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77 Cards in this Set
- Front
- Back
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what are general clinical uses of glucocorticoids/mineralocorticoids?
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*replacement therapy
*management of inflammatory dz *treatment of severe allergic rxn *treatment of certain cancers *dx of disorders of adrenal fxn |
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what are general organ and tissue effects?
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*metabolic
*catabolic *stress resistance *plasma blood cell level effects *immunosuppressive *anti-inflammatory |
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what is an impt natural glucocorticoid?
what are some therapeutic natural preps of this? |
cortisol/hydrocortisone
*cortef *a-hydrocort *hydrocortone *solu-cortef |
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what are short to medium acting glucocorticoids?
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*cortisone
*prednisone(sterapred) *prednisolone(Orapred, Prednoral, Predacort, Pediapred) *Methylprednosolone(Medrol, Depo-medrol, A-methapred, solu-medrol) |
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what is an intermediat acting glucocorticoid?
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triamcinolone
(Nasacort AQ, Azmacort, Aristospan, Amcort, Kenalog) |
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what are long acting glucocorticoids?
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*dexamethasone(decadron, Dexone LA)
*Betamethasone (Celestone, Diprolene) |
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what are locally acitn glucocorticoids?
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*Beclomethasone(beconase AQ, Qvar)
*Budesonide(pulmicort, Rhinocort Aqua) *Fluticasone(Flovent, Flonase, Veramyst) *Flunisolide(Aerobid, Nasarel) *Mometasone(Asmanex, Nasonex) |
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what glucocorticoids are used as replacement therapy for primary addison's dz?
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1. hydrocortisone(cortef)
2. Fludrocortisone(florinef acetate) |
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what glucocorticoids/mineralocorticoids are used as therapy for secondary or tertiary addisons (adrenocortical deficiency)
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1. same as primary
(hydrocortisone and fludrocortisone) |
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which are used as replacement therapy for congenital adrenal hyperplasia(CAH)
which can be given pregnant women |
1. hydrocortisone or Prednisone
2. Dexamethasone (PREGNANT) 3. Fludrocortisone |
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which are used as replacement therapy for adrnealectomy?
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1. hydrocortisone and fludrocortisone
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what is used to dx cushings dz?
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dexamethasone suppression test
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what is used to stimulate fetal lung maturation?
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betamethasone (celestone)
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what are the mineralocorticoids?
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*aldosterone
*Fludrocortisone *Deoxycorticosterone |
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what are the therapeutic uses of mineralocorticoids?
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1. replacement therapy for primary adrenocortical deficiency
2. replacement therapy for congenital adrenal hyperplasia 3. replacement therapy following adrenalectomy |
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what are corticoteroid receptor antagonists?
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1. spironolactone
2. Eplerenone(Inspra) 3. Mifepristone(RU 486) Mifeprex) |
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what are corticosteroid Synthesisi inhibitors?
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1. Ketoconazole(Nizoral)
2. Metyrapone(Metopirone) |
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what are the corticosteroids?
what is the common precursor |
steroid hormones produced by adrenal cortex
cholesterol is common precursor |
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what is release of glucocorticoids regulated by?
what is relese of mineralocorticoids regulated by? |
gluco= corticotropin (ACTH)
mineralo=renin angiotensin system |
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what does the mineralocorticoids regulate?
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sodium and potassium reabsorption
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where do corticosteroids bind in target tissue cell?
what is the glucocorticoid recepter a member of? |
corticosteroids bind to ubiquitous specific cytoplasmic receptors that transport steroid into nucleus
the glucocorticoids is part of superfamily of receptors that include thryoid and steroid hormones |
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what is the genomic effect?
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gene expression that is altered by the steroid receptor complex
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what are the sequence of events in genomic mechanism of corticosteroid action?
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1. passive entry into cell
2. bind to and activate spefici receptor 3. release heat shock PRO 90 or 70 4. dimerization of activated steroid receptor complex 5. activated dimer enters nucleus and binds to nuclear response elements 6. regulates transcription of target genes |
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what is the nongenomic effect mediated through?
can these be blocked by RNA or PRO synthesisi inhibitors? |
mediated through activation of MEMBRANE (not intracellular) receptors
NOT BLOCKED by inhibitors of RNA or PRO synthesis |
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what is the metabolic effect of glucocorticoids trying to preserve?
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maintain an adequate glucose supply to brain
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what are metabolic ways that glucocorticoids can increase glucose in blood?
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1. stimulate gluconeogenesis
2. decrease glucose uptake into muscle and fat tissue 3. increase liver glycogen deposition 4. stimulates lipolysis and lipogenesis |
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what are consequences of increased liver lipolysis and lipogenesis assoc with too much glucocorticoid?
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CUSHINGs symptoms such as moon facies and buffalo hump
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what are the catabolic effects of gluco?
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*muscle PRO catabolism and lipolysis
*osteoporosis *inhibit growth in kids |
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what are the stress resistance effects ?
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*hyperglycemia
*slight BP increase |
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what are the plasma blood cell effects?
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*decrease circulating lymphocyte, monocyte
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what blood plasma cell level effects?
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*decreased lymphocyte and monocyte
*decreased immune response |
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what are the immunosuppresive effects?
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*inhibits macrophages
*reduce levels of lymphocytes (decreased cell mediated immunity) |
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what are the anti-inflammatory effects?
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*decreased Pain, heat, redness and swelling mediated through an effect on circulation and fxn of peripheral leukocytes(migration inhibited)
*reduced lymphocytes *inhibited macrophages *inhibition of phospholipase A1 *inhibition of cyclooxygenase COX-2 *decrease of histamine |
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what are other effects on:
water? fat? vit D? fetus? |
*excretion of water loads
*promotes fat redistrubtion *inhibis vit d on calcium absortption (bone loss) *surfactant in fetus |
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what can happen at large doses?
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*behaioral disturbances
*peptic ulcers |
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what is secretion of cortisol regulated by?
what does it vary with? |
regulated by ACTH
varies with circadian rhythm |
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what methods of administration are good for cortisol?
is olasma bound hormone active? what metabolism does cortisol go through |
excellent oral and good topical
only free hormone is active undergoes hepatic and renal metabolism |
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where are glucocorticoids inactivated?
what are c/i of glucocorticoids |
in the liver by glucouronidation therefore they are c/i in liver failure patients
liver failure, peptic ulcer and HTN(cortisol has salt retaining) |
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how do the synthetic cortisol analogs compare to cortisol?
what are the three classifications of synthetic glucocorticoids? |
synthetics are:
*longer half life *longer duration of action *decreased salt retaining activity *enhanced penetration of lipid barriers for topical use three classifications are a. short to medium acting b. intermediate acting c. long acting |
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what are the short to medium acting?
what is the number 1 Rx'd |
*cortisone
*Prednisone *Prednisolone(Orapred, Prednoral, Predacort, Pediapred) *Methylprednisolone (#9) PREDNISONE IS NUMBER 1 |
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what is the intermediate acting glucocorticoid?
what is a good method of administration for this what # Rx is this? how much more potent are the intermediate than cortisol? |
Triamcinolone
(Nasacort AQ, Azmacort, Aristopan, Amcort, Kenalog) has good topical activity is #10 10x more potent |
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what are the long acting glucocorticoids?
how much more potent than cortisol are these? what is good method of enhancement? |
*Dexamethasone
*Betamethasone 25x more potent(MOST POTENT) good topical activity in comparison to intermediate acting glucocorticoids |
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regarding antiinflammatory effects what specifically is inhibited?
regarding inflammatory tx what is specifically inhibited? |
anti inflammatory= leukotrienes (and prostaglandins)
inflammation=thromboxanes and prostaglandins |
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what is the structure of cortisol?
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a 6 sided steroid w/ ABC ring and a 5 sided D ring
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what are the locally acing glucocorticoids?
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1. Beclomethasone
2. Budenoside 3. Fluticasone 4. Flunisolide 5. Mometasone |
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what locally acting glucocorticoids can be used in the tx of asthma and allergic rhinitis?
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1.Beclomethasone
2. BUdesonide 3. FLuticasone 4. FLunosilide |
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what locally acting glucocorticoids treat only rhinits
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mometasone
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what intermediate acting corticosteroid txs asthma and allergic rhinitis?
how is it usually administered? |
triamcinolone
usually given nasally (rest usually oral) |
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if u give someone dethamexasone and it has no effect then what is cause of cushings
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an adrenal or ectopic tumor
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how can you tell the difference b/w adrenal and ectopic tumor
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low ACTH in presence of adrenal tumor
high acth in presence of ectopic tumor |
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if you give someone dethamexasone and it decreases cortisol then what is cause of cushings
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a pituitary dependent cushings desease
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what is the major reason to use steroid for nonadrenal reasons?
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inflammatory or immunological
eg. pulonary dz, allergic rn, skin dz, eye dz, gi dz, inflamation of bones, joints, organ transplant rejection, infection and collagen vascular disorder |
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what are some other clinical uses of steroids regarding:
hematologyK? Neurologic disorder? Chemo? Metabolites? Specific syndrome? |
treat hematologic cancers
(leukemia in peds, lymphoma and MM) *treat MS *manage chemo induced vomiting *treat Mountain Sickness |
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how are steroids excreted?
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in urine after glucouronidation by hepatic microsomal enzymes
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what are the adverese effects of steroids?
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Cushing like syndrome
*altered fat deposition *DM from hyperglycemia *Muscle wasting, weight gain *osteoporosis *salt retention, edema HTN *peptic ulcer *impaired healing *cataracts and glaucoma |
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how can you reduce the adverse effects?
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local or topical application
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how should steroid therapy be stopped?
what can instant withdrawal cause |
gradually
DECREASE OVER SEVERAL MOTNHS. instant withdrawal can cause lethal, acute adrenal insufficiency syndrome |
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what are the contraindications of steroid use?
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1. DM
2. Peptic Ulcer 3. Osteroporosis 4. Glaucoma 5. Infections 6. Psychological Disturbance 7. Heart dz 8. HTN w/ congestive heart failure |
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what are the mineralocorticoids
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*aldosteron
*fludrocortisone |
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what is the mechanism of action of aldosterone?
what absorption is increased/decreased |
salt retaining activity
promotes reabsorbption of Na, HCO3, H2O, at distal tubule decreases reabsorption of K and H ions |
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what is the clinical use of aldosterone?
how can hyperaldosteronism affect metabolite metabolism levels? how can hyperadlosteronism affect blood pH? what do you tx hyperaldosteronism with? |
not used clinically
hyperaldosteronism can cause Hypernatremia, hypokalemia can cause metabolic alkalosis, increased plasma volume and HTN tx with spironolactone |
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what is the most potent and widely prescribed mineralocorticoid?
what is this drug a favored replacement therapy for? |
Fludrocortisone
following an adrenalectomy |
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what are clinical uses of fludrocortisone?
what are adverse effects |
*ONLY USED FOR REPLACEMENT THERAPY
1. after adrnealectomy 2. congenital adrenal hyperplasia 3. addisons dz adverse effects similar to hyperaldosteronism |
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what are mineralocorticoids usually rx's with?
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short acting glucocorticoids
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what are the two ways that corticosteroids can be antagonized?
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1. block receptor
2. inhibit synthesis |
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what are the corticosteroid receptor antagonists?
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*spironolactone
*Mifespristone/ RU86 (abortion pill |
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what is mech of action of spironolactone?
what is a drug that works similar to spironolactone? |
*aldosteron receptor antagonis that inhibits reabsorption of Na
Eplerenone(Inspra) |
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what is the clinical use of spironolactone?
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corticosteroid overproduction such as in Primay aldosteronism
*also tx hypokalemia, and tx's edema and HTN |
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what are the adverse effects of spironolactone?
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hyperkalemia (cardiac arrythmias)
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what is the mechanims of action of Mifepristone/ RU 86
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it is a PARTIAL steroid agonist
it blocks glucocorticoid and progesterone receptor antagonist |
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what is the clinical use of RU86?
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cushings syndrome drue to adrenal carcinoma or ectopic ACTH secretion
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what are the three drugs that inhibit synthesis of cortisol?
when do you use these drugs? |
1. ketoconazole
2. Metyrapone use these drugs if surgical therapy of adrenal cancer is impractical or unsuccessful due to metastases |
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what is mechanism of action of ketoconazole?
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it is an antifungal agent that inhibits P450 enzyme necessary fro ALL steroids (gonadal and adrenal)
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what are the clinical uses of ketoconazole(nizoral)
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*tx of cushings
*tx of adrenal carcinoma *tx of prostate cancer |
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what is the mechanism of action of metryapone?
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selective inhibitor of glucocorticoid synthesis
it inhibits 11beta hydroxylase (last step in cortisol synthesisi) |
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how is metyrapone u sed clinically?
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to treat cushings
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what are the adverse effects of myterapone?
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-salt and water retention
-HIRSUTISM -GI distubance |
