Melperonum

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Melperonum
Cognitores
ChemSpider	14646
PubChem	15387
DrugBank	DB09224
Natura chemica


Formula summarum	C ₁₆H ₂₂FNO
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 Melperoni

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.

Melperono effectus sedativus est. Codex ATC est N05AD03.

Melperonum potissime D₃-, deinde alpha₂-, alpha₁-, D₃-, 5-HT_2A-, receptoria obsident.

Receptorium	Affinitas ligandi K_i (nM)^[1]	Annotatio
serotonini 5-HT_1A	2,200
serotonini 5-HT_1D	3,400
serotonini 5-HT_2A	230	Serotonini receptoriorum affinitas altissima
serotonini 5-HT_2C	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)

Effectus primi transitus magnus. Tempus semivitae biologicum $t_{\frac {1}{2}}$ .^[2] 3-4 horae est. Excretio est per urinas et biles.

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

Exempli (!) sunt:

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

↑ PDSP.
↑ Goldbook.
↑ 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).
↑ 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).
↑ 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).