drugs used in OBESITY

Question 1

groups of drugs included:

Answer 1

1. anorexiants
2. lipase (pancreatic) inhibitor
3. GLP-1 receptor agonist
4. serotonin agonist
5. drugs combinations

Question 2

anorexiants → drugs included:

Answer 2

1. phentermine

2. diethylpropion

Question 3

anorexiants → mechanism of action:

Answer 3

1. ↑ release of norepinephrine, dopamine & serotonin (sympathetic nervous system) → fight or flight mode → ↓ appetite
2. result → decrease the appetite

Question 4

anorexiants → indications:

Answer 4

1. recommended for SHORT-term use (<3 months)

2. may lead to tolerance within weeks → weight loss plateaus

Question 5

anorexiants → CONTRAindications:

Answer 5

1. uncontrolled HT
2. cardiovascular disease
3. arrhythmias
4. HF
5. stroke

Question 6

anorexiants → side effects:

Answer 6

1. cardiovascular → ↑ BP, tachycardia
2. CNS → insomnia, restlessness, alters sexual behavior, hormonal secretion & mood
3. others → dry mouth, headache, constipation

Question 7

lipase inhibitor → drug included:

Answer 7

1. orlistat

Question 8

lipase inhibitor → mechanism of action:

Answer 8

1. inhibition of gastric & pancreatic lipase → ↓ absorption of dietary fats
2. DECREASE fat absorption by 30%

Question 9

lipase inhibitor → pharmacokinetics:

Answer 9

3 times/day with major meals (if they contain lipids)

Question 10

lipase inhibitor → indications:

Answer 10

1. BMI > 30

2. BMI > 28 with risk factors

Question 11

lipase inhibitor → CONTRAindications:

Answer 11

1. pregnancy
2. chronic malabsorption
3. cholestasis

Question 12

lipase inhibitor → side effects:

Answer 12

(may be decreased if combined with cholestyramine)

1. changes in bowel function (due to unabsorbed fat)
2. fatty/oily stool, oily spotting
3. intestinal gas with discharge
4. a feeling of urgency &/or increased no. of bowel movements
5. poor bowel control
6. kidney & liver TOXICITY (rare)

Question 13

GLP-1 receptor agonist → drug included:

Answer 13

liraglutide

Question 14

lipase inhibitor → side effects:

Answer 14

1. nausea
2. vomiting
3. constipation

Question 15

serotonin agonist → drug included:

Answer 15

1. lorcaserin

Question 16

serotonin agonist → mechanism of action:

Answer 16

1. selectively activates 5-HT2c receptors in CNS → DECREASE appetite
2. if pat. doesn’t lose at least 5% of bodyweight after 12 weeks → the drug should be discontinued

Question 17

serotonin agonist → indication:

Answer 17

chronic weight management

Question 18

serotonin agonist → CONTRAindications:

Answer 18

1. severe renal impairment
2. history of heart failure → use with caution
3. concomitant use with SSRIs, SNRIs, MAOIs & other serotogenic drugs → risk of serotonin syndrome

Question 19

serotonin agonist → side effects:

Answer 19

1. nausea
2. constipation
3. headache
4. dizziness
5. dry mouth
6. lethargy
7. valvulopathy
8. rare → mood changes, suicidal ideation

Question 20

combination drugs → drugs included:

Answer 20

1. phentermine + topiramate

2. bupropion + naltrexone

Question 21

combination drugs → mechanism of action:

Answer 21

1. topiramate → anticonvulsant, precise mechanism is unknown
2. bupropion → inhibitor of dopamine & norepinephrine uptake
3. naltrexone → μ-opiod receptor antagonist (mu)

Question 22

combination drugs → pharmacokinetics:

Answer 22

topiramate → dosed in steps, escalating dose every 2 weeks

Question 23

combination drugs → indication:

Answer 23

long-term treating of obesity

Question 24

combination drugs → CONTRAindications:

Answer 24

1. pregnancy (teratogenic)

2. concomitant use of MAOIs → serotonin syndrome

Question 25

combination drugs → side effects:

Answer 25

phentermine + topiramate:

1. ↑ HR
2. paresthesias
3. suicidal ideation
4. cognitive dysfunction

bupropion + naltrexone:

1. nausea, vomiting
2. constipation
3. dry mouth
4. potential cardiovascular risk