Page 536 - fbkCardioDiabetes_2017

512 Obesity And Weight Management - Current Concepts

PHARMACOLOGICAL THERAPY ture, Decreased energetic efficiency, and Decreased
caloric intake as an appetite suppressant
Current FDA-Approved Anti-Obesity Drugs
The most common adverse effects were dry mouth,
• ORLISTAT.
paresthesia, constipation, insomnia, dizziness, and
• LOCARSERIN.
Dysguesia
• PHENTERMINE/ TOPIRAMATE.
This combination reduces the blood level of ethinyl
• SIBUTRAMINE. estradiol levels by almost 16% could result in -De-
creased contraceptive efficacy and increased break-
• NALTREXONE/BUPROPION
through bleeding.
• LIRAGLUTIDE/EXENATIDE
The rate of depression and anxiety was 4-7 times
• METFORMIN. higher among patients randomized to high-dose
ORLISTAT phentermine/topiramate when compared with those
in the placebo group. This drug combination is asso-
Orlistat inhibits lipase and it is an enzyme that helps ciated with greater weight loss than other available
in breaking triglycerides down into fatty acids and is strategies and a more favorable side-effect profile. Its
produced in the pancreas and stomach. This results effect on total cholesterol, LDL cholesterol, and HDL
in a lower rate of fat absorption by almost 30%. Orli- cholesterol levels is positive.
stat also reduces total cholesterol and LDL cholester-
ol. This medication could be considered in patients SIBUTRAMINE
who have the metabolic syndrome. Sibutramine widely used after its approval by the
USFDA in 1997. It is a serotonergic and adrenergic
Contraindication - Pregnancy, chronic malabsorption
syndromes, cholestasis. drug – inhibits the re uptake of serotonin and norepi-
nephrine. It is converted into 2 pharmocologically ac-
Adverse effects - Oily Spotting, flatus with discharge, tive metabolites- N- desmethyl and N- bisdesmethyl
fecal Urgency, fatty/oily stool, increased defecation, sibutramine Sibutramine suppresses appetite, caus-
fecal incontinence. es satiety,↑thermogenesis mainly through its active
LORCASERIN metabolites

Lorcaserin is a serotonin or 5-hydroxytryptamine (5- In a 12 month trial in overweight and obese adults
HT) agonist. Serotonin is involved in the regulation who had BMI of 25kg/m2 or greater weight loss was
of appetite and food intake behavior. Lorcaserin is 4.45 kg. There was a decrease in HbA1C level . Waist
metabolized by the liver and excreted renally, cannot circumference was reduced. Sibutramine showed po-
be removed by hemodialysis. Lorcaserin appears to tential benefits by improving biochemical risk factors
be more beneficial in the first few months and slowly associated with obesity, including plasma glucose,
loses its ability to maintain long-term weight loss. insulin, triglycerides, total cholesterol, LDL and HDL.

This medication does not reduce LDL cholesterol and NALTREXONE/BUPROPION
has no effect on HDL cholesterol, but it reduces total Naltrexone is an opioid receptor antagonist used for
cholesterol and triglyceride levels. Potential increased alcohol and narcotic addiction. Bupropion is an anti-
rate of cancer remains a concern. depressant that is also beneficial to promoting tobac-
PHENTERMINE/TOPIRAMATE co cessation and weight loss. Bupropion is a selective
reuptake inhibitor of dopamine and noradrenaline; it
A nonselective stimulator of synaptic reduces cravings for nicotine and food most likely
A) Noradrenaline, due to increasing the extracellular dopamine level.
B) Dopamine, The effect of this combination is to reduce hunger;
it has no effect on energy metabolism.
C) Serotonin release
Topiramate - Anticonvulsant drug that blocks volt- The most common reported adverse events were
age-dependent sodium channels, glutamate recep- nausea, headache, constipation, dizziness, vomiting,
tors, and carbonic anhydrase, and augments the ac- and dry mouth, compared with the placebo group.
tivity of gaminobutyrate. This medication is a good choice for patients who
smoke and have a mild to moderate level of depres-
Phentermine has been used as an appetite suppres- sion.
sant in the US since 1959. Increased energy expendi-

GCDC 2017