It is a drug of the antimuscarinic class.
It was developed to treat overactive bladder contraction with associated problems such as increased frequency of urination and urge incontinence .
Solifenacin (INN, trade name Vesicare) is manufactured and marketed by Astellas, GlaxoSmithKline, and Teva Pharmaceutical Industries.
It is available as a brand name drug. It is not available as a generic drug.
Solifenacin comes only as a tablet to take by mouth.
Why is the Vesicare used?
Solifenacin is used to treat the symptoms of overactive bladder (OAB). These symptoms include:
- A strong urge to urinate with leaking or wetting accidents.
- A strong urge to urinate immediately.
- Urinate more often than usual.
How does it work?
Solifenacin is in a class of medications called urinary antagonists.
Normally, when the bladder fills with urine, it expands. Once it has fully expanded, it sends a message to your brain telling you that you are ready to urinate. When you urinate, your bladder muscles contract, which starts the flow of urine.
When you have an overactive bladder, your muscles contract before your bladder fully expands, causing frequent urination .
Solifenacin works by stopping sudden contractions of the bladder muscles and increasing the amount of urine the bladder can hold. This helps control the release of urine and helps reduce symptoms.
Vesicare (solifenacin succinate) is a muscarinic receptor antagonist.
Chemically, solifenacin succinate is butanedioic acid, composed of (1S) – (3R) -1-azabicyclo [2.2.2] oct-3-yl 3,4-dihydro-1-phenyl-2 (1H) iso-quinolinecarboxylate (1: 1) which has an empirical formula of C23H26N2O2 • C4H6O4, and a molecular weight of 480.55.
Solifenacin Succinate is a white to pale yellow-white crystal or crystalline powder. It is freely soluble at room temperature in water, glacial acetic acid, dimethyl sulfoxide, and methanol.
Each Vesicare tablet contains 5 or 10 mg of solifenacin succinate and is formulated for oral administration. In addition to the active ingredient solifenacin succinate, each Vesicare tablet also contains the following inert ingredients:
- Lactose monohydrate, cornstarch, hypromellose 2910, magnesium stearate, talc, polyethylene glycol 8000 and titanium dioxide with yellow ferric oxide (5 mg Vesicare tablet) or red ferric oxide (10 mg Vesicare tablet).
Solifenacin is contraindicated for people with urinary retention, gastric retention, uncontrolled or poorly controlled angle-closure glaucoma, severe liver disease (Child-Pugh class C), and hemodialysis.
Long QT syndrome is not a contraindication, although solifenacin, like tolterodine and darifenacin, binds to hERG channels in the heart and can prolong the QT interval. This mechanism appears to be rarely clinically relevant.
Warning about other conditions : You should not take this drug if you have urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. Use this medicine with caution if you have a heart problem called QT prolongation (irregular heart rate).
Swelling ( Angioedema ) Warning : In rare cases, this drug may cause swelling of the face, lips, tongue, or throat. If swelling occurs and you have trouble breathing, call or go to the emergency room right away.
Dementia warning : Research has indicated that this type of medication can cause effects similar to those caused by medications called anticholinergics. This can increase your risk of dementia.
Vesicare side effects
The most common side effects of solifenacin are dry mouth, blurred vision, urinary tract infection, and constipation . Like all anticholinergics, solifenacin rarely causes hyperthermia due to decreased perspiration.
Vesicare can affect your central nervous system. This could lead to side effects such as headache, confusion, hallucinations, and drowsiness when starting or increasing your dose of this medicine.
Symptoms can include:
- Decreased sweating.
- Increased body temperature (fever).
- Difficulty breathing or chest pain.
- Swelling of your face, lips, tongue, or throat that makes it difficult for you to breathe.
- Severe itching
- Hives , skin rash, or swelling.
If these effects are mild, they can go away in a few days to a couple of weeks. Call your doctor right away if you have serious side effects. Call 911 if your symptoms are life threatening or if you think you have a medical emergency.
Other side effects
This drug comes with several warnings.
This medicine can cause a severe allergic reaction. Symptoms can include:
- Difficulty breathing.
- Swelling of the face, lips, throat, or tongue.
Call or go to the nearest emergency room if you have these symptoms. Taking it again could be fatal (cause death). Talk to your doctor about other drug options that may work for you.
Alcohol Interaction Warning
Using beverages that contain alcohol can make bladder symptoms worse.
Warnings for people with certain health conditions
For people with bladder problems : You should not use this drug if you have urinary retention. Use this medicine with caution if you have other problems emptying your bladder. This can increase your risk of urinary retention.
For people with stomach problems : You should not use this medicine if you have gastric retention. Use this medicine with caution if it has delayed or slowed the emptying of your stomach.
For people with narrow-angle glaucoma : Use this drug with caution if you have an eye disorder called narrow-angle glaucoma. If you have uncontrolled narrow-angle glaucoma, you should not use this medicine.
For people with liver problems : This drug is processed by your liver. If you have liver problems, more of the drug may stay in your body longer, putting you at risk for side effects.
Use this medicine with caution. Your doctor may reduce your dose and monitor your liver function during treatment.
For people with kidney problems : This drug is processed by the kidneys. If you have kidney problems, more of the drug may stay in your body longer, putting you at risk for side effects.
Use this medicine with caution. Your doctor may lower your dose and monitor your kidney function during treatment.
For people with an irregular heart rate : Use this drug with caution if you have QT interval prolongation (irregular heart rate).
Warnings for other groups
For pregnant women: This drug is a category C pregnancy drug. That means two things:
Research in animals has shown adverse effects to the fetus when the mother takes the drug.
Not enough human studies have been done to be sure how the drug might affect the fetus.
For women who are breastfeeding : It is not known if this drug passes into breast milk. Doing so can cause side effects in a child who is breastfed.
Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breast-feeding or to stop taking this medicine.
For children : The safety and efficacy of this medicine in children under 18 years of age have not been established.
How to take Vesicare
All possible dosages and forms may not be included here. Your dose, form, and how often you take it will depend on:
- The condition that is being treated.
- The severity of your condition.
- Other medical conditions you have.
The recommended dose of Vesicare is 5 mg once a day. If the 5 mg dose is well tolerated, the dose can be increased to 10 mg once a day. Vesicare should be taken with water and swallowed whole. E lVesicare can be taken with or without food.
For patients with severe renal impairment (CLcr <30 ml / min), a daily dose of Vesicare greater than 5 mg is not recommended.
For patients with moderate hepatic impairment (Child-Pugh B), a daily dose of Vesicare greater than 5 mg is not recommended. The use of Vesicare is not recommended in patients with severe hepatic impairment (Child-Pugh C).
When administered with strong CYP3A4 inhibitors such as ketoconazole, a daily dose of Vesicare greater than 5 mg is not recommended.
Typical dosage : 5 mg taken once a day.
Dose increase : if necessary, your doctor may increase your dose to 10 mg once a day.
Infant dose (ages 0-17 years). This medicine has not been studied in children. It should not be used in children under 18 years of age.
Before starting and during treatment with this medicine, your doctor may check your:
- Liver function
- Kidney function.
- Prior authorization.
Many insurance companies require a prior authorization for this drug.
Special dosing considerations
For people with kidney problems: If you have severe kidney disease, your dose should not be more than 5 mg per day.
For people with liver problems: If you have moderate liver disease, your dose should not be more than 5 mg per day. If you have severe liver disease, you should not use this drug.
Take as indicated
Solifenacin is used for long-term treatment. It comes with serious risks if you don’t take it as prescribed.
If you stop taking the medicine or don’t take it at all: Your overactive bladder symptoms likely won’t improve.
If you miss a dose or don’t take the medicine on time : Your medicine may not work as well or it may stop working altogether. For this medicine to work well, a certain amount must be in your body at all times.
If you take too much : you could have dangerous levels of the drug in your body. You may have the following symptoms:
- Blurry vision.
- Dilated pupils.
- Loss of consciousness.
If you think you have taken too much of this medicine, call your doctor or seek guidance from the American Association of Poison Control Centers.
What to do if you miss a dose : If you miss a dose of this medicine, skip that dose and take your next dose as scheduled for the next day. Do not take two doses of this medicine on the same day.
Storage : store solifenacin at room temperature. Keep it at 77 ° F (25 ° C). Keep this medicine away from high temperatures.
Always carry your medicine with you. When flying, never put it in a suitcase. Always carry the original prescription-labeled container with you.
Solifenacin is metabolized in the liver by the cytochrome P450 enzyme CYP3A4.
When administered concomitantly with drugs that inhibit CYP3A4, such as ketoconazole, the metabolism of solifenacin is impaired, leading to an increase in its concentration in the body and a reduction in its excretion.
As noted above, solifenacin can also prolong the QT interval. Therefore, administering it concomitantly with drugs that also have this effect, such as moxifloxacin or pimozide, may theoretically increase the risk of arrhythmia.
To help avoid interactions, your doctor should handle all of your medications with care.
Mechanism of action
Solifenacin is a competitive cholinergic receptor antagonist, selective for the M3 receptor subtype. The binding of acetylcholine to these receptors, particularly M3, plays a critical role in smooth muscle contraction.
By preventing the binding of acetylcholine to these receptors, solifenacin reduces smooth muscle tone in the bladder, allowing the bladder to retain large volumes of urine and reducing the number of urination, urgency, and incontinence episodes.
Due to a long elimination half-life, a once-daily dose can offer 24-hour control of smooth muscle tone in the urinary bladder.
Peak plasma concentrations are reached 3 to 8 hours after absorption from the intestine.
In the bloodstream, 98% of the substance is bound to plasma proteins, mainly acidic. Metabolism is mediated by the liver enzyme CYP3A4 and possibly others.
There is a known active metabolite, 4R-hydroxysolifenacin, and three inactive ones, the N-glucuronide, the N-oxide and the 4R-hydroxy-N-oxide.
The elimination half-life is 45 to 68 hours. 69% of the substance, both in its original form and in the form of metabolites, is excreted via the kidneys and 23% through the faeces.
Like other anticholinergics, solifenacin is an ester of a carboxylic acid containing (at least) one aromatic ring with an alcohol containing one nitrogen atom.
While in the prototype anticholinergic atropine the bicyclic ring is tropane, solifenacin replaces it with quinuclidine.
The free base is a yellow oil, while the solifenacin succinate salt forms yellowish crystals.
History of the Vesicare
The compound was studied using animal models by Yamanouchi Pharmaceutical Co., Ltd. of Tokyo, Japan. It was known as YM905 when it was in the studio in the early 2000s.
Society and culture
A 2006 cost-effectiveness study found that 5 mg of solifenacin had the lowest cost and highest efficacy among the anticholinergic medications used to treat overactive bladder in the United States, with an average medical cost per successfully treated patient of $ 6863 per year.
Our goal is to provide you with the most relevant and current information. However, since medications affect each person differently, we cannot guarantee that this list includes all possible dosages.
This information is not a substitute for medical advice. Always talk to your doctor or pharmacist about the correct dosages for you.