Desmopressin

Therapeutic

Treatment of nocturia due to nocturnal polyuria (intranasal); indicated as antidiuretic replacement therapy in central cranial diabetes insipidus; indicated for patients with hemopilia A.

Structural features

SMILES

NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O

Sequence

XYFQNCPrG-NH2

Molar mass

1069.22 g/mol

Constitutional members:

9

Natural amino acids

7

D-Amino acids

1

N-terminus

deamino

C-terminus

NH2

Cyclic

yes

Members/cycle

6

Bond to form cycle

side chain-to-side chain (disulfide)

Lipidation

no

Glycosylation

no

Route of administration

NASAL, ORAL, SL, IV, IM, SC

Terminal half-life

Following an intranasal dose of 1.66 mcg of desmopressin, the median apparent terminal half-life was 2.8 hours. Terminal half-life significantly increased from 3 hours in normal healthy patients to 9 hours in patients with severe renal impairment. The oral terminal half life of desmopressin ranges from 2 to 3.11 hours.

Protein binding

17.3 ± 1.5%

Absorption and Bioavailability

The bioavailability of 1.5 mg/mL desmopressin administered by the intranasal route was between 3.3 and 4.1%. The absolute bioavailability of orally administered desmopressin varies between 0.08% and 0.16% where the mean maximum plasma concentration is reached within 2 hours.

References