Endocrine Drugs Flashcards
What are 2 examples of Sulphonylureas?
Gliclazide
Glimepiride
What is the MoA of sulphonylureas?
Stimulates B cells of the pancreas to produce more insulin
Increase cellular glucose uptake and glycogenesis; reduces gluconeogenesis
Glicazide is short acting (12 hours approx)
what are the indications for sulphonyulereas?
T2DM with diet and exercise
list some side effects of sulphonyuleras?
Hypoglycaemia Rashes Nausea Vomiting Stomach pain Indigestion Weight gain
What is important clinically regarding pharmacokinetics/dynamics for sulphonyulereas?
Renally excreted so accumulate in renal failure
Glimepiride is long acting sulphonylureas
What info should be given to patient before starting a sulphonyulerea?
Compliance important
Maintain consistent diet
Avoid alcohol
What is an example of a biguanide?
Metformin
what is the MoA of metformin?
Increase the activity of AMP-dependent protein kinase (AMPK)
This inhibits gluconeogenesis
Reduces insulin resistance
What are the indications for a biguanide?
Type 2 diabetes mellitus along with diet and exercise
Metabolic and reproductive abnormalities associated with Polycystic ovarian syndrome
List some side effects of metformin:
Diarrhoea Nausea Vomiting Taste disturbances Lack of apetite Risk of lactic acidosis in patients with renal failure
What is important clinically regarding pharmacokinetics/dynamics for metformin?
Not recommended in pregnancy and renal failure (eGFR <30 mls/min)
Absorption reduces when taken with food
What info should be given to patient before starting metformin?
take at same time every day
avoid alcohol
What is metformin’s affect on weight?
It does not increase weight (may loose some due to side effects)
What are 2 examples of GLP-1 (glucagon like peptide) Agonists?
Exanatide
Liraglutide
What is the MoA for a GLP-1 Agonist?
GLP-1 is a hormone that is released after meals to increase insulin secretion
These drugs are a GLP-1 agonist - it increases insulin secretion, decreases glucagon secretion and reduces hunger
what is the indication for GLP-1 agonists?
T2DM
list some side effects of GLP-1 agonists:
Hypoglycaemia
Nausea
Vomiting
Diarrhoea
What is important clinically regarding pharmacokinetics/dynamics for exanatide and liraglutide?
It can lower glucose alone, but when given in combination with metformin, sulfonylureas, and/or insulin it can improve glucose control
Renally excreted so dose adjustment needed in renal failure
What info should be given to patient before starting a GLP-1 agonist?
Only given as injections
Twice a day
what is the synthetic thyroid hormone drug called?
levothyroxine
what is the MoA for levothyroxine?
Thyroxine increases the metabolic rate of all tissues in the body
Synthetically prepared levo-isomer of thyroxine
Acts like T4 and gets converted to T3 in the liver and kidney
Maintain brain function, food metabolism, and body temperature, among other effects
what are the indications for synthetic thyroid hormone?
Hypothyroidism
Chronic lymphocytic thyroiditis
list some side effects of levothyroxine
Chest pain Coma Diarrhoea Tachycardia Itching Muscle cramps (shouldn't happen if dose is correct)
What is important clinically regarding pharmacokinetics/dynamics for levothyroxine?
Primarily eliminated by the kidneys
Intravenous formulations are available
The half-life is long (6 to 7 days) so thyroid function should be rechecked 6 weeks after a dose adjustment
what info should be given to patient before starting levothyroxine?
Take 30-60 minutes before breakfast.
what are 2 examples of anti-thyroid drugs - thionamides?
Carbimazole
Propylthiouracil
what is the MoA of thionamides?
Reduces activity of peroxidase enzyme (required for the production of thyroid hormones)
May also reduce peripheral conversion of T4 to T3
Carbimazole is a pro-drug
what are the indications for carbimazole and propylthiouracil?
Hyperthyroidism
Thyrotoxicosis
Preparing patients for thyroid surgery
list some side effects of thionamides:
rash
agranulocytosis
sore throat
What is important clinically regarding pharmacokinetics/dynamics for thionamides?
Carbimazole is rapidly metabolised to thiamazole. The mean peak plasma concentration occurs one hour
It crosses the placenta and can be found in breast milk
The effect of anti-thyroid drugs can take several weeks to occur so are usually prescribed alongside a beta-blocker to reduce symptoms of hyperthyroidism
what info should be given to patient before starting a thionamide?
Compliance is important
Regular blood checks will be needed to monitor treatment response and renal, hepatic function and full blood counts.
