Opicaponum

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**Opicaponum**
Cognitores
ChemSpider	24667564
PubChem	15602694
DrugBank	DB11632
Natura chemica

Formula summarum	C ₁₅H ₁₀Cl ₂N ₄O ₆
Massa molaris	413.17 g/mol
Natura pharmacologica
Codex ATC	N04BX04 (WHO)
Tempus semivitae biologicum	0.7-3.2 h
Spatium effectuum	>24 h
Excretio	renibus (13%), faecibus (67%)
Ad usum therapeuticum
Applicatio	per os

Opicaponum (abbreviatura: OPC) est medicamentum pharmaceuticum imprimis neurologiae ad morbum Parkinson tractandum adhibitum. Substantia gregi inhibitorum COMT attribuitur, quod significat, ut enzymum COMT (catechol-O-methyltransferasis) inhiberetur. Effectus Opicaponi longiores aliorum substantiorum huius gregis sunt.

Adhuc aliqui hepatotoxici effectus Tolcaponi incogniti sunt^[1].

Natura Opicaponi[recensere | fontem recensere]

Natura chemica[recensere | fontem recensere]

Opicaponum est derivatum chemicum oxadiazoli. Nomen chemicum (IUPAC) est (4E)-4-[3-(2,5-dichloro-4,6-dimethyl-1-oxido-pyridin-1-ium-3-yl)-2H-1,2,4-oxadiazol-5-ylidum]-2-hydroxy-6-nitrocyclohexa-2,5-dien-1-onum. Massa molaris est 413.17 g/mol.

Solubilitas in aqua 1,2,4-oxadiazoli causa bene est, et ob appendicem N-oxidi pyridini toxicitas cellularum (prae Tolcapono) parva et obsessio enzymi COMT magna^[2].

1,2,4-oxadiazolum
Pyridinum

Natura pharmacologica[recensere | fontem recensere]

Opicaponum est inhibitor enzymi COMT. Propterea in morbo Parkinson tractando adhibetur. Codex ATC est N04BX04 (WHO).

Pharmacodynamica[recensere | fontem recensere]

Opicaponum enzymum inhibit. Effectus Opicaponi simul selectivi et reversibiles sunt. Spatium effectuum dosis singularis plus quam 24 horas est.

Pharmacocinetica[recensere | fontem recensere]

Tempus semivitae biologicum Opicaponi est circiter sesquihora (0.7-3.2 h).

Effectus Opicaponi[recensere | fontem recensere]

Effectus pharmacologici[recensere | fontem recensere]

Ut supra scriptum Opicaponum enzymum COMT inhibet. Deminutionis degradationis neurotransmissoris DOPA causa incrementum neurotransmissoris praesynaptici fit.

Effectus secundarii[recensere | fontem recensere]

Dyskinesiae

Interactiones[recensere | fontem recensere]

Usus medicinus[recensere | fontem recensere]

Quamquam tempus semivitae biologicum eius valde breve est, prae aliis inhibitoribus COMT ut Entacapono vel Tolcapono spatium effectuum longius sustinetur, paene viginti quattuor horae^[3].

Dosis 50 mg Opicaponi vespere^[1] cum intervallo minimo unius horae ab L-DOPA commendata est.

Notae[recensere | fontem recensere]

↑ ^1.0 ^1.1 Scott L. J. (Sep 2016). "Opicapone: A Review in Parkinson's Disease". Drugs 76 (13): 1293-1300
↑ Kiss L. E., Ferreira H. S., Torrão L., Bonifácio M. J., Palma P. N., Soares-da-Silva P., Learmonth D. A. (Apr 2010). "Discovery of a long-acting, peripherally selective inhibitor of catechol-O-methyltransferase". Journal of medicinal chemistry 53 (8): 3396-411
↑ Rocha J. F., Almeida L., Falcão A., Palma P. N., Loureiro A. I., Pinto R., Bonifácio M. J., Wright L. C., Nunes T., Soares-da-Silva P. (Nov 2013). "Opicapone: a short lived and very long acting novel catechol-O-methyltransferase inhibitor following multiple dose administration in healthy subjects". British journal of clinical pharmacology 76 (5): 763-75

[SCOTT16-1] 1.0 ^1.1 Scott L. J. (Sep 2016). "Opicapone: A Review in Parkinson's Disease". Drugs 76 (13): 1293-1300

[2] Kiss L. E., Ferreira H. S., Torrão L., Bonifácio M. J., Palma P. N., Soares-da-Silva P., Learmonth D. A. (Apr 2010). "Discovery of a long-acting, peripherally selective inhibitor of catechol-O-methyltransferase". Journal of medicinal chemistry 53 (8): 3396-411

[3] Rocha J. F., Almeida L., Falcão A., Palma P. N., Loureiro A. I., Pinto R., Bonifácio M. J., Wright L. C., Nunes T., Soares-da-Silva P. (Nov 2013). "Opicapone: a short lived and very long acting novel catechol-O-methyltransferase inhibitor following multiple dose administration in healthy subjects". British journal of clinical pharmacology 76 (5): 763-75

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