Tolterodine
Mechanism :
Tolterodine is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors.
Indication :
- Urinary Urgency
- Urinary incontinence
- Urinary frequency
Contraindications :
Contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma, and in patients who have demonstrated hypersensitivity to the drug or its ingredients. Caution in liver and renal impairment.
Dosing :
<35 kg:
2 mg/day PO once daily.
>35 kg:
4 mg/day PO once daily.
Usually effective within 4 weeks.
Adverse Effect :
Frequently seen adverse reactions include constipation, dyspepsia, nausea, abdominal discomfort. Dry mouth, blurred vision, drowsiness, paraesthesia, dry skin, facial flushing, headache and dizziness may also occur.
Interaction :
Ketoconazole: An inhibitor of the drug metabolizing enzyme CYP3A4, significantly increased plasma concentrations of tolterodine when coadministered to subjects who were poor metabolizers.
Macrolide antibiotics: Avoid use with macrolide antibiotics.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 30-50 | Dose as in normal renal function. Use with caution |
| 10-30 | 1 mg twice daily. Use with caution |
| <10 | 1 mg twice daily. Use with caution |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
| HD | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
| HDF/High flux | Unlikely to be dialysed. Dose as in GFR<10 mL/min |
| CAV/VVHD | Unlikely to be dialysed. Dose as in GFR=10–30 mL/min |
Hepatic Dose :
For immediate release tablet: Use cautiously. The dose is halved
For extended release formulation:
Mild to moderate hepatic impairment: dose is halved.
Severe hepatic impairment: Do not use the drug.