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Pharmacology > Men & Women's Health > Flashcards

Men & Women's Health Flashcards

1
Q

Alpha blockers

A

“alpha-adrenergic antagonists”

dynamic component of BPH is smooth muscle tone; alpha receptors stimulate constriction of prostate smooth muscles and may cause urinary obstruction; therefore antagonizing these receptors prevents constriction

Alpha blockers have quick onset of relief (within days)

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2
Q

Alpha blockers: alpha-1 selective antagonists

A

long-acting: terazosin & doxazosin

approved for HTN and BPH

take at bedtime to prevent orthostatic effects; also start with low doses and titrate up to relief of symptoms to avoid orthostasis

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3
Q

Alpha blockers: Uroselective agents

A

Afluzosin & Tamsulosin

ability to relieve BPH symptoms without decreased likelihood of hypotension

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4
Q

Alpha blockers: Uroselective agents: Tamsulosin

A

long-acting

selective antagonism at the alpha-1A receptor

decreases intra-urethral pressure without systemic BP reduction

Start at 0.4mg daily- usually no titration required (may still be some systemic effect, esp. with 0.8mg daily dosing)

SE: abnormal ejaculation (educate, but not a reason to DC)

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5
Q

Alpha blockers: Uroselective agents: afluzosin

A

Not selective for a specific alpha receptor subtype

extended release form displays clinical uroselectivity (selects prostate over vascular tissue)

even less systemic hypotension than tamsulosin

does not result in significant ejaculatory dysfunction, but it is more costly than tamsulosin

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6
Q

5alpha-Reductase Inhibitors

A

finasteride & dutaseride

reduce hypertrophy of the prostate gland itself by inhibiting the enzyme that converts testosterone to dihydrotestosterone (DHT) in prostate cells (DHT is a prostate growth regulator)

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7
Q

5alpha-Reductase Inhibitors: Finasteride

A

specific inhibitor of type 2 5alpha-reductase

reduces prostate size by 20-30%

***key predictor for positive treatment outcome is baseline prostate volume (need prostate volume of greater than 40mL to see benefit)

average of 6mo to see significant symptom reduction, so is often used in conjunction with alpha blockers initially

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8
Q

5alpha-Reductase Inhibitors: Dutaseride

A

inhibits both type 1 & 2 5alpha-Reductase

similar considerations as finasteride

need baseline prostate volume of 40-50mL to see positive outcomes and symptom relief

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9
Q

BPH Therapy

A

goal: improve symptoms, limit progression, prevent complications

mild BPH: watchful waiting (usually lack symptoms and may never experience disease progression)

Moderate/severe BPH: alpha blockers; uroselective agent if patient likely to have BP issues; 5alpha-Reductase inhibitor as add-on therapy if patient has prostate size greater than 40mL

Severe BPH and/or Secondary complications: surgical intervention

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10
Q

Phosphodiesterase-Inhibitors

A

sildenafil, vardenafil, tadalafil

inhibit PDE type 5, which inhibits degradation of cGMP, resulting in elevated levels of cGMP which results in relaxation of smooth cavernosal smooth muscle

still requires arousal to facilitate response

tadalafil has a longer half-life and don’t need to take directly prior to sex

sildenafil and vardenafil have absorption problems with high fat meals

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11
Q

Phosphodiesterase Inhibitors: Contraindications & Precautions

A

Avoid nitrate use (additive hypotensive effects; safe window not well established- 24-48hrs)

precaution for concurrent use with non-specific alpha blockers for BPH (hypotension due to systemic vasodilation)

acute ETOH use may cause additive dizziness

use lower doses in renal/hepatic dysfunction

CYP450 3A4 Inhibitors

best to avoid in: Recent MI/stroke, CHF class II and higher, uncontrolled arrhythmias, and hypotensive patients

ADRs: priapism (immediate ER), headache, flushing, dyspepsia, vision changes

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12
Q

Erectile Dysfunction Treatment

A

phosphodiesterase inhibitors are typically first-line

consider referral to urologist if first line does not work

under advice of urology expert, other meds such as apomorphine or intracavernosal injections may be used

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13
Q

Oral Contraceptives

A

most are combined estrogen & progestin (COC)

COC: less than 1 in 100 pg with perfect use
Progestin only: 2 of 100 pg with perfect use

missed doses can increased risk of pg

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14
Q

OC: Estrogen Component MOA/ADRs

A

prevents ovulation

alters endometrial lining and hinders implantation of egg

ADR: n/v, irritability, *clots, breast enlargement/tenderness, bloating/edema, cyclic HA

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15
Q

OC: Progestin Component MOA/ADRs

A

causes cervical mucous thickening (entry barrier)

reduces Fallopian tube mobility (decreases sperm transport)

alters endometrial lining and hinders implantation of egg

ADR: inc’d bleeding/spotting, diarrhea, fatigue, lactation, decreased libido, depressed mood (adding estrogen may decrease ADR)

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16
Q

“ACHES” mneumonic

A

for clots with estrogen pill use

A: abdominal pain (severe)
C: chest pain/cough/SOB
H: headache (severe), weakness, numbness
E: eye/vision problems
S: severe leg/calf pain
17
Q

Depo-Medroxyprogeseterone Acetate (Depo Provera)

A

IM q3mo

progestin only

approx 3 in 100 pg

18
Q

Ortho Evra patch

A

estrogen/progestin combo

change weekly x3wk, no patch on week 4

apply to buttocks, stomach, upper outer arm, or torso

studies showed no diff in absorption with heat, cold, or water (but be careful if patch falls off!)

19
Q

Nuva Ring

A

estrogen/progestin combo

insert vaginally once a month

leave in for 3 weeks, take out week 4

20
Q

DIAPPERS mneumonic

A

determining underlying cause of incontinence (will guide therapy)

D: delirium
I: infection
A: atrophic vaginitis/urethritis (due to decreased estrogen levels)
P: pharmaceuticals
P: psychological factors
E: excess urine output/polyuria
R: restricted mobility
S: stool impaction/constipation
21
Q

Stress incontinence

A

during episodes of elevated intra-abdominal pressure (cough, laugh, sneeze, lifting)

occurs most frequently in women, and may occur short term post partum

non-pharm tx often best choice

may use alpha-adrenergic agonists, estrogens, or TCAs

22
Q

Urge incontinence

A

characterized by loss of moderate to large amounts of urine with the inability to delay voiding if the bladder is perceived on being full

often associated with increased frequency

tx with anticholinergics, oxybutynin, tolterodine (Detrol), or TCAs

23
Q

Overflow incontinence

A

related to outflow obstruction

characterized by leaking small amounts of urine, poor stream, dribbling, and feeling of incomplete emptying (often associated with BPH)

24
Q

Functional incontinence

A

functionally fine, but cannot reach toilet (mobility/dementia)

25
Q

Mixed incontinence

A

two or more underlying pathologies

26
Q

Treatment of Urinary Incontinence

A

multiple non-pharm therapies (pelvic wall muscle strengthening exercises)

pharm tx includes: alpha-adrenergic agonists, estrogens, tricyclic antidepressants (TCAs), anticholinergics

27
Q

alpha-adrenergic agonists for urinary incontinence

A

promote contraction of smooth muscle and increase sphincter tone

not considered appropriate tx in most algorithms due to lack of evidence

pseudo-ephedrine sometimes used to manage mild stress incont (federally regulated OTC)

28
Q

estrogen use for urinary incontinence

A

for incont in post-menopausal women with urogenital atrophy

used for stress incontinence

topical or intra-vaginal preparations

29
Q

tricyclic antidepressant (TCA) use for urinary incontinence

A

inhibit NE uptake and may increase urethral tone due to an enhanced alpha-adrenergic effect

used for stress & urge incontinence

used for their anticholinergic effects

imipramine most widely used for this indication; also used for bed-wetting in children

30
Q

anticholinergics used for urinary incontinence

A

effective for control

questionable decrease of AchE inhibitors used to treat dementia (drugs may act against each other)

31
Q

oxybutynin

A

anticholinergic and smooth muscle relaxant properties

may be used as scheduled or as needed before an event

32
Q

tolterodine

A

competetive agonist of muscarinic receptors

CYP2D6 & 34A metabolism- check for drug interactions

33
Q

Treatment of Overflow incontinence

A

most often related to BPH

use BPH meds such as alpha adrenergic antagonists (alpha blockers) or 5alpha-reductase inhibitors

Pharmacology (11 decks)

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