Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
28 Cards in this Set
- Front
- Back
|
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
|
