Dabigatran Etexilate Mesylate
Brand Name: Pradaxa
Common Dosage Forms:
Capsules: 75 mg and 150 mg.
FDA Indications/Dosages:
Indicated to reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation:
In patients with CrCL >30 mL/min: 150 twice a day.
In patients with CrCL 15-30 mL/min: 75 mg twice a day.
Converting from parenteral anticoagulants: Start 0-2 hours before the next dose of the parental anticoagulant is due.
Converting to a parental anticoagulant: Wait 12 hours (CrCL >30 mL/min) or 24 hours (CrCL 15-30 mL/min) after the last dose of PRADAXA before starting a parental anticoagulant.
Converting from warfarin: Stop warfarin and wait until the INR is below 2.0.
Converting to warfarin: Start warfarin before stopping PRADAXA based on the CrCL (>50 mL/min=3 days, 30-50 mL/min=2 days, 15-30 mL/min=1 day).
Monitor: RFT.
Pharmacology/Pharmacokinetics: Dabigatran and its metabolites are competitive, direct thrombin inhibitors. Thrombin is an important component of the coagulation cascade, converting fibrinogen into fibrin. Both free and clot-bound thrombin, and thrombin-induced platelet aggregation are inhibited. Oral bioavailability is low at 3% to 7% and is affected by the activity of P-glycoprotein. Dabigatran etexilate is converted after absorption into dabigatran. Protein-binding is relatively low at 35%. Elimination occurs primarily in the urine.
Drug Interactions: Rifampin and St. John’s Wort may decrease blood levels of dabigatran through induction of P-glycoprotein in the intestine and kidney. P-glycoprotein inhibitors (verapamil, dronedarone, ketoconazole, amiodarone, quinidine) may increase dabigatran levels.
Contraindications/Precautions: Contraindicated in patients with active pathological bleeding. Serious bleeding episodes can occur during therapy. Use caution in patients at risk for bleeding. Use with caution in patients on drugs which increase bleeding (anti-platelet agents, heparin, NSAIDs, and fibrinolytic therapy). Monitor patients for the signs and symptoms of blood loss. PREMATURE DISCONTINUATION OF THERAPY INCREASES THE RISK OF THROMBOTIC EVENTS. MAY CAUSE SPINAL/EPIDURAL HEMATOMA in patients who are receiving neuraxial anesthesia or undergoing spinal puncture. Renal function should be accessed prior to starting therapy and at least yearly in patients over the age of 75 years and in those with CrCL <50 mL/min. Disrupting therapy can increase the risk for stroke. Discontinue use 1-2 days before surgery (CrCL >50 mL/min) or 3-5 days before surgery (CrCL <50 mL/min). Use with caution in the elderly and nursing mothers. Pregnancy Category C.
Adverse Effects: The most common adverse effects are also potentially serious and include bleeding, dyspepsia, nausea, upper abdominal pain, GI hemorrhage, and diarrhea.
Patient Consultation:
May be taken with or without food.
Swallow the capsule whole, do not break, chew or empty the pellets from the capsule.
If a dose is missed, take it as soon as possible. If it is closer to the time of your next dose than the dose you missed, skip the missed dose and return to your dosing schedule. Do not double doses.
Do not discontinue therapy without first consulting physician. You may need to temporarily stop therapy during certain procedures. Be sure to tell all your physicians and your dentist you are currently taking this medication.
Contact a physician if you experience any of the following: unusual bleeding of any kind, pink or brown urine, red or dark stools, coughing or vomiting blood, unusual bruising, unusual pain or swelling, headaches, or dizziness.
Store PRADAXA in its original container. Only remove the dose you are taking and tightly close the container after removing your dose. After opening a bottle of PRADAXA, use within 4 months.
Do not take OTC aspirin, ibuprofen, or naproxen without the knowledge of your physician.