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Solifenacin

 
Drug Info: Solifenacin

Brand names: VESIcare®



Solifenacin Succinate Oral tablet

What is this medicine?

SOLIFENACIN (sol i FEN a cin) is used to treat overactive bladder. This medicine reduces the amount of bathroom visits. It may also help to control wetting accidents.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•difficulty passing urine
•glaucoma
•intestinal obstruction
•kidney disease
•liver disease
•an unusual or allergic reaction to solifenacin, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. This medicine can be taken with or without food. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, use it as soon as you can. If it is almost time for your next dose, use only that dose. Do not use double or extra doses.

What may interact with this medicine?

•atropine
•medicines for fungal infections, like fluconazole, itraconazole, ketoconazole or voriconazole
•oxybutynin
•scopolamine

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

It may take 2 or 3 months to notice the full benefit from this medicine.

You may need to limit your intake tea, coffee, caffeinated sodas, and alcohol. These drinks may make your symptoms worse.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.

This medicine may cause dry eyes and blurred vision. If you wear contact lenses, you may feel some discomfort. Lubricating drops may help. See your eye care professional if the problem does not go away or is severe.

Avoid extreme heat. This medicine can cause you to sweat less than normal. Your body temperature could increase to dangerous levels, which may lead to heat stroke.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•blurred vision or difficulty focusing vision
•breathing problems
•chest pain or palpitations
•confusion
•fast, irregular heartbeat
•feeling faint or lightheaded, falls
•severe dizziness
•trouble passing urine or change in the amount of urine
•unusually weak or tired

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•constipation
•headache
•indigestion or stomach upset
•nausea

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 11/30/2004 8:40:00 AM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Wikipedia: Solifenacin
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Solifenacin
Systematic (IUPAC) name
1-azabicyclo[2.2.2]oct-8-yl (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate
Identifiers
CAS number 242478-38-2
ATC code G04BD08
PubChem 443937
DrugBank APRD00168
Chemical data
Formula C23H26N2O2 
Mol. mass 362.465 g/mol
Pharmacokinetic data
Bioavailability 90%
Protein binding 98%
Metabolism Hepatic (CYP3A4-mediated)
Half life 45 to 68 hours
Excretion Renal (69.2%) and fecal (22.5%)
Therapeutic considerations
Licence data

US FDA:link

Pregnancy cat.

B3(AU) C(US)

Legal status

POM(UK) -only(US)

Routes Oral

Solifenacin (rINN), marketed as solifenacin succinate under the trade name Vesicare, is a urinary antispasmodic of the anticholinergic class. It is used in the treatment of overactive bladder with or without urge incontinence. It is marketed and manufactured by Astellas and GlaxoSmithKline.

Contents

Pharmacology

Mechanism of action

Solifenacin is a competitive muscarinic acetylcholine receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle. By preventing the binding of acetylcholine to these receptors, solifenacin reduces smooth muscle tone in the bladder, allowing the bladder to retain larger volumes of urine and reducing the number of micturition, urgency and incontinence episodes. Because of a long elimination half life, a once-a-day dose can offer 24 hour control of the urinary bladder smooth muscle tone.

Contraindications

Solifenacin should not be taken by people with a history of previous hypersensitivity to it, urinary retention, gastric retention, uncontrolled or poorly controlled closed-angle glaucoma, or severe liver disease (Child-Pugh class C). It is also contraindicated in long QT syndrome, as solifenacin,like tolterodine and darifenacin, binds to HERG channels and may prolong the QT interval.

Interactions

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. The manufacturer recommends that the dosage of solifenacin not exceed 5 mg a day if it is taken with a potent CYP3A4 inhibitor.

As stated above, solifenacin may also prolong the QT interval. Therefore, it should not be administered concomitantly with drugs which also have this effect, such as moxifloxacin or pimozide.

Side effects

The most common side effects of solifenacin are dry mouth, blurred vision, and constipation. As all anticholinergics, solifenacin may rarely cause heat prostration due to decreased perspiration.

Pharmacoeconomics

In a study of cost-effectiveness analysis, the average medical cost per overactive bladder patient with successful treatment is reported to be lowest for 5 mg solifenacin ($6863 per annum) among anticholinergic drugs to treat overactive bladder in the United States (Pharmacotherapy 2006, 26 1694-1702).


 
 

 

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