Indication |
For symptomatic relief of dysuria, urgency, nocturia, suprapubic
pain, frequency and incontinence as may occur in cystitis, prostatitis,
urethritis, urethrocystitis/urethrotrigonitis. |
Pharmacodynamics |
Flavoxate is a spasmolytic flavone derivative that acts by
relaxing the smooth muscle in the urinary tract. Flavoxate is a
competitive muscarinic receptor antagonist indicated for the treatment
of overactive bladder with symptoms of urge urinary incontinence,
urgency, and urinary frequency. Muscarinic receptors play an important
role in several major cholin-ergically mediated functions, including
contractions of urinary bladder smooth muscle and stimulation of
salivary secretion. |
Mechanism of action |
Flavoxate acts as a direct antagonist at muscarinic acetylcholine
receptors in cholinergically innervated organs. Its
anticholinergic-parasympatholytic action reduces the tonus of smooth
muscle in the bladder, effectively reducing the number of required
voids, urge incontinence episodes, urge severity and improving
retention, facilitating increased volume per void. |
Absorption |
Well absorbed from gastrointestinal tract. |
Volume of distribution |
Not Available |
Protein binding |
Not Available |
Metabolism |
Not Available |
Route of elimination |
57% of the flavoxate HCl was excreted in the urine within 24 hours. |
Half life |
Not Available |
Clearance |
Not Available |
Toxicity |
The oral LD50 for flavoxate HCl in rats is 4273 mg/kg. The oral
LD50 for flavoxate HCl in mice is 1837 mg/kg. Symptoms of overdose
include convulsions, decreased ability to sweat, (warm, red skin, dry
mouth, and increased body temperature), hallucinations, increased heart
rate and blood pressure, and mental confusion. |