Instructions for Sibutin tablets 5 mg blister No. 30
Composition
active ingredient: oxybutynin hydrochloride;
1 tablet contains oxybutynin hydrochloride 5 mg;
Excipients: lactose monohydrate, microcrystalline cellulose, potato starch, calcium stearate.
Dosage form
Pills.
Main physicochemical properties: flat-cylindrical tablets with beveled edges and a score, white or almost white in color.
Pharmacotherapeutic group
Drugs used in urology. Drugs for the treatment of frequent urination and urinary incontinence. ATX code G04B D04.
Pharmacological properties
Pharmacodynamics
Oxybutynin has a direct antispasmodic effect on the smooth muscle fibers of the detrusor, as well as an anticholinergic effect, blocking the effect of acetylcholine on M-cholinoreceptors of smooth muscle. These properties cause relaxation of the bladder detrusor. In patients with unstable bladder, Sibutin increases bladder volume and reduces the frequency of spontaneous detrusor contractions.
Pharmacokinetics
After oral administration, oxybutynin is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations occurring in less than 1 hour and then declining biexponentially with a half-life of 2 to 3 hours. The maximum effect is observed within 3-4 hours, with residual effects occurring after 10 hours.
Steady-state concentrations are reached after 8 days of oral administration. In elderly patients who lead an active lifestyle, oxybutynin does not show the ability to accumulate and its pharmacokinetics do not differ from those in other adult patients. However, in debilitated elderly patients, the values of Cmax and AUC increase significantly. Oxybutynin is extensively metabolized in the liver, primarily by cytochrome P450 enzymes, in particular CYP 3A4, which is found mainly in the liver and intestinal walls; its metabolites also have M-cholinoblocking effects. The main route of excretion is the kidneys.
Indication
Urinary incontinence, urgency or frequency of urination in cases of bladder instability due to neurogenic bladder dysfunction (detrusor hyperreflexia) as seen in diseases such as multiple sclerosis and spina bifida, or due to idiopathic detrusor instability (motor urge incontinence). Also used to control overactive bladder following bladder or prostate surgery or associated cystitis.
Application to children.
Oxybutynin hydrochloride is indicated for use in children for:
Urinary incontinence, urgency or frequency of urination in case of bladder instability due to idiopathic overactive bladder or neurogenic bladder dysfunction (detrusor overactivity); nocturnal enuresis associated with detrusor overactivity, in combination with non-drug treatment, in case of ineffectiveness of other therapy.
Contraindication
Hypersensitivity to the active substance or to any of the other components of the drug; myasthenia gravis; narrow-angle glaucoma or shallow anterior chamber of the eye; patients with fever or in conditions of increased ambient temperature, due to the risk of provoking hyperpyrexia; children under 5 years of age; esophageal dysfunction, including hiatal hernia; functional or organic gastrointestinal obstruction, including pyloric stenosis, paralytic ileus, intestinal atony; patients with ileostomy, colostomy, toxic megacolon; severe ulcerative colitis; patients with urinary tract obstruction when urinary retention may be exacerbated, for example with prostatic hypertrophy.
Interaction with other medicinal products and other types of interactions
When used simultaneously with lisuride, there is a risk of impaired consciousness, therefore regular clinical monitoring of patients is necessary.
Sibutin should be used with caution with other anticholinergic agents due to the possibility of potentiation of the anticholinergic effect.
There have been isolated reports of interactions between anticholinergics and phenothiazines, amantadine, neuroleptics (e.g. phenothiazines, butyrophenones, clozapine), other anticholinergic antiparkinsonian agents (e.g. biperiden, levodopa), antihistamines, quinidine, digitalis preparations, tricyclic antidepressants, atropine and related compounds such as atropine antispasmodics, and dipyridamole. Caution should be exercised when oxybutynin is used concomitantly with these medicinal products.
Due to decreased gastric motility, oxybutynin may impair the absorption of other drugs.
Oxybutynin is metabolized by the cytochrome P450 isoenzyme CYP3A4. Concomitant administration with a CYP3A4 inhibitor may inhibit the metabolism of oxybutynin and increase its exposure. Oxybutynin may antagonize prokinetics.
Patients should be advised that alcohol may increase drowsiness caused by anticholinergic agents such as oxybutynin.
Application features
The drug should be used with caution in elderly patients who may be more sensitive to the effects of oxybutynin and may require a dose reduction (see section "Method of administration and dosage"). The drug should also be used with caution in patients with autonomic neuropathy, gastrointestinal diseases, including severe gastrointestinal motility disorders, patients with hepatic or renal insufficiency or cerebrovascular insufficiency.
Anticholinergics should be used with caution in elderly patients due to the risk of cognitive impairment.
After taking the drug Sibutin, clinical manifestations of hyperthyroidism, coronary heart disease, chronic heart failure, arterial hypertension, prostatic hyperplasia, cardiac arrhythmias, and tachycardia may increase.
There have been reports of anticholinergic CNS effects (e.g. hallucinations, restlessness, confusion, somnolence). Observation is recommended, especially during the first few months after initiation of therapy or dose increase. If anticholinergic CNS effects develop, discontinuation of treatment or dose reduction should be considered (see section 4.5).
Since oxybutynin may cause angle-closure glaucoma, patients should be advised to seek immediate medical attention if they experience sudden loss of visual acuity or eye pain.
Oxybutynin is not considered safe for patients with porphyria because it has shown porphyrinogenicity in animal and in vitro studies.
Long-term use of the drug Sibutin may lead to the development of dental caries due to a decrease or cessation of salivation. In this regard, regular check-ups of the condition of the teeth are recommended during long-term use of the drug.
Anticholinergic drugs should be used with caution in patients who are concomitantly taking drugs (e.g. bisphosphonates) that may cause or exacerbate esophagitis.
In case of urinary tract infection, antibacterial therapy should be prescribed.
Patients with rare hereditary forms of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take Sibutin due to the lactose content.
Ability to influence reaction speed when driving vehicles or other mechanisms
The drug may cause decreased visual acuity or drowsiness. Patients should not drive or operate machinery unless it has been determined that the drug does not impair the patient's ability to perform physical or mental tasks.
Use during pregnancy or breastfeeding
The safety of oxybutynin during pregnancy has not been established. Oxybutynin should be avoided during pregnancy unless there are no safer alternatives.
The medicine should not be prescribed to women during breastfeeding.
Method of administration and doses
The drug is to be administered orally. The tablet can be divided into two equal doses.
Adults
The usual dose is 5 mg 2-3 times a day. The dose can be increased to a maximum of 5 mg 4 times a day to achieve a clinical effect, provided that adverse reactions are tolerated.
Elderly patients
In elderly patients, the half-life of the drug is increased, therefore, a dose of 2.5 mg 2 times a day is recommended, especially for debilitated patients. The dose can be increased to 5 mg 2 times a day to obtain a clinical effect, provided that adverse reactions are well tolerated.
Children from 5 years old
Neurogenic bladder instability, nocturnal enuresis: the usual dose is 2.5 mg 2 times a day. The dose may be increased to 5 mg 2-3 times a day to obtain a clinical effect, provided that adverse reactions are well tolerated. In nocturnal enuresis, the last dose should be taken before bedtime.
Children
The drug is contraindicated in children under 5 years of age. There are limited data on the possibility of using oxybutynin in children with monosymptomatic nocturnal enuresis (not associated with detrusor overactivity). The drug should be used with caution in children over 5 years of age, as they may be more sensitive to the effects of oxybutynin, in particular with regard to the manifestation of adverse reactions from the central nervous system and psyche.
Overdose
Symptoms. Symptoms of drug overdose develop in order from increased common central nervous system side effects (from restlessness and agitation to psychotic behavior) to circulatory disorders (hot flashes, low blood pressure, circulatory failure, etc.), respiratory failure, paralysis, and coma.
immediate gastric lavage; in case of severe anticholinergic syndrome that is life-threatening, neostigmine (or physostigmine) can be used in the dosage recommended in the instructions for medical use of these drugs; treatment of fever.
For severe anxiety or agitation, administer diazepam intravenously at a dose of 10 mg.
For tachycardia, administer propranolol intravenously.
In case of urinary retention, bladder catheterization is indicated.
In case of respiratory muscle paralysis, perform artificial ventilation of the lungs.
Adverse reactions
Gastrointestinal: nausea, constipation, dry mouth, abdominal discomfort, diarrhea, vomiting, gastroesophageal reflux, decreased appetite, anorexia, dysphagia, pseudo-obstruction in patients with risk factors (elderly or constipated patients taking other medications that reduce intestinal motility).
Infections and infestations: urinary tract infection.
Central nervous system: headache, dizziness, drowsiness, seizures, impaired cognitive function.
Psychiatric: agitation, hallucinations, nightmares, confusion, anxiety, paranoia, impaired cognitive function in elderly patients, symptoms of depression, addiction (in patients with a history of addiction to medications and other addictive substances), disorientation, delirium.
Immune system disorders: hypersensitivity.
Cardiac: tachycardia, cardiac arrhythmia.
Vascular: hot flashes (more pronounced in children than in adults).
On the part of the organs of vision: blurred vision, dilated pupils, increased intraocular pressure, angle-closure glaucoma and dry conjunctiva.
Injuries, poisoning and procedural complications: heat stroke.
Renal and urinary disorders: urinary retention, dysuria.
Skin and subcutaneous tissue disorders: dry skin, skin rash, urticaria, angioedema, hypohidrosis, photosensitivity.
Expiration date
3 years.
Storage conditions
Store in original packaging at a temperature not exceeding 25 ºС.
Keep out of reach of children.
Packaging
10 tablets in a blister; 3 blisters in a pack.
Vacation category
According to the recipe.
Producer
JSC "KYIV VITAMIN FACTORY".
Location of the manufacturer and its business address
04073, Ukraine, Kyiv, Kopylivska St., 38.
