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Glucocorticoids
Pharm
93
Medical
Kindergarten
04/27/2010

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Cards

Term
What is the mineralcorticoid?
Definition
Fludrocortisone
Term
What is are the two actions of Mifeprisone (Ru-486)?
Definition
Abortion pill that acts as a Glucocorticoids Antagonists and a Progesterone Receptor Antagonist
Term
Which hormone displays an 8 o'clock Diurnal Secretion Variation?
Definition
Cortisol
Term
Which Pituitary Hormone triggers the release of Adrenal Cortisol?
Definition
ACTH
Term
What is the main Hypothalamic regulator released to trigger the ANterior Pituitary to realease ACTH?
Definition
CRH (Corticotrophin Releasing Hormone)
Term
Where are the ACTH receptors found?
Definition
Mainly the Zona Fasciculata and some on the Zona Reticularis
Term
Binding of ACTH at the Zona Fasiculata stimulates the release of what?
Definition
Cortisol from the Adrenal Gland
Term
The use of High-Dose Exogenous Corticosteroids such as Prednisone can negatively feedback inhibit at what level?
Definition
It will block Pituitary and Hypothalamic stimulation of the Adrenal Glands decreasing endogenous production of Cortisol
Term
What is the precursor molecule for aldosterone
Definition
corticosterone, cortisol, testoterone, and esrodiol?,Cholesterol
Term
What is the main enzyme regulated that converts cholesterol to pregnenolone?
Definition
20,22-Desmolase, Cholesterol Side Chain Cleavage
Term
Which reaction does the enzyme 20
Definition
22-Desmolase carry out?,It does Cholasterol side cain cleavage in the conversion of Cholesterol to Pregnenolone
Term
What molecules are needed along with 20
Definition
22-Desmolase in order to convert Cholesterol to Pregnenolone?,NADPH, Molecular Oxygen, and the enzyme is a p450 member
Term
Which enzymes are found in the areas of the adrenal cortex which produces Cortisol?
Definition
17-alpha hydroxylase, 21-beta hydroxylase, and 11-beta hydroxylase
Term
What type of enzymes typically utilize NADPH and molecular oxygen?
Definition
Cytochrome p450 enzymes, which can be Induced or Inhibited
Term
What is the first step in Steroid Hormone action?
Definition
Plasma Binding
Term
Where does the Steroid bind?
Definition
To the Glucocorticol Receptor
Term
Where is the Glucocoticol Receptor found?
Definition
In the Nucleus
Term
What is the Glucocorticol Receptor bound to?
Definition
DNA at the Glucocorticoid Response Element
Term
How is Cortisol found in circulation?
Definition
Bound to Cortisol Binding Globulin
Term
How is Testosterone and Estridiol found in circulation?
Definition
Bound to Sex Steroid Binding Globulins
Term
Are Hormones typically bound in circulation by globulins?
Definition
Yes
Term
Which form of the Steroid hormone is Lipophilic and able to cross the cell membrane and be active?
Definition
The Free Form not bound to Globulin
Term
Are there specific nuclear recpetors for the different Steroid Hormones?
Definition
Yes
Term
What is the N-terminal region of the Steroid Receptor responsible for?
Definition
Transcription Activation
Term
What is the Central region of the Steroid Hormone Receptor responsible for?
Definition
BInding to the DNA at the Glucocorticoid Receptor Element
Term
What is the Ligand Region of the Steriod Hormone Receptor responsible for?
Definition
Binding of the Hormone itself
Term
What happens after the Hormone binds the receptor?
Definition
Dimerization
Term
What happens after dimerization of the Hormone receptor?
Definition
BInding to the DNA at the glucocorticoid response element
Term
What happens after binding of the Glucocorticoid Response Element?
Definition
Activation of the Transactivation Domain with the Trascription Machinery
Term
What is a characterisitic of Steroid hormone Receptors found in the cytoplasm or nucleus?
Definition
They are found in a Un-Liganded high affinity state
Term
What is the function of the chaperones?
Definition
Keep the Steroid Hormone Recpetors in their HIgh Affinity state until a ligand comes along
Term
What are the chaperones associatted with glucocorticoid receptors?
Definition
HSP 90, HSP 70, and IP (immunophillin)
Term
What happens to the chaperone when a Steroid Hormone binds to the ligand region of the receptor?
Definition
They fall apart
Term
What is the basic structure of a steroid hormone?
Definition
They have an A,B,C, and D ring
Term
What type of steroid is Cortisol?
Definition
C-21 Steroid
Term
How are Steroids metabolized?
Definition
Successive reductions in the A ring
Term
Where specifically is Cortisol reduced?
Definition
Reduction of the 4-5 position 3-Keto Group
Term
What happens to Cortisol after reduction in the metabolization process?
Definition
Glucoronidation to form a more water soluble product for excretion in the urine
Term
What are the effects of Adrenal Steroids on Carbohydrates
Definition
Proteins, and Fat Metabolism?,Increase Plasma Glucose, Increase Mobilization of Amino Acids from Tissue, and Inhibit Glusoce Uptake by fat cells
Term
What are the effects of Adrenal Steroids on Electrolyte and Water Metabolism?
Definition
Increase Sodium Reabsorption, Increase Potassium Secretion, and Inhibit Calcium Absorption from Intestines
Term
What are the Anti-INflammatory and Immunosuppressive effects of Adrenal Steroids?
Definition
Inhibit Arachadonic Acid (Cyclooxygense2 and Phospholipase A2), Inhibit Cytokine Production and Release (NF Kappa B), and Inhibit production of Adhesion Molecules
Term
Do Adrenal Steroids increase gluconeogenesis?
Definition
Yes so increase plasma glucose
Term
What is a long term effect of Protein Mobilization by Adrenal Steroids?
Definition
Muscle Wasting
Term
What is the main Adrenal Homrone that regulates Sodium and Potassium flux in the Kidneys?
Definition
Aldosterone, Increases Sodium Reabsorption and Potassium Secretion
Term
Does Cortisol have any effect on the Sodium/Potassium exchange?
Definition
Yes has some mineralcorticoid activity just not as potent as Aldosterone
Term
How does Cortisol act to inhibit Ca absorption in the Gut?
Definition
Anatagonist of Vitamin D, Also Increase Sodium/Potassium exchange which causes increased Ca excretion in the Feces
Term
What 2 enzymes do Corticosteroids inhibit which lead to Anti-inflammatory and Immunosuppresant response?
Definition
Block Cyclooxygenase 2 and Phospholipase A2
Term
What is the product of Cyclooxygenase 2?
Definition
Prostaglandins
Term
What effect does Corticosteroids have on Cytokins?
Definition
Inhibit their production and release
Term
Which phenonmenon does the anti-Cytokine action of Corticosteroids use?
Definition
Block NF Kappa B
Term
Which adhesion molecules can Adrenal Steroids inhibit the production of?
Definition
ELAM1 and ICAM1 on the endothelial cells
Term
What hormone basically inhibits the responsiveness to tissue injury?
Definition
Corticosteroids
Term
What is the only thing corticosteroids are used to TREAT?
Definition
Adrenal Insufficiency
Term
What symptoms can be ALLEVIATED with the use of corticosteroids?
Definition
Allergic Reactions, Eye Disease, GI Inflammatory Bowel Disease, Joint Inflamation, Nephrotic Syndrome, Skin Diseases, and Asthma
Term
What is the half-life of cortisol expressed in?
Definition
Hours but certainly not Days
Term
What are the three areas of action that synthetic Cortisol are aimed at improving?
Definition
Increased Half-life, More Potent, Less Salt Retention Activity
Term
What are the 3 Categories of Glucocorticoids?
Definition
Short-acting, Intermediate-acting, and Long-acting
Term
What is Hydrocortisone also known as?
Definition
Cortisol, Same as Endogenous
Term
Which Glucocorticoid has a baseline value of 1 for anti-inflammatory and salt-retention?
Definition
Hydrocortisone
Term
What category does Prednisone fall under?
Definition
Short-acting
Term
What is th anti-inflammatory value of Prednisone?
Definition
4 so 4 times the anti-inflammatory action of Cortisol
Term
What is the salt-retention activity of Prednisone?
Definition
1/3rd of endogenous
Term
Will prednisone result in Hypertension?
Definition
No
Term
What is a Intermediate Glucocorticoid?
Definition
Triamcinolone
Term
What is the Anti-Inflammatory activity of Triamcinolone?
Definition
5x
Term
What is salt retention activity of Triamcinolone?
Definition
0, none
Term
What are the two Long-Acting Glucocorticoids?
Definition
Dexamathasone and Betamethasone
Term
What is the Anti-inflammatory activity of Dexamethasone and Betamethasone (Long-acting)?
Definition
Very Potent, 25-40x
Term
What is the Salt retention activity of the long acting glucocorticoids?
Definition
Nearly Zero
Term
Which glucocorticoid has a Salt-Retention activity of 250x acting as a potent Mineralcorticoid?
Definition
Fludrocortisone, also has 10x anti inflammatory activity
Term
Which glucocorticoid is likely to induce HTN?
Definition
Fludrocortisone
Term
Which glucocorticoid is often found in the inhalant preparations used to treat asthma?
Definition
Beclomethasone, Budesonide, and Flunisolide, Intermediate Glucocorticoid
Term
Which glucocorticoids must be activated?
Definition
Prednisone, Methylprednisone, and Cortisone
Term
What enzyme activates Predisone
Definition
Methylpredisone, and Cortisone?,Hepatic 11 Beta-hydroxysteroid dehydrogenase 1
Term
What is the active form of Prednisone?
Definition
Prednisolonen
Term
What is the active form of Methylpredisone?
Definition
Methylprednisolone
Term
What is the active form of Cortisone?
Definition
Cortisol
Term
Are Steroids usually orally active?
Definition
Yes
Term
What is common about Dexamethasone
Definition
Betamethasone, Triacinolone, and predisone?,Orally Active
Term
Why are topical and inhalant forms of Glucocorticoids developed?
Definition
To prevet some the side effects of the parental corticosteroids
Term
What are the side effects of Corticosteroid Therapy?
Definition
1. Hyperglycemia 2. Retarded Growth in Children 3. Negative Nitrogen and Calcium Balance 4. Sodium Retention 5. Suppression of Hypothalamic, Pituitary, Adrenal Axis 6. Hypertension 7. Muscle Wasting 8. Osteoporosis 9. Mood Disorders 10. Immunsuppression 11. Cataracts in Children
Term
What is the problem with using Long-acting Corticosteroids for extended periods of time?
Definition
Decrease Endogenous Production, so when Exogenous is removed can Tank, Must Ween off Slowly
Term
What side effect of Corticosteroids is reversible?
Definition
Hyperglycemia or the uncovering of Latent Diabetes
Term
What side effect of corticosteroids is not reverisble?
Definition
Cataracts in Children
Term
What Corticosteroids are often found in Asthma Inhalers?
Definition
Budesonide and Flunisolide
Term
What is an oral form of Budesonide used to treat and why?
Definition
Inflammatory Bowel DIsease, not readily absorbed so stays in the Bowel Lumen
Term
What is a side effect of Inhaled Steroids?
Definition
Candidaiasis and Dysphonia, due to immunosupression of local depositions in the mouth
Term
What are oral preparations of Corticosteroids used for?
Definition
Poison Ivy, Psoriasis, or Itching
Term
What is Ketoconazole?
Definition
Anti-fungal
Term
What drugs can block Steroid Hormone Synthesis?
Definition
Ketoconazole, Aminogluthemide which can be used in the Treatment of Cushings Disease
Term
What drug seletively destroys adrenocortical cells and can be used in the treatment of Adrenal Carcinoma?
Definition
Mitotane
Term
Can the Inhalant and Topical Preparations lead to parental type side effects?
Definition
Yes is overly used or placed on a highly vascular area
Term
What are of the man is better to scratch?
Definition
Scrotum, due to easy absorption of topical steroids
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