Melperonum

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Melperonum est substantia sedativum atque antipsychotica levior, ideoque praecipue ad therapiam insomniam praescriptum.

Natura chemica[recensere | fontem recensere]

Melperonum in butyrophenonis numeratur. Id est haloperidolo structura chemica causa simile, sane quidem effectus antipsychotici sui pauci sunt.

Melperonum ut benperidolum et haloperidolum et triperidolum est butyrophenonorum (butyrophenonum est 1-phenylbutan-1-onum). Structura chemica melperoni est 4-fluorum-4-(4-methyl-piperidino)-butyrophenonum.

Massa molaris est 263.35 g/mol.

Natura pharmacologica[recensere | fontem recensere]

Melperono effectus sedativus est. Codex ATC est N05AD03.

Pharmacodynamica[recensere | fontem recensere]

Melperonum potissime D3-, deinde alpha2-, alpha1-, D3-, 5-HT2A-, receptoria obsident.

Receptorium Affinitas ligandi
Ki (nM)[1]
Annotatio
serotonini 5-HT1A 2,200
serotonini 5-HT1D 3,400
serotonini 5-HT2A 230 Serotonini receptoriorum affinitas altissima
serotonini 5-HT2C 2,100
serotonini 5-HT6 1,254
serotonini 5-HT7 578
adrenergici α1 180
adrenergici α2 180
acetylcholini M1 >10,000 exigue
acetylcholini M2 2,400
acetylcholini M3 >10,000 exigue
acetylcholini M4 4,400
acetylcholini M5 >10,000 exigue
dopamini D2 194 Haloperidolum: 1.55 (fortius)
dopamini D3 8.95 Dopamini receptoriorum affinitas altissima; Haloperidolum: 0.74 (fortius)
dopamini D4 555
histamini H1 580 Haloperidolum: 1,800 (levius)

Pharmacocinetica[recensere | fontem recensere]

Effectus primi transitus magnus. Tempus semivitae biologicum .[2] 3-4 horae est. Excretio est per urinas et biles.

Effectus non grati[recensere | fontem recensere]

Cum uso melperoni animum advertere ad effectus secundarios et interactiones necesse est.

Effectus secundarii[recensere | fontem recensere]

Exempli (!) sunt:

  • Dystonia
  • Akathisia
  • Hypersalivatio
  • Miosis

Interactiones[recensere | fontem recensere]

Melperonum est inhibitor CYP2D6.[3][4][5]

Nexus interni

Notae[recensere | fontem recensere]

  1. PDSP.
  2. Goldbook.
  3. Gahr, M; Gastl, R; Kölle, MA; Schönfeldt-Lecuona, C; Freudenmann, RW (2012). "Successful treatment of schizophrenia with melperone augmentation in a patient with phenotypic CYP2D6 ultrarapid metabolization: a case report". Journal of Medical Case Reports 6 (1): 49  (Anglice).
  4. Köhnke, MD; Lutz, U; Wiatr, G; Schwärzler, F; Weller, B; Schott, K; Buchkremer, G (April 2006). "Cytochrome P450 2D6 dependent metabolization of risperidone is inhibited by melperone". European Journal of Clinical Pharmacology 62 (4): 333–334  (Anglice).
  5. Grözinger, M; Dragicevic, A; Hiemke, C; Shams, M; Müller, MJ; Härtter, S (January 2003). "Melperone is an inhibitor of the CYP2D6 catalyzed O-demethylation of venlafaxine". Pharmacopsychiatry 36 (1): 3–6  (Anglice).