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Therapeutics > Lecture 17: Corticosteroid drugs > Flashcards

Lecture 17: Corticosteroid drugs Flashcards

1
Q

Therapuetic use of corticosteroids

A

-primary adrenal insufficiency
-allergic reactions
-inflammation/autoimmune diseases
-asthma
-anti-cancer

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2
Q

Allergic reactions treated by corticosteroids

A

-insect stings
-angioedema

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3
Q

inflammation and autoimmune diseases treated by corticosteroids

A

-burstitits, synovitis, tendonitis
-rheumatoid arthritis
-lupus
-IBS
-chronic hepatitis

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4
Q

Cortisol

A

-active form
-11 hydroxyl

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5
Q

Cortisone

A

-inactive form
-11 hydroxyl oxidized to ketone
-effective as cortisol
-do not give to patients with impaired livers

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6
Q

11 B-hydroxysteroid dehydrogenase

A

-catalyzes oxidation of cortisol to cortisone
-reversible reaction
-in liver

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7
Q

Short acting corticosteroids (8-12hr)

A

-hydrocortisone
-cortisone

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8
Q

intermediate acting corticosteroids (12-36hr)

A

-prednisone
-prednisolone
-methylprednisolone
-triamcinolone

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9
Q

long-acting corticosteroids (36-54hr)

A

-dexamethasone
-betamethasone

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10
Q

Synthetic glucocorticoids

A

-fludrocortisone
-prednisone/prednisolone
-methylprednisone
-triamcinolone
-dexamethasone
-betamethasone

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11
Q

Fludrocortisone

A

-a-Florine at C-9
-greater glucocorticoid activity
-strong mineralcorticoid activity
-intense Na+ retention that leads to edema
-used in MC therapy

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12
Q

Prednisone/Prednisolone

A

-double bond between C1 and C2
-more GC activity
-reduced MC activity
-interconvertable by 11B-hydroxysteroid dehydrogenase

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13
Q

11B-hydroxysteroid dehydrogenase

A

-converts prednisone to prednisolone and vice versa
-11B OH to =O

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14
Q

Methylprednisolone

A

-6a-methyl group
-similar potency to prednisolone
-reduced MC activity

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15
Q

Triamcinolone

A

-9a-F and 16a-OH
-similar to prednisone
-reduced MC activity
-inc hydroPHILIcity
-low oral bioavailability

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16
Q

Dexamethasone

A

-16a-methyl group
-inc lipoHILIcity = inc binding = stronger effect
-inc stability in plasma
-reduced MC activity

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17
Q

Betamethasone

A

-enantiomer of dexamethasone at C-16
-similar properties

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18
Q

21-esters

A

-21-hydroxyl group modified to ester
-prodrugs activated by hydrolysis by esterases

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19
Q

21-ester groups

A

-acetate or butyrate
-succinate
-phosphate

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20
Q

21- acetate or butyrate

A

-inc lipoPHIlicity
-prolonged action upon IM or articular injection

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21
Q

21- Succinate group

A

-soluble
-slow hydrolysis (30-45min)

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22
Q

21- phosphate group

A

-inc solubility
-rapid hydrolysis by phosphatases (10min)
-IV or IM injection for emergency conditions

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23
Q

1,2 double bond SAR

A

-inc GR to MR ratio by 5x

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24
Q

11 B-OH SAR

A

-required for GR/MR activity
-more important for GR

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25
Q

21-OH, F, Cl SAR

A

-required for activity
-ester prodrug must be hydrolyzed to OH for max activity

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26
Q

17a-O SAR

A

-required for GR activity

27
Q

16-O or B-CH3 SAR

A

-dec MR activity

28
Q

9a-F or Cl SAR

A

-enhances GR and MR potency

29
Q

6a-CH3 or F SAR

A

-enhances GR to MR ratio

30
Q

Mech of glucocorticoid action in asthma

A

-will NOT stop attack while happening
-inhibit airway inflammation
-use prophylactically

31
Q

GC effect on airway

A

-do not relax any muscle
-mod cytokine and chemokine production
-inhibit eicosanoid synthesis
-inhibit accumulation of immune cells in lung
-dec vascular permeability

32
Q

inhaled gc

A

-use prophylactically
-treat astma
-max effects seen after weeks
-compliance is concern

33
Q

Desired properties of inhaled GCs

A

-high potency
-minimal systemic affects
-prolonged action

34
Q

inhaled GC solutions

A

-high lipophilicity
-low oral bioavailability (most is swallowed)
-rapid clearance

35
Q

high lipophilicity effect

A

-tighter binding
-better penetration
-prolonged action by forming microcrystals

36
Q

inhaled GC drugs

A

-triamcinolone acetonide
-beclomethasone dipropionate
-Flunisolide
-Budesonide
-mometasone furoate
-fluticasone propionate

37
Q

Triamcinolone acetonide

A

-inhaled GC
-resistant to hydrolysis
-8x more potent than prednisolone

38
Q

Beclomethasone dipropionate

A

-inhaled GC
-converted rapidly to monopropionate by hydrolysis
-14x more potent than dexamethasone

39
Q

Flunisolide

A

-inhaled GC
-rapid absorption
-rapid metabolism (first-pass)
-minimal adverse effect with long-term therapy

40
Q

Budesonide

A

-inhaled GC
-mixture of epimers at 16,17 butylacetal
-faster topical uptake
-low oral availability
-extensive FP metabolism

41
Q

Mometasone furoate

A

-inhaled GC
-highly potent
-more rapid onset
-negligible availability (rapid metabolism and low oral bioavailability)

42
Q

Fluticasone propionate

A

-inactivated by hydrolysis of thioester (FP metabolism)
-highly lipoPHILIC
-INsoluble
-high potent
-poor absorption from GI
-rapid topical uptake

43
Q

Desired properties of topical GCs

A

-high lipophilicity for fast absorption
-minimal systemic effect
-prolonged action

44
Q

Topical GC metabolism

A

-absorbed thru skin
-metabolized in liver
-excreted to urine or bile

45
Q

low potency topical GCs

A

-safest for chronic application
-hydrocortisone cream

46
Q

topical GCs with high potency

A

-risk systemic exposure
-should be used only for short duration of treament

47
Q

Halogenated analogues

A

-usually potent topical GCs

48
Q

Topical GC forms

A

-acetonide/ester forms
-21-chlorocorticoids
-9a

49
Q

Acetonide/ester topical GCs

A

-better potency bc high lipophilicity

-triamcinolone acetonide
-fluocinonide
-betamethasone valerate

50
Q

21-chlorocorticoids

A

-sub 21-OH with Cl
-very high potency
-topical anti-inflammatory

51
Q

Fluticasone propionate and mometasone furoare

A

-topical GCs
-medium potency
-high lipophilicity but poor solubility
-poor dissolution into inflamed tissue

52
Q

Adverse effects of GCs

A

-crossover MC activity
-metabolic effects
-Cushing’s-like effects
-impaired glucose tolerance
-immunosuppression
-ulcer risk
-CNS effects
-cataracts
-addisonian crisis

53
Q

Adverse effect of GC crossover MC activity

A

-Na+ and water retention
-HTN
-correctable with selective GCs

54
Q

Metabolic adverse effects of GC

A

-steroid myopathy
-reduce bone growth in kids
-osteoporosis

55
Q

steroid myopathy

A

-high doses over time cause wasting of proximal muscles

56
Q

Osteoporosis caused by GCs

A

-inhibit osteoblasts
-can be prevented by bisphosphonate

57
Q

Cushing’s like effects

A

-redistribution of fat
-moon face
-buffalo hump

58
Q

Impaired glucose tolerance form GCs

A

-HYPERglycemia from gluconeogenesis
-dec insulin response (only diabetes)

59
Q

Adverse effects of immunosuppression by GCs

A

-inc susceptibility
-impaired healing

60
Q

adverse effects of GCs on CNS

A

-linked to glucose metabolism
-euphoria
-depression

61
Q

Addisonian crisis

A

-adrenal insufficiency upon GC withdrawal
-delay recovery of hypothalmus and pituitary
-dec ACTH release and response to ACTH
-related to dose and duration of therapy

62
Q

Addisonian crisis cause

A

-negative feedback on hypothalmus and pituitary from prolonged doses of GCs

63
Q

Symptoms of Addisonian crisis

A

-inability to withstand stress
-HYPOtension
-weakness

Therapeutics (78 decks)

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