Flavoxate 100mg Film-Coated Tablets

Flavoxate 100mg Film-Coated Tablets

FLAVOXATE
(flavoxate hydrochloride), 100mg Film Coated Tablet (Taj Pharma)

DESCRIPTION

FLAVOXATE® (flavoxate HC1) tablets contain flavoxate hydrochloride, a synthetic urinary tract spasmolytic.

Chemically, flavoxate hydrochloride is 2-piperidinoethyl 3-methyl-4-oxo-2-phenyl-4H-1-benzopyran-8-carboxylate hydrochloride. The empirical formula of flavoxate hydrochloride is C24H25NO4• HCl. The molecular weight is 427.94

FLAVOXATE® is supplied in tablets for oral administration. Each round, white, film-coated FLAVOXATE® tablet is debossed with the product name FLAVOXATE® and contains flavoxate hydrochloride, 100 mg. Inactive ingredients consist of calcium phosphate, hypromellose, magnesium stearate, polyethylene glycol, starch and talc.

CLINICAL PHARMACOLOGY

Flavoxate hydrochloride counteracts smooth muscle spasm of the urinary tract and exerts its effect directly on the muscle.

In a single study of 11 normal male subjects, the time to onset of action was 55 minutes. The peak effect was observed at 112 minutes.

57% of the flavoxate HC1 was excreted in the urine within 24 hours.

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.

PHARMACOKINETIC PROPERTIES

Oral studies in man have indicated that flavoxate is readily absorbed from the intestine and converted, to a large extent, almost immediately to MFCA.

Following an IV dose (equimolar to 100 mg), the following parameters were calculated for flavoxate: T½ 83.3 mins: apparent volume of distribution 2.89 l/kg. The apparent distribution of MFCA was 0.20 l/kg. No free flavoxate was found in urine (24 hours). However, 47% of the dose was excreted as MFCA.

Following single oral dosing to volunteers of 200 mg and 400 mg flavoxate, almost no free flavoxate was detected in the plasma. The peak level of MFCA was attained at 30-60 mins after the 200 mg dose and at around two hours following the 400 mg dose. The AUC for the 400 mg dose was approximately twice as large as the AUC for the 200 mg dose. About 50% of the dose was excreted as MFCA within 12 hours; most being excreted within the first 6 hours.

After repeated oral dosing (200 mg, TDS, 7 days) the cumulative excretion of metabolites stabilised at 60% of the dose on the third day remaining almost unchanged after one week.

SPECIAL POPULATION

Flavoxate and Pregnancy

Caution when used during pregnancy.

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Flavoxate and Lactation

It is unknown whether flavoxate (metabolites) is excreted in human milk. A risk to the suckling child cannot be excluded. Flavoxate should not be used during breast-feeding. Caution when used during lactation

Flavoxate and Children

Safety and efficacy in children younger than 12 years of age not established.

Flavoxate and Geriatic

Information Not Available

INDICATION
For symptomatic relief of dysuria, urgency, nocturia, suprapubic pain, frequency and incontinence as may occur in cystitis, prostatitis, urethritis, urethrocystitis/urethrotrigonitis

DOSAGE AND ADMINISTRATION

Adults and children over 12 years of age

One or two 100 mg tablets 3 or 4 times a day. With improvement of symptoms, the dose may be reduced. This drug cannot be recommended for infants and children under 12 years of age because safety and efficacy have not been demonstrated in this age group.

Urinary incontinence, urgency and frequency, Bladder spasms due to catheterisation, Dysuria
Adult: Usual dose: 200 mg tid.

CONTRAINDICATIONS

FLAVOXATE® (flavoxate HC1) is contraindicated in patients who have any of the following obstructive conditions: pyloric or duodenal obstruction, obstructive intestinal lesions or ileus, achalasia, gastrointestinal hemorrhage and obstructive uropathies of the lower urinary tract.

– Hypersensitivity to the active substance

– Gastrointestinal obstructive conditions or ileus

– Gastro-intestinal haemorrhage

– Achalasia

– Urinary retention

– Glaucoma

– Myasthenia gravis

SPECIAL WARNINGS AND PRECAUTIONS FOR USE

The use in children below the age of <12 years is not recommended.

Since the renal clearance of the active metabolite accounts more than 50% of the dose, renal impairment may significantly affect the product kinetics. Caution is therefore required in patients with renal impairment.

As the tablets contain lactose, its use is not recommended in patients with rare hereditary problems of galactose intolerance, the total lactase deficiency or glucose- galactose malabsorption

ADVERSE EFFECTS

The source of the below ADRs frequencies is represented by data collected through clinical trials, observational studies, and spontaneous reporting.

In the table below, adverse reactions are reported and listed by MedDRA system organ class and frequency: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000), not known (cannot be estimated from available data). Within each frequency grouping the observed adverse reactions are presented in order of decreasing seriousness.

System Organ Class Frequency Preferred Terms
Immune system disorders Not known Hypersensitivity, anaphylactic reaction, anaphylactic shock
Psychiatric disorders Not known Confusional state
Nervous system disorders Uncommon Somnolence
Eye disorders Uncommon

Not known

Visual impairment

Glaucoma

Cardiac disorders Not known Palpitations
Gastrointestinal disorders Uncommon

Common

Vomiting, dry mouth, dyspepsia

Nausea

Hepatobiliary disorders Not known Jaundice, liver disorder, hepatic enzyme abnormal
Skin and subcutaneous tissue disorders Uncommon

Rare

Not known

Rash

Urticaria, pruritus

Erythema

Renal and urinary disorders Rare Urinary retention
General disorders and administration site conditions Rare Fatigue

 

DRUG INTERACTIONS

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Monitor therapy

Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Exceptions: Cannabidiol. Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Avoid combination

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Monitor therapy

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Avoid combination

Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Avoid combination

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Monitor therapy

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Monitor therapy

Opioid Agonists: Anticholinergic Agents may enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Monitor therapy

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Monitor therapy

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Avoid combination

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

OVERDOSE

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

STORAGE

Do not store above 30°C. Keep blister strips in the outer carton

Manufactured in India by:
TAJ PHARMACEUTICALS LTD.
Mumbai, India
Unit No. 214.Old Bake House,
Maharashtra chambers of  Commerce Lane,
Fort, Mumbai – 400001
at:Gujarat, INDIA.
Customer Service and Product Inquiries:
1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
E-mail: tajgroup@tajpharma.com

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Taj Generics (Taj Pharma) provides a wide range of products to the Indian market, including an extensive range of generics and specialty products; Our products cover a vast array of therapeutic categories, and we offer an extensive range of dosage forms and delivery systems including oral solids, controlled-release, steriles, injectables, topicals, liquids, transdermals, semi-solids and high-potency products. Our Generics portfolio offers over 1500 products in the major therapeutic areas of gastro-intestinal, cardiovascular, pain management, oncology, anti-infectives, paediatrics and dermatology.