Desmopressin is a structural analog of arginine vasopressin, human pituitary hormone. The difference is the substitution of cysteine and deamination of L-arginine, D-arginine. This leads to a significant prolongation of period and complete lack vasoconstrictor effect. Desmopressin increases the permeability of epithelia of distal convoluted tubules and increases the reabsorption of water, which leads to a reduction in urine output, increased urine osmolarity while reducing plasma osmolarity, decrease in urinary frequency and reducing nocturia (nocturia). PharmacokineticsBioavailability of desmopressin in a sublingual form in doses of 200, 400 and 800 micrograms is about 0.25%. The maximum concentration (C max ) of desmopressin plasma levels achieved for 0.5-2 hours after drug administration and directly proportional to the applied dose: after receiving the 200, 400 and 800 ug C max was 14, 30 and 65 pg / ml, respectively. Desmopressin not penetrate the blood-brain barrier. Desmopressin is excreted by the kidneys, the half-life is 2.8 hours.
Indications for use:
- Central diabetes insipidus;
- Primary nocturnal enuresis in children older than 6 years old;
- Nocturia (nocturnal polyuria) as symptomatic therapy.
- Hypersensitivity to desmopressin or other ingredients;
- Habitual or psychogenic polydipsia (with a volume of urine formation 40 ml / kg / 24 hours);
- Heart failure and other conditions requiring the appointment of diuretic drugs;
- Renal insufficiency moderate and severe (creatinine clearance below 50 ml / min);
- Children under 6 years of age;
- Syndrome of inappropriate antidiuretic hormone products. If you have one of these diseases, before taking this medication, you should consult with your doctor.Precautions: . Renal insufficiency (creatinine clearance greater than 50 mL / min), fibrosis of the bladder, disorders of water and electrolyte balance, the potential risk of increased intracranial pressure, pregnancy, advanced age (65 years and older) Pregnancy and lactation There were no side effects on during pregnancy, the health of the pregnant woman, the fetus and the newborn when receiving sustanon 350 . However, caution should be exercised when administering the pregnant. The dose, which desmopressin may enter the body of the newborn with breast milk of women receiving the higher dose (approx. 300 mg) desmopressin is not able to influence the child’s urine output. The decision to continue breastfeeding is accepted, if the benefit to the mother outweighs the potential risk to the child. Sustanon 350 must be taken some time after the meal, as the food intake reduces the absorption of the drug and its effectiveness. Central diabetes insipidus: The recommended starting dose Minirin ® 60 mg 3 times a day. Subsequently the dose varies depending on the therapeutic effect. The recommended daily dose is in the range 120-720 mg. The optimal maintenance dose is 60-120 mg 3 times per day sublingually. The primary nocturnal enuresis: The recommended starting dose of 120 mg at night. In the absence of the effect of the dose can be increased to 240 mg. During treatment it is necessary to restrict fluid intake in the evening. Recommended continuous course of treatment is 3 months. The decision to continue treatment is made based on clinical data sustanon 350, which will be observed after discontinuation of the drug for 1 week. Nocturia: The recommended starting dose is 60 mg sublingually for the night. If no effect in 1 week dose increased to 120 mg sublingual and subsequently to 240 g by increasing the dose with a frequency of less than one time per week. If after 4 weeks of treatment and dose adjustment adequate clinical response is observed, it is not recommended to continue taking the drug .
The most common side effects observed in cases where treatment is not limited fluid intake, and there are fluid retention and / or hyponatremia, which can be asymptomatic or manifested by the following symptoms: headache, dizziness, nausea, vomiting, dry mouth, peripheral edema, body weight, in severe cases -. cramp If any of these instructions side effects are compounded, or if you notice any other side effects not mentioned in the instructions, inform your doctor.
Overdosing increases the duration of action of the drug and increase the risk of fluid retention and hyponatremia. In case of overdose, seek medical advice. Treatment of hyponatremia should be individualized, it is obligatory to discontinuation of the drug and the abolition of restrictions on fluid intake. If you have symptoms of overdose possible infusion of isotonic or hypertonic sodium chloride solution. In the case of severe fluid retention (convulsions and unconsciousness) treatment should be added to furosemide.
Interaction with other drugs:
Tricyclic antidepressants, selective serotonin reuptake inhibitors, chlorpromazine and carbamazepine, may cause a syndrome of inappropriate secretion of antidiuretic hormone, may increase the antidiuretic effect and increase fluid retention risk and hyponatremia. Simultaneous use of nonsteroidal anti-inflammatory agents also increases the risk of side effects. The combination with loperamide It can lead to a threefold increase in plasma concentration of desmopressin and increase the risk of side effects (fluid retention, hyponatremia). It is likely that other drugs that lower the tone and motility of the smooth muscles of the intestine, may have a similar effect. When concomitant administration sustanon 350 with the above drugs for the prevention of hyponatremia need regular determination of sodium concentration in the blood plasma.
It is mandatory to minimize the restriction for the reception of fluid 1 hour before receiving and for 8 hours after drug administration in patients with primary nocturnal enuresis. Failure to do so can lead to side effects. A high risk of side effects, patients are older than 65 years with initially low concentration of sodium in the blood plasma and polyuria 2.8-3.0 liters per day. In the case of occurrence of acute urinary incontinence, dysuria and / or nocturia, urinary tract infection sustanol 300, in cases of suspected tumor of the bladder or prostate, in the presence of polydipsia and decompensated diabetes, it is necessary to make a diagnosis and treatment of these conditions and diseases prior to treatment . when acute arisen related diseases, such as systemic infections, fever, gastroenteritis, accompanied by an imbalance of fluids and electrolytes, the drug should be discontinued. with the utmost care prescribers elderly patients (65 years and older) in connection with a high risk of side effects (water retention and hyponatremia). When assigning in these cases it is necessary to determine plasma sodium concentration prior to drug administration, 3 days after the beginning of the reception and for each dose is increased. It is necessary to monitor the patient’s condition during the period of receiving.