Diabetes Drugs

Question 1

Exenatide

Answer 1

Glp 1 analogue
Increases half life
Derived from exendin 4

Question 2

Liraglutide

Answer 2

Glp 1 analogue
Acetylated human glp1
Slow release due to self association that delays absorption, plasma binding (via fa and albumin) and stability against metabolic degradation
Causes dose dependent tumors in rats

Question 3

Lixisenatide

Answer 3

39 aa derivative of exendin 4
Omitted proline 38 and addition of 6 lysines
Increased affinity for glp 1r
Decreased cleavage by dpp4

Question 4

Sitagliptin

Answer 4

Dpp4 inhibitor
Inhibit glp 1 breakdown
Only produces a affect when blood sugar is elevated
Causes release of glp1 from small intestine
Does not inhibit gastric emptying
Binds to a different site to the proteolytic site

Question 5

Lispro

Answer 5

Insulin rapid acting analogue
Pk to kp at b28/29
Blood glucose lowering agent
Impairs dimerisation

Question 6

Aspart

Answer 6

Insulin fast acting analogue
P-d b28
Lowers blood glucose
Repulsion of charges at dimer interface

Question 7

Glulisine

Answer 7

Insulin rapid acting analogue
Decreases zn2+ free self assembly 
Change in conformation, hexamer less stable
Cant hold onto zn
N(asparigine)-k b3 
K-E (glutamic acid) b29

Question 8

Detemir

Answer 8

Long acting insulin analogues
Omitted T
K plus c14 myristic acid
Binds to albumin thus decreased breakdown to mono

Question 9

Glargine

Answer 9

Long acting insulin analogues
Asp-glycine a21
T plus 2 arginines 
Shifts pI from 5.4 to 7 which is the same as the ph 
Precipitating it

Question 10

Degludec

Answer 10

V.long acting insulin analogue 
Omitted t 
Added dicarboxylic acid 
Forms polymers 
Does not bind to albumin

Question 11

PEGlispro

Answer 11

V.long acting insulin analogue 
Lispro kp mod
Lysine has a polyetheline pegulation 
Increases hydrodynamic radius, stability, 
Protects against proteolytic degradation
Decreased renal clearence

Question 12

Acarbose

Answer 12

Alpha glucosidase
Pseudotetrasaccharide 4 sugars and cyclic group
Blocks by revesible binding competatively
Dose dependent manner
Oligosaccharide binding site
Hydrolysis is prevented

Question 13

Miglitol / voglibose

Answer 13

Alpha glucosidase
Inhibition
Systemically absorbed
However not metabolised and filtered by kidneys

Question 14

Sglt 2 inhibitors

Answer 14

Phlorizin

Dapagliflozin

Question 15

Taspoglutide
What does it affect
Other facts

Answer 15

Glp1 receptor agonist
Uses unnatural aa
Haulted at phase 3 because of gi and hypersensitivity