Haloperidolum

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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, K_i (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-HT_1A	1927
serotonini 5-HT_2A	53	^[3]
serotonini 5-HT_2C	10,000
serotonini 5-HT₆	3666
serotonini 5-HT₇	377.2
adrenergicum α_1A	12
adrenergicum α_2A	1130
adrenergicum α_2B	480
adrenergicum α_2C	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 $t_{\frac {1}{2}}$ .^[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
- Dystonia
- Akathisia
- Rigiditas musculorum
2. Depressio
3. Somnolentia
4. Hypotensio

Alia

Intervallum QT prolongatum

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 Calcii canalium inhibitores Diltiazemum Felodipinum 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 Fructus averrhoae carambolae Silybum marianum	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

↑ Anglice mania of bipolar disorder; hic formae fem. pluralis, quia haec diagnosis duas interruptiones saltim postulat
↑ https://web.archive.org/web/20131108013656/http://pdsp.med.unc.edu/pdsp.php
↑ 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
↑ 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
↑ http://goldbook.iupac.org/B00658.html
↑ 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

[1] Anglice mania of bipolar disorder; hic formae fem. pluralis, quia haec diagnosis duas interruptiones saltim postulat

[2] ttps://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] ttp://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

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