Gyn pharm Flashcards by Stacey Hansen

E2 is AKA this, and is the natural hormone
Most potent

17 beta estradiol

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17 beta estradiol is metabolized by this

First pass in liver

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This estrogen form has greater concentration than estradiol during pregnancy and after menopause

Estrone

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This is the synthetic steroidal estrogen most frequently used in hormonal contraceptives

Ethinyl estradiol

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These are two dietary components found in soy and flax, with estrogen agonist/antagonist activity
Relatively low potency

Isoflavones and lignans

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Estrogens undergo hydroxylation via these

CYP3A4 and CYP2C9

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Unopposed continuous treatment with estrogen causes an increased incidence of this type of cancer

Endometrial

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Smoking increases the risks of of exogenous estrogens – especially this

Thromboembolism

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What is the paradoxical effect of estrogen on the cardiovascular system?

Protective premenopause
AEs at higher concentrations of replacement estrogens

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Estrogens increase the risk of these 2 types of disease

Gallbladder
Thromboembolic

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How does estrogen help patients with Turner syndrome?

Mimics puberty and supports bone health

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How are the levels of FSH and LH at menopause?

Increase

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When do menopause vasomotor symptoms resolve?

within 3-5 years

without treatment

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Paroxetine is indicated for this during menopause

Vasomotor symptoms

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This SSRI is indicated for vasomotor symptoms of menopause

Paroxetine

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This is a DHEA delivered as an intravaginal insert
For dyspareunia caused by vulvovaginal atrophy

Prasterone

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Prasterone is this molecule delivered as an intravaginal insert

DHEA

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Prasterone is used to treat this

Dyspareunia

(caused by vulvovaginal atrophy)

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Synthetic progestin is derived from modification of either of these

Testosterone
17a-hydroxyprogesterone

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Testosterone derived progestin may retain some of this activity

Androgenic

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These 2 progestins have the most potent progestational, androgenic, and anti-estrogenic activity

Levonorgestrel
Norgestrel

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Levonorgestrel and Norgestrel are progestins derived from this

Testosterone

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Do Levonorgestrel and Norgestrel have estrogenic or anti-estrogenic activity?

Anti-estrogenic

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These 2 progestins derived from testosterone have slight estrogenic activity

Norethindrone
Ethynodiol diacetate

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Norethindrone and Ethynodiol diacetate are derived from this

Testosterone

Megestrol acetate, Medroxyprogesterone acetate, and Hydroxyprogesterone caproate are progestins derived from this

17a-OH progesterone

These are 3 progestins derived from 17a-OH progesterone

Megestrol acetate Medroxyprogesterone acetate Hydroxyprogesterone caproate

This is a synthetic progestin related to spironolactone

Drospirenone

Drospirenone has these 2 effects

Anti-androgenic Anti-aldosterone

Drospirenone is a synthetic progestin related to this

Spironolactone

These are 2 anti-progestins

Ulipristal acetate Mifepristone

Ulipristal acetate and Mifepristone are this type of drug

Anti-progestins (selective progesterone receptor modulators; SPRMs)

Ulipristal acetate has these 2 indications

Emergency contraception Uterine fibroids

Ulipristal acetate is contraindicated in these 3 settings

Liver disease Pregnancy Lactation

Ulipristal acetate has drug interactions with this

CYP3A4 substrates

This drug delays or prevents ovulation Indicated for emergency contraception and uterine fibroids

Ulipristal acetate

This is a progesterone antagonist that is also a glucocorticoid antagonist

Mifepristone

Mifepristone has these activities

Progesterone antagonist Glucocorticoid antagonist

Mifepristone has these 3 indications

Hyperglycemia in Cushings Pregnancy termination (until day 70) Stimulate SM contraction (when used w/ prostaglandin agonist)

Mifepristone used with prostaglandin agonist Misoprostol (PGE1 analog) is used for this

Stimulate uterine smooth muscle contraction

Mifepristone is used with this to stimulate uterine smooth muscle contraction

Prostaglandin agonist Misoprostol - PGE1 analog

Mifepristone is approved as an abortifacient until this day of pregnancy

Mifepristone has these 5 contraindications

Pregnancy Anti-coag therapy Bleeding disorders Adrenal insufficiency Breast feeding

Combination hormonal contraceptives (CHC) contain both of these

An estrogen and progestin

These are 3 types of estrogens in hormonal contraceptives

Ethinyl estradiol Estradiol valerate Mestranol

The contraceptive patch contains both of these drugs

Ethinyl estradiol Norelgestromin

This form exposes women to 60% higher overall estrogen levels than CHC pills

Contraceptive patch (b/c of the sustained hormone release from the patch)

the vaginal ring contains both of these drugs

Ethinyl estradiol Norelgestromin

Smokers over this age should not use CHC

Contraceptive AEs of venous thrombosis and liver effects are due to this component

Synthetic estrogens

Contraceptive AEs of hyperlipidemia, hyperglycemia, and atherosis are due to this component

Progestins

Should a patient with a history of DVT, stroke, or MI use CHC?

NO contraindicated

Risk of this type of cancer increases with CHC

Cervical cancer

Risk of these 2 types of cancers decrease with CHC

Ovarian and endometrial

This type of contraceptive can be used during lactation

Progestin-only

Can Progestin-only contraceptives be used during lactation?

Yes

What is Norethindrone?

Progestin only pill

This is a progestin-only pill

Norethindrone

This is a depot prep containing progestin alone Implanted under skin of upper arm Effective for 3 years

Etonogestrel

What is Etonogestrel?

Depot prep of progestin alone (implanted under skin of upper arm)

This is a progestin-only IM injection q3 months May cause reduced bone density if used for 2+ years

Medroxyprogesterone acetate

Medroxyprogesterone acetate contains this

Progestin only

This is the main side effect of progestin-only contraceptives

Menstrual cycle irregularity (breakthrough bleeding, spotting, amenorrhea)

These are 2 types of IUDs

Copper IUD IUDs that release Levonorgestrel

IUDs are recommended for women with no history of this

Pelvic inflammatory disease

This is the MOA of IUDs

cause inflammatory reaction (increased cytokine synthesis) in the uterus that is toxic to sperm and ova

This form of contraceptive causes an inflammatory response (increased cytokines) in the uterus that is toxic to sperm and ova

IUD

These are 5 methods of postcoital/emergency contraception

Progestin alone (levonorgestrel) Ulipristal acetate (SPRM) High dose CHC High dose steroids IUD

This progestin-only drug is used for postcoital/emergency contraception

Levonorgestrel

This component of high dose CHC is a strong emetic

Estrogen

These delay/prevent ovulation, disrupt the uterine endometrium and pituitary gonadotropin secretion, interfere with gamete transport Cause development of a non-receptive endometrium

High dose steroids

Antiretrovirals and antiepileptics have what effect on steroidal contraceptives?

Decrease efficacy

How do Coumarin, acetaminophen, levothyroxine, and lamotrigine interact with steroidal contraceptives?

Their efficacy is decreased

List 4 drugs whose efficacy is decreased by steroidal contraceptives

Coumarin Acetaminophen Levothyroxine Lamotrigine

How do Cyclosporine, theophylline, imipramine, corticosteroids, and tizanidine interact with steroidal contraceptives?

Their efficacy is increased

Is the efficacy of corticosteroids changed when used with steroidal contraceptives?

Yes - increased efficacy

Tamoxifen is an estrogen agonist at this

Uterus and bone

Tamoxifen is an estrogen antagonist at this

Breast (so indicated for ER+ breast cancer)

Raloxifene is an estrogen agonist at this

Bone

Raloxifene is an estrogen antagonist at this

Endometrium Breast

This SERM is an antagonist at the hypothalamus Blocks the early follicular phase negative feedback of E2 Results in increased number of mature follicles

Clomiphene citrate

Clomiphene citrate is what type of drug?

SERM (antagonist at hypothalamus)

Clomiphene citrate is an estrogen antagonist at this site

Hypothalamus

Clomiphene citrate is indicated for this

Fertility increases ovulation rate; increases number of mature follicles

This is the AE of Clomiphene citrate

Thick cervical mucus

This SERM is indicated for dyspareunia caused by vulvar and vaginal atrophy after menopause

Ospemifene

Ospemifene is a SERM indicated for this

Dyspareunia (caused by vulvar/vaginal atrophy after menopause)

Ospemifene is an estrogen agonist at these sites

Vaginal epithelium endometrium bone

This is the AE of Ospemifene

Risk of VTE

This is the indication for Bazedoxifene

Vasomotor symptoms of menopause

This SERM does not cause CNS symptoms of menopause (such as hot flashes)

Bazedoxifene

This is an estrogen receptor antagonist 7a-alkylamine derivative of estradiol

Fulvestrant

What is the MOA of Fulvestrant?

Inhibits estrogen receptor dimerization is an antagonist

This is the indication for Fulvestrant

ER+ metastatic breast cancer in postmenopausal women with disease progression on Tamoxifen

these are 2 SERMs indicated for breast cancer

Tamoxifene Raloxifene

Does Fulvestrant affect all tissues that express estrogen receptors?

Yes so will cause hypoestrogenic symptoms

Anastrozole is this type of drug

Reversible aromatase inhibitor

Letrozole is this type of drug

Reversible aromatase inhibitor

Exemestane is this type of drug

Irreversible aromatase inhibitor

List 3 aromatase inhibitors

Anastrozole Letrozole Exemestane

Aromatase inhibitors are indicated for this

ER+ metastatic breast cancer (when tamoxifen has failed)

With use of this type of drug, all tissues that respond to estrogen will be affected Resulting in symptoms of hypo-estrogenicity (e.g. hot flashes), vaginal dryness, decreased libito Creates a chemical menopause

Aromatase inhibitors

Administering GnRH-superagonists in a continuous manner results in this

Down-regulation of GnRH receptors in the pituitary = inhibition of FSH and LH

With use of this type of drug, there is a flare-up in steroid secretion from the drugs at first Due to initial increase in LH/FSH Eventually is downregulated

GnRH superagonists

Leuprolide is this type of drug

GnRH superagonist

Goserelin is this type of drug

GnRH superagonist

Nafarelin is this type of drug

GnRH superagonist

Histrelin and triptorelin are this type of drug

GnRH superagonist

This type of drug is indicated for uterine fibroids, endometriosis, precocious puberty, and prostate cancer

GnRH superagonist

GnRH superagonist are indicated in this frequency for pregnancy and cancer

Pulsatile for pregnancy Continuous for cancer

This type of drug is administered in pulsatile mechanism for pregnancy, and continuous for cancer

GnRH superagonist

With use of GnRH superagonists, initial "flare" of steroidogenesis may require treatment with this

Androgen or estrogen receptor blocker

Degarelix is this type of drug

GnRH antagonist

Ganirelix, Cetrorelix, and Elagolix are this type of drug

GnRH antagonists

This is the main indication for GnRH antagonists

Prevention of estrogen/LH surge during super-stimulation

This GnRH antagonist is also used for prostate cancer

Degarelix

Degarelix is a GnRH antagonist also used for this

Prostate cancer

This GnRH antagonist is also used for pain of endometriosis

Elagolix

Menotropin, Urofollitropin, and Follitropin are this type of drug

Gonadotropins (combos of LH and FSH)

These are 4 types of treatment for ER+ breast cancer

SERMs (tamoxifen, raloxifene) ER antagonist (Fulvestrant) Aromatase inhibitors GnRH superagonists

These are 3 types of treatments for ER+ Her2- breast cancer

CDK4 and CDK6 inhibitors mTOR inhibitor Microtubule inhibitor

Palbociclib, Ribociclib, and bemaciclib are this type of drug

CDK4 and CDK6 inhibitors

Palbociclib, Ribociclib, and bemaciclib are used to treat this

ER+, Her2- breast cancer (are CDK4 and CDK6 inhibitors)

List the 3 CDK4 and CDK6 inhibitors that may be used in the treatment of ER+, HER2- breast cancer

Palbociclib Ribociclib Bemaciclib

This mTOR inhibitor may be used in the treatment of ER+, HER2- breast cancer

Everolimus

This microtubule dynamic inhibitor may be used in the treatment of ER+, HER2- breast cancer

Eribulin

Everolimus and Eribulin can be used to treat this

ER+, HER2- breast cancer

These are 3 types of treatments for ER-, HER2+ breast cancer

HER2 antibodies Ado-trastuzumab emtansine EGFR/EGFR2 inhibitors (Lapatinib, Neratinib)

What are Lapatinib and Neratinib?

Dual EGFR and EGFR2 tyrosine kinases inhibitors

These are 2 dual EGFR and EGFR2 tyrosine kinases inhibitors

Lapatinib Neratinib

These are 2 HER2 antibodies

Trastuzumab Pertuzumab

Ad-trastuzumab emtansine is conjugated to this, and can be used to treat ER- HER2+ breast cancer

Mertansine (which binds tubulin)

These are 4 types of drugs that can be used to treat endometriosis (surgery is also an option)

CHCs Progestins GnRH antagonist (Elagolix) GnRH superagonists (Leuprolide)

These are 5 types of treatment for fibrocystic breast condition

Bromocriptine Oral contraceptives Progestins Tamoxifen Danazol

This is a dopaminergic agent that cuts prolactin secretion Can be used to treat fibrocystic breast condition

Bromocriptine

This is a weak androgen and antiestrogen that may be used in the treatment of fibrocystic breast condition

Danazol

These are 4 types of treatment for Hirsutism

Oral contraceptives Glucocorticoids Spironolactone Eflornithine

What is the MOA of Eflornithine?

Ornithine decarboxylase inhibitor

This is an ornithine decarboxylase inhibitor Indicated for hirsutism

Eflornithine

Eflornithine is indicated for this

Hirsutism

This drug is an agonist at 5-HT1a and antagonist at 5-HT2a receptors Indicated for hypoactive sexual desire disorder

Flibanserin

Flibanserin is indicated for this

Hypoactive sexual desire disorder

How can Black Cohosh interfere with steroids?

Is a natural SERM

St John's wort has this effect on steroids

Induces CYP3A4 = increased metabolism

Grapefruit juice has this effect on CYP3A4

Inhibits

This Stimulates uterine contractions Indications: augmentation of labor, prevention or control of uterine bleeding after delivery AE: uterine rupture, maternal and/or fetal death

Oxytocin

This is a PGE1 agonist Used for prevention of NSAID ulcers and induction of labor

Misoprostol

What is Misoprostol?

PGE1 agonist

What is Dinoprostone?

PGE2 agonist

What is Carboprost?

PGF2a agonist

These are 3 prostaglandin agonists that can be used to stimulate myometrium contraction

Misoprostol (PGE1) Dinoprostone (PGE2) Carboprost (PGF2a)

This ergot alkaloids stimulates uterine contractions, used to prevent uterine bleeding and atony after delivery or expulsion of the placenta

Methylergonovine

These are 5 types of tocolytics (prevent or halt premature labor)

Progesterone Beta 2 agonists Ca2+ channel blockers MgSO4 COX inhibitors

This progesterone may be used as a tocolytic

Hydroxyprogesterone caproate

This beta 2 agonist may be used as a tocolytic

Terbutaline

This Ca2+ channel blocker may be used as a tocolytic

Nifedipine

This compound uncouples excitation-contraction coupling of smooth muscle cells of the myometrium Used as tocolytic

MgSO4

This NSAID can be used as a tocolytic

Indomethacin

This antihistamine and vit B6 analog combo is used for N&V of pregnancy

Doxylamine + Pyridoxine

Doxylamine is this type of drug

H1-antihistamine

Doxylamine is used in combo with this for nausea and vomiting of pregnancy

Pyridoxine

Doxylamine + Pyridoxine combo is indicated for this

Nausea and vomiting of pregnancy

Gyn pharm Flashcards

(162 cards)