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Description pharmaceutical form:
Tablet 0.1 or 0 2 mg: white, round, flat, scored on one side.
Suction. Ingestion Cmax in plasma is reached within h of 0.9 Vd is 0.2–0.3 l/kg. Simultaneous eating can reduce the extent of absorption from the gastrointestinal tract by 40%.
Distribution. Absorption by ingestion is 5%. Desmopressin does not cross the BBB.
Excretion. Excreted by the kidneys. T1/2 the ingestion of 1.5–2.5 h.
Description pharmacological action:
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 molecule vasopressin — deamination of L-cysteine and substitution of 8-L-arginine-8-D-arginine.
Desmopressin increases the permeability of the epithelium of the distal convoluted tubules of the nephron for water and increases its reabsorbqiyu. Structural changes combined with significantly enhanced antidiuretic ability to lead to a less pronounced effect of desmopressin on the smooth muscles of blood vessels and internal organs compared with vasopressin, hence the lack of spastic unwanted side effects. In contrast to vasopressin longer-acting and does not cause increased blood pressure.
The use of desmopressin in diabetes insipidus of Central origin leads to a decrease in urine output, simultaneous increase osmolarity and decrease in urine osmolarity of blood plasma. This leads to a reduction in the frequency of urination and nocturia reduction.
The maximum antidiuretic effect when administered occurs within 4-7 h. Antidiuretic effect when administered at a dose of 0.1–0.2 mg up to 8 h at a dose of 0.4 mg — up to 12 hours.
With caution: elderly patients (over 65 years) due to the high risk of side effects (fluid retention, hyponatremia). In appointing the drug therapy of the individual 3 days after you start taking and each time you increase the dose, you should determine the concentration of sodium in the blood plasma and to monitor the patient’s condition.
Caution: renal failure, fibrosis of the bladder, disorders of water and electrolyte balance, potential risks of increasing intracranial pressure, pregnancy.
Application of pregnancy and breast-feeding:
According to the known data, the use of desmopressin in pregnant women with diabetes insipidus has not been noted side effects on pregnancy, the health of the pregnant woman, fetus and newborn.
However, it is necessary to relate the expected benefit to the mother and the potential risk to the fetus.
Studies have shown that the amount of desmopressin that enter the body of a newborn in breast milk of women receiving higher doses of desmopressin significantly less than that which could affect diuresis.
The most frequently side effects are observed in cases where the treatment is performed without fluid restriction — fluid retention and/or hyponatremia, which can be asymptomatic or manifest the following symptoms.
CNS and peripheral nervous system: headache, dizziness, in severe cases, convulsions.
From the digestive system: nausea, vomiting, dry mouth.
Other: peripheral edema, weight gain, transient tachyarrhythmia, redness of the eyes.
It is known that while the use of desmopressin with oxybutynin or imipramine gipokaliemicakie possible seizures.
If any of the following in the description of the side effects worsen or the patient noticed any other side effects not mentioned in the description, you should inform the doctor.
While the use of desmopressin increases the effect of hypertensive agents.
While the use of buformin, tetracycline, drugs lithium, norepinephrine weaken the antidiuretic effect of desmopressin.
While the use of desmopressin, NSAIDs may increase the risk of side effects.
While the use of indomethacin enhances but does not increase the duration of action of desmopressin.
With simultaneous use of tricyclic antidepressants, SSRIs, and narcotic analgesics, NSAIDs, lamotrigine, chlorpromazine and carbamazepine, can cause the syndrome of inappropriate secretion of antidiuretic hormone may potentiate antidiuretic effect of desmopressin and increase the risk of fluid retention and hyponatremia.
When using desmopressin with loperamide may three-fold increase in the concentration of desmopressin in plasma, which significantly increases the risk of fluid retention and the occurrence of hyponatremia. There may be other drugs that slow down peristalsis, can cause a similar effect.
While the use of desmopressin with Dimethicone may decrease the absorption of desmopressin.
Method of application and dose:
Inside. The optimal dose picked individually.
The medicine should be taken shortly after a meal, since a meal may affect the absorption of the drug and its effectiveness.
Diabetes insipidus of Central Genesis: the recommended starting dose for children over 4 and adults is 0.1 mg 1-3 times per day. Subsequently the dose is adjusted depending on the response to treatment. Typically, 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 per day.
Primary nocturnal enuresis: the recommended initial dose for children over 5 and adults is 0.2 mg at 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 taken based on clinical data, which will occur after drug withdrawal for 1 week. Necessary to monitor compliance with fluid restriction in the evening.
Nocturia in adults: the recommended initial dose is 0.1 mg at night. If no effect within 7 days, dose increased to 0.2 mg and subsequently 0.4 mg (frequency of increasing the dose is not more than 1 times a week). You should be aware of the dangers of fluid retention in the body. If after 4 weeks of treatment and dose adjustment adequate clinical effect is not observed, continue the use of the drug is not recommended.
Symptoms: increase duration of action of desmopressin and increase the risk of fluid retention (headache, nausea, vomiting, peripheral edema, convulsions), and hyponatremia, where the concentration of sodium ions in blood plasma below 135 mmol/L.
Treatment: you should consult a doctor. When hyponatremia is the discontinuation of the drug, the abolition of restrictions on fluid intake, it is possible to conduct infusion or 0.9% hypertonic solution of sodium chloride. If severe fluid retention (convulsions and loss of consciousness) — to the above treatment should be added furosemide.
Hyponatremia occurs most frequently in patients of advanced age (over 65 years). The necessary control in the treatment of children, adolescents, patients with risk of increased intracranial pressure. To avoid the development of side effects should be mandatory to limit to a minimum fluid intake for 1 hour before application and for 8 h after administration of the drug in patients with primary nocturnal enuresis.
The native drug should not be used when there are other additional reasons for fluid retention and electrolyte disorders. High risk of adverse effects are elderly patients with initially low concentration of sodium in the blood plasma and polyuria from 2.8 to 3 liters.
To prevent the development of hyponatremia is to increase the frequency of determination of sodium in blood plasma, especially with simultaneous use with drugs that cause the syndrome of inappropriate secretion of antidiuretic hormone (tricyclic antidepressants, SSRI, narcotic analgesics, lamotrigine, chlorpromazine and carbamazepine) and NSAIDs. In the event of acute urinary incontinence, dysuria and/or nocturia, urinary tract infections, suspected bladder cancer or prostate cancer, the presence of polydipsia and decompensated diabetes mellitus diagnosis and treatment of these conditions and diseases should be carried out before the start of treatment of the individual.
With the development in the treatment of systemic infections, fever, gastroenteritis, the drug should be discontinued.
The potential impact on the ability to drive or to perform work requiring high speed physical and mental reactions. Currently, data about the possible impact of the drug on the individual’s ability to drive 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, require high concentration and psychomotor speed reactions. We recommend caution when driving or operating machinery.