DIABETES DRUGS Flashcards
What type of drugs is alogliptin, sitagliptin and linagliptin?
DPP4 inhibitors
What type of drug is metformin?
Biguanide
What type of drug is pioglitazone?
A thiazolidinedione
What type of drugs are canagliflozin, dapagliflozin, ertugliflozin?
SGLT2 inhibitors
What type of drugs are gliclazide, glimeperide, tolbutamide?
Sulfonylureas
What type of drugs are dulaglutide, exenatide, Liraglutide?
GLP-1 agonists
Whats the suffix for DPP4 inhibitors?
-gliptin
Whats the suffix for thiazolidinediones?
-glitazone
Whats the suffix for SGLT2 inhibitors?
-flozin
Whats the suffix for sulfonylureas?
-ide
Whats the suffix for GLP1 agonists?
-tide
Whats the MOA of DPP4 inhibitors?
Inhibits DPP4 which prevents inactivation of glucagon-like peptide which is an incretin
Whats the MOA of GLP1 agonists?
mimic the action of endogenous GLP-1 (incretin) to enhance insulin secretion and inhibit glucagon secretion from pancreatic islet cells.
Whats the MOA of metformin?
Decreases gluconeogenesis, intestinal absorption of glucose and increases insulin sensitivity by increasing peripheral glucose uptake and reabsorption.
Whats the MOA of thiazolidinediones?
Activate PPARs which are a group of nuclear receptors that when activated, increase insulin sensitivity by acting on adipose, muscle, and, to a lesser extent, liver to increase glucose utilization and decrease glucose production.
Whats the MOA of SGLT2 inhibitors?
Inhibit SGLT2 in the PCT to prevent reabsorption of glucose and facilitate its excretion in urine
Whats the MOA of sulfonylureas?
close ATP-sensitive K-channels in the beta-cell plasma membrane, and so initiate a chain of events which results in insulin release.
What are the contraindications of thiazolidinediones?
HF
Previous or active bladder cancer or uninvestigated macroscopic haematuria
Whats the first line drug of choice in type 2 diabetes?
Metformin
When should SGLT2 inhibitors be given in addition to metformin?
If the patient has a high risk of developing CVD, has CVD or has chronic HF
If metformin is contraindicated, what drug is first choice for type 2 diabetes?
SGLT2 mono therapy if the patient has risk of, has CVD or chronic HF
DPP4 inhibitor or sulfonylureas or pioglitazone if patient doesnt have above
When should GLP1 mimetic treatment be considered?
If triple therapy with metformin and 2 other oral drugs is not effective, not tolerated or contraindicated then consider triple therapy by switching 1 drug for GLP1 mimetic
NICE like patients to have achieved a > 11 mmol/mol (1%) reduction in HbA1c and 3% weight loss after 6 months to justify the ongoing prescription of GLP-1 mimetics.
When should you consider insulin therapy for type 2 diabetes?
When dual therapy has not continued to control HbA1c to below the person’s individually agreed threshold
Which antidiabetic drugs cause weight gain?
Pioglitazone
Sulfonylureas
Insulin
Which antidiabetic drugs cause weight loss?
SGLT2 inhibitors
GLP1 mimetics
Which antidiabetic drugs are weight neutral?
DPP4 inhibitors
Metformin
Which antidiabetic drugs carry risk of hypoglycaemia?
Insulin
Sulfonylureas - moderate risk
Which diabetics should statin be offered in?
Only pt with 10 year cardiovascular risk >10%
What is the incretin effect?
In normal physiology an oral glucose load results in a greater release of insulin than if the same load is given intravenously
This is because L cells of the ileum release GLP1
What are incretins?
hormones that are secreted from the gastrointestinal tract into the circulation in response to nutrient ingestion that enhance glucose-stimulated insulin secretion
What are common side effects of metformin?
GI side effects
Lactic acidosis
What are common side effects of sulfonylureas?
Hypoglycaemic episodes
Increased appetite and weight gain
SIADH - hyponatraemia
Hepatotoxicity
Bone marrow suppression
Peripheral neuropathy
Dont give in breast feeding or pregnancy!
What are common side effects of pioglitazone?
Weight gain
Fluid retention
Liver impairment
Fracture risk
Increased risk of bladder cancer
What are common side effects of DPP4 inhibitors?
Pancreatitis
What are metformin contraindications?
Renal dysfunction
Impaired hepatic dysfunction
Congestive HF
Metabolic acidosis
When should you add another drug when a pt is on metformin?
If HbA1c rises to 58 mmol/mol (7.5%)
Before this you can titrate metformin up and make lifestyle changes
If a pt is not tolerating metformin due to GI side effects, what should you do next?
Start metformin modified release
- this has a better GI SE profile. This is also only given once daily
Whats the most effective oral antidiabetic agent? Whats the biggest risk with this?
Sulfonylureas -gliclazide
Greatest risk of hypoglycaemia
Why should you stop metformin when you are sick?
Dehydration makes it more likely to develop lactic acidosis
Why should you stop sulfonylureas when you are sick?
If you are unable to eat and drink then you are more likely to develop hypos
Why should you stop SGLT2 when you are sick?
Dehydration can make it more likely to develop ketoacidosis
What are the major adverse efefcts of GLP-1 mimetics?
Nausea and vomiting
Exanatide - pancreatitis
What are the adverse side effects of SGLT2 inhibitors?
Urinary and genital infections
Normoglycaemic ketoacidosis
Increased risk of lower-limb amputation
Weight loss
How are GLP-1 mimetics administered?
Subcutaneous injections!
