Lypressin (Systemic)


VA CLASSIFICATION
Primary: HS702
Secondary: CV900

Commonly used brand name(s): Diapid.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Antidiuretic (central diabetes insipidus)—

Indications

Accepted

Diabetes insipidus, central (treatment)—Lypressin is indicated for the prevention or control of polydipsia, polyuria, and dehydration associated with central diabetes insipidus caused by insufficient antidiuretic hormone.
—Lypressin may be useful in patients who are unresponsive to other forms of therapy or who have shown various adverse reactions to other preparations of antidiuretic hormone of animal origin.
—Lypressin is ineffective in the treatment of polyuria associated with nephrogenic or psychogenic diabetes insipidus, renal disease, hypokalemia, hypercalcemia, or the administration of demeclocycline or lithium.


Pharmacology/Pharmacokinetics

Physicochemical characteristics:
Source—
    Lypressin is a synthetic vasopressin analog.
Molecular weight—
    1056.22

Mechanism of action/Effect:

Increases water reabsorption in the kidney by increasing the cellular permeability of the collecting ducts, resulting in an increase in urine osmolality with a concurrent decrease in urine output.


Other actions/effects:

Little pressor activity.

Absorption:

Rapid from nasal mucosa.

Biotransformation:

Renal and hepatic.

Half-life:

Approximately 15 minutes.

Onset of action:

Within 1 hour.

Time to peak effect:

30 to 120 minutes.

Duration of action:

3 to 4 hours.

Elimination:
    Renal, a small amount unchanged.


Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to vasopressin may also be sensitive to lypressin.

Carcinogenicity

Studies have not been done. {01}

Pregnancy/Reproduction

Pregnancy—
Studies have not been done in either animals or humans. {01}

FDA Pregnancy Category C. {01}

Breast-feeding

It is not known whether lypressin is distributed into breast milk. {01} However, problems in humans have not been documented.

Pediatrics

Appropriate studies on the relationship of age to the effects of lypressin have not been performed in the pediatric population. However, pediatrics-specific problems that would limit the usefulness of this medication in children are not expected.


Geriatrics


No information is available on the relationship of age to the effects of lypressin in geriatric patients.

Drug interactions and/or related problems
The following drug interactions and/or related problems have been selected on the basis of their potential clinical significance (possible mechanism in parentheses where appropriate)—not necessarily inclusive (» = major clinical significance):


Note: Combinations containing any of the following medications, depending on the amount present, may also interact with this medication.

Carbamazepine or
Chlorpropamide or
Clofibrate    (may potentiate the antidiuretic effect of lypressin when used concurrently)


Demeclocycline or
Lithium or
Norepinephrine    (may decrease the antidiuretic effect of lypressin when used concurrently)


Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Risk-benefit should be considered when the following medical problems exist
Allergic rhinitis or
Nasal congestion or
Upper respiratory infection    (may interfere with absorption of lypressin through the nasal mucosa)


Hypertensive cardiovascular disease    (although pressor effects of lypressin are minimal)


Sensitivity to lypressin{01}


Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention
Incidence rare
    
Inadvertent inhalation (continuing cough; feeling of tightness in chest; shortness of breath; troubled breathing)
    
water intoxication and overdose (coma; confusion; continuing headache; drowsiness; problems with urination; seizures; weight gain)



Those indicating need for medical attention only if they continue or are bothersome
Incidence less frequent or rare
    
Abdominal or stomach cramps
    
excessive administration with drippage into pharynx (heartburn)
    
headache
    
increased bowel movements
    
irritation or pain in the eye
    
itching, irritation, or sores inside nose
    
runny or stuffy nose





Overdose
For specific information on the agents used in the management of lypressin overdose, see Furosemide in Diuretics, Loop (Systemic) monograph.

For more information on the management of overdose or unintentional ingestion, contact a Poison Control Center (see Poison Control Center Listing ).

Treatment of overdose
To enhance elimination—Diuresis with furosemide and hypertonic saline if there is a risk of congestive heart failure. {01}

Supportive care—Withdrawal of lypressin and restriction of fluid intake. {01} Correction of electrolyte imbalance. {01} Patients in whom intentional overdose is known or suspected should be referred for psychiatric consultation. {01}


Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Lypressin (Systemic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Allergies to lypressin or vasopressin

Proper use of this medication
» Importance of not using more medication than the amount prescribed

Proper administration technique

» Proper dosing
Missed dose: Using as soon as possible; not using at all if almost time for next dose; not doubling doses

» Proper storage


Side/adverse effects
Signs of potential side effects, especially inadvertent inhalation or water intoxication


General Dosing Information
Lypressin is administered intranasally; it should not be inhaled.

Patients with nasal congestion, allergic rhinitis, and upper respiratory infections may experience decreased efficacy because of a decrease in absorption through the nasal mucosa. Larger doses of lypressin or adjunctive therapy may be required in such patients.

Since more than 2 or 3 sprays per nostril usually results in wastage, it is recommended that the time interval between sprays be reduced rather than increasing the number of sprays if a patient requires more than 3 sprays.


Nasal Dosage Forms

LYPRESSIN NASAL SOLUTION USP

Usual adult and adolescent dose
Antidiuretic
Intranasal, 1 or 2 sprays in each nostril four times a day.

Note: Whenever the frequency of urination increases or increased thirst develops, the patient may administer 1 or 2 sprays to control these symptoms.
If the regular daily dosage of lypressin does not control nocturia, an additional dose may be given at bedtime.
The dosage has ranged from 1 spray per day at bedtime to 10 sprays in each nostril every three to four hours.



Usual pediatric dose
Children up to 6 weeks of age—Safety and efficacy have not been established in children less than 6 weeks of age. {01}

Children 6 weeks of age and over— See Usual adult and adolescent dose.{01}

Strength(s) usually available
U.S.—


0.185 mg (equivalent to 50 USP Posterior Pituitary Units) per mL; or approximately 0.007 mg (equivalent to 2 Posterior Pituitary Units) per spray (Rx) [Diapid (methylparaben) (propylparaben)]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. Protect from freezing.

Auxiliary labeling:
   • For the nose.

Note: Instruct patient to assume a vertical position with head upright and to hold bottle upright when administering the spray.




Revised: 07/01/1993



References
  1. Diapid package insert (Sandoz—US), 6/1/88.
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