Dabigatran etexilate may provide a promising alternative for the treatment of postprocedural vision loss after ppv. A direct thrombin inhibitor, dabigatran etexilate (hereinafter referred to as dabigatran) was approved in the Russian Federation for prevention of thromboembolic complications in orthopaedic practice (2009), for prevention of ischaemic embologenic stroke in atrial fibrillation (2011) and for treatment of recurrent thrombosis of deep veins and pulmonary artery thromboembolism (2014). Additional administration of 2 × 110 mg dabigatran etexilate (Pradaxa(®)), a novel direct thrombin inhibitor, resulted in a prompt and marked improvement of visual acuity, which indicated improved blood flow in the central vessels of the optic nerve. Dabigatran etexilate appeared to have several pharmacokinetic and pharmacodynamic advantages over warfarin, as well as a favorable efficacy and safety profile being at least noninferior and often superior to warfarin in patients with non-valvular AF. The latter was shown in the clinical trials, meta-analyses and studies with 'real-world' data. Currently ongoing trials will expand the body of evidence on warfarin and will aid decision making in currently controversial areas. Important limitations of dabigatran etexilate include contraindications for its use in patients with prosthetic heart valves and end-stage chronic kidney disease.
| Molecular Weight | 723.84 |
| Formula | C35H45N7O8S |
| CAS Number | 872728-81-9 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Thrombopoietin/Thrombin Products |
|---|
| Desirudin
Desirudin is a thrombin inhibitor that inhibits thrombosis and venous stasis thrombosis.Desirudin can be used in studies related to thrombocytopenia or platelet dysfunction. |
| TP508
TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. |
| Succinyl-(Pro58, D-Glu65)-Hirudin (56-65) (sulfated)
Succinyl-(Pro58,D-Glu65)-Hirudin (56-65) (sulfated) is a hirugen-like peptide, and has high affnity for thrombin than Hirugen, with a KD < 100 nM. |
| Thrombin receptor peptide ligand
Thrombin receptor peptide ligand is a thrombin receptor antagonist peptide that can be used as an antithrombotic agent. |
| Z-Gly-Pro-Arg-4MβNA
Z-Gly-Pro-Arg-4MβNA is the cleavage of the substrate of thrombin to release free 4-methoxy-2-naphthylamine (4MβNA). |
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