Included in the formulation
АТХ:G.04.B.D Spasmolytics
G.04.B.D.04 Oxybutynin
Pharmacodynamics:The drug is a non-selective blocker of M3-cholinergic receptors. The drug reduces the tone of smooth muscles: GIT, bile and urinary tract, uterus, especially well relaxes the smooth muscles of the bladder. In patients with a neurogenic bladder, it increases its capacity, relaxes and reduces the frequency of detrusor cuts, restrains urge and reduces the number of urination (involuntary and voluntary).
Pharmacokinetics:Absorption is fast. The volume distribution of 193 liters. Biotransformation in the liver (CYP3A4), metabolites - phenylcyclohexylglycolic acid and desethyloxybutynin. Maximum concentration is achieved (usual tablets after ingestion) after 45 minutes. Half-life (sustained-release tablets) 13.2 h for R-oxybutynin and 12.4 h for S-oxybutynin. Maximum concentration in adults 1 ng / l for R-oxybutynin and 1.8 ng / l for S-oxybutynin, in children 0.7 ng / l for R-oxybutynin and 1.3 ng / L for S-oxybutynin. Elimination mainly by the kidneys.
The elimination half-life is 2 hours.
Indications:Urinary incontinence, nocturnal enuresis in children. Neurogenic bladder (including hyperreflexia of detrusor in multiple sclerosis or spina bifida).
XIV.N30-N39.N30 Cystitis
V.F90-F98.F98.0 Enuresis of inorganic nature
XIV.N30-N39.N31 Neuromuscular dysfunction of the bladder, not elsewhere classified
XIV.N30-N39.N31.2 Neurogenic weakness of the bladder, not elsewhere classified
XVIII.R30-R39.R30.0 Dizuria
XVIII.R30-R39.R32 Urinary incontinence, unspecified
Contraindications:Intestinal obstruction, impairment of urine outflow from the bladder, obstructive disorders GIT, paralytic ileus, severe ulcerative colitis, enlargement of the colon (including toxic, complicated with ulcerative colitis), intestinal atony, uropathy of obstructive etiology, age under 5 years, myasthenia gravis, breast-feeding, glaucoma, hypersensitivity, acute bleeding with unstable parameters of the cardiovascular system, pregnancy.
Carefully:Diseases of the liver, kidneys, thyrotoxicosis, advanced age, IHD, chronic heart failure, arrhythmias, hypertension, prostatic hyperplasia, diaphragmatic hernia, diarrhea accompanying incomplete intestinal obstruction (especially in patients with ileo- or colostomy), elderly age.
Pregnancy and lactation:Category FDA - B. The drug is contraindicated in pregnancy and lactation.
Dosing and Administration:Orally.
Adults: 5 mg 2-3 times a day.
Children older than 5 years: 2.5-3 mg 2 times a day. Then the dose can be increased to 5 mg 2-3 times a day.
Elderly patients: 2.5-3 mg twice a day, if necessary, increase the dose to 5 mg 2 times a day. At night enuresis - last reception before a dream.
Side effects:From the side nervous system: drowsiness, dizziness, decreased visual acuity.
From the side digestive system: nausea, dry mouth, constipation, diarrhea, abdominal pain.
Other: dry skin, difficulty urinating, hot flashes, arrhythmias, urinary retention.
Overdose:Symptoms: excitation CNS (anxiety, tremor, irritability, convulsions, delirium, hallucinations), face redness, fever, nausea, vomiting, tachycardia, hypo- or hypertension, respiratory failure, paralysis, coma.
Treatment: maintenance of respiratory function, induction of vomiting, gastric lavage; it is possible to use activated carbon and laxatives; To reverse the symptoms of anticholinergic intoxication, physostigmine is prescribed; with hyperpyrexia - cold compresses, including with ice, alcohol wiping.
Interaction:Ketoconazole, itraconazole and other inhibitors of CYP3A4 - a change in the pharmacokinetics of oxybutynin (increase the concentration of the drug).
Anticholinergic drugs increase the side effects of oxybutynin.
Ethanol and sedatives increase dizziness and drowsiness.
Amantadine strengthens (mutually) cholinolytic effect.
On the background haloperidol the likelihood of increased intraocular pressure increases.
Nitroglycerine. Oxibutinin weakens salivation and causes dry mouth, thereby hampering sublingual absorption.
Pilocarpine in the form of eye drops increases (mutually) a decrease in the production of intraocular fluid. Against the background of the systemic action of pilocarpine, the probability of conduction disruption increases.
On the background propofol (postnarcosis period), the hypnotic effect increases.
Risedronic acid. Against the background of oxybutynin, the risk of gastrointestinal tract damage (esophagitis, gastritis, gastroduodenitis, etc.) increases.
Cisapride increases (mutually) the frequency and / or severity of anticholinergic side effects, such as dry mouth, constipation, drowsiness, etc.
Ethidronic acid. On the background of oxybutynin, the risk of GI tract damage (esophagitis, gastritis,gastroduodenitis and others).
Special instructions:Impact on the ability to drive vehicles and manage mechanisms.
They are used with caution in patients whose activity requires increased concentration of attention, high speed of psychomotor reactions.