STIMATE- desmopressin acetate spray, metered
CSL Behring LLC
Rx only
DESCRIPTION
Stimate � (desmopressin acetate) is a synthetic analogue of the natural pituitary hormone 8-arginine vasopressin (ADH), an antidiuretic hormone affecting renal water conservation. Stimate � Nasal Spray contains 1.5 mg/mL desmopressin acetate in an aqueous solution at a pH of approximately 5. Stimate � Nasal Spray's compression pump delivers 0.1 mL (150 mcg) of solution per spray.
Mol. Wt. 1183.34 Empirical formula: C46 H64 N14 O12 S2 �C2 H4 O2 �3H2 O
CLINICAL PHARMACOLOGY
Stimate � Nasal Spray contains as active substance, desmopressin acetate, which is a synthetic analogue of the natural hormone arginine vasopressin. One spray or 0.1 mL (150 mcg) of Stimate � Nasal Spray solution has an antidiuretic activity of about 600 International Units.
Desmopressin acetate has been shown to be more potent than arginine vasopressin in increasing plasma levels of Factor VIII activity in patients with hemophilia and von Willebrand's disease Type I.
Dose-response studies were performed in healthy persons using doses of 150 to 450 mcg, administered as one to three sprays. The response to Stimate � Nasal Spray is dose-related, with maximal plasma levels of 150 to 250 percent of initial concentrations achieved for both Factor VIII and von Willebrand factor. The increase is rapid and evident within 30 minutes, reaching a maximum at about 1.5 hours.
Stimate Indications and Usage
Before the initial therapeutic administration of Stimate � Nasal Spray , the physician should establish that the patient shows an appropriate change in the coagulation profile following a test dose of intranasal administration of Stimate � Nasal Spray.
Desmopressin acetate is also available as a solution for injection (DDAVP� Injection) when the intranasal route may be compromised. These situations include nasal congestion and blockage, nasal discharge, atrophy of nasal mucosa, and severe atrophic rhinitis. Intranasal delivery may also be inappropriate where there is an impaired level of consciousness.
Hemophilia A
Stimate � Nasal Spray is indicated for patients with hemophilia A with Factor VIII coagulant activity levels greater than 5%.
Desmopressin acetate will also stop bleeding in patients with hemophilia A with episodes of spontaneous or trauma-induced injuries such as hemarthroses, intramuscular hematomas or mucosal bleeding.
In the outpatient setting during two clinical trials where patients recorded bleeding episodes, Stimate � Nasal Spray provided effective hemostasis 100% of the time in 2 of the 5 patients. For those patients not responding in 100% of bleeding occasions, 45% (14 of 31) of bleeding episodes were effectively controlled with Stimate � Nasal Spray.
Desmopressin acetate is not indicated for the treatment of hemophilia A with Factor VIII coagulant activity levels equal to or less than 5%, or for the treatment of hemophilia B, or in patients who have Factor VIII antibodies.
von Willebrand's Disease (Type I)
Stimate � Nasal Spray is indicated for patients with mild to moderate classic von Willebrand's disease (Type I) with Factor VIII levels greater than 5%.
Desmopressin acetate will also stop bleeding in mild to moderate von Willebrand's disease patients with episodes of spontaneous or trauma-induced injuries such as hemarthroses, intramuscular hematomas, mucosal bleeding or menorrhagia.
In the outpatient setting during two clinical trials where patients recorded bleeding episodes, Stimate � Nasal Spray provided effective hemostasis 100% of the time in 75% of the patients (n=16). For those patients not responding in 100% of bleeding occasions, 78% (64 of 82) of bleeding episodes were effectively controlled with Stimate � Nasal Spray.
Patients may respond in a variable fashion depending on the type of molecular defect they have. Bleeding time and Factor VIII coagulant activity, ristocetin cofactor activity, and von Willebrand factor antigen should be checked after initial administration of Stimate � Nasal Spray to ensure that adequate levels have been achieved.
Stimate � Nasal Spray is not indicated for the treatment of severe classic von Willebrand's disease (Type I) and when there is evidence of an abnormal molecular form of Factor