Steroid hormones Flashcards
what is the function of aminoglutethimide ?
it inhibit the conversion of cholesterol to pregnenolone via p450scc enzyme
This will inhibit the whole adrenal hormones cascades cuz pregnenolone is the precursor of all adrenal hormones
what is the function of ketoconazole/ metyrapone ?
inhibit the 11 b hydroxylase which will inhibit the formation of aldosterone/ cortisol
11 B hydroxylase is the enzyme responsible for forming aldosterone and cortisol
what is fludrocortisone ?
a synthetic mineralocorticoids
when is fludrocortisone used?
it is a synthetic mineralocorticoids so it is used in aldosterone deficiency
like patients with primary adrenal insufficiency —-> Addison disease
Flud —> fluid —> aldosterone —> increase fluid and sodium retention
what are the common uses of glucocorticoids a?
anti inflammatory , allergic , autoimmune , other disorders
what are the administration methods of glucocorticoids and what is the best one? ?
oral, parental, inhalation , topical
topical / inhalation are the best
cuz well tolerated and avoid most systemic adverse effects of glucocorticoids
what are the short acting low potency glucocorticoids ?
cortisol
cortisone
fludrocortisone
what is the other name of cortisol?
hydrocortisone is the pharmaceutical name for cortisol
what is the special feature of cortisone ?
cortisone is a prodrug , requires activation by the LIVER
once its metabolized it will become hydrocortisone
Cortisone is js more stable as a prodrug than cortisol ( hydrocortisone )
which one you should administer in liver failure?
cortisol ( hydrocortisone ) because it doesnt require activation unlike cortisone which requires metabolization
what are the uses of cortisol and cortisone?
hormone replacement therapy in adrenal insufficiency patients
anti inflammatory agents BUT the more potent ones are used for most inflammatory , allergic , autoimmune disorders
what are the medium potency , intermediate acting glucocorticoids?
prednisone
prednisolone
methylprednisolone
Triamcinolone
what are the uses of medium potency intermediate acting glucocorticoids ?
systemic treatments
what is the special feature about prednisone?
in the body it gets converted to prednisolone
so in cases of liver failure you cant give prednisone
what are the uses of intermediate acting glucocorticoids?
cancer
inflammation
allergy
autoimmune disorders
action last for 12 to 36
what are the high potency long acting glucocorticoids ?
betamethasone
dexamethasone
budesonide
what are the uses of betamethasone?
systemic use
topical treatment of skin disorders —> psoriasis , atopic dermatitis and neurodermatitis
what are the uses of dexamethasone?
diagnostic dexamethasone suppression test
treatment of neoplastic , infections , inflammatory conditions
how is budesonide administered ?
inhalation
what are the indications for steroids?
inflammation, allergy, autoimmune disorders —> suppress inflammation and immune dysfunction associated with disease affecting most every organ in the body
Cancer
Respiratory distress
adrenal insufficiency
congenital adrenal hyperplasia
cushing syndrome
dermatological diseases
other disorders
which steroid drug is used in LUPUS?
prednisone —-> intermediate
which steroid drug is used in multiple sclerosis?
prednisone
metyhlprednisolone –> intermediate
dexamethasone ———-> long acting
which drug is used in ulcerative colitis ?
methylprednisolone –> intermediate
budesonide –> inhaled long acting
what are the drugs indicated for allergic rhinitis
beclomethasone ——-> long acting
what is the newest agent for allergic rhinitis ?
ciclesonide
what are the agents for asthma ?
triamiclnolone
budesonide
ciclesonide
flunisolide
mometasone
flucticasone
why are glucocorticoids used in cancer?
lymphotoxic effects
used in lymphocytic leukemia and lymphomas
why is dexamethasone used in combination with other drugs for cancer?
it prevents emesis during cancer chemotherapy
what is the drug used in respiratory distress syndrome ?
betamethasone —> long acting
why is betamethasone the drug choice for respiratory distress syndrome?
it is used in premature infants
and it acts by promoting fetal lung maturation in the same manner as endogenous cortisol
what hormones are deficient in primary adrenal insufficiency ?
cortisol
aldosterone
androgens
what hormones you have to give in primary adrenal insufficiencies ?
Fludrocortisone —-> for aldosterone
hydrocortisone –> for cortisol
what hormones are deficient in secondary adrenal insufficiency ?
cortisol and androgens
ALDOSTERONE IS NORMAL
secondary adrenal insufficiency is usually due to prolonged administration of corticoids and ACTH deficiency
what hormones you have to give secondary adrenal insufficiency ?
you only give cortisol —> hydrocortisone /glucocorticoids
no need for fludrocortisone cuz no aldosterone deficiency
what is acute adrenal insufficiency?
aka adrenal crisis, addisonian crisis
medical emergency that happens when someone is under stress but there are not corticoids to help him
how do you treat acute adrenal insufficiency ?
IV hydrocortisone 48 hours
followed by long term oral hydrocortisone
how is chronic adrenal insufficiency treated?
HYDROCORTISONE orally in a manner that mimics the circadian secretion of cortisol —–> 2/3 of the dose at morning and 1/3 of it at the nigt
what is congenital adrenal hyperplasia? CAH
group of disorders caused by specific enzyme deficiencies that impair the synthesis of cortisol and aldosterone
this usually results in a shift towards androgens
why do we have adrenal hyperplasia in cases of CAH?
cuz impaired synthesize of cortisol and aldosterone will result in increased ACTH —>Hyperplasia
what are the characteristics of CAH?
since theres a shift towards production of adrenal androgens —> virilization —–> masculinization —-> in girls
pseudo hermaphroditism —-> in girls
what is the commonest enzyme defect in CAH?
21 hydroxylase –> 90% of the cases
11b hydroxylase —-> 9% of the cases
how is CAH treated?
hydrocortisone to stop ACTH secretion
fludrocortisone to treat aldosterone deficiency
how do you treat cushing syndrome due to excessive levels of ACTH?
surgery
irradiation
adrenal steroid inhibitors
cuz its usually due to pituitary adenoma that release excessive ACTH –> adrenal hyperplasia
other causes : adrenal adenomas, adrenal carcinomas, ectopic corticotropin ACTH secreting tumors
how is cushing syndrome diagnosed ?
free cortisol levels in the urine
dexamethasone suppression test
person with cushing syndrome dexamethasone will not suppress corticotropin ( ACTH ) secretion
what are the dermatologic conditions where you use corticosteroids ?
Atopic ( contact )
sberrheic dermatitis
pruritus –> itching
psoriasis
sunburn
on which part of the skin you use low potency drugs?
areas of thin skin —-> face and eyes
intertriginous areas where skin is folded or overlapped
which part of the skin you use medium potency drugs?
ear
trunk
Arm
legs
scalp
which part of the skin you use high potency drugs?
palms and soles
what are the low potency TOPICAL STEROIDS?
hydrocortisone –> cortisol
desonide
hydrate under de Sun
what are the medium potency topical steroids ?
Triamcinolone
fluticasone
Try the flute
what are the high potency steroids?
desoximetasone
fluocinonide
Remove your socks ( de sox ) when you have flu
what are the very high potency steroids ?
betamethasone
dexamethasone
clobetasol
A BCD ( Beta clobe dexa )
what are the other uses of glucocorticoids ?
hypercalcemia
sarcoidosis
immunosuppressants to prevent organ rejection
what are the side effects of long term uses of glucocorticoids ?
Symptoms of cushing syndrome
moon face
Brusing
peptic ulcer
hypertension
centripetal obesity
Striae
menstral disturbance
Etc
what is the major Adrenal androgen and whats its major use?
Dehydroepiandrosterone DHEA
major androgen secreted by the cortex
extremely weak androgen —> converted to testosterone
NO CLINICAL USE
what is aminoglutethimide ?
corticosteroid synthesis inhibitor that inhibit P450SCC
stops conversion of cholesterol to pregnenolone
what are the uses of aminoglutethimide?
it inhibits all steroids
Breast cancer
malignant adrenocortical tumors
Cushing syndrome along with metyrapone
what is metyrapone ?
corticosteroid synthesis inhibitor that inhibit 11B hydroxylase enzyme
it inhibits aldosterone / cortisol pathway and shifts it all to androgen pathway
what are the uses of metyrapone ?
cushing syndrome along with aminoglutethimide
me tired ill sleep on the cushion
what are ketoconazole and fluconazole ?
antifungal drugs that inhibit many Cytochrome P450 enzymes INCLUDING CYTOCHROMES USED IN STEROID BIOSYNTHESIS
what are the uses of ketoconazole and fluconazole?
cushing syndrome
also inhibit androgen synthesis
what is the side effect of ketoconazole and fluconazole ?
gynecomastia in males
what is spironolactone ?
corticosteroid receptor antagonist
IT competes with aldosterone for mineralocorticoid –> aldosterone receptor in RENAL TUBES
what are the uses of spironolactone ?
Potassium sparing diuretic —> we want to keep potassium in
Hyperaldosteronism
Secondary hyperaldosteronism –> due to heart failure ( HF will cause low CO for kindey —> renin —> aldosterone ), bartter syndrome
which type primary hyperaldosteronism we use spironolactone ?
Primary hyperaldosteronism CAUSED BY BILATERAL ADRENAL HYPERPLASIA
Hyperaldosteronism caused by ALDOSTERONE producing adenoma IS TREATED BY SURGERY
what is mifepristone ?
Receptor antagonist for progesterone and glucocorticoid
used for cushing syndrome
