Fesoterodina
Fesoterodina Uses, Dosage, Side Effects, Food Interaction and all others data.
Fesoterodina 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 | Fesoterodina |
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 | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Fesoterodina 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).
Fesoterodina is also used to associated treatment for these conditions: Urinary Bladder, Overactive
How Fesoterodina works
Fesoterodina, 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. 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.
MANAGEMENT: Caution is advised if fesoterodine is administered with grapefruit or grapefruit juice.
Fesoterodina 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
Fesoterodina 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
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