Haloperidolum

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Haloperidolum
Haloperidolum
Haloperidolum
Natura chemica
Formula chemica C21H23CIFNO2
Massa molaris 375.9 g/mol
PubChem 3559
DrugBank DB00502
Natura pharmacologica
Codex ATC N05AD01 (WHO)
Semivita biologica 14-37 h (per os)
21 h (i.m.)
Metabolismus iecore (hepaticus)
Excretio faecibus et per urinas
Ad usum therapeuticum
Applicatio per os, i.m. (, i.v.)
MedlinePlus a682180 (Anglice)

Haloperidolum est substantia antipsychotica et propterea medicamentum, quod cogitari potest, ad therapiam schizophreniarum praescriptum, maniae interruptionum bipolarium[1] sicut syndroma Tourette, delirii.

Haloperidolum in ordinis mundi sanitarii indicem exemplarem medicamentorum essentialium receptum est.

Natura Haloperidoli

Natura chemica

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

Natura pharmacologica

Codex ATC est N05AD01 (WHO).

Pharmacodynamica

Haloperidolum potissime D2- et D3-receptoria obsidet.

Receptorium Haloperidoli affinitas ligandi, Ki (nM)[2] Actio pharmacodynamica
dopamini D1 -
dopamini D2 1.55 agonista inversa
dopamini D3 0.74 agonista inversa
dopamini D4 5 - 9 agonista inversa
dopamini D5 - -
serotonini 5-HT1A 1927
serotonini 5-HT2A 53 [3]
serotonini 5-HT2C 10,000
serotonini 5-HT6 3666
serotonini 5-HT7 377.2
adrenergicum α1A 12
adrenergicum α2A 1130
adrenergicum α2B 480
adrenergicum α2C 550
histamini H1 1,800
muscarinicum acetylcholini M1 10,000
σ1 3
σ2 54
σ2 54
Receptorium NMDA, subunitas NR1A/2B 3,000[4]

Pharmacocinetica

Tempus semivitae biologicum .[5] 14 — 37 h est. Excretio est per urinas et biles.

Effectus Haloperidoli

Haloperidolum est substantia antipsychotica et butyrophenonum.

Effectus histopathologici

Haloperidolum effectus quoque structurae synaptibus ostendit. Numerus spinarum dentriticarum (per significans iter AKT-GSK-3 beta) minuitur[6].

Effectus pharmacologici

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

Effectus secundarii

Exempli (!) sunt:

Saepe (1%-10%)

  • 1. Symptomata extrapyramidalia
  • 2. Depressio
  • 3. Somnolentia
  • 4. Hypotensio

Alia

Interactiones

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

Pharmaca cum effectibus Haloperidoli substrati
Inhibitores cum Haloperidoli effectibus fortioribus Inductores cum Haloperidoli effectibus minoribus
  • Antihypertensiva
  • Antiarrhythmica
    • Amiodaronum
    • Dronedaronum
  • Antidepressiva
    • Fluvoxaminum
    • Nefazodonum (forte)
  • Diuretica/Hormonta
    • Conivaptanum (forte)
  • Antibiotica
    • Ciprofloxacinum
    • Macrolida
      • Clarithromycinum (forte)
      • Erythromycinum (forte)
      • Telithromycinum (forte)
  • Antiemetica
    • Aprepitantum
  • Fungicida/-statica
    • Fluconazolum
    • Ketoconazolum (forte)
    • Isavuconazolum
    • Itraconazolum (forte)
    • Posaconazolum (forte)
    • Voriconazolum (forte)
  • Proteasis inhibitores
    • Atazanavirum-Ritonavirum
    • Boceprevirum (forte)
    • Cobicistatum (forte)
    • Indinavirum (forte)
    • Lopinavirum cum Ritonaviro (forte)
    • Nelfinavirum (forte)
    • Ritonavirum (forte)
    • Saquinavirum (forte)
    • Telaprevirum (forte)
  • Idelalisibum (forte)
  • Imatinibum
  • Nilotinibum
  • Ribociblibum (forte)
  • Glucocorticoides
    • Dexamethasonum (forte)
  • Verapamilum
  • Hormonta
    • GH
  • Plantae
  • 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

  1. ↑ Anglice mania 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 Psychopharmacol 27 (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 Pharmacol 50 (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, and aripiprazole on the dendritic spine". Eur Neuropsychopharmacol: S0924-977X(18)30067-1