Product Overview
[Drug Name]
Generic Name: Tolterodine Tartrate Tablets
Trade Name: Dikang Tolterodine Tartrate Tablets, 2mg x 14 tablets
[Main Ingredient]
The main ingredient of this product is tolterodine tartrate. Chemical Name: (R)-N-,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine L(+)-tartrate. Molecular Formula:
C22H31NO-C4H6O6 Molecular Weight: 475.57
[Properties]
This product is a film-coated tablet that appears white after removal of the film coating.
[Indications/Main Functions]
This product is indicated for the treatment of urinary frequency, urgency, or urge incontinence due to overactive bladder.
[Specifications]
2mg x 14 tablets
[Dosage and Administration]
The recommended initial dose is 2 mg twice daily. The dose can be lowered to 1 mg twice daily based on the patient's response and tolerance. For patients with hepatic impairment or those taking CYP3A4 inhibitors (see Drug Interactions), the recommended dose is 1 mg twice daily.
[Adverse Reactions]
The side effects of this drug are generally tolerable and disappear after discontinuation. This drug may cause mild to moderate anticholinergic effects, such as dry mouth, dyspepsia, and decreased tear production. 1. Common: Autonomic Nervous System: Dry mouth (>1/100) Gastrointestinal System: Dyspepsia, constipation, abdominal pain, flatulence, vomiting; Systemic: Headache; Eyes: Dry eyes; Skin: Dry skin; Mental: Drowsiness, nervousness; Central Nervous System: Paresthesia. 2. Less Common: Autonomic Nervous System: Dysregulation (<1/100) Systemic: Chest pain. 3. Rare Systemic: Allergic reaction (1/1000) Urinary System: Urinary retention; Central Nervous System: Confusion.
[Contraindications]
1. Contraindicated in patients with urinary retention, gastric stagnation, and uncontrolled narrow-angle glaucoma. 2. This product is contraindicated in patients with a confirmed allergic reaction. 3. This product is contraindicated in patients with myasthenia gravis, severe ulcerative colitis, or toxic megacolon.
[Drug Interactions]
Coadministration with other anticholinergic drugs may enhance therapeutic effects but also increase adverse reactions. Conversely, muscarinic receptor agonists may reduce the efficacy of this product. Other drugs that require cytochrome P450 2D6 (CYP2D6) or CYP3A4 for metabolism or inhibit cytochrome activity may interact pharmacokinetically with this product. For example, coadministration with fluoxetine (fluoxetine is a strong inhibitor of CYP2D6, and fluoxetine is metabolized to demethylfluoxetine, a CYP3A4 inhibitor) may slightly increase the amount of unbound tolterodine and its 5-hydroxymethyl metabolite, but this does not result in a clinically significant interaction. Extreme caution is advised when coadministering strong CYP3A4 inhibitors, such as macrolide antibiotics (erythromycin and clarithromycin) or antifungals (ketoconazole, miconazole, and itraconazole). Clinical studies have shown no interaction between this product and warfarin or oral contraceptives (levonorgestrel/ethinylestradiol). Clinical studies have also failed to demonstrate that this product inhibits the activity of CYP2D6, 2C19, 3A4, or 1A2.
[Precautions]
1. This product may cause blurred vision. Those who drive, operate machinery, or perform hazardous work while taking this product should exercise caution. 2. For patients with significantly impaired liver function, the single dose should not exceed half a tablet (1 mg). 3. This product should be used with caution in patients with impaired renal function, autonomic nervous system disorders, or hiatal hernias. 4. Due to the risk of urinary retention, this product should be used with caution in patients with bladder outlet obstruction. Due to the risk of gastric retention, this product should also be used with caution in patients with gastrointestinal obstructive diseases, such as pyloric stenosis. 5. There is no experience with this medication in children and it is not recommended for use in children. 6. Pregnant women should use this medication with caution. If taking this medication during breastfeeding, breastfeeding should be discontinued.
[Pediatric Use]
There is no experience with this medication in children and it is not recommended for use in children.
[Elderly Use]
The information is unclear.
[Overdose]
The maximum dose administered to volunteers was a single dose of 12.8 mg of L-tartrate tolterodine. The most serious adverse reactions were dysregulation and dysuria. In this case of overdose, gastric lavage and activated charcoal were used for treatment. Symptomatic treatment is as follows: Severe central anticholinergic effects (e.g., hallucinations, severe excitement) are treated with physostigmine. Seizures or marked excitement are treated with benzodiazepines. Respiratory insufficiency: Treat with artificial respiration. Tachycardia: Treat with beta-blockers. Urinary retention: Treat with urinary catheterization. Mydriasis: Use pilocarpine eye drops or place the patient in a dark room.
[Pharmacology and Toxicology]
This product is used to relieve symptoms of urinary frequency, urgency, and urge incontinence caused by overactive bladder. It is a competitive M2 cholinergic receptor blocker. Animal studies suggest that this product has higher selectivity for the bladder than for the salivary glands, but this has not been clinically confirmed. After oral administration, this product is metabolized in the liver to its active metabolite, the 5-hydroxymethyl derivative, which is the primary pharmacological agent. Its anticholinergic activity is similar to that of this product. Both are highly selective for M2 cholinergic receptors and have little effect or affinity on other neurotransmitter receptors and potential cellular targets (such as calcium channels).
