ENDO + REPRO: THIAZOLIDINEDIONES Flashcards
1
Q
Thiazolidinediones: INDICATIONS
A
- Type 2 diabetes mellitus: As a single agent in overweight patients where metformin is contraindicated or not tolerated
- Added as a second agent to metformin or a sulphonylurea where blood glucose control is inadequate on one drug and the metformin/ sulphonylurea combination is contraindicated or not tolerated
- Added as a third agent with metformin and a sulphonylurea where blood glucose control is inadequate as an alternative to starting insulin
2
Q
Thiazolidinediones: MOA
A
- Insulin sensitisers
- They lower blood glucose by activating the gamma subclass of nuclear peroxisome proliferatoractivated receptors (PPARγ)
- This induces genes which enhance insulin action in skeletal muscle, adipose tissue and the liver, with increased peripheral glucose uptake and utilisation and reduced hepatic gluconeogenesis
- Do not stimulate pancreatic insulin secretion so do not cause hypoglycemia
- Can cause weight gain which can increase IR
3
Q
Thiazolidinediones: ADVERSE EFFECTS
A
- gastrointestinal upset, anaemia and minor neurological effects such as dizziness, headache and disturbed vision.
- More serious side effects include oedema and cardiac failure, particularly where pioglitazone is prescribed with insulin
- Associated with small increase in the risk of bladder cancer and an increase in bone fractures in women
- Idiosyncratic reactions include severe liver toxicity
4
Q
Thiazolidinediones: WARNINGS
A
- CI in heart failure, use with caution in patients with cardiovascular dx
- CI if there is known bladder cancer or macroscopic haematuria
- Used with caution inpatients with risk factors for bladder cancer (eg. smoking, occupational exposure, prior pelvic irradiation)
- Careful consideration should be given when prescribing pioglitazone for elderly patients who tend to have an increased risk of cardiac dx, bladder cancer, and bonef racture
- Use in caution in patients with hepatic impairment
5
Q
Thiazolidinediones: INTERACTIONS
A
- Pioglitazone combined with other antidiabetic drugs, increases the risk of adverse effects, e.g. hypoglycaemia and cardiac failure
6
Q
Thiazolidinediones: EXAMPLES
A
- Pioglitazone