Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C46H64N14O12S2 |
Molecular Weight | 1069.217 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 7 / 7 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC3=CC=C(O)C=C3)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N4CCC[C@H]4C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O
InChI
InChIKey=NFLWUMRGJYTJIN-PNIOQBSNSA-N
InChI=1S/C46H64N14O12S2/c47-35(62)15-14-29-40(67)58-32(22-36(48)63)43(70)59-33(45(72)60-18-5-9-34(60)44(71)56-28(8-4-17-52-46(50)51)39(66)53-23-37(49)64)24-74-73-19-16-38(65)54-30(21-26-10-12-27(61)13-11-26)41(68)57-31(42(69)55-29)20-25-6-2-1-3-7-25/h1-3,6-7,10-13,28-34,61H,4-5,8-9,14-24H2,(H2,47,62)(H2,48,63)(H2,49,64)(H,53,66)(H,54,65)(H,55,69)(H,56,71)(H,57,68)(H,58,67)(H,59,70)(H4,50,51,52)/t28-,29+,30+,31+,32+,33+,34+/m1/s1
Molecular Formula | C46H64N14O12S2 |
Molecular Weight | 1069.217 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 7 / 7 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Desmopressin is a chemical that is similar to Antidiuretic Hormone (ADH), which is found naturally in the body and is produced by the hypothalamus and stored, in the posterior pituitary gland. The main function of ADH is to regulate extracellular fluid volume in the body. ADH secretion is stimulated by angiotensin II, linking it to the renin-angiotensin-aldosterone system (RAAS). ADH stimulates water reabsorption in the kidneys by causing the insertion of aquaporin-2 channels on the apical surface of cells of the distal convoluted tubule and collecting tubules. Desmopressin also causes vasoconstriction through its action on vascular smooth muscle cells of the collecting tubules. It increases urine concentration and decreases urine production. Acetate salt of desmopressin is sold under brand name DDAVP with different formulations: DDAVP Nasal Spray is indicated as antidiuretic replacement therapy in the management of central cranial diabetes insipidus and for management of the temporary polyuria and polydipsia following head trauma or surgery in the pituitary region. It is ineffective for the treatment of nephrogenic diabetes insipidus. DDAVP Injection is indicated for patients with hemophilia A with factor VIII coagulant activity levels greater than 5% and is indicated for patients with mild to moderate classic von Willebrand’s disease (Type I) with factor VIII levels greater than 5%. It was suggested that desmopressin-induced relaxation was mediated by a receptor subtype sharing both V1A and V2 pharmacological profiles.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2363078 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | DDAVP (NEEDS NO REFRIGERATION) Approved UseCentral Diabetes Insipidus: Desmopressin acetate tablets are indicated as antidiuretic replacement therapy in the management of central diabetes insipidus and for the management of the temporary polyuria and polydipsia following head trauma or surgery in the pituitary region. Desmopressin acetate tablets are ineffective for the treatment of nephrogenic diabetes insipidus. Patients were selected for therapy based on the diagnosis by means of the water deprivation test, the hypertonic saline infusion test, and/or response to antidiuretic hormone. Continued response to desmopressin acetate can be monitored by measuring urine volume and osmolality. Primary Nocturnal Enuresis: Desmopressin acetate tablets are indicated for the management of primary nocturnal enuresis. Desmopressin acetate tablets may be used alone or as an adjunct to behavioral conditioning or other non-pharmacologic intervention. Launch Date1978 |
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Primary | DDAVPP Approved UseHemophilia A: DDAVP Injection 4 mcg/mL is indicated for patients with hemophilia A with factor VIII coagulant activity levels greater than 5%. DDAVP will often maintain hemostasis in patients with hemophilia A during surgical procedures and postoperatively when administered 30 minutes prior to scheduled procedure. DDAVP will also stop bleeding in hemophilia A patients with episodes of spontaneous or traumainduced injuries such as hemarthroses, intramuscular hematomas or mucosal bleeding. 2 DDAVP 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 DDAVP in patients with factor VIII levels between 2% to 5%; however, these patients should be carefully monitored. von Willebrand’s Disease (Type I): DDAVP Injection 4 mcg/mL is indicated for patients with mild to moderate classic von Willebrand’s disease (Type I) with factor VIII levels greater than 5%. DDAVP will often maintain hemostasis in patients with mild to moderate von Willebrand’s disease during surgical procedures and postoperatively when administered 30 minutes prior to the scheduled procedure. DDAVP will usually stop bleeding in mild to moderate von Willebrand’s patients with episodes of spontaneous or trauma-induced injuries such as hemarthroses, intramuscular hematomas or mucosal bleeding. Those von Willebrand’s disease patients who are least likely to respond are those with severe homozygous von Willebrand’s 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 DDAVP to ensure that adequate levels are being achieved. DDAVP 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 VIII antigen. Launch Date1984 |
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Primary | DDAVPP Approved UseHemophilia A: DDAVP Injection 4 mcg/mL is indicated for patients with hemophilia A with factor VIII coagulant activity levels greater than 5%. DDAVP will often maintain hemostasis in patients with hemophilia A during surgical procedures and postoperatively when administered 30 minutes prior to scheduled procedure. DDAVP will also stop bleeding in hemophilia A patients with episodes of spontaneous or traumainduced injuries such as hemarthroses, intramuscular hematomas or mucosal bleeding. 2 DDAVP 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 DDAVP in patients with factor VIII levels between 2% to 5%; however, these patients should be carefully monitored. von Willebrand’s Disease (Type I): DDAVP Injection 4 mcg/mL is indicated for patients with mild to moderate classic von Willebrand’s disease (Type I) with factor VIII levels greater than 5%. DDAVP will often maintain hemostasis in patients with mild to moderate von Willebrand’s disease during surgical procedures and postoperatively when administered 30 minutes prior to the scheduled procedure. DDAVP will usually stop bleeding in mild to moderate von Willebrand’s patients with episodes of spontaneous or trauma-induced injuries such as hemarthroses, intramuscular hematomas or mucosal bleeding. Those von Willebrand’s disease patients who are least likely to respond are those with severe homozygous von Willebrand’s 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 DDAVP to ensure that adequate levels are being achieved. DDAVP 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 VIII antigen. Launch Date1984 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
98 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3141199/ |
300 μg single, nasal dose: 300 μg route of administration: Nasal experiment type: SINGLE co-administered: |
DESMOPRESSIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
483 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3141199/ |
300 μg single, nasal dose: 300 μg route of administration: Nasal experiment type: SINGLE co-administered: |
DESMOPRESSIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.62 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3141199/ |
300 μg single, nasal dose: 300 μg route of administration: Nasal experiment type: SINGLE co-administered: |
DESMOPRESSIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
6 mg 1 times / 3 days single, oral Studied dose Dose: 6 mg, 1 times / 3 days Route: oral Route: single Dose: 6 mg, 1 times / 3 days Sources: |
unhealthy, 75 years n = 1 Health Status: unhealthy Condition: nocturia Age Group: 75 years Sex: M Population Size: 1 Sources: |
Other AEs: Agitation, Vomiting... |
25 ug 1 times / day steady, sublingual Dose: 25 ug, 1 times / day Route: sublingual Route: steady Dose: 25 ug, 1 times / day Sources: |
unhealthy, adult n = 135 Health Status: unhealthy Condition: Nocturia Age Group: adult Sex: F Population Size: 135 Sources: |
Other AEs: Headache... Other AEs: Headache (below serious, 7 patients) Sources: |
240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Other AEs: Tonsillitis, Upper respiratory tract infection... Other AEs: Tonsillitis (below serious, 1 patient) Sources: Upper respiratory tract infection (below serious, 1 patient) Headache (below serious, 1 patient) Blepharitis (below serious, 1 patient) Tonsillar hypertrophy (below serious, 1 patient) Abdominal pain (below serious, 1 patient) Enterocolitis (below serious, 1 patient) Stomatitis (below serious, 2 patients) Dermatitis atopic (below serious, 1 patient) Skin papilloma (below serious, 1 patient) Asthenia (below serious, 2 patients) Malaise (below serious, 1 patient) Arthropod bite (below serious, 1 patient) |
0.5 ug/kg 2 times / day multiple, intravenous MTD Dose: 0.5 ug/kg, 2 times / day Route: intravenous Route: multiple Dose: 0.5 ug/kg, 2 times / day Sources: |
unhealthy, median age 55.5 years n = 6 Health Status: unhealthy Condition: bleeding Age Group: median age 55.5 years Sex: M+F Population Size: 6 Sources: |
DLT: Hyponatremia... |
1 ug/kg 1 times / day multiple, intravenous Studied dose Dose: 1 ug/kg, 1 times / day Route: intravenous Route: multiple Dose: 1 ug/kg, 1 times / day Sources: |
unhealthy, median age 55.5 years n = 6 Health Status: unhealthy Condition: bleeding Age Group: median age 55.5 years Sex: M+F Population Size: 6 Sources: |
DLT: Hyponatremia... Dose limiting toxicities: Hyponatremia (grade 3, 33.3%) Sources: |
1 ug/kg 2 times / day multiple, intravenous Studied dose Dose: 1 ug/kg, 2 times / day Route: intravenous Route: multiple Dose: 1 ug/kg, 2 times / day Sources: |
unhealthy, median age 55.5 years n = 2 Health Status: unhealthy Condition: bleeding Age Group: median age 55.5 years Sex: M+F Population Size: 2 Sources: |
DLT: Hyponatremia, Hypertonia... Dose limiting toxicities: Hyponatremia (grade 3, 100%) Sources: Hypertonia (grade 3, 50%) |
0.75 ug 1 times / day multiple, intranasal Recommended Dose: 0.75 ug, 1 times / day Route: intranasal Route: multiple Dose: 0.75 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 454 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 454 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Disc. AE: Nasal discomfort, Hyponatremia... AEs leading to discontinuation/dose reduction: Nasal discomfort (0.2%) Sources: Page: nda/2017/201656Orig1s000MedR.pdfHyponatremia (0.2%) Dizziness (0.4%) Blood sodium decreased (0.4%) Dysuria (0.4%) Nasal congestion (0.2%) |
1.5 ug 1 times / day multiple, intranasal Recommended Dose: 1.5 ug, 1 times / day Route: intranasal Route: multiple Dose: 1.5 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 448 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 448 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Disc. AE: Nasal discomfort, Hyponatremia... AEs leading to discontinuation/dose reduction: Nasal discomfort (0.7%) Sources: Page: nda/2017/201656Orig1s000MedR.pdfHyponatremia (0.7%) Dizziness (0.2%) Blood sodium decreased (0.2%) Dysuria (0.2%) Nasal congestion (0.4%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Agitation | 6 mg 1 times / 3 days single, oral Studied dose Dose: 6 mg, 1 times / 3 days Route: oral Route: single Dose: 6 mg, 1 times / 3 days Sources: |
unhealthy, 75 years n = 1 Health Status: unhealthy Condition: nocturia Age Group: 75 years Sex: M Population Size: 1 Sources: |
|
Vomiting | 6 mg 1 times / 3 days single, oral Studied dose Dose: 6 mg, 1 times / 3 days Route: oral Route: single Dose: 6 mg, 1 times / 3 days Sources: |
unhealthy, 75 years n = 1 Health Status: unhealthy Condition: nocturia Age Group: 75 years Sex: M Population Size: 1 Sources: |
|
Headache | below serious, 7 patients | 25 ug 1 times / day steady, sublingual Dose: 25 ug, 1 times / day Route: sublingual Route: steady Dose: 25 ug, 1 times / day Sources: |
unhealthy, adult n = 135 Health Status: unhealthy Condition: Nocturia Age Group: adult Sex: F Population Size: 135 Sources: |
Abdominal pain | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Arthropod bite | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Blepharitis | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Dermatitis atopic | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Enterocolitis | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Headache | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Malaise | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Skin papilloma | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Tonsillar hypertrophy | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Tonsillitis | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Upper respiratory tract infection | below serious, 1 patient | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Asthenia | below serious, 2 patients | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Stomatitis | below serious, 2 patients | 240 ug 1 times / day steady, sublingual (max) Dose: 240 ug, 1 times / day Route: sublingual Route: steady Dose: 240 ug, 1 times / day Sources: |
unhealthy, children|adolescents n = 45 Health Status: unhealthy Condition: Nocturnal enuresis Age Group: children|adolescents Population Size: 45 Sources: |
Hyponatremia | 16.7% DLT |
0.5 ug/kg 2 times / day multiple, intravenous MTD Dose: 0.5 ug/kg, 2 times / day Route: intravenous Route: multiple Dose: 0.5 ug/kg, 2 times / day Sources: |
unhealthy, median age 55.5 years n = 6 Health Status: unhealthy Condition: bleeding Age Group: median age 55.5 years Sex: M+F Population Size: 6 Sources: |
Hyponatremia | grade 3, 33.3% DLT |
1 ug/kg 1 times / day multiple, intravenous Studied dose Dose: 1 ug/kg, 1 times / day Route: intravenous Route: multiple Dose: 1 ug/kg, 1 times / day Sources: |
unhealthy, median age 55.5 years n = 6 Health Status: unhealthy Condition: bleeding Age Group: median age 55.5 years Sex: M+F Population Size: 6 Sources: |
Hyponatremia | grade 3, 100% DLT |
1 ug/kg 2 times / day multiple, intravenous Studied dose Dose: 1 ug/kg, 2 times / day Route: intravenous Route: multiple Dose: 1 ug/kg, 2 times / day Sources: |
unhealthy, median age 55.5 years n = 2 Health Status: unhealthy Condition: bleeding Age Group: median age 55.5 years Sex: M+F Population Size: 2 Sources: |
Hypertonia | grade 3, 50% DLT |
1 ug/kg 2 times / day multiple, intravenous Studied dose Dose: 1 ug/kg, 2 times / day Route: intravenous Route: multiple Dose: 1 ug/kg, 2 times / day Sources: |
unhealthy, median age 55.5 years n = 2 Health Status: unhealthy Condition: bleeding Age Group: median age 55.5 years Sex: M+F Population Size: 2 Sources: |
Hyponatremia | 0.2% Disc. AE |
0.75 ug 1 times / day multiple, intranasal Recommended Dose: 0.75 ug, 1 times / day Route: intranasal Route: multiple Dose: 0.75 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 454 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 454 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Nasal congestion | 0.2% Disc. AE |
0.75 ug 1 times / day multiple, intranasal Recommended Dose: 0.75 ug, 1 times / day Route: intranasal Route: multiple Dose: 0.75 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 454 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 454 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Nasal discomfort | 0.2% Disc. AE |
0.75 ug 1 times / day multiple, intranasal Recommended Dose: 0.75 ug, 1 times / day Route: intranasal Route: multiple Dose: 0.75 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 454 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 454 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Blood sodium decreased | 0.4% Disc. AE |
0.75 ug 1 times / day multiple, intranasal Recommended Dose: 0.75 ug, 1 times / day Route: intranasal Route: multiple Dose: 0.75 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 454 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 454 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Dizziness | 0.4% Disc. AE |
0.75 ug 1 times / day multiple, intranasal Recommended Dose: 0.75 ug, 1 times / day Route: intranasal Route: multiple Dose: 0.75 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 454 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 454 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Dysuria | 0.4% Disc. AE |
0.75 ug 1 times / day multiple, intranasal Recommended Dose: 0.75 ug, 1 times / day Route: intranasal Route: multiple Dose: 0.75 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 454 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 454 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Blood sodium decreased | 0.2% Disc. AE |
1.5 ug 1 times / day multiple, intranasal Recommended Dose: 1.5 ug, 1 times / day Route: intranasal Route: multiple Dose: 1.5 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 448 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 448 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Dizziness | 0.2% Disc. AE |
1.5 ug 1 times / day multiple, intranasal Recommended Dose: 1.5 ug, 1 times / day Route: intranasal Route: multiple Dose: 1.5 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 448 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 448 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Dysuria | 0.2% Disc. AE |
1.5 ug 1 times / day multiple, intranasal Recommended Dose: 1.5 ug, 1 times / day Route: intranasal Route: multiple Dose: 1.5 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 448 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 448 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Nasal congestion | 0.4% Disc. AE |
1.5 ug 1 times / day multiple, intranasal Recommended Dose: 1.5 ug, 1 times / day Route: intranasal Route: multiple Dose: 1.5 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 448 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 448 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Hyponatremia | 0.7% Disc. AE |
1.5 ug 1 times / day multiple, intranasal Recommended Dose: 1.5 ug, 1 times / day Route: intranasal Route: multiple Dose: 1.5 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 448 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 448 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Nasal discomfort | 0.7% Disc. AE |
1.5 ug 1 times / day multiple, intranasal Recommended Dose: 1.5 ug, 1 times / day Route: intranasal Route: multiple Dose: 1.5 ug, 1 times / day Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
unhealthy, median age 65.5 years n = 448 Health Status: unhealthy Condition: nocturia Age Group: median age 65.5 years Sex: M+F Population Size: 448 Sources: Page: nda/2017/201656Orig1s000MedR.pdf |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.ferring.ca/media/1152/english-nocdurna-pm-control-no-168240-3sep2014.pdf#page=13 Page: 13.0 |
unlikely |
PubMed
Title | Date | PubMed |
---|---|---|
Oxytocin- and vasopressin-induced growth of human small-cell lung cancer is mediated by the mitogen-activated protein kinase pathway. | 2004 Dec |
|
Further neuroendocrine evidence of enhanced vasopressin V3 receptor responses in melancholic depression. | 2004 Jan |
|
Investigation of mechanism of desmopressin binding in vasopressin V2 receptor versus vasopressin V1a and oxytocin receptors: molecular dynamics simulation of the agonist-bound state in the membrane-aqueous system. | 2006 Apr 5 |
|
Characterization of a novel and selective V1B receptor antagonist. | 2008 |
Patents
Sample Use Guides
Hemophilia A and von Willebrand’s Disease (Type I): DDAVP Injection 4 mcg/mL is administered as an intravenous infusion at a dose of 0.3 mcg DDAVP/kg body weight diluted in sterile physiological saline and infused slowly over 15 to 30 minutes. In adults and children weighing more than 10 kg, 50 mL of diluent is recommended; in children weighing 10 kg or less, 10 mL of diluent is recommended. Blood pressure and pulse should be monitored during infusion. If DDAVP Injection 4 mcg/mL is used preoperatively, it should be administered 30 minutes prior to the scheduled procedure.
Diabetes Insipidus: This formulation is administered subcutaneously or by direct intravenous injection. DDAVP Injection 4 mcg/mL dosage must be determined for each patient and adjusted according to the pattern of response. Response should be estimated by two parameters: adequate duration of sleep and adequate, not excessive, water turnover. The usual dosage range in adults is 0.5 mL (2.0 mcg) to 1 mL (4.0 mcg) daily, administered intravenously or subcutaneously, usually in two divided doses. The morning and evening doses should be separately adjusted for an adequate diurnal rhythm of water turnover. For patients who have been controlled on intranasal DDAVP and who must be switched to the injection form, either because of poor intranasal absorption or because of the need for surgery, the comparable antidiuretic dose of the injection is about one-tenth the intranasal dose.
Central Diabetes Insipidus: The dosage of DDAVP Tablets must be determined for each individual patient and adjusted according to the diurnal pattern of response. Response should be estimated by two parameters: adequate duration of sleep and adequate, not excessive, water turnover. Patients previously on intranasal DDAVP therapy should begin tablet therapy twelve hours after the last intranasal dose. During the initial dose titration period, patients should be 6 observed closely and appropriate safety parameters measured to assure adequate response.
Central Cranial Diabetes Insipidus: DDAVP Nasal Spray dosage must be determined for each individual patient and adjusted according to the diurnal pattern of response. Response should be estimated by two parameters: adequate duration of sleep and adequate, not excessive, water turnover. Patients with nasal congestion and blockage have often responded well to intranasal DDAVP. The usual dosage range in adults is 0.1 to 0.4 mL daily, either as a single dose or divided into two or three doses. Most adults require 0.2 mL daily in two divided doses. The morning and evening doses should be separately adjusted for an adequate diurnal rhythm of water turnover. For children aged 3 months to 12 years, the usual dosage range is 0.05 to 0.3 mL daily, either as a single dose or divided into two doses. About 1/4 to 1/3 of patients can be controlled by a single daily dose of DDAVP administered intranasally.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23534885
It was investigated the influence of desmopressin on platelet endothelial interactions in vitro. (DDAVP) improves recruitment of activated platelets to collagen but simultaneously increases platelet endothelial interactions in vitro. DDAVP increases von Willebrand factor (VWF) on endothelial cells (ECs) and in plasma. VWF could facilitate platelet deposition on subendothelial collagen. VWF also facilitates platelet/EC interactions. Therefore DDAVP could precipitate thromboembolic events. Resting or TRAP-activated platelets and EC were treated individually or simultaneously with 0.4 ng/ml DDAVP. Fluorophor-labeled platelets (10(6)/ml) were resuspended in reconstituted blood and superfused across EC and collagen in an in vitro flow chamber model at arterial shear (320 s(-1)). Adhesion of platelets to the respective surface was recorded fluorescence microscopically and platelet covered area was assessed. DDAVP pretreatment of platelets did not affect adhesiveness of resting or TRAP-activated platelets for collagen or EC. DDAVP has no direct effect on platelets. Blood samples from DDAVP-treated patients do not exhibit significantly augmented platelet deposition on collagen ex vivo.
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