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68 Cards in this Set
- Front
- Back
Principal androgen in men?
What secretes 95% of it? What secretes 5% of it? |
Testosterone
Leydig cells Adrenal Cortex |
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What are the plasma levels of Testosterone in males after puberty?
When do they start to decline? |
0.6 mg/dL
after age 50 |
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What is the level of Testosterone in females?
What 2 sites secrete Testosterone in females? |
.03 mg/dL (vs. 0.6 in males)
Adrenal Cortex & Corpus Luteum |
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What are 2 weak androgens secreted along with Testosterone in men?
What is their precursor? |
Androstenedione & De-hydro-epi-androsterone (DHEA)
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In target tissues, Testosterone is converted into active and inactive metabolites...what are the 2 ACTIVE metabolites?
Which is the major active androgen in most tissues? |
1. Dihydro-testosterone
2. Estradiol Dihydrotestosterone |
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In the Liver, Testosterone is metabolized into what 2 INACTIVE METABOLITES?
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1. Andro-sterone
2. Etio-cholan-olone |
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List the changes that both Testosterone and Dihydrotestosterone cause at PUBERTY
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1. general GROWTH-promoting properties
2. Penile & Scrotal growth 3. Thicker and oilier skin with more SEBACEOUS glands 4. appearance of pubic, axillary, and beard hair 5. Laryngeal growth, thicker vocal cords = lower-pitched voice 6. Accelerated Skeletal growth & Epiphysial closure 7. Growth of Prostate and Seminal Vesicles 8. Stimulating and maintaining Male Sexual fxn |
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List the 2 changes produced by Testosterone & Dihydrotestosterone in EARLY ADULTHOOD & MIDLIFE
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1. gradual development of MALE PATTERN BALDNESS = begins with recession of hair at temples & vertex
2. development of BENIGN PROSTATIC HYPERPLASIA or PROSTATIC CANCER |
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Serum Testosterone declines gradually as men age so that by age 80 free testosterone concentration is about ____% of that at age 20
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40%
**may be related to decreases in energy, libido, muscle mass/strength, and bone mineral density |
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Why is Oral Testosterone ineffective?
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b/c it is catabolized in the liver
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What type of preparations of Testosterone are able to bypass hepatic catabolism and are injected IM every 2-4 wks in Hypogonadal males
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synthetic preps as LIPOPHILIC ESTERS dissolved in OIL
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List 3 esters that are used to prolong and have greater activity release of free testosterone at injection sites
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Propionate
Enan-thate Cypio-nate **are not Androgens themselves but help in the slow release of Testosterone |
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What are the 2 uses of Synthetic Androgens?
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1. Anabolic effects (but increase in muscle strength is ALWAYS accompanied by adverse effects)
2. treating Testosterone deficiency |
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What do large doses of Synthetic Androgens cause in Adult Males?
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suppress Gonadotropin secretion ➡ testicular atrophy
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What can happen if Synthetic Androgens are given to women?
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develop Secondary Male characteristics
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What product is reduced in the urine due to taking Synthetic Androgens? What is the cause?
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Urinary Nitrogen
Increased protein synthesis or decreased protein breakdown |
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When would Synthetic Androgens be used in boys?
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as a growth stimulator in boys with delayed puberty
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List 5 uses of Synthetic Androgens in treating women
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1. Postpartum breast engorgement
2. Endometriosis 3. Endometrial bleeding (& to enhance libido) after menopause 4. Postmenopausal Osteoporosis (alone or combined with estrogens) 5. Chemotherapy of Premenopausal breast tumors |
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Give 3 situations in which Synthetic Androgens would be used as a protein anabolic agent to reverse protein loss
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1. after trauma
2. after surgery 3. prolonged immobilization |
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What are the possible adverse effects of Anabolic Steroid abuse?
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1. suppress endogenous Testosterone
2. suppress Sperm production 3. may cause Gynecomastia 4. may cause Virilization |
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What are 2 possible adverse effects if Synthetic Androgens are given to elderly males to replace low androgen levels
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1. may worsen Benign Prostatic Hyperplasia
2. increase risk of Prostate CA |
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What are the adverse effects of Synthetic Androgens in Women?
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1. Acne
2. Hirsutism 3. Amenorrhea 4. Clitoral enlargement 5. deep voice 6. ALTER SERUM LIPIDS TO INCREASE ATHEROSCLEROTIC SUSCEPTIBILITY |
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What are the adverse effects of Synthetic Androgens in Men? (6)
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1. Acne (nathan)
2. Sleep apnea 3. Erythrocytosis 4. Gynecomastia 5. Azoospermia 6. decreased testicular size = due to decreased Gonadotropin secretion (FSH/LH) |
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List 2 Gonadotropin-releasing hormone (GnRH) analogs used for gonadal suppression in treatment of Prostatic Cancer
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Gose-relin
Leu-prolide |
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Antifungal imidazole used to inhibit adrenal and gonadal steroid synthesis to treat Cushing's disease (adrenal) and Prostate Cancer (gonadal)
What is it's mechanism of action? |
Ketoconazole
inhibits Desmolase |
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5-alpha-reductase inhibitor that reduces conversion of Testosterone to Dihydrotestosterone
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Fin-asteride
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What is Finasteride used to treat?
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Benign Prostatic Hyperplasia
**5-alpha-reductase inhibitor |
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3 non-steroidal competitive inhibitors of androgens (anti-androgens) used to treat PROSTATIC CARCINOMA
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F-lutamide
Bica-lutamide Ni-lutamide |
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Aldosterone antagonist used clinically as a potassium-sparing diuretic, also lowers 5-alpha-reductase activity to lower plasma levels of Testosterone & Androstenedione
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Spironolactone
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Cottonseed derivative used as a male contraceptive in China
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Gossypol
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2 major constituents of Bone
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Calcium & Phosphate
**bones contains 98% of total body Ca++; 85% of total body Phosphate |
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Which has higher intestinal absorption, phosphate or calcium?
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Phosphate
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Larger amounts of ______ are present in bone and reabsorbed by the Kidneys
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Calcium
**more calcium is present in bone; more calcium is reabsorbed in the kidney as compared to Phosphate |
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Calcium enters the body only through the __1__ resulting in daily absorption of about __2__. An obligatory loss of 150 mg/day occurs in __3__ & __4__ secretions, and in sloughed __5__ cells
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1. intestine
2. 300 mg 3. mucus 4. biliary 5. intestinal |
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What accounts for a fecal loss of 650 mg/day of Calcium?
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1. mucosal + biliary secretions & sloughed intestinal cells = 150 mg
2. redisual 500 mg remaining from the unabsorbed intake (800 mg intake; 300 is absorbed) |
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What is urinary excretion of Ca++ determined by?
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Tubular reabsorption
-highly efficient = more than 98% of the 9 g filered daily is reabsorbed |
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What are the prinipal regulators of Calcium bone homeostasis?
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1. PTH
2. Vitamin D |
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What is the primary function of PTH?
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to keep Ca++ concentration in the extracellular fluid constant
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What is the plasma half-life of PTH?
How is it removed from the body? |
2-5 min
hepatic and renal clearance |
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What influences the secretion of PTH from the parathyroid gland?
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low Ca++ = secretion of PTH
high Ca++ = inhibition of PTH secretion |
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In what 2 ways does PTH increase the plasma concentration of Ca++
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1. increase Bone resorption = increase Ca++ mobilization
2. increase reabsorption of Ca++ in Kidneys |
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List the 6 preparations of Vitamine D
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Calci-fed-iol
Calci-triol Chole-calci-ferol **Dihydro-tachy-sterol** Doxy-calci-ferol Ergo-calci-ferol |
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What are the sources of Vitamin D?
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1. formed in skin by UV radiation
2. Plants |
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Intrinsic and dietary forms of Vitamin D are inactive precursors that have to be converted to active metabolites of which _______ is the most active
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Calci-triol
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In what 3 ways does Vitamin D regulate Ca++ homeostasis?
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1. increase bone resorption
2. kidneys to increase tubular reabsorption 3. small intestines to increase Ca++ absorption |
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What does deficiency of Vitamin D in children cause?
In adults? |
Children = Rckets
Adults = Osteomalacia |
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The only regulator affecting intestinal Ca++ absorption
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Vitamin D
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Hormone secreted by Parafollicular cells (C cells) in the Thyroid when serum Ca++ is high
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Calcitonin
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What is the action of Calcitonin? How does it achieve it?
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Lowers serum Ca++
inhibits Osteoclastic bone resorption; reduces tubular reabsorption of Ca++ & phosphate |
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What 3 diseases is Calcitonin used to treat?
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1. Paget's disease = excessive breakdown & formation of bone tissue
2. Hypercalcemia 3. Osteoporosis |
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How do Glucocorticoids affect Ca++ homeostasis? (2)
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1. antagonize Vitamin D-stimulated intestinal Ca++ absorption
2. stimulate renal Ca++ excretion **ultimately cause decreased body Calcium |
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What do Glucocorticoids block the synthesis of in bone?
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Collagen synthesis
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What 3 conditions are Glucocorticoids used to treat in regards to Mineral Homeostasis?
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1. to reverse Hypercalemia in Lymphomas
2. Sarcoidosis (has hypercalcemia due to elevated conversion of vitamin D to its active form in Epithelioid macrophages) 3. Vitamin D intoxication |
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How do Estrogens prevent accelerated bone loss?
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act by decreasing PTH-induced bone resorption
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Are Estrogens more effective in preventing or restoring bone loss?
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PREVENTING
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Used for treatment or prevention of Postmenopausal Osteoporosis
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Estrogens
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What is the ending for all Pyrophosphate analogs of Bisphosphonates?
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-DRONATE
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What is the mechanism of action of the -DRONATE's?
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Bisphosphonate pyrophosphate analogs
Act by retarding formation & dissolution of hydroxyapatite crystals in the skeleton = decrease bone resorption |
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What is the adverse effect of the -Dronate's?
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Gastric irritation
**< 10% of oral doses is absorbed |
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What are the -Dronate's used clinically to treat?
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1. Hypercalcemia associated with malignancy (bone metastases)
2. Osteoporosis 3. Syndromes of ectopic calcification 4. Paget's disease = enlarged & deformed bones |
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Diuretic used to treat HypercalciURIA
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Thiazides
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Explain why Thiazides are used to treat HypercalciURIA
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1. block sodium reabsorption in distal tubule
2. increase Calcium-sodium exchange in basolateral membrane 3. Increase Ca++ reabsorption = reduced renal excretion |
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Cytotoxic antibiotic used for treatment of Paget's disease and Hypercalcemia
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Plica-mycin (Mithramycin)
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Define Osteoporosis
Who is it most common in? |
abnormal bone loss predisposing to fractures
Postmenopausal women (but also occurs in older men) |
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Aside from Menopause and aging, what other 5 things can Osteoporosis result from?
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1. Chronic treatment with Glucocorticoids
2. Endocrine disorders such as Thyrotoxicosis or Hyperparathyroidism 3. Malabsorption syndrome 4. Alcohol abuse 5. Idiopathic |
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What is Postmenopausal Osteoporosis due to?
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Estrogen deficiency
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Partial Estrogen Agonist used to prevent Postmenopausal Osteoporosis BUT does NOT affect Endometrium or Breast
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Ralox-ifene
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What is idiopathic Osteoporosis in Elderly men usually treated with?
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Vitamin D & dietary Calcium
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