Drug Table - Reproduction Flashcards
Class for: Estradiol (valerate & cypionate) Estrone sulfate Equilin sulfate Quinestrol
Estradiol esters
steroidal
Class for:
Ethinyl estradiol
Mestranol
Alkyl estrogen
Mechanism for: Estradiol (valerate & cypionate) Estrone sulfate Equilin sulfate Quinestrol
Ethinyl estradiol
Mestranol
Absorbed through skin, mucus membranes,
GI Tract; body-wide distribution via sexhormone
binding globulin
Therapeutics for: Estradiol (valerate & cypionate) Estrone sulfate Equilin sulfate Quinestrol
Ethinyl estradiol
Mestranol
Contraception, primary hypogonadism,
postmenopausal hormone therapy
Imp side effects for: Estradiol (valerate & cypionate) Estrone sulfate Equilin sulfate Quinestrol
Ethinyl estradiol
Mestranol
Weight gain, HTN; less commonly,
may cause breast cancer, DVT,
cervical and endometrial cancer
Other side effects for: Estradiol (valerate & cypionate) Estrone sulfate Equilin sulfate Quinestrol
Ethinyl estradiol
Mestranol
Nausea, breast tension/pain,
vaginal bleeding, headache
Misc for: Estradiol (valerate & cypionate) Estrone sulfate Equilin sulfate Quinestrol
Ethinyl estradiol
Mestranol
Strongly contraindicated in breast or endometrial cancers, endometriosis, undiagnosed vaginal bleeds; relatively contradinicated in pregnancy, thromboembolic disease, HTN, hepatic disease, family history of breast or uterine cancer
Diethylstilbestrol class
Non-steroidal
synthetic estrogen
Diethylstilbestrol Imp side effect
Increased risk of clear cell
adenocarcinoma of vagina & cervix
Tamoxifen citrate (Nolvadex) class
Non-steroidal antiestrogen;
selective
estrogen receptor
modifier
Tamoxifen citrate (Nolvadex) mechanism
Blocks estrogen from binding ER and
causing growth in ER(+) breast cancer
Tamoxifen citrate (Nolvadex) therapeutics
ER(+) breast cancer
Tamoxifen citrate (Nolvadex) imp side effects
Pro-estrogenic effect on uterine epithelium (increase risk of endometrial cancer); partial estrogen agonist in bone and endometrium
Tamoxifen citrate (Nolvadex) misc
Anti-estrogenic effect on mammary
epithelium; must be used in very
high doses
Clomiphene citrate (Clomid) class
Non-steroidal antiestrogen
Clomiphene citrate (Clomid) mechanism
Blocks estrogen binding to hypothalamic
receptors (no estradiol negative feedback
on gonadotropins) –> increased secretion
of gonadotropins & LH –> ovulation
Clomiphene citrate (Clomid) therapeutics
Stimulate ovulation in patients who
want to get pregnant
Clomiphene citrate (Clomid) imp side effects
Hot flashes, multiple pregnancy
Clomiphene citrate (Clomid) other side effects
Stomach pain, headache, upset
stomach, vomit
Clomiphene citrate (Clomid) misc
Cis-isomer (zuclomiphene) is a weak
estrogen agonist; trans-isomer
(enclomiphene) is a potent estrogen
antagonist
Class
Micronized progesterone
Transvaginal progesterone
Natural
progesterone
Therapeutics for
Micronized progesterone
Transvaginal progesterone
Contraception, hormone replacement
therapy
Imp side effects for
Micronized progesterone
Transvaginal progesterone
Fatigue, drowsiness
Misc for
Micronized progesterone
Transvaginal progesterone
Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
Class for: Medroxyprogesterone Norethindrone Norgestrel Megestrol
Synthetic
progesterone
Therapeutics for: Medroxyprogesterone Norethindrone Norgestrel Megestrol
Contraception, hormone replacement
therapy
Imp side effects for: Medroxyprogesterone Norethindrone Norgestrel Megestrol
Edema, abdominal bloating; less
commonly: strong androgenic
effects (hirsutism, acne)
Other side effects for: Medroxyprogesterone Norethindrone Norgestrel Megestrol
Anxiety, irritability, depression,
muscular pain; increased risk of
thrombus and PE
Misc for: Medroxyprogesterone Norethindrone Norgestrel Megestrol
Contraindicated in thromboembolic disorders or patients with such a history, liver disease (metabolised in the liver), undiagnosed vaginal bleeding, pregnancy (atrophy of endometrium leading to birth defects)
Class for:
Monophasic Ortho-Novum
Biphasic Ortho-Novum
Triphasic Ortho-Novum
Combination pill
Mechanism for:
Monophasic Ortho-Novum
Biphasic Ortho-Novum
Triphasic Ortho-Novum
Constant level of estrogen suppresses FSH,
LH surge; progesterone suppresses LH
surge, thickens cervical mucus, leads to
endometrial atrophy
Therapeutics for:
Monophasic Ortho-Novum
Biphasic Ortho-Novum
Triphasic Ortho-Novum
Contraception
Imp side effects for:
Monophasic Ortho-Novum
Biphasic Ortho-Novum
Triphasic Ortho-Novum
As with synthetic estrogen and
progesterones
Monophasic Ortho-Novum Misc
Consistent dose of estrogen and
progestin (only take 21 days)
Biphasic Ortho-Novum Misc
Fixed estrogen, progestin increased
for days 11-21
Triphasic Ortho-Novum Misc
Fixed or variable estrogen, while
progestin increases in 3 phases (1-7,
8-14, 15-21)
Mini-pill class
Progestin only
Mini-pill mechanism
As progestin
Mini-pill Therapeutics
Less effective than combination pill for contraception; use when patient has estrogen contraindication; good in lactating women (estrogen reduces milk production)
Mini-pill imp side effect
More likely to produce irregular menstrual cycle (estrogen required to provide stability to endometrium)
Mini-pill other side effect
Suppresses endometrial cancer
Levonorgestrel (Plan B) class
Synthetic
progestogen
Levonorgestrel (Plan B) Mechanism
Not known
Levonorgestrel (Plan B) Therapeutics
Prevent implantation
Levonorgestrel (Plan B) Imp side effect
Likely the same as combination
oral contraceptives
Levonorgestrel (Plan B) misc
Must be taken within 72 hours of
coitus
Mifepristone (RU-486, Korlym) class
Anti-progestin;
glucocorticoid
receptor
antagonist
Mifepristone (RU-486, Korlym) Mechanism
Competitively binds to progesterone
receptor (leading to detachment of fetus);
glucocorticoid recepter antagonist
Mifepristone (RU-486, Korlym) Therapeutics
Abortion; Cushing’s Syndrome
Mifepristone (RU-486, Korlym) Misc
Must take early in pregnancy (by day 49); oral administration; must be given by doctor in medical facility prepared for surgery if abortion incomplete
Class for:
Sildenafil citrate (Viagra)
Vardenafil HCl (Levitra)
Tadalafil (Cialis)
PDE5 inhibitor
Mechanism for: Sildenafil citrate (Viagra) Vardenafil HCl (Levitra) Tadalafil (Cialis)
Bind catalytic site of PDE5; inhibits PDE5
breakdown of cGMP –> decreased Ca –>
smooth muscle relaxation –> erection
Therapeutics for:
Sildenafil citrate (Viagra)
Vardenafil HCl (Levitra)
Tadalafil (Cialis)
Erectile dysfunction; does not trigger an
automatic erection, but improves
response to sexual stimulation
Imp side effects for:
Sildenafil citrate (Viagra)
Vardenafil HCl (Levitra)
Tadalafil (Cialis)
Headache, dizziness, change in
vision (NAION)
Other side effects for:
Sildenafil citrate (Viagra)
Vardenafil HCl (Levitra)
Tadalafil (Cialis)
Flushing, upset stomach, stuffy
or runny nose, UTI, diarrhea
Misc for: Sildenafil citrate (Viagra) Vardenafil HCl (Levitra)
Oral (once/day max); half-life of 4 hours, peak plasma concentration in 1-2 hours; contraindicated if on nitrates or α-blockers (unsafe drop in BP)
Misc for:
Tadalafil (Cialis)
Oral (once/day max); half-life of 17.5 hours, peak plasma concentration in 1-2 hours; contraindicate if on nitrates or α-blockers (unsafe drop in BP)
