Insulin and Oral Hypoglycaemic Agents Flashcards
normal daily profile of insulin btw breakfast, lunch and dinner
Types of insulin available?
what type of insulin are most patients on now?
- Animal Porcine and Bovine
- Recombinant DNA technology
- Human short acting insulins
- Human rapid acting insulin analogues
- Isophane intermediate acting insulin
- Long acting basal analogue insulins
- Very long acting basal analogue insulins
why r insulins made as soluble preparations?
do delay the absorpion from injection site
and overcome the short plasma half life!
What is the difference between the different types of insulin available?
All types of insulin act the same way once absorbed into the bloodstream. The different types of insulin just have different absorption properties.
(its the way they enter the system that distinguishes them from each other!)
how do u change the absorbtive properties of different types of insulin?
play around and move the aa in the B chain
for example!
if u play with these…for example from B26-30
if u tinker with them, ex, take proline & put in aspartine in there,>> u can form smthing called ASPARTATE INSULIN >> which is a very common insulin we use everyday called Novorapid
what is the use of this
it makes it a very rapidly absorped insulin
what r the 6 Main Insulin Categories
- Ultrafast acting
- Rapid acting
- Short acting
- Intermediate acting
- Long acting
- Very long acting
which insulin type was turned down? what is used instead?
Not currently used to avoid confusion in prescribing.
Rapidly acting insulin’s are used as a substitute
“Rapid Acting insulins”
Peaks, Duration, onset, when to inject?
Novorapid, Apidra, Humalog
in solution they r monomors! single insulin molecules!
• Rapid onset of action 5 to 15 minutes
- Inject just before eating
- Peaks ~ 60 minutes
- Duration 4 to 6 hours
Short acting insulin
Peaks, Duration, onset, when to inject?
Intermediate acting insulin
Peaks, Duration, onset, when to inject?
they cover you in the afternoon and through the night!
so in the morning b4 breakie, u have ur shot of rapid or short acting, then u’ll take the intermediate acting
Long and very acting insulin >>gives u a fairly FLAT background profile
what is the significance of this?
it prevent hypoglycemia from occuring
Administration of insulin?
· Injections , pens
· Insulin pump therapy
o Primarily for type 1 diabetes
o Only rapidly acting insulin is administered in this way
o Some of these pumps have sensors that detect hyperglycaemia or hypoglycaemia and adjust insulin administration accordingly
Adverse effects of insulin
· Hypoglycaemia - confusion
· Hyperglycaemia – short term and long term (microvascular, microvascular) complications
· Lipodystrophy – lipohypertrophy or lipoatropy due to fat being stimulated instead of beta cells (increased incidence with older types of insulin)
· Painful injections
· Insulin allergies
what is Lipodystrophy
u don’t see it much now a days w/ the human insulins cuz theyre fairly pure
How do we treat Type 2 diabetes?
Type is either from>> Insulin resistance or beta cell failure”
we treat depending on the cause…
Biguanides, sulphonylureas, thiazolidinediones, DPP4 inhibitors, α- Glucosidase inhibitors, SGLT2s, GLP1 analogues and Insulin
Plus non pharmacologic methods
- bariatric surgery
- very low calorie diets
• Above require patient education and ability to monitor results of therapy
what could lead to poor adherence to the medication?
NICE Targets in Type 2 Diabetes regarding their HbA1c
what is this test measuring?
In general target for all is HbA1c 6.5 to 7.5%
HbA1c 6.5%:Diet and first 2 treatment steps
HbA1c 7.5%:Beyond this or if at> risk of severe hypoglycaemia
HbA1C: monitors how ur blood glucose has been over past 3 months! amount of G that attaches to ur RBC as it comes out of ur bone marrow, lives for 3 months and circulates.
List the Mechanisms of actions of types of oral hypoglycaemic agents
· Increase release of glucose from beta cells
· Decrease insulin resistance
· Mimic actions of glucagon like peptide
· SGLT 2 inhibitors
Sulphonylureas
action? side effects? most commonly used type?
Stimulate beta cell to release insulin ( attach to voltage gated channel)
SIDE EFFECTS:
- is gunna make u “sulk”>> cuz ull have weight gain! (insulin> stimulates ur apetite)
- hypoglycemia
Gliclazide
Biguanides
action? side effects? most commonly used type?
side effects:
- Limits weight gain> due to decreased apetite
- decreases heptic uptake of lactate> Lactic acidosis (rare)
- Vitamin B12 deficiency (uncommon)
MOSTLY GI SYMPTOMS!
Stop if CKD < 30ml/min or significant comorbidities
α glucosidase inhibitor
action? side effects? most commonly used type?
very rarely used!
Only 1 available in the class >>
Acarbose
Thiazolidinediones
action? side effects? most commonly used type?
glitterzone girls have sexy thighs and have many PAARtners
Action
bind to and activate one or more peroxisome proliferator-activated receptors (PPARs)
when activated, this recepter binds to DNA, triggering expression and repression of sepecific genes, and coding for proteins that regulate glucose and lipid metabolism
SIDE EFFECTS
- CVS concerns w/> Rosiglitazone
- Pioglitazone > weight gain, fluid retention and HF, effects on bone metabolism and bladder cancer
Rarely used nowadays
what r incretins?
r a group of metoblic hormones secreted from the gut in response to food ingestion, they stimulate the pancreas to secrete insulin.
Physiological effects of GLP-1
Glucagon Like Peptide 1 Therapies (GLP1)
action? side effects? most commonly used type?
- increasing # of these incretin molecules would help with those w/ diabetes! BUT……*
- the action of these r limited bc they r evetually broken down by enzyme DPP-4*
so we have GLP-1 mimetics (Gliptins {oral} or DPP- 4 inhibitors )> inject to resist degredation by DPP-4
ACTION:
- Increase insulin secretion from the beta cells
- Decreases production of Glucagon from alpha cells
- -increased saiety>> less likely to eat more>> weight loss*
- -may experience nausea>> so we give them a low dose bl bidaya*
- -pancreatitis> overstimulation of pancreas*
SIDE EFFECTS
- GI symptoms, nausea, loose stools or diarrhoea
- GORD
- Low risk of hypoglycaemia
- Occasional painful to inject
- Pancreatitis and pancreatic carcinoma
DO NOT USE ON PATIENTS U HAVE GFR< 30ml (CKD stage 4) > bc it tends to accumalate as a renal excretion and we dont want it to accumalate due to side effects itll cause
best form of administration of Glucagon Like Peptide 1 Therapies
(Gliptins or DPP- 4 inhibitors)?
and why?
Gliptins> oral
DPP-4 inhibitors> injectibles
DPP-4 injected!
bc u get a HIGHER level of GLP-1 injection than u do with the oral preparation.
Glifozins
action? side effects? names?
ACTION >> blocks SGLT2- inhibitors > Glucose excreted!
Dapagliflozin, Canagliflozin and Empagliflozin
SIDE EFFECTS:
- weight loss> loosing sugar
- Increase risk of UTI symptoms including genital & urinary infections especially in women (5%)
- Polyuria
- Hypoglycaemia risk low
Can be used for patients with Type1 and Type 2 diabetes as add on therapy !
which drug causes nausea?
DPP- 4 inhibitors
which drug Increase has risk of lower urinary tract symptoms ?
Glifozins
which drug may cause Lactic acidosis ?
metformin
which drugs cause weight gain?
Sulphonylureas
Glitazones
what type of insulin is administered in the pump therapy?
Only rapidly acting insulin
what is can be adminstered if a diabetic patients has “severe insulin-induced hypoglycemia?
how is it given? wha does it do?
GLUCAGON (im, sc, iv)
glycogen sythesis is reduced, therefire blocking the affects of insulin in the liver!
- which drug does not effect insluin secretion?
biguanids.. metaformin
