Toviaz LP Uses, Dosage, Side Effects and more

Toviaz LP is an antimuscarinic prodrug for the treatment of overactive bladder syndrome.

In-vivo the fesoteridine prodrug is broken down into its active metabolite, 5-hydroxymethyl tolterodine (5-HMT), by plasma esterases. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. Therefore, acting as a competitive muscarinic receptor antagonist, fesoterodine ultimately acts to decrease the detrusor pressure by its muscarinic antagonism, thereby decreasing bladder contraction and consequently, the urge to urinate.

Trade Name	Toviaz LP
Availability	Prescription only
Generic	Fesoterodine
Fesoterodine Other Names	FESO, Fesoterodina, Fesoterodine
Related Drugs	oxybutynin, Myrbetriq, solifenacin, tolterodine, mirabegron, Ditropan, Detrol, VESIcare
Type
Formula	C₂₆H₃₇NO₃
Weight	Average: 411.5769 Monoisotopic: 411.277344055
Protein binding	5-HMT: 50% to albumin and alpha1-acid glycoprotein
Groups	Approved
Therapeutic Class
Manufacturer
Available Country	France
Last Updated:	January 7, 2025 at 1:49 am

Uses

Toviaz LP is an antimuscarinic agent used in the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.

For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).

Toviaz LP is also used to associated treatment for these conditions: Urinary Bladder, Overactive

How Toviaz LP works

Toviaz LP, once converted to its active metabolite, 5-hydroxymethyltolterodine, acts as a competitive antagonists at muscarinic receptors. This results in the inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.

Toxicity

Rat, Oral, LD50: ~ 681 mg/kg Mouse, Oral, LD50: ~ 316 mg/kg Rat, Intravenous, NOAEL: 10 mg/kg Mouse, Intravenous, NOAEL: 10 mg/kg

Food Interaction

Take with or without food.

[Moderate] MONITOR: Coadministration with moderate inhibitors of CYP450 3A4 such as grapefruit juice may increase the plasma concentrations of fesoterodine's active metabolite, 5-hydroxymethyl tolterodine, which is partially metabolized by the isoenzyme.

The possibility of prolonged and

Because 5-hydroxymethyl tolterodine is also metabolized by CYP450 2D6, the clinical significance of the interaction may be greater in patients who are CYP450 2D6-deficient, or so-called poor metabolizers of CYP450 2D6 (approximately 7% of Caucasians and less than 2% of Asians and individuals of African descent) who may rely more on the 3A4 metabolic pathway for clearance of the drug.

MANAGEMENT: Caution is advised if fesoterodine is administered with grapefruit or grapefruit juice.

Patients should be advised to notify their physician if they experience potential adverse effects of fesoterodine such as irregular heartbeat, blurry vision, difficulty urinating, dry mouth, headache, drowsiness, dizziness, gastrointestinal upset, or constipation.

Toviaz LP Drug Interaction

Moderate: tolterodine, fentanylMinor: modafinilUnknown: calcium / vitamin d, multivitamin with minerals, heparin, potassium chloride, lithium, loteprednol ophthalmic, pregabalin, metoprolol, metoprolol, pramipexole, acetaminophen, vitamin a topical, bioflavonoids, sotalol, cyanocobalamin, ascorbic acid, cholecalciferol

Toviaz LP Disease Interaction

Major: GI retention, narrow-angle glaucoma, urinary retentionModerate: hepatic dysfunction, myasthenia gravis, renal dysfunction

Volume of Distribution

IV, 5-HMT: 169 L

Elimination Route

Tmax (5-HMT): 5 hours post-adminitration of fesoterodine. AUC (0,∞)= 49.5 ng·h/ ml
Bioavailability, 5-HMT = 52%

Half Life

7-8 hours for the active metabolite 5-hydroxymethyl tolterodine

Clearance

5-HMT, healthy subjects: 14.4 L/h 5-HMT is also secreted into the nephron.

Elimination Route

Renal: 70% of fesoterodine was recovered in urine as 5-HMT; 35% carboxy metabolite; 18% carboxy-N-desisopropylmetabolite, and 1% N-desisopropyl metabolite Fecal: 7% Hepatic: fesoterodine elimination via CYP2D6 and CYP3A4