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77 Cards in this Set
- Front
- Back
What two types of hormones are we concerned with in pharmacology?
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peptide and steroid
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What are the organs of the endocrine system?
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-hypothalamus/pituitary
-thyroid/parathyroid -pancreas -adrenal gland -testes/ovaries |
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When drugs are used with specific therapeutic goals in mind, how are they used?
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(1) diagnosis
(2) metabolic action (3) effect on reproductive system |
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Endocrine drugs are rarely a cure, instead, what do they do?
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Replace
Antagonize Supplement |
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Describe a peptide hormone.
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-cell signaling is quick (via increase in cAMP or IP3 secondary messengers); more rapid action
-water soluble -given parenterally because easily degraded in the GI tract |
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Describe a steroid hormone.
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-lipid soluble, therefore can co more places
-can go topically, orally or parenteral -works on the cell nucleus to synthesize new proteins (increases mRNA) |
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What affects solubility of a drug?
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the form in which an endocrine drug is prepared as a therapeutic
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What defines the route which a drug is given?
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the form
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What affects absorption of a drug?
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-route of administration
-solubility/insolubility |
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What indirectly affects drug duration?
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absorption
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What is one way to change solubility of a drug?
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prepare as a salt
-insoluble salts increase rate of absorption, but also increase duration -soluble salts - give IV |
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What effect does pharmaceutics have?
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on absorption
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What are ways to alter absorption?
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-change the vehicle used
-change the size of particles (larger the size, decrease drug absorption) |
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What type of hormone do you use if your therapeutic goal is diagnosis? What is your goal by injecting this hormone?
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peptide - injection (many are pituitary hormones)
Goal: to see if organ works |
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Your therapeutic goal is diagnosis - why would you inject ACTH (or its synthetic derivative cosyntropin?
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to see if adrenal cortex works
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Your therapeutic goal is diagnosis - why would you inject ADH (vasoptessin)? Where is ADH normally found?
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-to diagnose and treat diabetes insipidus
-comes from posterior pituitary gland |
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What are three examples of using hormones as a diagnostic agent?
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(1) ACTH
(2) TSH (3) ADH -if you give the drug and the endocrine organ works, then it is not a problem with that organ - more a problem of the pituitary gland |
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What produces parathyroid hormone and calcitonin?
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PTH- parathyroid gland (releases Ca++)
calcitonin-thyroid gland (puts Ca++ back in) |
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What would you use to increase Ca++ levels when they are low?
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-soluble Ca++ salts given IV (Ca++ gluconate)
-PTH is not readily available |
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What would you do to decrease Ca++ levels in the body (like in the case of a neoplasia or rodenticide poisoning)?
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(1) dilute the body with saline
(2) calcitonin (side effects are allergies or decreased side effects) |
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Why would an animal have high Ca++ levels?
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neoplasia or
toxicosis caused by the rodenticide cholecelciferol |
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Name two metabolic and antimetabolic actions (ions) in vet med?
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(1) Ca++ equilibrium
(2) Iodine metabolism |
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What is the role of iodine?
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Helps make thryoid hormone
-this plays a role in maintaining the: (1) CNS (2) skin (3) general metabolism |
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Name a T4 thyroid drug we use to treat hypothyroidism.
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levothyroxine - this is a prodrug therefore requires an active liver to become active
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Compare T3 and T4.
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T3= very short half life and is much more potent than T4 (4X) (microgram doses); dose more often
T4=has a longer half life, it is a prodrug, dose less often (mg doses) |
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What species requires a higher dose of thyroid hormone and why?
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canine - due to increased clearance rate
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Describe the pharmacokinetics of thyroid hormone?
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>90% protein bound (much watch what other drugs are used with this)
-metabolized in the liver -p/o administration -fecal elimination -does not have a wide margin of safety |
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When would you use antithyroid drugs and what is the most common species to use it in?
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-use for diseases causing decreased weight and increased activity (hyperthyroidism)
-used in cats a lot |
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What radioactive isotope could you use to treat hyperthyroidism?
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Iodine 131
-decreases both size of thyroid and release of thyroid hormone |
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What compound (not radioactive) could you use to treat hyperthyroidism?
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thioamides (methimazole)
-it prevents I going to T4 and thus decreases synthesis of thyroid hormones |
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Which route would you normally administer an thioamide? What are the side effects of this drug?
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PO (topical is questionable)
-side effect is vomiting, lethargy and immune mediated anemia |
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What cells make insulin and glucagon?
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insulin = beta
glucagon = alpha |
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What forms can diabetes mellitus be in ?
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type1: insulin dependent (usually dogs); beta cells don't work
type2: insulin independent (usually cats) |
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How would a vet treat type I vs. type 2 diabetes mellitus?
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the same - treat with insulin (humans treat type 2 differently)
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What is the difference in the way diabetes mellitus is managed in humans vs. animals?
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humans - managed in a narrow range
animals - range is not as important as owner ease of care b/c animal does not live as long |
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What is the difference between human insulin and vet insulin?
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Human: products are rapid absorption and short duration (for closer management); has a human protein; larger concentrations (100 U/ml)
Vet: products are long acting; porcine source; concentrations are (40 U/ml) |
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What are insulin suspensions made with to make them longer acting?
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-protein and zinc
-takes longer to absorb therefore they last longer |
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What is the duration of a short-acting insulin? How are these given?
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-lasts 1-5 hours
-onset to peak is 1/6 - 1.5 hours -given IV or SubQ |
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What is the duration of a intermediate-acting insulin? How are these given?
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-lasts 18-24 hours
-onset to peak is 1-12 hours -given SC once or twice daily |
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What is the duration of a long-acting insulin? How are these given?
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-lasts 20-24 hours
-onset to peak is 1-8 hours -given SC once daily |
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How is hypoglycemia treated?
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with glucagon - has quick onset (1 min)and short duration (20 min)
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What happens when an overdose of insulin is given and you have hypoglycemia?
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-rapid onset
-CNS: weakness, confusion, convulsions, psychoses -SKIN: moist, pallid OTHER: shallow, rapid breathing |
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What happens to an animal in a diabetic coma (hyperglycemia?
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-gradual onset
-CNS: drowsy, dim vision -SKIN: dry, flushed OTHER: acetone breath, thirst, rapid pulse, air hunger |
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Why would you give an animal glucagon?
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-used to treat hypogylcemia due to insulin overdose or shock
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What is caused by hypo activity of the adrenal gland?
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Addison's disease
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What is caused by hyper activity of the adrenal gland?
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Cushings Disease
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What are glucocorticoids used for?
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(1) membrane stabilizers
(2) Anti-inflammatory (3) immune suppression (4) promotion of gluconeogenesis (5) cerebral edema (6) neoplasia (7) aid parturition in the bovine |
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What are some adverse effects of glucocorticoids when given?
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(1) immune suppression
(2) GI irritation (3) adrenal suppression (4) catabolic changes - a dog that has Cushings (too much glucocorticoids) changes the way fats and proteins are used in the body (5) behavioral effects (6) cateracts |
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How can glucocorticoids be administered?
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oral, injection, topically
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Why would you want glucocorticoids over mineralocorticoids?
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Na retention
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What are two natural glucocorticoids?
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-cortisone - the pro drug therefore need an active liver
-hydrocortisone (cortisol) |
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What four things are necessities as part of the structure of glucocorticoids?
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(1) =O at (C-3)
(2) double bond at (C-4 to C-5) (3) -OH (or =O if a prodrug) at (C-11) (4) -OH basic steroid at (C-21) |
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What are the two shot acting glucocorticoid drugs? What is their length of action? Which one is the pro-drug and what does it look like?
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hydrocortisone (C11= -OH)
cortisone - the pro-drug (C11=O) -lasts 8-12 hours |
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What does an additional bond between (C1-C2) on a glucocorticoid mean? (3 things)
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(1) increase glucocorticoid effect, decrease mineralcorticoid effect
(2) increase duration of action because it is a foreign compound (3) increase potency (can use a lower dose) |
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What drugs have an additional double bond on the glucocorticoid? What is their duration of action?
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-prednisone (with =O on C11) - Pro Drug
-prednisolone (with =OH on C11) -duration of action is 12-36 hours |
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What does adding a F on C-9 of a glucocorticoid do?
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-increases the potency, therefore you can decrease the dose
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What does adding a -CH3 on (C-16) of a glucocorticoid do - on top of the double bond between C1-C2?
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increases the action of glucocorticoids even more than the others; increases the duration of action even more
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Where would you add a F on a glucocorticoid?
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C-9
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Where would you add an CH3 on a glucocorticoid?
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C-16
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Name the two long-acting drugs we are concerned with as glucocorticoids? What is their duration of action?
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-dexamethasone
-betamethasone -24-72 hours |
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What bonds does dexamtheasone have?
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-all the bonds a glucocorticoid should have (4) with an OH at (C-11)
-a double bone at (C1-C2) -a F at C-9 -A CH3 at (C-16) |
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As the glucocorticoids get to be longer lasting, what happens?
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-duration of action increases
-potency of glucocortiocids increases -potency of mineralcorticoids decreases |
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Name two soluble salts.
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succinate and phosphate salts
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IV preparations should be in what type of form?
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solutions
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Are suspensions or solutions more slowly absorbed?
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suspensions - therefore they last longer
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How are glucocorticoids metabolized?
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-by microsomal enzymes - cytochrome P450 for oxidation to active C11-OH
-glucaronidation |
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What type of salt would you use for a topical glucocorticoid?
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insoluble salt
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What are the species differences in half life for glucocorticoids?
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Horse (1/2 hr) < dog (2 hrs) < man (3 hrs) <cow (6 hrs)
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What do you use mineralcorticoids to treat? What drug would you use?
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Addision's Disease
-cortisone |
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What disease would you use adrenocorticoid antagonists to treat?
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Cushings Disease
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What do adrenocorticoid antagoinists do?
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(1) decrease synthesis OR increase biotransformation
(2) cytotoxic action (3) MAO-B inhibitor that decreases dopamine and shuts of ACTH |
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What drug is often used to increase milk production in cows?
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growth hormone (somatotropin)
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What type of compounds are steroids?
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C-III
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Is testosterone highly protein bound?
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YES
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What is testosterone (steroids) mainly used for?
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debilitating diseases, but high chance for abuse by athletes
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What are some long term effects and problems associated with the use of androgens?
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-C-III record keeping, human abuse
-damage to liver and germ cells -change in lipid metabolism and electrolyte balance (Na retention) -dermal effects |
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What are two antiandrogens.
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estrogen, GnRH
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