Term
| Testosterone is produced by... |
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Definition
| Testes Leydig cells under the influence of LH |
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Term
| In the cytoplasm of the target cell, testosterone... |
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Definition
| Is converted to DHT by 5a-reductase |
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Term
| Androgens: androgenic physiological effects |
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Definition
Male repro tract, puberty, secondary sex characteristics
Male accessory sex glands
Growth of long bones, epiphyseal closure (actually caused by testosterone being converted to estradiol by aromatase)
Behavioral changes
Baldness |
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Term
| Androgens: catabolic physiological effects |
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Definition
Inc. protein deposition in tissues
Inc. erythropoiesis
BPH via DHT |
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Term
| Androgens: used as tx in these conditions |
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Definition
Induce puberty
Replacement tx for male hypogonadism
Reverse neg. nitrogen balance from catabolic states (trauma, surgery)
Stim. erythropoiesis in severe anemia
Stim. female libido, gynecological disorders |
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Term
| Androgens: S/E not CV, renal, liver, immune |
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Definition
Small balls, no sperm
BPH
Bald
Muscle tightness, tendon rupture
Short
Acne (and hirsutism, amenorrhea, clit enlargement, deepened voice in women)
Gynecomastia in men
Virilized kids |
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Term
| Androgens: S/E CV, renal, liver, immune |
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Definition
CV: dose-dep't inc. LDL and dec. HDL, cardiomegaly, HTN, MI, stroke
Renal: retention of salt, water
Liver: reversible inc. in LFTs
Immune: inhibited |
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Term
| Bicalutamide, flutamide: class, indication, MOA |
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Definition
Anti-androgenic/androgenR antagonist
Prostatic carcinoma
Competitively block androgenR in the cancer
This happens in the HT, though, and so LH/testosterone can't feedback inhibit and so their levels inc.
Give along w/ GnRH analog |
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Term
| Bicalutamide is preferred over flutamide b/c... |
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Definition
| Bicalutamide is less hepatotoxic and can be taken p.o. qd |
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Term
Spironolactone also has a partial agonist effect at...
It's used for... |
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Definition
Androgen/estrogen/progesterone R
Inhibits CYP17 that synth. testosterone
Hirsutism in post-menopausal ladies |
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Term
| Leuprolide, goserelin: class, admin, MOA |
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Definition
Anti-androgenic/GnRHR agonist
IM depot
Initially stim FSH/LH release
But continuous release causes pit GnRHR to downregulate
Dec. LH secretion
Plasma testosterone 10% of nl w/in 2 wks |
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Term
| Leuprolide, goserelin: indications, S/E |
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Definition
Prostatic carcinoma (given w/ bicalutamide to prevent tumor flare up/bone symptoms from the initial testosterone inc.)
Endometriosis, uterine fibroid tumors
Central precocious puberty
Hot flashes, sweating
Edema
Gynecomastia
Dec. libido |
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Term
| Doxazosin, tamsulosin: indications, MOA |
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Definition
BPH
Block a1a adrenoreceptors
Smooth muscle relaxes, dec. resistance to urinary flow
Less hesitancy (more rapid initiation), greater peak flow rate, more complete emptying |
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Term
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Definition
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Term
| Tamsulosin is special b/c... |
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Definition
It's more selective for a1a adrenoreceptors
Less dizziness and orthostatic hypotension
Inc. ejac. dysfxn (b/c of a1a selectivity) |
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Term
| Doxazosin, tamsulosin: S/E |
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Definition
Dizziness, orthostatic hypotension (remember that a1R help prevent syncope)
Nasal congestion (unopposed cholinergic VD)
Impotence
Fatigue, somnolence
Peripheral edema |
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Term
| Dutasteride, finasteride: MOA |
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Definition
Dut. inhibits both isozymes of 5a-reductase, fin. inhibits type 2 found in prostate
Testosterone not made into DHT
Fin: plasma, prostate DHT falls by 70%, plasma testosterone rises by 10%
Plasma LH doesn't change! |
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Term
| Dutasteride, finasteride: BPH effects |
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Definition
Dec. prostate size by 3 mo, continues 1-2 yrs
Avg. shrinkage is 25% (greater response the bigger the prostate), associated w/ dec. BPH symptoms
Smaller size maintained as long as on meds
Dec. need for TURP or TUNA! |
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Term
| Dutasteride, finasteride: S/E |
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Definition
Prevents hair loss
Impotence, dec. libido
Dut., fin. 5mg suppresses PSA by 50%
Fin. 1mg doesn't suppress PSA
New baseline PSA has to be est. 1 yr after initiation of tx |
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Term
| DDAVP: indications, admin, issues w/ admin |
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Definition
Nocturnal enuresis
Nasal spray, duration of action 6-20 hrs
Allergic rhinitis, nasal congestion slow URI absorption |
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Term
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Definition
Binds V2R in CD principal cells
Reabsorb water, dec. urinary volume |
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Term
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Definition
Atherosclerosis
DM
Prostatectomy
SSRIs
Smoking
Spinal cord injury |
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Term
| IIEF scores: what's good, what's bad |
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Definition
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Term
| Alprostadil: indications, admin, MOA |
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Definition
ED if unresponsive to sildenafil
Topical--urethral suppository, penile head gel/cream (injections no longer done)
PGE1R agonist
Suppository: onset w/in 5-10 min, done 30-60 min
Gel, cream: onset w/in 30-40 min |
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Term
| Sildenafil, tadalafil, vardenafil: indications, MOA |
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Definition
PDEase5 inhibitors
cGMP kinase not on
MLC phosphatase not on
Relaxation of vascular smooth muscle
Sildenafil: onset w/in 30-60 min, done w/in 4-5 hrs
Tadalafil: onset w/in 30-45 min, done w/in 24 hrs
Vardenafil: onset w/in 60 min, done w/in 4-5 hrs |
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Term
| Sildenafil, tadalafil, vardenafil: S/E |
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Definition
Headache, flushing
Impaired blue-green color discrim. from partial blockade of PDEase6 in retinal cones
non-arteritic ischemic optic neuropathy from dec. blood flow to optic nerve, rare and can result in permanent loss of vision |
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Term
| Sildenafil, tadalafil, vardenafil: drug-drug interactions |
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Definition
Nitrates: severe hypotension, chest pain, MI, ischemic stroke
a-blockers doxazosin for BPH: hypotension (fine w/ tamsulosin, though, b/c it doesn't really lower BP) |
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