Driptan, pills 5mg, 30pcs

Composition

1 tablet contains: Active ingredient: oxybutynin hydrochloride – 5.00 mg. Auxiliary substances: microcrystalline cellulose – 17.8 mg; lactose-153.3 mg; calcium stearate-1.9 mg

Pharmacological action

Pharmacodynamics

Oxybutynin has an antispasmodic effect on detrusor smooth muscle fibers, as well as an anticholinergic effect, blocking the action of acetylcholine on smooth muscle m-holinoreceptors. These properties contribute to the relaxation of the bladder detrusor. In patients with unstable bladder function, the drug increases the volume of the bladder and reduces the frequency of spontaneous detrusor contractions.

Pharmacokinetics

When taken orally, oxybutynin is rapidly absorbed in the gastrointestinal tract – the maximum concentration (Cmax) in plasma is reached in less than 1 hour, and then decreases in two phases with a half-life of 2-3 hours. The maximum effect is observed within 3-4 hours, the residual effect can last for more than 10 hours.

The equilibrium concentration is reached after 8 days of oral use of the drug. In elderly patients who lead an active lifestyle, oxybutynin does not seem 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 (area under the concentration-time curve) significantly increase. Okibutinin is extensively metabolized in the liver, primarily by cytochrome P450 enzymes, in particular CYP3A4, which is found mainly in the liver and intestinal walls; the metabolites also have a M-holinoblocking effect.

The main route of elimination is through the kidneys. Only 0.3-0.4% of the unchanged drug is detected in the urine of rats after 24 hours and 1% in the urine of dogs after 48 hours. Consequently, oxybutynin is almost completely metabolized in rats and dogs.

Indications

Adults – urinary incontinence, urgent urge to urinate and frequent urination associated with instability of bladder function, resulting either as a result of neurogenic disorders (detrusor hyperreflexia) in diseases such as multiple sclerosis and spina bifida, or due to idiopathic disorders of detrusor function (motor emergency urinary incontinence). – hyperactivity of the bladder that occurs after surgery on the bladder or prostate, or with concomitant cystitis. Children over 5 years of age – urinary incontinence, urgent urination and frequent urination associated with unstable bladder function, either as a result of idiopathic bladder hyperactivity or neurogenic bladder dysfunction (detrusor hyperactivity);- nocturnal enuresis associated with detrusor hyperactivity, in combination with non-drug methods, if other therapy is ineffective.

Use during pregnancy and lactation

Pregnancy safety of oxybutynin use during pregnancy has not been established. Animal studies have shown that the use of the drug in doses that have a toxic effect on the maternal body causes reproductive toxicity. Available animal studies are not sufficient to assess the effect of the drug on pregnancy, fetal development, childbirth, or postnatal development. The drug should not be used in pregnant women, except in cases where the intended benefit to the mother from its use exceeds the potential risk to the fetus. Breast-feeding periodin animal studies, oxybutynin is found in breast milk. Accordingly, the drug should not be used during breastfeeding.

Contraindications

-hypersensitivity to the Active ingredient or to any of the excipients;- myasthenia gravis;- angle – closure glaucoma or small anterior chamber of the eye;-patients with hyperthermia or in conditions of high ambient temperature due to the risk of heat stroke;- children under 5 years of age due to insufficient data on efficacy and safety;- esophageal dysfunction, including hiatal hernia;- functional or organic obstruction of the gastrointestinal tract (GI), including pylorostenosis, paralytic intestinal obstruction, intestinal atony;-presence of ileostomy, colostomy, toxic expansion of the colon (megacolon), severe ulcerative colitis; – infravesical obstruction of the bladder, in which urinary retention can be caused, including prostatic hypertrophy;- the period of breastfeeding. Due to the fact that the drug contains lactose, Driptan® is contraindicated in congenital galactosemia, glucose-galactose malabsorption, lactase deficiency, galactose intolerance.

With caution

– elderly people due to the fact that they may be more sensitive to the action of the drug (it may be necessary to reduce the dose, see the section “Dosage and use”);- pathology of the autonomic nervous system;- other serious diseases of the gastrointestinal tract that are not listed in the section “Contraindications”;- hepatic or renal insufficiency; – cerebrovascular disorders; – children over 5 years of age due to the fact that they may be more sensitive to the action of the drug, especially with regard to the development of side effects from the nervous system and mental disorders;- pregnancy (see the section “Use during pregnancy and lactation”).

Elderly patients should take anticholinergic medications with caution because of the risk of cognitive impairment.

After the appointment of oxybutynin, symptoms of hyperthyroidism, coronary vascular diseases, chronic heart failure, arterial hypertension, prostatic hyperplasia, as well as heart rhythm disorders, tachycardia may increase.

Anticholinergic effects from the nervous system were noted (for example, hallucinations. agitation, confusion, drowsiness). Monitoring of the condition is recommended, especially in the first few months of treatment after starting therapy or increasing the dose.

Consideration should be given to discontinuing therapy or reducing the dose in case of nervous system effects (see section “Interactions with other medicinal products”).

Due to the fact that oxybutynin may cause the development of angle-closure glaucoma, you should immediately consult a doctor if you suddenly lose visual acuity or have eye pain.

Caution should be exercised when taking oxybutynin in patients with iorphyria, as the drug has caused an increase in porphyrinogen synthesis in animal studies and in vitro.

Long-term use of oxybutynin may contribute to the development of tooth decay by reducing or suppressing saliva production. If you are taking the drug for a long time, you should be regularly monitored by a dentist.

Anticholinergic medications should be taken with caution at the same time as medications (such as bisphosphonates). which can cause or exacerbate esophagitis.

Side effects

Nausea, constipation, diarrhea, abdominal discomfort, urinary retention, drowsiness or insomnia, general weakness, headache, dizziness, arrhythmia, visual disturbances (mydriasis, accommodation paralysis), increased intraocular pressure, decreased sweating, dry mouth, impotence, allergic reactions.

Interaction

Caution should be exercised when using Driptan® with other anticholinergic drugs due to the possible increase in anticholinergic action. There have been reports of rare interactions between anticholinergic drugs and phenothiazines, amantadine, neuroleptics (e. g., phenothiazines, butyrophenones, clozapine), other anticholinergic antiparkinsonian drugs (e. g., biperidone, lsvodoi), antihistamines, quinidine, digitalis preparations, tricyclic antidepressants, atropine, atropine-like drugs, and other anticholinergic drugs. antispasmodics and dipyridamole. Caution should be exercised when using Driptan® concomitantly with these medications. The drug may affect the absorption of other drugs, reducing gastrointestinal motility. Oxybutyin is metabolized by the cytochrome P450 isoenzyme CYP3A4. Concomitant use with CYP3A4 inhibitors may inhibit the metabolism of oxybutyline and enhance its action. Oxybutyline may reduce the effects of prokinetic therapy. Concomitant use of oxybutynin with cholinesterase inhibitors may reduce the effectiveness of the latter. Alcohol can increase drowsiness caused by taking anticholinergic drugs such as oxybutynin.

How to take it, course of use and dosage

Inside (by mouth). The tablet can be divided into two equal parts.

Adults

The usual dose of the drug is 5 mg 2-3 times a day. If necessary, it is possible to increase the dose to 5 mg 4 times a day, which gives a satisfactory clinical result with good tolerability.

Elderly patients

In elderly patients, the elimination half-life may be prolonged, so an initial dose of 2.5 mg 2 times a day is usually sufficient, especially in debilitated patients. If well tolerated, the dose can be increased to 5 mg 2 times a day.

Children (over 5 years old)

In case of unstable bladder function: the usual dose of the drug is 2.5 mg 2 times a day. To achieve a clinical response, the dose can be increased to 5 mg 2-3 times a day if well tolerated.

Nocturnal enuresis: 2.5 mg 2 times a day. To achieve a clinical response, the dose can be increased to 5 mg 2-3 times a day, provided that it is well tolerated. The last dose should be taken at night.

Children (under 5 years old)

The use of Driptan® in children under 5 years of age is contraindicated (see the section “Contraindications”).

Overdose

Symptoms of oxybutynin overdose gradually increase from an increase in the usual side effects from the central nervous system (from anxiety and emotional arousal to psychotic behavior), circulatory disorders (“hot flashes” of blood, a drop in blood pressure, circulatory failure, etc. ) to respiratory failure, paralysis and coma.

Treatment for overdose is symptomatic:

1. Immediate gastric lavage. 2. If a life-threatening anticholinergic syndrome develops, neostigmine bromide (or physostigmine) may be used in doses according to the instructions for medical use.

Symptomatic treatment in case of fever. In case of significant agitation or irritability,10 mg of diazspam should be administered intravenously.

If tachycardia develops, propranolol should be administered intravenously. If urination is delayed, use a catheter. In case of paralysis of the respiratory muscles, artificial ventilation is necessary.

Special instructions

Caution is necessary in cases of impaired renal and hepatic function, hyperthyroidism, coronary heart disease, heart failure, arrhythmia, arterial hypertension, prostate adenoma, hiatal hernia.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Oxybutynin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults by doctor’s prescription, Children by doctor’s prescription, Children over 5 years of age

Indications

Enuresis