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Metabolism > Drugs Used in Obesity > Flashcards

Drugs Used in Obesity Flashcards

1
Q

What are the medical complications of obesity?

A

diabetes, coronary heart disease, hypertension, sleep apnoea, osteoarthritis, asthma and cancer

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2
Q

Where do satiety signals come from and what do they signal via?

A

satiety signals come from the stomach and liver and signal via the vagus nerve and sympathetic nerves to the medulla and then to the hypothalamus

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3
Q

What are the adiposity signals and where do they signal to?

A

insulin and leptin - signal to the hypothalamus

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4
Q

What are the central peptides that increase food intake?

A

NPY, melanin concentrating hormone, agouti-related peptide, orexin A and B, endocannabinoids

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5
Q

What are the central peptides that decrease food intake?

A

alpha-MSH, urocortin, corticotrophin releasing hormone, serotonin, noradrenaline

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6
Q

What are the peripheral peptides that increase food intake?

A

ghrelin

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7
Q

What are the peripheral peptides that decrease food intake?

A

CCK, insulin and leptin

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8
Q

What are the plasma levels of leptin proportional to?

A

body fat

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9
Q

When in the day are plasma leptin levels highest?

A

midday

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10
Q

Where is leptin secreted from?

A

adipocytes

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11
Q

Where are the receptors for leptin?

A

on the hypothalamus

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12
Q

How does leptin cross the blood brain barrier?

A

via a transporter (which is saturable)

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13
Q

What factors may lead to leptin resistance in obesity?

A

saturating the transport process, decreased sensitivity of the receptor and decreased sensitivity of the second messenger system

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14
Q

What are the different strategies to target obesity?

A

increase the peptides which inhibit food intake, decrease the peptides which stimulate food intake, decrease absorption of fats, increase metabolism of fats, increase thermogenesis

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15
Q

What are the only two current treatments available for obesity?

A

phentermine and orlistat

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16
Q

What is the mechanism of action of sibutramine and why was it withdrawn as a treatment?

A

decreases NA and serotonin reuptake - withdrawn because of cardiovascular complications

17
Q

What is the mechanism of rimonabant and why was it withdrawn as a treatment?

A

CB1 receptor antagonist - withdrawn because of increased risk of suicide

18
Q

What is the mechanism of action of phentermine?

A

blocks neuronal reuptake of NA, DA and 5-HT - although more selective for NA

19
Q

What are the adverse effects of phentermine?

A

increased BP, increased HR, insomnia, nervousness, headache, dry mouth

20
Q

What are the contraindications for phentermine?

A

use with other weight loss drugs, use with antidepressants, use in pregnancy

21
Q

Why can phentermine be only used for 3 weeks?

A

because tolerance develops

22
Q

What is topiramate, what is it used to treat and what is it used to treat off label?

A

topiramate is a treatment for epilepsy and migraines but it is used off label for weight loss and to improve insulin sensitivity although the mechanism is unknown

23
Q

What are the adverse effects of topiramate?

A

dizziness, taste alteration, teratogenic (cleft palate), parasthesia

24
Q

What is the mechanism of action of orlistat?

A

gastric and pancreatic lipase inhibitor - decreases fat absorption by 30% - if lipase can’t act then triglycerides can’t be absorbed so are excreted

25
Q

How much body weight is lost with orlistat?

A

5-10%

26
Q

What has orlistat been shown to reduce?

A

body weight, blood glucose, insulin tolerance, dyslipidaemia, blood pressure

27
Q

What are the adverse effects of orlistat?

A

after a fatty meal will get diarrhoea and faecal fat leakage

28
Q

What must be given in combination with orlistat?

A

a vitamin D and E supplement

29
Q

Can orlistat be used long term?

A

yes

30
Q

Why is an analogue of amylin potentially a treatment for obesity?

A

because amylin improves sensitivity of the brain to leptin and also slows the absorption of food for feeling of satiety and lower peak in blood glucose

31
Q

Why is glucagon like peptide 1 analogue potentially a treatment for obesity?

A

because it improves senstivity to insulin and slows the absorption of food for feeling of satiety and lower peak in blood glucose

32
Q

Why is diglyceride acyltransferase inhibitor a potential treatment for obesity?

A

stops deposition of fat

Metabolism (16 decks)

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