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FA complete review part 4 Pharmacology

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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