Risperidonum
Risperidonum est substantia antipsychotica et propterea medicamentum ad therapiam schizophreniarum praescriptum.
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Cave: notitiae huius paginae nec praescriptiones nec consilia medica sunt. |
Risperidonum in ordinis mundi sanitarii indicem exemplarem medicamentorum essentialium receptum est.
Natura Risperidoni
recensereNatura chemica
recensere
Risperidonum est substantia benzisoxazoli derivata, Aripiprazolo igitur sive Ziprasidono simile. Structura sua est 3-{2-[4-(6-fluorum-1,2-benzisoxazol-3-yl)piperidino]aethylo}-2-methylo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidino-4-onum.
Massa molaris sua est 410.48 g/mol. Codex ATC est N05AX08.
Pharmacodynamica
recensereRisperidonum dopamini- et serotonini- et histamini- et adrenergica receptoria obsidet.
| Receptorium | Affinitas ligandi, Ki (nM)[1] | Actio |
|---|---|---|
| serotonini 5-HT1A | 423 | antagonista |
| serotonini 5-HT1B | 14.9 | antagonista |
| serotonini 5-HT1D | 84.6 | antagonista |
| serotonini 5-HT2A | 0.17 | agonista inversus |
| serotonini 5-HT2B | 61.9 | agonista inversus |
| serotonini 5-HT2C | 12.0 | agonista inversus |
| serotonini 5-HT5A | 206 | antagonista |
| serotonini 5-HT6 | 2,060 | antagonista |
| serotonini 5-HT7 | 6.60 | antagonista Irreversibilis (seu pseudo-irreversibilis)[2] |
| dopamini D1 | 244 | antagonista |
| dopamini D2 | 3.57 | antagonista |
| dopamini D2L | 4.16 | antagonista |
| dopamini D2S | 4.73 | antagonista |
| dopamini D3 | 3.6 | agonista inversus |
| dopamini D4 | 4.66 | antagonista |
| dopamini D5 | 290 | antagonista |
| adrenergicorum α1A | 5.0 | antagonista |
| adrenergicorum α1B | 9.0 | antagonista |
| adrenergicorum α2A | 16.5 | antagonista |
| adrenergicorum α2B | 108 | antagonista |
| adrenergicorum α2C | 1.30 | antagonista |
| Receptoria Muscarinica acetylcholini (mAChR) | >10,000 | exigue |
| histamini H1 | 20.1 | agonista inversus |
| histamini H2 | 120 | agonista inversus |
Pharmacocinetica
recensereTempus semivitae biologicum .[3] est 20 h (applicatio intra muscularem: 2-3 d). Excretio est per urinas (70%) et per biles(14%). Risperidoni metabolitus activus (cum virtute antipsychotica) Paliperidonum est.
Risperidonum substratum Cytochromatis P450 CYP2D6 est.
Effectus Risperidoni
recensereEffectus non grati
recensereCum usu Risperidoni, animum advertere ad effectus secundarios et interactiones necesse est.
Notae
recensere- ↑ https://web.archive.org/web/20131108013656/http://pdsp.med.unc.edu/pdsp.php
- ↑ Smith, C.; Rahman, T.; Toohey, N.; Mazurkiewicz, J.; Herrick-Davis, K.; Teitler, M. (2006). "Risperidone Irreversibly Binds to and Inactivates the h5-HT7 Serotonin Receptor". Molecular Pharmacology 70 (4): 1264–1270
- ↑ Goldbook.