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Colin CPR II > PHARM - BP and ED Pharmacology > Flashcards

PHARM - BP and ED Pharmacology Flashcards

1
Q

What is BPH?

A

Benign Prostatic Hyperplasia

Prostate cells proliferate (non-cancerous)

Causes bladder outlet obstruction, as well as urethra constriction

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2
Q

What are the symptoms of BPH?

A
  • Interrupted stream
  • Urinary Frequency
  • Urinary Hesitation
  • Bladder Fullness
  • Dribbling
  • Urinary Urgency
  • Weak Stream
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3
Q

What type of drugs can be used to treat BPH?

A

Alpha 1 Antagonists and Steroid 5-alpha Reductase Inhibitors

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4
Q

Which Alpha 1 Antagonists are used to treat BPH?

A

STAT-D

  • Silodosin
  • Tamsulosin
  • Alfuzosin
  • Terazosin
  • Doxazosin

All alpha-1 Antagonists end in -osin

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5
Q

What effects of Alpha 1 Antagonists specificalyl helps with BPH?

A

Alpha 1 Antagonists:

  • Reduce spasm
  • Relax prostatic smooth muscle
  • Relax urinary sphincter smooth muscle
  • Improve urinary flow
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6
Q

What receptors do drugs used to treat BPH target?

A

Alpha-1 Antagonists in this case of treating BPH are targeting Alpha-1A and Alpha-1D receptors

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7
Q

Where will you find Alpha-1A and Alpha-1D receptors?

A

Alpha-1A receptors are found in the prostate and the bladder outlet

Alpha-1D receptors are found in the Detrusor muscles of the bladder

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8
Q

What is the best mono therapy for prompt relief of BPH symptoms (days)?

A

Alpha-1 Antagonists

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9
Q

Which Steroid 5-alpha Reductase Inhibitors are used to treat BPH?

A
  • Finasteride

- Dutasteride

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10
Q

Why does the prostate enlarge in BPH?

A
  • Aging

- Dihydrotestosterone, Testosterone (DHT is 10x more potent than T)

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11
Q

What is SAR?

A

SAR is just Steroid 5-alpha Reductase

There is a Type 1 SAR (SAR-1) and a Type 2 SAR (SAR-2)

SAR-1 and SAR-2 are responsible for the conversion of serum Testosterone (T) into Dihydrotestosterone (DHT) in cells

A prostate that has undergone hyperplasia (as in BPH) has excess SAR-2

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12
Q

What are the direct effects of SAR-Inhibitors?

A

Testosterone accumulation

DIhydrtestosterone depletion

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13
Q

What are the indirect effects of SAR-inibitors?

A

Androgen receptor less occupied

No gene transcription

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14
Q

What is ED?

A

Erectile Dysfunction

Consistent or recurrent inability to acquire or sustain an erection of sufficient rigidity and duration for sexual intercourse

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15
Q

What are some risk factors for developing ED?

A

Obesity

Stress

Smoking

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16
Q

How does an erection generally occur?

A

Blood flows into the corpora cavernosa and corpus spongiosum (glans penis)

Nitric Oxide facilitates smooth muscle relaxation

  • Maximize blood flow
  • Penile engorgement

Relaxed smooth muscle leads to blood in sinusoids and a rigid organ

17
Q

What is the secondary messenger cascade responsible for maintaining an erection?

A
  • Nitric Oxide Synthase converts L-Arginine to NO
  • NO signals the production of cGMP
  • cGMP normally leads to a decrease in intracellular Ca2+
  • Decreased intracellular Ca2+ leads to smooth muscle relaxation
  • Smooth muscle relaxation causes an erection
18
Q

How does a penis return from erect to flaccid?

A

cGMP is required to maintain an erection

  • cGMP causes a decrease in intracellular Ca2+
  • Decreased intracellular Ca2+ causes smooth muscle relaxation and an erection

PDE-5 converts cGMP to 5’-GMP, stopping downstream signaling for erection maintenance

19
Q

What class of drugs are used to treat ED?

A

Phosphodiesterase-5 (PDE-5) Inhibitors

PGE1 Agonists

20
Q

How do PDE-5 Inhibitors work?

A

PDE-5 converts cGMP to 5’GMP

cGMP is required to maintain an erection

PDE-5 Inhibitors competitively inhibit PDE-5 thus preventing its 5’-GMP production and maintaining high levels of cGMP

21
Q

What are the names of PDE-5 Inhibitor drugs?

A
  • Sildenafil (viagra)
  • Vardenafil (Levitra)
  • Tadalafil (Cialis)
  • Avanafil (Stendra)
22
Q

How do PGE1 Agonists work?

A

PGE1 Agonist (Alprostadil) activates the PGE1 receptor

Activated PGE1 activates Adenylate Cyclase

Adenylate Cyclase increases intracellular cAMP production

cAMP promotes a decrease in intracellular Ca2+

Decreased intracellular Ca2+ induces smooth muscle relaxation, allowing erection to be maintained

Colin CPR II (12 decks)

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