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Solifenacin Succinate

Pronunciation: (SOE-li-FEN-a-sin SUX-i-nate)
Class: Anticholinergic

Trade Names

Vesicare
- Tablets, oral 5 mg
- Tablets, oral 10 mg

Pharmacology

Competitive muscarinic receptor agonist.

Pharmacokinetics

Absorption

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

Distribution

Plasma protein binding is approximately 98%, principally to alpha-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 half-life is approximately 45 to 68 h. Approximately 69% of the administered dose is recovered in the urine and 22.5% in the feces. Less than 15% is recovered in the urine as intact solifenacin.

Special Populations

Renal Function Impairment

There is a 2.1-fold increase in AUC and 1.6-fold increase in half-life of solifenacin in patients with severe renal impairment.

Hepatic Function Impairment

There is a 2-fold increase in the half-life and 35% increase in AUC of solifenacin in patients with moderate hepatic impairment. Solifenacin is not recommended for patients with severe hepatic impairment (Child-Pugh class C).

Elderly

Elderly volunteers (65 to 80 y of age) showed that C _max , AUC, and half-life values were 20% to 25% higher compared with younger volunteers (18 to 55 y of age).

Children

The pharmacokinetics of solifenacin have not been established in children.

Gender

The pharmacokinetics of solifenacin are not significantly influenced by gender.

Race

The number of subjects of different races studied is not adequate to make any conclusions on the effect of race on the pharmacokinetics of 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

Adults

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

Renal Impairment
Adults

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

Hepatic Impairment
Adults

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

CYP3A4 Inhibitors
Adults

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 between 59° and 86°F.

Drug Interactions

Potassium preparations (eg, potassium chloride)

Passage of solid doseforms of potassium chloride through the GI tract may be delayed or arrested because of slowing of GI motility by solifenacin. Coadministration of solid doseforms of potassium chloride and solifenacin is contraindicated. Potassium chloride liquid may be a suitable alternative.

Potent CYP3A4 inhibitors (eg, atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole)

May elevate solifenacin plasma concentrations, increasing the risk of adverse effects. It is recommended not to exceed a 5 mg daily dose of solifenacin when administered with therapeutic doses of potent CYP3A4 inhibitors.

Strong CYP3A4 inducers (eg, rifampin)

Solifenacin plasma concentrations may be reduced, decreasing the pharmacologic effect.

Adverse Reactions

Cardiovascular

Hypertension (1%); QT prolongation, torsades de pointes (postmarketing).

CNS

Dizziness, fatigue (2%); depression (1%); confusion, hallucinations, headache (postmarketing).

EENT

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

GI

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

Genitourinary

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

Hypersensitivity

Hypersensitivity reactions, including angioedema with airway obstruction, pruritus, rash, and urticaria (postmarketing).

Respiratory

Cough (1%).

Miscellaneous

Influenza (2%); lower-limb edema (1%); peripheral edema (postmarketing).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hypersensitivity

Angioedema of the face, lips, tongue, and/or larynx has been reported.

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, or clinically important bladder outflow obstruction, and in patients with a history of QT prolongation or who are taking medications known to prolong the QT interval.

Overdosage

Symptoms

Acute

Decreased level of consciousness, mental status changes, severe anticholinergic effects.

Chronic

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

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 at once 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 if they 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: inability to urinate, severe abdominal pain, sudden eye pain.
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.
Inform patients that solifenacin may produce angioedema, which could result in life-threatening airway obstruction. Instruct patient to promptly discontinue the medication and seek medical attention immediately if edema of the tongue or laryngopharynx or difficulty breathing is experienced.