Detrusitol

Detrusitol has an m-anticholinergic effect.

Indications Detrusitol

It is used in cases of increased functional activity of the bladder, which is characterized by frequent and irresistible urges to urinate, as well as increased frequency of urination and urinary incontinence.

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Release form

It is available in tablets of 1 and 2 mg, as well as in capsules with prolonged action of 2 and 4 mg.

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Pharmacodynamics

The drug is a selective antagonist of muscarinic endings, with high selectivity for urinary endings. At the same time, it does not have a pronounced effect on other endings.

The drug reduces the activity of the detrusor (the muscles that provide contraction of the bladder and subsequent excretion of urine), reduces the frequency of spontaneous contractions carried out by it, and at the same time relaxes. The drug effect is noted after 1 month of treatment.

Detrusitol also helps to reduce the volume of salivation.

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Pharmacokinetics

Peak values in the blood are observed after 2-5 hours from the moment of taking the drug. The equilibrium level of the substance is observed after 4 days. The drug concentration indicators increase when the drug is taken with food.

The absolute bioavailability index is 17%.

Metabolism occurs in the liver, with the participation of the CYP2D6 isoenzyme. In its process, an active 5 decay product is formed, which significantly potentiates the effect of the drug. If there is a deficiency of the isoenzyme, the substance undergoes a process of dealkylation by other isoenzymes, as a result of which an inactive metabolic product is formed. With a deficiency of the CYP2D6 isoenzyme, an increase in the values of the active element in the blood is noted (approximately 7 times).

Approximately 77% of the drug is excreted via the kidneys. The half-life of the substance is 6 hours.

In case of problems with liver/kidney function, the levels of tolterodine and its active metabolic product double.

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Dosing and administration

It is recommended to take 4 mg of the drug per day. Tablets of 2 mg are taken twice a day, and capsules of 4 mg are taken once a day. Taking the medicine does not depend on food intake. Capsules should be swallowed whole.

The daily dose of the medication can be reduced to 2 mg if necessary.

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Use Detrusitol during pregnancy

There have been no tests using Detrusitol during pregnancy, so prescribing the medication during this period is prohibited.

Since there is no information regarding the excretion of tolterodine into breast milk, its use during breastfeeding should be avoided.

Contraindications

Main contraindications:

• the presence of intolerance to the elements of the therapeutic agent;
• closed-angle glaucoma;
• imperative urges that are provoked by an organic disease;
• urinary retention;
• ulcerative colitis;
• myasthenia gravis;
• megacolon;
• slow rate of gastric emptying;
• fructose or sucrase-isomaltase malabsorption.

Caution is required when prescribing to people with decreased intestinal motility, severe urinary tract obstruction, renal/hepatic insufficiency, pyloric stenosis, neuropathy, and hiatal hernia.

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Side effects Detrusitol

Often, taking medication causes dryness of the oral mucosa.

Sometimes or rarely, the following side effects are observed:

• feeling sleepy, tired, confused, nervous, or weak, and also having hallucinations, dizziness, or headaches;
• vomiting or constipation, abdominal pain and flatulence;
• visual disturbances, as well as dryness in the sclera;
• development of bronchitis, pain in the sternum, weight gain, as well as dry skin (when taking tablets) and sinusitis (when taking capsules);
• dysuric symptoms, urinary retention;
• a feeling of heartbeat rhythm, blood rushing to the face, and tachycardia;
• the appearance of peripheral edema or urticaria.

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Overdose

In case of poisoning, the following symptoms are observed: pupils dilate, there is a feeling of pronounced excitement, problems with urination or its retention begin, convulsions or hallucinations develop, and accommodation or respiratory disorders occur.

Therapy begins with gastric lavage, and then the patient must take an enterosorbent. After this, symptomatic procedures are performed:

• Physostigmine is used to eliminate hallucinations and feelings of excitement;
• Benzodiazepines are used to relieve seizures;
• treatment of tachycardia requires the use of β-blockers;
• to relieve respiratory failure, the artificial ventilation procedure is used;
• Catheterization is required to treat urinary retention.

Interactions with other drugs

Anticholinergic drugs potentiate the effects of tolterodine and also increase the likelihood of side effects.

The drug reduces the effectiveness of cisapride with metoclopramide. And the effect of Detrusitol is weakened when combined with m-anticholinergics.

There is a possibility of interaction with drugs that are metabolized by hemoprotein P450, as well as CYP2D6 or CYP3A4.

If there is a deficiency of the isoenzyme CYP2D6, it is forbidden to use clarithromycin, meconazole, and also erythromycin, ketoconazole and itraconazole, because the drug indicators may increase, which will lead to intoxication.

The medication does not have a pharmacological interaction with warfarin, and also with combined oral contraception (in tablets).

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Storage conditions

Detrusitol must be stored under standard conditions for medicinal products. Temperature – no higher than 25°C.

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Shelf life

Detrusitol can be used for 2 years from the date of release of the therapeutic drug.

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Application for children

The drug is not prescribed to people under 18 years of age, because no studies have been conducted regarding the safety of its use at this age.

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Analogues

Analogues of the drug are substances such as Urotol and Roliten.

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Reviews

Detrusitol does not have too many reviews, but they mostly confirm the high effectiveness of the drug. The drug copes well with the manifestations of urinary overactivity - frequent urination - helping to reduce its frequency and facilitate urine retention.

Some patients consider capsules to be more effective than tablets, recommending their use.

A small number of commenters noted that taking the drug causes dryness of the oral mucosa, but this is a fairly rare symptom, and also has a low degree of severity.