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28 Cards in this Set

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Corticosteroids bind to what?
Glucocorticoid or mineralocorticoid receptors
What does the steroid-receptor complex do?
Regulate gene transcription.
What structural criteria must be met for glucocorticoid activity?
1. Ketone at C3
2. Double bond btw C4 and C5
Small modification in the basic corticosteroid structure alter what? x5
1. Drug half-life
2. Carb. potency
3. Anti-inflammatory potency
4. Sodium retaining potency
5. Transcortin binding
Give example of clinical modification of a corticosteroid on position 9.
Fluoride at C9 will increase potency
Give example of clinical modification of a corticosteroid on position 16.
Methyl group on C16 will increase anti-inflammatory AND decrease sodium retention
What has VERY HIGH glucocorticoid potencies?
Betamethasone
Dexamethasone
Triamcinolone
What has HIGH glucocorticoid potencies?
Prednisone
Methylprednisone
What has VERY LOW glucocorticoid potencies?
Fludrocortisone
What has VERY HIGH mineralocorticoid potencies?
Fludrocortisone
What has LOW mineralocorticoid potencies?
Prednisone
Methylprednisone
What has VERY LOW mineralocorticoid potencies?
Betamethasone
Dexamethasone
Triamcinolone
From clinical standpoint, what do you want?
High anti-inflammatory (glucocorticoid potency) and low sodium-retaining (mineralocorticoid potency)
What are some systemic routes of administration and when do you use each?
Oral - Long term therapy

IM/IV - Emergency
What are some local routes of administration and when do you use these?
Topical (eyes/skin)
Intra-articular (arthritic joints)
Nose spray (rhinitis)
Inhalation (asthma)
Corticosteroid metabolism occurs where?
liver
What are the steps in steroid metabolism?
Reduction of double bond at 4 and 5 (making it inactive)

Conjugation of inactive metabolite.

Excretion
What affects steroid metabolism?
Liver disease - won't be able to readily convert it into active form
Name short acting (8-12 hrs) corticosteroids.
cortisone
hydrocortisone
Name long acting (36-54 hrs) corticosteroids.
betamethasone
dexamethasone
Name intermediate acting (12-36 hrs) corticosteroids.
Triamcinolone
methylprednisone
Prednisone
Prednisolone
Fludrocortisone
General considerations for toxicity and/or side effects.
Route of administration(systemic vs. local)

Dosage

Length of therapy
Side effects of short term systemic.
No serious side effects
Side effects of long term systemic
a. Cushingoid features (fat redistribution)

b. sodium retention (edema, heart failure, hypertension)

c. potassium loss (muscle weakness)

d. glucose intolerance (glycosuria/overt diabetes mellitus)

e. weight gain

f. loss of skin collagen

g. osteoporosis*

h. peptic ulcers

i. HPA axis suppression

j. CNS effects (psychosis, insomnia, nervousness, euphoria, depression)

k. susceptibility to infection

l. triamcinolone-weight loss and sedation

m. masking of symptoms of other diseases
Local use of steroids
Topical

Inhaled

Nasal
When would you use inhaled steroids?
Candidal infection of mouth

Throat irritation

Dysphonia
When would you use nasal steroids?
HA

Nasal irritation

Dry Nose

Nosebleed
When would you use topical steroids?
Epidermal atrophy