Diabetes Medications
Pharmacology and Prescription Information
| Drug class | MoA | Examples | Overall clinical profile | Important side effects | Caution and contraindications |
|---|---|---|---|---|---|
| Biguanides | Metformin | Enhances the effect of insulin by:
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| SGLT-2 inhibitor | Dapagliflozin, empagliflozin | Inhibit SLGT-2 in proximal renal tubule → ↓ glucose reabsorption |
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It is normal to see glycosuria (typically ++ / +++ on urine dipstick) in those who take SGLT-2 inhibitors |
Reduced efficacy if eGFR <45 |
| Thiazolidinediones (TZD) | Pioglitazone | Activation of PPARγ in adipocytes → ↑ insulin sensitivity (increases glucose uptake into cells) | No warnings in renal impairment | ELBOW:
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| Sulfonylurea | Glicazide, glimepiride | ↑ Insulin secretion | Useful to rapidly lower blood glucose |
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| DPP-4 inhibitor | Sitagliptin, linagliptin | Inhibits DPP-4 (enzyme that breaks down GLP-1) → ↑ GLP-1 activity |
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| GLP-1 agonist | Liraglutide, exenatide, semaglutide | 3 main effects of GLP-1:
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Has multiple additional benefits:
Note that it is given via an injection |
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Acarbose is another anti-diabetic drug, but rarely used:
- It has a poorer anti-hyperglycaemic effect than many other antidiabetic drugs
- MoA: Reduce GI glucose absorption
- AEs: bloating, flatulence, diarrhoea
High-Yield Facts
Metformin Dosing
- Starting dose: 500mg daily
- Maximum dose: 2g daily (usually 1g BD)
- Timing to take metformin
- OD → take with breakfast
- BD → take with breakfast and dinner
- TDS → take with breakfast, lunch and evening meal
Drugs at Risk of Hypoglycaemia
2 main drugs:
- Insulin
- Sulfonylurea
SGLT-2 inhibitors carry a smaller risk of hypoglycaemia, but can occur if used in combination with insulin / sulfonylurea
Drugs at Risk of Weight Gain
Drugs that can cause weight gain:
- Insulin
- Sulfonylurea
- TZD (pioglitazone)
Effect on weight for other drugs:
- Weight neutral: metformin, DPP-4 inhibitor
- Weight loss: GLP-1 agonist, SGLT-2 inhibitor
Drugs in Renal Impairment
The following drugs can be safely used in renal impairment:
- TZD (pioglitazone)
- Linagliptin (NB other DPP-4 inhibitors require dose-reduction)
Summary of other drugs in renal impairment:
| Drug | Use in renal impairment |
|---|---|
| Metformin | Avoid if eGFR <30 |
| SGLT-2 inhibitor | Avoid if eGFR <15
NB reduced efficacy if eGFR <45 |
| Sulfonylurea | Dose reduction in renal impairment
Avoid in severe renal impairment (due to risk of hypoglycaemia) |
| DPP-4 inhibitor (apart from linagliptin) | Dose reduction if eGFR <45 |
| GLP-1 agonist | Avoid in renal impairment (exact cut-offs depend on the drug) |
Drugs to avoid in T1DM
The only drugs that should be used in T1DM are:
- Insulin – all patients
- Metformin – if BMI >25 kg/m2
ALL other drugs should NOT be used in T1DM. See this article on management of T1DM.
Drugs and Pregnancy
The only drugs that are safe in pregnancy are:
- Insulin
- Metformin
All other drugs should be stopped. See this article on management of diabetes in pregnancy
Drugs to Avoid in Pancreatitis
DPP4 inhibitors and GLP-1 agonists should NOT be used in patients with a history of pancreatitis, or should be stopped immediately if a patient on them develops acute pancreatitis
References