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US Brand Name
- DDAVP Rhinal Tube
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 IU. 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.
The percentage increase of Factor VIII and von Willebrand factor levels in patients with mild hemophilia A and von Willebrand's disease was not notably different from that observed in normal healthy individuals when treated with 300 mcg of Stimate® Nasal Spray. In patients with von Willebrand's disease, levels of Factor VIII coagulant activity and von Willebrand factor antigen remained greater than 30 U/dL for 8 hours after a 300 mcg dose of Stimate® Nasal Spray.1 After 300 mcg of Stimate® Nasal Spray, the percentage increase of Factor VIII and von Willebrand factor levels in patients with mild hemophilia A and von Willebrand's disease was less than observed after 0.3 mcg/kg of intravenous desmopressin acetate.
Plasminogen activator activity increases rapidly after intravenous desmopressin acetate infusion, but there has been no clinically significant fibrinolysis in patients treated with desmopressin acetate.
The effect of repeated intravenous desmopressin acetate administration when doses were given every 12 to 24 hours has generally shown a diminution of the Factor VIII activity increase noted after a single dose. It is possible to reproduce the initial response in some patients after an interval of one week, but other patients may require as long as 6 weeks.2
The half-life of Stimate® Nasal Spray was between 3.3 and 3.5 hours, over the range of intranasal doses, 150 to 450 mcg. Plasma concentrations of Stimate® Nasal Spray were maximal approximately 40 to 45 minutes after dosing.
The bioavailability of Stimate® Nasal Spray when administered by the intranasal route as a 1.5 mg/mL solution is between 3.3 and 4.1 percent.
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.
1. Lethagen S, Harris AS and Nilsson IM: Intranasal desmopressin (DDAVP) by spray in mild hemophilia A and von Willebrand's disease type I. Blut, 60:187-191, 1990.
2. Lethagen S, Harris AS, Sjörin E and Nilsson IM: Intranasal and intravenous administration of desmopressin: Effect on FVIII/vWF, pharmacokinetics and reproducibility. Thromb. Haemost., 58:1033-1036, 1987.
CSL Behring LLC
Stimate Drug Class
Stimate is part of the drug class:
Vasopressin and analogues
Stimate® (desmopressin acetate) is a synthetic analogue of the natural pituitary hormone 811 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. It is chemically defined as follows:
Mol. Wt. 1183.34 Empirical formula: C46H64N14O12S2 ∙C2H4O2∙3H2O
1-(3-mercaptopropionic acid)-8-D-arginine vasopressin monoacetate (salt) trihydrate.
Stimate Nasal Spray is provided as an aqueous solution for intranasal use.
Each mL contains:
|Desmopressin acetate||1.5 mg|
|Sodium chloride||7.5 mg|
|Citric acid monohydrate||1.7 mg|
|Disodium phosphate dehydrate||3 mg|
|Benzalkonium chloride||0.1 mg|
|Purified water||To 1 mL|
Desmopressin acetate has infrequently produced changes in blood pressure causing either a slight elevation in blood pressure or a transient fall in blood pressure and a compensatory increase in heart rate. The drug should be used with caution in patients with coronary artery insufficiency and/or hypertensive cardiovascular disease.
Stimate Nasal Spray should be used with caution in patients with conditions associated with fluid and electrolyte imbalance, such as cystic fibrosis, heart failure and renal disorders because these patients are prone to hyponatremia.
There have been rare reports of thrombotic events (thrombosis, acute cerebrovascular thrombosis, acute myocardial infarction) following desmopressin acetate injection in patients predisposed to thrombus formation. No causality has been determined; however, the drug should be used with caution in these patients.
Severe allergic reactions have been reported rarely. Fatal anaphylaxis has been reported in one patient who received intravenous DDAVP® (desmopressin acetate). It is not known whether antibodies to desmopressin acetate are produced after repeated administration.
Since Stimate Nasal Spray is used intranasally, changes in the nasal mucosa such as scarring, edema, or other disease may cause erratic, unreliable absorption in which case Stimate Nasal Spray should be discontinued until the nasal problems resolve. For such situations, DDAVP® Injection should be considered.
Information for Patients
Patients should be informed that the bottle accurately delivers 25 sprays of 150 mcg each. Any solution remaining after 25 sprays should be discarded since the amount delivered thereafter may be substantially less than 150 mcg of drug. No attempt should be made to transfer remaining solution to another bottle. Patients should be instructed to read accompanying directions on use of the spray pump carefully before use.
Patients should also be advised that if bleeding is not controlled, the physician should be contacted.
Laboratory tests for assessing patient status include levels of Factor VIII coagulant, Factor VIII antigen and Factor VIII ristocetin cofactor (von Willebrand factor) as well as activated partial thromboplastin time. Factor VIII coagulant activity should be determined before giving Stimate Nasal Spray for hemostasis. If Factor VIII coagulant activity is present at less than 5% of normal, Stimate Nasal Spray should not be relied on.
von Willebrand's Disease
Laboratory tests for assessing patient status include levels of Factor VIII coagulant activity, VWF:RCo and VWF:Ag.
Although the pressor activity of desmopressin acetate is very low, its use with other pressor agents should be done only with careful patient monitoring. The concomitant administration of drugs that may increase the risk of water intoxication with hyponatremia (e.g., tricyclic antidepressants, selective serotonin re-uptake inhibitors, chlorpromazine, opiate analgesics, NSAIDS, lamotrigine and carbamazepine) should be performed with caution.
DDAVP® Injection has been used with epsilon aminocaproic acid without adverse effects.
Carcinogenicity, Mutagenicity, Impairment of Fertility
There have been no long-term studies in animals to assess the carcinogenic, mutagenic or impairment of fertility potential of Stimate Nasal Spray.
Pregnancy Category B
Reproduction studies performed in rats and rabbits by the subcutaneous route at doses up to 10 mcg/kg/day have revealed no evidence of harm to the fetus due to desmopressin acetate. This dose is equivalent to 10 times (for Factor VIII stimulation) or 38 times (for diabetes insipidus) the systemic human dose based on a mg/M2 surface area.
There are no adequate and well-controlled studies in pregnant women. Several publications of desmopressin acetate's use in the management of diabetes insipidus during pregnancy are available; these include a few anecdotal reports of congenital anomalies and low birth weight babies. However, no causal connection between these events and desmopressin acetate has been established. A 15-year, Swedish epidemiologic study of the use of desmopressin acetate in pregnant women with diabetes insipidus found the rate of birth defects to be no greater than that in the general population. As opposed to preparations containing natural hormones, desmopressin acetate in antidiuretic doses has no uterotonic action and the physician will have to weigh the therapeutic advantages against the possible risks in each case.
There have been no controlled studies in nursing mothers. A single study in postpartum women demonstrated a marked change in plasma, but little if any change in assayable DDAVP® in breast milk following an intranasal dose of 10 mcg. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Stimate Nasal Spray is administered to a nursing woman.
Use in infants and children will require careful fluid intake restriction to prevent possible hyponatremia and water intoxication. Stimate Nasal Spray should not be used in infants younger than 11 months in the treatment of hemophilia A or von Willebrand's disease; safety and effectiveness in children between 11 months and 12 years of age has been demonstrated.
Clinical studies of Stimate did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently than younger subjects. However, other post marketing experience has indicated the occurrence of hyponatremia with the use of desmopressin acetate and fluid overload. Therefore, in elderly patients fluid intake should be adjusted downward in an effort to decrease the potential occurrence of water intoxication and hyponatremia. Particular attention should be paid to the possibility of the rare occurrence of an extreme decrease in plasma osmolality that may result in seizures, and that could lead to coma.
Patients who do not have need of antidiuretic hormone for its antidiuretic effect should be cautioned to ingest only enough fluid to satisfy thirst, in an effort to decrease the potential occurrence of water intoxication and hyponatremia.
As for all patients, dosing for geriatric patients should be appropriate to their clinical condition.
Signs of overdose may include confusion, drowsiness, continuing headache, problems with passing urine and rapid weight gain due to fluid retention. (See WARNINGS.) In cases of overdosage, the dosage should be reduced, frequency of administration decreased, or the drug withdrawn according to the severity of the condition.
There is no known specific antidote for desmopressin acetate or Stimate Nasal Spray.
An oral LD50 has not been established. An intravenous dose of 2 mg/kg in mice demonstrated no effect.
How is Stimate Supplied
A 2.5 mL bottle with spray pump capable of delivering 25 sprays of 150 mcg (NDC 0053-6871321 00).
Store at room temperature not to exceed 25°C (77°F) for the period indicated by the expiration date on the label. Discard six months after being opened. Store bottle in upright position.
Revised June 2013
CSL Behring LLC
King of Prussia, PA 19406-0901
US License No. 1767
PATIENT INSTRUCTION GUIDE Stimate® Nasal Spray (Pronounced Stim-ate) desmopressin acetate)
Read this patient information leaflet before you start taking Stimate® Nasal Spray and each time you get a refill. There may be new information. This information does not take the place of talking to your healthcare provider about your medical condition or your treatment.
What is the most important information I should know about Stimate Nasal Spray?
All patients using Stimate Nasal Spray are at risk for water intoxication, fluid overload and low sodium levels in the blood. You must follow your healthcare provider's instructions on limiting the amount of fluid you can drink when taking Stimate Nasal Spray.
- Do not drink more than you need to satisfy your thirst.
- You can have serious side effects such as seizures, coma, and death from drinking too much fluid.
- Children and elderly patients are at higher risk for these conditions and must follow their healthcare provider's restrictions on drinking fluids.
Call your healthcare provider right away if you have any of the following symptoms while using Stimate Nasal Spray. They may mean that your blood sodium level is low:
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Using Stimate Nasal Spray the wrong way may cause it not to work to control bleeding.
- Call your healthcare provider right away if you have any uncontrolled bleeding.
What is Stimate Nasal Spray?
Stimate Nasal Spray is a prescription medicine used to stop some types of bleeding in people with mild hemophilia A or mild to moderate von Willebrand's disease Type 1.
Stimate Nasal Spray should not be used in children under 11 months of age.
What should I tell my healthcare provider before I use Stimate® Nasal Spray?
Before taking Stimate Nasal Spray, tell your healthcare provider about all of your medical conditions, including if you:
- Have any nasal problems such as a stuffy nose, have ever had surgery on your nose, or have trouble breathing through your nose. You may need to use another form of this medicine.
- Have or have had any heart, blood circulation, or blood pressure problems. Have a condition that causes fluid or water imbalance problems such as:
- Cystic fibrosis
- Heart failure
- Kidney problems
- Have or have had a condition that causes you to be very thirsty.
- Are pregnant or plan to become pregnant. It is not known if Stimate Nasal Spray will harm your unborn baby.
- Are breast-feeding or plan to breast-feed. It is not known if Stimate Nasal Spray passes into your breast milk. You and your healthcare provider should decide if you will take Stimate Nasal Spray.
Tell your healthcare provider and pharmacist about all the medicines you take, including prescription and non-prescription medicines, such as over-the-counter medicines, vitamins, supplements and herbal remedies.
Using Stimate Nasal Spray with certain other medicines can affect the way Stimate Nasal Spray works.
Know the medicines you take. Keep a list of them and show it to your healthcare provider and pharmacist when you get a new medicine.
It is especially important to tell your healthcare provider if you take:
- Blood pressure or heart medicines
- Anti-anxiety medicines
- Pain relievers such as narcotics or non-steroidal anti-inflammatory medicines (NSAIDs)
- Seizure medicines
- Medicines for over-active urinary bladder
- Ask your healthcare provider or pharmacist if you are not sure if your medicine is one of these.
How should I use Stimate Nasal Spray?
- Use Stimate Nasal Spray exactly as your healthcare provider told you. Do not use more Stimate Nasal Spray or take it more often than your healthcare provider told you.
- The Stimate Nasal Spray pump provides the correct dose of your medicine. For detailed instructions on how to use the nasal spray pump, see the Patient Instructions for Use at the end of this leaflet.
- The nasal spray pump delivers 25 sprays of Stimate Nasal Spray and each spray contains a measured amount of medicine. Any medicine left in the spray pump after 25 sprays should be thrown away because, at that time, the amount of medicine in each spray may be a lot less than the correct amount. Do not put any leftover medicine into another bottle.
- If your symptoms do not improve, or if they become worse, contact your healthcare provider. Do not stop taking Stimate Nasal Spray without talking to your healthcare provider.
- If you use too much Stimate Nasal Spray, call your healthcare provider or go to the nearest hospital emergency department right away.
What are the possible side effects of Stimate Nasal Spray?
Stimate Nasal Spray may cause serious side effects that come from having too much water in the body. See "What is the most important information I should know about Stimate Nasal Spray?".
Common side effects of Stimate Nasal Spray include:
- Occasional facial flushing
- Nasal congestion
- Runny nose
- Sore throat
- Upper respiratory infections.
Tell your healthcare provider about any side effect that bothers you or does not go away. These are not all the possible side effects of Stimate Nasal Spray. If you have questions, talk to your healthcare provider.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
How should I store Stimate Nasal Spray?
- Store at room temperature, but not higher than 77°F (25°C).
- Throw away Stimate Nasal Spray six months after it is opened, or when the expiration date has passed, if this date is before the six months is up.
- Store Stimate Nasal Spray standing upright.
Keep Stimate Nasal Spray and all medicines out of the reach of children.
General information about Stimate Nasal Spray
Medicines are sometimes prescribed for conditions that are not mentioned in the patient leaflet. Do not use Stimate Nasal Spray for a condition for which it was not prescribed. Do not give Stimate Nasal Spray to other people, even if they have the same symptoms you have. It may harm them.
This patient information leaflet summarizes the most important information about Stimate Nasal Spray. If you would like more information about Stimate Nasal Spray, talk with your healthcare provider. You can ask your healthcare provider or pharmacist for information about Stimate Nasal Spray that is written for health professionals. For more information, go to www.Stimate.com or call CSL Behring Medical Affairs at 1-800-504-5434.
What are the ingredients in Stimate Nasal Spray?
Active ingredients: desmopressin acetate Inactive ingredients: sodium chloride, citric acid monohydrate, disodium phosphate dihydrate, benzalkonium chloride, purified water.