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Reproductive
FA complete review part 4 Pharmacology
| Question | Answer |
|---|---|
| Clomiphene stimulates the secretion of: | GnRH |
| In which structure does Clomiphene works on? | Hypothalamus |
| Stimulates the secretion of GnRH in the hypothalamus by blocking negative feedback? | Mechanism of action of Clomiphene |
| Which drug or medications work directly in the Ovary? (list) | 1. Oral contraceptives 2. Danazol |
| Inhibition on the ovary directly is done by: | Oral contraceptives and Danazol |
| What drugs inhibit P-450c17 (enzyme)? | Ketoconazole and Danazol |
| What is prevented to be synthesized by Ketoconazole and Danazol as thy ibnibitb P-450c14? | Androstenedione and Testosterone |
| Anastrozole inhibits which enzyme? | Aromatase |
| Which drug works by inhibiting Aromatase? | Anastrozole |
| Aromatase inhibitor | Anastrozole |
| What form of Estrogen is inhibited/stimulated by SERMs? | Estradiol |
| What is prevented by the action of SRRMS? | Gene expression in Estrogen-responsive cells |
| Which medications are known to inhibit specifically the synthesis of testosterone in men as it is secreted from the testes? | Ketoconazole and Spironolactone |
| Which diuretic is known to inhibit the production of testosterone? | Spironolactone |
| 5a-reductase inhibitor | Finasteride |
| What is prevented to form (convert) by the use of Finasteride? | Dihydrotestosterone |
| List of medication otha act by inhibiting the Androgen-receptor complex | 1. Flutamide 2. Cyproterone 3. Spironolactone |
| What is prevented by the inhibition of the Androgen-receptor complex? | Gene expression in Androgen-responsive cells |
| What medications (not list), can be used in order to prevent the gene expression in androgen-responsive cells? | Flutamide, cyproterone, and spironolactone |
| What is the mechanism of action of Leuprolide? | GnRH analog with agonist properties when used in pulsatile fashion; GnRH antagonist if used in continuous fashion |
| How does it have to be Leuprolide administered in order to have GnRH agonist properties? | Pulsatile fashion |
| Leuprolide has GnRH antagonistic properties when adminter in a _____________________ fashion. | Continuous fashion |
| What is the clinical use of Leuprolide? | Uterine fibroids, endometriosis, precocious puberty, prostate cancer, and infertility |
| What cancer is treated with Leuprolide? | Prostate cancer |
| What are common adverse effects of Leuprolide? | Hypogonadism, decreased libido, erectile dysfunction, nausea, and vomiting. |
| GnRH agonist/or antagonist depending on administration format? | Leuprolide |
| What are types of Estrogens? | Ethinyl estradiol, DES, and mestranol |
| MOA of Estrogens | Bind estrogen receptors |
| What are the clinical uses for estrogens? | 1. Hypogonadism or ovarian failure 2. Menstrual abnormalities 3. Hormone replacement therapy in postmenopausal women |
| What are associated adverse effects of Estrogen therapy? | 1. Increased risk of endometrial cancer 2. Bleeding in postmenopausal women 3. Clear cell adenocarcinoma of vaginia in females exposed to DES in utero 4. Increased risk of thrombi |
| What are some contraindications for estrogen usage? | - ER (+) breast cancer, - Hx of DVTs - Tobacco use in women > 35 years old. |
| What are possible cancer that can develop due to estrogen therapy? | Endometrial cancer and Clear cell adenocarcinoma of vagina |
| Which condition is associated with increased risk in postmenopausal women to develop endometrial cancer if treated with estrogen? | If the therapy is given without progesterone |
| In order to develop clear cell adenocarcinoma of vagina due to estrogen therapy, the woman has to be exposed to: | DES in utero |
| Degarelix is an _________________________ _____________________ . | GnRH antagonist |
| What are associated adverse effects of Degarelix? | Hot flashes and liver toxicity |
| What is the clinical use for Degarelix? | Prostate cancer |
| What kind of drugs are Goserelin and Leuprolide? | GnRH analogs |
| What are common Selective estrogen receptor modulators (SERMs)? | Clomiphene, Tamoxifen, Raloxifene |
| Antagonist at estrogen receptors in hypothalamus. | Clomiphene |
| Which SERM prevents normal feedback inhibition and increase the release of LH and FSH from pituitary, which stimulates ovulation? | Clomiphene |
| How does Clomiphene stimulate ovulation? | By preventing normal feedback inhibition of GnRH, thus increasing the release of LH and FSH. |
| Which type of infertility is treated with Clomiphene? | Infertility due to anovulation |
| What are associated side effects of Clomiphene therapy? | Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, and visual disturbances. |
| Estrogen antagonist at breast; Estrogen agonist at bone, uterus. | Tamoxifen |
| What is a severe adverse effect of Tamoxifen? | Increased risk of thromboembolic events and endometrial cancer |
| What is the clinical use for Tamoxifen? | Treat and prevent recurrence of ER/PR (+) breast cancer. |
| Estrogen antagonist at breast and uterus, but agonist at bone. | Raloxifene |
| What activity increases the chances of thromboembolic events in people taking Raloxifene or Tamoxifen? | Smoking |
| What are the associated adverse effects seen with Raloxifene? | Increased risk of thromboembolic events, but NO increased risk of endometrial cancer |
| Which SERM is associated with increased risk of developing Endometrial cancer, Tamoxifen or Raloxifene? | Tamoxifen |
| What is the main or primary use for Raloxifene? | Osteoporosis |
| SERM used to treat osteoporosis | Raloxifene |
| List of common Aromatase inhibitors: | Anastrozole, Letrozole, and Exemestane |
| What is the mechanism of action of aromatase inhibitors? | Inhibit peripheral conversion of androgens to estrogen |
| What is the clinical use of Aromatase inhibitors? | ER (+) breast cancer in postmenopausal women |
| What are the main conditions treated with hormone replacement therapy? | Relief or prevention of menopausal symptoms, and osteoporosis |
| How does HRT treats/prevents postmenopausal osteoporosis? | Increased estrogen leads to a decrease in osteoclastic activity. |
| What are the associated risks of unopposed estrogen replacement therapy? | Increased risk o f endometrial cancer, - Possible cardiovascular risk |
| What are some common Progestins? | Levonorgestrel, medroxyprogesterone, etonogestrel, norethindrone, and megestrol |
| Levonorgestrel is a very common ________________. | Progestin |
| What is MOA of progestins? | Bind to progesterone receptors, decreasing growth and increase vascularization of endometrium, and thickening cervical mucus |
| What are the effects of progestins in the endometrium? | Increase growth and vascularization Thicken the cervical mucus |
| What are two common antiprogestins? | Mifepristone and Ulipristal |
| Mifepristone is an _____________________________. | Antiprogestin |
| MOA of antiprogestins | Competitive inhibitors of progestins at progesterone receptors |
| What is the clinical use for Mifepristone? | Termination of pregnancy |
| Mifepristone must be given with ___________________ to terminate a pregnancy. | Misoprostol |
| Ulipristal is used for: | Emergency contraception |
| What drugs if given together can case termination of pregnancy? | Mifepristone with misoprostol |
| Combined contraception is composed of: | Progestins and ethinyl estradiol |
| Ethinyl estradiol + Progestins = | Combined contraception |
| What are the possible presentations of combined contraception? | Pill, patch, and vaginal ring |
| How does combined therapy prevent pregnancy? | 1. Progestins and Estrogen inhibit LH/FSH and thus prevent estrogen surge 2. Progestins cause thickening of cervical mucus, thereby limiting access of sperm to uterus 3. Progestins inhibit endometrial proliferation --> less suitable for implantation |
| What does the inhibition of LH/FSH cause in combined contraception? | No estrogen surge --> No LH surge == NO ovulation |
| List of people with contraindicated combined therapy: | 1. Smokers > 35 years old 2. Patients with increased risk of CV disease 3. Migraine patients 4. Breast cancer patients 5. Liver disease patients |
| Which component of combined contraceptive causes a less suitable endometrium for explanation? | Progestins |
| What is the mechanism of action of the Copper intrauterine device? | Produces local inflammatory reaction toxic to sperm and ova, prevention fertilization and implantation; hormone free |
| How does a young woman with a Copper intrauterine device is wrong by saying, "this method has my hormones all over the place"? | The copper intrauterine device is hormone free |
| Apparatus used for contraception that provides a hostile and toxic environment for sperm and ova? | Copper intrauterine device |
| What is the most effective emergency contraception? | Copper intrauterine device |
| What are associated adverse effects of Copper intrauterine device as a contraceptive method? | -Havier or longer menses, dysmenorrhea. - Risk of PID with insertion |
| What are Tocolytics? | Medications that relax the uterus |
| What are some common Tocolytics? | Terbutaline, Nifedipine, and indomethacin |
| What is the purpose of using tocolytics? | Reduce contraction frequency in preterm labor and allow time for administration of steroids or allowance for transference to proper obstetrical care unit. |
| Terbutaline is a: | B2-agonists tocolytic |
| What is the purpose of administering steroids to preterm baby? | Promote fetal lung maturity |
| What is the mechanism of action of Danazol? | Synthetic androgen that act as partial agonist at androgen receptors. |
| What are the clinical uses for Danazol? | Endometriosis (MC), and Hereditary angioedema |
| Which common obstetric conditions is treated with Danazol? | Endometriosis |
| "Chocolate cyst" pathology is often treated with ___________. | Danazol |
| Synthetic androng that act as a partial agonist at androgen receptor | Mechanism of action of Danazol |
| Adverse effects of Danazol: | - Weight gain, edema, acne - Hirsutism, masculinization - Decreased HDL levels - Hepatotoxicity - Pseudotumor cerebri |
| Agonists at androgen receptor | Testosterone and Methyltestosterone |
| Organic androgen receptor agonist | Testosterone |
| Synthetic androgen receptor agonist | Danazol |
| What are the main uses of Testosterone (exogenous)? | 1. Treat hypogonadism and promote development of secondary sex characteristics 2. Stimulate anabolism to promote recovery after burn or injury |
| What is the lesser common used for testosterone? | Stimulate anabolism to promote recovery after burn or injury |
| What is the adverse effect of exogenous testosterone in females? | Masculinization |
| What is the adverse effect of exogenous testosterone in males? | Decrease intratesticular testosterone leading to inhibited release of LH which cause gonadal atrophy |
| Male gonadal atrophy is often seen as a adverse effect of exogenous __________________. | Testosterone |
| What is a male and female adverse effect of the use of testosterone? | Premature closure of epiphyseal plate, increase in LDL, and decrease in HDL. |
| List of common antiandrogenic medications? | 1. Finasteride 2. Flutamide 3. Ketoconazole 4. Spironolactone |
| Which is more potent, DHT or Testosterone? | DHT |
| Enzyme that converts testosterone into DHT? | 5-alpha-reductase |
| Testosterone ----X------------> DHT. What is X? | 5-alpha-reductase |
| What is an important and common 5a-reductase inhibitor? | Finasteride |
| What are the 2 uses for Finasteride? | 1. BPH 2. Male-pattern baldness |
| What associated adverse effects of Finasteride? | Gynecomastia and sexual dysfunction |
| MOA of Flutamide: | Nonsteroidal competitive inhibitor at androme receptors |
| Which medication is a non-steroidal competitive inhibitor at androgen receptors? | Flutamide |
| What is the clinical use for Flutamide? | Prostate carcinoma |
| What is the overall purpose of Ketoconazole? | Inhibits steroid synthesi |
| Which enzymes are inhibited by Ketoconazole? | - 17, 20 desmolase - 17-a-hydroxylase |
| Antiandrogen known to inibito 17-alpha-hydroxylase | Ketoconazole |
| What is the result of Ketoconazole inhibition of desmolase and 17a-hydroxylase? | Inhibit steroid synthesis |
| What is the main use for Ketoconazole? | Reduce androgenic symptoms of PCOS |
| Which are antiandrogens that can be used to reduce androgenic symptoms of PCOS? | Ketoconazole and Spironolactone |
| What are the associated adverse effects of Ketoconazole and Spironolactone? | Gynecomastia and amenorrhea |
| Spironolactone works by: | Inhibition of steroid binding, by inhibiting desmolase and 17-a hydroxylase. |
| What is the difference in MOA between Spironolactone and Ketoconazole? | Ketoconazole ---- inhibits steroid SYNTHESIS Spironolactone --- inhibits steroid BINDING |
| Which antiandrogen inhibits steroid synthesis, Ketoconazole or Spironolactone? | Ketoconazole |
| Which antiandrogen inhibits steroid binding, Ketoconazole or Spironolactone? | Spironolactone |
| alpha-1 antagonist used to treat BPH by inhibit smooth muscle contraction. | Tamsulosin |
| Which medication is seen as Selective for alpha-1A/D receptors on prostate vs vascular a-1B recetpros? | Tamsulosin |
| Which alpha receptors on prostate are selective by Tamsulosin | Alpha-1A/D |
| Tamsulosin MOA: | Alpha-1 antagonist used in BPH, that inhibits smooth muscle contraction |
| Which three medications are known to treat BPH? | Finasteride, Tamsulosin and Tadalafil |
| What are common Phosphodiesterase type 5 inhibitors? | Sildenafil, vardenafil, and tadalafil |
| PDE-5 inhibitors cause an _____________ in cGMP. | Increase |
| The increase in cGMP caused by sildenafil leads to: | Prolonged smooth muscle relaxation in response to nitric oxide |
| Which part of hte peins recieves more blood by the use of Viagra? | Corpus cavernosum of penis |
| While blood flow to corpus cavernosum of penis is increased, what other effect occurs with PDE-5 inhibitors? | Decrease poumomary vascular resistance |
| What is the clinical use for PDE-5 inhibitors? | 1. Erectile dysfunction 2. Pulmonary hypertension 3. BPH (Tadalafil only) |
| Which is the only PDE-5 inhibitor used to treat BPH? | Tadalafil |
| Adverse effects with PDE-5 inhibitors: | - Headache, flushing, dyspepsia, cyanopsia - Risks of life-threatening hypotension if taken with nitrates |
| Which are extremely contraindicated in a patient taking sildenafil? | Nitrates |
| What is the MOA of MInoxidil? | Direct arteriolar vasodilator |
| Clinical use for Minoxidil | 1. Androgenetic alopecia (pattern baldness) 2. Severe refractory hypertension |
| Why would a male try to hide the fact he is taking MInoxidil? | Its primary clinical use is for androgenetic alopecia |
| Which are drugs that treat male baldness? | Minoxidil and Finasteride |
Created by:
rakomi
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