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Haloperidolum

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Haloperidolum
Haloperidolum
Haloperidolum
Natura chemica
Formula chemicaC21H23CIFNO2
Massa molaris375.9 g/mol
PubChem3559
DrugBankDB00502
Natura pharmacologica
Codex ATCN05AD01(WHO)
Semivita biologica14-37 h (per os)
21 h (i.m.)
Metabolismusiecore (hepaticus)
Excretiofaecibus et per urinas
Ad usum therapeuticum
Applicatioper os, i.m. (, i.v.)
MedlinePlusa682180(Anglice)

Haloperidolum estsubstantiaantipsychotica et proptereamedicamentum, quod cogitari potest, ad therapiamschizophreniarum praescriptum, maniae interruptionum bipolarium[1] sicutsyndroma Tourette, delirii.

Haloperidolum inordinis mundi sanitariiindicem exemplarem medicamentorum essentialium receptum est.

Natura Haloperidoli

[recensere |fontem recensere]

Natura chemica

[recensere |fontem recensere]

Structura chemica Haloperidoli est 4-[4-(4-chlorphenyl)-4-hydroxypiperidino]-4-fluor-butyrophenonum, quod estatomofluori et butyrophenonum (anulus aromaticus (benzenum)) etbutanum cumketono et piperidinum (anulus cum uno atomo nitrogenii (ammina secundaria)) et alius anulus aromaticus cum atomochlori. Massa molaris est 375.86 g/mol.

Natura pharmacologica

[recensere |fontem recensere]

Codex ATC estN05AD01(WHO).

Pharmacodynamica

[recensere |fontem recensere]

Haloperidolum potissimeD2- etD3-receptoria obsidet.

ReceptoriumHaloperidoli affinitas ligandi,Ki (nM)[2]Actio pharmacodynamica
dopamini D1-
dopamini D21.55agonista inversa
dopamini D30.74agonista inversa
dopamini D45 - 9agonista inversa
dopamini D5--
serotonini 5-HT1A1927
serotonini 5-HT2A53[3]
serotonini 5-HT2C10,000
serotonini 5-HT63666
serotonini 5-HT7377.2
adrenergicum α1A12
adrenergicum α2A1130
adrenergicum α2B480
adrenergicum α2C550
histamini H11,800
muscarinicum acetylcholini M110,000
σ13
σ254
σ254
Receptorium NMDA, subunitas NR1A/2B3,000[4]

Pharmacocinetica

[recensere |fontem recensere]

Tempus semivitae biologicumt12{\displaystyle t_{\frac {1}{2}}}.[5] 14 — 37 h est. Excretio est per urinas et biles.

Effectus Haloperidoli

[recensere |fontem recensere]

Haloperidolum est substantia antipsychotica etbutyrophenonum.

Effectus histopathologici

[recensere |fontem recensere]

Haloperidolum effectus quoque structurae synaptibus ostendit. Numerus spinarum dentriticarum (persignificans iterAKT-GSK-3 beta) minuitur[6].

Effectus pharmacologici

[recensere |fontem recensere]

Praeter desiderabiles cum uso Haloperidoli animum advertere ad effectus secundarios et interactiones necesse est.

Effectus secundarii

[recensere |fontem recensere]

Exempli (!) sunt:

Saepe (1%-10%)

Alia

Interactiones

[recensere |fontem recensere]

Cum Haloperidolum subtratum enzymiCYP3A4 esset, inhibitores CYP3A4 effectus Haloperidoli augere possint, inductores invicem diminuere, per exemplum:

Pharmaca cum effectibus Haloperidoli substrati
Inhibitores cumHaloperidoli effectibusfortioribusInductores cumHaloperidoli effectibusminoribus
  • Anticonvulsiva
    • Carbamazepinum (forte, quoque P-gp)
    • Phenytoinum (forte)
    • Fosphenytoinum (forte)
    • Oxcarbazepinum (forte)
    • Eslicarbazepinacetatum
    • Topiramatum
    • Phenobarbitalum (forte)
    • Primidonum (forte)
  • Antidepressiva
    • Hypericum perforatum (forte, quoque P-gp)
  • Antihypertensiva
    • Bosentanum (forte, endothelini receptoris inhibitor)
  • Substantiae antiretrovirales
    • Efavirenzum (forte)
    • Etravirinum (forte)
    • Nevirapinum (forte)
  • Substantiae antineoplasticae
    • Dabrafenibum
    • Enzalutamidum
    • Mitotanum (forte)
  • Antibiotica
    • Rifabutinum (forte)
    • Rifapentinum (forte)
    • Nafcillinum (forte)
    • Rifampicinum (forte)
  • Hormonta
    • Triiodthyroninum (T3)
  • Antiandrogena
    • Apalutamidum
  • Modafinilum
  • Quercetinum
  • Capsaicinum

Nexus interni

Notae

[recensere |fontem recensere]
  1. Anglicemania of bipolar disorder; hic formae fem. pluralis, quia haec diagnosis duas interruptiones saltim postulat
  2. https://web.archive.org/web/20131108013656/http://pdsp.med.unc.edu/pdsp.php
  3. Suzuki H, Gen K, Inoue Y(2013)."Comparison of the anti-dopamine D₂ and anti-serotonin 5-HT(2A) activities of chlorpromazine, bromperidol, haloperidol and second-generation antipsychotics parent compounds and metabolites thereof".J Psychopharmacol27(4): 396-400 
  4. Ilyin VI, Whittemore ER, Guastella J, Weber E, Woodward RM(Dec 1996)."Subtype-selective inhibition of N-methyl-D-aspartate receptors by haloperidol".Mol Pharmacol50(6): 1541-50 
  5. http://goldbook.iupac.org/B00658.html
  6. Takaki M, Kodama M, Mizuki Y, Kawai H, Yoshimura B, Kishimoto M, Sakamoto S, Okahisa Y, Yamada N(2018)."Effects of the antipsychotics haloperidol,clozapine, andaripiprazole on the dendritic spine".Eur Neuropsychopharmacol: S0924-977X(18)30067-1 
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