Melperonum

compositum chemicum
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Melperonum
Cognitores
ChemSpider 14646
PubChem 15387
DrugBank DB09224
Natura chemica
Melperonum
Melperonum
Formula summarum C
16
H
22
FNO
Massa molaris 263.35 g/mol
Natura pharmacologica
Codex ATC N05AD03 (WHO)
Tempus semivitae biologicum 3-4 horae
Metabolismus iecore (hepaticus)
Excretio renibus (70%)
Ad usum therapeuticum
Applicatio per os, i.m.

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

Natura MelperoniRecensere

Natura chemicaRecensere

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 pharmacologicaRecensere

Melperono effectus sedativus est. Codex ATC est N05AD03.

PharmacodynamicaRecensere

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)

PharmacocineticaRecensere

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

Effectus MelperoniRecensere

Effectus non gratiRecensere

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

Effectus secundariiRecensere

Exempli (!) sunt:

InteractionesRecensere

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

Nexus interni

NotaeRecensere

  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).