Melperonum

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

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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.

Natura Melperoni

Natura chemica

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

Melperono effectus sedativus est. Codex ATC est N05AD03.

Pharmacodynamica

Melperonum potissime D₃-, deinde alpha₂-, alpha₁-, D₃-, 5-HT_2A-, 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

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

Effectus Melperoni

Effectus non grati

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

Effectus secundarii

Exempli (!) sunt:

• Dystonia
• Akathisia
• Hypersalivatio
• Miosis
• Prolongatio intervalli QT

Interactiones

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

Nexus interni

• Pharmacologia

Notae

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).