week 9 male and female repo x2 Flashcards
contraception, infertility, menupause symptoms
what is the moa of **Ethinyl Estradiol/Drospirenone **(Yaz, Yasmin) & Ethinyl Estradiol/Norgestimate (Ortho Cyclen, Ortho Tri-Cyclen)?
- These are combined oral contraceptives (OCPs) containing ethinyl estradiol (an estrogen) and a progestin (drospirenone or norgestimate).
- Estrogen (ethinyl estradiol): Binds to estrogen receptors.
- Progestins (drospirenone/norgestimate): Bind to progesterone receptors, decreasing endometrial proliferation and increasing cervical mucus viscosity.
Together, they:
* **Inhibit LH and FSH **via negative feedback to the hypothalamus and pituitary.
* Prevent ovulation by blocking the LH surge.
* Thicken cervical mucus, making it harder for sperm to penetrate.
* Make the endometrium less suitable for implantation.
Mnemonic: “OCPs STOP Pregnancy”
Suppresses LH/FSH
Thickens mucus
Ovulation blocked
Prevents endometrial thickening
What are the clinical uses of combined OCPs Estradiol/Drospirenone, Ethinyl Estradiol/Norgestimate/drospirenone (Yaz, Yasmin, Ortho Cyclen, Ortho Tri-Cyclen)?
Contraception, dysmenorrhea, endometriosis, PCOS
What are the major adverse effects of combined OCPs?
Estradiol/Drospirenone, Ethinyl Estradiol/Norgestimate/drospirenone (Yaz, Yasmin, Ortho Cyclen, Ortho Tri-Cyclen)?
Breakthrough bleeding, breast tenderness, venous thromboembolism (VTE), hypertension, hepatic adenomas.
“3 B’s & 3 T’s” Mnemonic
Bleeding (breakthrough)
Breast tenderness
Blood clots (VTE risk)
Thromboembolism
Tumors (hepatic adenomas)
Tension (hypertension)
In which populations are combined OCPs contraindicated?
Women >35 who smoke, history of thromboembolism, estrogen-dependent tumors.
Don’t Give OCPs To HOT Women”
History of thromboembolism
Older than 35 & smoking
Tumors (estrogen-dependent cancers)
What is the mechanism of action of progestins?
Desogestrel, Levonorgestrel, Norgestimate, Norethindrone, Drospirenone
Bind progesterone receptors → decrease endometrial growth, increase vascularization, thicken cervical mucus.
“Progestins = PROtect against Pregnancy”
Progesterone receptor binding
Reduces endometrial proliferation
Obstructs sperm (thickens cervical mucus)
Thin endometrium (prevents implantation)
What are the clinical uses of progestins?
Desogestrel, Levonorgestrel, Norgestimate, Norethindrone, Drospirenone
Contraception (pills, IUDs, implants, injections), endometrial cancer treatment, abnormal uterine bleeding.
What are the major adverse effects of progestins?
Desogestrel, Levonorgestrel, Norgestimate, Norethindrone, Drospirenone
Menstrual irregularities, mood changes, weight gain, bloating, possible increased risk of breast cancer.
MOA of Levonorgestrel
Progestrin aganonist- Binds progesterone receptors, leading to:
Thickened cervical mucus → Inhibits sperm penetration.
Endometrial atrophy → Prevents implantation.
Suppresses LH surge → Prevents ovulation (less reliably in emergency contraception).
What the clinical uses of Levonorgestrel?
Emergency contraception (Plan B, high-dose form).
Long-acting reversible contraception (IUD form).
Treatment of abnormal uterine bleeding (part of some hormonal IUDs).
Endometrial protection in hormone therapy.
“Levonorgestrel = Long-lasting & Emergency”
Long-acting (IUD form).
Emergency contraception (Plan B).
Very effective at thickening mucus.
Ovulation suppression (partial).
No estrogen (progestin-only).
adverse effects of levonorgestrel
Irregular menstrual bleeding (common).
Headache, nausea, breast tenderness.
Ovarian cyst formation (temporary, usually resolves spontaneously).
Potential weight gain and mood changes.
moa of copper IUD
spermicidal
adverse effects of copper Iud
heavier mustrual bleeding, increased mustral cramping- rare uterine perforation
What is the mechanism of action (MOA) of mifepristone?
Competitive progesterone receptor antagonist → Blocks progesterone action on the uterus.
What is mifepristone used for?
Medical abortion (with misoprostol) & emergency contraception.
At high doses, mifepristone also acts as a glucocorticoid receptor antagonist (used for inoperable Cushing’s syndrome).
Why is mifepristone combined with misoprostol for abortion?
Mifepristone → Blocks progesterone → Endometrial shedding & detachment.
Misoprostol (PGE₁ analog) → Induces uterine contractions for expulsion.
What are the adverse effects of mifepristone?
Heavy bleeding, cramping, nausea, vomiting, infection (rare).
What is the mechanism of action (MOA) of misoprostol and how does misoprostol work in medical abortion?
PGE₁ analog → Binds prostaglandin receptors → Increases uterine contractions & gastric mucus secretion.
Stimulates uterine contractions & cervical ripening, expelling the pregnancy (used after mifepristone).
What are the clinical uses of misoprostol?
Medical abortion (with mifepristone).
Induction of labor (off-label use).
NSAID-induced ulcer prevention.
Postpartum hemorrhage (PPH) treatment (uterotonic effect).
What is the mechanism of action of methotrexate (MTX)?
Inhibits dihydrofolate reductase (DHFR), leading to decreased thymidine monophosphate (dTMP) and impaired DNA synthesis.
Antimetabolite (Folate Analog), Immunosuppressant
What phase of the cell cycle does methotrexate target?
Methotrexate acts on the S-phase of the cell cycle, which is the DNA synthesis phase.
What are the non-oncologic indications for methotrexate?
What are the oncologic indications for methotrexate?
non oncologic:
* Autoimmune diseases such as rheumatoid arthritis, psoriasis, inflammatory bowel disease, and systemic lupus erythematosus
* Immunosuppressive therapy for vasculitis
Oncologic:
* Acute lymphoblastic leukemia (ALL)
* Lymphomas
* Choriocarcinoma
* Ectopic pregnancy (as a first-line treatment)
What are the major adverse effects of methotrexate?
Bone marrow suppression (myelosuppression), which is dose-limiting
Liver toxicity (hepatotoxicity), leading to elevated liver function tests and fibrosis
Inflammation of mucous membranes (mucositis), which can cause oral ulcers and gastrointestinal irritation
Pulmonary fibrosis
Birth defects (teratogenicity), including neural tube defects in fetuses
What is the mechanism of action of clomiphene?
Clomiphene acts as a selective estrogen receptor modulator that blocks estrogen receptors in the hypothalamus, thereby reducing the negative feedback from estrogen and increasing the secretion of gonadotropins (FSH and LH), which in turn stimulates ovulation.
What are the adverse effects of clomiphene?
Clomiphene may cause adverse effects such as hot flashes, ovarian enlargement, an increased risk of multiple pregnancies, and visual disturbances.
What is the primary clinical use of clomiphene?
Clomiphene is primarily used to treat infertility in women who experience anovulation, particularly in cases of polycystic ovary syndrome (PCOS).
What is the mechanism of action of menotropins?
Menotropins are composed of both follicle-stimulating hormone (FSH) and luteinizing hormone (LH), which work together to stimulate the growth of ovarian follicles and promote ovulation in females, as well as support spermatogenesis in males.
What are the adverse effects associated with menotropins?
The use of menotropins can lead to adverse effects such as ovarian hyperstimulation syndrome (OHSS), a higher likelihood of multiple pregnancies, and an increased risk of thromboembolic events.
What is the primary clinical use of menotropins?
Menotropins are commonly used in assisted reproductive techniques, such as in vitro fertilization (IVF), to stimulate the development of multiple ovarian follicles.
What is the mechanism of action of follitropin?
Follitropin is a recombinant form of FSH that directly stimulates the maturation of ovarian follicles in women and aids in spermatogenesis in men.
What are the adverse effects of follitropin?
The use of follitropin can lead to adverse effects including ovarian hyperstimulation syndrome, a heightened risk of multiple pregnancies, and potential allergic reactions.
What is the clinical application of follitropin?
Follitropin is primarily used to stimulate follicular development in women undergoing fertility treatments.
What is the mechanism of action of hCG?
hCG mimics the action of luteinizing hormone (LH) by binding to the LH receptors, which in women triggers ovulation and in men stimulates the production of testosterone by the Leydig cells.
What are the adverse effects of hCG?
The administration of hCG can lead to adverse effects such as ovarian hyperstimulation syndrome, an increased risk of multiple pregnancies in women, and gynecomastia in men.
What is the main clinical use of hCG?
hCG is used clinically to induce ovulation in women experiencing infertility and to stimulate testosterone production in men with hypogonadism.
