DM Type 2 Drugs Flashcards
What are the drugs used for Type 2? (1st/2nd/3rd line)
How does Metformin Work?
It increases insulin sensitivity
Pros [4] & Cons of Metformin [3]
- Well tolerated
- Effective
- Weight neutral
- Improves mortality & CV complications
Cons:
- GI side effects
- Vit B12 malabsorption
- Lactic Acidosis
What do Sulphonyureas do? [2]
Give an example
Glimepiride
Blocks ATP-sensitive K+ channels leading to increased insulin secretion
Pros [4] and cons of Sulphonyureas? [2]
Contraindications [4]
Pros:
- Rapid action so good for the acutely ill
- Well tolerated
- Rapid titration
Cons:
- Risk hypo
- Weight gain
- Contraindicated in pregnant/breastfeeding
- Cautioned in renal/hepatic disease
MOA Thiazolidinediones[2]
Give an eg
Pioglitazone
Increases insulin sensitivity in muscle/fat/liver by acting on PPar gamma receptors
Pros [2] and cons [4] of Thiazolidinediones
- Effective for insulin resistance
- Safe with CV system
Cons:
- Weight gain
- Fluid retention
- Increases bone turnover -> fractures
- Bladder cancer
Example of a DPP-IV inhibitor and how they work?
Saxagliptin
DPP-IV is an enzyme that breaks down incretin hormones.
Inhibitors extend incretin half-lives.
Incretin hormones cause glucose dependant insulin release and glucagon inhibition
Pros and cons of DPP-IV?
- Well tolerated
- Usuable in renal impairment
- Weight neutral
- No Hypo risk
Cons:
- Small effects
- CI in pregnancy/breastfeeding
- PAncreatitis/pancreatic cancer
- Nausea
Example and function of SGLT-2 inhibitors? [3]
Gliflozins e.g. empagliflozin
Inhibit Sodium Glucose Transporter 2 in the proximal tubule of the kidney.
Thus increases Glc & Na excretion in urine
Effects of SGLT-2 inhibitors?
Diuretic Effect - Postural hypotension & dehydration
Glucouric Effect - Weight loss from pissing out so many calories
Na Excretion - Lowers BP
Greater risk of urogenital infections
Which Type 2 meds are injectable and which ones oral?
Oral:
- Metformin
- Sulphonyureas
- Thiazolidinediones
- DPP-IV inhibitors
- SGLT2 Inhibitors
Injected:
- Insulin
- GLP-1 analogue
Example and function of GLP-1 analogues?
Liraglutide
GLP-1 is an incretin hormone.
DPP-IV resistant analogues are injected (which cause Glc dependant Insulin release & glucagon inhibition) which have a much longer biological half-life.
What drugs can replace sulphonyurea’s as 2nd line Type 2 treatment if neccessary? [3]
- Thiazolidinediones e.g. pioglitazone
- DPP-IV inhibitors e.g. Sitagliptin
- SGLT-2 inhibitors e.g. Empagliflozin
How do DPP-IV inhibitors work? [4]
They inhibit DPP-IV, an enzyme that breaks down incretin hormones [1]
This prolongs the life of incretins [1] allowing them to cause Glc Dependant Decrease in Glucagon [1] release and Increase in Insulin Release [1]
Pros [4] and cons [4] of DPP-4 inhibitors?
Pros
- Well tolerated
- Weight Neutral
- Works in renal impairment
- No hypoglycaemic risk
Cons:
- small effect
- CI in pregnant/breastfeeding
- risk of pancreatitis/pancreatic cancer
- Nausea
How do GLP-1 analogues work? [3]
Similar to DDP-IV inhibitors.
GLP-1 is an incretin [1], the analogues are resistant to DPP-4 degradation [1] so have a longer half life causing:
- Glc dependant insulin release and glucagon inhibition [1]
Pros [1] & Cons [1] of GLP-1 Analogues?
Pros - Do cause some weight loss for those overweight
Cons - Nausea (by delaying gastric emptying)
Example of each Type 2 drug? [5]
Biguanides - Metformin
Sulphonyureas - Glimepiride
Thiazolidinediones - Pioglitazone
DPP-IV inhibitors - Saxagliptin
GLP-1 Analogue - Liraglutide
T2DM patients on metformin
Indications to start?
HbA1c rises to 58 mmol/l [3]
Metformin is 1st line if HbA1c has risen to 48mmol/mol on lifestyle measures.
HbA1c remains 58mmol/mol: triple therapy or consider insulin therapy
- Eg METFORMIN + GLIPTIN + SULFONYLUREA
Further management of T2DM for second line therapy
T2DM patients who can’t tolerate metformin: what to do when HbA1c rises to 58 mmol/mol?
When would insulin therapy be considered?
• GLIPTIN + PIOGLITAZONE
If despite double therapy, HbA1c remains at 58 mmol/mol
When starting insulin therapy what must be continued?
Continue metformin
If triple therapy is not effective, management of T2DM
If triple therapy is not effective or tolerated consider switching one of the drugs for a GLP-1 mimetic:
* BMI ≥ 35 kg/m² and specific psychological or other medical problems associated with obesity or
* BMI < 35 kg/m² and for whom insulin therapy would have significant occupational implications or weight loss would benefit other significant obesity-related comorbidities
* only continue if there is a reduction of at least 11 mmol/mol [1.0%] in HbA1c and a weight loss of at least 3% of initial body weight in 6 months
