IGP-9 Kouzi Test 1 - Mens and Women's Health

What are the selective alpha 1 adrenoceptor antagonists

prazosin

doxazosin

terazosin

tamsulosin

alfuzosin

ALL of the selective alpha 1 adrenoceptor antagonists that we use in BPH are ___________ (__________) pharmacologic antagonists.

competitive

(reversible)

Prazosin is contraindicated with

BP medications

T or F: Selective alpha 1 adrenoreceptor antagonists decrease the size of the prostate gland.

false, does not decrease the size

which selective alpha-1 adrenoreceptors cause less hypotension

tamsulosin

silodosin

(high affinity for A1)

How do selective alpha-1 adrenoreceptors work?

block A1 receptors causing relaxation of the prostate and allowing peeing to be easier

Use of alpha-1 adrenoreceptors

treat urinary obstruction and retention

Main ADR of selective alpha-1 adrenoreceptors

postural hypotension

why do selective alpha-1 adrenoreceptors cause postural hypotension

block alpha 1 in vascular smooth muscle cells of arteries and veins = vasodilation

what drugs are an antiandrogen

finasteride

dutasteride

antiandrogens are also known as

5a-reductase inhibitors

T or F: Antiandrogens decrease the size of the prostate gland.

true

How do finasteride and dutasteride work?

inhibits 5-DHT and prevents the conversion of testosterone and DHT = decreases the size of the gland

what is responsible for prostate proliferation

dihydrotestosterone (DHT)

ADRs of antiandrogens/5a reductase inhibitor

decreased libido

erectile and ejaculatory dysfunction

what are the muscarinic receptor antagonists (anticholingerics)

oxybutynin

trospium

darifenacin

solifenacin

tolterodine

fesoterodine

how do muscarinic receptor antagonists work

bind to muscarinic (M2 & M3) receptor in the urinary tract = relaxation of smooth muscle, slow voiding, increased bladder capacity.

what are the 3 uses for muscarinic receptor antagonists

overactive bladder

bladder spasms

urinary incontinence

which muscarinic receptor antagonist is nonselective? (binds to ALL M1-M5)

trospium

which muscarinic receptor antagonists binds only to M2 and M3

tolterodine

Which muscarinic receptor antagonists antagonists binds to M3 receptors mainly

fesoterodine

oxybutynin

darifenacin

solifenacin

[FODS]

what is the predominant subtype of the beta receptor in the bladder?

beta-3

what drugs are selective beta-3 adrenoreceptor agonists

mirabegron

how does mirabegron work?

binds to B3 receptor and activates it = increased adenylyl cyclase concentration (cAMP) => relaxes smooth muscle and slows voiding

what are the PDE-5 inhibitors?

sildenafil

tadalafil

vardenafil

avanafil

T or F: · PDE-5 inhibitors are effective in men with loss of sexual potency due to cord injury or other damage to innervation and in men lacking libido.

False, are not effective

What must be able to happen before a PDE-5 inhibitor works?

sexual arousal (prerequisite)

🍑 👴👓lord have murthy"

how do PDE-5 inhibitors work?

(PDE-5 breaks down cGMP)

Inhibit PDE-5 = more cGMP = vasodilation and harder erection 😈 😏

what drug is a synthetic form of prostaglandin E1 (PGE1)

alprostadil

how does alprostadil work?

binds to GPCRs and activates adenylyl cyclase (more cAMP) = vasodilation and harder erection 😈 😏

how do you administer alprostadil?

urethra suppository

injection in PP 💉🍆

Spironolactone is a K sparing diuretic, an ___________ antagonist and anti_______ that can treat ___________.

aldosterone antagonist

antiandrogen

hirsutism

how does spironolactone work for excessive hair growth

partial agonist at the androgen and inhibits biosynthesis of androgen = decrease testosterone and DHT

what the helly is eflornithine?

Topical cream used to treat hirsutism

Ornithine decarboxylase inhibitor

how does eflornithine work?

irreversibly inhibits ornithine decarboxylase and inhibits biosynthesis of polyamines = decrease in hair growth

Estrogens are used for

HRT

hormonal contraception

post-menopausal

osteoprosis

what are the natural estrogens

estradiol

estrone

estriol (made from androgens)

what are the synthetic steroidal estrogens

ethinyl estradiol

mestranol

quinestrol

what are the synthetic nonsteroidal estrogens

(Im not remembering these, put in for completion)

✌😜✌

dienestrol

diethylstilbestrol

benzestrol

hexestrol

methestrol

methallenestril

chlorotrianisene

When estrogen binds to the estrogen receptor (ER), the complex will dimerize...

What happens when ER alpha and ER alpha or ER beta and ER beta forms a dimer

homodimer

When estrogen binds to the estrogen receptor (ER), the complex will dimerize...

What happens when ER alpha and ER beta forms a dimer

heterodimer

T or F: heterodimers have unique effects compared to homodimers.

true, homodimers are classic estrogen signaling

what is the most important natural progestin in humans?

progesterone

what are the first generation progestins

hydroxyprogesterone

medroxyprogesterone

megestrol

what are the second generation progestins

dimethisterone

norethindrone

norethindrone acetate

what are the third generation progestins

norgestimate

desogestrel

gestodene

which generation are the most closely related synthetic progestins, both pharmacologically and chemically, to progesterone.

first generation progestins

what are the clinical uses for progestin?

HRT

hormonal contraception producing long-term ovarian suppression

how do progestins work?

bind to progesterone receptor, dimerize/activate, form homodimers and heterodimers = bind to DNA and alter gene expression

what is the most important natural androgen secreted by the testis

testosterone

In some tissues, testosterone is converted to estradiol by the ___________ enzyme.

aromatase

what are the synthetic androgens with both androgenic and anabolic activity?

methyltestosterone

fluoxymesterone

oxymetholone

oxandrolone

what are the natural androgens?

testosterone

DHT

DHEA

androstenedione

In many target tissues, testosterone is converted to dihydrotestosterone by the ____________ enzyme. In these tissues, dihydrotestosterone is the major active androgen.

5α-reductase

basically how do androgens work?

bind to androgen receptor, regulate gene transcription = proteins exert androgenic effects

what are the two preparations of hormonal contraception?

progestin only

estrogen + progestin

what are the formulations hormonal contraceptives can be made.

oral

IUD

implantable (subcutaneous)

vaginal rings

LA IM

how do estrogens and progestin combinations work?

inhibit gonadotropins = STOP ovulation and prevents implantation of the egg

what are the two non-hormonal contraception

copper IUD

Phexxi

how does the copper IUD work?

Acts as a spermicide where it triggers an inflammatory response and kills sperms = NO fertilization

what is Phexxi composed of

Citric acid+Lactic acid+Postassium bitartrate

T or F: Copper IUD must be inserted after 3 days of protected sex?

false, 5 days or

phexxi is in what dosage form and how does it work?

vaginal gel, that once inserted decreases the pH of the vagina and inhibits sperm motility preventing fertilization

what are the different drugs for emergency contraception?

mifepristone

ulipristal

how does mifepristone work?

"antiprogestin" antagonist on progesterone receptor and glucocorticoid receptor, inhibiting signaling exerting luteolytic properties

What drug is a SPRM and inhibits ovulation

ulipristal

how does ulipristal work?

a selective progesterone receptor modulator (SPRM) that partial agonizes, decreasing receptor signaling and stimulates negative feedback loop control over LH and FSH

what drug inhibits gonadal function and suppresses ovarian function

Danazol

how does danazol work?

agonist at the progesterone, glucocorticoid and androgen receptor =

Negative feedback loop control over LH and FSH.

Inhibits P450c17 = inhibition of testosterone synthesis

How does clomiphene work?

Anti-estrogen (pure antagonist) that induces ovulation by inhibiting negative feedback of estrogen = increasing release of LH and FSH

what are the selective estrogen receptor modulators (SERMs)?

bazedoxifine

ospemifene

how do SERMs work?

partial agonist at estrogen receptor, produce estrogenic and antiestrogenic effects = recruit coregulators and transcription factors

what are the neurokinin 3 receptor antagonists

fezolinetant

how does fezolinetant work?

block NK3 receptor = prevent hot flashes

what is the steroid vaginal insert used for severe dyspareunia associated with menopausal vulvar and vaginal atrophy?

prasterone (Intrarosa)

how does prasterone (Intrarosa) work?

natural androgen (DHEA) which improves dryness. MOA not understood

what dopamine receptor agonists are used to treat hyperprolactinemia?

bromocriptine

cabergoline

how do bromocriptine and cabergoline work to treat hyperprolactinemia?

bind to D2 receptor = inhibit prolactin secretion = ovulation

what is the preferred drug for the treatment of hyperprolactinemia because:

cabergoline (greater efficacy and less ADE)

what drugs are used N/V in pregnancy?

doxylamine-pyridoxine

brand name of doxylamine-pyridoxine

diclegis

T or F: Use of doxylamine-pyridoxine combination does not increase the risk of birth defects.

true

doxylamine has substantial ___________ and ___________ properties

sedative

anticholinergic