Brand names: DDAVP, Minirin, Stimate
Drug class: Pituitary

Medically reviewed by Drugs.com on Oct 10, 2024. Written by ASHP.

Introduction

Synthetic polypeptide analog of arginine vasopressin (antidiuretic hormone [ADH]); reduces urinary output and plasma osmolality and increases urine osmolality, as well as dose-dependent increases in plasma factor VIII (antihemophilic factor), plasminogen activator, and, to a lesser degree, factor VIII-related antigen and ristocetin cofactor activities.

Uses for Desmopressin Acetate

Diabetes Insipidus

Intranasally, orally, or parenterally for prevention or control of polydipsia, polyuria, and dehydration in diabetes insipidus caused by a deficiency of endogenous posterior pituitary ADH (neurohypophyseal diabetes insipidus).

Intranasal desmopressin considered drug of choice for chronic treatment of mild to severe neurohypophyseal diabetes insipidus, because of relatively long duration of action and relative lack of adverse effects.

Polyuria and Polydipsia

Intranasally, orally, or parenterally for management of temporary polyuria and polydipsia associated with trauma or surgery in the pituitary region.

Not effective in controlling polyuria caused by renal disease, nephrogenic diabetes insipidus, hypokalemia or hypercalcemia; variable efficacy in controlling polyuria secondary to administration of lithium.

Primary Nocturnal Enuresis

Orally for management of primary nocturnal enuresis.

Used alone or as an adjunct to behavioral therapy and/or other nondrug measures; may be effective in some cases refractory to standard therapies (e.g., imipramine, enuresis alarms).

Although some desmopressin intranasal preparations (i.e., solutions containing 0.1 mg/mL) initially received approval by FDA for treatment of primary nocturnal enuresis, this approval was withdrawn in 2007 because of the risk of serious hyponatremia that may result in seizures and death, particularly in children. (See Water Intoxication under Cautions.)

Treatment usually not indicated until a child reaches 6 years of age; condition will spontaneously remit in 15% of patients every year thereafter.

Rule out other possible etiologies (e.g., neurologic and/or spinal abnormalities, diabetes insipidus or diabetes mellitus, chronic renal failure, bacteriuria [especially in girls]) before initiation of drug therapy.

Hemophilia A

Generally indicated in patients with hemophilia A with factor VIII coagulant activity >5%; designated an orphan drug by FDA for this use.

Intranasally or parenterally for management of spontaneous or trauma-induced bleeding episodes (e.g., hemarthrosis, intramuscular hematoma, mucosal bleeding) in patients with mild hemophilia A.

Intranasally or parenterally for maintenance of hemostasis during surgical procedures and postoperatively when administered 30 minutes prior to scheduled procedure.

Not indicated for patients with hemophilia A with factor VIII coagulant activity ≤5%, hemophilia B, or patients with factor VIII antibodies. Use may be justified in patients with factor VIII coagulant activity between 2–5% in certain clinical situations; carefully monitor patient if drug is used in this situation.

Not effective in patients with severe hemophilia A.

von Willebrand Disease

Generally indicated in patients with mild to moderate classic von Willebrand disease (type 1) with factor VIII coagulant activity >5%; designated an orphan drug by FDA for this use.

Intranasally or parenterally for management of spontaneous or trauma-induced bleeding episodes (e.g., hemarthrosis, intramuscular hematoma, mucosal bleeding) in patients with mild to moderate type 1 von Willebrand disease.

Parenterally for maintenance of hemostasis during surgical procedures and postoperatively when administered 30 minutes prior to scheduled procedure in patients with mild to moderate type 1 von Willebrand disease.

Drug of choice for management of mild to moderate type 1 von Willebrand disease, especially in patients with plasma factor VIII activity >5%.

Patients with severe homozygous von Willebrand disease with factor VIII coagulant activity and factor VIII/von Willebrand antigen concentrations <1% least likely to respond; variable response in other patients depending on type of molecular defect associated with disease.

Not indicated for patients with severe type 1 von Willebrand disease or when there is evidence of an abnormal molecular form of factor VIII antigen.

May be effective for management of bleeding in some, but not all, patients with type 2A, 2M, or 2N von Willebrand disease^{† [off-label]}.

Usually not used in patients with type 2B von Willebrand disease^{† [off-label]} because of an increased risk of thromboembolic events and transient thrombocytopenia; although, has been effectively used in some patients with type 2B von Willebrand disease^{† [off-label]}.

Not effective for management of bleeding in patients with type 3 von Willebrand disease^{† [off-label]}.

Uremia

Has been used IV to increase factor VIII activity and reduce bleeding time in uremic patients^{† [off-label]} with prolonged bleeding times and hemorrhagic tendencies. Reduced bleeding time and normal hemostasis observed in some additional uremic patients who received IV drug before surgery or renal biopsy.

Diagnostic Uses

Has been used intranasally in adults and children to evaluate ability of kidneys to concentrate urine^†.

Sickle Cell Anemia

Has been used intranasally in a small number of patients with sickle cell anemia to induce hyponatremia resulting in decreased mean corpuscular hemoglobin concentrations and degree of sickling for the prevention and treatment of sickle cell crisis^†, but safety and efficacy not established.

Desmopressin Acetate Dosage and Administration

Administration

Administer intranasally, orally, or by sub-Q injection, direct IV injection, or slow IV infusion.

Repeated administration every 12–24 hours may result in a gradual diminution of the increase in plasma factor VIII activity observed with a single dose; initial response reproducible when a period of 2–3 days or 1–6 weeks elapses between IV or intranasal administration, respectively.

Intranasal Administration

Use intranasal preparations in children under adult supervision in order to monitor dose and fluid intake.

Nasal solutions containing 0.1 mg of drug per mL used for treatment of diabetes insipidus; nasal solution containing 1.5 mg of drug per mL used for treatment of hemophilia A or von Willebrand disease.

Administer nasal solutions containing 0.1 or 1.5 mg of drug per mL using the spray pump supplied by manufacturers; alternatively, nasal solutions containing 0.1 mg/mL may be administered using a calibrated nasal tube supplied by manufacturers.

Intranasal spray pump provided by manufacturers delivers 0.1 mL of solution per actuation. When administering nasal solution containing 0.1 mg/mL using the spray pump, each 0.1-mL spray delivers a dose of 10 mcg; administer the solution using a nasal tube if a dose other than a multiple of 10 mcg is required (e.g., in pediatric patients).

Nasal tube has 4 graduation markings that measure 0.05, 0.1, 0.15, or 0.2 mL and may be used to administer 5, 10, 15, or 20 mcg, respectively.

When administering nasal solution containing 1.5 mg/mL using the spray pump, each 0.1-mL spray delivers a dose of 150 mcg; use parenteral therapy if a dose other than a multiple of 150 mcg is required.

Administer a test dose of the nasal solution containing 1.5 mg/mL prior to initial use to establish appropriate patient response in coagulation profile.

Administer nasal solution intranasally according to the manufacturer’s instructions to ensure that drug is deposited high in nasal cavity and does not pass down the throat.

Generally not administered intranasally when changes in nasal mucosa (e.g., scarring, edema) may cause erratic, unreliable absorption of drug; do not use or discontinue drug until nasal problems resolve. Consider using desmopressin injection.

Do not administer intranasally when nasal congestion and blockage, nasal discharge, atrophy of nasal mucosa, or severe atrophic rhinitis is present; however, patients with nasal congestion and blockage have often responded well to intranasal therapy.

Intranasal therapy may be inappropriate when patient has impaired consciousness.

Alternative route of administration may be needed when nasal packing is present or during recovery from surgery in patients who have undergone cranial surgical procedures (e.g., transsphenoidal hypophysectomy).

IV Administration

Monitor BP and pulse during infusion.

Dilution

Hemophilia A or von Willebrand disease, IV infusion: Dilute the appropriate dose in 10 or 50 mL of 0.9% sodium chloride injection for administration in children weighing ≤10 kg or in adults and children weighing >10 kg, respectively.

Rate of Administration

Hemophilia A or von Willebrand disease, IV infusion: Slowly infuse IV over 15–30 minutes.

Dosage

Available as desmopressin acetate; dosage expressed in terms of salt.

Diabetes Insipidus or Polyuria and Polydipsia: Adjust dosage according individual requirements (e.g., diurnal pattern of response). Estimate response by both adequate duration of sleep and adequate, not excessive, water turnover. Adjust morning and evening doses separately for an adequate diurnal rhythm of water turnover.

Primary Nocturnal Enuresis: Adjust dosage according individual requirements and response.

Hemophilia A or von Willebrand Disease: Determine need for additional doses of drug or use of blood products for hemostasis based on clinical response (determined by laboratory tests) and condition of patient. Consider tendency toward tachyphylaxis (decreasing responsiveness) to drug when doses are repeated more frequently than every 48 hours.

von Willebrand Disease: Recommended (by National Hemophilia Foundation’s Medical and Scientific Advisory Council [MASAC]) that drug be administered no more frequently than once every 24 hours and used for no more than 3 consecutive days, unless such therapy is recommended by a clinician with expertise in treatment of the disease.

Pediatric Patients

Diabetes Insipidus

Neurohypophyseal

Intranasal

Children 3 months to 12 years of age: Initially, ≤5 mcg (0.05 mL of a solution containing 0.1 mg/ml).

Usual dosage range: 5–30 mcg (0.05–0.3 mL of a solution containing 0.1 mg/mL) daily given intranasally in a single evening dose or in 2 divided doses.

Use lowest effective dosage; about 25–33% of children and adults controlled with a single daily dose.

Restrict fluid intake.

Oral

Children ≥4 years of age: Initially, 0.05 mg twice daily; adjust subsequent dosage according to response.

0.1–0.8 mg daily given in divided doses is optimal dosage range for most patients.

Increase or decrease total daily dosage in the range of 0.1–1.2 mg divided into 2 or 3 daily doses as needed to obtain adequate antidiuresis.

Initiate oral therapy 12 hours after the last intranasal dose in patients who previously received intranasal therapy.

Restrict fluid intake.

IV

Children ≥12 years of age: Usually, 2–4 mcg daily by direct IV injection given in 2 divided doses.

Generally, administer one-tenth of the maintenance intranasal dosage parenterally in patients being switched from intranasal to direct IV injection therapy.

Use lowest effective dosage. During long-term use, patients rarely may develop tolerance to drug and require cautious increase in dosage to achieve an adequate therapeutic response.

Restrict fluid intake.

Sub-Q

Children ≥12 years of age: Usually, 2–4 mcg daily by sub-Q injection given in 2 divided doses.

Generally, administer one-tenth of the maintenance intranasal dosage parenterally in patients being switched from intranasal to sub-Q injection therapy.

Use lowest effective dosage. During long-term use, patients rarely may develop tolerance to drug and require cautious increase in dosage to achieve an adequate therapeutic response.

Restrict fluid intake.

Primary Nocturnal Enuresis

Oral

Children ≥6 years of age: Initially, 0.2 mg at bedtime; dose may be adjusted up to 0.6 mg to achieve desired response. In children being switched from intranasal to oral therapy, initiate oral therapy the night following (24 hours after) the last intranasal dose. Duration of therapy not established in pediatric patients responding to therapy; some experts have suggested it is reasonable to continue therapy for 3–6 months, and after 3–6 months, therapy can be withdrawn and the patient reevaluated.

Restrict fluid intake for a minimum of 1 hour before drug administration and continue fluid restriction until next morning or at least 8 hours after drug administration. Some experts recommend that not more than 240 mL of fluid be consumed by children on any night when drug is used.

Interrupt drug therapy during episodes of fluid and/or electrolyte imbalance (e.g., systemic infections, fever, recurrent vomiting or diarrhea) and under conditions associated with increased water intake (e.g., extremely hot weather, vigorous exercise).

Hemophilia A

Intranasal

Children 11 months to 12 years of age: Usually, 300 mcg (0.1 mL or 1 spray from the spray pump into each nostril of a solution containing 1.5 mg/mL). Dosage of 150 mcg (0.1 mL or 1 spray from the spray pump into a single nostril of a solution containing 1.5 mg/mL) may be sufficient in patients who weigh <50 kg. Administer 2 hours prior to surgery if using preoperatively.

IV

Children ≥3 months of age: Usually, 0.3 mcg/kg by slow IV infusion; administer 30 minutes prior to scheduled procedure if using preoperatively.

Restrict fluid intake.

von Willebrand Disease

Type 1

Intranasal

Children 11 months to 12 years of age: Usually, 300 mcg (0.1 mL or 1 spray from the spray pump into each nostril of a solution containing 1.5 mg/mL). Dosage of 150 mcg (0.1 mL or 1 spray from the spray pump into a single nostril of a solution containing 1.5 mg/mL) may be sufficient in patients who weigh <50 kg. Administer 2 hours prior to surgery if using preoperatively.

IV

Children ≥3 months of age: Usually, 0.3 mcg/kg by slow IV infusion; administer 30 minutes prior to scheduled procedure if using preoperatively.

Restrict fluid intake.

Diagnostic Uses†

Testing for Renal Urine Concentrating Capacity†

Intranasal

10 mcg (0.1 mL of a solution containing 0.1 mg of drug per mL) has been administered intranasally in nonfasting infants 1–12 weeks of age.

20 mcg (0.2 mL of a solution containing 0.1 mg of drug per mL) has been administered intranasally in nonfasting children 2–15 years of age.

Urine sample was collected in 1–5 hours and specific gravity of urine was determined. An average individual usually concentrates urine to a specific gravity of ≥1.020 under test conditions.

Adults

Diabetes Insipidus

Neurohypophyseal

Intranasal

10–40 mcg (0.1–0.4 mL or 1–4 sprays from the spray pump of a solution containing 0.1 mg/mL) given intranasally in 1–3 divided doses daily.

Alternatively, 5–40 mcg (0.05–0.4 mL of a solution containing 0.1 mg/mL) has been recommended.

Most adults require 20 mcg daily administered in 2 divided doses in the morning and the evening.

Use lowest effective dosage; about 25–33% of adults and children controlled with a single daily dose.

Restrict fluid intake.

Oral

Initially, 0.05 mg twice daily; adjust subsequent dosage according to response.

0.1–0.8 mg daily given in divided doses is optimal dosage range for most patients.

Increase or decrease total daily dosage in the range of 0.1–1.2 mg divided into 2 or 3 daily doses as needed to obtain adequate antidiuresis.

Initiate oral therapy 12 hours after the last intranasal dose in patients who previously received intranasal therapy.

Restrict fluid intake.

IV

Usually, 2–4 mcg daily by IV injection given in 2 divided doses.

Generally, administer one-tenth of the maintenance intranasal dosage parenterally in patients being switched from intranasal to direct IV injection therapy.

Use lowest effective dosage. During long-term use, patients rarely may develop tolerance to drug and require cautious increase in dosage to achieve an adequate therapeutic response.

Restrict fluid intake.

Sub-Q

Usually, 2–4 mcg daily by sub-Q injection given in 2 divided doses.

Generally, administer one-tenth of the maintenance intranasal dosage parenterally in patients being switched from intranasal to sub-Q injection therapy.

Use lowest effective dosage. During long-term use, patients rarely may develop tolerance to drug and require cautious increase in dosage to achieve an adequate therapeutic response.

Restrict fluid intake.

Primary Nocturnal Enuresis

Oral

Initially, 0.2 mg at bedtime; dose may be adjusted up to 0.6 mg to achieve desired response. Initiate oral therapy the night following (24 hours after) the last intranasal dose in patients previously on intranasal therapy.

Restrict fluid intake for a minimum of 1 hour before drug administration and continue fluid restriction until next morning or at least 8 hours after drug administration.

Interrupt drug therapy during episodes of fluid and/or electrolyte imbalance (e.g., systemic infections, fever, recurrent vomiting or diarrhea) and under conditions associated with increased water intake (e.g., extremely hot weather, vigorous exercise).

Hemophilia A

Intranasal

Usually, 300 mcg (0.1 mL or 1 spray from the spray pump into each nostril of a solution containing 1.5 mg/mL). Dosage of 150 mcg (0.1 mL or 1 spray from the spray pump into a single nostril of a solution containing 1.5 mg/mL) may be sufficient in patients who weigh <50 kg. Administer 2 hours prior to surgery if using preoperatively.

IV

Usually, 0.3 mcg/kg by slow IV infusion; administer 30 minutes prior to scheduled procedure if using preoperatively.

Restrict fluid intake.

von Willebrand Disease

Type 1

Intranasal

Usually, 300 mcg (0.1 mL or 1 spray from the spray pump into each nostril of a solution containing 1.5 mg/mL). Dosage of 150 mcg (0.1 mL or 1 spray from the spray pump into a single nostril of a solution containing 1.5 mg/mL) may be sufficient in patients who weigh <50 kg. Administer 2 hours prior to surgery if using preoperatively.

IV

Usually, 0.3 mcg/kg by slow IV infusion; administer 30 minutes prior to scheduled procedure if using preoperatively.

Restrict fluid intake.

Diagnostic Uses†

Testing for Renal Urine Concentrating Capacity†

Intranasal

10–40 mcg (0.1–0.4 mL of a solution containing 0.1 mg of drug per mL) has been administered intranasally to fasting or nonfasting adults.

Urine sample was collected in 1–5 hours and specific gravity of urine was determined. Average individual usually concentrates urine to a specific gravity of ≥1.020 under test conditions.

Special Populations

Geriatric Patients

Select dosage with caution, usually initiating therapy at the low end of the dosing range because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.

Cautions for Desmopressin Acetate

Contraindications

• Known hypersensitivity to desmopressin acetate or any ingredient in the formulation.

• Moderate to severe renal impairment (Cl_cr <50 mL/minute).

• Hyponatremia or a history of hyponatremia.

Warnings/Precautions

Warnings

Water Intoxication

In late 2007, FDA reported results of a review of 61 postmarketing cases of hyponatremic-related seizures associated with use of desmopressin. In 55 cases, sodium concentrations ranged from 104–130 mEq/L during the seizure event. Two of these 55 cases were fatal; both patients experienced hyponatremia and seizures. However, direct contribution of drug to fatalities not clear. Intranasal formulations were used in 36 cases; 25 of these cases involved pediatric patients (i.e., patients <17 years of age). Most commonly reported indication for use in the 25 pediatric patients was nocturnal enuresis. In 39 of the 61 cases, patients received at least one concomitant drug or disease that also may be associated with hyponatremia and/or seizures. As a result, use of intranasal preparations for treatment of primary nocturnal enuresis no longer is approved by FDA; other approved indications for individual intranasal preparations were not changed.

Reserve intranasal preparations for situations in which oral therapy is not feasible.

Use with caution in patients at risk for water intoxication with hyponatremia.

Hyponatremia reported very rarely during international postmarketing surveillance. Desmopressin is a potent antidiuretic and use may result in water intoxication and/or hyponatremia; hyponatremia may be fatal unless properly diagnosed and treated. Fluid restriction recommended; careful medical supervision required.

Carefully adjust fluid intake downwards, particularly in pediatric and geriatric patients, to reduce the risk of potential water intoxication and hyponatremia. Observe all patients for signs and symptoms associated with hyponatremia (i.e., headache, nausea/vomiting, decreased serum sodium, weight gain, restlessness, fatigue, lethargy, disorientation, depressed reflexes, appetite loss, irritability, muscle weakness, spasms or cramps, abnormal mental status [e.g., hallucinations, decreased consciousness, confusion]); severe symptoms may include seizure, coma, and/or respiratory arrest. Consider the possibility of a rare occurrence of a substantial decrease in plasma osmolality that may result in seizures, which may lead to coma.

Use with caution in patients with habitual or psychogenic polydipsia and in patients who are receiving certain drugs (e.g., tricyclic antidepressants, SSRIs) as these patients may be more likely to drink excessive amounts of water resulting in an increased risk for hyponatremia. (See Specific Drugs under Interactions.)

Type 2B von Willebrand Disease

Do not use in patients with type 2B or platelet-type (pseudo) von Willebrand disease^† because of the risk of platelet aggregation and thrombocytopenia. (See von Willebrand Disease under Uses.)

Sensitivity Reactions

Hypersensitivity Reactions

Severe allergic reactions reported rarely. Anaphylaxis reported rarely with IV and intranasal administration, including isolated cases of fatal anaphylaxis with IV administration.

Not known whether antibodies to drug are produced after repeated administration.

General Precautions

Cardiovascular Effects

Changes in BP resulting in either a slight increase in BP, which may respond to dosage reduction, or a transient decrease in BP and a compensatory increase in heart rate reported infrequently.

Thrombotic events (e.g., thrombosis, acute cerebrovascular thrombosis, acute MI) reported rarely in patients predisposed to thrombus formation; causal relationship to drug not determined.

Use with caution in patients with coronary artery insufficiency and/or hypertensive cardiovascular disease or in patients predisposed to thrombus formation.

Diseases Associated with Fluid and Electrolyte Imbalances

Use with caution in patients with conditions associated with fluid and electrolyte imbalances (e.g., cystic fibrosis, heart failure, renal disorders); these patients are prone to hyponatremia.

Patient Monitoring

Diabetes Insipidus or Polyuria and Polydipsia Associated with Head Trauma or Surgery: Monitor urine volume and osmolality, and in some cases, plasma osmolality.

Primary Nocturnal Enuresis: Monitor serum electrolytes at least once if therapy is continued for >7 days.

Hemophilia A: Monitor factor VIII and factor VIII/ristocetin cofactor (von Willebrand factor) activities, factor VIII antigen concentrations, and aPTT. Determine factor VIII coagulant activity prior to initiating therapy for hemostasis; do not rely upon drug if factor VIII coagulant activity is <5% of normal.

von Willebrand Disease: Monitor factor VIII and factor VIII/ristocetin cofactor activities and factor VIII/von Willebrand factor antigen concentrations to ensure an adequate response is being achieved; determination of skin bleeding time also may be useful.

Specific Populations

Pregnancy

Category B.

Lactation

Not known whether drug is distributed into milk; use with caution.

Pediatric Use

Carefully restrict fluid intake in pediatric patients to prevent possible hyponatremia and water intoxication.

Intranasal therapy has no effect on growth hormone, prolactin, or LH concentrations in children.

Diabetes Insipidus:Desmopressin tablets have been used safely for up to 44 months in pediatric patients ≥4 years of age with diabetes insipidus. In younger pediatric patients, adjust dosage according to individual need to prevent excessive decrease in plasma osmolality resulting in hyponatremia and possible seizures.

Safety and efficacy of desmopressin injection not established in pediatric patients <12 years of age with diabetes insipidus.

Carefully adjust dosage of oral therapy or nasal solution (containing 0.1 mg of drug per mL) according to individual needs and tolerance in pediatric patients with diabetes insipidus, with particular attention to the risk of an extreme decrease in plasma osmolality and resulting hyponatremia or seizures in young children.

Occasional change in response to nasal solution containing 0.1 mg of drug per mL in pediatric patients with diabetes insipidus reported (e.g., decreased responsiveness, shortened duration of effect), usually after periods >6 months. No evidence that change in responsiveness results from development of binding antibodies; may result from local inactivation of peptide.

Intranasal drug preferred to vasopressin injection and oral antidiuretic agents (e.g., chlorpropamide) because of frequency of adverse effects of these agents in pediatric patients with diabetes insipidus.

Nocturnal Enuresis: Desmopressin tablets have been used safely for <6 months in pediatric patients ≥6 years of age with primary nocturnal enuresis.

Interrupt therapy during acute intercurrent illness characterized by fluid and/or electrolyte imbalance (e.g., systemic infections, fever, recurrent vomiting or diarrhea) and under conditions associated with increased water intake (e.g., extremely hot weather, vigorous exercise).

Hemophilia or von Willebrand Disease: Do not use the nasal solution containing 1.5 mg of drug per mL for the treatment of hemophilia A or von Willebrand disease in pediatric patients <11 months of age; safety and efficacy established in pediatric patients 11 months to 12 years of age.

Do not use desmopressin injection for the management of hemophilia A or von Willebrand disease in pediatric patients <3 months of age.

Geriatric Use

Carefully restrict fluid intake in geriatric patients to prevent possible hyponatremia and water intoxication. Hyponatremia and fluid overload reported during postmarketing surveillance.

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger patients. Other reported clinical experience has not identified differences in response between geriatric patients and younger adults.

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.

Substantially eliminated by kidneys; risk of toxic reactions may be greater in patients with impaired renal function. Monitor renal function and adjust dosage accordingly since geriatric patients are more likely to have decreased renal function.

Renal Impairment

Contraindicated in patients with moderate to severe renal impairment (Cl_cr <50 mL/minute).

Common Adverse Effects

With intranasal therapy, adverse effects may include transient headache, nausea, nasal congestion, rhinitis, flushing (e.g., facial), mild abdominal cramps or pain, epistaxis, sore throat, cough, upper respiratory infection, dizziness, conjunctivitis, ocular edema, lacrimation disorder, itchy or light-sensitive eyes, asthenia, chills, warm feeling, nostril pain, vomiting, GI disorder, somnolence, insomnia, pain, chest pain, palpitations, tachycardia, dyspepsia, edema, agitation, balanitis, vulval pain, increased BP, hyponatremia, severe allergic reactions (including anaphylaxis), convulsion, coma.

With oral therapy, adverse effects may include increased AST, headache, abnormal thinking, diarrhea, edema-weight gain.

With parenteral therapy, adverse effects may include transient headache, nausea, mild abdominal cramps, vulval pain, injection site reactions (local erythema, swelling, burning or severe pain), facial flushing, BP changes (increased BP; decreased BP with compensatory increased heart rate), tachycardia, hyponatremia, excessive water retention, water intoxication, severe allergic reactions (including anaphylaxis), thrombotic events (acute cerebrovascular thrombosis, acute MI).

Drug Interactions

Drugs that Increase the Risk of Water Intoxication with Hyponatremia

Use with caution in patients receiving concomitant therapy with drugs that may increase the risk of water intoxication with hyponatremia.

Specific Drugs

Desmopressin Acetate Pharmacokinetics

Absorption

Bioavailability

About 10–20% of a dose is absorbed through nasal mucosa following intranasal administration.

Minimally absorbed from GI tract following oral administration; bioavailability is about 5% compared with intranasal administration and about 0.16% compared with IV administration of the drug.

Peak plasma concentrations attained by 0.9 or 1.5 hours following oral or intranasal administration, respectively.

Bioavailability of a nasal solution (containing 1.5 mg of drug per mL) is about 3.3–4.1%; peak plasma concentrations attained 40–45 minutes after a dose.

Exact fraction of drug absorbed following sub-Q injection not quantitatively determined; bioavailability determined qualitatively using urine output data.

Onset

Antidiuretic effects occur within 15–60 minutes or at 60 minutes and peak in 1–5 or 4–7 hours following intranasal or oral administration, respectively.

Increased plasma concentrations of factor VIII and von Willebrand factor evident within 30 minutes and peak at about 1.5 hours following intranasal administration of 150–450 mcg of drug (1–3 sprays of a solution containing 1.5 mg of drug per mL).

Increased plasma factor VIII activity occurs within 15–30 minutes and peaks between 1.5–2 hours following IV infusion.

Duration

Varies among patients with a specific dose.

Antidiuretic effects persist 5–21 hours and abruptly end over a period of 60–90 minutes following intranasal administration.

Special Populations

Nasal congestion reportedly does not interfere with efficacy of intranasal drug, however, increased dosage may be required.

Percentage increase of factor VIII concentrations in patients with mild hemophilia A and von Willebrand disease not substantially different from healthy individuals.

Distribution

Extent

Not known whether distributed into human milk or crosses placenta.

Elimination

Metabolism

Metabolic fate not known.

Does not appear to be degraded by aminopeptidases or other peptidases that cleave oxytocin and endogenous vasopressin in the plasma during late pregnancy.

Elimination Route

Excreted principally in urine.

Half-life

3.3–3.5 hours following intranasal administration of 150–450 mcg of drug (1–3 sprays of a solution containing 1.5 mg of drug per mL).

1.5–2.5 hours (on average and independent of dosage) following oral administration.

Biphasic; mean initial and terminal plasma half-life of 7.8 and 75.5 minutes (range: 0.4–4 hours), respectively, following IV or intranasal (solution containing 0.1 mg of drug per mL) administration.

Special Populations

Renal clearance of drug decreases with decreasing renal function. Terminal half-lives of desmopressin averaged 3.7, 4.8, 7.2, or 10 hours following administration of a single IV dose of 2 mcg of drug in individuals with normal renal function (average Cl_Cr of 103 mL/minute), mild renal impairment (average Cl_Cr of 72 mL/minute), moderate renal impairment (average Cl_Cr of 37 mL/minute), or severe renal impairment (average Cl_Cr of 16 mL/minute; not on dialysis), respectively.

Stability

Storage

Intranasal

Solution

Commercially available nasal solutions preserved with benzalkonium chloride: Controlled room temperature (20–25°C, not to exceed 25°C); store container in upright position.

Commercially available nasal solutions preserved with chlorobutanol: 2–8°C; stable for 3 weeks at controlled room temperature (20–25°C).

Commercially available nasal solutions containing 1.5 mg of drug per mL: Discard 6 months after opening.

Oral

Tablets

20–25°C; avoid exposure to excessive heat or light.

Parenteral

Injection

2–8°C; avoid freezing.

Actions

• Synthetic analog of arginine vasopressin (antidiuretic hormone [ADH]); vasopressin maintains serum osmolality within a normal range by increasing reabsorption of water by the collecting ducts in the kidneys resulting in increased urine osmolality and decreased urinary flow rate.

• Desmopressin has same effects on water reabsorption as does vasopressin in patients with neurohypophyseal diabetes insipidus.

• Elicits a greater antidiuretic response, on a weight basis, than does arginine vasopressin.

• Therapeutic doses do not directly affect urinary sodium or potassium excretion, or serum sodium, potassium, or creatinine concentrations.

• Antidiuretic potency of IV administration is about 10 times that following intranasal administration.

• Dose-dependent increases in plasma factor VIII (antihemophilic factor), plasminogen activator, and, to a lesser degree, factor VIII-related antigen and ristocetin cofactor activities.

• Rapidly increases plasminogen activator activity following IV administration; however, clinically important fibrinolysis not reported to date.

• Elicits a greater increase in plasma factor VIII activity, on a weight basis, than does arginine vasopressin in patients with hemophilia or type I von Willebrand disease.

• Reduced smooth muscle contracting and vasopressor properties compared with vasopressin and lypressin (no longer commercially available in the US); mean arterial pressure may increase as much as 15 mm Hg with intranasal doses of ≥40 mcg.

• Usual intranasal doses do not cause skin pallor or severe smooth muscle or abdominal cramps, unlike vasopressin and lypressin.

• Not reported to stimulate uterine contractions.

• Does not stimulate adrenocorticotropic hormone release or increase plasma cortisol concentrations, unlike vasopressin.

Advice to Patients

• Importance of discussing with patient and/or guardian the risk of potential water intoxication and/or hyponatremia, fluid restriction (particularly in pediatric and geriatric patients), and monitoring of fluid intake (particularly during acute intercurrent illness [e.g., systemic infections, fever, recurrent vomiting or diarrhea] and under conditions associated with increased water intake [e.g., extremely hot weather, vigorous exercise]). Importance of promptly informing clinicians if the patient’s fluid intake changes or if symptoms of hyponatremia (e.g., nausea, vomiting, fatigue, muscle cramps or weakness) occur.

• Importance of instructing patients on proper use of nasal tube or spray pump in order to obtain optimum results. Importance of informing patients to consult patient instructions on nasal spray provided by the manufacturer before use. Importance of administering intranasal preparations in children under adult supervision in order to monitor dose and fluid intake.

• Importance of informing patients that a bottle of nasal solution containing 0.1 mg of drug per mL accurately delivers 50 doses of 10 mcg of drug per dose. Discard any solution remaining after 50 doses, since the amount delivered thereafter may be substantially <10 mcg of drug. Do not attempt to transfer any remaining solution to another bottle.

• Importance of informing patients that a bottle of nasal solution containing 1.5 mg of drug per mL accurately delivers 25 doses of 150 mcg of drug per dose. Discard any solution remaining after 25 doses, since the amount delivered thereafter may be substantially <150 mcg of drug. Do not attempt to transfer any remaining solution to another bottle.

• Importance of patients receiving nasal solution containing 1.5 mg of drug per mL to inform clinicians if bleeding is not controlled.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs (e.g., tricyclic antidepressants, SSRIs, chlorpromazine, opiates, NSAIAs, lamotrigine, carbamazepine), as well as any concomitant illnesses (e.g., hyponatremia, habitual or psychogenic polydipsia, cystic fibrosis, heart failure, renal disorders).

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Reload page with references included

Frequently asked questions

• How does Noctiva work?
• What is the difference in Nocdurna dosage between men and women?

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