Module 11. Urologic Disorders

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Table 2. Dosing of Oral Pharmacologic Agents (PDE5 Inhibitors) for the Treatment of ED9,11
Medication (Brand) and strengths Usual dose Dose adjustment

Avanafil

(Stendra)

50, 100, and 200 mg tablets

100 mg orally once daily (range, 50-200 mg) as early as approximately 15 min before sexual activity

Concomitant use with potent CYP3A4 inhibitorsa: Do not use

Concomitant use with moderate CYP3A4 inhibitorsb: Do not exceed 50 mg once daily, approximately 30 min before sexual activity

Concomitant use with an α-receptor antagonist; patients should be stable on the α-receptor antagonist first, then start treatment at 50 mg once daily approximately 30 min before sexual activity

Severe hepatic impairment: No data available; avoid use

CrCl < 30 mL/min: No data available; avoid use

Sildenafil

(Viagra)

25, 50, and 100 mg tablets

50 mg orally up to once daily (range, 25-100 mg) 1 h prior to sexual activity (range, 0.5-4 h)

Geriatric males: 25 mg orally 1 h prior to sexual activity up to once daily

CrCl < 30 mL/min: 25 mg orally up to once daily

Hepatic impairment (mild to moderate): 25 mg orally up to once daily

Concomitant use with potent CYP3A4 inhibitorsa: 25 mg orally up to once daily (maximum dosing frequency of every 48 h if used with ritonavir)

Tadalafil

(Cialis)

2.5, 5, 10, and 25 mg tablets

As needed use: 10 mg orally once daily (range, 5-20 mg) 0.5 h up to 36 h prior to sexual activity

Once-daily use:

2.5 mg orally once daily; may increase to 5 mg once daily

CrCl 30-50 mL/min - as needed use: starting dose of 5 mg orally; maximum dose of 10 mg not more than once every 48 h; once daily use: no dosing adjustment necessary

CrCl < 30 mL/min – as needed use: maximum dose of 5 mg not more than once every 72 h; once daily use: not recommended

Hepatic impairment (mild to moderate) – as needed use: not to exceed 10 mg daily; once daily use: not extensively studied in this patient population; use caution

Concomitant use with potent CYP3A4 inhibitorsa – as needed use: maximum dose of 10 mg, not to exceed every 72 h; once daily use: 2.5 mg orally daily

Vardenafil

(Levitra and Staxyn)

Levitra: 2.5, 5, 10, and 25 mg tablets

Staxyn: 10 mg orally disintegrating tablets

Oral tablet: 10 mg orally once daily (range, 5-20 mg) 1 h prior to sexual activity

Orally disintegrating tablet: 10 mg orally once daily 1 h prior to sexual activity; maximum dose of 10 mg daily; if lower dose required, use regular tablet

Geriatric males: initial dose of 5 mg orally once daily

Hepatic impairment (moderate): initial dose of 5 mg orally once daily, not to exceed 10 mg daily; do not use orally disintegrating tablet in patients with moderate or severe hepatic impairment given higher systemic exposure than regular tablet

Concomitant use with an α-receptor antagonist: patients should be stable on the α-receptor antagonist first, then vardenafil may be added; reduce initial dose to 5 mg (or 2.5 mg if certain CYP3A4 inhibitors also given)

Concomitant use with potent CYP3A4 inhibitorsa: 2.5 or 5 mg up to once daily depending on the agent (maximum dosing frequency of every 72 h if used with ritonavir)

Abbreviations: CrCl, creatinine clearance; CYP3A4, cytochrome P450 3A4.

a Potent CYP3A4 inhibitors include drugs such as erythromycin, ritonavir, ketoconazole, itraconazole, saquinavir
b Moderate CYP3A4 inhibitors include drugs such as erythromycin, amprenavir, aprepitant, diltiazem, fluconazole, fosamprenavir, verapamil


Table 6. Antimuscarinic and β-3 Adrenergic Agonist Agents Used for the Treatment of Urinary Incontinence11
Medication (Brand) and strengths Usual dose Dose adjustment
Oral antimuscarinics

Darifenacin (Enablex)

7.5 and 15 mg extended-release tablets

7.5 mg extended-release tablet once daily initially; may increase to 15 mg once daily after 2 weeks if needed

Concomitant use with potent CYP3A4 inhibitorsa: do not exceed 7.5 mg daily

Not recommended for use in patients with severe hepatic impairment; for patients with moderate hepatic impairment, do not exceed 7.5 mg daily

Fesoterodine (Toviaz)

4 and 8 mg extended-release tablets

4 mg extended-release tablet once daily initially; may increase to 8 mg once daily if needed

Concomitant use with potent CYP3A4 inhibitorsa: do not exceed 4 mg daily

Not recommended for use in patients with severe hepatic impairment

For patients with severe renal impairment, do not exceed 4 mg daily

Oxybutynin (Ditropan XL; immediate-release formulations and extended-release 15 mg tablets are available only as generics)

Immediate-release: 5 mg tablets; 5 mg/5 mL solution and syrup

Ditropan XL: 5, 10, and 15 mg extended-release tablets

Immediate-release: 5 mg 2-3 times daily; maximum of 5 mg 4 times daily (20 mg daily)

Extended-release: 5-10 mg once daily; dose may be increased by 5 mg weekly; maximum dose of 30 mg daily

Immediate-release; geriatric patients: 2.5 mg 2-3 times daily initially, 5 mg 3 times daily may be tolerated

Lower dosages of immediate-release may be needed in hepatic impairment; extended-release formulations not recommended for use in hepatic impairment


Extended-release formulations not recommended in severe renal impairment

Solifenacin (Vesicare)

5 and 10 mg tablets

5 mg once daily; may increase to maximum of 10 mg once daily

Concomitant use with CYP3A4 inhibitors: do not exceed 5 mg daily

CrCl ≤ 30 mL/min: do not exceed 5 mg daily

Not recommended for use in patients with severe hepatic impairment; do not exceed 5 mg daily in patients with moderate hepatic impairment

Tolterodine (Detrol and Detrol LA)

1 and 2 mg immediate-release tablets

2 and 4 mg extended-release capsules

Immediate-release: 2 mg twice daily; may reduce to 1 mg twice daily based on response and tolerability

Extended-release: 4 mg once daily; may reduce to 2 mg once daily based on response and tolerability

CrCl ≤ 30 mL/min or hepatic impairment: reduce dose to 1 mg twice daily for immediate-release; 2 mg once daily for extended-release

Concomitant use with CYP3A4 inhibitors: reduce dose to 1 mg twice daily for immediate-release; 2 mg once daily for extended-release

Trospium (both immediate- and extended-release products available as generics only)

20 mg immediate-release tablets

60 mg extended-release capsules

Immediate-release: 20 mg twice daily; may reduce to 20 mg once daily at bedtime based on tolerability; maximum 60 mg daily

Extended-release: 60 mg once daily in the morning

CrCl < 30 mL/min: reduce dose to 20 mg once daily at bedtime for immediate-release; extended-release dosage form not recommended

Use with caution in patients with hepatic impairment

Nonoral antimuscarinics

Topical oxybutynin (Gelnique)

10% topical gel

Gelnique 10% topical gel: Apply 1 packet of 10% gel once daily (100 mg)

May be applied to abdomen, upper arms/shoulders, or thighs, rotate site so same site not utilized on consecutive days

No dosing adjustment recommendations

Transdermal oxybutynin (Oxytrol [prescription] and Oxytrol for Women [over-the-counter])b

3.9 mg/24 h transdermal patch

Apply 1 patch to abdomen, hip, or buttock twice weekly (3.9 mg daily)

Every 3-4 days, rotate site to avoid irritation

β-3 adrenergic agonist

Mirabegron (Myrbetriq)

25 and 50 mg extended-release tablets

25 mg once daily; dose may be increased up to 50 mg once daily; maximum dose 50 mg once daily

Moderate hepatic impairment: do not exceed 25 mg once daily; not recommended in severe hepatic impairment

CrCl = 15-29 mL/min: do not exceed 25 mg once daily

CrCl < 15 mL/min: not recommended

Abbreviations: CrCl, creatinine clearance; CYP3A4, cytochrome P450 3A4.

a Potent CYP3A4 inhibitors include drugs such as erythromycin, ritonavir, ketoconazole, itraconazole, saquinavir
b Over-the-counter transdermal oxybutynin is approved for women ≥ 18 years; prescription transdermal oxybutynin is approved for women and men