Sibutin

Sibutin is a medicine used for urological disorders - urinary incontinence and urinary frequency.

The component oxybutynin has a direct antispasmodic effect on the smooth muscle fibers of the detrusor, and at the same time has an anticholinergic effect, blocking the activity of acetylcholine relative to smooth muscle m-cholinergic receptors. Similar effects lead to relaxation of the urea detrusor. [1]

In people whose bladder is unstable, the medication increases its volume and reduces the amount of detrusor contractions that occur spontaneously. [2]

Indications Sibutin

It is applied in case of such violations:

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

In addition, it is prescribed to control the overactivity of the urea that has developed after operations performed on the ureter or prostate, as well as in the case of cystitis that occurs against the background. [3]

In pediatrics, oxybutynin hydrochloride can 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 are ineffective.

Release form

The release of the therapeutic substance is made in tablets - 10 pieces inside the cell plate; there are 3 such records in the box.

Pharmacokinetics

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

Equilibrium indicators are noted after 8 days of drug use. In elderly people with an active lifestyle, oxybutynin does not cumulate, therefore, its pharmacokinetic characteristics are similar to those observed in other adults. But in elderly people with poor health, the Cmax values, as well as the AUC, 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 found inside the intestinal walls and liver); metabolic elements of oxybutynin also have m-anticholinergic activity.

Excretion mainly takes place through the kidneys.

Dosing and administration

The medication is taken orally; the tablet is allowed to be divided in half - 2 equal portions.

Adult dosages.

The standard serving per day is 10-15 mg (5 mg 2-3 times). It is allowed to increase it to the maximum value (20 mg - 4-fold intake of 5 mg), which is allowed if negative symptoms are tolerated and to obtain clinical influence.

Elderly persons.

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

In pediatrics - over 5 years of age.

With nocturnal enuresis and neurogenic instability of urea activity: it is necessary to apply 2.5 mg 2 times a day. An increase in dosage is possible with good tolerance of negative signs - up to 10-15 mg (5 mg 2-3 times a day). When using drugs during nocturnal enuresis, the last portion is consumed in the evening, before bedtime.

• Application for children

Persons under the age of 5 should not be prescribed Sibutin. There is only limited information regarding the use of oxybutynin in childhood with monosymptomatic nocturnal enuresis (not due to detrusor overactivity).

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

Use Sibutin during pregnancy

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

The use of drugs while breastfeeding is prohibited.

Contraindications

The main contraindications:

• severe intolerance associated with the active element or other constituent components of the drug;
• myasthenia gravis;
• narrow-angle glaucoma or small anterior ocular chamber;
• persons with a febrile state or with an increased temperature of the environment, because this can provoke hyperpyrexia;
• disorders of esophageal activity, including a hernia that affects the alimentary opening;
• blockage of the gastrointestinal tract, which is of an organic or functional nature - this includes intestinal blockage 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 an exacerbation of urinary retention may occur - for example, with prostate hypertrophy).

Side effects Sibutin

Among the side effects:

• lesions of the gastrointestinal tract: constipation, diarrhea, nausea, xerostomia, abdominal discomfort, vomiting, loss of appetite, GERD, dysphagia, anorexia and pseudo-occlusion in people with risk factors (persons with constipation, using medications that weaken intestinal motility, or the patient's old age);
• infections and invasions: damage to the urethra;
• problems with the work of the central nervous system: drowsiness, severe headaches, cognitive impairment, dizziness and seizures;
• mental disorders: nightmares, paranoia, agitation, anxiety, hallucinations and confusion, and in addition, disorientation, cognitive impairment in the elderly, delirium, signs of depression and dependence (in people with a history of dependence on drugs or other substances, from which dependence appears);
• immune disorders: increased sensitivity;
• heart problems: arrhythmia or tachycardia;
• vascular lesions: hot flashes (they are more intense in children);
• visual disturbances: mydriasis, visual blurredness, angle-closure glaucoma, increased IOP values, as well as dryness of the conjunctiva;
• intoxication, trauma or procedural complications: the development of heatstroke;
• 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 a rash), Quincke's edema and hypohidrosis.

Overdose

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

In case of poisoning, symptomatic actions are usually performed:

• immediate gastric lavage procedure;
• in the case of an intense life-threatening anticholinergic syndrome, neostigmine (or physostigmine) can be used - in a portion that is prescribed according to the instructions of these drugs;
• treatment of a febrile condition.

If there is very intense excitement or anxiety, 10 mg of diazepam is injected intravenously.

In case of tachycardia, an IV injection of propranolol is required.

If urinary retention is observed, urea catheterization is performed.

With paralysis of the respiratory muscles, mechanical ventilation is performed.

Interactions with other drugs

Use with lisuride can lead to impaired consciousness, which requires constant medical supervision in such patients.

It is necessary to carefully combine Sibutin and other anticholinergic substances, because this can enhance anticholinergic activity.

The interaction of anticholinergic drugs and amantadine, phenothiazines, neuroleptics (for example, butyrophenones or clozapine), other anticholinergic antiparkinsonian drugs (for example, levodopa or biperiden), quinidine, antihistamines, tricyclics, digitalis and its related compounds (for example, antispasmodics of an atropine nature). Therefore, it is necessary to combine oxybutynin with such drugs very carefully.

Since the medication can weaken gastric motility, it can reduce the absorption of other medications.

Oxybutynin undergoes metabolic processes using the CYP3A4 isoenzyme of the hemoprotein P450. The introduction together with an agent that slows down the action of CYP3A4, can suppress the metabolic processes of oxybutynin, increasing its exposure.

The drug can have an antagonistic effect against prokinetics.

The introduction together with substances that slow down the activity of cholinesterase, can cause a weakening of their effect.

Patients should take into account that drinking alcohol can potentiate drowsiness associated with the action of anticholinergic substances (among them oxybutynin).

Storage conditions

Sibutin must be kept out of the reach of small children. Temperature values are not higher than 25 ° С.

Shelf life

Sibutin can be used for a 36-month term from the moment the therapeutic product is sold.

Analogs

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

Reviews

Sibutin is receiving good reviews as a remedy for nocturnal enuresis, but at the same time, many parents in the comments complain about the side symptoms that develop in children after taking the medication. Among them, hallucinations are especially distinguished.