Diabetes - Pharmacology Flashcards
What are the types of pharmacological treatments for T2DM?
biguanides - metformin
sulphonylureas - gliclazide, tolbutamide
DPP-4 (gliptins) - linagliptin, sitagliptin
thiazolidinediones - pioglitazone
GLP-1 - liraglutide, exenatide
SGLT-2 (flozins) - dapagliflozin, canaglipflozin
alpha glycosidase inhibitors - acarbose post prandial regulators - repaglinide
= rarely used
How does metformin work?
increase insulin sensitivity and uptake by skeletal muscle
suppress hepatic (liver) gluconeogenesis
What are the advantages and disadvantages of metformin? What are the cautions advised?
advantages
- cause weight loss
- does no cause hypoglycaemia
disadvantages
- GI discomfort is common - nausea, vomiting
- risk of lactate accumulation = lactic acidosis
cautions
- cannot be used in renal (kidney) impairment (CrCl < 30mL/min)
- must be stopped in acute kidney injury
- cannot be used in hepatic (liver) impairment
How do sulphonylureas work?
gliclazide, tolbutamide
stimulates pancreatic insulin secretion by blocking potassium channels in pancreatic beta cells
What are the advantages and disadvantages of sulphonylureas? What are the cautions advised?
advantages
- good reduction in Hb1Ac
disadvantages
- GI discomfort is common
- weight gain
- hypersensitivity reactions = hepatic toxicity, rash, agranulocytosis
cautions
- risk of hypoglycaemia (no regulation)
- increased risk of renal (kidney) or hepatic (liver) impairment
= cannot be used in either states
How do GLP-1 agonists work?
glucagon-like peptide 1 agonist
- liraglutide
increase insulin secretion from beta cells after meals
suppresses glucagon release
reduces gastric emptying, increases satiety (fullness)
- are not oral administered = subcutaneous injection
What are the advantages and disadvantages of GLP-1 agonists? What are the cautions advised?
advantages
- weight loss = consider if BMI is > 35
disadvantages
- GI discomfort is common
caution
- injectable
- increased risk of pancreatitis (due to site of action)
How do DPP-4 inhibitors (gliptins) work?
sitagliptin
delays inactivation of GLP-1 = inhibit the enzyme that would break down GLP-1
What are the advantages and disadvantages of DPP-4 inhibitors? What are the cautions advised?
advantages
- well tolerated
- reduces appetite leading to weight loss
disadvantages
- GI discomfort is common
- headaches
- sore throat
- hypersensitivity
cautions
- increased risk of pancreatitis, urticaria (rash, hives), angioedema
- dose must be titrated in chronic kidney disease
How do SGLT-2 inhibitors work?
- dapagliflozin
inhibit renal absorption of glucose
What are the advantages and disadvantages of SGLT-2 inhibitors? What are the cautions advised?
advantages
- weight loss
- can improve blood pressure
disadvantages
- increased UTIs
- euglycaemic diabetic ketoacidosis
cautions
- avoid in chronic kidney disease
- risk of hypoglycaemia if taken with hypoglycaemics
- avoid with diuretics (excessive urination would occur)
How do thiazolidinediones work?
- pioglitazone
enhance insulin action
- increased peripheral insulin uptake and reduced gluconeogenesis
What are the advantages and disadvantages of thiazolidinediones? What are the cautions advised?
advantages
- increases insulin sensitivity
disadvantages
- weight gain
- peripheral oedema
cautions
- heart failure
- hepatic impairment
- bladder cancer
- increased bone fracture
What are the categories of drugs?
insulin providers, insulin sensitisers, incretin based therapies or other
insulin sensitiser
- metformin, pioglitazone
insulin provider
- insulin, sulphonylureas, meglitinides (repaglinide)
incretin based therapy
- DPP-4 inhibitor
- GLP-1 agonist
renal glucose uptake inhibitors
- SGLT-2 inhibitors
gastrointestinal glucose absorption inhibitor
- acarbose
Which drug can be taken in renal impairment?
liraglutide
- GLP-1 agonist
