Diabetes Drugs Flashcards
Mechanism of metformin?
1) increases insulin sensitivity
2) decreases glucose production by the liver (gluconeogenesis)
Key side effects of metformin?
1) GI upset: abdo pain, diarrhoea, N&V
2) Lactic acidosis (e.g. 2ary to AKI)
Is metformin safe in pregnancy?
Yes
What can be tried in patients with GI side effects from standard-release metformin?
Modified release metformin
Does metformin cause hypoglycaemia?
No
What class of drug is metformin?
Biguanide
Does metformin cause weight gain?
No - may cause weight loss.
Contraindications to metformin?
1) Acute metabolic acidosis (including lactic acidosis and DKA)
2) Stop if serum creatinine >150
3) Stop during periods of suspected tissue hypoxia (for example, due to myocardial infarction, sepsis).
Give some examples of SGLT-2 inhibitors
-gliflozin
Empagliflozin, canagliflozin, dapagliflozin and ertugliflozin.
Mechanism of SGLT-2 inhibitors?
1) SGLT-2 inhibitors block action of the sodium-glucose co-transporter 2 protein (found in the proximal tubules of the kidneys).
2) The sodium-glucose co-transporter 2 protein usually acts to reabsorb glucose from the urine back into the blood.
3) By blocking this, more glucose is excreted in the urine.
Can SGLT-2 inhibitors cause hypoglycaemia?
Yes - when used with insulin or sulfonylureas.
When can SGLT-2 inhibitors cause hypoglycaemia?
When used with insulin or sulfonylureas.
Indications for SGLT-2 inhibitors?
1) T2DM:
- monotherapy if metformin inappropriate
- in combination with insulin or other antidiabetic drugs
2) Symptomatic HF (empagliflozin and dapagliflozin)
3) CKD (dapagliflozin)
Impact of SGLT-2 inhibitors on the heart?
Reduce the risk of CVS disease.
Which SGLT-2 inhibitor is licensed for use in CKD?
Dapagliflozin
Which SGLT-2 inhibitor is licensed for use in HF?
Empagliflozin and dapagliflozin
Notable side effects of SGLT-2 inhibitors?
1) Glycosuria (glucose in urine(
2) Increased urine output and frequency
3) Genital and urinary tract infections (e.g., thrush)
4) Weight loss
5) DKA (notably with only moderately raised glucose)
6) Lower-limb amputation may be more common in patients on canagliflozin (unclear if this applies to the others)
7) Fournier’s gangrene (rare but severe infection of the genitals or perineum)
Which diabetic drug can cause DKA?
SGLT-2 inhibitors - patients are counselled about the features of DKA and when to seek emergency medical input.
Which diabetic drug can increase the risk of lower limb amputation?
SGLT-2 inhibitors
Do SGLT-2 inhibitors cause weight gain?
No - cause weight loss
What class of drug is pioglitazone?
A thiazolidinedione
Mechanism of pioglitazone?
1) increases insulin sensitivity
2) decreases liver production of glucose
Does pioglitazone cause hypoglycaemia?
Not typically
Notable side effects of pioglitazone?
1) weight gain
2) fluid retention
3) liver dysfunction
4) increased risk of bone fractures
5) a small increase in the risk of bladder cancer
6) visual impairment
What is the most common sulfonylurea?
Gliclazide
Mechanism of gliclazide?
Sulfonylureas stimulate insulin release from the pancreas.
What are the 2 notable side effects of gliclazide?
1) weight gain and increased appetite
2) hypoglycaemia
What are incretins?
Hormones produced by the GI tract that are secreted in response to a large meal.
Role of incretins?
Act to reduce blood sugar by:
1) Increasing insulin secretion
2) Inhibiting glucagon production
3) Slowing absorption by the gastrointestinal tract
What is the main incretin?
Glucagon-like peptide-1 (GLP-1).
What are incretins inhibited by?
An enzyme called dipeptidyl peptidase-4 (DPP-4).
Role of DPP-4 inhibitors in diabetes?
Block action of DPP-4 (usually inhibits incretin), allowing increased incretin activity (which works to reduce blood glucose).
Give 2 examples of DPP-4 inhibitors
1) sitagliptin
2) alogliptin
What are the 2 notable side effects of DPP-4 inhibitors (-gliptins)?
1) headaches
2) acute pancreatitis
Which diabetic medication can cause acute pancreatitis?
DPP-4 inhibitors e.g. sitagliptin
Role of GLP-1 mimetics in diabetes?
Mimic action of GLP-1 (incretin).
Give 2 examples of GLP-1 mimetics
1) exanatide
2) liraglutide
How are GLP-1 mimetics given?
SC injections
Which GLP-1 mimetic may also be used for weight loss in non-diabetic obese patients?
Liraglutide
What are the notable side effects of GLP-1 mimetics?
1) Reduced appetite
2) Weight loss
3) Gastrointestinal symptoms, including discomfort, nausea and diarrhoea
Give the a) onset, b) peak and c) duration of rapid-acting insulins
a) 5 mins
b) 1 hour
c) 3-5 hours
Give the a) onset, b) peak and c) duration of short-acting insulins
a) 30 mins
b) 3 hours
c) 6-8 hours
Give the a) onset and b) duration of long-acting insulins
a) 1-2 hours
b) up to 24 hours
Give 2 examples of rapid acting insulins
NovoRapid, Humalog
Which diabetic drug is associated with fractures?
Pioglitazone