| Class | Oral hypoglycaemic |
|---|---|
| Chemistry |
Biguanide |
| Routes of administration |
Oral only |
| Absorption |
Completely absorbed, oral bioavailability 40-60% |
| Solubility |
pKa=12.4; good water solubility |
| Distribution |
VOD= 1-4 L/kg; minimally protein bound |
| Metabolism |
Minimal metabolism |
| Elimination |
90% of the dose is cleared renally |
| Time course of action |
Half life 6 hrs |
| Target receptor |
Complex I of the mitochondrial respiratory chain (and, indirectly, AMPK) |
| Mechanism of action |
By disabling the mitochondrial respiratory chain, biguanides decrease the ATP supply to hepatocytes, activating AMPK (a fuel-sensing enzyme which regulates the balance of anabolic and catabolic activity). The result is an activation of fatty acid oxidation and a deactivation of glycogenolysis and gluconeogenesis. Systemic glucose delivery from the liver is therefore decreased. |
| Clinical effects |
Hypoglycaemia, but also: |
| Literature reference |
Rena et al, 2017 |
| CICM details of understanding | Level 3 |
| Mentioned around Deranged Physiology | |
| Related SAQs |