Le Zai
Le Zai Uses, Dosage, Side Effects, Food Interaction and all others data.
Le Zai is a competitive, specific muscarinic receptor antagonist which exhibits a selectivity for the urinary bladder over salivary glands, which have been demonstrated in non clinical pharmacological in vivo studies. Le Zai has a high specificity for muscarinic receptors. A major active metabolite (5-hydroxymethyl derivative) of tolterodine exhibits a pharmacological profile which is similar to that of the parent compound. In extensive metabolisers this metabolite contributes significantly to the therapeutic effect of tolterodine. The effect of treatment can be expected within 4 weeks.
Le Zai is a competitive muscarinic receptor antagonist. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and the 5-hydroxymethyl metabolite exhibit a high specificity for muscarinic receptors, since both show negligible activity or affinity for other neurotransmitter receptors and other potential cellular targets, such as calcium channels. Le Zai has a pronounced effect on bladder function. The main effects of tolterodine are an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure, consistent with an antimuscarinic action on the lower urinary tract.
| Trade Name | Le Zai |
| Availability | Prescription only |
| Generic | Tolterodine |
| Tolterodine Other Names | Tolterodina, Tolterodine, Tolterodinum |
| Related Drugs | oxybutynin, Myrbetriq, solifenacin, mirabegron, Ditropan, Detrol, VESIcare, trospium |
| Type | |
| Formula | C22H31NO |
| Weight | Average: 325.4876 Monoisotopic: 325.240564619 |
| Protein binding | Approximately 96.3%. |
| Groups | Approved, Investigational |
| Therapeutic Class | BPH/ Urinary retention/ Urinary incontinence |
| Manufacturer | |
| Available Country | China |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Le Zai Tartrate is used for the treatment of overactive bladder with symptoms of urinary urgency, frequency, and/or urge incontinence.
Le Zai is also used to associated treatment for these conditions: Urinary Bladder, Overactive
How Le Zai works
Both tolterodine and its active metabolite, 5-hydroxymethyltolterodine, act as competitive antagonists at muscarinic receptors. This antagonism results in inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.
Dosage
Le Zai dosage
The recommended dose for tolterodine is 2 mg twice daily. In case of troublesome side effects the dose may be reduced from 2 mg to 1 mg twice daily.
The recommended total daily dose of tolterodine is 2 mg (1 mg b.i.d.) for patients with impaired renal function, impaired liver function, or receiving concomitant medication with potent CYP3A inhibitors, such as macrolide antibiotics (e.g. erythromycin and clarithromycin) or azole antifungal agents (e.g. ketoconazole, itraconazole and miconazole). After six months the need for further treatment should be considered.
Side Effects
Le Zai may cause mild to moderate antimuscarinic effects, like dryness of mouth, dyspepsia and/or reduced lacrimation.
Precaution
Le Zai should be used with caution in the following patients:
- at risk for urinary retention
- at risk for decreased gastrointestinal motility
- with impaired renal function
- with impaired hepatic function
Organic reasons for urge and frequency should be considered before treatment.
Interaction
Pharmacokinetic interactions are possible with other drugs metabolised by or inhibiting cytochrome P450 2D6 (CYP2D6) or CYP3A4. Concomitant treatment with fluoxetine does not result in a clinically significant interaction.
Ketoconazole, a potent inhibitor of CYP3A, significantly increased plasma concentrations of tolterodine when coadministered to poor metabolisers (i.e. persons devoid of CYP2D6 metabolic pathway).
Clinical studies have shown no interactions with warfarin or combined oral contraceptives (ethinyloestradiol or levonorgestrel).
Food Interaction
- Take with food.
Le Zai Alcohol interaction
[Moderate] GENERALLY AVOID:
Use of anticholinergic agents with alcohol may result in sufficient impairment of attention so as to render driving and operating machinery more hazardous.
In addition, the potential for abuse may be increased with the combination.
The mechanism of interaction is not established but may involve additive depressant effects on the central nervous system.
No effect of oral propantheline or atropine on blood alcohol levels was observed in healthy volunteers when administered before ingestion of a standard ethanol load.
However, one study found impairment of attention in subjects given atropine 0.5 mg or glycopyrrolate 1 mg in combination with alcohol.
Alcohol should generally be avoided during therapy with anticholinergic agents.
Patients should be counseled to avoid activities requiring mental alertness until they know how these agents affect them.
Le Zai Drug Interaction
Moderate: diphenhydramine, metoprolol, metoprolol, mirabegron, acetaminophen / hydrocodoneMinor: duloxetine, acetaminophenUnknown: aspirin, aspirin, calcium / vitamin d, apixaban, omega-3 polyunsaturated fatty acids, pregabalin, polyethylene glycol 3350, albuterol, levothyroxine, cyanocobalamin, ascorbic acid, cholecalciferol, cetirizine
Le Zai Disease Interaction
Major: angle-closure glaucoma, GI/urinary obstructionModerate: CNS, hepatic dysfunction, myasthenia gravis, QT prolongation, renal dysfunction
Volume of Distribution
- 113 ± 26.7 L
Half Life
1.9-3.7 hours
Elimination Route
Following administration of a 5-mg oral dose of 14C-tolterodine solution to healthy volunteers, 77% of radioactivity was recovered in urine and 17% was recovered in feces in 7 days.
Pregnancy & Breastfeeding use
There are no studies in pregnant women. Therefore, tolterodine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Use of tolterodine during lactation should be avoided since no data on excretion of the drug into breast milk in humans is available.
Contraindication
Le Zai is contraindicated in those patients with urinary retention, uncontrolled narrow angle glaucoma, known hypersensitivity to tolterodine or any other component of the drug.
Special Warning
Pediatric use: Safety and effectiveness of tolterodine in children have not been established.
Geriatric use: No overall differences in safety were observed between the older and younger patients treated with Le Zai.
Acute Overdose
Overdosage with Le Zai Tartrate capsules can potentially result in severe central anticholinergic effects and should be treated accordingly. ECG monitoring is recommended in the event of overdosage.
Storage Condition
Store in a cool and dry place. Protect from light. Keep out of the reach of children.
Innovators Monograph
You find simplified version here Le Zai
Le Zai contains Tolterodine see full prescribing information from innovator Le Zai Monograph, Le Zai MSDS, Le Zai FDA label
FAQ
What is Le Zai used for?
Le Zai is used treat overactive bladder a condition in which the bladder muscles contract uncontrollably and cause frequent urination, urgent need to urinate, and inability to control urination.
How safe is Le Zai?
Le Zai is safe and shows efficacy, particularly at a dosage of 2 mg bid, in the treatment of older patients with urinary symptoms attributable to overactive bladder.
What are the common side effects of Le Zai?
The common side effects are include:
- dry mouth
- headache
- feeling dizzy, sleepy, or a spinning sensation (vertigo)
- diarrhoea or being sick (vomiting)
- constipation
- farting and burping (wind)
- stomach pain
- dry eyes
- blurred vision
- problems or pain when peeing, and not being able to empty your bladder
Is Le Zai safe during pregnancy?
Le Zai is not usually recommended in pregnancy because there's not enough information available to say it's safe for you and your baby.
If you're trying to get pregnant or you're already pregnant, talk to your doctor about whether taking tolterodine is right for you.
Is Le Zai safe during breastfeeding?
Le Zai is not usually recommended while breastfeeding. However, some breastfeeding mothers may still need it.
It is not known how much Le Zai gets into breast milk, but this is likely to be small.
How long does Le Zai take to work?
Le Zai begins to work within 3 to 8 hours but it may take up to 4 weeks before it takes full effect. If the symptoms do not improve after 1 to 2 weeks, talk to your doctor.
How long will I take Le Zai?
Usually, you'll need to take Le Zai for a long time.
After 4 weeks your doctor will check that Le Zai is helping your symptoms. They'll also do a review every 6 to 12 months after that to check it's still working for you.
Take Le Zai until your doctor tells you to stop. Do not stop taking it just because you feel better.
Is Le Zai safe to take for a long time?
Do not take Le Zai for longer than you need to. Your doctor will check every 6 to 12 months that your treatment is still needed.
Is Le Zai safe to take with painkillers?
It's safe to take Le Zai with everyday painkillers like paracetamol and ibuprofen.
Can I drink alcohol with Le Zai?
Avoid drinking alcohol when you first start taking Le Zai, or if your dose is increased, to see how you feel.Le Zai combined with alcohol can make you feel very sleepy.
Drinking alcohol may make you more likely to need to get up in the night to pee.
Is there any food or drink I need to avoid?
You can eat normally while taking Le Zai. If you have urinary incontinence, cut down on alcohol and drinks containing caffeine, such as tea, coffee and cola.
Will I gain or lose weight?
You may gain weight when you take Le Zai tablets. If you start to have problems with your weight while taking Le Zai, talk to your pharmacist or doctor.
Will Le Zai affect my contraception?
Le Zai does not stop contraceptive pills working, including the combined pill or emergency contraception.
Will Le Zai affect my fertility?
There's no clear evidence to suggest that taking tolterodine will reduce fertility in either men or women.
However, speak to a pharmacist or your doctor before taking it if you're trying to get pregnant.
Can I drive after taking Le Zai?
Do not drive a car, ride a bike, use tools or operate machinery if tolterodine makes you sleepy, gives you blurred vision, or makes you feel dizzy.
Can I stop taking Le Zai?
If you want to stop taking Le Zai, talk to your doctor first.
If you've been taking it for at least 6 months, your doctor may suggest at your review that you can stop taking it for up to 4 weeks to see how your symptoms change without it.
Some people find that the improvement in their symptoms continues after they've stopped taking the medicine.
What happen if I take too much Le Zai?
Taking 1 extra dose of Le Zai is unlikely to harm you.
However, you may get more side effects, such as a dry mouth or headache.
The amount of tolterodine that can lead to an overdose varies from person to person, and too much Le Zai can be dangerous.
What happen if I forget to take Le Zai?
If you forget to take a dose, take it as soon as you remember, unless it's nearly time for your next dose. In this case, just skip the missed dose and take your next dose as normal.
Never take 2 doses at the same time. Never take an extra dose to make up for a forgotten one.
Who can and can't take Le Zai?
Le Zai can be taken by most adults. It can also be taken by children aged 2 years and over, on the advice of their specialist.
Does Le Zai affect liver?
Le Zai may causes liver problems also anyother symtom.
