Men's Health Drugs Flashcards
1
Q
what are the two forms of 5a-reductase?
where are they found and what do they do?
A
- Two forms of 5-AR have been identified:
Type I: predominantly in skin, liver and bone
Type II: predominantly in
* _urogenital_ tissue in men * _genital skin_ in men & women * convert testosterone to DHT (more potentform)
2
Q
what is role of aromatase?
where is it found?
A
= CYP-19
- converts testosterone into estrogen (estradiol)
3
Q
what are the androgenic and anabolic effects of testosterone
A
4
Q
androgen esters
- include what drugs?
- have what “benefits” over endogenous androgens?
A
testosterone cryptionate, testosterone enanthate
- have greater bioavailability than endogenous testosterone
- are injected IM, and thus bypass first pass metabolism
5
Q
alkylated androgens
- include what drugs?
- have what “benefits” over endogenous testosterone?
- AEs?
A
methyltestosterone, oxandrolone, fluxoymeterone
- have greater anabolic effects than endogenous testosterone (anabolic effects > androgenic effects)
- ofted used by athletes as performance enhancers
- AE:
- high risk for liver toxicity
- atherosclerosis (low HDL, high LDL)
-
prostatic hyperplasia - excess testosterone stimulation
- BPH (transitional zone)
- prostate cancer (peripheral zone)
6
Q
androgens - clinical uses
A
- replacement therapy in hypogonadal men
- as protein anabolic agents to
- reverse protein loss after trauma/surgery
- to slow loss of lean muscle d/t aging
- in growth stimulators in boys with delayed puberty
7
Q
androgen general AEs in
- men
- boys
- pregnant women
A
in all: acne
- men
- erythrocytosis (anabolic effec)
- gynecomastia - development of breast tissue d/t conversion of testosterone to estradiol in adipose
- testicular atrophy
- BPH –> urinary retention
- prostate cancer
- boys
- premature epiphyseal closure
- pregnancy
- masculization/undermasculization of external genitalia of fetus
8
Q
androgens contraindications
A
- pregnant women
- male pts with breast or prostate carcinoma
- young children
9
Q
what are the major classes of anti-androgens?
A
- steroid synthesis inhibitors
- 5a-reductase (5-AR) inhibitors
- androgen receptor (AR) antagonists
10
Q
ketoconazole
- what kind of drug?
- MOA?
- clinical uses?
- AEs?
A
- an antiandrogen
- MOA: inhibits steroid synthesis
- clinical uses
- cushing’s (hypercortisolism)
- prostate cancer
- fungal infection
- AE
- hepatotoxicity
11
Q
5a reductase inhibitors
- include what kind of drugs?
- what kind of drug
- MOA
- clinical uses
- AEs
A
- asteride: finasteride, dutasteride
- are anti-androgens
- MOA:
- finasteride: inhibits type II 5-AR (in reproductive tissues only)
- dustasteride: inhibits type I & type II 5-AR
- clinical uses
- BPH
- hirsutism (excessive hair growth)
- alopecia in males?
- AEs
- impotence
- hypotension
12
Q
androgen receptor agonists
- include what drugs?
- are what kind of drug?
- MOA
- clinical uses
- AEs
A
- amide: flutamide, bicalutamide, nilutamide, enzalutamide
- antiandrogens
- MOA: competititive antagonist at androgen receptor
- clinical uses:
- prostate cancer
- management of excess androgen effects in women
- AEs:
- hepatic injury
- hot flash
- diarrhea
13
Q
phosphodiesterase inhibitors
- include which drugs
- MOA
- clinical uses
- PK
- AE/CI
- drug drug interactions
A
- afil: sildenafil, tadalafil, vardafil
- MOA:
- sustain vasodilation
- inhibit phosphodiesterases that degrade cGMP (which induced PKG, which induces smooth muscle relaxation)
- sustain vasodilation
- clinical uses:
- ED
- BPH
- PAH
- PK
- metabolized by CYP-3A4
- tadalafil half life = 17.5 hrs
- AE:
- flushing / diarrhea / hypotension / heachache / vision & hearing loss
- CI:
- CYP-3A4 inhibitors: ketoconazole
- CYP-3A4 inducers: rifampin
- organic nitrates (nitroglycerin)
14
Q
what are the clinical uses of each PDE-5 inhibitor?
A
- ED: all
- BPH: tadalafil
- PAH: sildenafil, tadaafil
15
Q
PDE-5 inhibitors are C/I when pt on what other drugs?
A
- nitroglycerin
- ketoconazole (CYP-3A4 inhibitor)
- rifampin (CYP-2A4 inducer)
