Drug information of Desmopressin

Mechanism of effect

Desmopressin emulates the actions of endogenous human ADH (refer to Pharmacology section above). Desmpressin is a structural analogue of ADH modified by deamination of 1-cysteine and substitution of 8-L-arginine by 8-D-arginine. Compared to natural ADH, desmopressin elicits a great antidiuretic response on weight basis.

Pharmacodynamic

Desmopressin is a synthetic analogue of the natural antidiuretic hormone (ADH or vasopressin) that is produced by the hypothalamus and stored in the posterior pituitary gland. The main function of ADH is to regulate extracellular fluid volume in the body.

ADH secretion is stimulated by angiotensin II, linking it to the renin-angiotensin-aldosterone system (RAAS). ADH stimulates water reabsorption in the kidneys by causing the insertion of aquaporin-2 channels on the apical surface of cells of the DCT and collecting tubules.

 It also causes vasoconstriction through its action on vascular smooth muscle cells of the collecting tubules. The efficacy of desmopressin for managing bleeds in patients with hemophilia A or von Willebrand’s disease Type I arises from its ability to elicit dose-dependent increases in plasma factor VIII (antihemophilic factor), plasminogen activator, and to a lesser extent, factor VIII-related antigen and ristocetin cofactor activities; these changes improve blood clotting.

Pharmacokinetics

Absorption

Bioavailability: 3.5% (nasal); 5% (oral; compared to intranasal, 0.16% compared to IV)

Onset: ADH effect (intranasal), 60 min; hemophilia and von Willebrand disease (IV), 30 min

Duration: 6-14 hr (intranasal, IV infusion, oral)

Peak plasma time: 1-5 hr (intranasal); 0.25 hr for 0.83 mcg dose and 0.75 hr for 1.66 mcg dose (preservative-free nasal spray)

Metabolism

Unknown

Elimination

Half-life: 3.5 hr (intranasal); 3 hr (IV); 2-3 hr (PO); 2.8 hr (1.66 mcg dose; preservative-free nasal spray)

Excretion: Urine

Dosage

Adults

Diabetes Insipidus

Intranasal (DDAVP)

• 10-40 mcg/day qDay or divided q8-12hr
• Adjust morning and evening doses separately for appropriate diurnal rhythm of water turnover

PO

• Initial: 0.05 mg q12hr
• Effective range: 0.1-1.2 mg divided q8-12hr
• Observe fluid restriction
• If switching to PO from intranasal, start PO at least 12 hours after last intranasal dose

IV/SC

• 2-4 mcg/day divided q12hr or one-tenth the maintenance of intranasal dose 

Hemophilia A & Von Willebrand Disease

Hemophilia with factor VIII levels greater than 5%; von Willebrand disease (type I)

0.3 mcg/kg IV over 15-30 minutes IV (for pre-op, 30 min before procedure) 

(Intranasal (Stimate

• <50 kg: 150 mcg; for pre-op, give 2 hr before procedure
• >50 kg: 300 mcg; for pre-op, give 2 hr before procedure 

Nocturnal Enuresis

Oral: 0.2 to 0.6 mg once before bedtime. 

Intranasal:

• Patients not at increased risk for hyponatremia: 1 spray of 1.66 mcg in either nostril nightly ~ 30 min before going to bed
• Patients at risk for hyponatremia: 0.83 mcg in either nostril nightly ~ 30 min before going to bed; 0.83 mcg dose may have a lower risk of hyponatremia; may be increased to 1 spray of 1.66 mcg after at least 7 days

Uremic Bleeding in Acute or Chronic Renal Failure

0.4 mcg/kg IV over 10 minutes

Pediatrics

Diabetes Insipidus

3 months to 12 years (intranasal)

• 5-30 mcg/day qDay or divided q12hr (using 100 mcg/mL solution)

>12 years (intranasal)

• 10-40 mcg/day qDay/divided q12hr intranasal (using 100 mcg/mL solution)

3 months to 12 years (oral)

• Initial: 0.05 mg PO q12hr
• Effective range: 0.1-1.2 mg
• If switching to PO from intranasal, start PO at least 12 hours after last intranasal dose

>12 years (oral)

• Initial: 0.05 mg PO q12hr
• Effective range: 0.1-1.2 mg divided q8-12hr
• Observe fluid restriction
• If switching to PO from intranasal, start PO at least 12 hours after last intranasal dose

IV or SC administration

3 months to 12 years (IV/SC)

• 0.1-1 mcg qDay or divided q12hr
• Initiate at low dose and increase as necessary
• Monitor serum sodium levels and urine output

>12 years (IV/SC)

• 2-4 mcg/day divided q12hr or one tenth the maintenance of intranasal dose

Nocturnal Enuresis

>6 years: 0.2 mg PO qHS (up to 0.6 mg/day)

Hemophilia A & Von Willebrand Disease

0.3 mcg/kg IV over 15-30 minutes; for preop, 30 minutes before procedure 

1 spray (150 mcg) per nostril (300 mcg total dose) if >12 year of age or >50 kg body weight; administer a single spray (150 mcg) if patient > 12 years of age but < 50 kg body weight

Drug contraindications

Thirst , Congestive heart failure , Hypersensitivity to this drug , Uncontrolled hypertension

Side effects

Headache , nausea , vertigo , gastrointestinal disturbances , tiredness , Abdominal pain , Back pain , rhinitis

Interactions

Aripiprazole , Esomeprazole , Acetaminophen , Sertraline , Cetirizine , Fluoxetine , Quetiapine , Dextroamphetamine , lisdexamfetamine , Lamotrigine , Levothyroxine , Montelukast , Clonazepam , escitalopram , Aspirin , prednisone , Budesonide , fenoprofen , Flunisolide , Ciclesonide , Opium

Alerts

(Intranasal preservative-free (Noctiva

• Can cause hyponatremia, which may be life-threatening if severe .Very low sodium levels can be life-threatening, leading to seizures, passing out, trouble breathing, or death.
• Contraindicated in patients at increased risk of severe hyponatremia, such as patients with excessive fluid intake, illnesses that can cause fluid or electrolyte imbalances, and in those using loop diuretics or systemic or inhaled glucocorticoids
• Ensure serum sodium is normal before starting or resuming therapy; measure serum sodium within 7 days and approximately 1 month after initiating therapy or increasing dose, and periodically during treatment; monitor serum sodium frequently in patients >65 years and patients at increased risk of hyponatremia
• If hyponatremia occurs, therapy may need to be temporarily or permanently discontinued
• Tell your doctor BEFORE you take Desmopressin If you have heart failure (weak heart) or you have high blood pressure.
• Use with care in children. Talk with the doctor.

Points of recommendation

• Take with or without food.
• Take at bedtime for bedwetting.

• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• Talk with your doctor if you have an infection, a fever, loose stools (diarrhea), or are throwing up. Talk with your doctor if you will be out in very hot weather, will be active, or will be changing how much water you drink for any reason.

Pregnancy level

B

Related drugs

Felypressin , Vasopressin

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