Dabigatran
Also known as: Dabigatran etexilate mesylate
Dabigatran and its acyl glucuronides are competitive, direct thrombin inhibitors. Because thrombin (serine protease) enables the conversion of fibrinogen into fibrin during the coagulation cascade, its inhibition prevents the development of a thrombus. Both free and clot-bound thrombin, and thrombin-induced platelet aggregation are inhibited by the active moieties. This lowers the chances of blood clots formation in body and hence reduces the risk of stroke and blood clots in people with Atrial fibrillation.
Primary Characteristics
Dabigatran is also known as Dabigatran etexilate mesylate, .
Molecular Weight: 267.7 · Solubility in Water: 1.8 mg/mL. · Solubility in Alcohol: slightly soluble · Non-proprietary name: Dabigatran.
Pharmacokinetics
Absorption: Dabigatran has an oral bioavailability is 5% (±2%).
Distribution: Dabigatran has a volume of distribution is 50-70 L. plasma protein binding is 35%.
Elimination: it is metabolised via hepatic, plasma half-life is 12-17 hours, renal excretion is 7% after oral intake , 80% after IV administartion.
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Indications
Dabigatran is primarily indicated in conditions like Stroke, Thromboembolism.
Contraindications
Dabigatran is contraindicated in conditions like Bleeding, Hypersensitivity to any component of product.
Dosage
Dabigatran's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 75 mg | 75 mg | Every 12h | PO | For patients with severe renal impairment creatinine clearance (CrCl) 15-30 mL/min. Do not take the missed dose atleast 6 hours before next scheduled dose |
| 150 mg | 150 mg | Every 12h | PO | For patients with creatinine clearance (CrCl) >30 mL/min. Do not take the missed dose atleast 6 hours before next scheduled dose |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Dabigatran in overdosage may give rise to further complications which include Bleeding .
Dabigatran produces potentially life-threatening effects which include Bleeding . Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Dabigatran are hemorrhagic complications.
Dabigatran is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Anaphylactoid reactions, Bleeding , Chest pain, Chest tightness, Difficulty breathing, Dizziness, Dyspepsia , Epigastric discomfort, Esophagitis, Faintness , GI ulceration, Hypersensitivity reactions, Pruritus , Rashes , Swelling of face, Swelling of lips and tongue, Urticaria, Wheezing .
Warnings / Precautions
Interference in Pathology
Dabigatran may interfere in the diagnosis of Dabigatran prolongs the aPTT, ECT and TT.
Available Brands
None recorded.
Storage Conditions
Drug Classification
- 1.10.2 — Anticoagulants/Platelet deaggregators