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Pharm II Unit III > 4 Glucocorticoids > Flashcards

4 Glucocorticoids Flashcards

1
Q

What is the one mineralocorticoid?

A

Fludrocortisone

Mimics aldosterone - has mineralocorticoid and SOME glucocortiocoid activity

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2
Q

Drug used to treat adrenal insufficiency if you cannot get sufficient water and salt retention with glucocortiocoids alone

A

Fludrocortison

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3
Q

What is the major endogenous corticosteroid?

A

Cortisol

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4
Q

What is the synthetic form of cortisol?

A

Hydrocortisone

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5
Q

How does cortisol circulate in plasma?

A

Bound to cortisol binding protein

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6
Q

Why are most actions of cortisol slow onset and long acting?

A

Circulates bound to protein

Binds to cytoplasmic receptor —> stimulates gene transcription (slow process)

BUT it DOES have SOME rapid actions

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7
Q

Which effects of cortisol are RAPID?

A

Anti-inflammatory

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8
Q

Effect of glucocorticoids on carbs, proteins, and fats

A

Increases circulating levels of GLUCOSE, free fatty acids, and AAs

ANTAGONIZES insulin —> reduced uptake of glucose by muscles —> HYPERGLYCEMIA

Redistribution of body fat (extremities —> central)

Breakdown of muscle for use by liver (muscle atrophy)

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9
Q

CV effects of glucocorticoids

A

Increased vascular responsiveness to SYMPATHETIC stimulation (That’s why it’s great for ASTHMA)

Some Na+ and H20 retention

Increased CO (incr blood volume —> incr preload —> incr stroke volume) —> increased catecholamine effect

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10
Q

Normal range of cortisol to aldosterone like effects of corticosteroids?

A

200:1

Synthetic versions have increased ratio (minimize aldosterone effects)

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11
Q

Endocrine effects of glucocorticoids

A

Suppresses other hormone systems due to direct negative feedback on hypothalamus (CRH —> dec ACTH)

Inhibits action of vitamin D —> dec Ca2+ deposition
Increased PTH —> inc Ca2+ loss form bone

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12
Q

Why are the endocrine effects of glucocorticoids a big deal for long term use?

A

Inhibited Vit D and increased PTH —> bone loss

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13
Q

What are the immune system effects of glucocorticoids?

A

Immunosuppression with CHRONIC treatment

Blocks all steps in inflammation (RAPID effect)
• Reduces PLA2, COX2, Cytokines, IgE responses

Suppression of wound healing

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14
Q

CNS effects of glucocorticoids

A

Acute - occur rapidly!

Mood elevation
Insomnia, restlessness
Anxiety
Depression
Psychosis
Increased appetite
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15
Q

Cushing’s syndrome is due to …

A

Glucocorticoid excess

If ACTH excess if the reason - pituitary tumor

If cortisol excess is the reason - adrenal tumor or excess exogenous glucocorticoids

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16
Q

Lack of cortisol is a disease called…

A

Addison’s

Can be due to adrenal malfunction or pituitary malfunction

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17
Q

How is Cushing’s diagnosed

A

Dexamethasone suppression test

Measure baseline cortisol level in AM, administer dexamethasone in PM, measure again the following morning

Abnormal result = cortisol levels ≥50% suppressed (normally would cause extreme suppression of cortisol)

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18
Q

What is an Addisonian crisis?

A

Acute adrenal insufficiency

Must be treated immediately with corticosteroids to avoid circulatory collapse, dehydration, vomiting, hyperkalemia, DEATH

19
Q

Hydrocortisone works as both ______ and ______, while newer synthetics only have _______ effects.

A

Replacement and weak anti-inflammatory

Anti-inflammatory only

20
Q

Hydrocortisone and cortisone both have equal parts…

A

Mineralocorticoid and glucocorticoid properties

21
Q

What is the relationship between hydrocortisone/cortisone?

A

Cortisone must first be converted to hydrocortisone in the liver in order to be active - it therefore has slightly lower potency than hydrocortisone

22
Q

What is the main indication for the use of hydrocortisone?

A

Replacement therapy for adrenal insuffiency

23
Q

Prednisone and Prednisolone have more ______ effect than ______

A

Glucocorticoid > mineralocorticoid

Most commonly prescribed oral glucocorticoid

24
Q

Prednisone must first be converted to ______ in the liver in order to be active

A

Prednisolone

You therefore would want to use Prednisolone in someone who has poor liver function

25
Q

Triamcinolone (Kenalog) and Methylprednisolone (Medrol) have _______ mineralocorticoid effect

A

Virtually no

True of most newer glucocorticoids

Good for acute asthma exacerbations

26
Q

What are the different possible formations for glucocorticoids?

A

Oral for long term therapy

Injections for emergencies or depot administration

Inhaled/nasal for asthma and rhinitis

Topical

27
Q

Why do topical glucocorticoids cause skin atrophy?

A

Repeated application —> depot effect

28
Q

What happens when you are on chronic glucocorticoids and you have a stressful event/time period?

A

You must use increased amounts

2x for minor stress
Up to 10x for major stress

If not —> acute insufficiency —> life threatening

29
Q

Conditions other than adrenal insufficiency that can be treated with glucocorticoids

A

RA (decreases inflammation —> reduced pain, inc function)

Asthma - inhaled = first line treatment (inconjunction with B2 agonist)

Intranasal for rhinitis

30
Q

Therapeutic guidelines for glucocorticoid use

A

Use only as long as necessary and at the lowest effective dose

Start high and slowly taper once inflammation under control

Use LOCALLY whenever possible

Give on alternate days to avoid suppression of HPA axis

31
Q

Is short term glucocorticoid therapy likely to cause serious problems?

A

NOPE - 1-2 weeks will be just fine

32
Q

How do glucocorticoids adversely effect infections?

A

May mask symptoms

More susceptible to serious infections

But sometimes used in infection to reduce inflammation

33
Q

Adverse effect of glucocorticoids on hyperglycemia

A

May unmask diabetes in some patients

34
Q

CNS effects of glucocorticoids can occur even with ______

A

Acute treatment

Restlessness, insomnia, psychoses, increased appetite

35
Q

Adverse effect of glucocorticoids on the bones

A

Can cause Osteoporosis*** Most damaging and therapeutically limiting effect

Function of duration and dose

Treatments include Ca2+, Vit D, bisphosphonates

36
Q

Why do you have to taper glucocorticoids

A

> 1-2 weeks of high dose therapy suppresses HPA —> abrupt drug cessation can cause ACUTE ADRENAL INSUFFIENCY

Stress can also cause acute adrenal crisis in chronic patients

37
Q

Are there any contraindications for use of glucocorticoids in adrenal insufficiency

A

NO - THEY’LL DIE IF YOU DON’T TREAT THEM

38
Q

C/I for glucocorticoid use

A

NONE in adrenal insufficiency

Systemic bacterial or viral infection
Poorly controlled diabetes
Osteoporosis or other advanced bone disease
Heart disease or HTN with CHF
Immunosuppressive patients
Childhood
Pregnancy (unless using it to mature lungs prior to premature delivery)

39
Q

How does Ketoconazole work as a corticosteroid antagonist

A

Antifungal that inhibits steroid synthesis at very high doses

NON-SELECTIVE - will also suppress androgen synthesis

Used for PREOP suppression - one of the first line drugs for Cushing’s before surgery

40
Q

MOA for Mitotane

A

Adrenocorticolytic - causes adrenocortical atrophy

Used in primary adrenal carcinoma when surgery/radiation not feasible (not first line)

Causes severe GI distress

41
Q

MOA for Metyrapone (Metopirone)

A

Selective inhibitor of the terminal enzyme in cortisol synthesis - doesn’t effect other steroid production

Short term use while causes of Cushing’s being determined

Less toxic than Mitotane

42
Q

Only corticosteroid synthesis inhibitor that can be given in pregnancy

A

Metyrapone (Metopirone)

Because it doesn’t inhibit sex hormone synthesis

43
Q

What are the two receptor antagonists we discussed?

A

Glucocorticoid receptor antagonist = MIFEPRISTONE
• For inoperable Cushing’s patients
• Induces abortions (b/c inhibits progesterone receptors)

Mineralocorticoid receptor antagonist = SPIRONOLACTONE
• Potassium sparing diuretic —> can cause hyperkalemia
• Used for hyperaldosteronism and hirsutism

Pharm II Unit III (4 decks)

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