Английская Википедия:Ciraparantag
Шаблон:Short description Шаблон:Infobox drug
Ciraparantag (aripazine) is a drug under investigation as an antidote for a number of anticoagulant (anti-blood clotting) drugs, including factor Xa inhibitors (rivaroxaban, apixaban and edoxaban), dabigatran, and heparins (including fondaparinux, low molecular weight heparins (LMWH), and unfractionated heparin).[1][2]
Medical uses
Ciraparantag significantly reverses anticoagulation induced by a therapeutic dose of edoxaban within 10 minutes following injection.[3] This return to normal haemostasis persists over 24 hours following a single intravenous dose of the drug.[4] In addition to edoxaban, it also reverses the actions of LMWH and dabigatran.[5]
Pharmacology
Mechanism of action
According to in vitro studies, the substance binds directly to anticoagulants via hydrogen bonds and charge-charge interactions [3] from or to various parts of the molecule:[1]
| Hydrogen bonds | Rivaroxaban | Apixaban | Edoxaban | Dabigatran | Heparins |
|---|---|---|---|---|---|
| Guanidine part | Шаблон:Check mark | Шаблон:Check mark | Шаблон:Check mark | Шаблон:Check mark | |
| α-Amino group | Шаблон:Check mark | Шаблон:Check mark | Шаблон:Check mark | Шаблон:Check mark | |
| Amide nitrogen | Шаблон:Check mark | Шаблон:Check mark | Шаблон:Check mark | ||
| Amide oxygen | Шаблон:Check mark | Шаблон:Check mark |
Chemistry
Ciraparantag consists of two L-arginine units connected with a piperazine containing linker chain.[1]
See also
References
