Lec 10: Antiobesity Drugs Flashcards

1
Q

What condition (disease) is improved after weight loss (in women)

A

PCOS

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2
Q

What hormones are released from adipocytes

A
Leptin (paired with insulin)
Adiponectin - affect insulin sensitivity 
PAI-1 (haemostasis - form ลิ่มเลือด)
Angiotensinogen 
Pro inflammatory cytokins
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3
Q

What does Beta-3 adrenergic receptor increase?

A

Lipolysis

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4
Q

Why was Canabinoid-1 receptor antagonist drug, Rimonabant, withdrawn?

A

Because inhibiting cannabinoid receptors to lose weight also inhibits happiness therefore can cause depression and suicide

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5
Q

1st step of obesity management?

A

Exercise and dietary control

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6
Q

When is pharmacotherapy applied immediately in obesity patients?

A

When the patient has a BMI =/> 30 or 27 with obesity related diseases

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7
Q

Bariatric surgery is applied immediately only when patient …..

A

Has a BMI =/> 40 or 35 with obesity related comorbidities

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8
Q

Mech of action of antiobesity drugs

A

Reduce energy intake
Alter metabolism
Increase energy expenditure

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9
Q

What are anorexic agents

A

Appetite suppressants

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10
Q

Appetite suppressants

A

Phentermine, diethylpropion
Fenfluramine, dexfenfluramine
Sibutramine

All กระตุ้น catecholamine receptors

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11
Q

Thermogenic drugs

A

Adrenergic drugs
Beta-3 agonists
Thyroxine
Sibutramine

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12
Q

Thermogenesis in BAT

A

Beta3 receptors activated by cold stress —> cAMP increases and increases PKA —> PGC 1 increases and increase transcription of UCP1 gene —> burn fat for heat synthesis

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13
Q

Orlistat

Orlestra (fat substitute for cooking)

A

Drugs that decreases absorption of fat

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14
Q

Orlistat

A

Pancreatic lipase inhibitor

SE: fecal incontinence, fatty stool

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15
Q

Cetilistat

A

New drug same as orlistat

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16
Q

Anorectic drugs that increases 5-HT functions

A

Fenfluramine **

Dexfenfluramine, fluoxetine

Sibutramine*

17
Q

Agents increase catecholamine activities

A

Phentermine**

Phenylpropanolamine, mazindol, diethylproprion

18
Q

Bulk preparation

A

Methylcellulose, sterculia

Expands in stomach to make you full faster, but also makes you hungry faster

E.g. เม็ดแมงลัก

19
Q

Fen-phen

A

Fenfluramine (5-HT) and phentermine (catecholamine) —> appetite suppressant

AE: CARDIAC VALVULAR DISEASE & pulmonary hypertension —> withdrawn

20
Q

Sibutramine (meridia)

A

SNRI - serotonin norepinephrine reuptake inhibitor

Increases 5HT and NE —> increases satiety, dec hunger

NE stimulate thermogenesis (beta3 stim.)

Treat BMI 30 or 27 with comorbidities

21
Q

Absolute contraindication in SIBUTRAMINE

A

MAOI users (antidepressant) —> too much serotonin

Caution: SSRI users

22
Q

Locaserin

A

Selective serotonin receptor agonist

23
Q

Topiramate, zonisamide

A

Antiseizure agents

24
Q

Leptin analogues, transporter, receptor promotors

A

Antiobesity drugs

25
Q

Alpha-MSH analogues

A

Nervous pathway inhibitor/modulator (more msh induces more action of anorexigenic pathways)

Antiobesity drugs

26
Q

MC4 agonist

A

Activate POMC —> a-MSH—> low appetite

27
Q

Gastrointestinal-neural pathway agents

A

Increase CCK or GLP1 activity

Increases protein YY336 activity —> increase satiety

28
Q

Lorcaserin

A

Highly selective serotonergic 5-HT2C receptor agonist

Arcuate nucleus communicates with POMC neuron with 5HT thus stimulating the pathway with a-MSH which decreases appetite

May cause hypoglycemia in patients with DM2

C/I: pregnancy & breastfeeding

29
Q

Phentermine/topiramate ER

A

Phentermine - noradrenergic
Topiramate - GABA receptor activator

No serious AE

30
Q

Naltrexone/bupropion

A

Bupro= DA NE reuptake inhibitor

Naltre= opiate antagonist

No serious AE found yet but OPIATE antag so might suppress happiness cause depression

31
Q

Liraglutide

A

GLP-1 agonist —> DM drug

Decreases food intake, glucagon secretion

Increase insulin secretion