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Desmopressin 的理想化结构描述
P 050Desmopressin

由序列构建的理想化构象；并非实验结构或预测结构。

Desmopressin 化学结构（2D） 的理想化结构描述
P 050 · 2D化学结构（2D）

来自 PubChem SMILES 的 2D 描述

P 050已验证 2026-08-06
批准的药物

Desmopressin

别名：DDAVP · 1-deamino-8-D-arginine vasopressin · Minirin · Nocdurna · Stimate

Synthetic V2-selective vasopressin analogue approved in multiple named jurisdictions for product-specific indications including central diabetes insipidus, primary nocturnal enuresis, haemophilia A/von Willebrand disease, and nocturia; warnings vary by formulation and jurisdiction.

神经精神科

证据内容以英文维护。

Desmopressin 的理想化结构描述

由序列构建的理想化构象；并非实验结构或预测结构。

速览

ENTRY TYPE
approved drug
IDENTITY
Sequence verified

No structure asset recorded

TOP EVIDENCE
Grade A — Central diabetes insipidus
MAJOR STATUS
Jurisdiction-specific — see status table
SPORT
Prohibited — as of 2026-08-06
VERIFIED
2026-08-06

Bottom line

Desmopressin (DDAVP) is a synthetic analogue of vasopressin with two key modifications — deamination at position 1 and substitution of L-Arg with D-Arg at position 8 — conferring V2-receptor selectivity and prolonged . It is approved in multiple named jurisdictions, with product-specific indications for central diabetes insipidus, primary nocturnal enuresis, mild haemophilia A/von Willebrand disease (factor VIII release), and nocturia (by sublingual formulation). The injectable formulation carries a boxed warning for severe hyponatraemia and seizure.

Identity and composition

FieldVerified information
Preferred nameDesmopressin
Key aliasesDDAVP, 1-deamino-8-D-arginine vasopressin, Minirin, Nocdurna, Stimate
Molecular/sequence identityMpa-Tyr-Phe-Gln-Asn-Cys-Pro-D-Arg-Gly-NH₂ (synthetic modified nonapeptide; Mpa = 3-mercaptopropionic acid; disulfide bridge Mpa¹–Cys⁶)
Modifications/formDeamination at position 1 (3-mercaptopropionic acid replaces Cys to reduce proteolysis); D-Arg at position 8 (V2 selectivity); C-terminal amide
Stable identifiersCAS 16679-58-6; 5311065; DrugBank DB00035; UNII ENR1LLB0FP; ATC H01BA02
Identity caveatsDistinct from vasopressin — V2-selective, substantially longer (2–3 h vs 10–35 min), negligible V1a activity; not interchangeable for vasodilatory shock; different across the oral, intranasal, sublingual, and injectable routes

Development and approval status

JurisdictionStatus and indicationProduct/sourceAs of
FDA (US)Approved — central DI, primary nocturnal enuresis (PNE), haemophilia A with factor VIII >5%, von Willebrand disease (type 1), nocturia (sublingual)DDAVP (tablet, spray, injection), Nocdurna (sublingual), Stimate (high-concentration spray)Various NDA dates
EMA (EU)Approved — same indicationsMinirin (tablet, melt, spray, injection)Approved
MHRA (UK)Approved — sameDesmopressin (generic)Approved
Status is multi-axis
Desmopressin authorization and sport-status profileFour medicine-authorization axes reproduce only documented status rows; sport status is shown separately.UNITED STATESApproved — central DI, primarynocturnal enuresis (PNE),SOURCE / AS OFROW 1 / Various NDA datesEU/EEAApproved — same indicationsSOURCE / AS OFROW 2 / ApprovedUNITED KINGDOMApproved — sameSOURCE / AS OFROW 3 / ApprovedOTHER DOCUMENTEDSOURCE ROW OMITTEDSEE AUDIT REASONSOURCE / AS OFNOT PRESENT / NOT RECORDEDSPORT STATUS — SEPARATE FROM MEDICINE AUTHORIZATIONWADA: prohibited — desmopressin is a masking agent on the WADA Prohibited List (category S5,Diuretics and Masking Agents); prohibited at all times
Authorization belongs to the named product, use, place, and date; sport status is independent.
文字说明
UNITED STATES
FDA (US): Approved — central DI, primary nocturnal enuresis (PNE), haemophilia A with factor VIII >5%, von Willebrand disease (type 1), nocturia (sublingual)
EU/EEA
EMA (EU): Approved — same indications
UNITED KINGDOM
MHRA (UK): Approved — same
OTHER DOCUMENTED
No OTHER DOCUMENTED row is present in the source status table

Sport status: WADA: prohibited — desmopressin is a masking agent on the WADA Prohibited List (category S5, Diuretics and Masking Agents); prohibited at all times

Mechanism and pharmacology

Desmopressin is a selective agonist at the V2 receptor (renal collecting duct), stimulating Gs/AC/cAMP/PKA signalling leading to aquaporin-2 insertion and free water reabsorption. At high doses, it also stimulates V2-mediated release of von Willebrand factor and factor VIII from endothelial Weibel-Palade bodies. Its selectivity for V2 over V1a is >100-fold, minimising vasopressor effects. is 2–3 hours (vs 10–35 min for vasopressin). Well-characterised — high confidence.

Evidence by claim

Claim/indicationStageGradeBest human evidenceMain resultImportant limitations
Central diabetes insipidusApproved (global)AMultiple ; label dataEffective antidiuresisWell-established
Primary nocturnal enuresisApproved (global)AMultiple RCTs; regulatory reviewReduces wet nights vs Relapse common after discontinuation
Haemophilia A / von Willebrand diseaseApproved (FDA)APivotal clinical trialsIncreased factor VIII and vWF sufficient for minor procedures (Stimate intranasal spray)Efficacy limited to mild disease (FVIII >5%)
Nocturia (adults)Approved (sublingual)APivotal RCTsReduced nocturnal voidsFluid restriction required
Bedwetting in children on SubQOff-label?——Not approved for route in children
证据等级
  • AA级：已确定特定标签用途
  • BB级：中等人体证据
  • CC级：初步人体证据
  • DD级：仅临床前
  • EE级：轶事/营销声明
  • XX级：证据与该声明相矛盾或不支持该声明
了解有关证据分级的更多信息
Claim-evidence profile
Desmopressin claim-evidence profileA: 4 claims; B: 0 claims; C: 0 claims; D: 0 claims; E: 0 claims; X: 0 claimsCONTRADICTORY / NON-SUPPORTIVEA — Established for a specific labeled useGrade A: Established for a specific labeled use — current approval plus adequate controlled trials and post-market context.4 claimsCentral diabetes insipidusPrimary nocturnal enuresis+2 moreB — Moderate human evidenceGrade B: Moderate human evidence — multiple controlled studies or a strong pivotal study, but no current approval for the claim.0 claimsC — Preliminary human evidenceGrade C: Preliminary human evidence — small, uncontrolled, surrogate-endpoint, or early-phase studies.0 claimsD — Preclinical onlyGrade D: Preclinical only — in vitro or animal evidence with no adequate human efficacy evidence.0 claimsE — Anecdotal/marketing claimGrade E: Anecdotal/marketing claim — testimonials, extrapolation, or vendor claims without adequate scientific support.0 claimsX — Evidence contradicts or does not support the claimGrade X: Evidence contradicts or does not support the claim — adequate negative evidence, failed program, or claim inconsistent with the studied material.0 claims
This counts the page's claim rows; it does not average them into a score. All claims: Central diabetes insipidus; Primary nocturnal enuresis; Haemophilia A / von Willebrand disease; Nocturia (adults).
文字说明

Text alternative for the claim-evidence diagram. Each grade is defined below:

A — Established for a specific labeled use
4 claims: Central diabetes insipidus; Primary nocturnal enuresis; Haemophilia A / von Willebrand disease; Nocturia (adults)
B — Moderate human evidence
0 claims
C — Preliminary human evidence
0 claims
D — Preclinical only
0 claims
E — Anecdotal/marketing claim
0 claims
X — Evidence contradicts or does not support the claim
0 claims
United StatesApproved — central DI, primary nocturnal enuresis (PNE), haemophilia A with factor VIII >5%, von Willebrand disease (type 1), nocturia (sublingual)
EU/EEAApproved — same indications
United KingdomApproved — same

Key studies

StudyDesign/populationExposure studiedEndpoints and resultLimitations
FDA label DDAVPCentral DI — , multiple trials0.1–0.4 mg oral; 5–40 mcg intranasalControlled urine output, normalised serum sodiumSome older; no modern -controlled DI trial (ethically problematic)
PNE meta-analysis (many)Meta-analysis, children (n=1000+)0.2–0.4 mg oral at bedtime1.3 fewer wet nights/week vs placeboHigh response variability
Nocdurna pivotal trialNocturia adults, (n≈1000)25–100 mcg sublingualClinically meaningful reduction in nocturnal voidsFluid restriction protocol required

Dose and administration evidence

Approved labeled regimen

The label summary below is product-, indication-, and jurisdiction-specific; consult the full current label and a licensed clinician/pharmacist.

Route-specific regimens:

Stimate is a high-concentration intranasal spray; DDAVP injection is a separate product with a different formulation, route, and dose. These are NOT interchangeable.

Studied regimens (not recommendations)

No additional significant studied regimens beyond approved routes and doses.

What is not established

  • Long-term efficacy for nocturia (durability of effect)

  • Dose adjustment protocols for elective surgery in haemophilia/vWD

  • Optimal fluid-restriction protocols

  • Chronic intranasal use safety concerns (rhinological changes)

Safety

Established label risks

Boxed warning (injectable formulation, and sublingual Nocdurna): Severe hyponatraemia can result in seizure, coma, respiratory arrest, and death. Extreme caution with patients at risk: hyponatraemia-prone conditions, cystic fibrosis, concomitant drugs increasing water intake or ADH/cox-2 effect.

Injection boxed warning also includes: Contraindicated in patients receiving loop diuretics, systemic/inhaled glucocorticoids.

Major warnings (all routes):

Contraindications: Hyponatraemia, moderate-to-severe renal impairment (CrCl less than 50 mL/min), polydipsia, and (for injection) concomitant loop diuretics or glucocorticoids.

Human-study signals

Well-characterised safety profile. Hyponatraemia is the primary dose-limiting concern and is more common without fluid restriction.

Unknowns and product-quality risks

  • Chronic high-dose intranasal use may alter nasal mucosa absorption

  • Research chemical desmopressin products are adulterated and unsafe

  • Not for use in patients with cystic fibrosis without careful sodium monitoring

Interactions and special populations

  • Drugs increasing hyponatraemia risk: SSRIs, NSAIDs, carbamazepine, oxcarbazepine, lamotrigine, chlorpromazine, TCAs, thiazide diuretics, loop diuretics

  • Drugs decreasing effect: lithium, demeclocycline

  • Renal impairment: contraindicated if CrCl less than 50 mL/min

  • Elderly: higher hyponatraemia risk; monitor sodium

  • Pregnancy: no adequate studies; small amounts cross placenta; use if needed

  • Lactation: desmopressin excreted in breast milk in small amounts

Regulatory, compounding, and sport notes

  • : prohibited — desmopressin is a masking agent on the WADA Prohibited List (category S5, Diuretics and Masking Agents); prohibited at all times

  • US DEA: not scheduled

  • Prescription scheduling and access vary by jurisdiction and formulation; the US products reviewed in this monograph are prescription products

  • Multiple generic formulations available

  • Injection: boxed warning; oral: no boxed warning but strong hyponatraemia warning

Evidence gaps

Search notes

  • Databases and registries: PubMed, DailyMed, FDA Drugs@FDA, Prohibited List, EMA product information

  • Search terms: Desmopressin, DDAVP, Minirin, Nocdurna, Stimate, 16679-58-6, hyponatraemia, WADA

  • Last searched: 2026-08-06

  • Inclusion emphasis: regulatory labels, clinical trials, safety communications

Sources

  1. FDA label: DDAVP (desmopressin acetate) tablets. DailyMed. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=6d55baa9-2b62-469c-93ae-3909ab249332&version=7

  2. FDA label: Nocdurna (desmopressin sublingual). DailyMed.

  3. FDA label: Stimate (desmopressin nasal spray). DailyMed.

  4. DrugBank DB00035. https://go.drugbank.com/drugs/DB00035

  5. PubChem CID 5311065. https://pubchem.ncbi.nlm.nih.gov/compound/5311065

  6. WADA Prohibited List 2026. https://www.wada-ama.org/en/prohibited-list

专家观点

专家怎么说

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评论缺失并不构成对该化合物有利或不利的证据。

供应商、诊所和社交媒体的声明根据政策被排除在外，不计入评论。

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视频评论缺失并不构成对该化合物有利或不利的证据。

供应商和社交媒体的视频根据政策被排除在外，不计入评论。

问题

Is desmopressin FDA-approved?

Yes. Desmopressin products are FDA-, EMA-, and MHRA-approved for specified indications that include central diabetes insipidus, primary nocturnal enuresis, mild haemophilia A or von Willebrand disease, and nocturia. Indications and warnings differ by product; severe hyponatraemia is a central safety concern. See the monograph's jurisdiction-specific label summary.

What does the evidence show for desmopressin and bedwetting in children?

Multiple RCTs and meta-analyses (n=1000+) show desmopressin reduces wet nights by approximately 1.3 fewer per week compared to placebo in primary nocturnal enuresis. Evidence is graded A. However, relapse is common after discontinuation. The approved oral regimen is taken at bedtime with fluid restriction.

Is desmopressin the same as vasopressin?

No. Desmopressin is a synthetic analogue of vasopressin with deamination at position 1 and substitution of L-Arg with D-Arg at position 8. These modifications confer V2-receptor selectivity (>100-fold over V1a) and a prolonged half-life (2-3 hours vs 10-35 minutes). They are not interchangeable.

What are desmopressin's main safety signals?

Severe hyponatraemia can result in seizure, coma, respiratory arrest, and death, and certain desmopressin products carry a boxed warning. Contraindications and monitoring requirements differ by product and include important medicine interactions. Fluid restriction is required under relevant labels; see the monograph's product-specific safety summary.

Is desmopressin prohibited in sport?

Yes. Desmopressin is a masking agent on the WADA Prohibited List (category S5, Diuretics and Masking Agents) and is prohibited at all times. It is not scheduled under US DEA. Prescription scheduling and access vary by jurisdiction and formulation.

What evidence supports desmopressin for haemophilia A or von Willebrand disease?

Desmopressin is FDA-approved for mild haemophilia A (factor VIII above 5%) and type 1 von Willebrand disease. At high doses, it stimulates V2-mediated release of von Willebrand factor and factor VIII from endothelial stores, sufficient for minor procedures. Evidence is graded A. Efficacy is limited to mild disease.

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