Type 2 diabetes antidiabetics Flashcards
Metformin
Biguanide
First line treatment
No weight gain
No hypoglycaemia
Metformin MOA
Reduces hepatic glucose production
Inhibition of mitochondrial respiratory-chain complex 1
Inhibition of ATP synthesis
Increase in AMP
Activation of AMPK
Phosphorylation and inhibition of CRTC2
Inhibition of gluconeogenic gene expression
Metformin side effects
GI: diarrhoea, nausea, vomiting, gas, reduced appetite
Vitamin B12 deficiency: reduces intestinal absorption
Rare: lactic acidosis
Metformin brands
Bolamyn
Diagment
Glucient
Glucophage
Metabet
Sulfonylureas brands
Glibenclamide - Danol
Gliclazide - Diamicron
Glipizide - Glibenese, minodiab
Glimepiride - Amaryl
Tolbutamide
Sulfonylureas side effects
Hypoglycaemia
Weight gain
Sulfonylureas MOA
Stimulate insulin secretion from pancreatic beta cells
Bind to ATP gated K channel > leads to insulin secretion
Not effective for type 1 diabetes
Meglitinides brands
Repaglinide - Prandin
Nateglinide - Starlix
Take before meals
Maglitinides MOA
Prandial glucose regulators
Rapid onset
Short duration
Stimulate insulin secretion from pancreatic beta cells
Bind to ATP gated K channel > leads to insulin secretion
Thiazolidinediones
Glitazones
-Pioglitazine - Actos
Pioglitazine + metformin - Competact
Thiazolidinediones MOA
Increase insulin sensitivity by stimulating expression of insulin sensitive genes
Bind and activate nuclear receptor PPAR gamma
Thiazolidinediones side effects
Water retention
Weight gain
GLP1
Incretin
Stimulate beta cells to secrete insulin
Short half life
Degraded by peptidases
GLP1 mechanism
Food > release active GLP1 and GIP > DPP4 rapidly degrades incretins within minutes > Incretin effect > insulin release
GLP1 brands
Exenatide - Byetta, Bydureon
Liraglutide - Victoza
Lixisenatide - Lixumia
Dulaglutide - Trulicity
Semaglutide - Ozempic
DPP4 inhibitors
Gliptins
Inhibit activity of GLP1 and DPP4
DDP4 brands
Sitagliptin - Januvia
Sitagliptin + metformin - Janumet
Vildagliptin - Galvus
Vildagliptin + metformin - Eucreas
Saxagliptin - Onglyza
Alogliptin - Vipidia
Alogliptin + metformin - Vipdomet
Lingaliptin - Trajenta
Lingaliptin + metformin - Jentadueto
Saxagliptin + metformin - Kombolyze
Alpha glucosidase inhibtor MOA
Slows down absorption of starchy foods by intestine
Alpha glucosidase inhibitor brand
Acarbose - precose
Miglitol - glyset
SGLT2 inhibitors MOA
Inhibits glucose transporter, less glucose in urine
SGLT2 inhibitors brand
Dapagliflozin - Forxiga
Canaglifozin - Invokana
Empaglifozin - Jardiance
Therapy
Monotherapy
- Metformin
- DDP/ PIO / SU
Dual therapy
- Metformin + DDP/ PIO / SU/ SGLT
- DDP + PIO
- DPP + SU
- PIO + SU
Triple therapy
- Metformin + SU + DPP/ PIO/ SGLT
- Metformin + PIO/ SGLT
- Insulin therapy
Failed triple therapy
- Metformin + SU + GLP1
If hypoglycaemic
- SU
- Short acting insulin
Surgery for type 2 diabetes
Over 35 BMI
Protein Kinase C
Serine phosphorylation on IRS inhibits insulin signalling
Tyrosine kinase
Phosphorylation on IRS inhibits insulin signalling
