Detruzitol

Detruzitol has m-anticholinergic action.

Indications of the detruzitol

It is used with increased functional activity of the urea, in which there are frequent and irresistible urge to urinate, and besides this, the frequency of urination and the incontinence of urination processes are frequent .

[1], [2]

Release form

The release occurs in tablets with a volume of 1 and 2 mg, as well as capsules with prolonged exposure - a volume of 2 and 4 mg.

[3], [4], [5]

Pharmacodynamics

The drug is a selective antagonist of muscarinic endings, which has a high selectivity for the endings of the urea. At the same time, it has no significant effect on other endings.

The medicine reduces detrusor activity (those muscles that provide a contraction of the bladder and the subsequent excretion of urine), reduces the frequency of spontaneous contractions made by it, and at the same time relaxes it. The drug effect is observed after the lapse of the first month of treatment.

Detruzitol also helps to reduce the amount of saliva.

[6], [7],

Pharmacokinetics

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

The absolute bioavailability is 17%.

Metabolism proceeds inside the liver, with the participation of isoenzyme CYP2D6. In its process, an active 5 decay product is formed, a potentiating effect of the drug. If there is a lack of isoenzyme, the substance undergoes the process of dealkylation by other isoenzymes, resulting in the formation of an inactive metabolic product. If the isoenzyme CYP2D6 is deficient, the active element values inside the blood are increased (approximately 7 times).

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

In case of liver / kidney problems, the values of tolterodine with its active metabolic product are doubled.

[8], [9]

Dosing and administration

During the day, it is recommended to take 4 mg of the drug. Tablets with a volume of 2 mg are drunk twice a day, and capsules with a volume of 4 mg are administered once. The medication is not dependent on eating. Capsules must be swallowed whole.

The size of a daily dose of a medicine can be reduced to 2 mg if necessary.

[14], [15]

Use of the detruzitol during pregnancy

Testing with detrusitol during pregnancy was not carried out, so it is forbidden to prescribe a drug at this time.

Because there is no information on the excretion of tolterodine in breast milk, it is necessary to abandon its use in breastfeeding.

Contraindications

The main contraindications:

• the presence of intolerance with respect to the elements of the therapeutic agent;
• glaucoma of a closed angle;
• imperative urges, which are provoked by organic disease;
• retention of urination;
• Ulcerative form of colitis;
• myasthenia gravis;
• megacolon;
• slow rate of gastric emptying;
• malabsorption of fructose or sucrose-isomaltase.

Caution is required when appointing people with reduced intestinal motility, obstruction in the urinary ducts to a significant extent, kidney / liver failure, stenosis in the pylorus, neuropathy, and hernia in the esophageal area.

[10]

Side effects of the detruzitol

Often, the medication causes dry mouth mucous.

Sometimes, or occasionally, there are such side effects:

• sensation of drowsiness, fatigue, confusion, nervousness or weakness, and in addition the appearance of hallucinations, dizziness or headaches;
• vomiting or constipation, abdominal pain and flatulence;
• visual disorders, as well as dryness in the sclera region;
• development of bronchitis, pain in the sternum, weight gain, as well as cutaneous dryness (with the use of tablets) and sinusitis (with capsules);
• dysuric symptoms, delayed urination;
• sensation of the rhythm of the heartbeat, blood flowing to the face, and tachycardia;
• the appearance of peripheral swelling or urticaria.

[11], [12], [13]

Overdose

When poisoning, the following symptoms are noted: the pupils widen, there is a marked excitement, problems with urination or delay occur, convulsions or hallucinations develop, and accommodation disorder or respiratory processes develop.

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

• To eliminate hallucinations and a sense of excitement, physostigmine is used;
• To eliminate seizures, benzodiazepines are used;
• for the treatment of tachycardia requires the use of β-blockers;
• To remove respiratory insufficiency, use the IVL procedure;
• To treat delayed urination, catheterization is required.

Interactions with other drugs

Cholinolytic 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-holinolitics.

There is a possibility of development of interaction with drugs, the metabolism of which is carried out with the participation of hemoprotein P450, as well as CYP2D6 or CYP3A4.

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

The drug does not have a pharmacological interaction with warfarin, and in addition to oral contraception (in tablets) of a combined type.

[16], [17], [18]

Storage conditions

Detruzitol is required to be kept in standard for medicinal conditions. The temperature is not higher than 25 ° C.

[19], [20], [21], [22]

Shelf life

Detruzitol can be used for 2 years after the release of the therapeutic drug.

[23], [24], [25]

Application for children

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

[26], [27], [28], [29]

Analogues

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

[30], [31]

Reviews

Detrusitol has not too many reviews, but they basically confirm the high effectiveness of the drug. The drug perfectly copes with the manifestations of hyperactivity of urea - rapid urination - helping to reduce its frequency and facilitate the retention of urine.

Individual patients consider capsules to be more effective than tablets, recommending using them.

A small part of the commenters noted that taking drugs causes dryness of oral mucous membranes, but this is a rather rare symptom, besides having a low degree of severity.