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Vesikur

Vesikur - General Information

Vesikur (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 urge incontinence. [Wikipedia]

 

Pharmacology of Vesikur

Vesikur 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 and stimulation of salivary secretion.

 

Vesikur for patients

What is Vesicare?

Vesicare is a prescription medicine used in adults to treat the following symptoms due to a condition called overactive bladder:

  • Having to go to the bathroom too often, also called "urinary frequency"
  • Having a strong need to go to the bathroom right away, also called "urgency"
  • Leaking or wetting accidents, also called "urinary incontinence."

Vesicare has not been studied in children.

Who Should Not Use Vesicare?

Do not take Vesicare if you:

  • are not able to empty your bladder (also called "urinary retention")
  • have delayed or slow emptying of your stomach (also called "gastric retention")
  • have an eye problem called "uncontrolled narrow-angle glaucoma"
  • are allergic to Vesicare or any of its ingredients.

What are The Risks?

The most common side effects with Vesicare are:

  • Blurred vision. Use caution while driving or doing dangerous activities until you know how Vesicare affects you.
  • Dry mouth
  • Constipation. Call your doctor if you get severe stomach area (abdominal) pain or become constipated for 3 or more days.
  • Heat prostration due to decreased sweating can occur when drugs such as Vesicare are used in a hot environment.

What Should I Tell My Health Care Professional?

Before you start using Vesicare, tell your health care professional if you:

  • have any stomach or intestinal problems or problems with constipation
  • have trouble emptying your bladder or you have a weak urine stream
  • have an eye problem called narrow angle glaucoma
  • have liver problems
  • have kidney problems
  • are pregnant or trying to become pregnant, or are breastfeeding

Are There Any Interactions With Drugs or Foods?

Vesicare can interact with other medicines. Know the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Keep a list of them to show your health care professional and pharmacist.

How Do I Take Vesicare?

  • Take Vesicare exactly as prescribed. Your doctor may prescribe the lowest dose if you have certain medical conditions such as liver or kidney problems.
  • You should take one Vesicare tablet once a day.
  • You should take Vesicare with liquid and swallow the tablet whole.
  • You can take Vesicare with or without food.

Vesicare FDA Approved 11/2004
Patient Information Sheet Revised 05/2005

 

Vesikur Interactions

Do not exceed a 5 mg daily dose of VESIcare when administered with therapeutic doses of ketoconazole or other potent CYP3A4 inhibitors.

Patients with Congenital or Acquired QT Prolongation

In a study of the effect of solifenacin on the QT interval in 76 healthy women, the QT prolonging effect appeared less with solifenacin 10 mg than with 30 mg (three times the maximum recommended dose), and the effect of solifenacin 30 mg did not appear as large as that of the positive control moxifloxacin at its therapeutic dose. This observation should be considered in clinical decisions to prescribe VESIcare for patients with a known history of QT prolongation or patients who are taking medications known to prolong the QT interval.

 

Vesikur Contraindications

VESIcare is contraindicated in patients with urinary retention, gastric retention, uncontrolled narrow-angle glaucoma, and in patients who have demonstrated hypersensitivity to the drug substance or other components of the product.

 

Additional information about Vesikur

Vesikur Indication: For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency.
Mechanism Of Action: Vesikur 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Solifenacin
Synonyms: solifenacin succinate
Drug Category: Muscarinic Antagonists; Antispasmodics; Anti-Incontinence Agents
Drug Type: Small Molecule; Approved

Other Brand Names containing Solifenacin: Vesicare; Vesikur;
Absorption: The absolute bioavailability of solifenacin is approximately 90%, and plasma concentrations of solifenacin are proportional to the dose administered.
Toxicity (Overdose): Overdosage with solifenacin can potentially result in severe anticholinergic effects and should be treated accordingly. The highest solifenacin dose given to human volunteers was a single 100 mg dose. Intolerable anticholinergic side effects (fixed and dilated pupils, blurred vision, failure of heel-to-toe exam, tremors and dry skin) occurred on day 3 in normal volunteers taking 50 mg daily (5 times the maximum recommended therapeutic dose).
Protein Binding: Solifenacin is approximately 98% (in vivo) bound to human plasma proteins, principally to alpha1-acid glycoprotein.
Biotransformation: Solifenacin is extensively metabolized in the liver. The primary pathway for elimination is by way of CYP3A4; however, alternate metabolic pathways exist. The primary metabolic routes of solifenacin are through N-oxidation of the quinuclidin ring and 4R-hydroxylation of tetrahydroisoquinoline ring. One pharmacologically active metabolite (4R-hydroxy solifenacin), occurring at low concentrations and unlikely to contribute significantly to clinical activity, and three pharmacologically inactive metabolites (N-glucuronide and the N-oxide and 4R-hydroxy-N-oxide of solifenacin) have been found in human plasma after oral dosing.
Half Life: The elimination half-life of solifenacin following chronic dosing is approximately 45-68 hours.
Dosage Forms of Vesikur: Tablet Oral
Chemical IUPAC Name: [(8R)-1-azabicyclo[2.2.2]octan-8-yl] (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate; butanedioic acid
Chemical Formula: C27H32N2O6
Solifenacin on Wikipedia: https://en.wikipedia.org/wiki/Solifenacin
Organisms Affected: Humans and other mammals