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All about: Argatroban

Big Image Pronouncation: (ahr-GAT-troe-ban)
Class: Thrombin inhibitor

Trade Names:
Argatroban
- Injection 100 mg/mL

Mechanism of Action

Pharmacology

Binds reversibly to thrombin active site, exerting its anticoagulant effects by inhibiting thrombin-catalyzed or induced reactions, including activation of coagulation factors V, VIII, and XIII, protein C, and platelet aggregation.

Pharmacokinetics

Distribution

Distributes mainly in the extracellular fluid. Vd is 174 mL/kg. Approximately 54% is protein bound (20% to albumin and 34% to alpha-1-glycoprotein).

Metabolism

Hydroxylation and aromatization in the liver. CYP3A4/5 plays a minor role.

Elimination

Cl is approximately 5.1 mL/kg/min; t ½ is 39 to 51 min. Approximately 65% is excreted in the feces (through biliary secretion) and approximately 22% is excreted in the urine. At least 14% is recovered in the feces as unchanged drug and 16% in urine.

Onset

Immediate.

Peak

1 to 3 h (steady state).

Special Populations

Hepatic Function Impairment

Cl is reduced and t ½ is increased. Dosage adjustment is recommended.

Indications and Usage

As an anticoagulant for prophylaxis and treatment of thrombosis in heparin-induced thrombocytopenia (HIT); as an anticoagulant in patients with or at risk for heparin-induced thrombocytopenia undergoing percutaneous coronary intervention (PCI).

Contraindications

Overt major bleeding; hypersensitivity to this product or any component of this product.

Dosage and Administration

Coadministration of Warfarin
Adults (receiving argatroban up to 2 mcg/kg/min)

Measure international normalized ratio (INR) daily during coadministration of argatroban and warfarin. In general, doses of argatroban up to 2 mcg/kg/min can be discontinued when the INR is greater than 4. Repeat INR 4 to 6 h after stopping argatroban and, if the INR is below desired therapeutic range, resume argatroban infusion and repeat the procedure daily until desired therapeutic range on warfarin alone is achieved.

Adults (receiving argatroban at doses greater than 2 mcg/kg/min)

Temporarily reduce dose of argatroban to 2 mcg/kg/min and repeat the INR on argatroban and warfarin 4 to 6 h after reducing the argatroban dose; follow the process described above for administering warfarin and argatroban at doses up to 2 mcg/kg/min.

Hepatic Function Impairment
Adults

IV In patients with moderate hepatic function impairment, initial dose is 0.5 mcg/kg/min; monitor aPTT closely and adjust dose as clinically indicated.

HIT or Heparin-Induced Thrombocytopenia and Thrombosis Syndrome (HITTS)
Adults

IV Initial dose is 2 mcg/kg/min as a continuous infusion; after initial dose, the dose can be adjusted as clinically indicated (not exceeding 10 mcg/kg/min), until steady-state activated partial thromboplastin time (aPTT) is 1.5 to 3 times the initial baseline value (not to exceed 100 sec).

PCI in HIT or HITTS
Adults

IV Initial dose is 25 mcg/kg/min and bolus of 350 mcg/kg via large bore IV line administered over 3 to 5 min. Check activated clotting time (ACT) 5 to 10 min after bolus is completed. Proceed if ACT is greater than 300 sec. If ACT is less than 300 sec, administer an additional IV bolus dose of 150 mcg/kg, increase the infusion dose to 30 mcg/kg/min, and check the ACT 5 to 10 min later. If ACT is greater than 450 sec, decrease the infusion rate to 15 mcg/kg/min and check ACT 5 to 10 min later. Once ACT is between 300 and 450 sec, continue infusion dose for the duration of the procedure. In case of dissection, impending abrupt closure, thrombus formation during the procedure, or inability to achieve or maintain an ACT over 300 sec, additional bolus doses of 150 mcg/kg may be administered and the infusion dose increased to 40 mcg/kg/min. Check the ACT after each additional bolus or change in rate of infusion.

General Advice

  • Follow manufacturer's guidelines for diluting concentrated solution in sodium chloride 0.9% injection, dextrose 5% injection, or Ringer's lactate injection before infusing.
  • Do not mix with other injections or infusions.
  • Do not administer if particulate matter or discoloration noted.

Storage/Stability

Store vials at controlled room temperature (59° to 86°F). Diluted solution can be kept at room temperature for up to 24 h or in refrigerator (36° to 46°F) for up to 48 h. Do not freeze or expose to direct sunlight.

Drug Interactions

Anticoagulants, antiplatelet agents, thrombolytics

May increase risk of bleeding.

Heparin

Allow sufficient time for effects of heparin on aPTT to decrease before starting argatroban therapy.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension (11%); cardiac arrest (6%); ventricular tachycardia, bradycardia (5%); MI (4%); atrial fibrillation (3%); cerebrovascular disorder, coronary thrombosis, myocardial ischemia, coronary occlusion, angina pectoris (2%); aortic stenosis, arterial thrombosis, cerebrovascular disorder, vascular disorder (1%).

CNS

Headache (5%).

Dermatologic

Allergic skin reactions (including rash, bullous eruption; 1% to less than 10%).

GI

Minor hemorrhagic GI bleeding (14%); nausea (7%); diarrhea, vomiting (6%); abdominal pain (3%); major hemorrhagic GI bleeding (2%); gastroesophageal reflux disease (1%).

Genitourinary

Minor GU hemorrhage and hematuria (12%); UTI (5%); abnormal renal function (3%); major GU hemorrhage and hematuria (1%).

Hematologic

Minor decrease in hemoglobin and hematuria (12%); sepsis (6%); overall bleeding (hemorrhagic [5%]); retroperitoneal hemorrhage, major decrease in hemoglobin and hematocrit (1%).

Pulmonary

Hemoptysis, pneumonia (3%); lung edema (1%).

Respiratory

Allergic airway reactions (including coughing and dyspnea [10% or more]); dyspnea (8%); coughing (3%).

Miscellaneous

Chest pain (15%); back pain (8%); minor hemorrhagic event/groin, pain (5%); infection, fever (4%); minor hemorrhagic event/brachial (2%); general allergic reactions (1% to less than 10%).

Precautions

Monitor

Active clotting time (ACT)

Determine ACT prior to removal of arterial sheath. Do not remove sheath until ACT is less than 160 sec.

Bleeding/Bruising

Monitor patient for signs of bleeding, especially at vascular access sites, throughout therapy. If excessive or unusual bruising develops, or if bleeding develops (eg, epistaxis, hematuria, hematemesis, bloody or black, tarry stools) or is suspected (eg, unexplained fall in hematocrit or BP, or any other unexplained symptom develops), notify health care provider immediately.

Hematocrit/Hemoglobin

Ensure baseline hematocrit or hemoglobin and platelet count are obtained and evaluated prior to starting therapy.


Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hepatic Function

Use with caution.

Hemorrhage

Because hemorrhage can occur at any site in patients receiving argatroban, use with extreme caution in disease states or circumstances in which there is an increased danger of hemorrhage (eg, major surgery, severe hypertension, spinal anesthesia).

Parenteral anticoagulants

Ensure all parenteral anticoagulants have been discontinued before administering argatroban.

Overdosage

Symptoms

Excessive anticoagulation.

Patient Information

  • Advise patient, family, or caregiver that medication will be prepared and administered by health care professional in a hospital setting.
  • Instruct patient, family, or caregiver to report any of the following immediately: bleeding or unusual bruising, coughing, difficulty breathing, skin rash or reaction.

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