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

Natura chemica 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

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

Pharmacodynamica recensere

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

Pharmacocinetica recensere

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

Effectus Opicaponi recensere

Effectus pharmacologici recensere

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

Effectus secundarii recensere

Dyskinesiae

Interactiones recensere

Usus medicinus 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

↑ ^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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