pharm 9

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Author:
Neda317
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305732
Filename:
pharm 9
Updated:
2015-07-26 15:19:53
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pharm
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pharm
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596-598 repro
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  1. Leuprolide
    MOA
    • GnRH analog with agonist properties
    • when used in pulsatile fashion; antagonist
    • properties when used in continuous fashion
    • (downregulates GnRH receptor in pituitary
    • -> dec  FSH/LH).
  2. Leuprolide
    use
    • Infertility (pulsatile), prostate cancer
    • (continuous use following androgen receptor
    • blockade with flutamide), uterine fibroids
    • (continuous), precocious puberty (continuous)
  3. Leuprolide
    tox
    Antiandrogen, nausea, vomiting.
  4. Estrogens (ethinyl estradiol, DES, mestranol)
    moa
    Bind estrogen receptors.
  5. Estrogens (ethinyl estradiol, DES, mestranol)
    use
    • Hypogonadism or ovarian failure, menstrual abnormalities, hormone replacement therapy in postmenopausal women;
    • use in men with androgen-dependent prostate cancer.
  6. Estrogens (ethinyl estradiol, DES, mestranol)
    tox
    • inc risk of endometrial cancer, bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero,  inc risk of thrombi. Contraindications—ER ⊕ breast
    • cancer, history of DVTs.
  7. what are Selective estrogen receptor modulators
    • Clomiphene
    • Tamoxifen
    • Reloxifene
  8. Clomiphene
    moa
    use 
    cause
    • Antagonist at estrogen receptors (also partial agonist) in hypothalamus. Prevents normal feedback inhibition and
    • inc release of LH and FSH from pituitary, which stimulates ovulation. Used to treat infertility due to anovulation (e.g., PCOS).
  9. May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances.
  10. Tamoxifen
    MOA
    use
    • Antagonist at breast; agonist at bone, uterus; inc risk of thromboembolic events and endometrial cancer.
    • Used to treat and prevent recurrence of ER/PR ⊕ breast cancer.
  11. Raloxifene
    use
    Antagonist at breast, uterus; agonist at bone; inc risk of thromboembolic events but no increased risk of endometrial cancer (vs. tamoxifen); used primarily to treat osteoporosis.
  12. which one has no increased risk of endometrial cancer
    Raloxifene
  13. which one increased risk of endometrial cancer
    Tamoxifen
  14. why  Hormone replacement
    therapy
    • Used for relief or prevention of menopausal symptoms (e.g., hot flashes, vaginal atrophy),
    • osteoporosis (inc estrogen, dec  osteoclast activity).
    • Unopposed estrogen replacement therapy inc  risk of endometrial cancer, so progesterone is added.
    • Possible increased cardiovascular risk.
  15. Anastrozole/ exemestane
    Letrozole
    Aromatase inhibitors used in postmenopausal women with ER ⊕  breast cancer.
  16. Progestins
    moa
    use
    • MOA Bind progesterone receptors, dec growth and inc vascularization of endometrium.
    • USE Used in oral contraceptives and to treat endometrial cancer, abnormal uterine bleeding.
  17. Mifepristone (RU-486)
    moa
    use
    tox
    • MOA: Competitive inhibitor of progestins at progesterone receptors.
    • USE: Termination of pregnancy. Administered with misoprostol (PGE1).
    • TOX:Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain.
  18. Oral contraception(synthetic progestins,
    estrogen)
    • Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge-> no
    • LH surge -> no ovulation.
    • Progestins cause thickening of cervical mucus, thereby limiting access of sperm to uterus.
    • Progestins also inhibit endometrial proliferation -> endometrium is less suitable to the
    • implantation of an embryo
  19. Oral contraception(synthetic progestins,estrogen)
     Contraindications:
    • smokers >  35 years old (inc risk of cardiovascular events), patients with history of
    • thromboembolism and stroke or history of estrogen-dependent tumor.
  20. Terbutaline, ritodrine
     β2-agonists that relax the uterus; used to dec contraction frequency in women during labor.
  21. Danazol
    moa
    use 
    tox
  22. MECHANISM Synthetic androgen that acts as partial agonist at androgen receptors.
    • CLINICAL USE Endometriosis, hereditary angioedema.
    • TOXICITY Weight gain, edema, acne, hirsutism, masculinization, 􀁲 HDL levels, hepatotoxicity
  23. Testosterone, methyltestosterone
    moa
    MECHANISM Agonists at androgen receptors.
  24. Testosterone, methyltestosterone
    use
    Treats hypogonadism and promotes development of 2° sex characteristics; stimulation of anabolism to promote recovery after burn or injury.
  25. Testosterone, methyltestosterone
    tox
    • Causes masculinization in females; dec  intratesticular testosterone in males by inhibiting release of LH (via negative feedback) -> gonadal atrophy. Premature closure of epiphyseal plates. inc  LDL,
    • dec  HDL.
  26. Antiandrogens
    Testosterone + 5α-reductase  => DHT (more potent).
  27. Antiandrogens drugs
    • Finasteride
    • Flutamide
    • Ketoconazole
    • Spironolactone
  28. Finasteride
    • A 5α -reductase inhibitor (dec  conversion of
    • testosterone to DHT). Useful in BPH and
    • male-pattern baldness.
  29. Flutamide
    • A nonsteroidal competitive inhibitor at
    • androgen receptors. Used for prostate
    • carcinoma.
  30. Ketoconazole
    • Inhibits steroid synthesis (inhibits
    • 17,20-desmolase).
  31. Spironolactone
    Inhibits steroid binding, 17α -hydroxylase, and 17,20-desmolase.
  32. Ketoconazole and spironolactone are used totreat
    • polycystic ovarian syndrome to reduce
    • androgenic symptoms. Both have side effects of gynecomastia and amenorrhea.
  33. Tamsulosin
    • α1-antagonist used to treat BPH by inhibiting smooth muscle contraction.
    • Selective for α1A,D receptors (found on prostate) vs. vascular α1B receptors.
  34. Inhibit PDE-5 -> inc cGMP, smooth muscle
    relaxation in corpus cavernosum, inc blood flow, penile erection.
    Sildenafil, vardenafil, tadalafil
  35. Sildenafil, vardenafil, tadalafil
    tox
    • Headache, flushing, dyspepsia, cyanopsia
    • (blue-tinted vision). Risk of life-threatening
    • hypotension in patients taking nitrates.
  36. Minoxidil
    moa
    use
    • MOA: Direct arteriolar vasodilator.
    • USE: Androgenetic alopecia; severe refractory hypertension.

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