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

Structural changes in the arginine-vasopressin molecule (deamination of cysteine at position 1 and substitution L-arginine on D-arginine at position 8) cause a decrease in vasopressor activity and an increase in the antidiuretic effect of desmopressin. The drug increases the permeability of the epithelium of the distal sections of the convoluted tubules of the kidneys for water and increases its reabsorption. The use of desmopressin leads to a decrease in the volume of excreted urine and a simultaneous increase in the osmolarity of the urine and a decrease in the osmolarity of the blood plasma. This leads to a decrease in the frequency of urination and a decrease in nocturnal polyuria.

Antidiuretic activity manifests itself 15-30 minutes after dosing, reaches clinically significant within 1 hour and remains high for 8 hours after dosing.

Pharmacokinetics:

Bioavailability of desmopressin with intranasal administration is about 10%.

After the administration of 20 μg desmopressin is detected in the plasma after 15 minutes. The maximum concentration after intranasal administration is achieved after 1 hour. Desmopressin binds to proteins in a very small degree. It is excreted in human breast milk in low concentration. Desmopressin, like vasopressin, is metabolized mainly in the liver and kidneys.However deamination cysteine-1 gives it a resistance to enzymatic degradation, resulting in a significantly longer half-life of desmopressin. The half-life is about 4 hours. There is no information about enterohepatic circulation and the pharmacological activity of its metabolites.

Indications:

- Hdiabetes mellitus of central origin;

- primary nocturnal enuresis in children 5 years of age or older;

- diagnostic test for the concentration ability of the kidneys.

Contraindications:

Increased sensitivity to the drug, anuria, edema syndrome of various genesis, antidiuretic hormone syndrome of inappropriate secretion, plasma gipoosmolyarnost, decompensated heart failure (including history), the need for a diuretic therapy, hyponatremia, habitual polydipsia (congenital or psychogenic), predisposition to thrombosis, as well as allergic rhinitis, nasal congestion, swelling and scarring of the nasal mucosa, upper respiratory tract infections; impaired consciousness.

Carefully:

With kidney failure, fibrosis of the bladder, children under 1 year old and elderly,when violations of water-electrolyte balance, the potential risk of increased intracranial pressure, during pregnancy.

Pregnancy and lactation:

Preseyneks should be administered with caution to pregnant patients, despite the very low activity of desmopressin in stimulating labor.

The harmful effect of desmopressin on the fetus is not revealed.

The amount of desmopressin that can be transferred to a newborn with mother's milk is significantly less than that necessary to affect diuresis. However, it is advisable to exercise caution when prescribing treatment for breastfeeding women.

Dosing and Administration:

The drug is intended for intranasal administration.

Primary night enuresis

The initial dose for children (starting from 5 years) and for adults (up to age 65 years) who have primary nocturnal enuresis but with normal renal concentra- tion is 20 μg - one push of the dosing device (10 μg) in each nasal passage at night before bedtime.

If necessary, the dose should be increased to 40 mcg - two clicks on the dosing device (20 mcg) in each nasal passage.

The decision to continue treatment is taken after 3 months of continuous therapy on the basis of clinical data that will be observed after the drug is discontinued within one week.

In the case of treatment of enuresis, fluid intake should be limited to a minimum - only to quench thirst for 1 hour before and within 8 hours - after administration of the drug.

Non-diabetes mellitus of central origin

The dose is selected individually, however, according to clinical experience, the average daily dose in adults is 10-40 mcg, in children 10-20 mcg (one or two clicks on the dosing device (10-20 mcg) once or twice a day. This daily dose can be given once or it can be divided into 2-3 doses.

Test for the concentration ability of the kidneys

To determine the concentration ability of the kidneys, the following average doses are used: for adults, 40 μg; children older than 1 year - 10-20 mcg; children under the age of 1 year - 10 mcg.

Immediately after the administration of the drug, the patient must empty the bladder and during the test and 4 hours after the end of the application (only 8 hours), 2 portions of urine are taken to measure its osmolality.During the test, it is necessary to limit the intake of fluid (the volume of fluid that entered the body 1 hour before the test and within 8 hours after, should not exceed 0.5 liters).

For most patients, the normal urine osmolality after prescription is 800 mOsm / kg. In children, a urine concentration of 600 mOsm / kg should be achieved within 5 hours after the administration of the drug. If the osmolality index is found to be lower than this value, then the study should be repeated. Re-detection of a low value indicates a violation of the concentration ability of the kidneys, in which case the patient needs additional examination.

Side effects:

There may be: headache, abdominal pain, nausea, edema of the nasal mucosa, rhinitis and nosebleeds.

In rare cases, there are allergic reactions to the components of the drug in the form of skin manifestations.

In isolated cases - dizziness, increased blood pressure, algodismenorea, conjunctivitis, reduced tearing.

Treatment with desmopressin without a simultaneous decrease in fluid intake may be accompanied by fluid retention in the body,accompanied by hyponatremia, increased body weight, edema and in severe cases - transient neurologic disorders, mainly generalized seizures.

Overdose:

Overdose increases the risk of fluid retention and leads to seizures. In the case of hyponatremia, Presinex treatment should be immediately abolished and the fluid intake reduced to normalize the sodium level in the serum, in severe cases, a slow intravenous infusion of concentrated saline solutions simultaneously with furosemide.

Interaction:

Indomethacin may increase, but not increase, the duration of action of desmopressin.

Oral hypoglycemic agents, for example, glibenclamide, can reduce the duration of desmopressin.

Therapy in combination with drugs that cause the release of antidiuretic hormone and enhance anti-diuretic activity or disrupt the water-electrolyte balance, for example, tricyclic antidepressants (chlorpromazine and carbamazepine), clofibrate and chlorpropamide, increases the antidiuretic effect and increases the risk of fluid retention in the body.

Glybutide, tetracycline, lithium, norepinephrine weaken the antidiuretic effect.

Desmopressin enhances the action of hypertensive drugs.

Special instructions:

Care should be taken with regard to patients at risk of intracranial hypertension; patients with disturbed water and / or electrolyte balance and patients with disorders in which the hyperhydration of the body can be dangerous, for example, renal dysfunction, heart failure, cystic fibrosis or anesthesia.

Before prescription of Presayneks it is necessary to exclude diagnoses of psychogenic polydipsia and alcoholism.

The test for the concentration of kidneys in children under the age of 1 year should be performed only in a hospital.

Patients receiving treatment for primary nocturnal enuresis should be warned about the need to avoid excessive fluid intake and the need to stop taking Presaynex in case of vomiting and / or diarrhea until they restore normal fluid balance in the body.

To prevent fluid retention, care should be taken after conducting diagnostic tests to identifydiabetes insipidus or a study of the concentration ability of the kidneys. Do not force the injection of the fluid, either orally or parenterally, and patients should take as much fluid as they need to quench their thirst.

Presayneks should not be used in mucosal changes such as scars, edema or other diseases, as this can lead to uneven and unreliable absorption.

In patients with nasal disorders, including catarrhal diseases, there is a risk of unstable and / or reduced efficacy of the drug. This can also be observed in patients engaged in this type of activity, in which the drug can be removed from the nasal cavity before it is sucked, for example, when swimming.

Presinex should not be given to children who need doses less than 10 μg of desmopressin (in the form of hydrate acetate).

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

The intake of the drug does not adversely affect the ability to drive and other mechanisms.

Form release / dosage:Spray nasal dosed, 0.1 mg / ml.

Packaging:

6 ml (60 doses) solution in a vial with a metering device with a sprayer and a protective cap with an instruction embedded in the cardboard box.

Storage conditions:

In a place protected from light and inaccessible to children.

Do not freeze.

Store in an upright position.

At 25 ° C or lower PRESAYNEKS preparation can be stored for 1 month.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LS-002057

Date of registration:26.03.2012

The owner of the registration certificate:PIICH & TH C.P.L.PIICH & TH C.P.L. Italy

Manufacturer: & nbsp

MIPHARM, S.P.A. Italy

Information update date: & nbsp15.01.2016

Illustrated instructions

Instructions

Presinex (Presinex)