DESMOPRESSIN ACETATE

DESMOPRESSIN ACETATE- desmopressin acetate injection
Dr.Reddys’ Laboratories Inc

(desmopressin acetate)

4 mcg/mL

Rx Only

DESCRIPTION

Desmopressin Acetate Injection USP (desmopressin acetate) 4 mcg/mL is a synthetic analogue of the natural pituitary hormone8-arginine vasopressin (ADH), an antidiuretic hormone affecting renal water conservation. It is chemically defined as follows:

Mol. Wt. 1183.34

Empirical Formula: C 46 H 64 N 14 O 12 S 2 •C 2 H 4 O 2 •3H 2 O

Desmopressin Structure
(click image for full-size original)

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

Desmopressin Acetate Injection USP 4 mcg/mL is provided as a sterile, aqueous solution for injection.

Each mL provides:

Desmopressin acetate 4 mcg

Sodium chloride 9 mg

Hydrochloric acid to adjust pH to 4

CLINICAL PHARMACOLOGY

Desmopressin Acetate Injection 4 mcg/mL contains as active substance, desmopressin acetate, a synthetic analogue of the natural hormone arginine vasopressin. One mL (4 mcg) of Desmopressin Acetate Injection(desmopressin acetate) solution has an antidiuretic activity of about 16 IU; 1 mcg of Desmopressin Acetate Injection is equivalent to 4 IU.

Desmopressin Acetate Injection 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 0.1 to 0.4 mcg/kg body weight, infused over a 10-minute period. Maximal dose response occurred at 0.3 to 0.4 mcg/kg. The response to Desmopressin Acetate Injection of factor VIII activity and plasminogen activator is dose-related, with maximal plasma levels of 300 to 400 percent of initial concentrations obtained after infusion of 0.4 mcg/kg body weight. The increase is rapid and evident within 30 minutes, reaching a maximum at a point ranging from 90 minutes to two hours. The factor VIII related antigen and ristocetin cofactor activity were also increased to a smaller degree, but still are dose-dependent.

1. The biphasic half-lives of Desmopressin Acetate Injection were 7.8 and 75.5 minutes for the fast and slow phases, respectively, compared with 2.5 and 14.5 minutes for lysine vasopressin, another form of the hormone. As a result, Desmopressin Acetate Injection 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 Injection 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. When administered by injection, Desmopressin Acetate Injection has an antidiuretic effect about ten times that of an equivalent dose administered intranasally.

4. The bioavailability of the subcutaneous route of administration was determined qualitatively using urine output data. The exact fraction of drug absorbed by that route of administration has not been quantitatively determined.

5. The percentage increase of factor VIII levels in patients with mild hemophilia A and von Willebrand’s disease was not significantly different from that observed in normal healthy individuals when treated with 0.3 mcg/kg of Desmopressin Acetate Injection infused over 10 minutes.

6. Plasminogen activator activity increases rapidly after Desmopressin Acetate Injection infusion, but there has been no clinically significant fibrinolysis in patients treated with Desmopressin Acetate Injection.

7. The effect of repeated Desmopressin Acetate Injection administration when doses were given every 12 to 24 hours has generally shown a gradual diminution of the factor VIII activity increase noted with a single dose. The initial response is reproducible in any particular patient if there are 2 or 3 days between administrations.

Human Pharmacokinetics: Desmopressin Acetate Injection is mainly excreted in the urine. A pharmacokinetic study conducted in healthy volunteers and patients with mild, moderate, and severe renal impairment (n=24, 6 subjects in each group) receiving single dose desmopressin acetate (2 mcg) injection demonstrated a difference in Desmopressin Acetate Injection terminal half-life. Terminal half-life significantly increased from 3 hours in normal healthy patients to 9 hours in patients with severe renal impairment. (See CONTRAINDICATIONS.)

INDICATIONS AND USAGE

Hemophilia A: Desmopressin Acetate Injection 4 mcg/mL is indicated for patients with hemophilia A with factor VIII coagulant activity levels greater than 5%.

Desmopressin Acetate Injection will often maintain hemostasis in patients with hemophilia A during surgical procedures and postoperatively when administered 30 minutes prior to scheduled procedure.

Desmopressin Acetate Injection will also stop bleeding in hemophilia A patients with episodes of spontaneous or trauma-induced injuries such as hemarthroses, intramuscular hematomas or mucosal bleeding.

Desmopressin Acetate Injection 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.

In certain clinical situations, it may be justified to try Desmopressin Acetate Injection in patients with factor VIII levels between 2% to 5%; however, these patients should be carefully monitored.

von Willebrands Disease (Type I): Desmopressin Acetate Injection 4 mcg/mL is indicated for patients with mild to moderate classic von Willebrands disease (Type I) with factor VIII levels greater than 5%. Desmopressin Acetate Injection will often maintain hemostasis in patients with mild to moderate von Willebrands disease during surgical procedures and postoperatively when administered 30 minutes prior to the scheduled procedure.

Desmopressin Acetate Injection will usually stop bleeding in mild to moderate von Willebrands patients with episodes of spontaneous or trauma-induced injuries such as hemarthroses, intramuscular hematomas or mucosal bleeding.

Those von Willebrands disease patients who are least likely to respond are those with severe homozygous von Willebrands disease with factor VIII coagulant activity and factor VIII von Willebrand factor antigen levels less than 1%. Other 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 during administration of Desmopressin Acetate Injection to ensure that adequate levels are being achieved.

Desmopressin Acetate Injection is not indicated for the treatment of severe classic von Willebrands disease (Type I) and when there is evidence of an abnormal molecular form of factor VIII antigen. (See WARNINGS.)

Diabetes Insipidus: Desmopressin Acetate Injection 4 mcg/mL is indicated as antidiuretic replacement therapy in the management of central (cranial) diabetes insipidus and for the management of the temporary polyuria and polydipsia following head trauma or surgery in the pituitary region. Desmopressin Acetate Injection is ineffective for the treatment of nephrogenic diabetes insipidus.

Desmopressin Acetate Injection is also available as an intranasal preparation. However, this means of delivery can be compromised by a variety of factors that can make nasal insufflation ineffective or inappropriate. These include poor intranasal absorption, nasal congestion and blockage, nasal discharge, atrophy of nasal mucosa, and severe atrophic rhinitis. Intranasal delivery may be inappropriate where there is an impaired level of consciousness. In addition, cranial surgical procedures, such as transsphenoidal hypophysectomy, create situations where an alternative route of administration is needed as in cases of nasal packing or recovery from surgery.

CONTRAINDICATIONS

Desmopressin Acetate Injection 4 mcg/mL is contraindicated in individuals with known hypersensitivity to desmopressin acetate or to any of the components of Desmopressin Acetate Injection 4 mcg/mL.

Desmopressin Acetate Injection is contraindicated in patients with moderate to severe renal impairment (defined as a creatinine clearance below 50 mL/min).

Desmopressin Acetate Injection is contraindicated in patients with hyponatremia or a history of hyponatremia.

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