Steroid 2 Flashcards
What are the two main classes of adrenocorticoids?
- Glucocorticoids (hydrocortisone)
- Mineralocorticoids (aldosterone)
These classes are involved in CHO, lipid, and protein biosynthesis as well as water and electrolyte balance.
What are the main therapeutic effects of glucocorticoids?
Metabolism + anti-inflammatory effects
Glucocorticoids play a crucial role in managing inflammation and metabolic processes.
What are the pharmacokinetic modifications for glucocorticoids?
- Water solubility
- Lipid solubility
- Absorption and distribution
Modifications affect how glucocorticoids are processed in the body.
What are the pharmacodynamic modifications for glucocorticoids?
- Potency
- Side effects
These modifications influence the effectiveness and adverse effects of glucocorticoids.
List the categories of glucocorticoids based on their duration of action.
- Short-acting glucocorticoids (hydrocortisone & cortisone)
- Intermediate-acting glucocorticoids (prednisone, prednisolone, methylprednisolone & triamcinolone)
- Long-acting glucocorticoids (dexamethasone & betamethasone)
Different durations of action suit various therapeutic needs.
What is the role of 11β-hydroxysteroid dehydrogenase in glucocorticoid metabolism?
It is involved in the metabolism of glucocorticoids
This enzyme is crucial for the activation and inactivation of glucocorticoids.
Fill in the blank: The first-pass metabolism is associated with the _______ of aldosterone antagonists.
in vivo activation
First-pass metabolism refers to the initial processing of a drug in the liver before it reaches systemic circulation.
What are 9α-halogenated derivatives used for?
They are modifications of glucocorticoids
These derivatives enhance the therapeutic effects of glucocorticoids.
What does SAR stand for in the context of glucocorticoids?
Structure-Activity Relationship
SAR helps in understanding how different chemical structures affect biological activity.
True or False: Hydrocortisone is categorized as a mineralocorticoid.
False
Hydrocortisone is classified as a glucocorticoid.
What are the two main types of modifications for glucocorticoids?
- Pharmacokinetic modifications
- Pharmacodynamic modifications
These modifications are essential for optimizing drug efficacy and safety.
The addition of this conjugated double bond also makes the A ring
more resistant to inactivating reduction
reduction of ring A results in loss of activity.
also can be esterified at 21
The major metabolites (6b- and
16b-hydroxy) are both active metabolites (by cyp450)
Hydrocortisone sodium acetate
iv ad, very fast onset of action and rapidly excreted, in status asthmatics.
9α-halogenated derivatives
first they used bromine but it decreased the activity then switched to another halogens and noticed as the size of halogen decreased the GC activity increased
Methyl substituted analogues
methylation at position 6 potentiate GC activity and reduce the side effect of mineralo
Methylprednisolone contains a 6a-CH3
group, which essentially abolishes mineralo side effects (e.g.,
fluid retention, electrolyte imbalance) in therapeutic doses
and provides some steric hindrance to the reduction of the
already-resistant A ring
16α-hydroxyl analogues
similar GC to prednisolone, but the mineralo decreased (maybe due to the 16 alpha hydroxy group but reduced oral bioavailability
and to overcome this issue acetonide is made and it is 3 to 4 times more potent than triamcinolone cuz it reduces the metabolism
used for psoriasis and dermatosis
Methyl substituted analogues
methyl group stabilize the OH at position 17 from metabolism
higher lipophilicity and higher GC activity and higher recepter affinity and methyl group decreased the salt retention
Aldosterone antagonist
The 3-keto-4-ene A ring is essential for this antagonistic activity, and the opening of the lactone ring
dramatically reduces activity. The 7a-substituent increases both intrinsic
activity and oral activity.
