Antidiabetics

Question 1

MOA: Stimulate pancreatic insulin secretion by blocking ATP-dependent K+ channels in pancreatic beta-cell membranes and opening of voltage-gated Ca+ channels. The increase in intracellular Ca+ concentration stimulates insulin secretion (though only works in people with residual pancreatic function)

Answer 1

Sulfonylurea (Gliclazide)

Question 2

Indication: can be used to lower blood glucose in combination with Metformin, or as monotherapy where Metformin is contraindicated or not tolerated

Answer 2

Sulfonylurea (Gliclazide)

Question 3

Potentially serious side effect of Gliclazide?

Answer 3

Hypoglycaemia
More likely in high doses, or when used in combination with other glucose-lowering drugs, or when patient is acutely unwell (d/t impairment of renal and hepatic function)

Question 4

First line DOC for control of blood glucose in DM2?

Answer 4

Metformin

Question 5

MOA: Reduces hepatic glucose output (reduces gluconeogenosis and glycogenolysis). Increases uptake and utilisation of glucose by skeletal muscle via activation of AMP kinase. Opposes action of glucagon

Answer 5

Metformin (Biguanide)

Question 6

Common are rare (but important) side effects of Metformin?

Answer 6

Common: GI upset- N/V, taste disturbance, diarrhoea.
Rare, but important: Lactic acidosis

Question 7

In what instances should Metformin be witheld?

Answer 7

AKI and eGFR <30
Sepsis and severe tissue hypoxia
Significant acute illness

Use with caution in renal and hepatic impairment

Question 8

Target HbA1c for type 2 diabetics?

Answer 8

48 mmol/L or less

Question 9

How often should Hba1c levels be monitored for type 2 diabetic patients?

Answer 9

Measure HbA1c levels at 3–6 monthly intervals until the HbA1c is stable on unchanging treatment, then at 6-monthly intervals.

Question 10

MOA: Inhibits sodium-glucose transporter in proximal (S1 segment) convoluted tubule of nephron

Answer 10

Dapagliflozin

Question 11

Important adverse effects of Dapagliflozin? (2)

Answer 11

Increased risk of genital and urinary tract infections due to glycosuria
Risk of euglycaemic ketoacidosis

Question 12

Warnings/contraindications for Dapagliflozin?

Answer 12

Hold duing acute illness that causes or presents a risk of volume depletion or hypotension (also use with caution in combination with BP lowering drugs and diuretics for the same reason)

Question 13

How are GLP-1 agonists (Dulaglutide, Exenatide) administered?

Answer 13

Once weekly subcutaneous injection

Question 14

NICE guidelines: If triple therapy with Metformin and 2 other oral drugs is not effective, consider triple therapy by switching one drug for a ___________ for adults with type 2 diabetes who:
- Have a BMI of 35 +
- or have a BMI < 35 and can’t take insulin for occupational reasons or would benefit from weight loss due to significant obesity-related comorbidities

Answer 14

GLP-1 agonist (Dulaglutide, Exenatide)

Question 15

MOA of Linagliptin, Sitagliptin?

Answer 15

Dipeptidylpeptidase-4 (DPP4) inhibitors prevent incretin degredation, such as GLP-1, which are released from the intestine in response to food.

Question 16

DPP4 inhibitors (Linagliptin, Sitagliptin) are generally well-tolerated (most common s/e is GI upset), but they are associated with a small risk of what condition?

Answer 16

Pancreatitis

Question 17

Contraindications for this drug class include DM1, ketoacidosis, pregnancy, and breastfeeding

Answer 17

DPP4 inhibitors (Linagliptin, Sitagliptin)

Question 18

MOA: Stimulates glucose uptake and utilisation from the circulation into tissues, including skeletal mm and fat. Activates Na+/K+-ATPase, reducing serum K+ concentrations

Answer 18

Insulin

Question 19

List these types of insulin in order of onset/duration of action:
- Insulin glargine (Lantus)
- Soluble insulin (Actrapid)
- Isophane or NPH insulin (Humulin)

Answer 19

Short acting: Actrapid (soluble insulin)

Intermediate: Humulin (Isophane or NPH insulin)

Long-acting: Lantus (insulin glargine)

Question 20

Important side effects of insulin

Answer 20

Most important is HYPOGLYCAEMIA. Can also cause weight gain, and lipohypertrophy of injection site