Roliten

Rolitene (Tolterodine) is a drug that is used to treat the symptoms of hyperactive urination syndrome, also known as hyperurinary syndrome or urethral contraction syndrome. This syndrome is characterized by the inability to hold urine, resulting in a frequent and unexpected urge to urinate.

Tolterodine works by blocking certain receptors in the bladder, which helps reduce the frequency and force of urination. It is available in tablet or capsule form and is usually taken once a day. It is important to consult your doctor before starting to take this drug, as only a specialist can determine whether it is suitable for your condition and decide on the appropriate dosage.

Indications Rolled

1. Overactive urination syndrome (excessive frequency and/or strong urge to urinate).
2. Spontaneous urinary cramps (involuntary contraction of the bladder, leading to an unexpected urge to urinate).
3. Stigmata of a full bladder (patients who have difficulty urinating due to a full bladder).

Release form

1. Tablets: Rolitene Tablets may usually be available in the form of regular tablets or extended release (extended-release tablets). They may have different dosages depending on what they are intended for.
2. Capsules: Rolitene may also be available in capsule form, often with extended release, which helps maintain stable blood levels of the drug over a long period of time.

Pharmacodynamics

1. Blocking muscarinic receptors: Tolterodine blocks muscarinic receptors, which results in decreased contractility of the smooth muscles of the bladder. This mechanism helps to reduce the frequency of urination and curtail urinary incontinence.
2. Increasing bladder capacity: By blocking muscarinic receptors, tolterodine helps to relax the bladder wall and increase its capacity, which reduces the feeling of the need to urinate.
3. Reducing symptoms of urinary incontinence: Tolterodine is effective in reducing the symptoms of urinary incontinence, such as urinary frequency, urgency, incontinence, and the feeling of the need to urinate.
4. Improving symptoms of urinary frequency syndrome: Tolterodine may also be effective in treating urinary frequency syndrome by helping to reduce urinary frequency and reducing urgency.

Pharmacokinetics

1. Absorption: Tolterodine is well absorbed from the gastrointestinal tract after oral administration. Absorption may be delayed after food intake, but this usually does not significantly affect its efficacy.
2. Distribution: It is highly bound to plasma proteins (about 96%). Tolterodine has the ability to penetrate the blood-brain barrier.
3. Metabolism: Tolterodine is primarily metabolized in the liver to form the active metabolite 5-hydroxymethyl-tolterodine (5-HMT). This metabolite is more active than tolterodine itself.
4. Excretion: Tolterodine and its metabolites are excreted primarily through the kidneys. Half the dose is excreted unchanged through urine and also through bile.
5. Half-life: The half-life of tolterodine is about 2-3 hours, and for its active metabolite - about 3-4 hours.

Dosing and administration

The dosage and route of administration of tolterodine (trade name Rolitene) may vary depending on the individual patient and the doctor's recommendations. However, the usual standard recommended dose for adults is 2 mg twice daily. In some cases, the doctor may increase the dose to 4 mg twice daily, depending on the patient's response to treatment and tolerance to the drug.

The drug should be taken orally, swallowed whole, with or without food. For best results, it is recommended to take the tablets at the same time every day.

Use Rolled during pregnancy

The use of tolterodine (trade name Roliten) during pregnancy may potentially pose risks to the fetus and requires careful attention. Currently, a limited number of studies on the use of tolterodine during pregnancy are available, and its safety during this period has not been fully established.

If you have a need to take tolterodine during pregnancy, it is important to discuss this with your doctor. Your doctor can weigh the benefits of using the medicine for you against the risks to your developing baby, and make a decision based on your health and other factors.

It is generally best to avoid using medicines during pregnancy, especially in the first trimester when your baby's organs and systems are developing. If necessary, your doctor may prescribe tolterodine only if the benefits to the mother outweigh the potential risks to the baby.

Contraindications

1. Hypersensitivity: People with a known hypersensitivity or allergic reaction to tolterodine or other components of the drug should avoid using it.
2. Severe gastrointestinal disorders: In cases of acute constipation, ulcerative colitis, obstructive bowel disorders or other serious gastrointestinal disorders, the use of tolterodine may not be advisable.
3. Glaucoma: The drug may increase intraocular pressure, so its use is not recommended for open-angle glaucoma or in patients at risk of developing it.
4. Myasthenic syndrome: The use of tolterodine may be contraindicated in patients with myasthenic syndrome due to its muscarinic receptor antagonistic effects.
5. Tachyarrhythmias: The use of tolterodine may be contraindicated in patients with tachyarrhythmias as it may increase heart rate.
6. Severe liver and kidney impairment: If you have severe liver or kidney impairment, consult your doctor before starting tolterodine.
7. Major prostatic hypertrophy: Tolterodine should be used with caution in patients with prostatic hypertrophy as it may increase the risk of acute urinary retention.

Side effects Rolled

1. Very common side effects (more than 10%):

   • Dry mouth.

2. Common side effects (1-10%):

   • Headache.
   • Dizziness.
   • Fatigue.
   • Constipation.
   • Stomach pain.
   • Dyspepsia (indigestion).
   • Dry eyes.

3. Infrequent side effects (0.1-1%):

   • Dry skin.
   • Feeling of thirst.
   • Visual disturbances, including blurred vision.
   • Rapid heartbeat (tachycardia).
   • Urinary tract infections.
   • Difficulty urinating.

4. Rare side effects (0.01-0.1%):

   • Allergic reactions such as skin rash or itching.
   • Anaphylactic reactions.
   • Angioedema.
   • Confusion.
   • Hallucinations.
   • Tachycardia (fast heartbeat).
   • Urine retention.

5. Very rare side effects (less than 0.01%):

   • Psychiatric disorders (eg, anxiety, depression).
   • Convulsions.
   • Heart rhythm disturbances (including arrhythmias and heart failure).

Overdose

An overdose of tolterodine (Rolitene) can lead to serious side effects and complications. Signs of overdose may include increased symptoms of side effects such as dry mouth, constipation, visual disturbances, tachycardia, arrhythmias, drowsiness, dizziness and others.

Interactions with other drugs

1. CYP3A4 inhibitors: Drugs that inhibit the CYP3A4 enzyme (eg, ketoconazole, itraconazole, erythromycin, clarithromycin, ritonavir) may increase the blood concentration of tolterodine, which may increase its side effects.
2. Anticholinergics: Concomitant use with other anticholinergics (eg, atropine, scopolamine, some antidepressants and antipsychotics) may increase anticholinergic side effects such as dry mouth, constipation, blurred vision, and difficulty urinating.
3. CYP3A4 inducers: Drugs that induce the CYP3A4 enzyme (eg, rifampicin, phenytoin, carbamazepine) may decrease the blood concentration of tolterodine, which may reduce its effectiveness.
4. Drugs that prolong the QT interval: Concomitant use with drugs that prolong the QT interval (eg, class IA and III antiarrhythmic drugs, some antidepressants and antipsychotics) may increase the risk of cardiac arrhythmias.
5. Antifungals: Ketoconazole and itraconazole, as potent CYP3A4 inhibitors, may significantly increase levels of tolterodine and its active metabolite.
6. Drugs that change gastric pH: Antacids and other drugs that change gastric pH may affect the absorption of tolterodine.