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Niaprazine
Systematic (IUPAC) name
N-[4-[4-(4-fluorophenyl)piperazin-1-yl]butan-2-yl]pyridine-3-carboxamide
Identifiers
CAS number 27367-90-4
ATC code N05CM16
PubChem 71919
Chemical data
Formula C 20H25FN4O 
Mol. mass 356.437 g/mol
Physical data
Melt. point 131 °C (268 °F)
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life ~4.5 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral

Niaprazine (Nopron) is a piperazine derivative drug which acts as a sedating antihistamine as well as anticholinergic. It was invented in the 1970s [1], and is used in France, Italy and other European countries. It is mainly prescribed for its relatively strong sedative effects rather than as an antihistamine, and is used mainly for treating autism [2] and insomnia [3] in children and adolescents.

Side effects

Common side effects are: sedation during the day (especially during the first few days of treatment) and dizziness. Less common side effect is headache during the day.

Method of action

Niaprazine is a potent antagonist of the Histamine H1 receptor and is also an agonist at the serotonin receptors 5HT1A, 5HT2A and 5HT2C via its metabolite pFPP. Niaprazine enhances slow wave sleep.[4] It also antagonizes muscarinic acetylcholine receptors.

References

  1. ^ Duchene-Marullaz P, Rispat G, Perriere JP, Hache J, Labrid C. Some pharmacodynamical properties of niaprazine, a new antihistaminic agent. (French) Therapie. 1971 Nov-Dec;26(6):1203-9.
  2. ^ Rossi PG, Posar A, Parmeggiani A, Pipitone E, D'Agata M. Niaprazine in the treatment of autistic disorder. Journal of Child Neurology. 1999 Aug;14(8):547-50.
  3. ^ Younus M, Labellarte MJ. Insomnia in children: when are hypnotics indicated? Paediatric Drugs. 2002;4(6):391-403.
  4. ^ ZUCCONI et al. 1988, KALES: The pharmacology of sleep, 1995
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