Niaprazine

Jump to: navigation, search

{{Drugbox | IUPAC_name = N-{4-[4-(4-fluorophenyl)piperazin- 1-yl]butan- 2-yl}pyridine- 3-carboxamide | image = Niaprazine.png

| tradename = | Drugs.com = International Drug Names | pregnancy_category = | legal_status = Rx-only | routes_of_administration = Oral

| metabolism = | elimination_half-life = ~4.5 hours | excretion =

| CAS_number = 27367-90-4 | ATC_prefix = N05 | ATC_suffix = CM16 | PubChem = 71919 | ChemSpiderID = 64930 | UNII_Ref =  ☑Y | UNII = R2H3YN6E3L | KEGG = D07333

| C=20 | H=25 | F=1 | N=4 | O=1 | molecular_weight = 356.437 g/mol | smiles = Fc3ccc(N2CCN(CCC(NC(=O)c1cccnc1)C)CC2)cc3 }}

WikiDoc Resources for Niaprazine

Articles

Most recent articles on Niaprazine

Most cited articles on Niaprazine

Review articles on Niaprazine

Articles on Niaprazine in N Eng J Med, Lancet, BMJ

Media

Powerpoint slides on Niaprazine

Images of Niaprazine

Photos of Niaprazine

Podcasts & MP3s on Niaprazine

Videos on Niaprazine

Evidence Based Medicine

Cochrane Collaboration on Niaprazine

Bandolier on Niaprazine

TRIP on Niaprazine

Clinical Trials

Ongoing Trials on Niaprazine at Clinical Trials.gov

Trial results on Niaprazine

Clinical Trials on Niaprazine at Google

Guidelines / Policies / Govt

US National Guidelines Clearinghouse on Niaprazine

NICE Guidance on Niaprazine

NHS PRODIGY Guidance

FDA on Niaprazine

CDC on Niaprazine

Books

Books on Niaprazine

News

Niaprazine in the news

Be alerted to news on Niaprazine

News trends on Niaprazine

Commentary

Blogs on Niaprazine

Definitions

Definitions of Niaprazine

Patient Resources / Community

Patient resources on Niaprazine

Discussion groups on Niaprazine

Patient Handouts on Niaprazine

Directions to Hospitals Treating Niaprazine

Risk calculators and risk factors for Niaprazine

Healthcare Provider Resources

Symptoms of Niaprazine

Causes & Risk Factors for Niaprazine

Diagnostic studies for Niaprazine

Treatment of Niaprazine

Continuing Medical Education (CME)

CME Programs on Niaprazine

International

Niaprazine en Espanol

Niaprazine en Francais

Business

Niaprazine in the Marketplace

Patents on Niaprazine

Experimental / Informatics

List of terms related to Niaprazine

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

Niaprazine (Nopron) is a sedative-hypnotic drug of the phenylpiperazine class.[1] It has been used in the treatment of sleep disturbances since the early 1970s in several European countries, including France, Italy, and Luxembourg.[2][3] It is commonly used with children and adolescents on account of its favorable safety and tolerability profile and lack of abuse potential.[4][5][6][7][8][9]

Originally believed to act as an antihistamine and anticholinergic,[10] niaprazine was later discovered to have no significant binding affinity for either the H1 or the mACh receptors (Ki = > 1 μM), and was instead found to act as a potent and selective 5-HT2A and α1-adrenergic receptor antagonist (Ki = 75 nM and 86 nM, respectively).[11] It is virtually inactive at 5-HT1A, 5-HT2B, D2, and β-adrenergic, as well as at SERT and VMAT (Ki = all > 1 μM), but it does have some weak affinity for the α2-adrenergic receptor (Ki = 730 nM),[11] likely acting as an antagonist there as well.

Niaprazine has been shown to metabolize to the compound pFPP in a similar manner to how trazodone and nefazodone metabolize to mCPP.[12][13] It is unclear what role, if any, pFPP plays in the clinical effects of niaprazine.[11] However, from animal studies it is known that pFPP, unlike niaprazine, does not produce sedative effects, and instead exerts a behavioral profile indicative of serotonergic activation.[12]


References

  1. Kent, Angela; M. Billiard (2003). Sleep: physiology, investigations, and medicine. New York: Kluwer Academic/Plenum. ISBN 0-306-47406-9.
  2. Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. ISBN 3-88763-075-0.
  3. David J. Triggle (1996). Dictionary of Pharmacological Agents. Boca Raton: Chapman & Hall/CRC. ISBN 0-412-46630-9.
  4. Franzoni E, Masoni P, Mambelli M, Marzano P, Donati C (1987). "[Niaprazine in behavior disorders in children. Double-blind comparison with placebo]". La Pediatria Medica E Chirurgica : Medical and Surgical Pediatrics (in Italian). 9 (2): 185–7. PMID 2958783.
  5. Bodiou C, Bavoux F (1988). "[Niaprazine and side effects in pediatrics. Cooperative evaluation of French centers of pharmacovigilance]". Thérapie (in French). 43 (4): 307–11. PMID 2903572.
  6. Ottaviano S, Giannotti F, Cortesi F (October 1991). "The effect of niaprazine on some common sleep disorders in children. A double-blind clinical trial by means of continuous home-videorecorded sleep". Child's Nervous System : ChNS : Official Journal of the International Society for Pediatric Neurosurgery. 7 (6): 332–5. doi:10.1007/bf00304832. PMID 1837245.
  7. Montanari G, Schiaulini P, Covre A, Steffan A, Furlanut M (1992). "Niaprazine vs chlordesmethyldiazepam in sleep disturbances in pediatric outpatients". Pharmacological Research : the Official Journal of the Italian Pharmacological Society. 25 Suppl 1: 83–4. doi:10.1016/1043-6618(92)90551-l. PMID 1354861.
  8. Younus M, Labellarte MJ (2002). "Insomnia in children: when are hypnotics indicated?". Paediatric Drugs. 4 (6): 391–403. doi:10.2165/00128072-200204060-00006. PMID 12038875.
  9. Mancini J, Thirion X, Masut A; et al. (July 2006). "Anxiolytics, hypnotics, and antidepressants dispensed to adolescents in a French region in 2002". Pharmacoepidemiology and Drug Safety. 15 (7): 494–503. doi:10.1002/pds.1258. PMID 16700077.
  10. Duchene-Marullaz P, Rispat G, Perriere JP, Hache J, Labrid C (1971). "[Some pharmacodynamical properties of niaprazine, a new antihistaminic agent]". Thérapie (in French). 26 (6): 1203–9. PMID 4401719.
  11. 11.0 11.1 11.2 Scherman D, Hamon M, Gozlan H; et al. (1988). "Molecular pharmacology of niaprazine". Progress in Neuro-psychopharmacology & Biological Psychiatry. 12 (6): 989–1001. doi:10.1016/0278-5846(88)90093-0. PMID 2853885.
  12. 12.0 12.1 Keane PE, Strolin Benedetti M, Dow J (February 1982). "The effect of niaprazine on the turnover of 5-hydroxytryptamine in the rat brain". Neuropharmacology. 21 (2): 163–9. doi:10.1016/0028-3908(82)90157-5. PMID 6460945.
  13. International review of neurobiology. New York: Academic Press. 1988. ISBN 0-12-366829-8.

Linked-in.jpg