Term
What does SERMS stand for? |
|
Definition
Selective Estrogen Receptor Modulators |
|
|
Term
What does SERDS stand for? |
|
Definition
Selective Estrogen Receptor Down Regulators |
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|
Term
What results from the Pulsatile release of GnRH from the Hypothalamus? |
|
Definition
Triggers LH and FSH release from the Pituitary Gland which will trigger Estrogen Production |
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|
Term
What feedback inhibits the release of GnRH by the hypothalamus? |
|
Definition
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|
Term
What are the Estrogen levels in a young female? |
|
Definition
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|
Term
What happens at puberty to estrogen levels? |
|
Definition
Pulse Generator of GnRH turns on leading to increased LH/FSH/Estrogen |
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|
Term
What is happening during the Follicular phase of a adult womans cycle? |
|
Definition
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|
Term
What happens during the Luteal Phase of an adult womans cycle? |
|
Definition
Surge of LH which triggers an increase in Estrogen and Progestin |
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|
Term
What happens to Estrogen levels around 50 years old in a Woman? |
|
Definition
Estrogen levels Decrease (Menopause) |
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|
Term
What does the drop in estrogen at age 50 in women do to LH/FSH levels? |
|
Definition
Without the Feedback inhibition these Levels Sky Rocket |
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|
Term
In menses what is the first phase? |
|
Definition
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|
Term
What happens int the Follicular phase? |
|
Definition
Slow rise in LH which leads to Increase in Estrogen |
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|
Term
What triggers the transition from Follicular phase to Luteal Phase? |
|
Definition
Estrogen levels get so high they change from Negative Feedback to Positive feedbakc which Leads to a Surge in LH |
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|
Term
What does the surge in LH lead to? |
|
Definition
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|
Term
When is the Corpus Luteum formed? |
|
Definition
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|
Term
What does the Corpus Luteum produce? |
|
Definition
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|
Term
Which hormone helps the proliferation of the endometrium? |
|
Definition
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|
Term
What halts the proliferation of the Endometrium and leads to Vascularization? |
|
Definition
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|
Term
Why is the Endometrium vascularized? |
|
Definition
To prepare for the implantation of the Blastocyst |
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|
Term
What hormone is responsible for the rise in temperature a Woman experinces as they approach ovulation? |
|
Definition
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|
Term
Where does LH bind to trigger the formation of Estradiol? |
|
Definition
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|
Term
What happens when LH binds in the Theca Cells? |
|
Definition
Adenyl Cyclase/cAMP/PKA triggers expression of Proteins for Testosterone Synthesis |
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|
Term
What happens to the Testosterone Androstenedione after its produced in the Theca Cells? |
|
Definition
Diffuses into the Granulosa Cells |
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|
Term
What enzyme is highly active in the Granulosa Cells? |
|
Definition
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|
Term
What is the action of Aromatase in the Granulosa Cells? |
|
Definition
Converts Testosterone into Estradiol |
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|
Term
What determines the amount of Aromatase in Granulosa Cells? |
|
Definition
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|
Term
How does Estradiol travel in the blood? |
|
Definition
Bound to Albumin and SHBG, 2% is Free |
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|
Term
What are the physiologic functions of Estrogen? |
|
Definition
Libido, Feminization, Endometrial Development, Bone Antiresorption, Closre of Epiphyses, Nitrogen Balance, Water Retention, and Protein Synthesis by the Liver |
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|
Term
What two receptors does Estrogen bind to? |
|
Definition
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|
Term
What happens to the receptor when Estrogen binds? |
|
Definition
Dimerization and expression of specific genes |
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|
Term
Do all types of Estrogen Receptors bind with the same affinity? |
|
Definition
No leads to Specific Actions |
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|
Term
|
Definition
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|
Term
What is the overall action of SERMS? |
|
Definition
Can be estrogen Agonist or Antagonist depending on what tissue its in |
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|
Term
What is the action of SERDS? |
|
Definition
Selectively down regulate the expression of Estrogen Receptors in tissues |
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|
Term
What are the 17Beta-esters? |
|
Definition
Estradiol valerate and Estradiol cypionate |
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|
Term
How are these 17Beta-esters administered? |
|
Definition
IM since HIghly Lipophilic |
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|
Term
What are Estradiol Valerate and Estradiol Cypionate used for? |
|
Definition
Hormone Replacement Therapy |
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|
Term
What are the 17Alpha-Substituted Estrogens? |
|
Definition
Ethinyl Estradiol and Mestranol |
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|
Term
Are Ethinyl Estradiol and Mestranol orally active? |
|
Definition
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|
Term
What are Ethinyl Estradiol and Mestranol typically used as? |
|
Definition
Birth Control pills since very slowly metabolized by the liver |
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|
Term
What are the Conjugated Estrogens? |
|
Definition
Na+Estron Sulfate and Na+Equillin Sulfate |
|
|
Term
What are the conjugated Estrogens purified from? |
|
Definition
Horse Urine Hence Equillin |
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|
Term
What are the conjugated Estrogens typically used for? |
|
Definition
Hormone Replacement Therapy and Vaginal Atrophy |
|
|
Term
What drug was widely used to prevent miscarriages? |
|
Definition
|
|
Term
What was the problem with DES? |
|
Definition
Female offspring Developed Vaginal and Cervical Cancer |
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|
Term
What is used in combo with Ethinyl Estradiol and Mestranol in Birth Control? |
|
Definition
|
|
Term
What would happen if only estrogen was used? |
|
Definition
Unimpeded Endometrial Growth and Cancer |
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|
Term
Can estrogens be used to trigger Puberty? |
|
Definition
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|
Term
What is the problem with inducing puberty with Estrogen? |
|
Definition
Leads to closing of epiphyseal plates early if Max Height isnt already reached |
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|
Term
What hormone can be used to treat Prostate Cancer and Dysmenorrhea? |
|
Definition
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|
Term
What other than SSRIs can be used to treat Emotional Distress? |
|
Definition
Estrogen Oral Contraceptives |
|
|
Term
What is the effect of Estrogen on Osteoporosis? |
|
Definition
|
|
Term
What can be used to treat vaginal Atophy? |
|
Definition
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|
Term
What are the side effects of Estrogen Therapy? |
|
Definition
Nausea, Weight Gain, Edema, Endometrial Cancer, Cervical Cancer, Thromboemboli, Increased Blood Pressure, Gall Bladder Disease, and Risk of Breast Cancer |
|
|
Term
What is more likely to cause breat cancer Estrogen Alone or Estrogen with Progestins? |
|
Definition
|
|
Term
What iss estrogen replacement therapy a risk factor for? |
|
Definition
Heart Disease, Stroke, and Breast Cancer |
|
|
Term
What does Estrogen Therapy greatly increase rick of? |
|
Definition
130% increase in Pulmonary Embolism |
|
|
Term
What can estrogen decrease the risk of? |
|
Definition
Hip Fracture, Colon Cancer, and Uterine Cancer |
|
|
Term
What are the physiological Antagonists of Estrogen? |
|
Definition
Progesterone and Testosterone |
|
|
Term
Where does Progesterone work as a Estrogen antagonist? |
|
Definition
Feedback inhibits Hypothalamus and Pituitary also works in the Uterus |
|
|
Term
|
Definition
Tamoxifen, Clomiphene, and Raloxifene |
|
|
Term
What is used to treat Estrogen Receptor Positive Breast Cancer? |
|
Definition
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|
Term
What is a side effect of Tamoxifen? |
|
Definition
Can Cause endometrial Cancer due to Agonist activity in this Uterus, also Blood Clots |
|
|
Term
How long is Tamoxifen usually used? |
|
Definition
|
|
Term
What is the effect of Tamoxifen on liver enzymes? |
|
Definition
|
|
Term
Why is Tamoxifen only used for 5 years? |
|
Definition
By that time Increased Risk of Blood Clot out weighs Breast Cancer Benefits |
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|
Term
What drug is used to induce Ovulation in women with intact ovaries? |
|
Definition
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|
Term
Can Clomiphene be used in patients with venous thrombolytic disorders? |
|
Definition
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|
Term
How long is Clomiphene used for before the negatives outweight the Positives? |
|
Definition
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|
Term
What drug is used to treat Osteoporosis? |
|
Definition
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|
Term
Where does Raloxifene have agonist effects? |
|
Definition
In the Bone and Lipid Metabolism, so good for Cholesterol |
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|
Term
Where does Raloxifene act as an Antagonist? |
|
Definition
Brain, Breast, and Uterus |
|
|
Term
What drug is used prophalactically for breat cancer? |
|
Definition
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|
Term
How long can Raloxifene be used to reduce risk of breast cancer? |
|
Definition
|
|
Term
What are the Selective Estrogen Receptor Downregulators? |
|
Definition
|
|
Term
What is the 7-alpha alkylamide derivative of estradiol? |
|
Definition
|
|
Term
What is the MOA of Fulvestrant? |
|
Definition
Prevents Dimerization of Estrogen Receptors |
|
|
Term
What type of cancer is Fulvestrant useful in treating? |
|
Definition
Tamoxifen Resistant Breast Cancer and possible Estrogen Receptor Positive Ovarian Cancer |
|
|
Term
How is Fulvestrant administered? |
|
Definition
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|
Term
What are the Aromatase Inhibitor? |
|
Definition
Aminogluthemide, Formestane, Exemestane, and Anastrozole |
|
|
Term
Why is Aminogluthemide no longer used? |
|
Definition
Inhibits the Synthesis of Adrenocortical Steroids |
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|
Term
What is given with Aminogluthemide to combat Adrenocortical Steroid Inhibition? |
|
Definition
Hydrocortisone Supplementation |
|
|
Term
What are the Steroidal inhibitors of Aromatase? |
|
Definition
Formestane and Exemestane |
|
|
Term
What are the Non-steroidal Aromatase Inhibitors? |
|
Definition
|
|
Term
What are the Aromatase inhibitors used to treat? |
|
Definition
ER Positive Breast Cancer |
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|
Term
What is the risk of Uterine Cancer and Venous Thromboembolism with Aromatase inhibitors? |
|
Definition
|
|
Term
What are the negative side effects of Aromatase Inhibitors? |
|
Definition
|
|
Term
What is the MOA of Progestins? |
|
Definition
Decrease GnRH pulse Frequency |
|
|
Term
What do Progestins do in the body? |
|
Definition
Suppress Uterine Smooth Muscle Contraction, Stabilize Endometrium, Promote Vascularization, and Develop Mammary Glands |
|
|
Term
What effect do Progestins have on Thermogenesis? |
|
Definition
Increase Temp when Ovulation is occuring |
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|
Term
What are the two Progestin Receptors? |
|
Definition
PRA and PRB, distributed in different tissures throughout the body |
|
|
Term
How do the affinities of Progestin Receptors compare? |
|
Definition
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|
Term
What is the binding site of Progestins? |
|
Definition
Bind Nucleus-Bound Heat Shock Proteins |
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|
Term
What happens when Progetins bind Heat Shock Proteins? |
|
Definition
Dimerization, binding to Response elements and coactivators to regulate transcription |
|
|
Term
Which Progestin receptor type has stimulatory effects? |
|
Definition
PRB found in mammary glands |
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|
Term
Which Progestin receptor type is inhibitory? |
|
Definition
PRA Found in Endometrial Tissue |
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|
Term
What are the Therapeutic uses of Progestin? |
|
Definition
Oral Contraceptives, Uterine Bleeding, Endometriosis, and Breat/Endometrial Cancer |
|
|
Term
Is Progesterone orally active? |
|
Definition
|
|
Term
Why must Progesterone be given IM while suspended in Oil? |
|
Definition
|
|
Term
What are the two preparation types of Progestins? |
|
Definition
Progesterone Derivatives and Testosterone Derivatives |
|
|
Term
What are the Progesterone Derivatives? |
|
Definition
Medroxyprogesterone and Megestrol Acetate |
|
|
Term
What are the 19-Nortestosterone Derivatives? |
|
Definition
Norgestrel, Norethindrone, and Ethynodiol |
|
|
Term
How do 19-Nortestosterone Derivatives differ from Progesterone derivatives? |
|
Definition
They have more Androgenic Activity |
|
|
Term
What are the Progesterone Derivatives Used for? |
|
Definition
Long acting Injectable Contraceptive |
|
|
Term
What are the side effects of Progestins? |
|
Definition
Break through Bleeding and Decreased HDL |
|
|
Term
|
Definition
RU 486, competitive inhibitor of Progesterone and Glucocorticoid |
|
|
Term
|
Definition
Blocks Action of Progesterone on Estrogen Primed Endometrium |
|
|
Term
|
Definition
Increases Prostaglandins and Mestraul Bleeding |
|
|
Term
What drug is used to terminate pregnancy? |
|
Definition
RU 486 with Prostaglandin |
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|
Term
What are the side effects of Mifpristone? |
|
Definition
Nausea, Dizziness, and Abdominal Pain |
|
|
Term
What is endometrium growth outside the uterus typically in the Pertioneal Cavity? |
|
Definition
|
|
Term
What are the possible treatments for Endometriosis? |
|
Definition
|
|
Term
What does Leuprolide do in the short term? |
|
Definition
Increases GnRH acts as Agonist |
|
|
Term
What is the long term effect of Leuprolide? |
|
Definition
Suppresses GnRH and Steroidigenesis |
|
|
Term
What can be the side effect of Long term Leuprolide use? |
|
Definition
|
|
Term
What is the MOA of Medroxyprogesterone? |
|
Definition
Inhiits Gonadotrophin Secretion but also opposes the Estrogenic Stimulation of Endometriosis |
|
|
Term
Which drug can be given as a Intruterine Device to combat endometriosis? |
|
Definition
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|
Term
What are the side effects of Levonorgestel is used for longer than 5 years? |
|
Definition
Excessive Uterine Bleeding |
|
|
Term
What is the effect of Birth Control pills on endometriosis? |
|
Definition
Stabilize Estrogen and Progestin levels |
|
|
Term
What is the MOA of Danazol against endomertiosis? |
|
Definition
Reduces Estrogen Production by decreaseing FSH/LH |
|
|
Term
What are the side effects of Danazol? |
|
Definition
Poor Cholesterol, Hirutism, Hotflashes, and Deepening of the Voice |
|
|
Term
Why are progestins typically given in conjunction with estrogens during Hormone Replacement Therapy? |
|
Definition
To Inhibit Proliferation of Endometrial Tissue |
|
|
Term
What is the effect of Progestins on the Fallopian Tubes? |
|
Definition
Decrease Contractions of the Fallopian Tubes |
|
|
Term
What is the effect of Estrogens on the Fallopian Tubes? |
|
Definition
Increase Contractions of the Fallopian Tubes |
|
|
Term
What Triggers the formation of Hostile Cervical mucus? |
|
Definition
|
|
Term
What triggers the switch from Proliferative to Secretory phases of the endometrium? |
|
Definition
|
|
Term
What can inhibit smooth muscle contracton during pregnancy? |
|
Definition
|
|
Term
Which hormone can stimulte proliferation of Mammary Gland Tissue? |
|
Definition
Both Progesterone and Estrogen |
|
|
Term
Long exposure to Birth Control is a risk factor for what type of cancer? |
|
Definition
|
|
Term
What is the action of Clomiphene on fertility? |
|
Definition
Induces Fertility by competeing with estrogen at the Hypothalamus and Pituitary |
|
|
Term
What fertility drug us a partial estrogen receptor agonist? |
|
Definition
|
|
Term
In what percentage of Women will Clomiphene trigger Ovulation? |
|
Definition
90-95% with normal Ovarian Reserve |
|
|
Term
What are some of the side effects of Clomiphene? |
|
Definition
Multiple Births, Hot Flashes, Ovarian Enlargement, and Blurred Vision |
|
|
Term
After the intial administration of Clomiphene is pregancy most likely? |
|
Definition
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|
Term
When are Gonadotrophins used to stimulate Ovulation? |
|
Definition
When patient doesnt have a functioning Pituitary Gland |
|
|
Term
|
Definition
Urofollitropin, and HCG?,Gonadotropins used to stimulate Ovulation |
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|
Term
What must be monitored when using Gonadotrophins? |
|
Definition
Estradiol and Follicular Growth to prevent multiple Pregnancies |
|
|
Term
What is a common cause of infertility? |
|
Definition
|
|
Term
What is used to treat Hyperprolactinemia? |
|
Definition
|
|
Term
What is used to boost fertility in men? |
|
Definition
Gonadotropins and Clomiphene, to increase LH |
|
|
Term
Which estrogen derivatives are used in oral contraceptives? |
|
Definition
Mestronol and Ethinyl Estradiol |
|
|
Term
What are the Progesterones used in oral contraceptives? |
|
Definition
Norethindrone, Norgestrel, Ethynodiol Diacetate, and Levonorgestrel |
|
|
Term
Which of the Progesterone Derivtives have lower androgenic activity? |
|
Definition
Norgestrel and Levonorgestrel |
|
|
Term
What is the advantage of the new Multiphasic Oral Contraceptives? |
|
Definition
|
|
Term
What is the disadvantage of the Multiphasic Pills? |
|
Definition
If you miss a pill the possibilty of Ovulation is higher |
|
|
Term
What are the benefits of Borth Control other than not getting Preggers? |
|
Definition
Controls Dysmenorrhea, Decreased Endometrial/Ovarian Cancer, Decrease PID, Fibrocystic Disease, Ovarian Cysts, and Decreased ACne |
|
|
Term
What are some of the side effects of Birth Control? |
|
Definition
Breast Cancer, Cervical Cancer with HPV, MI, Thrombosis, Headache/Migraine, HDL and LDL Negative, and Glucose Tolerance |
|
|
Term
What is the effect of older Oral Contraceptives on Clotting Factors and Platelets? |
|
Definition
|
|
Term
What is the effect of older Oral Contraceptives on Prothrombin time? |
|
Definition
|
|
Term
What happens to Steroid Hormone Binding Globulins when using older forms of Birth Control? |
|
Definition
|
|
Term
What is the effect of older Contraceptives on Ang I and Ang II? |
|
Definition
|
|
Term
What is the effect of older contraceptives on cholesterol? |
|
Definition
|
|
Term
What is the effect of older contraceptives on LH/FSH/Estradiol/Progesterone? |
|
Definition
|
|
Term
What is the so called 'Mini Pill" for birth control? |
|
Definition
Progestin only formulation |
|
|
Term
What are the advantages of Progestin only Oral Contraceptives? |
|
Definition
Decreased Bleeding, Decreased Cramps, Ok for Breat Feeding Women, and Can be used by Smokers who have risk factor for CAD |
|
|
Term
Which oral contraceptive must be taken at the same time each day in order to be effective? |
|
Definition
Progestin Only Formulation |
|
|
Term
What form of Oral Contraceptives can cause Irregular Heavy Bleeding? |
|
Definition
|
|
Term
What are the Adverse side effects of Progestin only contraceptives? |
|
Definition
Breakthrough Bleeding, Headache, Mood Change, Weight Gain, Increased Acne, Decreased HDL, Increased LDL, Decreased Bone Density |
|
|
Term
What drugs are contraindicated in women with Thromboembolic Disorders? |
|
Definition
Medroprogesterone and Levonorgestrel |
|
|
Term
What drugs can interact with p450s to decrease the effectiveness of Oral Contraceptives? |
|
Definition
Tetracycline, Rifampin, Metronidazole, Penicillin, Anti-HIV Drugs, Anti-Epileptic Drugs, and St Johns Wort |
|
|
Term
What composes the Morning after pill? |
|
Definition
.50 mg of Ethinyl Estradiol and .25 mg of Norgestrel |
|
|
Term
When must the morning after pill be taken? |
|
Definition
WIthin 72 hours of exposure then again 12 hours later |
|
|
Term
What is the MOA of the Morning After Pill? |
|
Definition
Stimulates Endometrial Bleeding |
|
|
Term
|
Definition
Synthetic Progestin .75 mg of Levonorgestrel |
|
|
Term
What is the MOA of Plan B? |
|
Definition
Not Well Understood, May Inhibit or Delay Ovulation, Fertilizaton, Transport, or Implantation |
|
|
Term
How effective are the progestin only birth control pills? |
|
Definition
Block 80% of the time but are as effective as Combined at Preventing Pregnancy |
|
|
Term
What is the basis of Male Antifertility drugs? |
|
Definition
Inhibit LH and Endogenous Testosterone production |
|
|
Term
What is used to treat precocious puberty? |
|
Definition
|
|
Term
What is used to treat Hypogonadism? |
|
Definition
|
|
Term
If hypogonadism in a short stature boy what should be given with Androgens? |
|
Definition
|
|
Term
What is used to treat breast cancer? |
|
Definition
SERMs, SERDs, and Aromatase INhibitors |
|
|
Term
What is used to treat hyperprolactenimia? |
|
Definition
|
|