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Gastrointestinal System > Pharmacology & Treatment of Eating Disorders > Flashcards

Pharmacology & Treatment of Eating Disorders Flashcards

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1
Q

What happens to the appetite during acute stress? Why?

A

It decreases due to the release of adrenaline

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2
Q

How is obesity determined?

A

By calculating the BMI

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3
Q

What is the calculation for BMI?

A

(Weight)/ (Height)^2

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4
Q

What is the initial treatment for obesity?

A

Comprehensive lifestyle intervention: a combination of diet, exercise and behavioral modification.

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5
Q

What dietary changes are made during initial treatment for obesity?

A

Lower calorie intake, cut down on sugars and fats

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6
Q

How long does initial treatment continue?

A

Depends on the patient, usually they are monitored and based on their process you choose to continue or not

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7
Q

When is subsequent treatment initiated?

A

When patients are unable to achieve weight loss goals with a comprehensive lifestyle intervention alone

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8
Q

What is the indication that the initial treatment is successful?

A

The patient loses about 5% of body weight in the time period of 3 to 6 months

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9
Q

What are the options of the subsequent treatment?

A

Pharmacologic treatment
Surgery

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10
Q

What is the goal of therapy?

A

To prevent, reverse or improve the complications of obesity and improve quality of life

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11
Q

What are the characteristics required by an obese individual to initiate pharmacological therapy?

A

BMI > 30
OR
BMI > 27 with at least one weight-related comorbidity

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12
Q

Are most drugs long or short- term?

A

Short-term

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13
Q

Which drugs are used for long-term weight management?

A

The newer medications

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14
Q

When are drugs considered effective?

A

If they demonstrate at least a 5% greater reduction in body weight than placebo

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15
Q

What kind of comorbidities is obesity associated with?

A

Type 2 DM
HTN
Dyslipidemia
CHD

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16
Q

What is the correlation between BMI and morbidity/mortality?

A

The higher the BMI, the greater the risk of morbidity and mortality

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17
Q

Why has the role of drug therapy been questioned?

A

Concerns regarding efficacy, potential abuse, side effects and cost

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18
Q

What are examples of GLP1 receptor agonists?

A

Semaglutide
Liraglutide

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19
Q

What is the mechanism of action of GLP1 receptor agonists?

A

Chemically modified versions of GLP1, stimulating binding to GLP1 receptors

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20
Q

Where do GLP1 receptor agonists act?

A

CNS, areas of the brain like hypothalamus which are involved in the regulation of appetite and calorie intake.

Stomach, short period of satiety and loss of appetite by slowing gastric emptying.

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21
Q

How does slower gastric emptying help reduce weight?

A

Food remains in the stomach for longer, the stomach takes longer to empty out and thus sends a “hunger” signal (ghrelin). Slower rate of absorption of food in the bloodstream.

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22
Q

What do GLP1 agonists also stimulate secretion of?

A

Secretion of incretin which increases glucose-dependent insulin secretion

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23
Q

What is the effect of incretin?

A

Decreases inappropriate glucagon secretion.

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24
Q

Which kind of patients are GLP1 agonists preferred to be given to because of incretin?

A

Type 2 diabetes patients –> improve glycemic levels and reduce weight

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25
Is semaglutide long or short-term use?
Chronic weight management
26
What are the main side effects of GLP1 agonists?
GI side effects: nausea and vomiting Diarrhea Anorexia
27
What is the example of dual-acting GLP1 & GIP receptor agonist?
Tirzepatide
28
What is Tirzepatide?
A dual-acting GLP1 and GIP receptor agonist that is used as first-line medication
29
What is the function of GIP?
GIP increases insulin secretion, improves glucose tolerance and reduces gastric acid secretion
30
What is the mechanism of action of Tirzepatide?
The dual agonism decreases hyperglycemia severely more than just GLP1 agonists on their own, and reduces patient's appetite
31
What was the body weight percentage drop after giving Tirzepatide to patients with no diabetes?
16.5 % to 22.4% over 72 weeks
32
What are the PK of Trizepatide?
Subcutaneously given by weekly injection
33
What are the adverse effects of Trizepatide?
Nausea, Vomiting, Diarrhoea, Constipation and Increased Heart Rate
34
What should patients on GLP1 or dual acting GLP1/GIP agonists be monitored for?
Depressive symptoms and suicidal thoughts Unusual changes in mood or behaviour
35
What are the contraindications for both GLP1 and GLP1/GIP agonists?
Patients with personal or family history of medullary thyroid carcinoma Patients with multiple endocrine neoplasia syndrome type 2 Pregnancy
36
Why are GLP1 and GLP1/GIP agonists contraindicated during pregnancy?
Can cause teratogenicity, fetotoxicity and abortion (seen in animals)
37
What is an example of lipase inhibitors?
Orlistat
38
When are lipase inhibitors taken?
Only after fatty meals, it prevents the lipase enzymes from breaking down fats and being absorbed and stored in the body
39
What is the MOA of Orlistat?
Decreases the breakdown of fat into smaller molecules and therefore, decreases fat absorption by about 30% and increases fecal fat excretion
40
What are the pharmacokinetics of Orlistat?
Administered orally with each mean that contains fat Minimal systemic absorption, excreted in the feces No dosage adjustments required in patients with renal/hepatic dysfunction
41
What are the side effects of lipase inhibitors ?
Oily stool Diarrhea Decreased absorption of lipid soluble vitamins
42
What does Orlistat interfere with the absorption of?
Fat-soluble vitamins (vitamins A, D, E, and K) and β-carotene, patients should be advised to take a multivitamin supplement at bedtime Other medications
43
What other medications does Orlistat interfere with?
Amiodarone Cyclosporine Levothyroxine
44
Is Orlistat a short or long-term medication?
Available for long-term treatment of obesity but clinical utility is limited due to GI side effects
45
How are the GI side effects of Orlistat minimised?
Though low-fat diet and cholestyramine
46
What is cholestyramine?
A drug that reduces the re-absorption of bile in the body
47
What are the contraindication of Orlistat?
Pregnancy Patients with chronic malabsorption syndrome
48
What are anorexiants?
Appetite suppressants; sympathomimetic drugs and are classified as controlled substances
49
Why are anorexiants classified as controlled substances?
Due to dependence and abuse potential
50
What are examples of Anorexiants?
Phentermine Diethylpropion Benzphetamine Phendimetrazine
51
Are anorexiants approved as long or short-term medication treatments?
Short-term because of their potential side effects and potential abuse
52
What is the MOA of Phenetrmine?
Increases the release of norepinephrine and dopamine and inhibits their uptake in nerve terminals
53
What is the result of increasing levels of dopamine and norepinephrine?
Decrease appetite which facilitates weight loss
54
When does weight loss plateau?
When tolerance is achieved, discontinuation of drug should be progressive and not immediate
55
What re the pharmacokinetics of anorexiants?
Rapidly absorbed after oral administration Peak plasma concentration within 1 to 2 hours Undergo extensive first pass metabolism Metabolised to inactive compounds by the liver Elimination via the kidneys
56
What is the half life of anorexiants?
Short, 4 to 8 hours
57
What are the side effects of anorexiants?
Increase HR and BP Dizziness, headache and insomnia Changes in libido Constipation, diarrhoea and nausea
58
What are the contraindications fro anorexiants?
Patients with HTN, CVD, arrhythmias, HF or stroke and history of drug abuse
59
Which is the most widely prescribed weight loss drug?
Phentermine
60
What are combination drug treatments?
Combining two drugs with different mechanisms of action that improve efficacy
61
What are examples of combination drugs?
Phentermine-Topiramate Bupropion-Naltrexone
62
Is the combination drug Phentermine- Topiramate long or short term use?
Long term use
63
What is the MOA of Phentermine- Topiramate?
Topiramate affects the activity of two neurotransmitters: GABA enhancement and glutamate decrease Phentermine is a stimulant to contradict the sedation
64
What is the effect of Topiramate on its own?
Induction of sedation
65
What are the side effects of Phentermine- Topiramate?
Suicidal ideation, cognitive function decrease and dry mouth
66
What are the contraindication of Phentermine- Topiramate?
Contraindicated in pregnancy Patients with history of renal stones Patients with CVD
67
Why is Phentermine- Topiramate not given to patients with history of renal stones?
Topiramate is a weak carbonic anhydrase inhibitor, increases calcium excretion and decreases citrate in urine
68
Discontinuation of Phentermine- Topiramate?
Should not be stopped abruptly, can cause seizures
69
When was Bupropion-Nalterxone FDA-approved?
September 2014
70
Is Bupropion-Nalterxone first line treatment? Which kind of patients is it suggested to?
No, it could be prescribed for the obese smokers who desire pharmacology therapy for smoking cessation and obesity
71
What is Bupropion?
A weak dopamine and norepinephrine reuptake inhibitor
72
What is Bupropion used for?
Treatment of depression and smoking cessation.
73
What is Naltrexone?
Opioid-receptor antagonist used to treat alcohol and opioid dependence
74
What is the MOA of Bupropion-Nalterxone?
Stimulate POMC neurons through bupropion, Blocking the auto-inhibitory mechanisms of POMC with naltrexone
75
What is Bupropion-Nalterxone metabolised by?
By CYP2B6, low risk of drug to drug interactions
76
What are the side effects of Bupropion-Nalterxone?
Nausea, headache, seizure, constipation. Low risk of young adults becoming suicidal during initial treatment
77
Is Setmelanotide long or short term use?
Chronic weight management
78
Who is Setmelanotide used for?
Adult and paediatric patients 6 years of age and above with monogenic or syndromic obesity
79
What kind of deficiencies allow for Setmelanotide use?
POMC OCSK1 LEPR Bardet-Biedl Syndrome
80
What is the Bardet-Biedl syndrome?
Inherited disease that causes loss of night and peripheral vision
81
What is the MOA of Setmelanotide?
Acts on the MC4R agonist Potentially restores the function of an impaired MC4R pathway, reduces hunger
82
What is the MC4R?
Key part of the biological pathway that regulates hunger, calorie intake and energy expenditure
83
What is an example of serotonin agonists?
Lorcaserin
84
What is the effect of serotonin?
Reduces food intake in animals and human beings
85
What is the MOA of Lorcaserin?
Selective agonist that activates serotonin 2C receptors. Activation of POMC --> activation of melanocortin receptors Decrease in appetite
86
Was Lorcaserin used long or short term?
Long-term use
87
What drug does Lorcaserin have similar efficacy but lower side effects with?
Orlistat
88
Where are serotonin 2C receptors found?
Most in the central nervous system
89
When was Lorcaserin discontinued and why?
February 2020 because of an increased occurrence of cancer
90
What types of cancers were associated with Lorcaserin?
Colorectal, pancreatic and lung cancers
91
What were the side effects of Lorcaserin?
Nausea Headache Dry mouth Dizziness Constipation Mood changes and Suicidal Ideation
92
What are the pharmacokinetics of Lorcasterin?
Extensively metabolised in the liver to inactive metabolites and eliminated in the urine
93
What is the effect of Lorcaserin on Type 2 DM patients?
Higher risk of hypoglycemia
94
What are the contraindication of Lorcaserin?
Pregnancy
95
What are some examples of not recommended therapies?
Green tea, garcinia cambogia, conjugated lionelic acid chitosan calcium chromium, gambisan, hoodie gordonii
96
What are orexigenic drugs?
Appetite stimulants, increase appetite and enhance food consumption
97
When are orexigenics prescribed?
Severe appetite loss or muscle eating due to CF, anorexia, old age, cancer or AIDS
98
What are examples of oexigenics?
Corticosteroids Progesterone analogues Cannabinoids Serotonin antagonists Anabolic steroid Mirtazapine
99
What is an example of corticosteroids (orexigenic)?
Dexamethasone
100
What is the difference between glucocorticoids and progesterone analogues?
Progesterone analogues have fewer side effects
101
What is an example of serotonin antagonist?
Cyproheptadine
102
What is an example of cannabinoid?
Dronabinol
103
MOA of Dronabinol:
A synthetic version of THC acts on cannabinoid receptors in the brain. Relieves nausea
104
Which kind of patients are androgens given to?
Older persons to increase muscle mass or to help patients recovering from severe illness or injury
105
What is an example of an androgen?
Oxandrolone
106
What is an example of tetracyclic antidepressant?
Mirtazapine
107
What is the MOA of Mirtazapine?
Treatment for major depression, weight gain is a side effect

Gastrointestinal System (29 decks)

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