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Life Cycles Part I > Female Reproductive Pharmacology > Flashcards

Female Reproductive Pharmacology Flashcards

1
Q

Major Functions of the Reproductive Hormones

A
  • faciltate human growth
  • development, maturation and function of the reproductive system
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2
Q

Hormones act via two types of receptors: those that act at [] to modulate gene transcription and those that act at the [].

A

Hormones act via two types of receptors: those that act at nuclear receptors to modulate gene transcription and those that act at the classic G-protein coupled receptors.

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3
Q

The major source of GnRH is released from [].

A

The major source of GnRH is released from the preoptic nucleus.

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4
Q

The modulation of hormones can be done at a number of different levels:

A
  • directly at receptors on target tissues
  • altering the synthesis or breakdown of hormones
  • altering the feedback loops established in areas of the hypothalamus-pituitary axis
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5
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6
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7
Q

[] most potent of the human estrogens used for:

A

17beta-estradiol (estradiol) most potent of the human estrogens used for:

  • Contraceptive agent
  • Hormone replacement therapy
  • PCOS
  • Hirsutism
  • Severe acne
  • Hypogonadism
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8
Q

Estrogen Receptors

A
  • Estrogens act via 2 slightly different nuclear receptors alpha and beta estrogen receptors (αER and βER)
  • And a 3rd G-protein receptor called GPR30
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9
Q

The use of estrogen will [] [] the release of [] and [] preventing ovulation.

A

The use of estrogen will inhibit the mid-cycle surge of gonadotropin secretion from the hypothalamus decreasing the release of LH and FSH preventing ovulation.

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10
Q

Estrogen…what is it good for?

A
  • developmental actions, especially around puberty
  • neuroendocrine control of the menstrual cycle

-regulating the GnRH pulsatile release from the hypothalamus. This GnRH activity of the hypothalamus plays an important role on the gonadotropin cells of the anterior pituitary and the release of FSH (follicle development) LH (ovulation and estrogen levels)

•variety of effects on the reproductive tract

-ovarian function, fallopian tubes function, cervical mucus activity

•f metabolic effects outside of the reproductive tract, but are very important in things like cardiovascular function

-premenopausal women have a significant reduction in the incidence of coronary disease due to estrogen altering lipid function (primarily increase HDL and decrease LDL)

  • healthy bone growh by increasing osteoblast function
  • increased production of nitric oxide that may increase perfusion of organs such as the central nervous system (e.g., menopause with decreased estrogen may cause adverse cognitive effects)
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11
Q

The α-nuclear receptors are largely in the female [] , whereas the β nuclear receptors are found in [,]. The GPR30 receptors are widely distributed in many tissues including the [].

A

The α-nuclear receptors are largely in the female reproductive tracts, the breasts and hypothalamus, whereas the β nuclear receptors are found in brain, bone, heart, lungs intestinal mucosa, endothelial cells and ovarian granulosa cells. The GPR30 receptors are widely distributed in many tissues including the female reproductive organs.

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12
Q

The main estrogen used in contraceptives is [].

A

The main estrogen used in contraceptives is ethinyl estradiol.

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13
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A
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14
Q

Side Effects of Estrogen

A
  • alterations in female reproductive organs (i.e., vaginal bleeding, dysmenorrhea, breast cancer, etc.)
  • cardiovascular effects (i.e., chest pain, DVTs, stroke, etc.)
  • gastrointestinal effects (i.e., nausea, cramps, diarrhea, gastritis, etc.)
  • skin problems (i.e., chloasma, hirsutism, pruritus, etc.)
  • adverse effects on the eyes including retinal vascular thrombosis
  • CNS effects (i.e., headache, migraine, mental depression anxiety, irritability, etc.)
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15
Q

Estrogen based therapy is contraindicated in patients with:

A
  • stroke or prior thromboembolic event
  • estrogen dependent tumor
  • pregnancy
  • hypertriglyceridemia
  • smokers >35YO
  • should be avoided in women with migraines with aura and/or poorly controlled hypertension.
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16
Q

Progestin is a synthetic molecule that mimics the [] of the body.

A

Progestin is a synthetic molecule that mimics the endogenous progesterones of the body

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17
Q

Physiological actions of progestin’s will:

A
  • shut off the GnRH pulse
  • hypothalamic function
  • decrease FSH and LH release which is crucial for ovulation to occur
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18
Q

Extra reproductive effects of progesterone:

A
  • body temperature regulation
  • increase minute ventilations
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19
Q

Progestin Receptors

A
  • Progestin acts via two slightly different nuclear receptors A and B receptors ( PRA and PRB)
  • They are found in a number of tissues including the female reproductive system and hypothalamus however, much less is known about the progesterone receptor function and locations as compared to estrogen receptors.
  • Progestin compounds are also metabolized by the liver and can be given by multiple routes similar to estrogen compounds.
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20
Q
A
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21
Q

When would a patient need Progesterone only contraceptive pills (POCP)?

A
  • breast-feeding women, smokers over the age of 35 and some women with migraines.
  • Effectiveness varies and is not as reliable as the COCP with periods often becoming irregular.
  • Contraceptive injections of Progesterone only (Depo-Provera®, Noristerat®) and implants (Nexplanon®) have also been used with much more effectiveness than the oral form lasting a longer period of time.
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22
Q

Mechanism of Action of COCP (Estrogen and Progesterone receptor agonists)

A

•cause the Suppression of ovulation by causing a negative feedback to HP axis

  • Decreased frequency of GnRH pulses
  • Suppression of LH and FSH production
  • Inhibition of mid-cycle LH surge, suppression of ovulation

•As well as, Thickening of cervical mucus preventing sperm entry to upper genital tract (more due to progestin products)

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23
Q

Ethinyl Estradiol

A
  • Estrogen receptor agonist

•Often the estrogen found in birth control combined with progesterone

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24
Q

Ethinyl Estradiol Side Effects

A
  • Nausea
  • vomiting
  • cramps
  • headache
  • breast tenderness
  • change in sexual desire
  • mid-cycle (breakthrough) bleeding/spotting
  • increase CV events (thrombi)
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25
Q

Ethinyl Estradiol Contraindications

A
  • ER-positive breast cancer
  • history of DVTs
  • high blood pressure
  • high cholesterol
  • hypertriglyceridemia
  • diabetes
  • smokers >35YO
  • women with migraines with aura
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26
Q

Mestranol

A
  • Prodrug of Ethinyl Estradiol
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27
Q

Diethylstilbestrol (DES)

A
  • Estrogen receptor agonist
  • NO LONGER USED AS OC!
  • advanced androgen-dependent prostate cancer
  • advanced breast cancer in postmenopausal women
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28
Q

Diethylstilbestrol (DES) Side Effects

A
  • vaginal and breast cancer
  • teratogen
  • “DES daughters & sons” with abnormalities of the vagina, cervix, uterus & fallopian tubes, low sperm count, CNS disorders
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29
Q

Progesterone analogs (Norethindrone, Norgestrel, Ethynodiol Diacetate-Continuin® , Drospirenone–Yasmin® , Gestodone, etc.)

A
  • Progesterone receptor agonist
  • Often the combined with estrogen as oral contraceptives
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30
Q

Progesterone analogs Side Effects

A

•periods often becoming irregular

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31
Q

Progesterone only contraceptive pills (POCP) are for patients with:

A

•breast-feeding women, smokers over the age of 35 and some women with migraines

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32
Q

Progesterone only contraceptive pills (POCP) Side Effects

A
  • Effectiveness varies
  • irregular periods
  • GI disturbances contraceptive injections of
  • Progesterone have been used with much more effectiveness than the oral form lasting a longer period of time.
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33
Q

Hormone Replacement Therapy (HRT)

A
  • These include many differing doses of synthetic estrogen and progesterone combinations
  • Mechanism of action (Estrogen and Progesterone receptor agonists) Suppression of hot flashes, osteoporosis, vaginal atrophy, hypogonadism
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34
Q

Hormone Replacement Therapy (HRT) Side Efffects

A
  • same as for oral contraceptives
  • unopposed estrogen increases the risk of endometrial cancer
35
Q

Treatment for Hypogonadism

A

•Ethinyl Estradiol or Mestranol

  • Estrogen receptor agonists
36
Q

Day After Pills Plan B

A

1) Progesterone analogs (Norethindrone, Norgestrel, Ethynodiol Diacetate, Drospirenone, Gestodone, etc.)

•Progesterone receptor agonist (High Dose)

  • Approved in the prevention of pregnancy in the “day after” or referred to as “Plan B”.

•Side effects - GI disturbances, headache, menstrual changes, and visual disturbances.

2) Ulipristal (Ella®) Selective Progesterone Receptor Modulator (SPRM) (PR antagonist/agonist)
- Postpones follicular rupture delaying ovulation and delaying the maturation of the endometrium

37
Q

Mifepristone (RU-486®)

A
  • Termination of intrauterine pregnancy
  • Progesterone receptor antagonist Causes contraction of the myometrium terminating pregnancy
  • Side effects - heavy bleeding, uterine cramping/pain, GI effects such as nausea/vomiting and anorexia
  • often used with Misoprostol (Cytotec®), a PGE1 receptor agonist that induces contractions of the uterus. Often causes diarrhea and other unwanted GI effects
38
Q

Misoprostol

A
  • Induction of Labor
  • a synthetic prostaglandin (PGE1 receptor) agonist.
  • induces uterine contraction and causes cervical dilation
39
Q

Dinoprostone

A
  • Induction of Labor
  • a synthetic prostaglandin (PGE2 receptor) agonist
  • induces uterine contraction and causes cervical dilation
  • Side effects – Diarrhea, GI disturbances, excess uterine bleeding
40
Q

Oxytocin

A
  • Induction of Labor
  • A oxytocin receptor agonist causes uterine contraction, NOT indicated for elective induction of labor, but is indicated for the improvement of uterine contractions (often used with Ergonovine to decrease heavy bleeding after vaginal delivery and placenta delivery )
  • Side effects – excessive contraction of the uterus that can risk the health of the baby and lead to rupture of the uterus as well as cardiovascular risks
41
Q

Tocolytics

A

•slowing uterus contraction

42
Q

Terbutaline

A
  • Inhibition of Preterm Labor (tocolytic)
  • β2-adrenergic receptor agonist Inhibits uterine contraction
  • Side effects – tachycardia (also in seen fetus), nervousness, tremors, headache, hyperglycemia (also seen in fetus) and pulmonary edema. Pregnant women should NOT be given injections long-term (beyond 48–72 hours), and should not be given oral terbutaline for any type of prevention or treatment of preterm labor “due to of the potential for serious internal heart problems and death
  • Additional indication? for Asthma (fast acting bronchodilator)
43
Q

Nifedipine

A
  • Inhibition of Preterm Labor (tocolytic)
  • L-type calcium channel antagonist, Inhibits uterine contraction
  • Side effects- Low blood pressure, lightheadedness, headache, leg swelling, shortness of breath, potential heart failure
  • Additional indication? Inhibition of Preterm Labor (tocolytic) for angina and high blood pressure
44
Q

Magnesium sulfate

A
  • Inhibition of Preterm Labor (tocolytic)
  • alters neurochemical transmission and muscular excitability.
  • Magnesium sulfate remains the drug of choice for seizure prophylaxis in severe preeclampsia and for control of seizures in eclampsia
45
Q

Preeclampsia

A

-pregnancy complication characterized by high blood pressure, signs of damage to another organ system, (i.e., liver & kidneys)

46
Q

Eclampsia

A

•severe complication of preeclampsia - high blood pressure results in seizures during pregnancy

47
Q

Atosiban

A

•Oxytocin Receptor Antagonist (NOT in US yet – but soon)

48
Q

Clomiphene

A
  • Infertility
  • selective estrogen receptor modulators (SERMs), (mixed agonist/antagonist)
  • Inhibits endogenous estrogen acting at estrogen receptors in the hypothalamus and pituitary preventing the normal feedback – increasing LH and FSH release from the anterior pituitary- increasing ovulation and fertility.
  • Side effects - hot flashes, ovarian enlargement, multiple gestation pregnancy and visual disturbances.
49
Q

Leuprolide

A
  • Infertility
    • GnRH analog agonist when given in pulsatile fashion; stimulates the release of LH and FSH, increasing ovulation and likelihood of fertility
  • Side effects - nausea, vomiting, antiandrogen effects and menopausal symptoms
  • Additional Indications? Precocious Puberty = puberty occurring at an unusually early age continual Leuprolide acts here by shutting down estrogen flow
  • Prostate cancer
50
Q

Additional GnRH long-acting agonists include:

A
  • Goserelin (Zoladex®)
  • Histrelin (Vantas®)
  • Nafarelin (Synarel®)
  • Triptorelin (Decapeptyl®)
  • Side effects - hot flashes, vaginal dryness, headaches, mood changes, and decreased libido, ED
51
Q

human chorionic gonadotropin (hCG)

A
  • Infertility
    • stimulates the release of the egg during ovulation. hCG acts at the luteinizing hormone receptor of the ovary promoting the maintenance of the corpus luteum at the beginning of pregnancy. The corpus luteum secretes progesterone that enriches the uterus to sustain a growing fetus.
  • hCG is often used in combination with urofollitropin (Bravelle®, Fertinex®) to help promote the development of follicles (eggs) by the ovaries. Urofollitropin and follitropin are forms of FSH and act at the FSH receptor – Urofollitropin is purified urinary FSH (typically from urine of menopausal women) and follitropin is a recombinant preparation
  • Side effects - fatigue, irritability, depression, fluid buildup (edema), and swelling of the breasts in boys and men (gynecomastia), blood clot formation (thromboembolism) and carcinogenesis Infertility L
52
Q

Tamoxifen and Raloxifene - selective estrogen receptor modulators (SERMs)

A
  • treatment of breast cancer
  • mixed agonist/antagonist for the estrogen receptors depending on the receptor expressed in certain tissue
  • act as antagonists in breast tissue hence decreasing estrogen+ breast cancer proliferation
  • act as agonist at estrogen receptors in the bone, increasing bone density and can be prescribed for osteoporosis.
  • Side effects -increased risk of endometrial cancer (agonist at estrogen receptors on endometrial tissue)(Tamoxifen>Raloxifene), hot flashes, flushing, fatty liver, reduced cognition and increase risk of blot clots.
  • Contraindications -lactating women, pregnant or may become pregnant, history of DVT or pulmonary embolism
53
Q

Fluvestrant

A
  • treatment of breast cancer
  • pure estrogen receptor antagonist (injectable) used for breast cancer when there is a lack of response to other drugs in postmenopausal women.

•Side effects –GI disturbances, flushing, headaches, pain and swelling, difficulty in breathing, sleep disturbances,

54
Q

Anastrozole (reversible), Letrozole (reversible) and Exemestane (irreversible)

A
  • Aromatase inhibitors used in postmenopausal women with breast cancer.
  • Mechanism of action

-Inhibits conversion of testosterone or androstenedione into the estrogen analogs, hence decreasing estrogen.

•Side effects - include hot flashes, nausea and vomiting.

55
Q

Synthetic Estrogen and Progesterone

A

•Hirsutism, Polycystic Ovarian Syndrome (PCOS) and Acne in Women

56
Q

Spironolactone

A
  • Hirsutism, Polycystic Ovarian Syndrome (PCOS) and Acne in Women
  • antagonist at androgen receptors to block androgens
  • Side effects - gynecomastia, breast pain, hyperkalemia and urinary frequency (since it is also an aldosterone antagonist) impotence, ataxia and menstrual irregularities.
57
Q

Ketoconazole

A
  • inhibits the 17, 20 lyase (also called CYPc17, or 17, 20 desmolase) (antifungal activity - as taught in the I&I Block)
  • Decreases steroids including testosterone, DHT and estrogen analogs.
  • Side effects - nausea, vomiting, diarrhea, rash, headache, thrombocytopenia, gynecomastia and hepatotoxicity, as well as “drugdrug interactions by the inhibition of CYPs in the liver
58
Q

Metformin

A
  • suppressing liver glucose production via activation of AMP-kinase
  • (PCOS is correlated with insulin resistance –which often causes increases in GnRH pulses leading to increases in more LH vs. FSH and causing the ovaries to make more androgens) (Studies show metformin can decrease androgen production)
59
Q

Progesterone analogs & Danazol (a modified progesterone that has a number of sites of action)

A
  • Endometriosis & Amenorrhea
  • displace testosterone from SHBG-increasing testosterone
  • decrease LH surge
  • decrease estradiol prescribed for endometriosis but limited due to its masculinizing side-effects.
60
Q

Anastrozole and Exemestane

A
  • Endometriosis & Amenorrhea
  • aromatase inhibitors (Indication for endometriosis)
  • inhibit the synthesis of estrogens

•Side effects – masculinizing effects, hot flashes, elevation of liver enzymes, mood changes, weight gain,

61
Q

Elagolix

A
  • Endometriosis & Amenorrhea
  • a GnRH antagonist (Indication for endometriosis)
  • Side effects- decrease in BMD, hot flashes, nausea, insomnia, suicidal thoughts
62
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68
Q

A 50-YO woman with a high risk of breast cancer is started on tamoxifen for prophylaxis. What is the main mechanism of action of this drug?

a) Blocks estrogen receptors in breast tissue
b) Blocks estrogen receptors in the endometrium
c) Increases the risk of osteoporosis
d) Raises plasma LDL cholesterol and total cholesterol, lowers HDL
e) Reduces the risk of thromboembolic disorders

A

a) Blocks estrogen receptors in breast tissue

69
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76
Q

Methyltestosterone

A
  • an androgen receptor agonist, is used for hypogonadism, delayed onset of puberty by promoting secondary sex characteristics and can be used for impotence.
  • can be used in females with estrogen positive breast cancer again by a number of effects including the reduction in the production of estrogen by negative feedback. Common side effects include amenorrhea and other menstrual irregularities.
77
Q

Ethinyl Estradiol, Diethylstilbesterol (DES) or Mestranol

A
  • hypogonadisim in females, prostate cancer in males
  • These all bind the estrogen receptors as agonists and are used to treat hypogonadism, ovarian failure and contraception. These same drugs can also be used in males with androgendependent prostate cancer by a number of effects including the reduction of LH release by a negative feedback on the pituitary and hypothalamus resulting in the reduction of testosterone production.
78
Q

Finasteride

A
  • BPH
  • inhibits androgen production by inhibiting 5α-reductase, the enzyme responsible for converting testosterone to dihydrotestosterone. Dihydrotestosterone (DHT) is 3 times more potent than testosterone at the androgen receptor, hence blocking the production of DHT results in a significant decrease in androgen receptor effect on the prostate hyperplasia.
  • Finasteride is also prescribed for male-pattern baldness since testosterone is more likely to increase hair growth versus DHT. The hair follicles are affected differently based on the androgen (testosterone vs DHT) and other factors (i.e., IGF-1, TGFβ, etc.) present.
  • Side effects include a decreased libido, decreased ejaculate volume, gynecomastia, testicular pain and in some cases depression and anxiety.
79
Q

Flutamide

A
  • an androgen receptor antagonist that is used for metastatic prostate cancer.
  • Side effects include gynecomastia, GI upset and mild liver damage.
  • Bicalutamide (Casodex®, Cosudex®) acts in the same fashion as flutamide but has less side effects including no liver damage.
80
Q

Ketoconazole

A
  • antifungal but also prostate carcinoma
  • inhibiting the synthesis of steroids
  • Ketoconazole inhibits the 17, 20 lyase (also called CYPc17, or 17, 20 desmolase) enzyme therefore decreasing the following steroids including testosterone, DHT and estrogen analogs.
  • Side effects include nausea, vomiting, diarrhea, rash, headache, thrombocytopenia, gynecomastia and hepatotoxicity, as well as “drug-drug interaction” by the inhibition of CYPs in the liver.
81
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A
82
Q

Degarelix

A
  • a GnRH antagonist approved for the treatment of symptomatic advanced prostate cancer.
  • This antagonist can reduce levels of gonadotropins and androgens more rapidly than the GnRH agonists and avoid the testosterone surge seen with GnRH agonist (i.e., Leuprolide) therapy.
83
Q

Sildenafil, Vadenafil, Tadalafil

A
  • ED
  • These drugs inhibit phosphodiesterase-5 resulting in the increase in cGMP in the smooth muscle relaxation in the corpus cavernosum of the penis. This causes an increase in blood flow resulting in penile erection.
  • Side effects include headache , flushing, dyspepsia, impaired blue-green color vision, hypotension, GI disturbances.
  • Contraindicated with patients taking nitrates.
84
Q

Alprostadil

A
  • ED
  • a PGE1 agonist can be used in men that do not respond to sildenafil or similar drugs. Alprostadil causes the relaxation of smooth muscle allowing blood vessels to dilate. It has to be injected directly into the cavernosa or placed in the urethra as a mini-suppository, from which it diffuses into the cavernosal tissue.

Life Cycles Part I (24 decks)

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