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Therapeutics > Corticosteroids > Flashcards

Corticosteroids Flashcards

1
Q

Adrenocorticoids

A

Glucocorticoids
Mineralcorticoids

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2
Q

Glucocorticoids

A

Stress hormones
Increase circulating glucose concentrations
Potent anti-inflammatory effects

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3
Q

Mineralocorticoids

A

Na+ retention
Increase blood volume
Increase blood pressure

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4
Q

T/F: Epinephrine and Cortisol contrast each other

A

True

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5
Q

Adrenal insufficiency other name

A

Hypoadrenalism - Decreased secretion of steroid hormones by the adrenal cortex

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6
Q

Adrenal insufficiency causes

A

Destruction of the cortex by tuberculosis or atrophy (primary: Addison’s disease)
-Decreased secretion of ACTH due to diseases of anterior pituitary (secondary; no hypoaldosteronism

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7
Q

Adrenal insufficiency symptoms

A

Extreme weakness
Anorexia, anemia, nausea, vomiting
Low blood pressure (in primary only)
Mental depression

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8
Q

Cessation of long-term systemic glucocorticoid therapy can lead to

A

Addisonian symptoms

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9
Q

Cushing’s disease other name

A

Hyperadrenalism

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10
Q

Cushing’s disease causes

A

Tumors in the adrenal cortex (adrenal)
Increased production of ACTH due to non-pituitary carcinoma (pituitary)
Ectopic production of ACTH due to non-pituitary carcinoma (ectopic)

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11
Q

Cushing’s disease causes

A

Increased protein catabolism (easy bruising, wound healing, muscle wasting) increased glucose levels
Osteoporosis
opportunistic infections

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12
Q

Long-term therapeutic use of systemic glucocorticoids can lead to

A

Cushing’s symptoms

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13
Q

Change of cortisol to cortisone

A

OH on 11 is changed to ketone on 11

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14
Q

T/F: the conversion of cortisol to cortisone is reversible

A

True

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15
Q

T/f: cortisone is effective as cortisol, when used systemically

A

True

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16
Q

T/F: Cortisone should be used in patients with impaired liver function

A

False

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17
Q

Short acting systemic corticosteroids (8-12 hrs)

A

Hydrocortisone
Cortisone

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18
Q

Intermediate acting systemic corticosteroids (12-36hrs)

A

Prednisone
Prednisolone
Methylprednisolone
Traimcinolone

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19
Q

Long-acting systemic corticosteroids (36-54 hrs)

A

Dexamethasone
Betamethasone

20
Q

Fludrocortisone

A

Synthetic glucocorticoid
9a-F
Greater glucocorticoid activity
Strong mineralocorticoid activity
Intense Na+ retention leading to edema
Used in mineralocorticoid replacement therapy
(ADDITION OF F)
(intermediate)

21
Q

Prednisone/Prednisolone

A

Synthetic Glucocorticoids
Extra double bond between CI and C2
Altered ring structure
More potent glucocorticoid activity
Stronger binding to the glucocorticoid receptor
Reduced mineralocorticoid activity
Interconvertible by 11B hydroxysteroid dehydrogenase
(DOUBLE BOND ON THE TOP OF FIRST RING)
(intermediate)

22
Q

Methylprednisolone

A

Synthetic glucocorticoids
6a-methyl group
Potency similar to that for prednisolone
Reduced mineralocorticoid activity
(ADDITION OF METHYL ON CARBON 6)
(Intermediate)

23
Q

Triamcinolone

A

Synthetic glucocorticoids
9a-F and 16a-OH
Glucocorticoid activity similar to prednisone
Reduced mineralocorticoid activity
Increased hydrophilicity
Low oral bioavailability
(F AND OH)
(intermediate acting)

24
Q

Dexamethasone

A

16a-methyl group
Increased lipophilicity
Increased receptor binding
Significantly stronger effect
Increased stability in human plasma
Reduced mineralocorticoid activity
(Long duration)

25
Q

Betamethasone

A

Synthetic glucocorticoid
Enantiomer of dexamethasone at 16
Has similar properties as dexamethasone
(Long duration)

26
Q

21 esters properties

A

The hydroxyl group at 21 can be modified to an ester to control the property of glucocorticoids
Prodrugs activated through hydrolysis by esterases

27
Q

21 esters: Acetates

A

Acetate:
Increased lipophilicity
Prolonged action upon IM or intra-articular injection

28
Q

21 esters: Succinate

A

Soluble
Slow hydrolysis

29
Q

21 esters: Phosphate

A

Increased solubility
Rapid hydrolysis by phosphatases (~10 min)
IV or IM injection for emergency conditions

30
Q

Inhaled Glucocorticoids: Desired properties

A

High potency
Minimal systemic effects
Prolonged action

31
Q

Inhaled glucocorticoids: Solutions

A

High lipophilicity
Tighter binding to the receptor
Better tissue penetration
Prolonged action by forming poorly soluble microcrystals
Low oral bioavailability
70-90% of inhaled glucocorticoids is swallowed
Rapid
Short half-life

32
Q

Triamcinolone acetonide

A

Inhaled glucocorticoid:
Acetonide is resistant hydrolysis
8x more potent than prednisolone
(ADDITION OF STICKS)

33
Q

Beclomethasone dipropionate

A

Converted rapidly to 17-monopropionate by hydrolysis
14x more potent than deamethasone

34
Q

Flunisolide

A

Inhaled glucocorticoids
Rapid absorption from nasal or lung tissue
Rapid metabolism by the liver
Extensive first-path metabolism
Minimal systemic adverse effect with long-term therapy

35
Q

Budesonide

A

Inhaled Glucocorticoids
1:1 mix of epimers at 16,17-butylacetal
Faster topical uptake
Low oral bioavailability
Extensive first-path metabolism

36
Q

Mometasone furoate

A

Inhaled glucocorticoids
Highly potent
More rapid onset of action
Negligible systemic availability
Rapid metabolism
low oral bioavailability (<1%)

37
Q

Fluticasone Propionate

A

Inhaled Glucocorticoids
Inactivated by hydrolysis of thioester
Rapid first-path metabolism
Highly lipophilic and insoluble
Highly potent
Poor absorption from GI
Rapid topical uptake

38
Q

Topical Glucocorticoids desired properties

A

High lipophilicity for fast absorption
Minimal systemic effect
Prolonged action

39
Q

T/F: Topical Glucocorticoids are Halogenated analogues

A

True

40
Q

Topical Glucocorticoids examples

A

Triamcinolone acetonide
Fluocinonide
Betamethasone valerate (medium potency)
Acetonide or ester forms have better potency for topical applications due to high lipophilicity

41
Q

21-cholorocorticoids

A

Clobetasol propionate
Halobetasol propionate
Halcinonide
Substitution of a chlorine atom for the 21-hydroxyl group greatly enhances topical anti-inflammatory activity

42
Q

Fluticasone propionate and mometasone furoate have - potency

A

Medium, high lipophilicity and the highest binding affinity, but poor solubility
Poor dissolution into inflamed tissue

43
Q

Adverse effects of glucocorticoids: crossover mineralocorticoids activity

A

Sodium and water retention
Development of HTN
Correctable with selective synthetic glucocorticoids

44
Q

Adverse effects of glucocorticoids: Metabolic effects (increased glucose production):

A

Steroid myopathy
High doses over period of time cause wasting of proximal muscles
Reduced long bone growth in children
May cause premature closing of epiphyseal junction and stop growth
Osteoporosis
Pharmacological doses of glucocorticoids inhibit osteoblasts
can be prevented by bisphosphonate

45
Q

Adverse effects of glucocorticoids:

A

Cushing’s-like effects - redistribution of fat
-Moon face

Therapeutics (61 decks)

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