Argatroban

Structure of thrombin complexed with inhibitors similar to argatroban and lepirudin. Source: NIH.

Other Names

The drug is not sold by any other names and no generic form is available. The molecule's systematic chemical name is 1-[5-][(aminoiminomethyl)amino]-1-oxo-2-[[(1,2,3,4-tetrahydro-3-methyl-8-quinolinyl)sulfonyl]amino]pentyl]-4-methyl-2-piperidinecarboxylic acid, monohydrate.

Uses

• Argatroban is used to treat and reduce the risk of blood clots in patients who have had a reaction to heparin that resulted in reduced platelets and associated blood clots, a condition known as heparin-induced thrombocytopenia (HIT).
• Argatroban is also used in patients undergoing certain heart procedures such as percutaneous coronary interventions (PCI) who are at risk, or have had a reaction to heparin that resulted in reduced platelets and associated blood clots.

How Argatroban Is Taken

Argatroban is supplied in vials containing 250 mg of drug suspended in 2.5 mL of liquid for intravenous injection.

How It Works

Argatroban is a synthetic derivative of the naturally-occurring amino acid L-arginine and acts as a reversible direct thrombin inhibitor. The plasma half-life (the time it takes for the drug's concentration to fall by 50%) is about 45 minutes. The effect on blood clotting is measured by the activated partial thromboplastin time, or aPTT test, and dose adjustments are made based on the results of this test. Argatroban is metabolized by the liver.

Risks and Precautions

Argatroban should not be given to individuals who have major bleeding. It may act unpredictably in patients with liver disease, since it is normally metabolized by the liver.

Complications

Increased risk of bleeding is the most common complication of Argatroban. If the following conditions are present, the risk of bleeding may be increased:

• Severe high blood pressure
• Recent lumbar puncture, or spinal anesthesia
• Recent major surgery (especially involving the brain, spinal cord, or eye)
• Medical conditions that increase the tendency to bleed
• Stomach ulcers

Interactions

• Because certain other medications can interact with Argatroban, and may increase the risk of bleeding, a thorough medication history is needed before giving Argatroban, with special attention given to medications known to affect bleeding (such as aspirin and warfarin).

Side Effects

Bleeding is the most common side effect.

Other side effects may include:

• Shortness of breath
• Low blood pressure
• Fever
• Diarrhea

Alternatives

For patients with HIT, two drugs are approved for anticoagulation: argatroban and lepirudin. Lepirudin is a synthetic version of an anticoagulant hirudin found in the saliva of the blood-eating leech Hirudo medicinalis. In contrast to argatroban, lepirudin has a slightly longer half-life (~1 hour) and is eliminated by the kidneys, not the liver. Other anticoagulants include bivalirudin, indicated for patients undergoing PCI, and ximelgatran, which is not yet approved in the US.^[1]

References

1. ↑ Bauer KA. New anticoagulants. Hematology Am Soc Hematol Educ Program. 2006:450-6. Abstract | Full Text | PDF