Английская Википедия:Ciraparantag

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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

Шаблон:Reflist

Шаблон:Blood-drug-stub