Driptan - instructions for use, dose, side effects, contraindications

Active substanceOxybutyninOxybutynin

Similar drugsTo uncover

Driptan®

pills inwards

Laboratories SA Fournier. France

Novitrothane

pills inwards

STS Chemical Industries Co., Ltd. Israel

Dosage form: & nbsppills

Composition:

1 tablet contains:

active substance: hydroxybutynin hydrochloride 5.00 mg;

Excipients: cellulose microcrystalline 17.8 mg; lactose 153.3 mg; calcium stearate 1.9 mg.

Description:White round biconvex tablets with a risk on one side.

Pharmacotherapeutic group:antispasmodic

ATX: & nbsp

G.04.B.D Spasmolytics

G.04.B.D.04 Oxybutynin

Pharmacodynamics:

Oxibutinin has an antispasmodic effect on the detrusor's smooth muscle fibers, as well as an anticholinergic action, blocking the action of acetylcholine on smooth muscle m-cholinergic receptors. These properties help to relax the detrusor of the bladder. In patients with unstable bladder function, the drug increases the volume of the bladder and reduces the frequency of spontaneous detrusor cuts.

Pharmacokinetics:

Ingestion oxybutynin quickly absorbed in the gastrointestinal tract - maximum concentration (C_mOh) in plasma is reached in less than 1 hour, and then decreases biphasic with a half-life of 2-3 hours.The maximum effect is observed within 3-4 hours, the residual effect can persist for more than 10 hours.

The equilibrium concentration is achieved after 8 days of oral administration. In elderly patients who lead an active lifestyle, oxybutynin, apparently, does not accumulate, and its pharmacokinetics does not differ from that in the remaining adult patients. However, in attenuated elderly patients, the values of C_mOh and AUC (area under the curve "concentration-time") significantly increase. Oxybutynin is intensively metabolized in the liver, primarily by enzymes of the cytochrome P450 system, in particular CYP3A4, which is found mainly in the liver and intestinal walls; metabolites also possess m-cholinoblocking action. The main way of excretion through the kidneys. Only 0.3-0.4% of the unchanged drug is detected in urine in rats after 24 hours and 1% in urine in dogs after 48 hours. Consequently, in rats and dogs oxybutynin almost completely metabolized.

Indications:

Adults:

- Urinary incontinence, urgency to urinate and frequent urination associated with instability of the bladder function, either as a result of neurogenic disorders (detrusor hyperreflexia) in diseases such as multiple sclerosis and spina bifida, or due to idiopathic detrusor function (motor urgent urinary incontinence);

- hyperactivity of the bladder that occurs after surgery on the bladder or prostate gland, or with concomitant cystitis.

Children over 5 years:

- urinary incontinence, urgency to urinate and frequent urination associated with unstable bladder function, either as a result of idiopathic hyperactivity of the bladder or bladder dysfunction of a neurogenic nature (detrusor hyperactivity);

- nocturnal enuresis associated with detrusor hyperactivity, in combination with non-medicamentous methods with ineffectiveness of other therapy.

Contraindications:

- Hypersensitivity to the active substance or to any of the excipients;

- myasthenia gravis;

- an angle-closure glaucoma or a small anterior chamber of the eye;

- patients with hyperthermia or in conditions of high ambient temperature because of the risk of heat stroke;

- children under 5 years due to lack of data on efficiency and safety;

- violation of the function of the esophagus, including hernia of the esophageal aperture of the diaphragm;

- functional or organic obstruction of the gastrointestinal tract (GI tract), including pyloric stenosis, 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 by t.ch. hypertrophy of the prostate;

- the period of breastfeeding.

Due to the fact that the preparation contains lactose, Driptan® is contraindicated in congenital galactosemia, glucose-galactose malabsorption, lactase deficiency, galactose intolerance.

Carefully:

- Elderly people due to the fact that they may be more sensitive to the action of the drug (a dose reduction may be required, see section "Dosing and Administration");

- pathology of the autonomic nervous system;

- other severe gastrointestinal diseases not listed in the "Contraindications" section;

- hepatic or renal insufficiency;

- cerebrovascular disorders;

- children older than 5 years due to the fact that they may be more sensitive to the effect of the drug, especially with regard to the development of side effects from the nervous system and mental disorders;

- Pregnancy (see p.section "Application during pregnancy and during breast-feeding").

Elderly patients should be cautious about taking anticholinergics because of the risk of cognitive impairment. After the appointment of oxybutynin, symptoms of hyperthyroidism, coronary artery disease, chronic heart failure, hypertension, prostatic hyperplasia, as well as cardiac rhythm disturbances, tachycardia can be aggravated.

Anticholinergic effects from the nervous system (eg, hallucinations, agitation, confusion, drowsiness) were noted. It is recommended to monitor the condition, especially in the first few months of treatment after starting therapy or increasing the dose. Consideration should be given to discontinuing therapy or lowering the dose in the event of the development of effects from the nervous system (see section "Interaction with other drugs").

Due to oxybutynin may be the cause of the development of an angle-closure glaucoma, it is necessary to consult a doctor immediately if there is a sudden loss of visual acuity or pain in the eyes.

Caution should be exercised when taking oxybutynin in patients with porphyria, as in the animal and in vitro tests the drug caused an increase in the synthesis of porphyrinogens.

Long-term administration of oxybutynin can promote the development of caries by reducing or suppressing the production of saliva. With prolonged intake of the drug, regular follow-up at the dentist is necessary.

It is necessary to take with caution anticholinergic drugs simultaneously with drugs (such as bisphosphonates), which can cause or exacerbate esophagitis.

Pregnancy and lactation:

Pregnancy

The safety of oxybutynin during pregnancy is not established. Animal studies have shown that the use of the drug in doses that have a toxic effect on the maternal organism causes reproductive toxicity. Available animal studies are not sufficient to assess the effect of the drug on pregnancy, embryonic development, childbirth or postnatal development.

The drug should not be used in pregnant women,when the intended use for the mother from its use exceeds the potential risk to the fetus.

Breastfeeding period

In animal studies, it has been established that oxybutynin is found in breast milk. Accordingly, the drug should not be used during breastfeeding.

Dosing and Administration:

Inside (oral). 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, giving a satisfactory clinical result with good tolerability.

Elderly patients

In elderly patients, the elimination half-life can be increased, so an initial dose of 2.5 mg twice a day is usually sufficient, especially in weakened patients. With good tolerability, the dose can be increased to 5 mg twice a day.

Children (over 5 years)

With unstable function of the bladder: 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 per day with good tolerability.

Night enuresis: 2.5 mg twice 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 (up to 5 years)

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

Side effects:

Often (>1/10)	Often (from> 1/100 to <1/10)	Infrequently (from> 1/1000 to <1/100)	The frequency is unknown (it is impossible to estimate the frequency based on the available data)
Infectious and parasitic diseases
			urinary tract infection
Disorders from the gastrointestinal tract
nausea, constipation, dry mouth	diarrhea, vomiting	abdominal discomfort, anorexia, decreased appetite, dysphagia	gastroesophageal reflux
Disorders of the psyche
	confusion		agitation, anxiety, hallucinations, nightmarish dreams, paranoia, cognitive impairment in elderly patients, disorientation, delirium
Disturbances from the nervous system
dizziness, headache, drowsiness			cognitive disorders, convulsions
Heart Disease
			tachycardia, arrhythmia
Trauma, intoxication and complications of manipulation
			heatstroke
Disturbances on the part of the organ of sight
	dry eyes		closed angle glaucoma, mydriasis, increased intraocular pressure, blurred vision
Disorders from the kidneys and urinary tract
	retention of urination		dysuria
Vascular disorders
	"tides" of blood *
Disturbances from the skin and subcutaneous tissues
dry skin			angioedema, rash, hives, hypohydrosis, photosensitivity
Impaired immune system disorders
			hypersensitivity

* more pronounced in children than in adults

Overdose:

Symptoms overdoses of oxybutynin gradually increase from the increase of usual side effects from the side of the central nervous system (from anxiety and emotional arousal to psychotic behavior), circulatory disorders (blood flushes, falling blood pressure, circulatory failure, etc.) to respiratory failure, paralysis and coma .

Treatment with an overdose symptomatic:

1. Immediate gastric lavage.

2. In the case of development of a life-threatening anticholinergic syndrome, neostigmine (or physiostigmine) can be used in doses according to the instructions for medical use.

Symptomatic treatment in case of fever.With significant excitation or irritability, 10 mg of diazepam should be administered intravenously.

In the case of tachycardia, intravenously propranolol.

If urination is delayed, use a catheter.

In the case of paralysis of the respiratory muscles, artificial ventilation is necessary.

Interaction:

Care should be taken when using Driptan® with other anticholinergic drugs because of the possible increase in anticholinergic action.

There have been reports of rare interactions between anticholinergic drugs and phenothiazines, amantadine, neuroleptics (eg phenothiazines, butyrophenones, clozapine) with other anticholinergic antiparkinsonian drugs (eg biperidin, levodopa), antihistamines, quinidine, digitalis, tricyclic antidepressants, atropine, atropine-like antispasmodics and dipyridamole. Caution should be exercised when Driptan® is used simultaneously with these preparations.

The drug may affect the absorption of other medicines, reducing the motility of the gastrointestinal tract.

Oxybutynin is metabolized by cytochrome P450 isoenzyme CYP3A4. Simultaneous reception with inhibitors CYP3A4 can inhibit the metabolism of oxybutynin and enhance its action. Oxybutynin can reduce the effects of prokinetic therapy.

Simultaneous administration of oxybutynin with cholinesterase inhibitors may lead to a decrease in the effectiveness of the latter.

Alcohol can increase drowsiness caused by taking such anticholinergic drugs as oxybutynin.

Effect on the ability to drive transp. cf. and fur:

The drug may cause drowsiness or blurred vision. Patients should refrain from driving or other mechanisms, except when their physical and mental abilities have not changed.

Form release / dosage:

Tablets, 5 mg.

Packaging:

For 30 tablets in a blister of PVC / Aluminum foil.

For 1 or 2 blisters together with instructions for use in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014671 / 01

Date of registration:15.12.2008

The owner of the registration certificate:Laboratories SA Fournier.Laboratories SA Fournier. France

Manufacturer: & nbsp

RECIPHARM FONTAINE France

Representation: & nbspABBOTT LABORATORIES LLC ABBOTT LABORATORIES LLC Russia

Information update date: & nbsp10.08.2015

Illustrated instructions

Instructions

Driptan® (Driptane®)