pharm exam 3- mens health

what are the different reasons for testosterone being prescribed

primary application is management of androgen deficiency in males
(Testosterone is the principal endogenous androgen in both females and males)

Male hypogonadism –(main indication)**
[w/o androgens, puberty cannot happen ]

replacement therapy

- Delayed puberty – best to wait
-Replacement therapy in menopausal women – can alleviate symptoms

-Wasting in patients with AIDS – testos ↓ so risk for skeletal wasting ↑

-Anemias
(stimulates synthesis of erythropoietin; may also ↑ WBC & plts)

adverse effects of testosterone

-->Virilization-
(male enhancing) in women, girls & boys (we want virilization in males not females)

[in women can cause → acne, deep voice*, facial & body hair (hirsutism), male-pattern baldness*, increased libido, clitoral enlargement* & menstrual irregularities]

-->Premature epiphyseal closure
[ need xray of hand & wrist q 6 mos to evaluate androgen effects on children]

-->Hepatotoxicity
[(cholestatic hepatitis, hepatocellular carcinoma); need LFTs periodically]

-->Effects on cholesterol levels
(↓ HDL, ↑ LDL)

--> Prostate cancer
(don’t cause but does promote growth of prostate CA cells)

-->Edema
(androgen-induced retention of salt & water)

-->Gynecomastia
[in males receiving androgen replacement therapy (from conversion of certain androgens into estrogen)]

testosterone pregnancy risk category

Category X

testosterone abuse potential

SCHEDULE III CONTROLLED SUBSTANCE
(athletic performance)

significant risk-

Hypertension

suppression of release of LH and FSH = testicular shrinkage, sterility, gynecomastia, acne, reduction in HDL and increase in LDL

Renal damage

Psychological effects-
-->on mentally healthy: minimal impact
-->on psychologically fragile: could intensify aggression

how does PDE-5 inhibitors help erectile dysfunction

PDE-5 inhibitors block the breakdown of cGMP to GMP (PDE-5 would normally do this) which allows the blood to continue to flow into sinusoidal spaces (penis veins) → allowing the penis to remain erect

-->They only enhance normal erectile response in the presence of a stimulus (sexual arousal)
(Need to be taken 1 hour before sexual activity)

adverse effects of PDE-5 inhibitors

-Hypotension

-Priapism= painful erection > 6 hrs

(for ALL PDE5 Is → by 4 hrs need to go to ED
can damage penile tissue causing permanent loss of potency
need to have blood aspirated from corpus cavernosum and irrigation with a vasoconstrictor)

-Headache, dyspepsia, flushing, nasal congestion, diarrhea, rash, dizziness, mild transient visual disturbances, intensification of obstructive sleep apnea

-->Rare side effects

-Nonarteritic ischemic optic neuropathy (NAION) – irreversible blurring or loss of vision from blockage of blood to optic nerve

-Sudden hearing loss → usually in 1 ear, w/ dizziness, vertigo, & tinnitus (complete w/ 2/3 that have the issue)

what drug classes are contraindicated with the PDE-5 inhibitors.

-Nitrates

(Could cause life-threatening hypotension
ABSOLUTELY CONTRAINDICATED FOR MEN TAKING NITRATES
24 hours in between these medications for safety
& longer if using a CYP3A4 inhibitor or hepatic or renal pathology)

-Alpha blockers--> (dilate arterioles)

(Can cause symptomatic postural hypotension)

-Inhibitors of cytochrome P450 (CYP3A4)
--> Azole drugs, erythromycin, cimetidine, saquinavir, ritonavir, grapefruit juice

(Can suppress metabolism of sildenafil)

what are the two classes of drugs used for the managment of benign prostatic hyperplasia (BPH)

1. 5-Alpha-reductase inhibitors

2. Alpha1 antagonists

management of benign prostatic hyperplasia (BPH): what is the indication for 5-Alpha-reductase inhibitors

for very large obstruction (mechanical obstruction)

management of benign prostatic hyperplasia (BPH): what is the indication for Alpha1 antagonists

for smaller prostates (dynamic obstruction)

management of benign prostatic hyperplasia (BPH): common drug names for 5-Alpha-reductase inhibitors

Finasteride & Dutasteride

management of benign prostatic hyperplasia (BPH): 5-Alpha-reductase inhibitors MOA

-Delayed to growth of prostate and causes the shrinkage of enlarged prostatic tissue by blocking a hormone

(Extremely long half-life (5 weeks) – takes months to clear after stopping)

management of benign prostatic hyperplasia (BPH): 5-Alpha-reductase inhibitors ADVERSE EFFECTS

Lack of sexual desire

Reduced ability to ejaculate and failure to sustain ejaculation

Problems with ejaculation

what is finasteride (proscar) sold at lower doses to treat

propecia (treats male pattern baldness)

management of benign prostatic hyperplasia (BPH): Alpha1 antagonists common drugs

Alfuzosin, Doxazosin (& sustained release), Terazosin, Tamulosin (Flomax), Silodosin (Rapaflo) (best tolerated)

management of benign prostatic hyperplasia (BPH): Alpha1 antagonists MOA

Blockade of alpha1 receptors RELAXES smooth muscle in the bladder neck (trigone and sphincter), prostate capsule, prostatic urethra - reduces dynamic obstrux of urethra (opening is larger)

**they DO NOT reduce prostate size (as the 5-alpha-reductase inhibitors do)**

management of benign prostatic hyperplasia (BPH): Alpha1 antagonists SELECTIVE BLOCKERS adverse effects

Less likely to cause effect of non-selectives

can cause abnormal ejaculation

management of benign prostatic hyperplasia (BPH): Alpha1 antagonists NON SELECTIVE BLOCKERS adverse effects

Hypotension, fainting, dizziness, somnolence, and nasal congestion

↑ risk for floppy-iris syndrome w/ cataract surg
(tell ophthalmologist & postpone α-blocker therapy until after)

Vertigo
Headache
Stomach upset
Decreased amount of semen when ejaculation occurs