Везикар

Везикар Uses, Dosage, Side Effects, Food Interaction and all others data.

Везикар 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 incontinence episodes.

Везикар antagonizes the M2 and M3 muscarinic receptors in the bladder to treat an overactive bladder. It has a long duration of action as it is usually taken once daily. Patients taking solifenacin should be aware of the risks of angioedema and anaphylaxis.

Trade Name Везикар
Availability Prescription only
Generic Solifenacin
Solifenacin Other Names Solifenacin, Solifenacina
Related Drugs oxybutynin, Myrbetriq, tolterodine, mirabegron, Ditropan, Detrol, Botox, VESIcare, trospium, Gemtesa
Type
Formula C23H26N2O2
Weight Average: 362.473
Monoisotopic: 362.199428085
Protein binding

Solifenacin is 93-96% protein bound in plasma, mainly to alpha-1-acid glycoprotein.

Groups Approved
Therapeutic Class Anticholinergics (antimuscarinics)/ Anti-spasmodics, BPH/ Urinary retention/ Urinary incontinence
Manufacturer
Available Country Russia
Last Updated: September 19, 2023 at 7:00 am
Везикар
Везикар

Uses

Symptomatic treatment of urge incontinence and/or increased urinary frequency and urgency as may occur in patients with overactive bladder syndrome.

Везикар is also used to associated treatment for these conditions: Benign Prostatic Hyperplasia (BPH), Urinary Bladder, Overactive

How Везикар works

Везикар is a competitive muscarinic receptor antagonist. It has the highest affinity for M3, M1, and M2 muscarinic receptors. 80% of the muscarinic receptors in the bladder are M2, while 20% are M3. Везикар's antagonism of the M3 receptor prevents contraction of the detrusor muscle, while antagonism of the M2 receptor may prevent contraction of smooth muscle in the bladder.

Dosage

Везикар dosage

Adults, including the elderly: The recommended dose is Везикар Succinate 5 mg once daily. If needed, the dose may be increased to Везикар Succinate 10 mg once daily.

Children and adolescents: Safety and effectiveness in children have not yet been established. Therefore, Везикар Succinate should not be used in children.

Side Effects

The most common side effects are blurred vision, dry mouth, constipation & heat prostration. Other side effects include dizziness, fatigue, edema, palpitation and skin reactions. Disorientation, hallucination and convulsion may occur.

Toxicity

The LD50 of Везикар has yet to be determined.

Signs of overdose include severe anticholinergic effects, mental status changes, and decreased consciousness. In case of overdose, treat patients with gastric lavage and supportive measures. Monitor patients with an ECG.

Precaution

Other causes of frequent urination (heart failure or renal disease) should be assessed before treatment with Везикар. If urinary tract infection is present, an appropriate antibacterial therapy should be started. Везикар Succinate should be used with caution in patients with clinically significant bladder outflow obstruction at risk of urinary retention, gastrointestinal obstructive disorders, risk of decreased gastrointestinal motility, severe renal impairment (creatinine clearance 30 ml/min), moderate hepatic impairment, concomitant use of a strong CYP3A4 inhibitor, e.g. ketoconazole

Interaction

Concomitant medication with other drugs with anticholinergic properties may result in more pronounced therapeutic effects and side effects. The therapeutic effect of solifenacin may be reduced by concomitant administration of cholinergic receptor agonists. Везикар can reduce the effect of drugs that stimulate the motility of the gastro-intestinal tract, such as metoclopramide and cisapride. Ketoconazole & other CYP3A4 inhibitors increase the plasma concentration of solifenacin.

Food Interaction

  • Take with or without food.

Volume of Distribution

The volume of distribution of solifenacin is 600L.

Elimination Route

Везикар is well absorbed in the duodenum, jejunum, and ileum but not the stomach. Absorption occurs via passive diffusion and so no transporters are involved. The mean oral bioavailability of solifenacin is 88%. The Tmax of solifenacin is 3-8 hours with a Css of 32.3ng/mL for a 5mg oral dose and 62.9ng/mL for a 10mg oral dose.

Half Life

The elimination half life of solifenacin ranges from 33-85 hours.

Clearance

The clearance of solifenacin is 7-14L/h and a renal clearance of 0.67-1.51L/h.

Elimination Route

69.2±7.8% of a radiolabelled dose is recovered in the urine, 22.5±3.3% was recovered in feces, and 0.4±7.8% was recovered in exhaled air. 18% of solifenacin is eliminated as the N-oxide metabolite, 9% is eliminated as the 4R-hydroxy N-oxide metabolite, and 8% is eliminated as the 4R-hydroxy metabolite.

Pregnancy & Breastfeeding use

Use in pregnancy: There are no adequate data from the use of solifenacin succinate in pregnant women. Caution should be exercised while prescribing solifenacin to pregnant women.

Use in lactating mother: No data concerning the excretion of solifenacin into breast milk are available. The use of Везикар is avoided in lactating mother.

Contraindication

Везикар is contraindicated in patients with hypersensitivity to solifenacin or to any of the excipients. It is also contraindicated in myasthenia gravis, urinary retention, uncontrolled narrow angle glaucoma, severe gastro-intestinal condition (including toxic megacolon), patients undergoing haemodialysis, patients with severe hepatic impairment, patients with severe renal impairment or moderate hepatic impairment and on treatment with a strong CYP3A4 inhibitor, e.g. ketoconazole.

Special Warning

Patients with renal impairment: No dosage adjustment is necessary for patients with mild to moderate renal impairment (creatinine clearance > 30 ml/min). Patients with severe renal impairment (creatinine clearance 30 ml/min) should be treated with caution and receive no more than 5 mg Везикар SuccinateTablet once daily.

Patients with hepatic impairment: No dosage adjustment is necessary for patients with mild hepatic impairment. Patients with moderate hepatic impairment should be treated with caution and receive no more than 5 mg Везикар SuccinateTablet once daily.

Patients taking CYP3A4 inhibitors concomitantly: The maximum dose of Везикар Succinateshould be limited to 5 mg when treated simultaneously with ketoconazole or other potent CYP3A4 inhibitors e.g. ritonavir, nelfinavir or itraconazole.

Use in children: Safety and efficacy of solifenacin in children have not been established.

Innovators Monograph

You find simplified version here Везикар

Везикар contains Solifenacin see full prescribing information from innovator Везикар Monograph, Везикар MSDS, Везикар FDA label

FAQ

What is Везикар used for?

Везикар used to treat symptoms of an overactive bladder.

How safe is Везикар?

Taking 1 extra dose of Везикар is unlikely to harm you. However, you may get more side effects, such as a dry mouth or headache. The amount of Везикар that can lead to an overdose varies from person to person, and too much Везикар can be dangerous.

How does Везикар work?

Везикар works by relaxing the muscle that is found in the wall of the bladder. This helps to increase the volume of pee your bladder can hold and control the release of pee.

What are the common side effects of Везикар?

Common side effects of Везикар are include:

  • dry mouth
  • constipation
  • stomach pain
  • upset stomach
  • vomiting
  • heartburn
  • dry eyes
  • blurred vision
  • dry skin

Is Везикар safe during pregnancy?

 Везикар should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby.

Is Везикар safe during breastfeeding?

There is no published experience with Везикар during breastfeeding.

Can I drink alcohol with Везикар?

Limit drinking alcohol while your are taking Везикар. Alcohol can increase the risk of side effects.

Can I drive after taking Везикар?

You should know that Везикар may make you dizzy or drowsy or cause blurred vision. Do not drive a car or operate machinery until you know how this medication affects you.

When is the best time to take Везикар?

Try to take the tablet at the same time of day each day, as this will help you to remember to take your doses regularly. You can take Везикар either before or after meals.

How long does it take for Везикар to start working?

Most people start to notice improvement in symptoms about 4 weeks after starting Везикар. It can take up to 12 weeks to see the full effects.

Should Везикар be taken at night?

Night time dosing with Везикар would more effectively improve night time symptoms such as nocturia.

Does Везикар work immediately?

You will usually take this medicine long term to help keep your symptoms under control.Везикар starts to work within 3 to 8 hours, but it can take up to 4 weeks to reach its full effect.

How long does Везикар stay in my system?

Везикар has 90% bioavailability and a long half-life of 45–68 hours.

What happens if I stop taking Везикар?

If you stop taking the drug or don't take it at all symptoms will likely not improve.

Does Везикар lower blood pressure?

Therapeutically effective doses of Везикар did not increase heart rate or blood pressure.

Does Везикар cause constipation?

Везикар may cause constipation. Call your doctor if you get severe stomach pain or become constipated for 3 or more days. This medicine may cause dry mouth.

Can Везикар cause dementia?

Везикар can causes denimia also with other side effects.

Who should not take Везикар?

It shouldn't be used in children younger than 18 years.
You should not use Везикар if you have untreated or uncontrolled narrow-angle glaucoma, a blockage in your digestive tract, or if you are unable to urinate.

What happens if I miss a dose?

Skip the missed dose and use your next dose at the regular time. Do not take 2 doses on the same day.
Oral suspension: Take Везикар as soon as you can, but skip the missed dose if you are more than 12 hours late for the dose. Do not take two doses at one time.

*** Taking medicines without doctor's advice can cause long-term problems.
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