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Pharmacology > Repro-Endo: Female Repro > Flashcards

Repro-Endo: Female Repro Flashcards

1
Q

Mechanism of Leuprolide?

A
  • Leuprolide and Goserelin
  • GnRH anolog
  • Pulsatile –> Agonist
  • Continous –>Antagonist
  • -> Downregulates GnRH in Pituitary
  • -> Decrease LH and FSH
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2
Q

Clinical Use of Leuprolide?

A
  • Pulsatile –> Infertility
  • Continous –> w/ Flutamide for 1 wk Testosterone surge.
    • Prostate cancer
    • Uterine Fibroids
    • Endometriosis
    • Polycystic Ovary Syndrome
    • Precocious puberty
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3
Q

SEs Leuprolide?

A
  • Antiandrogen
  • Nausea
  • Vomiting
  • Headache (Light-headedness)
  • Hypoestrogenic state
    • Hot flashes
    • Vaginal dryness
    • Bone density loss
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4
Q

Mechanism of Estrogens?

A
  • Binds to Estrogen Receptors
  • Stimulates Endometrial Growth
  • Reduces LDL, Raises HDL
  • Steroidal: Ethinyl Estradiol and Mestranol
  • Nonsteroidal: Diethylstilbestrol (DES)
  • Natural: Premarin-conjugated estrogens
    • Soy Isoflavones, Red clover, Black cohosh, Vit. E
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5
Q

Clinical use of Estrogen?

A

Females:

  • Birth Control
  • Cycle regulation
  • Hypogonadism
  • Ovarian failure
  • Menstraul abnormalities
  • Hormone Replacement Therapy - post menopausal w/out a History of Breast Cancer
  • Men: Androgen-dependent Prostate cancer
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6
Q

SEs Estrogens?

A
  • Estrogen w/out Progesterone –> Endometrial cancer
  • DES –> Clear Cell Adenocarcinoma
  • Bleeding in the Postmenopausal women
    • Increased Risk of Thrombi (Hypercoagulable)
  • Contraindicated:
    • ER+ Breast cancer and History of DVTs
    • ​Uncontrolled HTN
    • Migraines w/ Aura
    • Smokers > 35 y.om (microthrombi risk)
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7
Q

(3) Selective Estrogen Receptor Modulators (SERMs)?

A
  1. Clomiphene
  2. Tamoxifen
  3. Raloxifene
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8
Q

Mechanism of Clomiphene?

A
  • Estrogen receptors Antagonist in Hypothalamus
  • Prevents normal feedback inhibition
  • -> Increased GnRH
  • -> Increased Release of LH and FSH from Pituitary
  • -> Stimulates ovulation (Increased)
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9
Q

Clinical use of Clomiphene?

A
  • Infertility due to Anovulation
    • PCOS
    • Fertility
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10
Q

SEs of Clomiphene?

A
  • Hot flashes - Temp. Control w/in Hypothalamus
  • Ovarian enlargment
  • Multiple simultaneous pregnancies
  • Visual Disturbances (Blurring, Diplopia)
  • GI and Breast Discomfort (tenderness)
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11
Q

Mechanism of Tamoxifen?

A
  • Partial Estrogen receptor Agonist/Antagonist (SERM)
  • Upregulates TGF-β
  • Must be activated by CYP2D6
    • ​SSRIs (Fluoxetine) inhibit CYP2D6 - contraindicated
  • Antagonist - Breast tissue
  • Agonist - Uterus (Endometrial Tissue) and Bone
    • A/w Endometrial cancer
    • A/w Thomboemboitic events
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12
Q

Clinical use of Tamoxifen?

A
  • Post-Menopausal (50+) women
  • Hormone Replacement Therapy (HRT) w/ Family History
  • ER+ Breast cancer
  • Progesterone-resistant Endometrial and Ovarian cancer
  • Melanoma
  • Osteoporosis
  • Discontinue after 5 years: acts as an Agonist in Breast
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13
Q

Mechanims of Raloxifene?

A
  • SERM
  • Antagonist - Breast and Uterus (Endometrium)
  • Agonist - Bone
    • Increased risk of Thromboembolic events
    • Decreased Resportpion of bone
  • ER+ Breast Cancer w/ History of Endometrial cancer
  • Osteoporosis
  • SE: Hot flashes, Sweating/warmth, Increased Vaginal Discharge, Joint/Muscle pain, Increased Thromboembolism
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14
Q

Hormone Replacement Therapy (HRT)?

A
  • Relief or Prevention of Menopausal symptoms
    • Hot flashes, Vaginal atrophy
    • Osteoporosis (Increased Estrogen, Decreased Osteoclast activity)
  • Unopposed Estrogen Replacement Therapy (ERT)
    • Incrased Risk of Endometrial cancer so Progesterone is added
  • Increased Cardiovascular risk in Older women /w Higher doses
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15
Q

Anastrozole (Letrozole) / Exemestane?

A
  • Aromatase Inhibitors used in Postmenopausal women w/ Breast cancer
  • Better than Aminoglutethimid, no effect on Mineralocorticoid or Glucocorticoid synthesis
  • Continue to be effective beyond 5 years
  • No Risk of Endometrial cancer or Thromboemboilic events
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16
Q

Mechanism of Progestins?

A
  • Megestrol, Medroxyprogesterone
  • Bind Progesterone receptors
  • Decrease growth
  • Increased Weight gain
    • ​Anorexia-cachaexia related to Cancer and AIDS
  • Increase Vascularization of Endometrium
  • -> Stimulates Endometrial glandular secretions
  • -> Spiral artery development
  • -> Suppresses ovulation
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17
Q

Clinical use of Progestins?

A
  • Birth Contorl and Ovulation suppresion
  • Menstrual cycle control
  • Stabilization of Endometrium
  • Uterine control and Protection
  • Stimulate appetitie in Cachectic patients
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18
Q

Mechanism of Mifepristone (RU-486)?

A
  • Competitive inhibitor of Progestins at Progesterone Receptors
  • -> Lose Progesterone –> Lose Endometrial layer
  • -> Lose Pregnancy
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19
Q

Clinical use of Mifepristone (RU-486)?

A
  • Termination of Pregnancy
  • -> Inhibit Progesterones –> Lose Pregnancy
  • Administered w/ Misoprostol (PGE1)
20
Q

SEs of Mifepristone (RU-486)?

A
  • Heavy Bleeding –> sloughing of Endometrial layer
  • Abdominal Pain
  • GI effects
    • Diarrhea
    • Nausea
    • Vomiting
    • Anorexia
21
Q

Oral Contraception?

(Synthetic Progestins, Estrogen)

A
  • Estrogen and Progestin inhibit LH / FSH
  • -> Prevent Estrogen surge
  • -> No LH surge –> No Ovulation
  • Progestins cause thickening of the Cervical mucus
  • -> Limiting access of Sperm to Uterus
  • Progestins inhibit Endometrial Proliferations
  • -> Endometrium less suitbale for Implantation of Embryo
  • Contraindicated: Smokers > 35 y.o. (Cardiovascular events), History of Thromboemobilsm, Stroke, ER+ tumor
22
Q

Terbutaline?

A
  • β2-adrenergic receptor agonist
  • Relaxes the Uterus (Myometrial relaxation)
  • Used to decrease Contraction Frequency in women during Labor
23
Q

Mechanism of Danazol?

A
  • Synthetic Androgen that acts as a Partial agonist at Androgen receptors
24
Q

Clinical use of Danazol?

A
  • Endometriosis
  • Hereditary Angioedema
25
Q

SEs of Danazol?

A
  • Androgenic effects
    • Weight gain
    • Edema
    • Acne
    • Hirsuitism
    • Masculinization
  • Decreased HDL lvls
  • Hepatotoxicity
26
Q

Mechanism of Testosterone, Methyltestosterone?

A
  • Agonist at Androgen receptors
  • Modifies gene transcription upon conversion to DHT
  • Negatively regulates LH production in Ant. Pit.
27
Q

Clinical use of Testosterone, Methyltestosterone?

A
  • Hypogonadism - Testicular failure
  • Anemia
  • Promotes secondary Sex characteristics
  • Anabolic stimulation to Promote recovery after Burn or Injury
28
Q

SEs of Testosterone, Methyltestosterone?

A
  • Premature closure of the Epiphyseal Plates
  • Increased LDL
  • Decreased HDL
  • Masculinization in Females
  • Decreased Intracellular Testosterone in Males by Inhibiting the release of LH (via negative feedback)
  • -> Gonadal atrophy
29
Q

Finasteride / Dutasteride?

A
  • 5α-reductase inhibitor (decreased conversion of Testosterone to DHT)
  • Benign Prostate Hyperplasia (BPH)
  • Promotes Hair growth –> Male pattern baldness
    • To prevent male-pattern hair loss, give a drug that will encourage female breast growth
  • SE: Breast enlargment/tenderness, Lip swelling, Testicular pain, GI distress (diarrhea, Ab pain) Loss of Libido, Erectile dysfunction
  • Pregnant women –> Hypospadias in Male fetus
30
Q

Flutamide?

A
  • Anti-androgen that COMPLETELY antagonized the Testosterone receptor
  • Used w/ Leuprolide (GnRH) for Testosterone surge
  • Nonsteroidal Competitive Inhibitor of Androgens at the Testosterone Receptor
  • Prostate cancer
  • Hirsutism in Women
  • SE: Hot flashes, Diarrhea, Nausea, Gynecomastia, Impotence, Hepatitis, Loss of Libido, Low Volume Ejaculate, Breast Tenderness and Enlargement
31
Q

Ketoconazole / Spironolactone?

A
  • Inhibits Steroid synthesis (BOTH)
  • Increases Estradiol-to-Testosterone ration (BOTH)
  • Displaces Estradiol and Dihydrotestosterone from Sex-Hormone-binding protein (Spironolactone only)
  • Inhibits 17,20-Desmolase
  • Used in PCOS to prevent Hirsuitism
  • Antiandrogen
  • SE: Gynecomastia, Amenorrhea, Hepato toxicity, Pruritus
32
Q

Spironolactone?

A
  • Inhibits Steroid binding
  • 17α-hydroxylase
  • 17,20-Desmolase
  • Used in PCOS to prevent Hirsuitism
  • SE: Gynecomastia and Amenorrhea
33
Q

Tamsulosin?

A
  • α1-antagonist
  • Inhibits Smooth Muscle contraction
  • Selective for α1A,D-receptors (found in Prostate)
    vs. α1B- receptors
  • Tx: BPH
34
Q

Mechanism of Sildenafil, Vardenafil, Tadalafil?

A
  • Inhibits Phosphodiesterase 5 (PDE5)
  • -> cGMP –> Vasodilates vascular Smooth muscle
  • -> Smooth muscle relaxation in the Corpus cavernosum
  • Increased Blood flow
  • -> Penile erection
  • Tx: Erectile Dysfuntion
  • Sildenafil and Vardenafil FILL the Penis
  • SE: Headache, Flushing, Dyspepsia, Blue-Green color vision alterations, Risk of Life-threatening-Hypotension
35
Q

Clinical use of Sildenafil, Vardenafil?

A
  • Treatment of Erectile dysfunction
36
Q

SEs of Sildenafil, Vardenafil?

A
  • Headache
  • Flushing
  • Dyspepsia
  • Alterations in Blue-Green color vision
  • Risk of Life-threatening Hypotension, Pts. taking Nitrates
  • “Hot and Sweaty” but then Headache, Heartburn, Hypotension
37
Q

Methotrexate?

A
  • Folic acid antagonist
  • Stops cellular Division
  • Ectopic Pregnancies
38
Q

Labor Inhibition (Tocolysis)?

A
  • Indomethacin (COX inhibitor)
    • ​Inhibits PG synthesis in the Uterus (PGE2, PGF2)
  • Nifedipine (Ca2+ channel blocker)​
  • Terbutaline (β2-adrenergic receptor agonist)
    • ​48 hours of delay
39
Q

Labor Promotion?

A
  • Prostaglandins - Cervical dilation, Tachysystole, Uterine rupture
    • Dinoprostone (PGE2 analog)
    • Misoprostol (PGE1 analog) (off-label)
  • Oxytocin - synthetic analog of Posterior Pituitary Hormone
    • Can be used to contract Spiral arteries
40
Q

Trastuzumab (Herceptin)?

A
  • Helps kill Breast cancer cells that Overexpress ERBB2
  • Ab-dependent Cytotoxicity
  • Herceptin is a Monoclonal Ab against erbB-2 (HER2/neu) –> member of the Epidermal Growth Factor Receptor family –> Metastatic Breast cancer
  • Cardiotoxicity, especially when combined
    w/ Anthacyclines (Doxorubicin)
41
Q

Oxytocin, Ergometrine

A
  • Binds Oxytocin receptor
  • -> stimulates the release of Intracellular Ca2+
  • -> Induces contraction of Smooth muscle cells in the Uterus and Myoepithelial cells of the Mammary Gland
  • Uterine contractions (Induce labor, abortion)
  • Milk letdown
  • Postpartum Uterine Hemorrhage
42
Q

Ritodrine, Salmeterol?

A
  • β2-Adrenergic agonists
  • Blockage of Uterine Contractions
  • Uterine relaxants are used in selected pts. to prevent Premature Labor occuring between 22 adn 33 seeks
  • SE: Pulmonary edema, Tremor, Arrhythmia
43
Q

Fulvestrant?

A
  • Pure Estrogen receptor antagonist
  • No Estrogen Agonist effects like Tamoxifen
  • 1x Month
  • Postmenopausal women whos cancer progresses on Tamoxifen or another Anti-Estrogen
44
Q

Aminoglutethimide?

A
  • Inhibits one of the P450 enxymes that Converts Cholesterol into Pregnenolone
  • All classes of Steroids are reduced
  • Inhibits the conversion of Androstenedione in the Peripheral tissues (Fat, Muscle) into Estrone and Estradiol by Blockin Aromatase enzyme
  • SEs: Lethargy, Drowsiness, Visual blurs, Maculopapular rash
45
Q

Pertuzumab?

A
  • Prevents HER2 monomers from Dimerizing
  • It is the Dimeric form of the receptor that actively stimulates the signal cascade that causes the Tumor to be more aggressive
  • Pertuzumab + Trastuzumab = Better w/ Both
46
Q

Lapatinib?

A
  • Used for Tx of Cancer expressing High lvls of HER-2 that no longer responds to Trastuzumab
  • Orally active Tyrosine Kinase Inhibitor
  • Targets both erbB-2 receptors (EGFR and Her2/neu)
  • Lapatinib + Chemo

Pharmacology (29 decks)

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