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
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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
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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
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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
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5
Q

Thiazolidinediones: INTERACTIONS

A
  • Pioglitazone combined with other antidiabetic drugs, increases the risk of adverse effects, e.g. hypoglycaemia and cardiac failure
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6
Q

Thiazolidinediones: EXAMPLES

A
  • Pioglitazone
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