• Brand: TOLERIN®
  • Generic name:TOLTERODINE
  • Pharmaceutical form:Tab
  • Amount: 100
  • Pharmaceutical group: NEPHROLOGY & UROLOGY
Download brochure TOLTERODINE

Antisposmodic (Urinary bladder)  (USPDI) 
(+)-(R)-2-{  -[(Diisopropylamino)ethyl]benzyl}-p-cresol tartrate C22H31NO,C4 H6O6 = 475.6                                             (Martindale)
Mechanism of action / Pharmacokinetics
Tolterodine is a competitive muscarinic receptor antagonist for overactive bladder. Infact it is a tertiary antimuscarinic with actions similar to those of atropine and have a greater selectivity for muscarinic receptors of the bladder. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative which exhibits antimuscarinic 
activity similar to tolterodine.   (Facts,PDR,Martindale,USPDI)                                                                       
Pharmacokinetics properties                                         
                                                                                                                        (USPDI,Facts)   Indications
Bladder hyperactivity   (USPDI)
Tolterodine Tablets are contraindicated in patients with urinary retention, gastric retention, uncontrolled narrow-angle glucoma 
and hypersensitivity to the drug or its ingredients.   (Facts,PDR)
Warning and precaution
- Patients with significantly reduced hepatic function should not receive doses>1mg twice daily.
- Treat patients with renal impairment with caution.
- Administer with caution to patients with clinically significant bladder outflow obstruction because of the risk of urinary retention. - Administer with caution to patients with GI obstructive disorders, such as pyloric stenosis, because of the risk of gastric retention.
- Use with caution in patients being treated for narrow-angle glaucoma. (Facts)
Category C
Use during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus. (Facts)
Breast - Feeding
Tolterodine is excreted into the milk of mice. It is not known whether tolterodine is excreted in human breast milk, therefore, 
discontinue administration during nursing . (Facts,PDR) 
Drug Interaction
- Fluoxetine a SSRI and cytochrome P450 2D6 inhibitor, significantly inhibits the metabolism of tolterodine in extensive metabolizers,
however, no dosage adjustment is necessary.
- Patients receiving cytochrome P450 3A4 inhibitors, such as macrolide antibiotics(erythromycin and clarithromycim), antifungal agents(ketoconazole, itraconazole and miconazole), or cyclosporine or vinblastine should not receive doses of tolterodine > 1mg bid.
- Tolterodine is not expected to influence the pharmacokinetics of drugs that are metabolized by cytochrome P450 2D6, such as 
flecainide, vinblastine, carbamazepine and TCAs.
- Tolterodine can prolong the QT interval and should be used with caution in patients receiving other drugs known to have this effect, particularly class Ia and class III antiarrhythmics.
- Coadministration of tolterodine immediate release up to 8mg for up to 12 weeks with diuretic agents such as indapamide, 
hydrochlorothiazide,triamterene,bendroflumethiazide,chlorothiazide,methylchlorothiazide or furosemide, did not cause any adverse ECG effects.
- Tolterodine immediate release 4 mg had no effect on the pharmacokinetics of an oral contraceptive.
- A few cases of agitation, anxiety, confusion, aggression and delusion precipitated by tolterodine in patients who had been stable on donepezil.    (USPDI,PDR,Martindale,Facts)
Adverse reaction
Accommodation abnormal; dry mouth; chest pain; fatigue; headache; influenza-like symptoms; vertigo; dizziness; abdominal pain; constipation; diarrhea; dyspepsia; dysuria; dry skin; arthralgia; xerophthalmia; somnolence; weight gain; infection; hypertension; flatulence; anaphylactoid reactions; including angioedema; 
tachycardia; palpations; peripheral edema; hallucinations.                                                                                                                                 (Facts -PDR-USPDI)
A 27-month-old child who ingested 5-7 tablets of 2mg tolterodine was treated with a suspension of activated charcoal and was hospitalized avernight with symptoms of dry mouth. The child fully recoverd . (Facts)
Dosage and Administration
To treat bladder problems:
   Adults - 1 to 2 mg two times a day .
   Children - use and dose must be determined by doctor.  (USPDI)  Storage
Store below 30    and away from heat & direct light. (USPDI)
How Supplied
Tolterodine tablets are available containing 1,2 mg tolterodine.The 1mg tablets are white, biconvex & film coated tablet . The 2mg 
tablets are white, biconvex, film coated and scored tablets.
1- PDR 2006                   2-USPDI 2006                   3-USPDI 204
4- Martindale 2007         5- Drug Facts ne-Tedaphar

Exclusive advice form

  • * Name and Family :
  • * E-mail :

  • * Security code :

Comments Form

  • * Name and Family :
  • * Email :
  • * Security code :

Subscribe To Newsletter

To receive special offers for our Newsletter.