U2ii: Understand the pharmacology of insulin preparations
Insulin
Very Short Acting
Short Acting
Long Acting
Chemical
Very Short Acting
Novorapid
Recombinant, synthetic very short acting insulin analogue
Short Acting
Actrapid
Recombinant synthetic short acting insulin analogue
Long Acting
Lantus
Recombinant synthetic long acting insulin analogue
Use
Very Short Acting
Hyperglycaemia
Mimics postprandial insulin spike
Short Acting
Hyperglycaemia
Mimics postprandial insulin spike
Long Acting
Hyperglycaemia
Mimics basal insulin release
Dose
Very Short Acting
Titrated to BSL
Short Acting
Titrated to BSL
Long Acting
Titated to BSL
Administered once daily at the same time each day
Presentation
Very Short Acting
Clear soln
100IU/ml
Short Acting
Clear soln
100IU/ml
Long Acting
Clear soln
100IU/ml
Route
Very Short Acting
IV
SC
Short Acting
IV
SC
Long Acting
SC only
Onset
Very Short Acting
5 min
Short Acting
30min
Long Acting
30-60min
Peak
Very Short Acting
30-60min
Short Acting
1-3h
Long Acting
no peak
DoA
Very Short Acting
2-5h
Short Acting
4-8h
(slower onset and prolonged DoA cd Novorapid)
Long Acting
16-24h
MoA
Binds insulin receptor
Stimulates autophosphorelation
PD
METABOLIC
Promotes E storage
Opposes catabolism
CHO
↑ glucose transport into cells (hepatic and extrahepatic)
↑ translocation of GLUT 4 (adipocytes/Muscle) ↑ glycogen synthesis ↓ gluconeogenolysis
FAT
↑ fat deposition
↑ FFA synthesis and TG storage
inhibits lipolysis
PROTEIN
↑ protein synthesis and a.a. uptake
↓ proteolysis
ELECTROLYTES
↑ K+ intracellularly
PK
Very Short Acting
A – rapid absorption after sc injection
M – Insulin proteases
Short Acting
A – rapid absorption after sc injection
M – Insulin proteases
Long Acting
A-on injection, the solution neurtralises forming microprecipitates
Small amounts of insulin are released from microprecipitates over 24hrs with no peak = allowing mimic of basal insulin levels in body
M – Insulin proteases
AE
Hypoglycaemia
Injection site irritation
Lipodystrophy
Rashes
Insulin allergy
Weight gain