416 Exam 4 ED, HRT Flashcards
MOA of PDE-5 inhibitors
Selective inhibition of phosphodiesterase type 5 isoenzymes
-inhibits catabolism of cGMP
PDE-5 inhibitor agents
Sildenafil (Viagra)
Vardenafil (Levitra, Staxyn)
Tadalafil (Cialis)
Avanafil (Stendra)
PDE-5 inhibitor DDI
Nitrates
Alpha blockers (terazosin, doxazosin)
3A4 inhibitors
PDE-5 inhibitor AE
- HA
- flushing
- congestion
- dyspepsia
- dizziness
- hypotension
- visual effects
- hearing loss
- back/limb pain/myalgia
- priapism
Sildenafil dosing
50mg prn
- onset: 30-60min
- duration: 4hrs
- empty stomach
- PDE-6
Tadalafil Dosing
10mg prn OR
- 5-5mg QD
- onset: 30min-6hr
- duration: 24-36hrs
- PDE-11
MOA of Alprostadil
Stimulates adenyl cyclase which increases cAMP and leads to enhanced blood flow to the corpora cavernosa
Alprostadil dosage forms
Intracevernosal injection (Caverject) Intraurethral insert (MUSE)
AE of intracavernosal Alprostadil
- cavernosal plaques
- penile curvature/pain
- priaprism
- injection site hematoma
AE of intraurethral Alprostadil
- urethral injury/pain
- priaprism
- female vaginal burning/pain
Primary trt for hyperprolactinemia
Dopamine agonist (cabergoline > bromocriptine)
Initial trt for ovulatory dysfunction
Clomiphene
MOA of clomiphene
SERM
- competes w/ estradiol for estrogen receptors at the hypothalamus
- blocks estrogen negative feedback at the hypothalamus
AE of clomiphene
- hot flashes
- mild abdominal or pelvic discomfort
- vaginal dryness, mood swings
- less frequent: dizziness, fatigue, breast tenderness, HA
CI with Clomiphene
- uncontrolled thyroid or adrenal dysfunction
- primary ovarian failure or ovarian cysts
- abnormal uterine bleeding
- hepatic disease
- pregnancy
First line trt for polycystic ovary syndrome (PCOS)
Metformin 1500-2000mg/d
Risks of HRT
- endometrial CA
- CV disease
- venous thromboembolism
- breast CA
- ovarian CA
- gallbladder disease
Endometrial CA
Add progestin for intact uterus
Cardiovascular disease
Younger age, closer to MP
Venous thromboembolism
Lowest dose (transdermal)
Breast CA
Low dose, short duration (<5yrs)
Ovarian CA
Short duration use (<5yrs)
Gallbladder disease
Transdermal
Benefits of HRT
- vasomotor symptom relief
- vaginal symptom relief
- osteoporosis prevention
Estrogens approved for
Vasomotor or vaginal menopause symptoms
Estrogen AE
- nausea, HA, breast tenderness, uterine bleeding
- may need to taper off when discontinuing
ABSOLUTE CI for estrogen therapy
- thromboembolic disease
- pregnancy
- active liver disease
- CAD
- CVD or TIA
- undiagnosed vaginal bleeding
- active breast or endometrial CA
Relative CI for estrogen therapy
- HTN
- hypertriglyceridemia
- impaired liver function
- fluid retention
- hypothyroidism
- ovarian CA
- exacerbation of endometriosis
- exacerbation of asthma, DM, migraine, SLE, epilepsy
- history of breast CA
Oral estrogen products
Conjugated equine estrogens (Premarin)
Initial/low dose: 0.3-0.45mg
Usual dose: 0.3-1.25mg
Transdermal estrogen product
Vivelle, Vivelle Dot (apply twice weekly)
Initial/low dose: 0.025mg/d
Usual dose: 0.025-0.1mg/d
Vaginal estrogen product (intravaginally)
Femring (replace q3m)
Intravaginal estrogens
Premarin
Estring (replace q90d)
Vagifem (twice weekly)
Progesterone AE
Irritability Depression HA Mood swings Bloating Fluid retention Sleep disturbances
Progesterone products
Medroxyprogesterone acetate (Provera) Micronized progesterone (Prometrium)
Oral combination products
CEE + MPA (Prempro)
Continuous
Transdermal combination product
Estradiol + levonorgestrel (Climara Pro)
Continous
SERM
Ospemifene (Osphena) 60mg QD
SERM combination product
CEE + Bazedoxifene (Duavee) 45/20mg daily
Non-hormonal options for vasomotor symptoms
Venlafaxine
Paroxetine (approved)
Gabapentin
Clonidine
Male hypogonadism
- reduced libido
- depression or dysthymia
- decreased spontaneous erections
- gynecomastia
- loss of auxiliary and pubic hair
- small or shrinking testes
- infertility
- hight, BMD, muscle loss
- hot flashes
- fatigue, decreased motivation
- incomplete sexual development
TRT CI
- history of breast or prostate CA (unelevated prostate nodule or PSA >4ng/ml)
- hematocrit >50% (epoetin alfa)
- untreated severe obstructive sleep apnea
- severe lower urinary tract symptoms
- uncontrolled/poorly controlled CHF
Testosterone transdermal patch
Androderm
Testosterone gel
Androgel 1%
Testim 1%
5-10g as single dose in the morning and titrate up in 14 day intervals
Testosterone transdermal spray
Fortesta 4-7 sprays once daily and titrate dose up at 14-35 day intervals
Testosterone transdermal solution
Axiron
Benefits of TRT therapy
- decreased body fat and visceral fat
- improved libido and sexual function
- improved mood
- improvements in cognition and vitality
- improvement in CV risk factors
- improvements in T2DM and metabolic syndrome
- increased bone mineral density
- increased muscle mass and strength
Risks of TRT
- cancers (prostate and breast)
- erythrocytosis
- gynecomastia
- sleep apnea
- acne, oily skin
- male pattern baldness
- liver toxicity
- dyslipidemia
- increase in CV outcomes
