英文药名: Toviaz(Fesoterodine Fumarate Tablets)

中文药名: 富马酸非索罗定缓释片

生产厂家: Pfizer Inc.

药品介绍

辉瑞（Pfizer）公司宣布美国FDA批准Toviaz（fesoterodine fumarate）缓释片治疗膀胱过度活动症（OAB）。Fesoterodine是选择性毒蕈碱M3受体拮抗剂，每日一次Toviaz（4mg/8mg）可以显著的减少患者急迫性尿失禁次数和排尿次数，明显改善患者生活质量。
本品获得批准是基于两项为期12周纳入1964例OAB患者的III期临床研究。研究结果显示，多达88%的本品8mg组患者急迫性尿失禁减少，安慰剂组为50%。本品8mg组每日排尿次数减少19%，安慰剂组为11%。用本品治疗早在第2周可见尿湿减少，且在 12周内维持。
临床研究中，最常见的不良反应为口干(发生率：安慰剂组7%；本品4mg组19%；本品8mg组35%)，多数为轻至中度，因口干的停药率不到1%。便秘的发生率较低(发生率：安慰剂组2%；本品4mg组4%；本品8mg组6%)。在长达3年的公开标签研究中，不良反应与先前研究中的相似。

规格：
4mg 84 片
   
8mg 84 片

TOVIAZ

Generic Name for TOVIAZ

Fesoterodine fumarate 4mg, 8mg; ext-rel tabs.

Legal Classification:

Rx

Pharmacological Class for TOVIAZ

Muscarinic receptor antagonist.

Manufacturer of TOVIAZ

Pfizer Labs

Indications for TOVIAZ

Overactive bladder (OAB) with urge urinary incontinence, urgency, and frequency.

Adult dose for TOVIAZ

Swallow whole. 4mg once daily; max 8mg once daily. Severe renal insufficiency (CrCl<30mL/min) or concomitant potent CYP3A4 inhibitors: max 4mg/day.

Children's dosing for TOVIAZ

Not recommended.

Contraindications for TOVIAZ

Urinary or gastric retention. Uncontrolled narrow angle glaucoma.

Warnings/Precautions for TOVIAZ

Severe hepatic impairment: not recommended. Bladder outlet obstruction. Controlled narrow angle glaucoma. Hepatic or renal dysfunction. Myasthenia gravis. Decreased gastric motility. Exposure to high environmental temperatures. Pregnancy (Cat.C). Nursing mothers.

Interactions for TOVIAZ

Increased levels with CYP3A4 inhibitors (eg, erythromycin). CNS depression with alcohol, other CNS depressants.

Adverse Reactions for TOVIAZ

Dry mouth, constipation, urinary retention/UTI, blurred vision, dry eyes, back pain, insomnia, dyspepsia.

How is TOVIAZ supplied?

Tabs—30, 90

Related Disease:

Overactive bladder

Pfizer Inc’s Toviaz (fesoterodine fumarate)
On October 31, 2008, the FDA approved the use of Toviaz (fesoterodine fumarate), a once-daily, extended-release tablet that has been clinically proven to reduce urinary urge, frequency, and incontinence in individuals experiencing symptoms of overactive bladder.1 The recommended starting dose for Toviaz is 4 mg, but may be increased to 8 mg, depending on the individual. Toviaz has only been approved for adults and has not yet been approved for pediatric use.1

Pharmacology and Pharmacokinetics
Toviaz is a competitive muscarinic receptor antagonist. Muscarinic receptors cause contractions of urinary bladder smooth muscle and also stimulate saliva secretion. After oral administration, Toviaz is rapidly hydrolyzed by nonspecific esterases to its active metabolite 5-hydroxymethyl tolterodine, which exhibits antimuscarinic effects. Toviaz is well-absorbed when taken orally, and food does not affect its absorption. Toviaz has low plasma protein binding, is primarily metabolized by the liver, and is excreted via the kidneys.2

Clinical Trials
A randomized, double-blind, placebocontrolled, multicenter trial was performed to determine the safety, efficacy, and tolerability of Toviaz. In the trial, 836 subjects with urinary frequency, urinary urgency, or urge urinary incontinence were randomized to placebo (n = 274), 4 mg fesoterodine (n = 283), or 8 mg fesoterodine (n = 279) once daily for 12 weeks.

The primary efficacy end point was the change in the number of micturitions per 24 hours. Coprimary end points were the change in the number of urge urinary incontinence episodes per 24 hours and the treatment response. Secondary efficacy end points were the change in mean voided volume per micturition and the number of continent days and urgency episodes per 24 hours. Tolerability and safety were assessed by evaluating adverse events, electrocardiograms, postvoid residual urine volume, laboratory parameters, and treatment withdrawals.

Treatment with 4- or 8-mg fesoterodine resulted in statistically significant improvements from baseline to end of treatment for the primary and coprimary end points compared with placebo (P <.05).

Results for most secondary end points, including mean voided volume per micturition, number of continent days, and number of urgency episodes per 24 hours, were also significantly improved versus placebo. The adverse events reported more frequently with fesoterodine than with placebo were dry mouth, constipation, and urinary tract infection.3

Precautions
In patients with mild or moderate renal insufficiency, no dose adjustment is needed. In patients with severe renal insufficiency, doses of Toviaz greater than 4 mg are not recommended.2

No dose adjustments are necessary with mild-to-moderate hepatic dysfunction. Patients with severe hepatic dysfunction should not take Toviaz, whereas it has not been studied in this patient population.

The most common side effects observed with Toviaz include dry mouth and constipation. The incidence of dry mouth was higher in patients receiving Toviaz 8 mg/day (35%) and those receiving 4 mg/day (19%), compared with those receiving placebo (7%). The incidence of constipation was lower in those patients receiving placebo (2%), compared with 4% of those taking Toviaz 4 mg/day and 6% of those taking 8 mg/day.2