Drugs-repro Flashcards
Testosterone
Methyltestosterone
M: agonists at androgen receptors
U: treat hypogonadism and promote development of 2º sex characteristics; stimulate anabolism to promote recovery after burn or injury.
E: masculinization in females; -intratesticular testosterone in males by inhibiting release of LH (via negative feedback)–>gonadal atrophy. Premature closure of epiphyseal plates. +LDL, - HDL
Finasteride
Antiandrogen
M: 5alpha-reductase inhibitor (- conversion of testosterone to DHT).
U: BPH and male pattern baldness
Ketoconazole
Antiandrogen
M: inhibits steroid synthesis (inhibits 17,20 desmolase/17alpha-hydroxylase).
U: PCOS to reduce androgenic symptoms
E: gynecomastia and amenorrhea
Spironolactone
Antiandrogen
M: inhibits steroid binding, 17/20 desmolase/17alpha-hydroxylase
U: PCOS to reduce androgenic symptoms
E: gynecomastia and amenorrhea
Tamsulosin
M: alpha1-antagonist, inhibits smooth muscle contraction. selective for alpha1A/D receptors (found on prostate) vs vascular alpha1B receptors
U: treat BPH
Sildenafil
Vardenafil
Tadalafil
Phosphodiesterase type 5 inhibitors
M: inhibit PDE5–>+cGMP–>prolonged smooth muscle relaxation in response to NO–>+blood flow in corpus cavernosum of penis, - pulmonary vascular resistance
U: erectile dysfunction, pulmonary hypertension, BPH(tadalafil only)
E: headache, flushing, dyspepsia, cyanopia (blue-tinted vision). risk of life-threatening hypotension in patients taking nitrates
Minoxidil
M: direct arteriolar vasodilator
U: androgenetic alopecia (pattern baldness), severe refractory hypertension .
Mifepristone
Ulipristal
Antiprogestins
M:competitive inhibitor of progestins at progesterone receptors
U: termination of pregnancy (mifepristone+misoprostol), emergency contraception (ulipristal)
Mifepristone + Misoprostol (PGE1 analog) used in combination for medically induced abortions. Misoprostol induces uterine contractions. Methotrexate is used for ectopic pregnancies
Combined contraception
Progestins and ethanol estradiol; forms include pill, patch, vaginal ring.
Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge–>no LH surge–>no ovulation
Progestins cause thickening of cervical mucus, thereby limiting access os sperm to uterus. Progestins also inhibits endometrial proliferation–>endometrium is less suitable to the implantation of an embryo.
Contraindications: smokers>35 years old(+risk of cardiovascular events), patients with +risk of cardiovascular disease (including history of venous thromboembolism, coronary artery disease, stroke), migraine (especially with aura), breast cancer
Combined contraception
Progestins and ethanol estradiol; forms include pill, patch, vaginal ring.
Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge–>no LH surge–>no ovulation
Progestins cause thickening of cervical mucus, thereby limiting access os sperm to uterus. Progestins also inhibits endometrial proliferation–>endometrium is less suitable to the implantation of an embryo.
Contraindications: smokers>35 years old(+risk of cardiovascular events), patients with +risk of cardiovascular disease (including history of venous thromboembolism, )
Copper intrauterine device
M: produces local inflammatory reaction toxic to sperm and ova, preventing fertilization and implantation; hormone free.
U: long-acting reversible contraception. Most effective emergency contraception.
E: heavier or longer menses, dysmenorrhea. Risk of PID with insertion (contraindicated in active pelvic infection)
Danazol
M: synthetic androgen that acts as partial agonist at androgen receptors.
U: endometriosis, hereditary angiodema
E: weight gain, edema, acne, hirsutism, masculinization, -HDL levels, hepatotoxicity, pseudo tumor cerebri.
Leuprolide
M: GnRH analog with agonist properties when used in pulsatile fashion; antagonist properties when used in continuous fashion (downregulates GnRH receptor in pituitary–> -FSH/LH).
U: uterine fibroids, endometriosis, precocious puberty, prostate cancer, infertility.
Ethinyl estradiol
DES
Mestranol
Estrogens
M: bind estrogen receptors.
U: hypogonadism or ovarian failure, menstrual abnormalities, hormone replacement therapy in postmenopausal women; use in men with androgen-dependent prostate cancer.
E: +risk of endometrial cancer (when given without progesterone), bleeding in postmenopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero, + risk of thrombi.
Contraindications-ER+breast cancer, history of DVTs
Clomiphene
Selective estrogen receptor modulators
M: antagonist at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and + release of LH and FSH from pituitary, with stimulates ovulation.
U: to treat fertility due to an ovulation (eg.PCOS).
E: may cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances.
