Desmopressin - 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 3-5%. 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 of cysteine-1 affords it resistance to enzymatic decay, which is expressed in a much 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:

- Non-diabetes mellitus of the central genesis;

- diagnostic test for the concentration ability of the kidneys.

Contraindications:

Hypersensitivity to the components of the drug, the syndrome of inadequate secretion of antidiuretic hormone, plasma hypo-osmolality, decompensated heart failure (including in the history), the need for diuretic therapy, hyponatremia, polydipsia (congenital or psychogenic), as well as allergic rhinitis, nasal congestion, edema and cicatricial changes in the nasal mucosa, upper respiratory tract infections; impaired consciousness.

Carefully:

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

Pregnancy and lactation:

Despite the very low activity of desmopressin in the stimulation of labor, it should be administered to pregnant patients with caution and only if the potential benefit to the mother exceeds the possible risk to the fetus.

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.

The use of the drug in children should be carried out under the supervision of adults.

Non-diabetes mellitus of central origin

The dose is selected individually, however, as clinical experience shows,

the average daily dose in adults is 10-40 μg, in children 10-20 μg (one or two clicks on the dosing device (10-20 μg) once or twice a day.) This daily dose can be given once or can be divided into 2-3 reception.

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 liquid (the volume of fluid that entered the body 1 hour before the test and within 8 hours after it should not exceed 0.5 liters).

For most patients, the normal osmolality of urine after administration of Desmopressin 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 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, 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, weight gain, swelling 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, desmopressin should be immediately withdrawn and the fluid intake reduced to the normal level of sodium in the serum, in severe cases - 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:

It is necessary to show special caution in patients at risk of intracranial hypertension; patients with a violation of water and / or electrolyte balance and patients with disorders in which Hyperhydration of the body can be dangerous, for example, a violation of kidney function, heart failure, cystic fibrosis or anesthesia.

Before prescribing the drug Desmopressin 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 conditions hospital.

To prevent fluid retention, care should be taken after conducting diagnostic tests to identify diabetes insipidus or to examine the concentration the ability of the kidneys. Do not do it to force the introduction of a liquid orally, parenterally, and patients should take as much fluid as they need to quench thirst.

Do not use Desmopressin with changes in the mucous membrane of the nasal cavity, such as: scars, edema or other diseases, as this can lead to uneven and incomplete absorption.

In patients with nasal disorders, including catarrhal diseases, there is a risk of unstable and / or reduced efficacy medicinal product. 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.

A drug Desmopressin Do not administer to children who require doses less than 10 μg of desmopressin (in the form of acetate).

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

Admission of the drug does not adversely affect the ability to manage car and other mechanisms.

Form release / dosage:

Spray nasal dosed, 10 mcg / dose.

Packaging:

5 ml (50 doses) in a vial of dark glass with a dosing device.

The bottle with instructions for use is placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004295/09

Date of registration:29.05.2009

Expiration Date:Unlimited

The owner of the registration certificate:AKTAVIS GROUP, AO AKTAVIS GROUP, AO Iceland

Manufacturer: & nbsp

INPAC, AS Norway

Representation: & nbspAktavis, Open Company Aktavis, Open Company

Information update date: & nbsp25.03.2017

Illustrated instructions

Instructions

Desmopressin (Desmopressin)