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Desmopressin Rhinal Tube (Desmopressin Acetate Rhinal Tube) - Description and Clinical Pharmacology

 
 



DESCRIPTION

Desmopressin Acetate Rhinal Tube is a synthetic analogue of the natural pituitary hormone 8-arginine vasopressin (ADH), an antidiuretic hormone affecting renal water conservation. It is chemically defined as follows:

1-(3-mercaptopropionic acid)-8-D-arginine vasopressin monoacetate (salt) trihydrate.

Desmopressin Acetate Rhinal Tube is provided as an aqueous solution for intranasal use.

Each mL contains:

Desmopressin acetate 0.1 mg
Chlorobutanol 5.0 mg
Sodium Chloride 9.0 mg
Hydrochloric acid to adjust pH to approximately 4

CLINICAL PHARMACOLOGY

Desmopressin Acetate Rhinal Tube contains as active substance desmopressin acetate, a synthetic analogue of the natural hormone arginine vasopressin. One mL (0.1 mg) of intranasal Desmopressin acetate has an antidiuretic activity of about 400 IU; 10 µg of desmopressin acetate is equivalent to 40 IU.

  1. The biphasic half-lives for intranasal Desmopressin acetate were 7.8 and 75.5 minutes for the fast and slow phases, compared with 2.5 and 14.5 minutes for lysine vasopressin, another form of the hormone used in this condition. As a result, intranasal Desmopressin acetate provides a prompt onset of antidiuretic action with a long duration after each administration.
  2. The change in structure of arginine vasopressin to Desmopressin acetate has resulted in a decreased vasopressor action and decreased actions on visceral smooth muscle relative to the enhanced antidiuretic activity, so that clinically effective antidiuretic doses are usually below threshold levels for effects on vascular or visceral smooth muscle.
  3. Desmopressin acetate administered intranasally has an antidiuretic effect about one-tenth that of an equivalent dose administered by injection.

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