Nocpres Tablet

Desmopressin is a synthetic analogue of arginine vasopressin (antidiuretic hormone, ADH) with enhanced antidiuretic activity, greater selectivity for V2 receptors, and a longer duration of action than endogenous ADH. It helps reduce urine production by increasing water reabsorption in the kidneys.

Desmopressin is used to treat central diabetes insipidus, primary nocturnal enuresis (bedwetting), and nocturia due to nocturnal polyuria. It is also used to manage mild hemophilia A and von Willebrand disease during minor surgical procedures by increasing plasma levels of clotting factors. Most formulations contain desmopressin acetate as the active ingredient.

Desmopressin is a synthetic analog of vasopressin used to reduce renal excretion of water in central diabetes insipidus and nocturia.

• Indicated for the treatment of nocturia due to nocturnal polyuria in adults who awaken at least 2 times per night to void (intranasal).

• Indicated as antidiuretic replacement therapy in the management of central cranial diabetes insipidus and for management of the temporary polyuria and polydipsia following head trauma or surgery in the pituitary region (intranasal/parenteral).

• Indicated for patients with hemophilia A with factor VIII coagulant activity levels greater than 5% or mild to moderate classic von Willebrand's Disease (Type I) with factor VIII levels greater than 5% during surgical procedures and postoperatively to maintain hemostasis (parenteral).

• Bleeding
• Central Diabetes Insipidus
• Nocturia
• Nocturnal Polyuria
• Polydipsia
• Polyuria
• Primary Nocturnal Enuresis

By mimicking the actions of endogenous ADH, desmopressin acts as a selective agonist of V2 receptors expressed in the renal collecting duct (CD) to increase water re-absorption and reduce urine production. Desmopressin has been shown to be more potent than ADH in increasing plasma levels of factor VIII activity in patients with hemophilia and von Willebrand's disease Type I . Desmopressin demonstrates markedly diminished pressor activity. Desmopressin administered intranasally has an antidiuretic effect about one-tenth that of an equivalent dose administered by injection .

Upon binding of desmopressin to V2 receptors in the basolateral membrane of the cells of the distal tubule and collecting ducts of the nephron, adenylyl cyclase is stimulated. The resulting intracellular cascades in the collecting duct lead to increased rate of insertion of water channels, called aquaporins, into the lumenal membrane and enhanced the permeability of the membrane to water .

Following nasal spray administration of 0.83 mcg and 1.66 mcg, median time to peak plasma concentrations (Tmax) was 0.25 and 0.75 hour, respectively . The peak plasma concentration was approximately 4.00 (± 3.85) pg/mL and 9.11 (± 6.90) pg/mL, respectively . The bioavailability of 1.5 mg/mL desmopressin administered by the intranasal route was between 3.3 and 4.1% .

The absolute bioavailability of orally administered desmopressin varies between 0.08% and 0.16% where the mean maximum plasma concentration is reached within 2 hours .

The distribution volume of orally administered desmopressin is 0.2 – 0.32 l/kg . It is not reported to cross the blood-brain barrier.

Following radioiodination (125I) in the N-terminal, the fraction of plasma protein binding of desmopressin was reported to be 17.3 ± 1.5% in a pharmacokinetic study involving healthy subjects .

Desmopressin is mainly excreted in the urine. About 65% of the amount of desmopressin absorbed after oral administration could be recovered in the urine within 24 hours .

Following an intranasal dose of 1.66 mcg of desmopressin, the median apparent terminal half-life was 2.8 hours . Terminal half-life significantly increased from 3 hours in normal healthy patients to 9 hours in patients with severe renal impairment . The oral terminal half life of desmopressin ranges from 2 to 3.11 hours .

Intravenous TDLo in humans is reported to be 0.3 µg/kg/10M . Desmopressin is associated with hyponatremia in case of overdose, which may require temporary or permanent discontinuation of the therapy depending on severity. The effects of hyponatremia include seizure, altered mental status (confusion, drowsiness or continuing headache), cardiac arrhythmias and worsening edema. Other signs of overdose may include oliguria and rapid weight gain due to fluid retention . In case of overdose, reduce the dose or frequency of drug administration, or discontinue use if appropriate. Assessment of serum sodium and initiation of appropriate medical treatment is recommended.

No interactions found.

• Treatment of diabetes insipidus: Dosage is individual in diabetes insipidus but the total daily sublingual dose normally lies in the range of 120 micrograms to 720 micrograms. A suitable starting dose in adults and children is 60 micrograms three times daily, administered sublingually. This dosage regimen should then be adjusted in accordance with the patient's response. For the majority of patients, the maintenance dose is 60 micrograms to 120 micrograms sublingually three times daily.
• Post-hypophysectomy polyuria/polydipsia: The dose of Nocpres Tablet 0.1 mg Melt should be controlled by measurement of urine osmolality.

• Adults and Children: It is recommended that patients be started on doses of 0.05 mg (1/2 of the 0.1 mg tablet) two times a day and individually adjusted to their optimum therapeutic dose. Most patients in clinical trials found that the optimal dosage range is 0.1 mg to 0.8 mg daily, administered in divided doses. Each dose should be separately adjusted for an adequate diurnal rhythm of water turnover. Total daily dosage should be increased or decreased in the range of 0.1 mg to 1.2 mg divided into two or three daily doses as needed to obtain adequate antidiuresis.
• Geriatric Use: This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.