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Drug Action II > Block 5: GU and ED Pharm > Flashcards

Block 5: GU and ED Pharm Flashcards

1
Q

How is the penile stimulated?

A

Stimulation of penile shaft by the nervous system leads to the secretion of nitric oxide (NO), causing the creation of cyclic guanosine monophosphate (cGMP)

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2
Q

How is cGMP broken down?

A

phosphodiesterase type 5 (PDE5)

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3
Q

Describe the mechanism of an erection?

A

Flaccid: Smooth muscles contracted > vasoconstriction > low blood flow
Erect: Smooth muscles relaxed > vasodilation > high flow

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4
Q

Describe the nerve supply of the penis?

A

Paraympathetic nerves from S2-4 nerve roots primarily control erectile function
Sympathetic nerves from T11-L2 control detumescence and also contribute to ejaculation and emission.

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5
Q

What is the difference between erection and detumescence?

A

Erection: Stimulation of the Parasympathetic fibers through tactile sensory stimuli to the penis, releases acetylcholine, Cholinergic stimulation increases Nitric Oxide and the generation of cGMP
DETUMESCENCE: Sympathetic (adrenergic) fibers which release norepinephrine, help to maintain the penis in its flaccid state

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6
Q

What is ED?

A

The consistent or recurrent inability to obtain and/or maintain an erection sufficient for satisfactory sexual activity

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7
Q

What are RF of ED?

A
  1. CVD
  2. Endocrine Disorders
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8
Q

In the majority of impotent men, erectile impairment has both a ___ and ___ basis?

A

psychological (emotional stress and psychiatric dx) and organic (physical dx)

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9
Q

What are the tx options for ED?

A
  1. PO – PDE5 inhibitors
  2. Cavernosal injections – Prostaglandin E1
  3. Urethral application: Prostaglandin E1 – PGE1
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10
Q

What are the PDE5is? MOA?

A

Indicated for men who produce insufficient amounts of NO
Sildenafil, Tadalafil, Vardenafil, Avanafil: selectively inhibiting the PDE5 preventing the hydrolysis of cGMP to inactive GMP causing accumulation and prolonging vasodilatory effect

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11
Q

Counseling point for PDE5i?

A

All require sexual stimulation for activation and generally must be taken at least ½ hour to one hour before anticipated sexual activity

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12
Q

What is the 1st line therapy for ED?

A

PDE5 inhibitors

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13
Q

CI for PDE5i?

A

Patients on nitrates

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14
Q

Sildenafil

Brand, Onset, ADR

A

Viagra
Onset: 30 minutes to ~4-5 hrs
ADR: HA, flushing, dyspepsia, DZ, rhinitis, abnormal vision

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15
Q

Tadalafil

Brand, Onset, ADR

A

Cialis
Onset: Two hours before sexual intercourse, longest half-life
ADR: Headache, flushing, rhinitis and back pain and myalgia

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16
Q

Vardenafil

Brand, Onset, ADR

A

Levitra
Onset: ~30 minutes to 5 hours
ADR: HA, flushing, rhinitis

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17
Q

Avanafil

Brand, ADR

A

Stendra
ADR: headache, flushing, and rhinitis (fewer ADRs than others)

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18
Q

PDE5is?

A
  1. Sildenafil (VIAGRA)
  2. Tadalafil (Cialis)
  3. Vardenafil (Levitra)
  4. Avanafil (Stendra)
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19
Q

Serious ADR with all PDE5is?

A
  1. Erection that will not go away (priapism)
  2. Sudden vision loss in 1 or both eyes
  3. Sudden hearing decrease or hearing loss
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20
Q

Intracavernosal Injection Therapy (ICI) products?

A
  1. Caverject: alprostadil
  2. Trimix: alprostadil, phentolamine, papaverin
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21
Q

Alprostadil

Brand, MOA, Forms, ADR

A

MUSE (IU), Caverject (IC), Befar (Topical)
MOA: Vasoactive prostaglandin E1 that stimulates adenyl cyclase, which raises cAMP that leads to lower Ca++ and relaxation of vascular smooth muscle
ADR: Penile pain, priapism, fibrosis

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22
Q

What are the components of a Trimix?

A

Papaverine: Inhibits PDE -> ↑ cAMP and cGMP -> vasodialation
Phentolamin: Mixed a-1 and a-2 competitive antagonist
Alprostadil: Vasoactive prostaglandin E1 (PGE-1)

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23
Q

Testosterone Replacement Therapy

Indication, ADR, Monitoring

A

Indication: Hypogonadism, ED, and testosterone def
ADR: Suppresses LH/FSH -> Infertility, gynecomastia
Monitoring: Hematocrit, LFT

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24
Q

Herbal supplements for ED?

A
  1. Epimedium
  2. Ginkgo
  3. L-arginine
  4. Red ginseng
  5. Yohimbine
25
Q

Flibanserin

Brand, Indication, MOA, ADR

A

Addyi
Indication: pre-menopausal women with hypoactive sexual desire disorder (HSDD)
MOA: Serotonin 1A agonist and a serotonin 2A antagonist reducing sexual interest and desire
ADR Hypotension and syncope

26
Q

What is produced by the prostate?

A

Prostate specific antigen (PSA)

27
Q

What is a prostate?

A

Fland that forms part of the male reproductive system between the bladder and urethra

28
Q

What is the function of the prostate?

A

Secrete an alkaline fluid of 70% seminal volume:

  1. Lubrication and nutrition for the sperm.
  2. Liquefaction of the seminal plug.
  3. Neutralize the acidic vaginal environment
29
Q

What is BPH?

A

Benign prostatic hyperplasia: enlarged prostate

  1. Static compression of the urethra (Increased glandular volume)
  2. Dynamic compression of the urethra (Smooth muscle component of the prostate)
  3. Difficulty in urination
  4. Autonomic tone in the prostate and bladder neck controlled by alpha-1 adrenergic receptors
  5. Dihydrotestosterone (DHT) is metaboized by type II 5-alpha-reductase promoting growth
30
Q

Sx of BPH?

A
  1. Storage sx
  2. Voiding sx
31
Q

First line therapy for BPH?

A
  1. Alpha 1 blockers: relaxes the prostate smooth muscle and reduces urethral resistance to flow
  2. 5-alpha reductase inhibitors – Inhibits formation of DHT to help “shrink” the prostate gland
32
Q

MOA of Alpha-1-blockers?

A

Sympathetic tone: Constricts the sphincter muscle via action at the a1 receptors. Prostate is rich in a1 receptors

To improve urination of BPH:
Reduce effects of noradrenergic tone in the prostate and sphincters by blocking a1 receptors

33
Q

Types of Long-acting Selective a1-blockers?

A
  1. Prazosin (minipress)
  2. TERAZOSIN (Hytrin)
  3. DOXAZOSIN (Cardura)
34
Q

Prazosin

Brand, MOA, Indication, ADR

A

Minipress
MOA: Selective α1 receptor blocker
Indication: Not approved for BPH (only for hypertension)
ADR: orthostatic hypotension from first dose phenomenon

35
Q

Doxazosin

Brand, Indication

A

Cardura
Indication: BPH, HTN

36
Q

Terazosin

Brand, Indication

A

Hytrin
Indication: BPH, HTN

37
Q

Types of Long-acting Selective a1A-blockers? Benefits?

A
  1. Silodosin (Rapaflo)
  2. Tamsulosin (Flomax)
  3. Alfuzosin (Xatral): Lacks a1-A receptor selectivity, but has “uroselectivity” to the prostate

Selective inhibition of the a1-A receptors in prostate reducing effect on BP on vasculature from less a1-B antagonism

38
Q

Tamsulosin

Brand, MOA, Indication

A

Flomax
MOA: Selective inhibition of the a1-A receptors in prostate
Indication: BPH

39
Q

Silodosin

Brand, MOA, Indication

A

Rapaflo
MOA: Highly selective inhibition of the a1-A receptors (uroselective) in prostate over a1-B
Indication: BPH

40
Q

Alfuzosin

Brand, MOA, Indication

A

Uroxatral
MOA: Does not have receptor selectivity at a1-A but has ‘uroselctivity’ and a lower incidence of ejaculatory dysfunction
Indication: BPH

41
Q

Alpha antagonist ADRs?

A
  1. Orthostatic hypotension
  2. Dizziness
  3. Stuffy nose
  4. Impaired ejaculation and sexual dysfunction
42
Q

Types of 5-alpha reductase inhibitors? MOA? ADR?

A
  1. Finasteride (Proscar)
  2. Dutasteride (Avodart)

MOA: Shrink the prostate
* Enzyme inhibitors reduce the amount of testosterone turned into DHT, a hormone required for prostate gland growth
* Onset is longer than alpha blockers and may take 3 months to see imporvement

ADR: Impotence, ED, decreased libido

43
Q

Benefits of using combo BPH therapy?

A

5a-Reductase Inhibitors: Arrest Disease Progression
a1-blockers: relieve sx rapidly

44
Q

What are the functions of a normal bladder?

A

Filling: Efficient and low pressure
Storage: Low pressure, with perfect continence
Emptying: Periodic complete urine expulsion, at low pressure, when convenient

45
Q

What is voiding?

A

Coordination of the ANS and somatic NS controlled by the pontine micturition center in the brainstem

46
Q

Describe the NS controls of voiding?

A

Parasympathetic receptors – Muscarinic - Pelvic Nerve: Bladder or detrusor (contraction)
Sympathetic receptors - Adrenergic - Hypogastric nerve:
* a1 – adrenergic (Contacts)
* b2 – adrenergic (relaxes)

47
Q

Describe the storage reflex of the bladder?

A
  1. Withdrawal of Parasympathetic (ACh) tone allows Sympathetic (NE) tone to dominate.
  2. **Sympathetic tone relaxes **the bladder (detrusor) smooth muscle via b2/b3 receptors.
  3. Sympathetic tone constricts the sphincter muscle via the a1 receptors
48
Q

Describe the micturition process?

A
  1. Withdrawal of Sympathetic (NE) tone and activation of Parasympathetic (ACh) tone
  2. Parasympathetic (ACh) tone causes constriction of the bladder (detrusor) smooth muscle via muscarinic receptor activation
  3. Sphincter muscle relaxes due to withdraw of sympathetic tone and increased parasympathetic tone
  4. Voluntary lower body muscle contraction assists with contracting the bladder
49
Q

What are the incontinence types?

A

Urge: Leakage accompanied by or immediately preceded by urinary urgency
Stress: Loss of urine with exertion, sneezing, or coughing
Mixed: Loss of urine associated with urgency and also with exertion, effort, sneezing, or coughing
OAB: A symptom complex of urgency, with or without urge incontinence,but usually with frequency and nocturia

50
Q

What is the differnence between OAB and SUI?

A

OAB: Bladder muscle experiences frequent involuntary contractions
SUI: Bladder muscle experiences a stress related contraction and support muscles are unable to remain shut

51
Q

OAB tx option?

A
  1. Behavioral therapy
  2. Medication (Anti-cholinergics, β3 Agonists)
  3. Combined therapy
  4. Minimally invasive therapy
  5. Surgery

Kegel exercises

52
Q

What is purpose for pharm tx of OAB?

A
  1. Inhibition of involuntary bladder contractions and spasticity (Muscarinic antagonists)
  2. Increased bladder capacity (Muscarinic antagonists and β3 receptor agonists)
53
Q

What are the effectiveness and ADRs of anticholinergics for OAB?

A

Efficacy:
* Less frequnecy
* Less urge UI
* Increased voided volume

ADR:
* Dry mouth
* Dyspepsia
* Constipation
* CNS effects

54
Q

What are the urogenital antispasmodics?

Brand, MOA

A

Flavoxate HCl (Urispas): Relaxes spasms, increases capacity of bladder
Oxybutynin HCl (Ditropan, Oxytrol, Gelnique): Decreases hyperreflexively of bladder and urge to void
Tolterodine (Detrol IR & LA): Used for urinary incontinence, frequency and
urinary urgency, & bed wetting and causes detrusor muscle relaxation
Darifenacin (Enablex): M3 selectivity
Solifenacin (Vesicare): M3 selectivity
Trospium (Sanctura IR, XL): Quaternary amine

55
Q

Fesoterodine

Brand, MOA, Indication

A

Toviaz
MOA: Rapidly hydrolyzed by esterases to the active metabolite (5-hydroxymethyl tolterodine)
Indication: Over-active bladder

56
Q

How do you improve urinary retention?

A
  1. Block parasympathetic cholinergic tone with antimuscarinic antagonists
  2. Allows noradrenergic sympathetic tone to dominate
    * Detrusor muscle relaxation
    * Sphincter contraction
57
Q

ADR of Antimuscarinics for OAB?

A
  1. Dry mouth
  2. Constipation
  3. Blurred vision
  4. DX
  5. Cognitive impairment (Flavoxate, Oxybutynin, Solifenacin)

ER may cause fewer ADRs

58
Q

Beta-3 Adrenergic Receptor Agonists

Brand, Indications, ADR

A

Mirabegron (Myrbetriq), Vibegron (Gemtesa)
Indication: OAB
ADR: Hypertension, tachycardia

59
Q

Mirabegron

MOA, CI

A
  1. Sympathetic tone relaxes the bladder (detrusor) smooth muscle via b2/b3 receptors
    MOA: Selective b3 receptor agonist that increases Sympathetic tone to the detrusor muscle, allowing relaxation of the detrusor muscle and increased bladder capacity
    CI: Severe uncontrolled hypertension, Moderate inhibitor of CYP2D6

Drug Action II (28 decks)

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