Acetate Nasal Spray

Desmopressin acetate is a synthetic analogue of the natural pituitary hormone 8-arginine vasopressin, an antidiuretic hormone affecting renal water conservation. It contains 1.5 mg/mL desmopressin acetate in a pH-adjusted aqueous solution with hydrochloric acid to 4.0  

Chlorobutanol (5.0 mg) and sodium chloride (9.0 mg) are the inactive ingredients. The compression pump delivers 0.1 mL (150 pg) of solution per spray 2.5 mL bottle. 

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Primary therapy is based on disease severity and type of hemorrhage.7 Most patients with mild to moderate disease and a minor bleeding episode can be treated with l-desamino-8-D-arginine vasopressin [desmopressin acetate (DDAVP)], a synthetic analog of the antidiuretic hormone vasopressin. DDAVP causes release of von Willebrand factor (vWF) and factor VIII from endogenous storage sites. This formulation increases plasma factor VIII levels by three- to fivefold within 30 minutes. The recommended dose is 0.3 mcg/kg intravenously (in 50 mL normal saline infused over 15 to 30 minutes) or subcutaneously or 300 meg intranasally via concentrated nasal spray every 12 hours. Peak effect with intranasal administration occurs 60 to 90 minutes after administration, which is somewhat later than with intravenous administration. Desmopressin infusion may be administered daily for up to 2 to 3 days. Tachyphylaxis, an attenuated response with repeated administration, may occur after several doses.8... 

For allergic rhinitis and other allergic or inflammatory nasal conditions, a nasal spray containing dexamethasone isonicotinate is available the acetate, phosphate, sodium phosphate and sodium metasulfobenzoate have also been used. 

A dose of 1 pg desmopressin acetate has antidiuretic activity that is equivalent to 4U arginine vasopressin. Desmopressin acetate has recently been evaluated in normal horses. The author and coworkers diluted desmopressin acetate (0.1 mg/ml) nasal spray in sterile water and administered 0.05pg/kg i.v. (25 pg, equivalent to 100 U of antidiuretic activity in a 500 kg horse) to horses with polyuria induced by repeated nasogastric intubation of water for 3 days. Urine was collected for 8h after desmopressin acetate administration and there was an increase in urine specific gravity to >1.020 from 2 to 7h after administration (Fig. 10.2). The drug had no effects on heart rate or systemic blood pressure. These preliminary data demonstrate that the i.v. administration of desmopressin acetate appears to be safe and a useful tool for the evaluation of horses with DI. 

NEO-SYNEPHRINE 12 h Bayer (U.S.) Oxymetazoline HCI 0.05% BKC, phenylmercuric acetate (0.002%), glycine, sorbitol Nasal spray bottle... 

Only two antidiuretic peptides are available for clinical use in the United States (1) Vasopressin (synthetic 8-l-arginine vasopressin Pitressin) is available as a sterile aqueous solution it may be administered subcutaneously, intramuscularly, or intranasally. (2) Desmopressin acetate (synthetic l-deamino-8-D-arginine vasopressin DDAVP, others) is available as a sterile aqueous solution packaged for intravenous or subcutaneous injection, in a nasal solution for intranasal administration with either a nasal spray pump or rhinal tube delivery system, and in tablets for oral administration. The therapeutic uses of vasopressin and its congeners can be divided into two main categories according to the type of vasopressin receptor involved. 

Nafarelin aoetate, another synthetic superagonist decapeptide analogue of GnRH, contains D-Nal(2) [Nal = 3-(2-naphthyl)-Ala] in place of Gly , but the C-terminus, Gly -NH2, is identical with natural GnRH (Fig. 7.12). Nafarelin acetate is available as a 0.2% nasal spray for the relief of endometriosis. Estrogen, of course, is needed for the growth of endometrial tissue thus. 

Several GnRH agonists are available, including leuprolide acetate (Lupron) and goserelin acetate (Zoladex), which are injectable agents, and nafarelin acetate (Synarel), which is administered via nasal spray. (Discussion about structure-activity relationships can be found in Chapter 7.)... 

Commercially available peptide hormones delivered as nasal spray solutions include Synarel (nafare-lin), Stimate NS (desmopressin), Suprefact (buserelin acetate), and Miacalcin (salmon calcitonin). A list of current drugs in the market, doses, and bioavailability along with a comparative bioavailability profile for oral desmopressin is presented in Table 86.3. 

Buserelin acetate Injection 1 mg/mL, 100 gg metered nasal spray. 

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