Argatroban is a synthetic direct thrombin inhibitor and the chemical name is 1-[5-[(aminoiminomethyl) amino]-1-oxo2[[(1,2,3,4-tetrahydro-3-methyl-8-quinolinyl)sulfonyl]amino]pentyl]-4-methyl-2- piperidinecarboxylic acid, monohydrate. Argatroban has 4 asymmetric carbons. One of the asymmetric carbons has an R configuration (stereoisomer Type I) and an S configuration (stereoisomer Type II). Argatroban consists of a mixture of R and S stereoisomers at a ratio of approximately 65:35.

The molecular formula of argatroban is C₂₃H₃₆N₆O₅S•H₂O. Its molecular weight is 526.66 g/mol. The structural formula is:

Argatroban Injection is a sterile, non-pyrogenic, clear, colorless to pale yellow, aqueous solution. It is supplied in a single use, clear glass vial containing 50 mg of argatroban in 50 mL solution. Each mL, contains 1 mg argatroban, 2 mg lactobionic acid, 2 mg L-methionine USP, 8 mg sodium chloride USP, and sodium hydroxide NF (for pH adjustment) in water for injection USP. The pH of the solution is approximately 8.8.

Last reviewed on RxList: 8/10/2011
This monograph has been modified to include the generic and brand name in many instances.