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Desmopressin

Nativa
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2019-09-19
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$69.94
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Clinical Pharmacology

Desmopressin is a structural analogue of the natural hormone arginine-vasopressin, with a pronounced antidiuretic effect. Desmopressin is obtained as a result of changes in the structure of the vasopressin molecule - deamination of L-cysteine ​​and replacement of 8-L-arginine with 8-D-arginine. Desmopressin increases the permeability of the epithelium of the distal parts of the convoluted nephron tubules to water and increases its reabsorption. Structural changes in combination with significantly enhanced antidiuretic ability lead to a less pronounced effect of desmopressin on the smooth muscles of the vessels and internal organs compared to vasopressin, which leads to the absence of unwanted spastic side effects. Unlike vasopressin, it acts longer and does not cause an increase in blood pressure. The use of desmopressin in non-diabetes mellitus of central genesis leads to a decrease in the volume of urine secreted and a simultaneous increase in the osmolarity of urine and a decrease in the osmolarity of blood plasma. This leads to a decrease in the frequency of urination and a decrease in nighttime polyuria.

The maximum antidiuretic effect when taken orally comes in 4-7 hours. The antidiuretic effect when taken orally at a dose of 0.1-0.2 mg - up to 8 hours, at a dose of 0.4 mg - up to 12 hours.

Indications

  • diabetes insipidus of central origin;
  • primary nocturnal enuresis in children over 5 years old;
  • nocturnal polyuria in adults (as a symptomatic therapy).

Composition

active substance: desmopressin acetate 100 μg;

Excipients: lactose monohydrate - 10 mg, crospovidone XL - 5 mg, magnesium stearate - 2 mg, ludipress - up to 200 mg (lactose monohydrate - 170.1 mg, crospovidone - 6.4 mg, povidone - 6.4 mg).

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Desmopressin

Dosage and Administration

Inside The optimal dose of the drug is selected individually. The drug should be taken some time after a meal, as a meal can affect the absorption of the drug and its effectiveness.

Central diabetes insipidus: the recommended initial dose for children over 4 years of age and adults is 0.1 mg 1-3 times / day. In the subsequent dose is selected depending on the response to treatment. Usually the daily dose is from 0.2 to 1.2 mg. For most patients, the optimal maintenance dose is 0.1-0.2 mg 1-3 times / day.

Primary nocturnal enuresis: The recommended initial dose for children over 5 years of age and adults is 0.2 mg per night. In the absence of effect, the dose may be increased to 0.4 mg. The recommended course of continuous treatment is 3 months. The decision to continue treatment should be made on the basis of clinical data that will be observed after discontinuation of the drug within 1 week. It is necessary to control compliance with the restriction of fluid intake in the evening.

Nighttime polyuria in adults: the recommended starting dose is 0.1 mg at night. If there is no effect for 7 days, the dose is increased to 0.2 mg and subsequently to 0.4 mg with an increase in dose with a frequency of no more than 1 time / week. It should be aware of the danger of fluid retention in the body. If after 4 weeks of treatment and dose adjustment of an adequate clinical effect is not observed, it is not recommended to continue using the drug.

Adverse reactions

The most common side effects are observed in cases where the treatment is carried out without limiting fluid intake - there are fluid retention and / or hyponatremia, which may be asymptomatic or manifest the following symptoms.

From the side of the central nervous system and peripheral nervous system: headache, dizziness; in severe cases - seizures.

On the part of the digestive system: nausea, vomiting, dry mouth.

Other: peripheral edema, weight gain, transient tachyarrhythmia, eye redness. It is known that with simultaneous use of desmopressin with oxybutinin or imipramine, hyponatremia convulsions are possible.

With care: renal failure, fibrosis of the bladder, disruption of water and electrolyte balance, the potential risk of increased intracranial pressure, pregnancy. With extreme caution, use the drug in elderly patients (over 65 years) due to the high risk of side effects (fluid retention, hyponatremia). When prescribing therapy with Nativ after 3 days from the start of the intake and with each dose increase, determine the concentration of sodium in the blood plasma and monitor the patient's condition.

Drug interactions

With the simultaneous use of desmopressin enhances the effects of hypertensive agents. With the simultaneous use of buformin, tetracycline, lithium preparations, norepinephrine weaken the antidiuretic effect of desmopressin. With the simultaneous use of desmopressin with NSAIDs may increase the risk of side effects. With simultaneous use of indomethacin increases, but does not increase the duration of the action of desmopressin. With the simultaneous use of tricyclic antidepressants, selective serotonin reuptake inhibitors, narcotic analgesics, NSAIDs, lamotrigine, chlorpromazine and carbamazepine, which can cause the syndrome of inappropriate secretion of antidiuretic hormone, can enhance the antidiuretic effect of desmopressin and lead to an increased risk of fluid retention, and increase the risk of holding fluid. When using desmopressin with loperamide, a threefold increase in the concentration of desmopressin in plasma is possible, which significantly increases the risk of fluid retention and the occurrence of hyponatremia. Perhaps other drugs that slow down peristalsis can cause a similar effect.With simultaneous use of desmopressin with dimethicone, it is possible to decrease the absorption of desmopressin.

Pregnancy and Lactation

According to known data, when using desmopressin in pregnant women with diabetes insipidus, there were no adverse effects on the course of pregnancy, on the state of health of the pregnant woman, fetus and newborn. However, the expected benefit to the mother and the potential risk to the fetus should be correlated.

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

Special instructions

Most often, hyponatremia occurs in elderly patients (over 65 years).

Control is needed in the treatment of children, adolescents, patients at risk of increasing intracranial pressure. In order to avoid the development of side effects, it is imperative to limit the intake of fluid to a minimum 1 hour before use and within 8 hours after taking the drug in patients with primary nocturnal enuresis.

Nativ should not be used when there are other additional causes for fluid retention and electrolyte disorders. Elderly patients with initially low plasma sodium concentration and polyuria from 2.8 to 3 liters have a high risk of side effects.

Prevention of the development of hyponatremia is to increase the frequency of determining sodium in the blood plasma, especially when used with drugs that cause the syndrome of inadequate secretion of antidiuretic hormone (tricyclic antidepressants, selective serotonin reuptake inhibitors, narcotic analgesics, lamotrigine, chlorpromazine and carbamosphicimesiproxiprophroximetamine. In the event of acute urinary incontinence, dysuria and / or nocturia, urinary tract infection, suspected bladder or prostate tumor, polydipsia and decompensated diabetes mellitus, diagnosis and treatment of these conditions and diseases should be carried out before starting treatment with Nativ.

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

Influence on ability to drive motor transport and control mechanisms

Currently, data on the possible effect of Nativ on the ability to drive a car and control mechanisms is missing. However, the use of the drug can lead to the development of such side effects as dizziness, headache, which can adversely affect the ability to drive and perform potentially hazardous activities that require increased concentration of attention and psychomotor reactions. It is recommended to be careful when driving a car or working with machinery.

Overdosage

Symptoms: an increase in the duration of the action of desmopressin and an increased risk of fluid retention (headache, nausea, vomiting, peripheral edema, convulsions), hyponatremia, in which the concentration of sodium ions in the blood plasma is below 135 mmol / l.

Treatment: in case of hyponatremia - cessation of the use of the drug, lifting the restriction on fluid intake, it is possible to conduct an infusion of 0.9% or hypertonic sodium chloride solution. In case of severe fluid retention (convulsions and loss of consciousness), furosemide should be added to the above therapy.

  • Brand name: Desloratadine
  • Active ingredient: Desloratadine
  • Dosage form: pills, film coated white or almost white, round, biconvex; the cross section is almost white or white with a creamy or white with a pinkish tinge.
  • Manufacturer: Canonpharma
  • Country of Origin: Russia

Studies and clinical trials of Desmopressin (Click to expand)

  1. Antidiuretic effect of desmopressin given in hemostatic dosages to healthy volunteers
  2. Synthesis of Conformationally Restricted Mimetics of γ-Turns and Incorporation into Desmopressin, an Analogue of the Peptide Hormone Vasopressin
  3. Acquired von Willebrand disease—hemostatic management of major orthopedic surgery with high-dose immunoglobulin, desmopressin, and continuous factor concentrate infusion
  4. Retrospective review of the management of elective surgery with desmopressin and clotting factor concentrates in patients with von Willebrand disease
  5. The use of desmopressin as a hemostatic agent: A concise review
  6. Clinical efficacy of desmopressin acetate for hemostatic control in patients with primary platelet disorders undergoing surgery
  7. Thrombosis following desmopressin for uremic bleeding
  8. Subcutaneous desmopressin (DDAVP) shortens the bleeding time in uremia
  9. Severe hyponatremia after repeated intravenous administration of desmopressin
  10. Abnormal proteolytic degradation of von willebrand factor after desmopressin infusion in a new subtype of von willebrand disease (ID)
  11. Plasmin generation and fibrin(ogen)olysis following desmopressin infusion
  12. Desmopressin (d-DAVP) effects on platelet rheology and von willebrand factor activities in uremia
  13. Effectiveness of high-dose intravenous immunoglobulin in a case of acquired von willebrand syndrome with chronic melena not responsive to desmopressin and factor VIII concentrate
  14. Desmopressin-induced thrombocytopenia in type i platelet discordant von willebrand disease
  15. von Willebrand's disease: Use of collagen binding assay provides potential improvement to laboratory monitoring of desmopressin (DDAVP) therapy
  16. Investigation of mechanism of desmopressin binding in vasopressin V2 receptor versus vasopressin V1a and oxytocin receptors: Molecular dynamics simulation of the agonist-bound state in the membrane–aqueous system
  17. DDAVP (Desmopressin) and solid phase peptide synthesis
  18. Use of desmopressin to prevent bleeding complications in patients treated with aspirin
  19. ChemInform Abstract: Stereoselective Synthesis of Ψ[CH2O] Pseudodipeptides and Conformational Analysis of a PheΨ[CH2O]Ala Containing Analogue of the Drug Desmopressin.
  20. Randomized controlled trial of desmopressin plus terlipressin vs. terlipressin alone for the treatment of acute variceal hemorrhage in cirrhotic patients: A multicenter, double-blind study
  21. Intranasal administration of peptides: Nasal deposition, biological response, and absorption of desmopressin
  22. Effects of concentration and volume on nasal bioavailability and biological response to desmopressin
  23. Effect of viscosity on particle size, deposition, and clearance of nasal delivery systems containing desmopressin
  24. Different properties of the paracellular pathway account for the regional small intestinal permeability to the peptide desmopressin

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