Solifenacin Succinate

Trade Names:
Vesicare
- Tablets 5 mg
- Tablets 10 mg

Pharmacology

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Competitive muscarinic receptor agonist.

Pharmacokinetics

Absorption

Bioavailability 90%. Steady-state C _max from 32.3 to 62.9 ng/mL for the 5 and 10 mg tablets, respectively. Plasma concentrations are proportional to the administered dose. C _max reached in 3 to 8 h.

Distribution

Plasma protein binding approximately 98%, principally to a ₁ -acid glycoprotein. Vd is 600 L.

Metabolism

Primarily metabolized by CYP3A4; however, alternate pathways exist. Pharmacologically active metabolite, 4R-hydroxy solifenacin, occurs in low concentrations and is unlikely to be clinically important. Three pharmacologically inactive metabolites have been found.

Elimination

Elimination t _½ is about 45 to 68 h. Approximately 69% of the administered dose is recovered in the urine and 22.5% in the feces. Less than 15% recovered in the urine as intact solifenacin.

Indications and Usage

Treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency.

Contraindications

Urinary retention, gastric retention, uncontrolled narrow-angle glaucoma, hypersensitivity to any component of the product.

Dosage and Administration

PO 5 mg once daily. If 5 mg dose is well tolerated, the dose may be increased to 10 mg/day.

PO Do not administer more than 5 mg/day in patients with CrCl less than 30 mL/min.

PO Do not administer more than 5 mg/day in patients with moderate hepatic function impairment (Child-Pugh B). Use in patients with severe hepatic function impairment (Child-Pugh C) is not recommended.

PO Do not administer more than 5 mg/day in patients taking therapeutic doses of ketoconazole or other potent CYP3A4 inhibitors.

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F).

Drug Interactions

May elevate solifenacin plasma concentrations, increasing the risk of side effects.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension (1%).

CNS

Dizziness, fatigue (2%); depression (1%).

EENT

Blurred vision (5%); dry eyes (2%); pharyngitis (1%).

GI

Dry mouth (28%); constipation (13%); dyspepsia (4%); nausea (3%); abdominal pain (2%); vomiting (1%).

Genitourinary

UTI (5%); urinary retention (1%).

Respiratory

Cough (1%).

Miscellaneous

Influenza (2%); lower limb edema (1%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Use with caution.

Hepatic Function

Use with caution.

Special Risk Patients

Use with caution in patients with decreased GI motility, narrow-angle glaucoma, clinically important bladder outflow obstruction.

Overdosage

Symptoms

Severe anticholinergic effects.

Fixed and dilated pupils, blurred vision, failure of heel-to-toe exam, tremors, and dry skin.

Patient Information

• Advise patient to read patient information leaflet before starting therapy and with each refill.
• Advise patient to take prescribed dose once daily without regard to meals, but to take with food if stomach upset occurs. Advise patient to swallow tablet whole with liquid and not to crush, chew, or break tablet.
• Advise patient that if a dose is missed to skip that dose and take the next dose at the regularly scheduled time the next day. Caution patient not to take 2 doses to catch up or to take 2 doses of medication in the same day.
• Caution patient not to change the dose or stop taking unless advised by health care provider. Advise patient to notify health care provider if symptoms do not improve or worsen.
• Advise patient that constipation and blurred vision are common side effects of therapy and to notify health care provider if constipation lasts more than 3 days.
• Instruct patient to stop taking the drug and notify health care provider immediately if any of the following occur: severe abdominal pain; sudden eye pain; or inability to urinate.
• Advise patient to avoid strenuous activity during periods of high temperature or humidity.
• Advise patient to take sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
• Inform patient that medication may cause pupils to dilate, resulting in intolerance to bright lights or sunlight. Advise patient to wear dark glasses to make bright lights or sunlight tolerable.
• Advise patient that drug may cause blurred vision and to use caution while driving or performing other tasks requiring good vision until effect on vision has been determined.

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