Roliten

Roliten (Tolterodine) is a medication used to treat the symptoms of overactive micturition syndrome, also known as over-urinary syndrome or excessive 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 as a tablet or capsule and is usually taken once a day. It is important to consult with your doctor before starting this medication, as only a specialist can determine if it is right for your condition and decide on the appropriate dosage.

Indications Rolitena

1. Overactive micturition syndrome (excessive frequency and/or strong urge to urinate).
2. Spontaneous urinary spasms (involuntary contraction of the bladder, resulting in an unexpected urge to urinate).
3. Stigmata of overflow bladder (patients experiencing difficulty urinating due to an overflow bladder).

Release form

1. Tablets: Roliten tablets can usually be found in regular tablets or extended release (extended release tablets). They can have different strengths depending on what they are intended for.
2. Capsules: Roliten may also be available in capsule form, often with an extended release, which allows for stable levels of the drug in the blood to be maintained over a long period of time.

Pharmacodynamics

1. Muscarinic receptor blockade: 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 reduce urinary incontinence.
2. Increased bladder capacity: By blocking muscarinic receptors, tolterodine helps relax the bladder walls and increase its capacity, which reduces the feeling of needing to urinate.
3. Reduction in urinary incontinence symptoms: Tolterodine is effective in reducing urinary incontinence symptoms such as urinary frequency, urgency, incontinence and the feeling of needing 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 meals, but this does not usually significantly affect its effectiveness.
2. Distribution: It has a high degree of plasma protein binding (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 via the kidneys. Half of the dose is excreted unchanged in the urine and also via the bile.
5. Elimination half-life: The elimination half-life of tolterodine is about 2-3 hours, and for its active metabolite it is about 3-4 hours.

Dosing and administration

The dosage and route of administration of tolterodine (trade name Roliten) may vary depending on the individual characteristics of the patient and the doctor's recommendations. However, the usual recommended dose for adults is 2 mg twice a day. In some cases, the doctor may increase the dose to 4 mg twice a day, depending on how the patient responds to treatment and tolerates the drug.

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

Use Rolitena during pregnancy

Use of tolterodine (trade name Roliten) during pregnancy may potentially pose risks to the fetus and requires careful attention. Limited studies on the use of tolterodine during pregnancy are currently available and its safety during this period has not been fully established.

If you need to take tolterodine during pregnancy, it is important to discuss it with your doctor. Your doctor can weigh the benefits of the medication for you and the risks to your baby's development, and make a decision based on your health and other factors.

It is generally preferable to avoid medications during pregnancy, especially in the first trimester when the 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 known hypersensitivity or allergic reaction to tolterodine or other components of the drug should refrain from using it.
2. Severe gastrointestinal disorders: In case of acute constipation, ulcerative colitis, obstructive bowel disorders or other serious gastrointestinal disorders, the use of tolterodine may be undesirable.
3. Glaucoma: The drug may increase intraocular pressure, so its use is not recommended in 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 antagonist effect on muscarinic receptors.
5. Tachyarrhythmias: Tolterodine may be contraindicated in patients with tachyarrhythmias as it may increase the heart rate.
6. Severe liver and kidney impairment: If you have severe liver or kidney impairment, consult your doctor before taking tolterodine.
7. Large prostatic hypertrophy: Tolterodine should be used with caution in patients with large prostatic hypertrophy as it may increase the risk of acute urinary retention.

Side effects Rolitena

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

   • Dry mouth.

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

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

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

   • Dry skin.
   • Feeling thirsty.
   • 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 of consciousness.
   • Hallucinations.
   • Tachycardia (rapid heartbeat).
   • Urinary retention.

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

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

Overdose

Overdose of tolterodine (Roliten) 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, arrhythmia, 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 levels of tolterodine, which may increase its side effects.
2. Anticholinergic drugs: Concomitant use with other anticholinergic drugs (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, rifampin, phenytoin, carbamazepine) may decrease the blood concentration of tolterodine, which may reduce its effectiveness.
4. Medicines 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. Antifungal drugs: Ketoconazole and itraconazole, as potent CYP3A4 inhibitors, may significantly increase the levels of tolterodine and its active metabolite.
6. Drugs that alter gastric pH: Antacids and other drugs that alter gastric pH may interfere with the absorption of tolterodine.