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Drugs > Endocrinology > Flashcards

Endocrinology Flashcards

1
Q

Name one anti-thyroid drug

A

Carbimazole

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2
Q

What is the mechanism by which carbimazole/anti-thyroid drugs works

A

Pro-drug - converted to thiamazole (aka methimazole)

Methimazole blocks thyroid peroxidase from coupling and iodinating thyrosine residues in thyroglobulin

Reduces levels of T3 and T4

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3
Q

What are the indications for carbimazole/anti-thyroid drugs

A
  1. Hyperthyroidism
  2. Preparatory treatment for thyroidectomy
  3. Pre and post therapy for radio-iodine Tx
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4
Q

What are the CIs for anti-thyroid medication/carbimazole?

A
  • Hypersensitivity
  • Haematological disorders - may cause bone marrow depression
  • Hepatitic insufficiency - may prolong half-life of carbimazole and cause liver damage
  • Stopped temporarily during radio-iodine treatment - may cause thyroid crisis

Intra-thoracic goitre - may cause goitre to expand initially, causing tracheal obstruction

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5
Q

What are the SEs of anti-thyroid medication/carbimazole

A
  • Hypothyroidism
  • Non-specific - fever, headache, abdo disturbance (CONSTIPATION, abdo pain etc)
  • Taste disturbance
  • Jaundice/hepatitis
  • Bone Marrow depression
  • Urticaria/rashes
  • Arthralgia
  • Myopathy
  • Alopecia
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6
Q

What are the potential drug interactions of carbimazole/anti-thyroid medications?

A

Not really known

  • Vit K antagonist - may enhance anticoagulation
  • Increase levels of theopyllines - may cause toxicity
  • Increase drug clearance of some drugs e.g. prednisone
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7
Q

How are anti-thyroid drugs/carbimazole excreted?

A

Renally (90%) and in faeces (10%)

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8
Q

Name the drug that is used in primary/secondary hypothyroidism and in severe hypothyroidism?

A

Levothyroxine - synthetic T4 - long term Tx for hypothyroidism

Liothyronine - synthetic T3 - shorter half life. Tx for severe hypothyroidism

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9
Q

What are the indications for levothyroxine?

A

Primary/secondary Hypothyroidism

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10
Q

What are the CIs for levothyroxine

A
  • Individuals with CHD - increased metabolism and HR may precipitate cardiac ischaemia
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11
Q

What are the SEs for levothyroxine?

A

HYPERTHYROIDISM - GI (diarrhoea, weight loss, anorexia); neuro (insomnia, tremor, restlessness), cardiac - palpitations, arrythmias

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12
Q

What are the potential interactions of levothyroxine?

A
  • Metabolism by CYP450 - increase dose with CYP450 inducers (e.g. carbamezapine, phenytoin)
  • Absorption reduced by anatacids and iron/Ca salts (separate administration by 4hrs)
  • Increased associated metabolism may increase insulin/hypoglycaemic control requirements of diabetics
  • May enhance effects of warfarin
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13
Q

How is levothyroxine eliminated?

A

Renally

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14
Q

Name a biphosphonate

A

Alendronate

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15
Q

What is the mechanism by which alendornate works?

A

Inhibits osteoclasts (inhibition and apoptosis) thereby reducing bone turnover, increase bone mass and reducing Ca in blood

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16
Q

What are the indications for alendronate/biphosphonates

A
  1. 1st line - Patients at risk of osteoperotic fragility #s
  2. Post menopausal women - reduces risk of vert/pelvic/NOF #s
  3. 1st line for Pagets disease -reduce bone turnover and reduces pain
  4. Hypercalcaemia in malignancy
  5. Bone mets (breast/myeloma) - reduces risk of pathological fractures, cord compression and need for radiotherapy/surgery
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17
Q

What are the CIs for alendronate/biphosphonates?

A
  • Hypocalcaemia
  • Renal insufficiency - renally excreted
  • Upper GI irritation - causes oesphagitis
  • Patients with major dental disease and smokers - jaw osteonecrosis
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18
Q

What are the SEs of biphosphonates/alendronate?

A

Oesphagitis

Jaw osteonecrosis

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19
Q

What are the potential interactions for biphosphonates/alendronate?

A
  • Binds calcium - so avoid before food/drugs containing calcium including milk, anatacids and Ca/iron salts
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20
Q

How should biphosphonates/alendronate be taken?

A
  • At least 30 mins before a meal or any medications - poorly absorbed and interacts with calcium containign substances
  • Take upright/standing with a full glass of water - prevent oesphagitis
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21
Q

Name one biguanide

A

Metformin

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22
Q

What is the mechanism by which metformin/biguanides work?

A

Reduces blood glucose and increases insulin sensitivity

Works by reducing liver production of glucose (by gluconeogenesis and glyconeolysis), increasing muscle uptake of glucose and reducing glucose uptake by intestine.

Reduces weight gain and increases weight loss

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23
Q

What are the indications for metformin?

A

Type II DM - either individually or in combo with another hypoglycaemic drugs e.g. sulphonylureas and insulin

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24
Q

What are the SEs of metformin?

A
  • GI upset (could lead to weight loss)
  • Lactic acidosis (inhibits pyruvate dehydrogenase,
    causing lactate accumulation). Caused by:
    - metformin accumulation (kidney impairment)
    - lactate accumulation (severe hypoxia e.g. MI,
    sepsis)
    - Impaired lactate clearance e.g. hepatic
    impairment)
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25
Q

What are the CIs for metformin use?

A
  • Severe kidney impairment (excreted unchanged by the kidney). Withhold in AKI. Reduce in moderate impairment
  • Hepatic failure/impairment - lactate accumulation
  • Severe tissue hypoxia e.g. MI, sepsis - increased lactate
  • Acute alcohol intoxication - could precipitate lactic acidosis
  • Chronic alcohol use - could cause hypoglycaemia
26
Q

What are the potential drug interactions of metformin?

A
  • Withhold for 48hrs after IV contrast due to increased risk of renal impairment
  • Caution when taking with drugs that may impair renal function e.g. ACEi, diuretics, NSAIDs
  • Efficacy of metformin reduced when taken with drugs that increase blood glucose e.g. prednisone, thiazides, loop diuretics
27
Q

How is metformin/biguanides excreted?

A

Renally

28
Q

What is the mechanism by which insulin works?

A
  • Increases tissue uptake of blood glucose - muscle cells, adipose tissue - and increases use of glucose as energy source
  • Increases glycogen, fat and protein synthesis, and inhibits gluconeogenesis breakdown and ketogenesis
  • Drives K+ into cells, reducing hyperkalaemia
29
Q

What are the indications for insulin?

A
  1. Type I diabetes (replace insulin) and type II (blood glucose control when other medications failed)
  2. Hyperkalaemia - before other measures are initiated
  3. IV insulin for diabetic emergencies e.g. ketoacidosis
30
Q

What are the SEs of insulin?

A

Hypoglycaemia

Lipohypertrophy (at injection site)

31
Q

What are the CIs of insulin therapy?

A

Renal impairment - reduces insulin excretion so increases risk of hypoglycaemia

32
Q

What are the drug interactions of insulin?

A
  • Combination with other hypoglycaemic meds increases risk of hypoglycaemia
  • Increase dose with corticosteroids concurrent therapy
33
Q

How is insulin excreted?

A

60% renal, 40% hepatic

34
Q

Name one sulphonylureas

A

Gliclazide

35
Q

What is the mechanism of gliclazide/sulphonylureas?

A

Increases pancreatic secretion of insulin (only works in individuals with functioning B cell function i.e. not type I diabetics!!)

Blocks ATP-ase dependent K channels on B cell membrane. This causes depolarisation and opening of voltage gate Ca channels. Increased intracellular calcium increases pancreatic insulin secretion.

36
Q

What the indications for gliclazide/sulphonylureas?

A

Type II DM - by itself when metformin alone is not tolerated/contraindicated or in combination when blood glucose is not adequately controlled.

37
Q

What are the CIs for gliclazide/sulphonylureas?

A
  • Hepatic impairment - metabolised by the liver so impairment could increase dose, thereby increasig risk of hypo
  • Renal impairment - metabolites excreted by kidneys
  • Cautioned in individuals at risk of hypos e.g. hepatic impairment, malnutrition, elderly, pituritary insufficiency
38
Q

What are the SEs of gliclazide/sulphonylureas?

A

Hypoglycaemia
Can cause weight gain (insulin = anabolic steroid)
GI Upset
Rare hypersensitivity reactions

39
Q

What are the drug interactions of gliclazide/sulphonylureas?

A

Increased risk of hypoglycaemia if given in combo with other blood sugar lowering drugs

Dose increased in blood glucose increasing drugs e.g. prednisone, thiazide, loop diuretics,

40
Q

How is gliclazides excreted?

A

60-70% renal, also in faeces

41
Q

Name one glucopeptide

A

Fludrocortisone

42
Q

What is the mechanism by which fludrocortisone works?

A

Indicated in Addison’s disease where their is mineralocorticoid (aldosterone) insufficiency. Fludrocortisone is used as replacement therapy

43
Q

What are the indications for fludrocortisone?

A
  1. Primary or secondary Addison’s disease - (replacement therapy for mineralcorticoids
  2. Salt-losing adrenogenital syndrome
44
Q

What are are the contraindications for fludrocortisone?

A
  • Hypertension hypernatraemia and hypokalaemia. May increase pressure and causing peripheral oedema
  • Hypersensitivity
  • Immunosuppression - may suppress symptoms and increase susceptibility and severity of infections (e.g. measles/chicken pox) - avoid live vaccine, avoid with associated TB infection.
  • Long term use may cause cataracts, glaucoma and eye infections
45
Q

What are SEs of fludrocortisone?

A
  • Psychiatric - insomnia, nervousness
  • Hypertension - headache, sweating
  • Immunosuppression
  • Electrolyte abnormalities
46
Q

What are the potential interactions of fudrocortisone?

A

Anabolic steroids - increases risk of fudrocortisone SEs.
Barbituates, carbamezapine, eostrogen, phenytoin, rifampin reduces fludrocortisones effectiveness

Life vaccines or smallpox vaccine as their effectiveness of these vaccine is decreased

Anticoagulants - reduced effectiveness or increased risk of side effects

47
Q

Name 3 calcium supplements and 1 vitamin d supplements

A

Calcium - calcium carbonate, calcium gluconate, colecalciferol

Vitamin D- alfacalcidol

48
Q

What is the mechanism by which calcium and vitamin D supplements exert their action

A

Calcium balance - controlled by parathyroid hormone and vit D (increase serum calcium) and calcitonin (reduces serum calcium)

Osteoperosis - reduced bone mass - restores +ve calcium balance

CKD - hyperphosphataemia and hypocalcaemia. Causes 2o hyperparathyroidism and renal osteodystrophy. Calcium and vitamin D supplements Tx and prevent this

Calcium (as calcium gluconide) increases myocyte threshold potential, reducing its excitability and prevents arrythmias

49
Q

What are the indications for calcium (colecalciferol) and vitamin D (alfacalcidol)

A
  1. Osteoperosis - reduces risk of fragility #s
  2. CKD - Tx and prevention of 2o hyperparathyroidism and renal osteodystrophy
  3. Hyperkalaemia - reduces myocyte threshold potential, reducing excitability and rprevents life threatening arrythmias
  4. Hypocalacemia - symptomatic (tetany, seizures, paraesthesia) and seizure

4 Vitamin D deficiency - Tx and prevention of rickets (children) and osteomalacia (adults)

50
Q

What are the contraindications for clacium/vitamin D supplements>

A

Hypercalaemia

51
Q

What are the potential SEs of vitamin D/calcium supplements?

A
  • Dyspepsia and constipation
  • CV collapse if given by IV too quickly
  • Tissue damage if given by subcut accidently
52
Q

What are the possible interactions of vitamin D/calcium supplements?

A
  • reduces absorption of iron, biphosphonates, tetracycline and levothyroxine
  • IV calcium should not be allowed to mix with sodium bicarbonate (can precipitate)
53
Q

Name one type of thiazolidinedione

A

Pioglitazone

54
Q

What is the indications of pioglitazone

A
  1. Single agent in overweight patients where metformin is contraindicated/not tolerated
  2. Added as second agent to metformin or sulphonylurea where blood glucose control = inadequate
  3. Added as third agent with metformin and sulphonylurea where blood glucose is inadequate as an alternative to insulin
55
Q

What in the mechanism by which pioglitazone/thiazolidinediones work?

A
  • Insulin sensitisers - lower blood glucose
  • By enhancing insulin action in skeletal muscle, adipose tissue and liver (increased peripheral glucose uptake and reduce hepatic gluconeogenesis)
  • Do NOT stimulate insulin secretion (do not cause hypos)
56
Q

SEs of thiazlidinediones/pioglitazone

A
  • Weight gain
  • GI upset
  • Anaemia
  • Minor neuro effect - dizziness, headache, disturbed vision

More serious

  • Oedema/Heart failure
  • Increased risk of bladder cancer
  • Increased bone fractures in women
  • Potential liver failure
57
Q

CIs of thiazlidinediones/pioglitazone

A
  • Heart failure/hepatic failure
  • Bladder cancer/those at increased risk e.g. smokers, occupational exposure, prior pelvic irritation
  • Caution in elderly (increased risk of SEs)
58
Q

Drug interactions pioglitazone

A

No sig drug interactions

59
Q

Name 2 DPP4 inhibitors

A

Sitagliptin, Vildagliptin

60
Q

What is the mechanism by which Sitagliptin, Vildagliptin/DPP4 inhibitors work?

A

DPP-4 inhibitors work by blocking the action of DPP-4, an enzyme which metabolises incretin hormone

Incretin:

  • inhibits glucagon release
  • increases insulin secretion
  • decreases gastric emptying
  • decreases blood glucose levels.
61
Q

SEs of DPP4 inhibitors/sitagliptin and vildagliptin

A

SE:

  • Increased risk of pancreatitis -
  • GI problems – DNV
  • flu-like symptoms – headache, runny nose, sore throat
  • skin reactions –red/purple rash

Drugs (9 decks)

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