Endocrine Flashcards
Name 3 examples of systemic cortiosteroids and 3 indications for their use:
- prednisolone, hydrocortisone, dexamethasone
- to treat allergic or inflamm disorders (anaphylaxis, asthma)
- supress autoimmune disease e.g. IBD, arthritis
- to treat some cancers (as part of chemo/to reduces tumour swelling)
- hormone replacement in Adrenal insufficiency or hypopituitarism
Corticosteroids MOA..bind to ____ receptors which ___ to the ___ and bind to _____-response elements that regulate ____ expression. They upregulate ___-_____ ___ and down-regulate ___-_____ ___.
They also suppress circulating ___ and __.
Metabolic effects include increased ____ from increased circulating amino and fatty acids released by catabolism of __ and fat.
Also have ______ effects, stimulating Na+ and water ___ and K+ ___ in the renal tubule
- glucocorticoid receptors –> translocate to nucleus, bind to glucocorticoid-REs
- regulate gene expression, upreg anti-inflamm genes, downreg. pro-inflamm genes
- supress circulating monocytes and eosinophils
- increased gluconeogenesis (from catabolism of muscle and fat)
- mineralocorticoid effect, Na+/water retention and K+ excretion
Name 8 important adverse effects that may arise from systemic corticosteroid therapy
(think about MOA to remember these)
- immunosuppression
- metabolic effects: DM, osteoporosis
- increased catabolism: proximal muscle weakness, skin thinning, easy bruising, gastritis
- mood/behaviour: insomnia, confusion, psychosis, suicidal ideation
- mineralocorticoid effects: HT, hypokalaemia, oedema
- adrenal atrophy in prolonged rx (–> addisonian crisis on sudden withdrawal..fatigue, weight loss, arthralgia)
What 2 medication classes should be considered alongside long-term systemic corticosteroid therapy to reduce adverse effects?
- bisphosphonates
- PPIs
When should you exercise caution in prescribing systemic corticosteroids?
- people with an infection
- children (can supress growth)
corticosteroids increase the risk of peptic ulcers/GI bleeding when used with ____
and enhance hypokalaemia when used in pts also taking __-agonists, th____, ___ or ___ diuretics.
Efficacy can be reduced by cytochrome P450 inducers such as….
- NSAIDS
- B2 agonists, theophylline, loop or thiazide
- rifampicin, phenytoin, carbamazepine
In a pt undergoing long-term systemic corticosteroid therapy who becomes acutely ill, what should you do with their dose while unwell and then once recovered?
(atrophic adrenal glands won’t be able to increase cortisol in response to stress - do this artificially)
- double the dose during acute illness
- reduce back to maintenance dose on recovery
Dipeptidyl peptidase 4 inhibitors are used in combo w Metformin for T2DM. What is the suffix for this class and by what mechanism to they exert their effects?
__gliptin e.g. sitagliptin, linagliptin
- incretins (GLP1 and GIP) are rapidly inactivated/hydrolysed by DDP-4
- inhibitors of this enzyme increase plasma conc of active incretins
- incretins promote insulin secretion and suppress glucagon release so lower BM
DPP-4 inhibitors e.g. sitagliptin, main SEs include:
-and <1 % develop acute _____ (suspect if persistent ___ pain)
SEs: GI upset, headache, nasopharyngitis, peripheral oedema
-<1%: acute pancreatitis, persistent abdo pain
Give 3 CIs for the use of DPP-4 inhibitors e.g. sitagliptin
NB: caution in elderly, those w pancreatitis hx or renal impairment
- CI: HISTORY OF HYPERSENSITIVITY TO CLASS
- CI: TYPE 1 DIABETES TREATMENT
- CI: KETOACIDOSIS
- CI: PREGNANCY
- CI: BREAST FEEDING
DPP-4 inhibitors e.g. sitagliptin efficacy and use is done via HbA1 results:
-if used as monotherapy target HbA1c is
- aim <48 mmol if monotherapy
- <53 mmol if with metformin
- if remains >58 mmol add on
Name 3 effects insulin has on processes:
- stimulates glucose uptake
- stimulates glycogen, lipid and protein synthesis
- inhibits gluconeogenesis and ketogenesis
- drives K+ into cells
Suggest one serious SE of insulin rx and one more cosmetic SE
- HYPOGLYCAEMIA (can -> coma/death), higher risk in renal impairment (less clearance)
- lipohypertrophy at site of repeated injection
Concurrent insulin use with other hypoglycaemic agents increases risk of hypoglycaemia. Concurrent use with what common drug class requires insulin doses to be increased?
-concurrent corticosteroid use
Metformin is a biguanide that lowers blood glucose mainly by reducing what? as well as what effect on muscle?
- reduces hepatic glucose output (glycogenolysis and gluconeogenesis)
- increased glucose uptake and use by skeletal muscle
Can monotherapy with metformin cause hypoglycaemia ?
NB: metformin can cause weight loss
-Nope
Suggest a common SEs of metformin use?
- GI upset: nausea, vomiting, taste disturbance, anorexia, diarrhoea
- rarely lactic acidosis
What organ excretes metformin
-kidney
if eGFR is
- <30mL/min
- stop in AKI
- stop if severe tissue hypoxia (e.g. sepsis, cardio/resp failure, MI)
Due to risk of hypoglycaemia, metformin should be withheld in acute ____ _____ and used caution in patients with chronic ____ ____
- acute alcohol intoxication
- chronic alcohol abuse
Metformin must be withheld before and for 48hrs after injection of what and why?
- IV contrast media
- as increased risk of renal impairment, metformin accumulation and lactic acidosis
Metformin and GI SEs when starting, how is best to manage?
- start on a low dose, increase gradually e.g. 500mg once daily
- swallow tablets whole with a glass of water, with or after food to minimise SEs
Metformin efficacy is assessed via HbA1 results:
- if used as monotherapy target HbA1c is < ____
- if used in combo with other drugs, target is ____ triggers an add on therapy
- aim <48 mmol if monotherapy
- <53 mmol if used in combo
- if remains >58 mmol add on
What blood test should be measured before starting Metformin? And repeated at least annuallly?
-U&Es to check renal function
if RF or deteriorating kidney function, repeat more regularly
