Sibutin

Sibutin is a medication used for urological disorders - urinary incontinence and frequent urination.

The component oxybutynin has a direct spasmolytic effect on the smooth muscle fibers of the detrusor, and at the same time has a cholinolytic effect, blocking the activity of acetylcholine on smooth muscle m-cholinergic receptors. Such effects lead to relaxation of the detrusor of the bladder. [ 1 ]

In people whose bladder function is unstable, the drug increases its capacity and reduces the number of spontaneous detrusor contractions that occur. [ 2 ]

Indications Sibutin

It is used in case of such violations:

• urinary incontinence;
• increased rate of urination or imperative urge to urinate, arising in case of unstable bladder function associated with neurogenic dysfunction (detrusor hyperreflexia), which develops with spina bifida and multiple sclerosis, or due to idiopathic instability of the detrusor (urgent motor urinary incontinence).

In addition, it is prescribed to control urinary hyperactivity that develops after operations on the urinary bladder or prostate, as well as in the case of cystitis that occurs against the background. [ 3 ]

In pediatrics, oxybutynin hydrochloride may also be used for nocturnal enuresis due to detrusor overactivity. In this case, it is used in combination with non-drug therapy if other methods have proven ineffective.

Release form

The therapeutic substance is released in tablets - 10 pieces in a cell plate; in a box - 3 such plates.

Pharmacokinetics

When taken orally, oxybutynin is absorbed into the gastrointestinal tract at a high rate; plasma Cmax values are reached after less than 60 minutes, and then they decrease biexponentially with a half-life of 2-3 hours. The maximum effect is observed for 3-4 hours, and the residual effect is observed for another 10 hours.

Equilibrium values are observed after 8 days of drug administration. In elderly people with an active lifestyle, oxybutynin does not accumulate, so its pharmacokinetic characteristics are similar to those observed in other adults. However, in elderly people with weakened health, the Cmax and AUC values increase significantly.

Oxybutynin undergoes intensive intrahepatic metabolic processes, primarily with the participation of enzymes of the structure of hemoprotein P450 (among them CYP 3A4, which is mainly contained inside the intestinal walls and liver); metabolic elements of oxybutynin also have m-anticholinergic activity.

Excretion occurs primarily via the kidneys.

Dosing and administration

The medication is taken orally; the tablet may be divided in half – 2 equal portions.

Adult dosages.

The standard daily dose is 10-15 mg (5 mg 2-3 times). It is allowed to increase it to the maximum value (20 mg - 4 times 5 mg), which is allowed if negative symptoms are tolerated and to obtain a clinical effect.

Elderly persons.

In elderly people, the half-life of the drug is longer, which is why they are prescribed a 2-time dose of 2.5 mg per day (the same regimen is recommended for weakened patients). The dosage may be increased to 2-time use of 5 mg - if there is good tolerance of negative effects, and the patient needs to achieve the development of clinical action.

In pediatrics – over 5 years of age.

In case of nocturnal enuresis and neurogenic instability of bladder function: it is necessary to use 2.5 mg twice a day. The dosage can be increased if negative symptoms are well tolerated – up to 10-15 mg (5 mg 2-3 times). When using the drug during nocturnal enuresis, the last dose is taken in the evening, before bedtime.

• Application for children

Sibutin should not be administered to children under 5 years of age. There is limited data on the use of oxybutynin in children with monosymptomatic nocturnal enuresis (not due to detrusor overactivity).

The medication is prescribed to children over 5 years of age with caution, because they may have a higher sensitivity to the effects of oxybutynin - for example, with respect to side effects associated with the psyche and central nervous system.

Use Sibutin during pregnancy

There is no information on whether it is safe to take oxybutynin during pregnancy. It is necessary to refuse its use during this period, except for situations when the patient does not have a safe analogue of Sibutin.

The use of drugs during breastfeeding is prohibited.

Contraindications

Main contraindications:

• severe intolerance associated with the active ingredient or other components of the drug;
• myasthenia gravis;
• narrow-angle glaucoma or small anterior chamber;
• people with a fever or elevated ambient temperature, as this can cause hyperpyrexia;
• disorders of esophageal function, including a hernia affecting the esophageal opening;
• gastrointestinal obstruction of organic or functional origin - this includes intestinal obstruction of a paralytic nature, pyloric stenosis and intestinal atony;
• colostomy, as well as ileostomy or toxic megacolon;
• severe ulcerative colitis;
• obstruction of the urethra (situations where urinary retention may worsen – for example, with prostate hypertrophy).

Side effects Sibutin

Side effects include:

• Gastrointestinal tract lesions: constipation, diarrhea, nausea, xerostomia, abdominal discomfort, vomiting, decreased appetite, GERD, dysphagia, anorexia and pseudo-obstruction in people with risk factors (people with constipation using medications that reduce intestinal motility, or elderly patients);
• Infections and invasions: damage to the urinary tract;
• problems with the central nervous system: drowsiness, severe headaches, cognitive impairment, dizziness and convulsions;
• mental disorders: nightmares, paranoia, agitation, anxiety, hallucinations and confusion, as well as disorientation, cognitive impairment in older people, delirium, signs of depression and addiction (in people with a history of addiction to medications or other addictive substances);
• immune disorders: increased sensitivity;
• problems with cardiac function: arrhythmia or tachycardia;
• vascular lesions: hot flashes (they are more intense in children);
• visual disturbances: mydriasis, blurred vision, closed-angle glaucoma, increased IOP, and dry conjunctiva;
• intoxication, injury or procedural complications: development of heat stroke;
• lesions of the urinary system and kidneys: dysuria or urinary retention;
• problems associated with the subcutaneous layer and epidermis: urticaria, photosensitivity, epidermal dryness (this includes rash), Quincke's edema and hypohidrosis.

Overdose

In case of intoxication, manifestations develop, starting with the potentiation of standard negative signs associated with the central nervous system (from agitation with anxiety to the development of psychotic behavior), and ending with a disorder of blood flow (decrease in blood pressure, hot flashes, insufficiency of blood flow processes, etc.), paralysis, respiratory failure and a comatose state.

In case of poisoning, symptomatic actions are usually performed:

• immediate gastric lavage procedure;
• in case of intense anticholinergic syndrome that is life-threatening, neostigmine (or physostigmine) can be used – in the dose prescribed according to the instructions for these drugs;
• treatment of feverish conditions.

If very intense agitation or anxiety is observed, 10 mg of diazepam is administered intravenously.

In case of tachycardia, intravenous injection of propranolol is required.

If urinary retention is observed, bladder catheterization is performed.

In case of paralysis of the respiratory muscles, artificial ventilation procedures are performed.

Interactions with other drugs

Use with lisuride may result in impaired consciousness, requiring constant medical supervision in such patients.

It is necessary to combine Sibutin and other anticholinergic substances with caution, because this may increase anticholinergic activity.

Interactions of anticholinergic drugs and amantadine, phenothiazines, neuroleptics (e.g. butyrophenones or clozapine), other anticholinergic antiparkinsonian drugs (e.g. levodopa or biperiden), quinidine, antihistamines, tricyclics, digitalis, dipyridamole, as well as atropine and its related compounds (e.g. atropine-type antispasmodics) are observed in isolated cases. Therefore, oxybutynin should be combined with such drugs very carefully.

Since the drug can weaken gastric motility, it can reduce the absorption of other drugs.

Oxybutynin is metabolized by the CYP3A4 isoenzyme of hemoprotein P450. Co-administration with a CYP3A4 inhibitor may inhibit oxybutynin metabolism, increasing its exposure.

The drug may have an antagonistic effect on prokinetics.

Administration together with substances that inhibit cholinesterase activity may cause a weakening of their effect.

Patients should take into account that drinking alcohol may potentiate drowsiness associated with the action of anticholinergic agents (including oxybutynin).

Storage conditions

Sibutin should be stored in a place closed to small children. Temperature values - not higher than 25°C.

Shelf life

Sibutin can be used for a period of 36 months from the date of sale of the therapeutic product.

Analogues

The analogs of the drug are Betmiga, Roliten, Urotol, Vesikar with Driptan, Urohol with Detruzitol, Novitropan and Dream-apo, as well as Spazmolit and Dreamtan-apo.

Reviews

Sibutin gets good reviews as a remedy for nocturnal enuresis, but many parents in the comments complain about side effects that develop in children after taking the medication. Among them, hallucinations are especially highlighted.