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Urology > Urology Pharmacology > Flashcards

Urology Pharmacology Flashcards

1
Q

Drugs used to treat BPH?

4

A
  1. Alpha-1 blockers
  2. 5 alpha-reductase inhibitors
  3. Combo
    Dutasteride-Tamulosin (Jalyn)
  4. Tadalafil (Cialis)
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2
Q

What are the alpha one blockers?
5

What is the Combo 5-alpha reductase inhibitor-alpha-1 blocker?

A
  1. Terazosin (Hytrin)
  2. Doxazosin (Cardura)
  3. Alfuzosin (Uroxatrol)
  4. Tamsulosin (Flomax)
  5. Silodosin (Rapaflo)

Dutasteride-Tamulosin (Jalyn)

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3
Q

Alpha-1 Blockers
1. More effective than 5-alpha-reductase inhibitors for what?

  1. MOA?
  2. Alpha-1 receptors are located where?

All drugs in this class have similar efficacy

A
  1. short and long term symptom management
  2. relax smooth muscle in the bladder neck and the prostatic capsule and prostatic urethra
  3. in the base of the bladder and in the prostate
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4
Q

Alpha-1 Blockers Efficacy
1. Symptom scores decreased by _____%?

  1. Urine flow rates increased by _____%?
  2. Which are more effective than the 5-alpha-reductase inhibitor Finasteride (Proscar)? 2
  3. Efficacy of Tamsulosin (Flomax) and Finasteride (Proscar) compare how?
A
  1. 30-40
  2. 16-25
  3. Doxazosin (Cardura) and Terazosin (Hytrin)
  4. were equal
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5
Q

Alpha-1 Blockers
SE
1. Most common? 2
2. Generally start dosing how?

A
  1. Most common are
    - dizziness and
    - orthostatic hypotension

2/ Generally start at a small dose at bedtime and titrate up slowly over several weeks

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6
Q
  1. Which alpha-1 blockers cause more BP lowering than others? 2
  2. When can it cause severe hypotension?
A
    • Terazosin (Hytrin) and
    • Doxazosin (Cardura) (cause more BP lowering than the others)

Tamsulosin (Flomax), Alfuzosin (Uroxatrol) and Silodosin (Rapaflo) have less BP effects

  1. Can cause severe hypotension if used with phosphodiesterase-5 inhibitors
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7
Q

Other SE of alpha-1 blockers?

3

A
  1. Asthenia (muscle weakness)
  2. Nasal congestion
  3. Problems with ejaculation

Found primarily with Tamsulosin (Flomax)
Can decrease volume of ejaculate by 90%
35% of patients may have no ejaculate
Up to 28% have retrograde ejaculation on Silodosin (Rapaflo)

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8
Q

5 alpha-reductase inhibitors

What are the meds? 2

A
  1. Finasteride (Proscar)

2. Dutasteride (Avodart)

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9
Q

5 alpha-reductase inhibitors

Only agents that provide long term what? 2

A
  1. decrease in prostate size and

2. decreased need for prostatic surgery

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10
Q

MOA of 5-ARI’s
1. Competitive inhibitor of both what? 2

  1. MOA?
  2. Serum dihydrotestosterone decreases by ___%?
    - Primary androgen in what?
  3. Serum testosterone increases by ____%
    - Decreases _______ size
A
    • tissue and
    • hepatic 5-alpha reductase
  2. inhibition of the conversion of testosterone to dihydrotestosterone and markedly suppresses serum dihydrotestosterone levels
  3. 70
    - prostate and hair follicles
  4. 10
    - prostatic
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11
Q

MOA of 5-ARI’s
1. May be how long to notice a reduction in symptoms?

  1. Increase in maximum what?
  2. Reduction in what by about 18%?
  3. Decreased need for ______?
  4. Decreased development of what?
  5. The larger the what the more effective the medication?
  6. Which one is usually more potent?
A
  1. up to a year
  2. urinary flow rate
  3. mean prostatic volume
  4. surgery
  5. acute urinary retention
  6. prostate volume
  7. Dutasteride (Avodart) may be more potent than Finasteride (Proscar)
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12
Q

MOA of 5-ARI’s
1. Major side effects? 2

  1. Timeline?
  2. _________ serum PSA by 50%
  3. Use a factor of __ when interpreting PSA results in the first 24 months of therapy
    Use a factor of __ after 24 months
  4. Decreased development of prostate cancer but concern for possible increased incidence of what?
A
    • Decreased libido
    • Ejaculatory or erectile problems
  2. May only have these effects for the first year of therapy
  3. Decreases
  4. 2, 2.5
  5. high grade lesions
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13
Q

Cialis for BPH

  1. MOA?
  2. What can you not use with it?
  3. Dosing?
  4. Takes how long to note symptom improvement for BPH?
A
  1. Cialis blocks PDE5 in the prostate and bladder
  2. Do not use with
    - nitrates or
    - alpha-1 blockers
  3. 5mg daily dose
  4. Takes 2-4 weeks to note symptom improvement when used for BPH
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14
Q

Erectile Dysfunction

Which drug classes for use? 2

A
  1. Prostaglandin injectable

2. Phosphodiasterase inhibitors

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15
Q

Erectile Dysfunction
Which drugs are in the following categories:
1. Prostaglandin injectable? 1
2. Phosphodiasterase inhibitors? 4

A
  1. Prostaglandin injectable
    - Alprostadil
  2. Phosphodiasterase inhibitors
    - Tadalafil (Cialis)
    - Vardenafil (Levitra)
    - Sildenafil (Viagra)
    - Avanafil (Stendra)
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16
Q

Alprostadil (Caverject, Muse)

  1. Drug category?
  2. Forms? 2
  3. MOA?
  4. Onset?
  5. Duration of action?
A
  1. Drug category: Prostaglandin, Vasodilator
  2. Forms:
    - Intracavernosal injections,
    - urethral pellets
  3. MOA
    Causes vasodilation by means of direct effect on vascular and smooth muscle; relaxes trabecular smooth muscle by dilation of cavernosal arteries when injected along the penile shaft, allowing blood flow to and entrapment in the lacunar spaces of the penis (ie, corporeal veno-occlusive mechanism)

Onset and duration of action

  1. Onset 5-20 minutes
  2. Duration less than 1 hour
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17
Q

Alprostadil (Caverject, Muse)
1. Contraindications? 3

  1. SE? 3
A
  1. Contraindications
    - Conditions that predispose the patient to priapism
    - Anatomic or fibrotic conditions of the penis
    - For the pellets (Muse) – urethral stricture, perineal pain
  2. Side effects
    - Syncope
    - Priapism
    - May cause BP lowering
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18
Q

Phosphodiasterase inhibitors MOA
1. The physiologic mechanism of erection of the penis involves release of what into where?

  1. NO then activates the enzyme _____________, which results in increased levels of cyclic guanosine monophosphate (cGMP),
  2. producing smooth muscle relaxation and inflow of blood to the what?
  3. Enhances the effect of NO by inhibiting what, which is responsible for degradation of cGMP in the corpus cavernosum?
  4. Do not directly cause what?
A
  1. nitric oxide (NO) in the corpus cavernosum during sexual stimulation
  2. guanylate cyclase
  3. corpus cavernosum
  4. phosphodiesterase type 5 (PDE-5)
  5. penile erections
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19
Q

Phosphodiasterase inhibitors Contraindications

2

A
  1. Men taking nitrates

2. Caution with alpha-1 blockers due to risk for severe hypotension

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20
Q

Phosphodiasterase inhibitors
Adverse reactions
6

A
  1. Severe hypotension (with nitrates or alpha-1 blockers)
  2. Common: flushing, headaches, dyspepsia
  3. Visual effects: transient blue vision with sildenafil (Viagra), may increase risk for nonarteritic ischemic optic neuropathy
  4. Hearing loss
  5. Priapism
  6. Drug interactions: CYP3A4 inhibitors may increase the serum concentration of the PDE-5
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21
Q

Administration of Phosphodiasterase inhibitors
1. In general take _____ prior to intercourse?

  1. Which drugs have a quicker onset of action (30 min)? 2
  2. What will delay the onset of action in Sildenafil (Viagra) and Vardenafil (Levitra)?
  3. ______ dose Tadalafil (Cialis) is available
  4. Duration of action ____ hours on average except for Tadalafil (Cialis) up to___ hours
A
  1. 60 min
  2. Vardenafil (Levitra) and Avanafil (Stendra)
  3. Food and alcohol
  4. Daily
  5. 8-12, 36
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22
Q

Hold nitrates for 1.___ hours after use of a PDE-5 or for 2.___ hours if used taldafil (Cialis)

A
  1. 24

2. 48

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23
Q

Testosterone replacement

Treats what?

A

To treat low testosterone levels in primary or secondary hypogonadism

24
Q
  1. Whats primary hypogonadism?

2. Secondary? 2

A
  1. Primary – Testes fail to produce testosterone

2. Secondary – Pituitary or hypothalamus malfunction

25
Q

Testosterone replacement

MOA?

A
  1. Direct action by binding to the androgen receptor
  2. Act in tissues that express the enzyme 5-alpha reductase
    - Converts to dihydrotestosterone
    - Binds more readily to the androgen receptor than testosterone
  3. Can act as an estrogen after converting to estradiol via an aromatase and bind to the estrogen receptor
26
Q

Testosterone replacement
Principles of therapy
1. Only use in men that are what?
2. Symptoms that are treated? 7

  1. Goal of therapy?
  2. Do not use it to treat impaired what?
    - why?
A
  1. Only for use in men who are hypogonadal
    • Decreased libido;
    • decreased AM erections;
    • loss of body hair;
    • low bone density;
    • gynecomastia;
    • small testes;
    • decreased muscle mass
  3. Goal of therapy is to return testosterone levels back to the normal range
  4. Do not use it to treat impaired spermatogenesis
    - Testosterone therapy suppresses pituitary gonadotropin secretion and leads to more impairment of spermatogenesis
27
Q

Testosterone replacement: Prior to starting therapy? 3

A
  1. Screen for prostate cancer in men over 50 or in men over age 40 if any risk factors
  2. Screen for erythrocytosis
  3. If sleep apnea is present, make sure it is being treated
28
Q

Side effects of testosterone?

10

A
  1. Polycythemia
  2. Worsening of BPH symptoms
  3. Acne
  4. Increase in PSA
  5. Oral and prolonged IM doses associated with a multitude of liver issues (jaundice, hepatitis, elevated LFTs)
  6. Increased risk of prostate cancer
  7. Decreased spermatogenesis
  8. Fluid retention
  9. Worsening of sleep apnea
  10. Possible increased risk of cardiovascular events
29
Q

Contraindications
Testosterone replacement?
7

A
  1. Known prostate cancer
  2. Known breast cancer
  3. Severe lower urinary tract symptoms
  4. HCT > 50%
  5. Untreated severe sleep apnea
  6. PSA > 4.0 mcg/L
  7. PSA > 3.0 mcg/L with any prostate CA risk factors
30
Q

Tesosterone replacement: On the FDA watch list?

Why?

A

The FDA is investigating the risk of stroke, heart attack, and death in men taking FDA-approved testosterone products. The FDA is evaluating information from 2 separate studies that suggest an increased risk of cardiovascular events among groups of men prescribed testosterone therapy, although the agency has not concluded that these products increase the risk of stroke, heart attack, or death.

31
Q

Tesosterone replacement: Many routes of delivery exist?

6

A
  1. Oral (hepatic side effects)
  2. Buccal tablet (BID)
  3. Subcutaneous pellet (replace 3-6 months)
  4. Nasal gel (TID)
  5. Parenteral (Long acting
    and Extra long acting (restricted prescribing))
  6. Transdermal/topical (Patch and
    Gel)
32
Q

Tesosterone replacement: Which formulation to use.
1. Whats a good first choice therapy?

  1. Labs to check while on testosterone?
    3
A
  1. Transdermal gel is a good first choice of therapy
  2. Labs
    - Serum testosterone,
    - hematocrit,
    - PSA prior to initiating therapy
33
Q

What are the gels for testosterone replacement? 4

A
  1. AndroGel
    Metered pump or packets
  2. Testim
    Dispensed in tubes of 50 or 100 mg
  3. Fortesta
    Metered dose pump
    Apply to front and inner thighs
  4. Axiron
    Metered dose pump
    Apply to each axilla
34
Q
  1. What is androderm?

2. Risks?

A
  1. Testosterone repleacement for worn on the arm or torso

2. Significant skin irritation and 1/3 of men discontinue use due to this side effect

35
Q

What are the drugs for IM testosterone? 2

Inject where?

A
  1. Testosterone enanthate (Delatestry)
  2. Testosterone cypionate (Depo-Testosterone)

Gluteal injections
Once weekly (50-100 mg) or
Once every 2 weeks (100-200 mg)

36
Q

Monitoring therapy for testosterone replacement?

4

A
  1. Serum testosterone
  2. Bone density
  3. PSA and DRE
  4. HCT
37
Q
  1. When would we check the serum testosterone after starting therapy or changing dose?
  2. If primary hypogonadism check what?
  3. Bone density: Recheck ________ until normalizes or stabilizes
  4. PSA and DRE: Check when after starting treatment?
  5. Problematic if what? 3
  6. HCT: check when after initiation of therapy?
    - DC if at what level?
A
  1. 2-3 months after starting treatment or changing dose
  2. If primary hypogonadism check for normalization of serum LH
  3. Q 2 years
  4. 3-6 months after starting treatment and then Yearly
    • prostate nodule;
    • increase in PSA > 1.4 in a year;
    • PSA velocity > 0.4 per year for 2 or more years
  6. 3-6 months after starting therapy then yearly
    - DC if HCT ≥ 54
38
Q

Urinary tract analgesics

What drug?

A

Phenazopyridine (Pyridium)

39
Q

Urinary tract analgesia

  1. Used for?
  2. Do not use if when?
  3. Which is prescription?
  4. Which are over the counter? 2
A
  1. Symptomatic relief of urinary burning, itching, frequency and urgency associated with UTI or post urologic procedures
  2. Do not use if GFR less than 50
  3. Pyridium is prescription
  4. OTC formulations: Azo-Gesic, Baridium , Urinary pain relief
40
Q

Phenazopyridine (Pyridium)
Prescribing considerations
1. Don’t use for more than how long?
2. Can turn skin and/or sclera what?

  1. Turns urine what color?
  2. ONly used for what?
  3. Other than orange urine the most common adverse reactions are what? 3
A
  1. 2 days
  2. yellow
  3. bright orange
  4. Only used for symptom relief, does not treat infection
    • headache,
    • dizziness and
    • stomach cramps
41
Q

Pentosan (Elmiron)

  1. Class?
  2. Indication?
  3. Dosing?
  4. Trial for how many months?
  5. MOA? 2
A
  1. Class: Urinary analgesic
  2. Indications: Interstitial cystitis
  3. 100 mg TID
  4. Trial for 3-6 months to determine efficacy
  5. MOA
    - the drug appears to adhere to the bladder wall mucosa where it may act as a buffer to protect the tissues from irritating substances in the urine
    - low-molecular weight heparinoid
42
Q

Pentosan (Elmiron): Adverse Reactions Significant 1% to 10%:
5

A
  1. Central nervous system: Headache (3%), dizziness (1%)
  2. Dermatologic: Alopecia (4%), rash (3%)
  3. Gastrointestinal: Rectal hemorrhage (6%), diarrhea (4%), nausea (4%), abdominal pain (2%), dyspepsia (2%)
  4. Hepatic: Liver function test abnormalities (1%; dose related)
  5. Cost for 100 mg tablets (100): $814.98
43
Q

Incontinence
1. Drug class?

  1. What drugs are in this class?
    6
A
  1. Muscarinic antagonists/Antispasmodics
    • Oxybutynin (Ditropan) (Ditropan XL) (Oxytrol transdermal patch)
    • Tolterodine (Detrol) (Detrol LA)
    • Trospium (Sanctura), (Trospium XR)
    • Solifenacin (Vesicare)
    • Darifenacin hydrobromide (Enablex)
    • Fesoterodine (Toviaz)
44
Q

Treatment of urgency, urgency-predominant mixed or OAB symptoms

  1. Do not use therpy in who?
  2. Contraindications in what? 2
  3. MOA? 2
A
  1. Do not use pharmacologic therapy in demented patients
  2. Contraindications for antimuscarinic agents
    - Gastric retention
    - Angle closure glaucoma
  3. MOA
    - Increase bladder capacity
    - Block basal release of acetylcholine during bladder filling resulting in decreased urgency
45
Q

Antimuscarinic agents
1. Compare extended release agents with immediate release agents in terms of adverse affects?

  1. Start with what dose?
  2. Evaluate for response when?
  3. On average takes at least how many weeks to peak efficiency?
  4. Reduce starting dose in what age?
  5. If you dont respond to what agent what can you do?
A
  1. Extended release agents have lower rates of adverse effects than immediate release agents
  2. Start with the lowest available dose
  3. Evaluate for response in 4-6 weeks
  4. On average takes at least 4 weeks to peak efficacy
  5. Reduce starting dose in age 60 or older
  6. May respond to one agent and not another so okay to try others in the same class
46
Q

Antimuscarinic agents
Adverse effects
7

A 
Discontinuation  rate of 58-71% at six months
Anticholinergic effects
1. Dry mouth, 
2. constipation, 
3. blurred vision to near objects, 
4. tachycardia,
5. drowsiness, 
6. decreased cognitive function, 
7. dizziness
47
Q

Considerations for prescribing Antimuscarinic agents
Generally prescribe which formulations?
2

A

Generally prescribe

  1. extended release or
  2. transdermal formulations
48
Q

Drug combos to avoid in Antimuscarinics?

11

A
  1. First generation antihistamines
  2. Muscle relaxants
  3. Some antipsychotics
  4. TCAs
  5. Ipratropium (Combivent)
  6. Tiotropium (Spiriva)
  7. Cholinesterase inhibitors (donepezil, rivastigmine, galantamine)
  8. Triospium and ETOH within 2 hours
  9. Mirabegron
  10. Metoprolol and darifenacin
  11. Grapefruit juice (darrifenacin, solifenacin, festerodine, tolerodine)
49
Q

What antimuscarinics are most commonly prescribed?

2

A
  1. Oxybutynin (Ditropan) (Ditropan XL) (Oxytrol transdermal patch)
  2. Tolterodine (Detrol) (Detrol LA)!!!!
50
Q

Common antibiotics for the treatment of UTI

5

A
  1. Ciprofloxacin
  2. Trimethoprim/sulfamethoxazole (Bactrim/Septra)
  3. Nitrofurantion (Macrodantin)
  4. Amoxicillin
  5. Ampicillin
51
Q

Ciprofloxacin

  1. Class?
  2. MOA?
  3. Pregnancy category?
  4. Black box warnings (2)?
  5. Adjust dose based on renal function?
  6. Urologic indications? 3
A
  1. Fluoroquinolone
  2. Inhibit the ability of the bacterial DNA to replicate- Inhibit DNA gyrase and topoisomerase IV necessary for replication of bacteria
  3. D
    • Tendon rupture
    • Qt prolongation
  5. yes, unless using moxifloxacin
    • Cystitis
    • UTI
    • Prostatitis

Urinary tract (DOC)- cipro covers pseudomonas

52
Q

Trimethoprim/sulfamethoxazole (Bactrim/Septra)

  1. Class?
  2. MOA?
  3. Pregnancy category?
A
  1. Sulfonamides
  2. Folic acid synthesis inhibitors
    (SMX inhibits dihydropteroate synthetase and TMP inhibits dihydrofolate reductase)
  3. Preg Cat C
53
Q

Nitrofurantion (Macrodantin)

  1. MOA?
  2. Pregnancy category?
  3. Urologic indications?
  4. What about using this drug in the setting of chronic kidney disease and decreased CrCl?
A
  1. Thought to disrupt bacterial cell wall synthesis through inhibition of bacterial enzymes
  2. Preg Cat B
  3. Only for treatment and prevention of uncomplicated urinary tract infections
  4. Cleared renally and is concentrated in the urine
    - Inadequate drug levels in the bladder if the creatinine clearance is abnormal (GFR
54
Q

Amoxicillin

  1. Class?
  2. MOA?
  3. Pregnancy category?
  4. Urologic indications?
A
  1. 2nd generation broad spectrum PCN
  2. Most β-lactam antibiotics work by inhibiting cell wall biosynthesis in the bacterial organism.
  3. B
  4. UTI in pregnancy
55
Q

Ampicillin

  1. Class?
  2. MOA?
  3. Pregnancy category?
  4. Urologic indications?
  5. What forms does this drug come in? 4
A
  1. 2nd generation broad spectrum PCN
  2. Most β-lactam antibiotics work by inhibiting cell wall biosynthesis in the bacterial organism.
  3. B
  4. UTI in pregnancy
  5. Injection, IV, Oral, and oral suspension

Urology (12 decks)

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