
http://www.nlm.nih.gov/medlineplus/druginfo/meds/a6011
10.html

• Mediator inflamasi berlebihan  merusak
hormon  resistensi insulin
• HGH  efisiensinya (?)  lipolisis & protein
sintesis  adiposit  TG  FFA & gliserol 
meningkat  cardiovascular disease