Drugs - diabetes Flashcards
What is the first line drug used in diabetes?
- Metformin
Metformin is __hyrdophillic/hydrophobic___
- hydrophilic
Where does metformin predominently concentrate?
- intestine
- liver
- kidney
Metformin is excreted___
- unchanged
Metformin can be described as a weak cellular poison.
True or false?
- True
Briefly explain the action of metformin?
- inhibition of complex 1 of electron transport chain
- fall in cellular ATP
- rise in AMP kinase
- reduction in gluconeogenesis
What is the rough drop in HbA1c by metformin?
- 18mmol/mol
What are side effects of metformin?
- GI intolerance
- MALA (metformin associated lactic acidosis)
Metformin dose should be __increased/decreased__ with decreasing renal function?
- decreased
- should start to be decreased when eGFR <45ml/min
- should be stopped when eGFR <30ml/min
Name the most commonly used sulphonylureas?
- Gliclazide
How do sulphonylureas work?
- bind to SURI
- closer of ATP sensitive K+ channels
- rise in membrane potential
- depolarisation
- opening of Ca2+ channels
- insulin released
sulphonylureas can be described as what?
- insulin secretagogues
Side effects of sulphonylureas
- increase weight
- risk of hypoglycaemia
- lack of CV benefit
What diabetes drug is known for its cardiovascular benefit?
- metformin
Name a thiazolidinediones drug?
- Pioglitazone
Thiazolidinediones are described as what type of drug?
- insulin sensitiser
Explain the effect of thiazolidinediones?
- increase fat mass storage
- removes fat from liver, muscle and pancreas
- increases adiponectin, increases insulin sensitivity
Side effects of thiazolidinediones
- increased weight
- reduction in blood pressure
- fluid retention
- fracture risk
Explain the incretin effect?
- equal amount of glucose given both IV and oral shows that less insulin is produced when IV
- GLP-1 in the gut good for increasing insulin production
What are the 2 types of drugs that work alongside the incretin effect?
- GLP-1 agonists
- DDP4 antagonists
What are the pathways of incretin drugs?
- amplify secretion of insulin
What is the simple result of GLP-1 agonists?
- increase insulin
- decrease glucagon
- decrease gastric emptying
Name a DDP4 inhibitor?
- sitagliptin
What is the role of DD4?
- Inactives GLP-1 and GIP
