Interacting drugs- summary

Anticoagulant Heparin, warfarin +  Agartropan

Prolongation of PT and INR

 Antiplatelet agents (Clopidogrel, NSAIDs Salicylates )  + Agartropan

Increased risk of bleeding

Glycoprotein IIb/ IIIa antagonists ( epifibatide tirofriban ) +  & vice versa

Agartropan safety and effectiveness not established

Thrombolytics ( alterplase, streptokinase +  Agartropan

Increased risk of bleeding

Anticoagulant Heparin, warfarin +    Agartroban

Concomittant use of agartroban and warfain results in prolongation of the PT and INR. Use of heparin is contraindicated in patients with HIT ( Heparin induced trombocytopenia )

Antiplatelet agents (Clopidogrel, NSAIDs Salicylates )  + Agartroban

Concomittant treatment with antipletelet agents may increase risk of bleeding

Glycoprotein IIb/ IIIa antagonists ( epifibatide tirofriban ) +  Agartoban

Safety and efectiveness of agartroban with glycoprotein  with glycoprotein IIa/IIIb anatgonists have not been Agartoban with established

Glycoprotein IIb/IIIa Thrombolytics ( alterplase, streptokinase +   Agartroban

Concomittant treatment with thrombolytics may increase risk of bleeding 

Heparin induced thrombocytopenia

Cardiovascular-

Atrial fibrillation, cardiac arrest, cerebrovascular disorders, hypotension, ventricular tachycardia

GI-

Abdominal pain, diarrhea, nausea, vomitig,

GU-

Abnormal renal function, yrinary tract infection

Respiratory-

Coughing, dyspnea, pneumonia

Miscellaneous-

Fever, infection,pain, sepsis

Overt major bleeding , hypersentivity to this product or any of its components

Warnings

Route of admin. Argotrpban is intended for IV admin. Discontinue all parentral anticoagulants before admin.f agartroban

Hemorrhage- Can occur at any site in the body in patient receiving agartroban. If the patient has an unexplained fall in hematrocrit, fall in blood pressure or any unexplained symptoms consider occurance of a hemorrhagic event. Use agartroban with extreme caution.

Hepatic function impairment- excercise caution when administering agartroban to patients with hepatic function impairment, start with a lower dose and carefully titrate until desired level of anticoagulation is acheived

Pregnancy- Use this drug in pregnancy only if clearly needed

Lactation- Because of potential risk for serious adverse reactions, decide whether to discontinue breast feeding or the drug taking into account the importance of th drug to the mother.

Children- Safety and effectiveness of agratroban including the appropiate anticoagulation goals and duration of therapy have not been established aming children .

Elderly- In clinical studies of adult patients, with HIT ot HITTS ( Heparin induced thrombocytopenia thrombosis syndrome ) the effectiveness of agartroban was not affected by age.

Indication-

Heparin induced thrombocytopenia

Dosage-

Initial dosage- Before administrring argatroban discontinue heparin therapy and obtain a baseline activated partial thromboplastim time ( aPTT).

The recommended initial dose of agratroban for adults without hepatic function impairment is 2cg/kg/min sadministered as a continuous infusion.

Inform patients that medicine may cause dizziness. They should not drive , operate machinery or do any thing else that could be dangerous until they know how they react to this medicine Advice patients that this medicine may reduce the number of clot-forming cells ( platelets ) in their blood.

To prevent bleeding advice patients to avoid situations in which bruising or injury may occur.

Tell patients to report any unusual bleeding , bruising, blood in stools, or dark tarry stools to their health provider

Tell your doctor of any severe adverse reactions - dificulty in breathing, hves, rash, swelling of mouth, chest pain, coffe brown vomit, confusion, dizziness , slurred speach etc,

Pharmacology

Agatropban is direct thrombin inhibitor that reversibly binds the thrombin active site. Agartropban does not require the cofactor antithromin III for antithrombin activity. Agratroban exerts its anticoagulant effect by inhibiting thrombin -catalyzed or thrombin induced reactions, including fibrin formation, activation of coagulation factors V VIII and XIII, activation of protein C, and platelet aggregation.

Pharmcokinetics

Argatroban distributes mainly in extracellular fluid as eveidenced by an apparent steady state volume of distribution of 174mL/kg ( 12.18L in an adult weighing 70Kg) Agartroban is 54% bound to human serum proteins, with binding to albumin and alpha -1 acid glycoprotein at 20% and 34% respy.

The total body clearance is approx. 5.1 ml/kg/min ( 0.31L/kg/hr ) for infusion doses upto 40mcg/kg/min Theterminal half life of agartroban ranges between 39 to 51 minutes Agartroban is excreted priomarily in fesces pesumably through biliary secretion.

Average percent recovery of unchanged drug, relativeto total dose was 16% in urine and at least 14% infeces

Pregnancy

Use this drug in pregnancy only if clearly needed

Lactation

Because of potential risk for serious adverse reactions, decide whether to discontinue breast feeding or the drug taking into account the importance of th drug to the mother.

Children-

Safety and effectiveness of agratroban including the appropiate anticoagulation goals and duration of therapy have not been established aming children

Elderly-

In clinical studies of adult patients, with HIT ot HITTS ( Heparin induced thrombosis - thrombocytopenia syndrome ) the efectiveness of agartroban was not affected by age.