Tolterodina
Tolterodina Uses, Dosage, Side Effects, Food Interaction and all others data.
Tolterodina 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. Tolterodina 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.
Tolterodina 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. Tolterodina 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 | Tolterodina |
| 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 | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Tolterodina Tartrate is used for the treatment of overactive bladder with symptoms of urinary urgency, frequency, and/or urge incontinence.
Tolterodina is also used to associated treatment for these conditions: Urinary Bladder, Overactive
How Tolterodina 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
Tolterodina 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
Tolterodina may cause mild to moderate antimuscarinic effects, like dryness of mouth, dyspepsia and/or reduced lacrimation.
Precaution
Tolterodina 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.
Tolterodina 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.
Tolterodina 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
Tolterodina 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
Tolterodina 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 Tolterodina.
Acute Overdose
Overdosage with Tolterodina 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 Tolterodina
Tolterodina contains Tolterodine see full prescribing information from innovator Tolterodina Monograph, Tolterodina MSDS, Tolterodina FDA label
FAQ
What is Tolterodina used for?
Tolterodina 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 Tolterodina?
Tolterodina 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 Tolterodina?
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 Tolterodina safe during pregnancy?
Tolterodina 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 Tolterodina safe during breastfeeding?
Tolterodina is not usually recommended while breastfeeding. However, some breastfeeding mothers may still need it.
It is not known how much Tolterodina gets into breast milk, but this is likely to be small.
How long does Tolterodina take to work?
Tolterodina 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 Tolterodina?
Usually, you'll need to take Tolterodina for a long time.
After 4 weeks your doctor will check that Tolterodina 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 Tolterodina until your doctor tells you to stop. Do not stop taking it just because you feel better.
Is Tolterodina safe to take for a long time?
Do not take Tolterodina for longer than you need to. Your doctor will check every 6 to 12 months that your treatment is still needed.
Is Tolterodina safe to take with painkillers?
It's safe to take Tolterodina with everyday painkillers like paracetamol and ibuprofen.
Can I drink alcohol with Tolterodina?
Avoid drinking alcohol when you first start taking Tolterodina, or if your dose is increased, to see how you feel.Tolterodina 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 Tolterodina. 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 Tolterodina tablets. If you start to have problems with your weight while taking Tolterodina, talk to your pharmacist or doctor.
Will Tolterodina affect my contraception?
Tolterodina does not stop contraceptive pills working, including the combined pill or emergency contraception.
Will Tolterodina 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 Tolterodina?
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 Tolterodina?
If you want to stop taking Tolterodina, 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 Tolterodina?
Taking 1 extra dose of Tolterodina 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 Tolterodina can be dangerous.
What happen if I forget to take Tolterodina?
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 Tolterodina?
Tolterodina 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 Tolterodina affect liver?
Tolterodina may causes liver problems also anyother symtom.
