lncont L.A Tolterodine Tartarate 4mg
L.A.Tablets
Composition :
Each tablet contains 4mg tolterodine tartarate.
Properties :
Incont (tolterodine) is a muscarinic receptor antagonist.
Pharmacokinetics :
Absorption:
The AUC of tolterodine long acting 4mg daily is equivalent to tolterodine immediate release4mg (2mg bid).
Cmax and Gmin levels oftolterodine long acting are about 75% and 150% oftolterodine immediate release, respectively.
Maximum serum concentrations oftolterodine long acting are observed 2 to 6 hours after oral administration.
Effect of Food :
There is no effect of food on the pharmacokinetics of tolterodine
long acting.
Distribution :
Tolterodine is highly bound to plasma proteins, unbound
concentrations oftolterodine average 3.7% ± 0.13% overthe
concentration range achieved in clinical studies. The 5-hydroxymethyl metabolite is not extensively protein bound,
with unbound fraction concentrations averaging 36% ± 4%.
Metabolism :
Tolterodine is extensively metabolized by the liver mediated by
the Cytochrome P450 following oral dosing. Tolterodine is metabolized into the phannacologically active 5-hydroxymethyl metabolite. Further metabolism leads to the formation of the 5-carboxylic acid and N- dealkylated 5 – carboxylic acid metabolites which account for 51%±14% and 29%±6.3% of the metabolites recovered in the urine, respectively.
Excretion :
Following administration of 5mg oral dose, 77% is recovered in urine and 17% is recovered in feces in 7 days. Less than 1% of the dose is recovered as intact tolterodine.5% to 14% is recovered as the active 5-hydroxymethyl metabolite.
Drug-Drug Interactions :
Fluoxetine:
No dose adjustment is required when Incont and Fluoxetine are co-
administered.
Other Drugs Metabolized By Cytochrome P450 Isoenzymes :
Tolteradine does not cause clinically significant interactions with other drugs metabolized by the major drug metabolizing CYP enzymes.
CYP3A4lnhibitors :
Potent CYP3A4 inhibitors such as azole antifungals (e.g,itraconazole, miconazole) or macrolide antibiotics (e.g,erythromycin, clarithromycin) or cyclosporine or vinblastine may lead to increases of tolterodine plasma concentrations.
Warfarin :
In healthy volunteers, co-administration of tolterodine 4mg (2mg b.i.d} for 7 days and asignal dose of warfarin 25 mg on day 4 has no effect on prothrombin time factor suppression or on the pharmacokinetics of warfarin
Oral Contraceptives :
Tolterodine 4mg (2mg b.i.d), has no effect on the phannacokinetics of oral contraceptives.
Diuretics : co administration of tolterodine up to 8mg (4mg b.i.d) for up
to 12 weeks with diuretic agents such as indapamide, triamterene,
bendroflumethiazide methylchlorothiazide or furosemide did not cause adverse electrocardiographic (ECG) effects.
Indications :
Incont tablets are indicated for the treatment of overactive bladder
with symptoms of urge urinary incontinence, urgency and frequency.
Contraindications :
Incont tablets are contraindicated in patients with urinary retention,
gastric retention and uncontrolled narrow angle glaucoma. Incont is also contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients.
Precautions :
-Incont LA should be administered with caution to patients with
clinically significant bladder outflow obstruction because of the risk of urinary retention.
-Incont LA should be administered with caution to patients with
gastrointestinal obstructive disorders, such as pyloric stenosis, because ofthe risk of gastric retention.
-Incont LA should be used with caution in patients being treated for
narrow angle glaucoma. For patients with significantly reduced hepatic or renal function, the recommended dose of Incont LA is 2mg daily.
-Like all antimuscarinics agents, Incont LA may produce blurred vision, dizziness, or drowsiness.
Pregnancy :
Incont is currently classified as (Pregnancy Category C). Incont should be used during pregnancy only if the potential benefit forthe mother justifies the potential risk to the fetus.
Nursing Mothers :
Incont should not be administered during nursing.
Pediatric Use :
Efficacy in pediatric population has not been established.
Geriatric Use :
No overall differences in safety were observed between older and
younger patients.
Adverse Reactions :
Incont, being anti muscarinic agent may cause dry mouth. headache, constipation, abdominal pain, urinary retention and dry eyes.
Overdosage :
Overdosage with Incont can potentially result in severe central
anticholinergic effects and should be treated accordingly.
Dosage :
The recommended dose of Incont LA is 4mg daily.
Incont LAshould be taken once daily with liquids and swallowed whole. The dose may be lowered to 2 mg daily based on individual response and tolerability.
Storage :
Store (15- 300)C away from direct sunlight & keep outof reach of children.
Package :
Box of 1 blister (each one contains 10 scored tablets).
I Keep out of reach of children
Manufactured by :
ADWIA Co. S.A.E 10″ of Ramadan City
EGYPT
