Urologic Agents

B&O Supprettes ® flavoxate (Urispas ®)
hyoscyamine (Levsin ®)  

Bladder instability (Overactive bladder)

darifenacin (Enablex ® ) oxybutynin (Ditropan ®)
solifenacin (Vesicare ® ) tolterodine (Detrol ® )
trospium (Sanctura ® )  

Urology - Bladder spasm

Belladonna and opium -    B&O Supprettes ®  top of page icon

Drug Category: Analgesic Combination.  Urinary Antispasmodic Agent.

Use:  Relief of moderate to severe pain associated with rectal or bladder tenesmus that may occur in postoperative states and neoplastic situations.  Pain associated with ureteral spasms not responsive to non-narcotic analgesics and to space
intervals between injections of opiates.

Dosing (Adults):  1 suppository rectally once or twice daily. Max 4 doses/day.

Supplied: #15 A: Belladonna extract 16.2 mg and opium 30 mg. #16 A: Belladonna extract 16.2 mg and opium 60 mg.

flavoxate (Urispas ®)  top of page icon

Use
Antispasmodic to provide symptomatic relief of dysuria, nocturia, suprapubic pain, urgency, and incontinence due to detrusor instability and hyper-reflexia in elderly with cystitis, urethritis, urethrocystitis, urethrotrigonitis, and prostatitis

Mechanism of Action
Synthetic antispasmotic with similar actions to that of propantheline; it exerts a direct relaxant effect on smooth muscles via phosphodiesterase inhibition, providing relief to a variety of smooth muscle spasms; it is especially useful for the treatment of bladder spasticity, whereby it produces an increase in urinary capacity

Dosage
Children >12 years and Adults: Oral: 100-200 mg 3-4 times/day; reduce the dose when symptoms improve

Dietary Considerations
Should be taken with water on an empty stomach.

Supplied
Tablet [film coated], as hydrochloride: 100 mg

hyoscyamine (Levsin ®)  top of page icon

Use
Oral: Adjunctive therapy for peptic ulcers, irritable bowel, neurogenic bladder/bowel; treatment of infant colic, GI tract disorders caused by spasm; to reduce rigidity, tremors, sialorrhea, and hyperhidrosis associated with parkinsonism; as a drying agent in acute rhinitis

Injection: Preoperative antimuscarinic to reduce secretions and block cardiac vagal inhibitory reflexes; to improve radiologic visibility of the kidneys; symptomatic relief of biliary and renal colic; reduce GI motility to facilitate diagnostic procedures (ie, endoscopy, hypotonic duodenography); reduce pain and hypersecretion in pancreatitis, certain cases of partial heart block associated with vagal activity; reversal of neuromuscular blockade

Mechanism of Action
Blocks the action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands and the CNS; increases cardiac output, dries secretions, antagonizes histamine and serotonin

Dosage
Children >12 years and Adults:
Gastrointestinal disorders
: 0.125-0.25 mg every 4 hours or as needed (before meals or food); maximum: 1.5 mg/24 hours.
Cystospaz®: 0.15-0.3 mg up to 4 times/day.

Oral (timed release): Children >12 years and Adults: Gastrointestinal disorders: 0.375-0.75 mg every 12 hours; maximum: 1.5 mg/24 hours

 I.M., I.V., SubQ: Children >12 years and Adults: Gastrointestinal disorders: 0.25-0.5 mg; may repeat as needed up to 4 times/day, at 4-hour intervals

 I.V.: Adults: Diagnostic procedures: 0.25-0.5 mg given 5-10 minutes prior to procedure

To reduce drug-induced bradycardia during surgery: 0.125 mg; repeat as needed

To reverse neuromuscular blockade: 0.2 mg for every 1 mg neostigmine (or the physostigmine/pyridostigmine equivalent)

Supplied
Capsule, timed release, as sulfate (Cystospaz-M® [DSC], Levsinex®): 0.375 mg
Elixir, as sulfate: 0.125 mg/5 mL (480 mL)
Hyosine: 0.125 mg/5 mL (480 mL)
Levsin®: 0.125 mg/5 mL (480 mL) [contains alcohol 20%; orange flavor]

Injection, solution, as sulfate (Levsin®): 0.5 mg/mL (1 mL)
Solution, oral drops, as sulfate: 0.125 mg/mL (15 mL)
Hyosine: 0.125 mg/mL (15 mL)
Levsin®: 0.125 mg/mL (15 mL) [contains alcohol 5%; orange flavor]
Tablet (Cystospaz®): 0.15 mg
Tablet, orally-disintegrating, as sulfate (NuLev™): 0.125 mg [contains phenylalanine 1.7 mg/tablet, mint flavor]
Tablet, sublingual, as sulfate: 0.125 mg
Levsin/SL®: 0.125 mg [peppermint flavor]
Symax SL: 0.125 mg

Bladder instability (Overactive bladder)

darifenacin (Enablex ® )  top of page icon

Use -Management of symptoms of bladder overactivity (urge incontinence, urgency, and frequency)

Mechanism of Action
Selective antagonist of the M3 muscarinic (cholinergic) receptor subtype. Blockade of the receptor limits bladder contractions, reducing the symptoms of bladder irritability/overactivity (urge incontinence, urgency and frequency).

Dosing (Adults)
: Symptoms of bladder overactivity - Initial: 7.5 mg orally once daily. If response is not adequate after a minimum of 2 weeks, dosage may be increased to 15 mg once daily. Dosage should not be increased in patients with hepatic impairment or in those receiving potent inhibitors of CYP3A4.

Hepatic dosing: Moderate impairment (Child-Pugh Class B): Daily dosage should not exceed 7.5 mg/day. Severe impairment (Child-Pugh Class C): Use is not recommended.

Supplied: Extended release tablet: 7.5 mg, 15 mg.

oxybutynin (Ditropan ®)  top of page icon

Exhibits 20% of the anticholinergic activity of atropine, however, has 4 to 10 times the antispasmodic activity.
Use - Antispasmodic for neurogenic bladder (urgency, frequency, urge incontinence) and uninhibited bladder

Mechanism of Action
Direct antispasmodic effect on smooth muscle, also inhibits the action of acetylcholine on smooth muscle (exhibits 1 /5 the anticholinergic activity of atropine, but is 4-10 times the antispasmodic activity); does not block effects at skeletal muscle or at autonomic ganglia; increases bladder capacity, decreases uninhibited contractions, and delays desire to void; therefore, decreases urgency and frequency

Dosing (Adults)
Oral: 5 mg 2-3 times/day up to 5 mg 4 times/day maximum.
Extended release: Initial: 5-10 mg once daily, may increase in 5-10 mg increments; maximum: 30 mg daily.
Transdermal: Adults: Apply one 3.9 mg/day patch twice weekly (every 3-4 days).
Note: Should be discontinued periodically to determine whether the patient can manage without the drug and to minimize resistance to the drug

Elderly: 2.5 to 5 mg 2-3 times/day

Administration
Oral: Immediate release tablets and solution should be administered on an empty stomach with water. Extended release tablets may be taken with or without food and must be swallowed whole; do not crush, divide, or chew.
Transdermal: Apply to clean, dry skin on abdomen, hip, or buttock. Select a new site for each new system (avoid re-application to same site within 7 days).

Supplied
Syrup, as chloride (Ditropan®): 5 mg/5 mL (473 mL)
Tablet, as chloride (Ditropan®): 5 mg
Tablet, extended release, as chloride (Ditropan® XL): 5 mg, 10 mg, 15 mg
Transdermal system (Oxytrol™): 3.9 mg/day (8s, 24s) [39 cm 2 ; total oxybutynin 36 mg]

solifenacin  (Vesicare ® )  top of page icon

Use - Treatment of overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence
Mechanism of Action - Inhibits muscarinic receptors resulting in decreased urinary bladder contraction, increased residual urine volume, and decreased detrusor muscle pressure.

Dosing (Adults):  Overactive bladder: 5 mg orally once daily. If tolerated, may increase to 10 mg orally once daily.

Renal Dosing: Use with caution in patients with reduced renal function ( Clcr <30 ml/minute: 5 mg/day).

Hepatic impairment: Use with caution in reduced hepatic function: Moderate: 5 mg/day. Severe impairment: Not recommended.

Supplied: 5 mg, 10 mg tablet.

tolterodine (Detrol ® )   top of page icon

Anticholinergic agent -demonstrates selectivity for urinary bladder receptors over salivary receptors.

Dosing (Adults)
:  Immediate release tablet: 2 mg orally twice daily. The dose may be lowered to 1 mg twice daily based on individual response and tolerability.
Extended release capsule: 4 mg once a day- dose may be lowered to 2 mg daily based on individual response and tolerability.

Renal Dosing (Crcl 10-30)/ hepatic impairment: Use with caution. 1 mg twice daily (regular release) or 2 mg daily (extended release).

Supplied: 1 mg, 2 mg tablet. 2 mg, 4mg extended release capsule.

trospium  (Sanctura ® )  top of page icon

Use - Treatment of overactive bladder with symptoms of urgency, incontinence, and urinary frequency

Mechanism of Action - Trospium antagonizes the effects of acetylcholine on muscarinic receptors in cholinergically innervated organs. It reduces the smooth muscle tone of the bladder.

Dosing (Adults)
:  Overactive bladder - 20 mg orally twice daily. In patients >75 years old or if crcl < 30 ml/min decrease dose to 20 mg once daily at bedtime.

Supplied: 20 mg tablet.
 

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.