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What are the natural androgens?
Testosteron DHT, Estrogen, etc.
In males and females, what is responsible for androgen release?
Males- Leydig→ LH→ testosterone
Females- Corpus Luteum
Why is DHT more potent?
Has a hydrogen on carbon 5.
Testosterone is regulated by…
Negative feedback.
What are the androgenic SE of testosterone?
Promotes male sexual characteristics- penile and sacral growth, Prostate and seminal vesticle growth, hair, layrnx. (Traits that make you a man)
Receptor properties of androgen receptors?
Nucleur Receptors
Steroid
PPAR
Thyroid
Modulates gene transcription
5 alpha reductase subytpes:
TYPE 1: Skin, bone, liver
Type 2: Genital skin, urogenital tissues
How is testosterone Converted into estradiol?
Aromatase
Which anabolic property in men is mediated by estradoiol?
Skeletal muscle growth
How is testosterone ester produced?
Esterifying a fatty acid to the 17 hydroxyl group.
How is testosterone released from these esters?
Testosterone is released from the esters through hydrolysis in vivo
What is the boxed warning of testosterone undecanoate?
Pulmonary oil microembolism
Why are testosterone esters not used as much?
Painful and variable concentration.
What is the problem with transdermal patches?
Skin irritations
Problems with gel and topical solution (1%) ?
Secondary exposure to children
Where should gels and topical solutions be applied?
Gels- shoulders, arms
Topical- Underarm
What can you do to reduce accidental contact of drug in normal individuals?
Nasal gel OR topical gel on thighs
What are some side effects of testosterone undecantoe?
Cough, dyspnea, analyphylaxis
What are the 5- alpha reductase inhibitors? MOA? A/E?
FInasteride, Dutasteride
MOA:Decreased prostate DHT, Increases urinary flow
A/E: Decreased libido
ADR’s of non specific alpha blockers?
Dizziness, hypertension, fatigue
MOA of PDE5 inhibitors? ADRS? CI?
MOA: Inhibit the breakdown of cGMP
ADR’S: HA, flushing, and vission
Nitrates
Major concerns with PDEI?
Priapism, vision loss, hearing loss, hypotension (relaxed)