Oral antidiabetics Flashcards
First things first, classes used in diabetes :
inhibiteurs des alpha-glucosidases, inhibiteurs de SGLT-2, sulfamides hypoglycemiants, incrinomimetiques (inhibiteurs de DPP-4 et agonistes GLP-1) , biguanides, glinides, glitazones.
Which of the antidiabetic drugs are secretagogue &how do they work, explain mechanism?
*Both sulfonylurea &glinide are secretagogues (only effective in type-2 diabetes) that work by blocking ATP sensitive K channels by binding to their specific receptors on the channels. The decrease in K efflux induces depolarization of the b-cells, both that &the increase in Ca influx stimulate insulin secretion.
Difference between glinides &sulfonylureas ?
Glinides have a rapid onset &a short duration of action in comparison to sulfonyureas, they are particularly effective in normalizing glucose levels after a meal, &are taken 1h to 30 mns before meals. Glinides share two common binding sites with sulfonylureas aside to a unique site. Glinides lack sulfur in their structure, which allows their consumption in cases of sulfur/sulfonylurea allergies.
When are glinides taken?
30mn to 1h before meals, since glinides have a rapid onset &a short duration of action. you can say ‘immediately before meals’
Glitazones; mechanism of action?
*Glitazones work on a molecular level by modulating gene expression. Their specific receptor is the PPAR-gamma present in liver, adipose tissues &skeletal muscles. They regulate lipid &glucose metabolism, adipocytes apoptosis &differentiation, insulin signal transduction, with the ultimate effect of increasing insulin sensitivity &decreasing its resistance. Slow on &offset over weeks to months.
When are biguanides taken?
Biguanides : Au milieu ou à la fin des repas Metformine
SGLT-2 inhibitors; mechanism of action.
*Sodium-glucose co-transporter inhibitors block SGLT-2 proteins involved in 90% of the glucose reabsorption in the proximal tubules. They are taken once daily, the increase risks of urinary/genitalia infections.
incrinomimetiques, what are they?
*Incrinomimetiques : incretins are intestinal hormones that stimulate the secretion of insulin after a meal, they also decrease glucogenesis by the liver.
alpha glucosidase inhibitors, best time to be taken?
at the start of the meal, big cup of water.
DPP-4 inhibitors, mechanism of action?
DPP-4 inhibitors increase levels of incretins in blood. DPP-4 are enzymes that degrade GLP-1 which is a key enteroendocrine factor responsible for the incretin effect.
Incrinomimetiques, two subclasses ?
DPP-4 inhibitors
GLP-1 agonists (inj)
DPP-4 inhibitors, mechanism of action?
DPP-4 inhibitors increase levels of incretins in blood. DPP-4 are enzymes that degrade GLP-1 which is a key enteroendocrine factor responsible for the incretin effect.
Sulfamides hypoglycemiants, medicaments ?
Sulfamides hypoglycemiants : Carbutamide, Chlorpropamide, Glibenclamide, Glibornuride, Gliclazide, Glimepiride, Glipizide, Gliquidone, Tolbutamide.
Glimepiride AMAREL. Gliclazide DIAMICRON. Glibenclamide DAONIL, EUGLUCAN. Glipizide OZIDIA.
Biguanides, medicaments ?
Metformine GLUCOPHAGE, STAGID.
Glinides, medicaments?
Repaglinide : NOVONORM, REPAGLINIDE