Block 2: Obesity

Question 1

What is the MOA of Naltrexone?

Answer 1

Blocks the action of dynorphin (opioid peptide) at k receptor

Question 2

Describe the structure of naltrexone?

Answer 2

1. Increasing the size of the N-sustituent to 3-5 C (allyl, CPM, CBM) typically results in antagonists except for buprenorphine (CPM) whi is a potent partial agonist at u receptor
2. Larger substituents on nitrogen return agonistic properties of the opioid

Question 3

What is the MOA of buproprion?

Answer 3

Selective dopamine reuptake inhibitor and weaker 5‐HT and NE reuptake inhibitor

Also antagonizes nicotine receptors

Question 4

Describe the SAR structure of bupropion?

Answer 4

1. Reduction of the ketone to an alcohol will form either the threo- or erythro- form of hydropupropian (20% activity)
2. t-butyl prevent N-dealkylation
3. 6-hydroxybupropion retains 50% activity

Question 5

Enzymatic interaction of buproprion?

Answer 5

CYP2B6

Question 6

MOA of Naltrexone/Bupropion?

Answer 6

α–MSH mediates the anorectic effect of POMC

β-endorphin is responsible for autoinhibitory feedback that inactivates the anorectic effect

Question 7

MOA of phentermine?

Answer 7

Releasing agent of norepinephrine in neurons, although, to a lesser extent, it releases dopamine and serotonin into synapses as well

Question 8

Phentermine Brand

Answer 8

Adipex-P, Lomaira, Ionamin

Question 9

phentermine/topiramate brand?

Answer 9

Osymia

Question 10

What agents are chemical alternative to diet and exercise?

Answer 10

1. Phentermine (Adipex-P, Lomaira, Ionamin) -
2. Phentermine/topiramate (Qsymia)

Question 11

brand name of topiramate?

Answer 11

Topamax

Question 12

MOA of topiramate?

Answer 12

Sulfamate‐substituted monosaccharide derived from fructose with a broad spectrum of activity

It blocks sodium channels, L‐type calcium currents enhancing GABA-mediated chloride flux

Question 13

What is the MOA of Diethylpropion?

Brand

Answer 13

Tenuate

Stimulant prodrug of the amphetamine/cathinone class (schedule IV)

Stimulates norepinephrine release and weakly inhibits the uptake of dopamine

Question 14

What is the function of catinone?

Answer 14

Stimulates the release of dopamine and inhibits the reuptake of epinephrine, norepinephrine and serotonin

Question 15

MOA of Phendimetrazine?

Brand

Answer 15

Bontril

1. Stimulant/appetite suppressant of the amphetamine class
2. prodrug of phenmetrazine
3. Phenmetrazine stimulates the release of norepinephrine and dopamine
4. bridged analogue of cathinone

Question 16

MOA of benzphetamine?

Brand

Answer 16

Didrex

1. Prodrug of amphetamine and methamphetamine
2. Works to suppress appetite and slightly increase metabolism

Question 17

MOA of Lorcaserin?

Brand?

Answer 17

Belviq

Selective 5-HT2C receptor agonist

Leads to POMC production and consequently promotes weight loss

Question 18

Liraglutide MOA

Brand, BBW

Answer 18

Saxenda, Victoza

GLP-1 receptor agonist works by increasing insulin release from the pancreas and decreases excessive glucagon release

BBW: thyroid tumors

Question 19

MOA Orlistat?

Mrand

Answer 19

Alli, Xenical

Inhibits gastric and pancreatic lipases

Frequent oily discharge and farts

Question 20

GLP1 agonist actions of semaglutide?

Answer 20

1. Mimic GLP1 to increase production of insulin.
2. Enhance growth of pancreatic beta cells.
3. Inhibits glucagon.
4. Reduces food intake by lowering appetite and slowing down digestion in the stomach.

Question 21

MOA of semaglutide?

Answer 21

1. GLP1 receptor agonist
2. Substitution of the alanine prevents chemical breakdown by dipeptyl peptidase-4
3. Lysine at GLP position 26 increases drug binding to blood protein and lengthens half-life.

Question 22

Semaglutide Brand?

Answer 22

Wegovy, Ozempic, Rybelsus