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

Desmopressin is a structural analogue of the natural hormone arginine-vasopressin, obtained as a result of changes in the structure of the vasopressin molecule-deamination of 1-cysteine and replacement of 8-L-arginine on the 8-D-arginine. These structural changes result in a combination with a significantly enhanced antidiuretic ability to have a less pronounced effect on the smooth muscles of the vessels and internal organs compared with vasopressin, which leads to the absence of undesirable spastic side effects. In contrast, vasopressin acts longer and does not cause an increase in blood pressure. The drug increases the permeability of the epithelium of the distal convoluted tubules of the nephron 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.

The maximum antidiuretic effect occurs when ingested after 4-7 hours.Antidiuretic effect with oral administration in a dose of 0.1-0.2 mg - up to 8 hours, at a dose of 0.4 mg - up to 12 hours.

Pharmacokinetics:

Suction

Absorption on intake is 5%. The time to reach the maximum concentration of desmopressin in the blood plasma (TS_mOh) is 2 hours. Simultaneous intake of food can reduce the degree of absorption by 40%. Absolute bioavailability with oral administration varies from 0.08% to 0.16%.

Distribution

The volume of distribution is 0.2-0.3 l / kg. Desmopressin does not penetrate the blood-brain barrier.

Metabolism

Metabolised in the kidneys.

Excretion

It is excreted by the kidneys. The half-life at ingestion (T₁_/₂) - 2-3 hours.

Indications:

- Non-diabetes mellitus of central origin;

- primary nocturnal enuresis in children older than 5 years;

- nocturnal polyuria in adults (as symptomatic therapy).

Contraindications:

- Hypersensitivity to desmopressin or other components of the drug;

- habitual or psychogenic polydipsia;

- heart failure and other conditions requiring the appointment of diuretics;

- hyponatremia, including in the anamnesis;

- renal failure of moderate and severe severity (creatinine clearance (CC) below 50 ml / min);

- syndrome of inappropriate production of antidiuretic hormone;

- children under 4 years (for treatment of diabetes insipidus) and 5 years (for treatment of primary nocturnal enuresis).

Pregnancy and lactation:

Pregnancy

According to known data, when using desmopressin in pregnant women with diabetes insipidus, there was no adverse effect on the course of pregnancy, on the health of the pregnant, fetus and newborn. However, before using desmopressin, the ratio of expected benefit to the mother and the potential risk to the fetus should be assessed.

Breastfeeding period

Studies have shown that the amount of desmopressin entering the body of a newborn with breast milk from a woman taking high doses of desmopressin is significantly less than that which can affect diuresis.

Dosing and Administration:

The optimal dose of desmopressin is selected individually. The drug should be taken orally after some time after eating, since eating can affect the absorption of the drug and its effectiveness.

Non-diabetes mellitus of central origin:

The recommended initial dose for children over 4 years and adults - 0.1 mg 1-3 times in day. AT the subsequent dose is changed depending on the response to the treatment.Usually the daily dose is in the range of 0.2-1.2 mg. For most patients, the optimal maintenance dose is 0.1-0.2 mg 1-3 times a day.

Primary night enuresis:

The recommended starting dose is 0.2 mg per night. In the absence of effect, the dose may be increased to 0.4 mg. It is necessary to monitor compliance with the restriction of fluid intake in the evening. The recommended course of continuous treatment is 3 months. The decision to continue treatment should be made on the basis of clinical data, which will be observed after the drug is discontinued within 1 week.

Nocturnal polyuria in adults:

The recommended starting dose is 0.1 mg per night. In the absence of effect within 1 week, the dose is increased to 0.2 mg and subsequently to 0.4 mg with increasing dose at a frequency of no more than 1 time per week. Remember the danger of fluid retention in the body. If after 4 weeks of treatment and dose adjustments adequate clinical effect is not observed, continue taking the drug is not recommended.

Side effects:

The following side effects noted with the use of desmopressin are distributed according to the frequency of occurrence according to the following gradation: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000,<1/1000); extremely rare (<1/10000); unspecified frequency (can not be determined from available data).

Immune system disorders: rarely - Allergic reactions.

Disturbances from the nervous system: often - headache, dizziness; frequency, unspecified - convulsions.

Disorders from the psyche: rarely - emotional lability (in children).

Disorders from the gastrointestinal tract: often - nausea, vomiting, dry mouth.

Heart Disease: infrequently transient tachyarrhythmia.

Disorders from the side of the organ of vision: infrequently hyperemia sclera.

General disorders and disorders at the site of administration: often - "hot flashes", peripheral edema, weight gain.

Taking desmopressin without a simultaneous restriction of fluid intake can lead to fluid retention in the body and / or hyponatremia, which may be asymptomatic or accompanied by headache, nausea, vomiting, weight gain, peripheral edema and, in severe cases, seizures.

When used simultaneously with imipramine or oxybutynin, hyponatremic convulsions are possible.

Overdose:

Overdose leads to an increase in the duration of action of desmopressin and an increased risk of fluid retention and hyponatremia.

Treatment hyponatremia should be individual, it is mandatory to stop taking the drug and to cancel the restriction on the intake of fluid. In the presence of overdose symptoms, infusion of an isotonic or hypertonic sodium chloride solution is possible. In case of severe fluid retention (seizures and loss of consciousness), therapy should be added furosemide.

In case of overdose, see a doctor.

Interaction:

With simultaneous application indomethacin may enhance, but not increase, the duration of desmopressin.

Tetracycline, lithium preparations, norepinephrine weaken the antidiuretic effect of desmopressin.

Simultaneous administration of non-steroidal anti-inflammatory drugs (NSAIDs) may increase the risk of side effects.

Desmopressin enhances the action of hypertensive drugs.

Tricyclic antidepressants, selective inhibitors of serotonin, chlorpromazine and carbamazepine, narcotic analgesics, lamotrigine capable of causing a syndrome of inadequate secretion of antidiuretic hormone, can enhance the antidiuretic effect of the drug and lead to an increased risk of fluid retention and hyponatremia.

When using desmopressin with loperamide, a threefold increase in desmopressin concentration in plasma is possible, which significantly increases the risk of fluid retention and the occurrence of hyponatremia. Perhaps other drugs that slow intestinal motility can cause a similar effect.

The combination of desmopressin with dimethicone may lead to a decrease in desmopressin absorption.

Special instructions:

It is necessary to control the treatment of children and patients at risk of increased intracranial pressure.

To avoid the development of side effects, it is mandatory to limit to a minimum the intake of fluid 1 hour before admission and within 8 hours after taking the drug in patients with a primary night enuresis. Non-compliance with this rule leads to the development of side effects.

The most common hyponatremia occurs in elderly patients (65 years and older) due to a high risk of side effects (including fluid retention, hyponatremia).High risk of side effects is in elderly patients with initially low concentration of sodium in blood plasma and polyuria from 2.8 to 3.0 liters. If the decision to treat desmopressin is taken, it is necessary to determine the concentration of sodium in the blood plasma and monitor the patient's condition before the appointment, 3 days after the start of the dose and at each dose increase.

Desmopressin should not be used in cases where there are other additional causes for fluid retention and electrolyte disorders.

Prevention of hyponatremia is to increase the frequency of determining the concentration of sodium in the blood plasma, especially in cases of simultaneous reception with drugs that cause the syndrome of inadequate secretion of antidiuretic hormone (tricyclic antidepressants, selective inhibitors of serotonin, chlorpromazine and carbamazepine) and non-steroidal anti-inflammatory drugs.

When there is acute urinary incontinence, dysuria and / or nocturia, urinary tract infections, with a suspected bladder tumor or prostate,in the presence of polydipsia and decompensated diabetes mellitus, the diagnosis and treatment of these conditions and diseases should be performed before the start of desmopressin treatment.

When developing against the background of treatment of systemic infections, fever, gastroenteritis, the drug should be stopped.

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

Data on the possible effect of desmopressin on the ability to control vehicles and mechanisms are not available. However, during the treatment period, headache and dizziness may occur, so care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, 0.1 mg and 0.2 mg.

Packaging:

For 10, 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 10, 20, 30, 40, 50 or 100 tablets in cans of polyethylene terephthalate.

One jar or 1, 2, 3, 4, 5, 6, 8 or 10 contour squares, together with the instructions for use, are placed in a cardboard package (bundle).

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° 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:LP-002764

Date of registration:17.12.2014

Expiration Date:17.12.2019

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Representation: & nbspOZONE LLC OZONE LLC Russia

Information update date: & nbsp25.03.2017

Illustrated instructions

Instructions

Desmopressin (Desmopressin)