Solifenacin

What is Solifenacin?

• Solifenacin (VESIcare) is a muscarinic antagonist used for the treatment of adults with overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency.
• Solifenacin (VESIcare LS) is used to for the treatment of neurogenic detrusor overactivity in pediatric patients aged 2 years and older.

Solifenacin structure

What are the uses of this medicine?

• Solifenacin (VESIcare) is s a prescription medicine for adults used to treat the following symptoms due to a condition called overactive bladder:
• Urge urinary incontinence: a strong need to urinate with leaking or wetting accidents
• Urgency: a strong need to urinate right away
• Frequency: urinating often

• Solifenacin (VESIcare LS) is a prescription medicine for children aged 2 years of age and older with a condition called neurogenic detrusor overactivity. It is used to increase the amount of urine your bladder can hold and reduce urine leakage.

Solifenacin Structural Formulae V.1

Overactive bladder:

• Overactive bladder occurs when you cannot control your bladder contractions.
• When these muscle contractions happen too often or cannot be controlled you can get symptoms of overactive bladder, which are urinary frequency, urinary urgency, and urinary incontinence (leakage).

How does this medicine work?

• Solifenacin is a competitive muscarinic receptor antagonist.
• Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of urinary bladder smooth muscle.
• It is an anticholinergic agent that inhibits muscarinic actions of acetylcholine on autonomic nerve endings, decreasing secretions and inhibiting gastrointestinal and bladder motility.
• Solifenacin increases the bladder capacity and decreases contractions and the urgency of urination.

Solifenacin

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are not able to empty your bladder (urinary retention).
• have delayed or slow emptying of your stomach (gastric retention).
• have an eye problem called “uncontrolled narrow-angle glaucoma”.
• are allergic to solifenacin succinate or any of the ingredients.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention any of the following:

• amiodarone (Nexterone, Pacerone)
• clarithromycin
• disopyramide (Norpace)
• dofetilide (Tikosyn)
• erythromycin (E.E.S., ERYC, Erythrocin)
• HIV protease inhibitors such as indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir, in Kaletra, in Viekira), and saquinavir (Invirase)
• itraconazole (Sporanox), ketoconazole, nefazodone
• pimozide
• procainamide
• quinidine (in Neudexta)
• sotalol (Betapace, Sorine, Sotylize)
• thioridazine

Is this medicine FDA approved?

• Solifenacin was approved for use in the United States in 2004 and it remains in clinical use.

How should this medicine be used?

Recommended dosage: VESIcare dosage:

• The recommended oral dose of solifenacin succinate is 5 mg once daily.
• If the 5 mg dose is well tolerated, the dose may be increased to 10 mg once daily.

Dosing Recommendations in Patients with Renal Impairment:

• Do not exceed 5 mg once daily in patients with severe renal impairment (CLcr < 30 mL/min/1.73 m2).

Dosing Recommendations in Patients with Hepatic Impairment:

• Do not exceed 5 mg once daily in patients with moderate hepatic impairment.
• Do not use solifenacin succinate in patients with severe hepatic impairment.

Dosing Recommendations in Patients Taking CYP3A4 Inhibitors:

• Do not exceed 5 mg once daily when solifenacin succinate is administered with strong CYP3A4 inhibitors such as ketoconazole.

VESIcare LS dosage: VESIcare LS oral suspension has a concentration of 1 mg/1 mL. The recommended doses are weight-based and are administered once daily.

Once Daily Recommended Dosage According to Patient Body Weight

Weight range	Starting dose	Maximum dose
9 kg to 15 kg	2 mL	4 ml
greater than 15 kg to 30 kg	3 ml	5 ml
greater than 30 kg to 45 kg	3 ml	6 ml
greater than 45 kg to 60 kg	4 ml	8 ml
greater than 60 kg	5 ml	10 ml

Do not exceed the recommended starting dose of VESIcare LS in patients with:

• Severe renal impairment creatinine clearance < 30 mL/min/1.73 m2. (2.2, 8.6)
• Moderate hepatic impairment (Child-Pugh B).
• VESIcare LS is not recommended in patients with severe hepatic impairment.
• Concomitant use of strong CYP3A4 inhibitors.

Administration:

• Solifenacin comes as a tablet (VESIcare) and a suspension (liquid; VESIcare LS) to take by mouth.

Solifenacin succinate tablets:

• Take solifenacin succinate tablet exactly as your doctor tells you to take it.
• You should take 1 solifenacin succinate tablet 1 time a day.
• You should take solifenacin succinate tablet with water and swallow the tablet whole.
• You can take solifenacin succinate tablet with or without food.
• If you miss a dose of solifenacin succinate tablet, begin taking solifenacin succinate tablet again the next day. Do not take 2 doses of solifenacin succinate tablet the same day.
• If you take too much solifenacin succinate tablet, call your doctor or go to the nearest hospital emergency room right away.

VESIcare LS oral suspension:

• Shake the bottle well before taking each dose.
• You should take VESIcare LS by mouth 1 time a day.
• Use an oral dosing device, such as an oral syringe, to correctly measure your dose. Ask your pharmacist for an appropriate oral dosing device.
• You should take VESIcare LS followed by water or milk. Avoid taking VESIcare LS at the same time with food or other drinks, as this may result in a bitter taste.
• Do not take 2 doses of VESIcare LS the same day.
• If you miss a dose of VESIcare LS, take it as soon as possible.
• If it has been 12 hours since taking the last dose of VESIcare LS, skip that dose and take the next dose at the usual time.
• If you take too much VESIcare LS, call your doctor or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 5 mg and 10 mg.
• As Oral suspension: 5 mg/5 mL (1 mg/mL) of solifenacin succinate.

This medicine is available in fallowing brand namesː

• VESIcare ; VESIcare LS

What side effects can this medication cause?

The most common side effects of this medicine may include:

• dry mouth
• constipation
• urinary tract infection
• blurred vision

Other side effects have been observed with anticholinergic drugs such as solifenacin succinate and may include:

• dry skin due to decreased sweating. Heat exhaustion or heat stroke can happen due to decreased sweating when solifenacin succinate tablets are used in hot environments. Symptoms may include:
• decreased sweating
• dizziness
• tiredness
• nausea
• increase in body temperature

Solifenacin succinate may cause serious side effects including:

• Serious allergic reaction
• Central Nervous System (CNS) effects

What special precautions should I follow?

• Solifenacin succinate can cause blurred vision or drowsiness. Do not drive or operate heavy machinery until you know how solifenacin succinate tablet affects you.
• Angioedema of the face, lips, tongue, and/or larynx have been reported with solifenacin succinate. Inform patients that angioedema and anaphylactic reactions have been reported in patients treated with solifenacin succinate. Angioedema and anaphylactic reactions may be life-threatening. Advise patients to promptly discontinue solifenacin succinate therapy and seek immediate attention if they experience edema of the tongue or laryngopharynx, or difficulty breathing.
• The use of solifenacin succinate, like other antimuscarinic drugs, in patients with clinically significant bladder outlet obstruction including patients with urinary retention, may result in further urinary retention and kidney injury.
• The use of solifenacin succinate, like other antimuscarinic drugs, in patients with conditions associated with decreased gastrointestinal motility may result in further decreased gastrointestinal motility.
• Solifenacin succinate is associated with antimuscarinic central nervous system (CNS) adverse reactions. Because solifenacin succinate, like other antimuscarinic agents, may cause central nervous system effects or blurred vision, advise patients to exercise caution in decisions to engage in potentially dangerous activities until the drug's effect on the patient has been determined.
• Solifenacin succinate should be used with caution in patients being treated for narrow-angle glaucoma.
• Solifenacin succinate is not recommended for use in patients at high risk of QT prolongation, including patients with a known history of QT prolongation and patients taking medications known to prolong the QT interval.
• Inform patients that solifenacin succinate, like other antimuscarinics, may cause dry skin due to decreased sweating. Heat prostration due to decreased sweating can occur when solifenacin succinate is used in a hot environment.
• It is not known if solifenacin succinate passes into your breast milk. You and your doctor should decide if you will take solifenacin succinate tablets or breastfeed.
• Solifenacin has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• antimuscarinic effects
• mental status changes
• decrease in the level of consciousness
• Intolerable antimuscarinic adverse reactions (fixed and dilated pupils, blurred vision, failure of heel-to-toe exam, tremors, and dry skin)

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• In the event of overdose with solifenacin succinate, treat with gastric lavage and appropriate supportive measures.
• ECG monitoring is also recommended.

Can this medicine be used in pregnancy?

• There are no studies with the use of solifenacin succinate in pregnant women or adolescents to inform a drug-associated risk of major birth defects, miscarriages, or adverse maternal or fetal outcomes.
• It is not known if solifenacin succinate will harm your unborn baby. Talk to your doctor if you are pregnant or plan to become pregnant.

Can this medicine be used in children?

• Solifenacin succinate tablets 5 mg and 10 mg tablets are not approved for use in children
• The safety and effectiveness of VESIcare LS have been established in pediatric patients aged 2 years and older for the treatment of neurogenic detrusor overactivity (NDO).
• The safety and effectiveness of VESIcare LS have not been established in pediatric patients less than 2 years of age.

What are the active and inactive ingredients in this medicine?

VESIcare LS:

• Active ingredient: solifenacin succinate
• Inactive ingredients: polacrilin potassium, methylparaben, propylparaben, propylene glycol, simethicone emulsion 30%, carbomer homopolymer Type B, xylitol, acesulfame potassium, natural orange flavor, sodium hydroxide, and purified water.

Solifenacin succinate tablets:

• Active ingredient : solifenacin succinate
• Inactive ingredients : corn starch, hypromellose, lactose monohydrate, and magnesium stearate. The film coating consists of: iron oxide yellow (5 mg solifenacin succinate tablet) or iron oxide red (10 mg solifenacin succinate tablet), polyethylene glycol (PEG), polyvinyl alcohol, titanium dioxide, and talc.

Who manufactures and distributes this medicine?

Solifenacin succinate tablets: Manufactured for:

• Graviti Pharmaceuticals Inc.,
• Wilmington, Delaware, USA.

VESIcare LS: Marketed and Distributed by:

• Astellas Pharma US, Inc.
• Northbrook, IL
• VESIcare LS is a registered trademark of Astellas US LLC.

What should I know about storage and disposal of this medication?

VESIcare LS:

• Store VESIcare LS at room temperature, between 68°F to 77°F (20°C to 25°C) with the cap closed.
• Store VESIcare LS in the original bottle.
• Throw away VESIcare LS oral suspension 28 days (4 weeks) after first opening.
• Safely throw away VESIcare LS that has expired or is unused.

Solifenacin succinate tablets:

• Store solifenacin succinate tablets between 59°F to 86°F (15°C to 30°C). Keep the bottle closed.
• Safely throw away medicine that is out of date or no longer needed.

Urologic agents

• Overactive bladder syndrome agents - darifenacin, fesoterodine, flavoxate, hyoscyamine, mirabegron, oxybutynin, solifenacin, tolterodine, trospium

• Dailymed label info on Solifenacin
• FDA Solifenacin

Solifenacin Resources
Latest articles Most recent articles Ongoing trials	Wikipedia

Solifenacin Resources
Latest articles Most recent articles Ongoing trials	Wikipedia