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27 Cards in this Set
- Front
- Back
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Name natural estrogens
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Estradiol, estriol, estrone
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Name semi-synthetic estrogens
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Ethinyl estradiol, estradiol valerate
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What are the effects of estrogens?
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- Induction of primary and secondary female sex characteristics
- Induce proliferative phase of menstrual cycle. - Hyperplasia of endometrium - Increased expression of progesterone receptor - Mammary gland preparation for lactation - Vasodilation - Na+ and water retention (mineralocorticord-like) - Increased vitamin K-dependent factor production - Increased platelet aggregation. - Increased fibrinolysis - Increased HDL, decreased LDL - More cholesterol in bile |
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Mechanism of action of estrogens?
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They bind to intracellular receptors, ER-a and ER-b. They can also bind to surfacebound G-protein coupled estrogen receptor, GPER, that will trigger faster effects of estrogen, like vasodilation
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When are estrogens indicated?
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- Hypogonadism- Postmenopausal therapy- Contraception- Menstrual bleeding disorders- Acne
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How are estrogens given?
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They are often combined with a progestin.
Can be given as oral tablets, vaginal formulations, transdermal patch, nasal spray and gel. Oral preps have more hepatic effects than the other |
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Pharmacokinetics of estrogens?
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Estradiol binds to sex-hormone binding globulin and albumin, while synthetic and semisynthetic ones bind only to albumin.
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Side effects of estrogens?
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- Risk of venous thrombosis- Cholestasis- Elevated plasma triglyceride levels- Uterine bleedings- Worsening of endometriosis- Endometrial hyperplasia or cancer - risk is eliminated by progestins.- Breast cancer - risk increases with progestins
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Contraindications of estrogens?
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Patients with current, previous or with family history of estrogen-sensitive cancers.
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What are selective estrogen receptor modulators?
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SERMs are partial agonists in some tissues, and antagonists in others. This gives them antiestrogen effects in some tissues, and mild estrogen effects in other.
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Name SERMs
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Tamoxifen, raloxifene, lasofoxifene
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Name antiestrogens
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Clomiphene, fulvestrant
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Indications of antriestrogens and SERMs?
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- Tamoxifen and fulvestrant treats estrogen receptor positive breast cancer
- Raloxifene and lasofoxifene treat osteoporosis. - Clomiphene is used to induce ovulation in anovulation, like in PCOS. |
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Mechanism of action of clomiphene?
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It inhibits estrogen binding in the anterior pituitary so there will be no negative feedback. This increases the secretion of GnRH and gonadotropin, which will stimulate the ovaries and induce ovulation.
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Side effects of SERMs?
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Tamofixen increases the risk of endometrial cancer and venous thrombosis by being an agonist in endometrium and hemostasis.
Raloxifene increases risk for venous thrombus |
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Name selective aromatase inhibitors
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Anastrozole, letrozole, exemestane (irreversible inhibitor).
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Indications for selective aromatase inhibitors?
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Estrogen-sensitive breast cancer and induction of ovulation
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Name progestins
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Progesterone (endogenous, medroxyprogesterone, levonorgestrel, megestrol
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Indications of progestins?
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- Used in substitution therapy in hypogonadism and postmenopause with an estrogen.
- Hormonal contraceptives - Menstrual bleeding disorders - Endometriosis - Treatment of early puberty in girls - Metastatic estrogen-depended breast and endometrial cancers - Prevention of preterm birth |
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Mechanism of action of progestins?
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They bind to intracellular receptors, progesterone receptor, PR, to alter gene expression.
They inhibit estrogen receptors |
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How can progestins be given?
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As a tablet, intramuscular injection, intravaginal preparations and IUDs.
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Pharmacokinetics of progestins?
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Progesterone has almost 0 % oral bioavailability, but progestins have higher and longer half-life.
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Side effects of progestins?
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Weak androgenic effects like:- Edema- Acne- Dyslipidemia
Other:- Headache- Breast swelling and tenderness- Depression- Abnormal uterine bleedins |
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Name antiprogestins/selective progesterone receptor modulators (SPRMs)
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Mifepristone, ulipristal
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Indications of mifepristone?
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Used to terminate early pregnancy together with a prostaglandin analogue like gemeprost or misoprostol. The prostaglandin is given 48 hours after the mifepristone
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Indications of ulipristal?
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Emergency postcoital contraception (day-after pill).
Uterine myomas |
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How is the mechanism of action of mifepristone?
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It upregulates prostaglandin receptors in the uterus, so they are sensitized then the prostaglandin analogues are given 48 hours later. This will initiate strong uterine contractions and medical abortion
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