INTRODUCTION: Dabigatran (Pradaxa, Prazaxa) is an anticoagulant medication that can be taken by mouth. It is being studied for various uses and in some cases is an alternative to warfarin, since it does not have to be monitored by blood tests, but offers similar results in terms of efficacy.
In case of major bleeding, there is an antidote, idarucizumab (sold under the brand name Praxbind). A large study sponsored by the manufacturer found that idarucizumab effectively reversed anticoagulation by dabigatran within minutes
THERAPEUTIC USES: Dabigatran is used to prevent strokes in those with atrial fibrillation not caused by heart valve issues, as well as deep vein thrombosis and pulmonary embolism in persons who have been treated for 5–10 days with parenteral anticoagulant (usually low molecular weight heparin), and to prevent deep vein thrombosis and pulmonary embolism in some circumstances.
It appears to be as effective as warfarin in preventing nonhemorrhagic strokes and embolic events in those with atrial fibrillation not due to valve problems
SIDE EFFECTS: The most commonly reported side effect of dabigatran is gastrointestinal upset. When compared to people anticoagulated with warfarin, patients taking dabigatran had fewer life-threatening bleeds, fewer minor and major bleeds, including intracranial bleeds, but the rate of gastrointestinal bleeding was significantly higher. Dabigatran capsules contain tartaric acid, which lowers the gastric pH and is required for adequate absorption. The lower pH has previously been associated with dyspepsia; some hypothesize that this plays a role in the increased risk of gastrointestinal bleeding.
A small but significantly increased risk of myocardial infractions (heart attacks) has been noted when combining the safety outcome data from multiple trials.
Reduced doses should be used in those with poor kidney function
Dabigatran may cause side effects. Tell your doctor if any of these symptoms occur:
· stomach pain
· upset stomach
· heartburn
· nausea
· unusual bruising or bleeding
· pink or brown urine
· red or black, tarry stools
· coughing up blood
· vomiting material that is bloody or looks like coffee grounds
· bleeding from the gums
· frequent nosebleeds
· heavy menstrual bleeding
· bleeding from a cut that lasts longer than normal
· joint pain or swelling
· headache
· dizziness or feeling faint
· weakness
· hives
· rash
· itching
· difficulty breathing or swallowing
· chest pain or tightness
· swelling of the face, throat, tongue, lips, eyes, arms, hands, feet, ankles, or lower legs
Dabigatran may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.
PHARMACOLOGY AND BIOCHEMISTRY: Antithrombins-
Endogenous factors and drugs that directly inhibit the action of THROMBIN, usually by blocking its enzymatic activity. They are distinguished from INDIRECT THROMBIN INHIBITORS, such as HEPARIN, which act by enhancing the inhibitory effects of antithrombins.
MECHANISM OF ACTION: It is a prodrug which is administered orally. It is a direct Thrombin inhibitor which reversibly blocks the catalytic site of thrombin and produce rapid anticoagulant action within 2 hours.
PHARMACOKINETICS: Oral bioavailability is low.
But the anticoagulant effect is consistent no monitoring is needed.
The plasma half life is 12-14 hours and Duration of action is 24 hours.
DRUG-DRUG INTERACTIONS:
Abciximab + Dabigatran = may increase the risk of bleeding, including severe and sometimes fatal hemorrhage
Drug+ ibuprofen=bruising, swelling, vomiting, blood in your urine or stools, headache, dizziness, or weakness.
Dabigatran +aspirin= Combining these medications can increase the risk of bleeding complications, brusing, vomiting.
REFERENCE: Tripathi K.D ; "Essentials of medical pharmacology"; Page no- 623-624
