Indications
PO, SL, Subcut, IV, Intranasal: Treatment of central
diabetes insipidus caused by a deficiency of vasopressin.
IV, Intranasal: Controls bleeding in certain types
of hemophilia and von Willebrand’s disease. Intranasal:
Nocturia due to nocturnal polyuria in patients who
awaken 2 times per night to void (Noctiva only). SL:
Nocturia in adults with 4 nocturnal voids (Noctdurna
only). PO, SL: Primary nocturnal enuresis.
Action
An analogue of naturally occurring vasopressin (antidiuretic
hormone). Primary action is enhanced reabsorption
of water in the kidneys. Therapeutic Effects:
Prevention of nocturnal enuresis. Maintenance
of appropriate body water content in diabetes insipidus.
Control of bleeding in certain types of hemophilia or
von Willebrand’s disease. Reduction in number of episodes
of nocturia.
Pharmacokinetics
Absorption: 1% absorbed following oral or SL administration;
nasal solution 10–20% absorbed; nasal
spray 3–4% absorbed.
Distribution: Distribution not fully known. Enters
breast milk.
Metabolism and Excretion: Primarily excreted in
urine.
Half-life: PO—1.5–2.5 hr; SL—2.8 hr; IV—75
min (qin renal impairment); Intranasal—1.8–3.5
hr.
TIME/ACTION PROFILE (PO, intranasal
antidiuretic effect; IV effect on factor
VIII activity)
ROUTE ONSET PEAK DURATION
PO 1 hr 4–7 hr unknown
SL unknown unknown unknown
Intranasal 1 hr 1–5 hr 8–20 hr
IV within min 15–30 min 3 hr†
†4–24 hr in mild hemophilia A.
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Hypersensitivity
to chlorobutanol; Patients with severe type I, type
IIB, or platelet-type (pseudo) von Willebrand’s disease,
hemophilia A with factor VIII levels 5% or hemophilia
B; Renal impairment (CCr 50 mL/min); Hyponatremia;
Polydipsia (Noctiva only); Primary nocturnal enuresis
(Noctiva only); Concurrent use with loop diuretics
or systemic/inhaled glucocorticoids (Noctiva only);
Known or suspected syndrome of inappropriate antidiuretic
hormone secretion (Noctiva only); Conditions
that can lead to electrolyte or fluid imbalances, including
gastroenteritis, salt-wasting nephropathies, or infection
(Noctiva only); HF (NYHA class II-IV) (Noctiva
only); Uncontrolled hypertension (Noctiva only).
Use Cautiously in: Angina pectoris; Hypertension;
Patients at risk for hyponatremia; Patients at risk forq
intracranial hypertension (Noctiva only); Urinary retention
(Noctiva only); HF (NYHA class I) (Noctiva only);
Patients who require use of other intranasal medications;
Geri:qrisk of hyponatremia; OB, Lactation:
Safety not established; Noctiva not recommended for
treatment of nocturia in pregnancy.
Adverse Reactions/Side Effects
CNS: SEIZURES, dizziness, drowsiness, headache, listlessness.
EENT: intranasal—epistaxis, nasal congestion,
nasal discomfort, rhinitis, sneezing. Resp:
dyspnea. CV: hypertension, hypotension, tachycardia
(large IV doses only). GI: mild abdominal cramps,
nausea. GU: vulval pain. Derm: flushing. F and E:
fluid retention, hyponatremia. MS: back pain. Local:
phlebitis at IV site.
Interactions
Drug-Drug: Loop diuretics, systemic glucocorticoids,
or inhaled glucocorticoidsqrisk of severe
hyponatremia; concurrent use with Noctiva contraindicated.
Chlorpromazine, SSRIs, TCAs, NSAIDs, thiazide
diuretics, or carbamazepine mayqrisk of
fluid retention and hyponatremia. Demeclocycline,
lithium, or norepinephrine may diminish the antidiuretic
response to desmopressin. Large doses may enhance
the effects of vasopressors.
Route/Dosage
Two sprays of Noctiva 0.83 mcg/spray are not interchangeable
with one spray of 1.66 mcg/spray formulation;
the 1.66 mcg/spray formulation should be used
for those patients who are taking 1.66 mcg dose.
Primary Nocturnal Enuresis
PO (Adults and Children 6 yr): 0.2 mg at bedtime;
may be titrated up to 0.6 mg at bedtime to achieve desired
response.
SL (Adults and Children): 120 mcg 1 hr before bedtime;
may be titrated up to 360 mcg at bedtime to
achieve desired response.
Diabetes Insipidus
PO (Adults and Children): 0.05 mg twice daily; adjusted
as needed (usual range: 0.1–1.2 mg/day for
adults or 0.1–0.8 mg/day for children in 2–3 divided
doses).
SL (Adults and Children): 60 mcg 3 times daily; adjusted
as needed (usual range: 120–720 mcg/day in
2–3 divided doses).
Intranasal (Adults and Children 12 yr):
DDAVP—5–40 mcg (0.0.05–0.4 mL)in 1–3 divided
doses.
Intranasal (Children 3 mo–12 yr): DDAVP—5–
30 mcg (0.05–0.3 mL) in 1–2 divided doses.
Subcut, IV (Adults and Children12 yr): 2–4
mcg/day in 2 divided doses.
Subcut, IV (Children 12 yr): 0.1–1 mcg/day in 1–
2 divided doses.
Hemophilia A/von Willebrand’s disease
Intranasal (Adults and Children 50 kg): Stimate—
1 spray (150 mcg) in each nostril.
Intranasal (Adults and Children 50 kg): Stimate—
1 spray (150 mcg) in one nostril.
IV (Adults and Children 3mo): 0.3 mcg/kg, repeated
as needed.
Nocturia
SL (Adults): Women—25 mcg at bedtime; Men—50
mcg at bedtime.
Intranasal (Adults 65 yr or other patients atq
risk for hyponatremia): Noctiva—1 spray (0.83
mcg) in one nostril 30 min before bedtime; after 7
days, mayqto 1 spray (1.66 mcg) in one nostril 30
min before bedtime.
Intranasal (Adults 65 yr): Noctiva—1 spray
(1.66 mcg) in one nostril 30 min before bedtime.
Availability (generic available)
Sublingual tablet: 25 mcg, 50 mcg, 60 mcg,
120 mcg, 240 mcg. Tablets: 0.1 mg, 0.2 mg. Nasal
spray (DDAVP): 10 mcg/spray. Nasal spray
(Noctiva): 0.83 mcg/spray, 1.66 mcg/spray. Nasal
spray (Stimate): 150 mcg/spray. Rhinal tube delivery
system-nasal solution: 2.5-mL vials with applicator
tubes (0.1 mg/mL). Injection: 4 mcg/mL.
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