Targeting obesity W1 Flashcards
(15 cards)
First line Medication for weight loss
Orlistat- a pancreatic lipase inhibitor
Widely used
An example of a withdrawn medication
Rimonabant - a CB1 inverse agonist
Repurposed medication
Semaglutide - GLP1 agonist
Targeting obesity via medication (3) what do we want to do
- Appetite suppression - eat less (semaglutide) or substances that expand in stomach to make us feel fu (methylcellulose). Nicotine also works to decrease appetite
- Decreased absorption - eat normal but absorb less (orlistat) and fibre supplements
- Increased metabolism - activation of brown adipose tissue (no drugs do this) - cold exposure
Fats are consumed as….
Glycerides which are Esthers of glycerol and fatty acids
They are too large to be absorbed
Pancreatic lipase breaks them down by Esther hydrolysis
Three fatty acids are then absorbed into the GI
Inhibition of lipase will reduce fat absorption
How are fatty acids absorbed and distributed? (3, EEA)
- Emulsification by bile.
- Enzymatic digestion by pancreatic lipase.
- Absorption of products of fat digestion depend on size.
How are fatty acids absorbed and distributed flow diagram?
Large fat droplets are emulsified by bile salts in the intestine lumen
The fatty acids and monoglycerides leave the micells and enter the epithelial cell
Fatty acids linked to form triglycerides
Fatty globule combine with proteins to form chylomicrons inside the Goldie
Chylomicrons are extruded from the epithelial cell and enter a lacteal
Lymph in the lacteal transports chylomicrons away from the intestine
Orlistat mechanism of action
Resembles a triglyceride and is recognised by lipase as a substrate
Block fat absorb in gut
Inhibits enzymes that break down fats
Production of orlistat
Semisynthetic
Produced via fermentation
Orlistat as a drug (history, dose, effects)
FDA approved in 1999
Prescription dose of 120 MG 3X daily
Significant GI side-effects, including wind and fetal incontinence
Is an example of aversion therapy where the side-effects encourage a patient to avoid eating fats?
Why is Orlistat prescribed an who for
Is used with an individualised low calorie and low-fat diet and exercise program to help people lose weight
It is used in overweight people who may also have high blood pressure, diabetes, high cholesterol, or heart disease
It is also used after weight loss to help people from gaining back that weight
Is a class of medication is called lipase inhibitors
Works by preventing some of the fat in food to eat from being absorbed into the intestines and then removed in the stall
Semaglutide drug for obesity. Structure and dose
It is a synthetic GLP-1
Contains lipophilic fatty acid attached to the peptide backbone
Dosage is 0.2 5MG once a week for four weeks and then increase 0.5 MG once a week for four weeks and then increased if necessary to 1MG once a week
What is GLP-1
Glucagon-Like Peptide-1 — it’s a hormone that your body naturally produces, mainly in the intestines, in response to food.
Made by L-cells
GLP1 agonist
mimics the action of the natural hormone GLP-1
It binds to the GLP-1 receptors and enhance its effects
It is destroyed by DPP-4
has a short half life of two minutes
for type two diabetes treatment
Lowers BG
what GLP-1 does (brain etc)
In the brain:
- Reduces appetite
In the pancreas:
- Increases insulin secretion
In the stomach:
-Slows gastric emptying
