Miscellaneous Quiz / Adrenal Drugs

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Can you name the Adrenal Drugs?

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Deoxycorticosterone class
SE: Lethary, dizziness, and skin rashs (at high doses)
SE: Osteoporosis, severe myopathy, cataracts, glaucoma, peptic ulcers, hypokalemia, edema, HTN
Mifepristone class
Cortisone class
Use: Decrease estrogen production in breast CA pts (used in w/ dexamethasone or hydrocortisone).
Anti-inflammatory: 25-40; Topical 10, Na Retaining: 0; Equivalent oral dose: 0.6 mg
MOA: Inhibits cholesterol side chain cleavage (p450scc) & other p450 enzymes required for steroid synthesis
Drospirenone class
Use: Primary aldosteronism (Conn's syndrome). Used as a diuretic in CHF. Tx hirsutism
Anti-inflammatory: 5; Topical 5; Na Retaining: 0; Equivalent oral dose: 4 mg
P-kinetics: Keep the dose low. Tx should not be decreased or stopped abruptly.
Use: Stimulation of fetal lung maturation - used in pregnant women to prevent RDS in preterm infants
Trilostane class
Topical 5, Na Retaining: 0; Equivalent oral dose: 4 mg
SE: Hepatotoxicity. Interferes w/ the metabolism of sex steroid hormones, warfarin, phenytoin, etc.
Hydrocortisone (Cortisol) class
P-kinetics: High plasma PRO binding activity (albumin and glycoprotein but not CBG). T1/2 ~ 20 hours
Use: Tx of non-adrenal disorders -Suppress inflammatory & immune responses (e.g. arthritis, lupus, UC, asthma, SJS) - Use medium- to intermediate-acting glucocorticoids.
Use: Dx purposes - dexamethasone suppression test - for Cushing's - measures response of the adrenal glands to ACTH
Metyrapone class
Anti-inflammatory: 10; Na Retaining: 0; Equivalent oral dose: 2 mg
Use: Cushing's syndrome, fungal infections
Meprednisone class
Anti-inflammatory: 4; Topical 0, Na Retaining: 0.3; Equivalent oral dose: 5 mg
Use: Tx of tpx rejection- reduces antigen expression from grafted tissue; delays revascularization; interferes w/ sensitization of cytotoxic Tcells & generation of Ab-forming cells
Use: Tx of disturbed adrenal function: (2) Adrenocortical hypo- or hyperfunction [congenital adrenal hyperplasia; glucocorticoid remediable aldosteronism (GRA)]
Use: Pheochromocytoma (esp. pre-op)
Use: For inoperable pts w/ adrenal CA who failed to respond to other txs. Abortificant (< 2mos). Emergency contraceptive (prevent ovulation).
Betamethasone class
Eplerenone class
MOA: A more selective receptor antagonist
Use: Tx hirsutism. May decrease PMDD. A progestin oral contraceptive (Yasmin)
Prednisone class
MOA: Blocks 11β-hydroxylase in steroid synthesis
MOA: Glucocorticoid receptor antagonist. Also blocks progesterone receptor (antiprogestin activity: a contraceptive-contragestive agent).
Phenoxybenzamine class
Anti-inflammatory: 5; Topical 4, Na Retaining: 0.3; Equivalent oral dose: 5 mg
Use: Pheochromocytomoa (esp intra-op) & ED
Use: HTN
Route: Injectable, pellets
Fludrocortisone class
Aminoglutethimide class
Special precautions: pts should be monitored for: hyperglycemia, glycosuria, edema or HTN, hypokalemia, peptic ulcers, osteoporosis.
Anti-inflammatory: 0.8; Topical 0, Na Retaining: 0.8; Equivalent oral dose: 25 mg
MOA: Blocks progesterone receptors & androgen receptors -> Na loss & K retention
SE: IV -Severe tachycardia, arrythmias, myocardial ischemia. Oral - tachycardia, nasal congestion, HA
Use: Prevention of chemo-induced emesis (e.g. dexamethasone prevents cisplatin-induced emesis)
MOA: Irreversible long-duration (14-48 hrs) blockade of α-receptor (α1 > α2). Also blocks H1-R, Ach-R, serotonin-R. Vasodilates & increases CO. Oral
SE: Hyperkalemia
Methylprednisone class
Route: Oral
Route: Oral, injected, topical
DOC Acetate (DOCA)
Route: Oral, injected
Anti-inflammatory: 0; Topical 0, Na Retaining: 20
SE: Salt & fluid retention, hirsutism, dizziness, GI upset
Paramethasone class
Anti-inflammatory: 30; Topical 10; Na Retaining: 0; Equivalent oral dose: 0.75 mg
Prenisolone class
Dexamethasone class
Use: Tx adrenal insufficiency associed w/ mineralocorticoid deficiency (i.e. Addison's dz)
Anti-inflammatory: 1; Topical 1, Na Retaining: 1; Equivalent oral dose: 20 mg
Use: Decrease steroid production in pts w/ Cushing's d/t adrenocortical CA (w/ metyrapone or ketoconazole)
Phentolamine class
Anti-inflammatory: 10; Topical 0, Na Retaining: 250; Equivalent oral dose: 2 mg
SE: impaired wound healing, hyperglycemia, hyperlipidemia, anxiety, insomnia, depression, steroid psychosis, infections,
Ketoconazole class
Fluprenisolone class
SE: Oversecretion or overdosing may result in hypokalemia, metabolic alkalosis, HTN.
Mitotane class
MOA: Act on mineralocorticoid receptors. Activation of the aldosterone receptor -> increased expression of Na/K/ATPase. Increase reabsorption of Na & excretion of K.
SE: Abd pain, uterine cramping, bleeding. Causes glucocorticoid resistance
MOA: Blocks synthesis of pregnenolone -> Decreased mineralocortioids, glucocorticoids & androgens/estrogens
Use: Tx pregnant women w/ Cushing's. Dx of adrenal insufficiency (measure blood levels of 11-deoxycortisol & urinary 17-hydroxysteroid)
Triamcinolone class
Contraindications: peptic ulcer, heart disease, HTN w/ heart failure, infectious diseases, psychosis, DM, osteoporosis, glaucoma
Spironolactone class
P-kinetics:Shorter t1/2 (5-7 hrs) than phenoxybenzamine
Has both glucocorticoid and mineralocorticoid activity
Aldosterone class
MOA: A potent competitive α-antagonist (α1 = α2). Minor inhibitory effect on serotonin-R. Agonistic effects on MR & H1/H2-R. Decreased PVR, increased cardiac stim (reflex)
MOA: An analogue of spironolactone. Has anti-mineralocortioid & anti-androgenic activities.
SE: Serious SE unusual for short-term tx (< 2 weeks). Major SE(> 2 weeks of treatment): Iatrogenic Cushing's syndrome, adrenal suppression, acute pancreatitis (high dose tx; rare).
Anti-inflammatory: 15; Topical 7, Na Retaining: 0; Equivalent oral dose: 1.5 mg
SE: Postural hypotension, tachycardia, nasal stuffiness, inhibition of ejaculation, fatigue, sedation, nausea
Use: Tx of disturbed adrenal function - (1) Adrenocortical insufficiency [Chronic = Addison's dz or Acute]
SE: Hyperkalemia, cardiac arrhythmia, gynecomastia, mentrual abnormalities, GI disturbances, skin rashes
Anti-inflammatory: 5; Na Retaining: 0; Equivalent oral dose: 4 mg

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