Reproductive/Endocrine Flashcards by Jasmine Carter

GnRH analog with agonist properties when used in pulsatile fashion; antagonist
properties when used in continuous fashion
(downregulates GnRH receptor in pituitary
􀁰that decreases 􀁲 FSH/LH).

Leuprolide

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What drug causes transient increase in pituitary LH secretion; which leads to a rise in testosterone levesl; continuous use will suppress LH release and leads to a decrease in testosterone levels

Leuprolide

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Antagonist at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and
increases􀁱 release of LH and FSH from pituitary, which stimulates ovulation

clomiphene

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Antagonist at breast; agonist at bone, uterus; increased􀁱 risk of thromboembolic events and endometrial
cancer.

tamoxifen

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Antagonist at breast, uterus; agonist at bone; increased risk of thromboembolic events but no increased risk
of endometrial cancer (

raloxifene

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Anastrozole, letrozole, exemestane are examples of:

aromatase inhibitors

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Inhibit peripheral conversion of androgens to estrogen.

aromatase inhibitors

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Used for relief or prevention of menopausal symptoms (eg, hot flashes, vaginal atrophy),
osteoporosis ( increased estrogen, decreased􀁲 osteoclast activity).

Unopposed estrogen replacement therapy ; increased 􀁱 risk of endometrial cancer, so progesterone is added.

Possible increased cardiovascular risk.

hormone replacement therapy

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Agonists at androgen receptors

testosterone, methyltestosterone

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5α-reductase inhibitor (􀁲decreases conversion of
testosterone to DHT).

Used for BPH and malepattern
baldness.

Finasteride

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Inhibits steroid binding, 17α-hydroxylase, and

17,20-desmolase.

Spironolactone

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Inhibits steroid synthesis (inhibits

17,20-desmolase).

Ketoconazole

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Nonsteroidal competitive inhibitor at androgen

receptors. Used for prostate carcinoma.

Flutamide

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α1-antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective for α1A,D receptors (found on prostate) vs vascular α1B receptors.

tamsulosin

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Direct arteriolar vasodilator.

minoxidil

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used to treat androgenic alopecia

minoxidil

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Sildenafil, vardenafil, tadalafil are examples of:

phosphodiesterase type 5 inhibitors

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Inhibit PDE-5 which increases􀁱 cGMP and causes􀁰 prolonged
smooth muscle relaxation in response to NO which increases􀁱 blood flow in corpus cavernosum of penis,
and decreases pulmonary vascular resistance.

phosphodiesterase type 5 inhibitors

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Risk of life threatening hypotension in patients taking nitrates

phosphodiesterase type 5 inhibitors

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Synthetic androgen that acts as partial agonist at androgen receptors.

danazol

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MC SE of danazol

decreased HDL levels and hepatoxicity

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β2-agonists that relax the uterus; used to decrease 􀁲 contraction frequency in women during labor.

terbutaline, and ritodrine

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Produces local inflammatory reaction toxic to sperm and ova, preventing fertilization and implantation; hormone free.

copper IUD

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Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge 􀁰 no
LH surge 􀁰 no ovulation.

Combined contraception

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Competitive inhibitors of progestins at progesterone receptors.

Mifepristone, ulipristal **Termination of pregnancy (mifepristone with misoprostol); emergency contraception (ulipristal)

Bind progesterone receptors, 􀁲 decreased growth and 􀁱 increased vascularization of endometrium, thicken cervical mucus.

progestins (Levonorgestrel, medroxyprogesterone, etonogestrel, norethindrone, megestrol, and many others when combined with estrogen)

MOA: work by suppressing pituitary LH secretion and subsequently decreasing ovarian androgen production.

Oral contraceptives

inhibition of phospholipase A2, and inhibition of | transcription factors such as NF-κB.

glucocorticoids

Sensitizes Ca2+-sensing receptor (CaSR) in parathyroid gland to circulating Ca2+ which decreases 􀁲 PTH.

cinacalcet

Synthetic analog of aldosterone with little glucocorticoid effects.

fludrocortisone

ADH antagonist (member of tetracycline family)

democycline

Propylthiouracil (PTU), methimazole are examples of

Thionamides

Inhibit oxidation of iodine to iodine by thyroid peroxidase

Thionamides

Inhibit iodination of tyrosyl resides (organification) on thyroglobulin to form MIT and DIT

Thionamides

Inhibiting coupling of MIT and DIT to form T3 and T4

Thionamides

Inhibit proteolytic release of T3 and T4 from thyroglobulin

High doses of iodide

inhibit conversion fo T4 to T3 via 5` deiodinase in peripheral tissues

Propranolol and Propylthiouracil (PTU)

Acromegaly, carcinoid syndrome, gastrinoma, glucagonoma, esophageal varices.

Somatostatin analog (octreotide)

What is a multifunctional enzyme responsible for catalyzing the oxidation of iodide, the iodination of thyroglobulin and the coupling reaction between 2. iodized tyrosine residues?

thyroid peroxidase

What removes the iodine groups from MIT and DIT for recycling?

iodotyrosine deiodinase

uptake of iodide from the blood is an energy dependent process carried out by?

the na-iodide symporter ; TSH stimulates this uptake and competitively inhibited by perchlorate and pertechnetate

What drug is 40% iodide by weight, thus can cause a number of alterations to thyroid function? IT can cause hypothyroidism due to decreased production of thyroid hormone. or hyperthyroidism by increasing thyroid hormone synthesis or destructive thyroiditis

Amiodarone

decrease androgen aromatization

aromatase inhibitors

decrease androgen synthesis

ketoconazole

decreased follicular cell stimulation

continuous GnRH stimulation by long acting GnRH analogs (ex. goserelin) suppresses LH and FSH release;d creating production of estrogens in the ovarian follicle.

decrease thyroid hormone synthesis by inhibiting thyroid peroxidase

PTU and methimazole

The most likely biochemical target of pioglitazone is:

intracellular nuclear receptor

Which selective estrogen receptor modulator inhibits the effects of estrogen on breast tissue and is effective for prevention and treatment of gynecomastia in patients on ADT?

Tamoxifen

The glucose lowering effects of TZDs requires __________________and protein synthesis, it takes several days to a few weeks after commencing TZd to observe significant results

alteration in gene transcription AKA transcription modulation

Glucocorticoids cause an increase in what organ's protein synthesis ?

Liver protein synthesis ; by increasing hepatic glycogenesis and gluconeogenesis

An increase in estrogen activity (raises or lowers) circulating ____ levels?

raises circulating TBG levels; so there will be an increased total T4 pool.

impairs ligand receptor binding?

flutamide

Decreased leydig cell stimulation by LH

leuprolide, goserelin, nafarelin, histrelin

Decrease synthesis of testosterone in the leydig cells of the testis

ketoconazole

Decreased peripheral androgen aromatization occurs with

aromatase inhibitors

3 parts to Hyperthyroidism treatment

Antithyroid drugs, radioactive iodine, surgical thyroidectomy

PTU and methimazole are associated with what SE?

agranulocytosis (absolute neutrophil count less than 500/mL

Check wbc count with differential for what antithyroid drugs?

PTU and methimazole * in patient that present with fever

Administration of what may prevent thyroid absorption of radioactive iodine isotopes by competitive inhibition?

Potassium iodide

anion inhibitors (perchlorate and pertechnetate) work by?

blocking iodide absorption by the thyroid gland via competitive inhibition

Thionamides (methimazole and PTU) work by?

decrease the formation of thyroid hormones by inhibiting thyroid peroxidase

iodide salts work by?

inhibiting synthesis as well as release of thyroid hormones

What occurs as a result of increased testosterone secretion or increased conversion of testosterone to DHT?

Hirsutism

What drug has anti-androgenic properties and is used to treat hirsutism?

spironolactone

Also, used to rx hirsutism are?

flutamide and finasteride

What is a GnRH agonist that causes first a transient increase then a decrease in both testosterone and DHT levels?

Leuprolide

What causes a discordant decease in DHT level?

finasteride

Mifepristone is an example of a?

anti-progestin

Reproductive/Endocrine Flashcards

(68 cards)