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FENOPAZ 5 MG

Quick Overview

Our aim is to reach out to the globe with in shortest possible time frame.

To promote this objective, not only we distribute and market our range of products globally through our distribution channels but we also undertake ‘contract manufacturing’& ‘formulation development ’of our wide range of generic products such as Fenopaz 5 which contains Solifenacin Succinate..... 5mg

FENOPAZ 5 MG

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Details

For the use only of a Registered medical practitioner, Hospital or Laboratory

FENOPAZ

 

COMPOSITION:

Fenopaz  5

Each film-coated tablet contains

Solifenacin Succinate                      5mg

Excipients                                        q.s.

Colours: Titanium Dioxide BP

 

CHEMISTRY: (3R)-1-Azabicyclo[2.2.2]oct-3-yl(1S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate compound with butanedioic acid (1:1).

CATEGORY: Muscarinic Antagonists, Urinary Antispasmodics.

 

PHARMACOLOGY

PHARMACODYNAMICS:

Solifenacin is a competitive muscarinic acetyl choline 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. 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 incontinence episodes.  

 

PHARMACOKINETICS:

Absorption

After oral administration of solifenacin succinate tablets peak plasma levels (Cmax) of solifenacin are reached within 3 to 8 hours after administration and at steady state ranged from 32.3 to 62.9 ng/mL for the 5 and 10 mg solifenacin succinate tablets, respectively.

The absolute bioavailability of solifenacin is approximately 90% and plasma concentrations of solifenacin are proportional to the dose administered.

 

Distribution

solifenacin is approximately 98% bound to human plasma proteins. Solifenacin is highly distributed to non-CNS tissues.

 

Metabolism

Solifenacin is extensively metabolized in the liver. The primary pathway for elimination is by way of CYP3A4; however, alternate metabolic pathways exist, that can contribute to the metabolism of solifenacin

 

Excretion

Less than 15% of the dose was reported to be recovered in the urine as intact solifenacin. The elimination half-life of solifenacin following chronic dosing is approximately 45-68 hours.

 

INDICATIONS:

Solifenacin succinate tablets is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and urinary frequency.

 

DOSAGE AND ADMINISTRATION:

The recommended dose of solifenacin succinate tablets is 5 mg once daily. If the 5 mg dose is well tolerated, the dose may be increased to 10 mg once daily. Solifenacin succinate tablets should be taken with water and swallowed whole. Solifenacin succinate tablets can be administered with or without food.

 

Dose Adjustment in Patients with Renal Impairment

For patients with severe renal impairment, a daily dose of solifenacin succinate tablets greater than 5 mg is not recommended.

 

Dose Adjustment in Patients with Hepatic Impairment

For patients with moderate hepatic impairment, a daily dose of solifenacin succinate tablets greater than 5 mg is not recommended. Use of solifenacin succinate tablets in patients with severe hepatic impairment is not recommended.

 

Dose Adjustment in Patients Taking CYP3A4 Inhibitors

When administered with potent CYP3A4 inhibitors such as ketoconazole, a daily dose of solifenacin succinate tablets greater than 5 mg is not recommended.

 

CONTRAINDICATIONS:

Solifenacin Succinate Tablets is contraindicated in patients with:

•  Urinary retention (see Warnings and Precautions).

•  Gastric retention (see Warnings and Precautions).

• Uncontrolled narrow-angle glaucoma (see Warnings and          Precautions).

• In patients who have demonstrated hypersensitivity to the      drug  (see Adverse Reactions).

 

WARNINGS AND PRECAUTIONS:

Angioedema and Anaphylactic Reactions

Angioedema of the face, lips, tongue and/or larynx have been reported with solifenacin. In some cases angioedema occurred after the first dose or after multiple doses. Angioedema associated with upper airway swelling may be life threatening. If involvement of the tongue, hypopharynx or larynx occurs, solifenacin should be promptly discontinued and appropriate therapy and/or measures should be taken.

Anaphylactic reactions have been reported rarely in patients treated with solifenacin succinate. In patients who develop anaphylactic reactions, solifenacin succinate should be discontinued and appropriate therapy and/or measures should be taken.

 

Urinary Retention

Solifenacin succinate tablets, like other anticholinergic drugs, should be administered with caution to patients with clinically significant bladder outflow obstruction because of the risk of urinary retention.

 

Gastrointestinal Disorders

Solifenacin succinate tablets, like other anticholinergics, should be used with caution in patients with decreased gastrointestinal motility.

 

Controlled Narrow-Angle Glaucoma

Solifenacin succinate tablets should be used with caution in patients being treated for narrow-angle glaucoma.

 

Hepatic Impairment

Solifenacin succinate tablets should be used with caution in patients with hepatic impairment. Doses of solifenacin succinate tablets greater than 5 mg are not recommended in patients with moderate hepatic impairment. Solifenacin Succinate Tablets is not recommended for patients with severe hepatic impairment.

 

Renal Impairment

Solifenacin Succinate Tablets should be used with caution in patients with renal impairment. Doses of solifenacin succinate tablets greater than 5 mg are not recommended in patients with severe renal impairment.

 

Patients with Congenital or Acquired QT Prolongation

Solifenacin succinate tablets should be used with caution for patients with a known history of QT prolongation or patients who are taking medications known to prolong the QT interval.

 

INTERACTIONS:

Potent CYP3A4 Inhibitors

Following the administration of 10 mg of solifenacin succinate tablets in the presence of 400 mg of ketoconazole, a potent inhibitor of CYP3A4, the mean Cmax and AUC of solifenacin was reported to be increased by 1.5 and 2.7-fold, respectively. Therefore, it is recommended not to exceed a 5 mg daily dose of solifenacin succinate tablets when administered with therapeutic doses of ketoconazole or other potent CYP3A4 inhibitors. The effects of weak or moderate CYP3A4 inhibitors were not examined.

 

CYP3A4 Inducers

Some of the reported drug metabolism studies have shown that solifenacin is a substrate of CYP3A4. Therefore, inducers of CYP3A4 may decrease the concentration of solifenacin.

Drugs Metabolized by Cytochrome P450

At therapeutic concentrations, solifenacin does not inhibit CYP1A1/2, 2C9, 2C19, 2D6 or 3A4 derived from human liver microsomes.

 

Warfarin

Solifenacin has no significant effect on the pharmacokinetics of R-warfarin or S-warfarin.

 

Oral Contraceptives

In the presence of solifenacin there are no significant changes in the plasma concentrations of combined oral contraceptives (Ethinyl estradiol/levonorgestrel).

Digoxin

Solifenacin had no significant effect on the pharmacokinetics of digoxin.

 

PREGNANCY AND LACTATION:

Pregnancy

Pregnancy Category C

There are no adequate and well-controlled studies reported in pregnant women.

Nursing Mothers

It is not known whether solifenacin is excreted in human milk. Because many drugs are excreted in human milk, Solifenacin Succinate Tablets should not be administered during nursing.

 

Effect to Drive & Use the Machine:

Since solifenacin, like other anticholinergics may cause blurred vision and uncommonly, somnolence and fatigue, the ability to drive and use machines may be negatively affected.

 

USE IN SPECIFIC POPULATIONS

Labor and Delivery

The effect of solifenacin succinate tablets on labor and delivery in humans has not been studied.

 

Pediatric Use

The safety and effectiveness of solifenacin succinate tablets in pediatric patients have not been established.

 

Geriatric Use

Similar safety and effectiveness are reported between older and younger patients treated with Solifenacin Succinate Tablets.

 

ADVERSE DRUG REACTIONS:

Expected adverse reactions of antimuscarinic agents are dry mouth, constipation, blurred vision (accommodation abnormalities), urinary retention and dry eyes. The incidence of dry mouth and constipation in patients treated with solifenacin succinate tablets was reported to be higher in the 10 mg compared to the 5 mg dose.

Severe fecal impaction, colonic obstruction and intestinal obstruction were reported all in the Solifenacin succinate tablets 10 mg dose, angioneurotic edema has been reported taking Solifenacin succinate tablets 5 mg dose.

 

OVERDOSAGE:

Overdosage with solifenacin succinate tablets can potentially result in severe anticholinergic effects and should be treated accordingly. The highest dose ingested in an accidental overdose of solifenacin succinate was 280 mg in a 5-hour period was reported to be associated with mental status changes.

Some cases reported a decrease in the level of consciousness. Intolerable anticholinergic side effects (fixed and dilated pupils, blurred vision, failure of heel-to-toe exam, tremors and dry skin) reported with 50 mg daily (5 times the maximum recommended therapeutic dose) and resolved within 7 days following discontinuation of drug.

 

In the event of overdose with Solifenacin Succinate Tablets, treat with gastric lavage and appropriate supportive measures. ECG monitoring is also recommended.

 

PRESENTATION: Blister of 10 Tablets

STORAGE: Store in a dry place below 30°C.

Keep out of reach of children.

LAST UPDATE: February 2014.