Peringatan Keamanan

Intravenous TDLo in humans is reported to be 0.3 µg/kg/10M MSDS. Desmopressin is associated with hyponatremia in case of overdose, which may require temporary or permanent discontinuation of the therapy depending on severity. The effects of hyponatremia include seizure, altered mental status (confusion, drowsiness or continuing headache), cardiac arrhythmias and worsening edema. Other signs of overdose may include oliguria and rapid weight gain due to fluid retention FDA Label. In case of overdose, reduce the dose or frequency of drug administration, or discontinue use if appropriate. Assessment of serum sodium and initiation of appropriate medical treatment is recommended.

Desmopressin

DB00035

small molecule approved

Deskripsi

Desmopressin (dDAVP), a synthetic analogue of 8-arginine vasopressin (ADH), is an antidiuretic peptide drug modified by deamination of 1-cysteine and substitution of 8-L-arginine by 8-D-arginine. ADH is an endogenous pituitary hormone that has a crucial role in the control of the water content in the body. Upon release from the stimulation of increased plasma osmolarity or decreased circulating blood volume, ADH mainly acts on the cells of the distal part of the nephron and the collecting tubules in the kidney T28. The hormone interacts with V1, V2 or V3 receptors with differing signal cascade systems.

Desmopressin displays enhanced antidiuretic potency, fewer pressor effects due to V2-selective actions, and a prolonged half-life and duration of action compared to endogenous ADH A31661. It has been employed clinically since 1972 and is available in various formulations including intranasal solution, intravenous solution, oral tablet and oral lyophilisate A31662. Desmopressin is indicated for the treatment of polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. It was also newly approved for the treatment of mild classical hemophilia and von Willebrand's disease for minor surgeries. The active ingredient in most formulations is desmopressin acetate. Nocdurna, or desmopressin acetate, was approved by the FDA on June 21st, 2018 for the treatment of nocturia due to nocturnal polyuria in adults. It is available as a sublingual tablet.

Struktur Molekul 2D

Berat 1069.22
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following an intranasal dose of 1.66 mcg of desmopressin, the median apparent terminal half-life was 2.8 hours [FDA Label]. Terminal half-life significantly increased from 3 hours in normal healthy patients to 9 hours in patients with severe renal impairment [FDA Label]. The oral terminal half life of desmopressin ranges from 2 to 3.11 hours [L1184].
Volume Distribusi The distribution volume of orally administered desmopressin is 0.2 – 0.32 l/kg [L1184]. It is not reported to cross the blood-brain barrier.
Klirens (Clearance) -

Absorpsi

Following nasal spray administration of 0.83 mcg and 1.66 mcg, median time to peak plasma concentrations (Tmax) was 0.25 and 0.75 hour, respectively FDA Label. The peak plasma concentration was approximately 4.00 (± 3.85) pg/mL and 9.11 (± 6.90) pg/mL, respectively FDA Label. The bioavailability of 1.5 mg/mL desmopressin administered by the intranasal route was between 3.3 and 4.1% L1183. 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 L1184.

Metabolisme

In vitro, in human liver microsome preparations, it has been shown that no significant amount of desmopressin is metabolised in the liver and thus human liver metabolism in vivo is not likely to occur L1184.

Rute Eliminasi

Desmopressin is mainly excreted in the urine. About 65% of the amount of desmopressin absorbed after oral administration could be recovered in the urine within 24 hours L1184.

Interaksi Obat

1132 Data
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Desmopressin.
Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Desmopressin.
Demeclocycline The therapeutic efficacy of Desmopressin can be decreased when used in combination with Demeclocycline.
Lamotrigine The risk or severity of adverse effects can be increased when Lamotrigine is combined with Desmopressin.
Lithium citrate The therapeutic efficacy of Desmopressin can be decreased when used in combination with Lithium citrate.
Lithium carbonate The therapeutic efficacy of Desmopressin can be decreased when used in combination with Lithium carbonate.
Lithium hydroxide The therapeutic efficacy of Desmopressin can be decreased when used in combination with Lithium hydroxide.
Tolvaptan The therapeutic efficacy of Desmopressin can be decreased when used in combination with Tolvaptan.
Fluvoxamine The risk or severity of hyponatremia can be increased when Fluvoxamine is combined with Desmopressin.
Citalopram The risk or severity of hyponatremia can be increased when Citalopram is combined with Desmopressin.
Fluoxetine The risk or severity of hyponatremia can be increased when Fluoxetine is combined with Desmopressin.
Duloxetine The risk or severity of hyponatremia can be increased when Duloxetine is combined with Desmopressin.
Trazodone The risk or severity of hyponatremia can be increased when Trazodone is combined with Desmopressin.
Paroxetine The risk or severity of hyponatremia can be increased when Paroxetine is combined with Desmopressin.
Sertraline The risk or severity of hyponatremia can be increased when Sertraline is combined with Desmopressin.
Sibutramine The risk or severity of hyponatremia can be increased when Sibutramine is combined with Desmopressin.
Nefazodone The risk or severity of hyponatremia can be increased when Nefazodone is combined with Desmopressin.
Escitalopram The risk or severity of hyponatremia can be increased when Escitalopram is combined with Desmopressin.
Zimelidine The risk or severity of hyponatremia can be increased when Zimelidine is combined with Desmopressin.
Dapoxetine The risk or severity of hyponatremia can be increased when Dapoxetine is combined with Desmopressin.
Milnacipran The risk or severity of hyponatremia can be increased when Milnacipran is combined with Desmopressin.
Desvenlafaxine The risk or severity of hyponatremia can be increased when Desvenlafaxine is combined with Desmopressin.
Seproxetine The risk or severity of hyponatremia can be increased when Seproxetine is combined with Desmopressin.
Levomilnacipran Desmopressin may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Indalpine The risk or severity of hyponatremia can be increased when Indalpine is combined with Desmopressin.
Ritanserin The risk or severity of hyponatremia can be increased when Ritanserin is combined with Desmopressin.
Alaproclate The risk or severity of hyponatremia can be increased when Alaproclate is combined with Desmopressin.
Valsartan Desmopressin may decrease the antihypertensive activities of Valsartan.
Ramipril Desmopressin may decrease the antihypertensive activities of Ramipril.
Esmolol Desmopressin may decrease the antihypertensive activities of Esmolol.
Betaxolol Desmopressin may decrease the antihypertensive activities of Betaxolol.
Remikiren Desmopressin may decrease the antihypertensive activities of Remikiren.
Guanadrel Desmopressin may decrease the antihypertensive activities of Guanadrel.
Olmesartan Desmopressin may decrease the antihypertensive activities of Olmesartan.
Atenolol Desmopressin may decrease the antihypertensive activities of Atenolol.
Diltiazem Desmopressin may decrease the antihypertensive activities of Diltiazem.
Minoxidil Desmopressin may decrease the antihypertensive activities of Minoxidil.
Treprostinil Desmopressin may decrease the antihypertensive activities of Treprostinil.
Amlodipine Desmopressin may decrease the antihypertensive activities of Amlodipine.
Nimodipine Desmopressin may decrease the antihypertensive activities of Nimodipine.
Prazosin Desmopressin may decrease the antihypertensive activities of Prazosin.
Trandolapril Desmopressin may decrease the antihypertensive activities of Trandolapril.
Lercanidipine Desmopressin may decrease the antihypertensive activities of Lercanidipine.
Benazepril Desmopressin may decrease the antihypertensive activities of Benazepril.
Bosentan Desmopressin may decrease the antihypertensive activities of Bosentan.
Enalapril Desmopressin may decrease the antihypertensive activities of Enalapril.
Doxazosin Desmopressin may decrease the antihypertensive activities of Doxazosin.
Candoxatril Desmopressin may decrease the antihypertensive activities of Candoxatril.
Nicardipine Desmopressin may decrease the antihypertensive activities of Nicardipine.
Losartan Desmopressin may decrease the antihypertensive activities of Losartan.
Moexipril Desmopressin may decrease the antihypertensive activities of Moexipril.
Nitroglycerin Desmopressin may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Desmopressin may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Desmopressin may decrease the antihypertensive activities of Cryptenamine.
Candesartan cilexetil Desmopressin may decrease the antihypertensive activities of Candesartan cilexetil.
Alprenolol Desmopressin may decrease the antihypertensive activities of Alprenolol.
Eprosartan Desmopressin may decrease the antihypertensive activities of Eprosartan.
Quinapril Desmopressin may decrease the antihypertensive activities of Quinapril.
Telmisartan Desmopressin may decrease the antihypertensive activities of Telmisartan.
Felodipine Desmopressin may decrease the antihypertensive activities of Felodipine.
Irbesartan Desmopressin may decrease the antihypertensive activities of Irbesartan.
Nitrendipine Desmopressin may decrease the antihypertensive activities of Nitrendipine.
Deserpidine Desmopressin may decrease the antihypertensive activities of Deserpidine.
Pentolinium Desmopressin may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Desmopressin may decrease the antihypertensive activities of Trimethaphan.
Carvedilol Desmopressin may decrease the antihypertensive activities of Carvedilol.
Bretylium Desmopressin may decrease the antihypertensive activities of Bretylium.
Terazosin Desmopressin may decrease the antihypertensive activities of Terazosin.
Acebutolol Desmopressin may decrease the antihypertensive activities of Acebutolol.
Captopril Desmopressin may decrease the antihypertensive activities of Captopril.
Bepridil Desmopressin may decrease the antihypertensive activities of Bepridil.
Bevantolol Desmopressin may decrease the antihypertensive activities of Bevantolol.
Practolol Desmopressin may decrease the antihypertensive activities of Practolol.
Cilazapril Desmopressin may decrease the antihypertensive activities of Cilazapril.
Saprisartan Desmopressin may decrease the antihypertensive activities of Saprisartan.
Spirapril Desmopressin may decrease the antihypertensive activities of Spirapril.
Mibefradil Desmopressin may decrease the antihypertensive activities of Mibefradil.
Oxprenolol Desmopressin may decrease the antihypertensive activities of Oxprenolol.
Dexpropranolol Desmopressin may decrease the antihypertensive activities of Dexpropranolol.
Debrisoquine Desmopressin may decrease the antihypertensive activities of Debrisoquine.
Celiprolol Desmopressin may decrease the antihypertensive activities of Celiprolol.
Nebivolol Desmopressin may decrease the antihypertensive activities of Nebivolol.
Sitaxentan Desmopressin may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Desmopressin may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Desmopressin may decrease the antihypertensive activities of Diethylnorspermine.
Nilvadipine Desmopressin may decrease the antihypertensive activities of Nilvadipine.
Pinacidil Desmopressin may decrease the antihypertensive activities of Pinacidil.
Bupranolol Desmopressin may decrease the antihypertensive activities of Bupranolol.
Temocapril Desmopressin may decrease the antihypertensive activities of Temocapril.
Riociguat Desmopressin may decrease the antihypertensive activities of Riociguat.
Indenolol Desmopressin may decrease the antihypertensive activities of Indenolol.
Hexamethonium Desmopressin may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Desmopressin may decrease the antihypertensive activities of Aliskiren.
Trimazosin Desmopressin may decrease the antihypertensive activities of Trimazosin.
Lacidipine Desmopressin may decrease the antihypertensive activities of Lacidipine.
Manidipine Desmopressin may decrease the antihypertensive activities of Manidipine.
Niguldipine Desmopressin may decrease the antihypertensive activities of Niguldipine.
Rauwolfia serpentina root Desmopressin may decrease the antihypertensive activities of Rauwolfia serpentina root.
Selexipag Desmopressin may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Desmopressin may decrease the antihypertensive activities of Angiotensin 1-7.

Target Protein

Oxytocin receptor OXTR
Vasopressin V2 receptor AVPR2
Vasopressin V1a receptor AVPR1A
Vasopressin V1b receptor AVPR1B

Referensi & Sumber

Synthesis reference: Krister Larsson, Thomas Mellbrand, Birgitta Mornstam, Jan Roschester, Jan-Ake Skoldback, "High purity desmopressin produced in large single batches." U.S. Patent US5674850, issued November, 1991.
Artikel (PubMed)
  • PMID: 11380629
    Leissinger C, Becton D, Cornell C Jr, Cox Gill J: High-dose DDAVP intranasal spray (Stimate) for the prevention and treatment of bleeding in patients with mild haemophilia A, mild or moderate type 1 von Willebrand disease and symptomatic carriers of haemophilia A. Haemophilia. 2001 May;7(3):258-66.
  • PMID: 3893256
    Richardson DW, Robinson AG: Desmopressin. Ann Intern Med. 1985 Aug;103(2):228-39.
  • PMID: 18690973
    Vande Walle J, Stockner M, Raes A, Norgaard JP: Desmopressin 30 years in clinical use: a safety review. Curr Drug Saf. 2007 Sep;2(3):232-8.
  • PMID: 15373927
    Agerso H, Seiding Larsen L, Riis A, Lovgren U, Karlsson MO, Senderovitz T: Pharmacokinetics and renal excretion of desmopressin after intravenous administration to healthy subjects and renally impaired patients. Br J Clin Pharmacol. 2004 Oct;58(4):352-8. doi: 10.1111/j.1365-2125.2004.02175.x.
  • PMID: 8222299
    Lundin S, Broeders A, Melin P: Pharmacokinetic properties of the tocolytic agent Mpa1, D-Tyr(Et)2, Thr4, Orn8-oxytocin (antocin) in healthy volunteers. Clin Endocrinol (Oxf). 1993 Sep;39(3):369-74.
Textbook
  • ISBN: 978-0-7020-3471-8
    32. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 399-400). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 145 • International brands: 2
Produk
  • Apo-desmopressin
    Tablet • 0.1 mg • Oral • Canada • Generic • Approved
  • Apo-desmopressin
    Tablet • 0.2 mg • Oral • Canada • Generic • Approved
  • Bipazen
    Solution • 4 mcg / mL • Intramuscular; Intravenous; Subcutaneous • Canada • Approved
  • Ddavp
    Solution • 4 ug/1mL • Intravenous • US • Approved
  • Ddavp
    Tablet • 0.1 mg/1 • Oral • US • Approved
  • Ddavp
    Tablet • 0.2 mg/1 • Oral • US • Approved
  • Ddavp
    Injection • 4 ug/1mL • Intravenous • US • Approved
  • Ddavp
    Injection • 4 ug/1mL • Intravenous • US • Approved
Menampilkan 8 dari 145 produk.
International Brands
  • Adiuretin — Ferring
  • DesmoMelt — Ferring

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