Argatroban: Effects, Uses & Risks

Argatroban belongs to the group of active substances known as anticoagulants and is used to inhibit blood clotting. The drug has been sold in Germany since 2005 under the name Argatra Multidose and is administered as an infusion solution.

What is Argatroban?

Argatroban belongs to the anticoagulant group of drugs and is used to inhibit blood clotting. As an anticoagulant, Argatroban binds directly to thrombin in the bloodstream and inhibits unwanted blood clotting. The drug is used exclusively for the treatment of heparin-induced thrombocytopenia, where it can achieve rapid success, although the side effects can be considerable. To prevent heart attacks or strokes, Argatroban is nevertheless frequently prescribed. It can be used in adult patients of all ages and can also be administered to pregnant women. Argatroban is available only as an infusion solution and therefore cannot be used for self-treatment.

Pharmacologic Action

Argatroban, when used correctly, which is free of side effects, should act solely on the blood circulation in the body or thrombin contained therein. The drug binds to thrombin and attempts to prevent its action – which includes, for example, the activation of various so-called clotting factors and the formation of fibrin. Furthermore, thrombin attempts to activate protein C, which also promotes blood clotting. Argatroban prevents or inhibits these negative effects for the patient, so that they should no longer occur if the dosage and duration of use are correct. Argatroban remains in the body for only 50 minutes before it is metabolized in the liver by an as yet unknown enzyme. In Germany, Argatroban is marketed under the name Argatra Multidose. Furthermore, the administration of Argatroban can have an alcoholizing effect on the patient due to the relatively high concentration of ethanol in the drug, which is why subsequent driving immediately after an infusion is not advisable. The alcohol in Argatroban may also cause the effects of other drugs, which are altered in their action by alcohol, to be enhanced or attenuated.

Medicinal use and application

Because it is an infusion solution, treatment with Argatroban is never done by yourself, but always by a doctor or otherwise trained professional. The exact dose and duration of administration is decided by the physician on an individual basis. Argatroban is used to inhibit or completely prevent the formation of blood clots in the patient’s circulation. It is used exclusively to treat so-called heparin-induced thrombocytopenia type II, which is also abbreviated as HIT II. Risks from the blood clots caused by HIT II include possible heart attacks, strokes, or breathing problems, as well as blood flow disturbances in the limbs. Argatroban, when used properly, can result in either relieving or stopping these symptoms (but not their cause). It is not for prevention and therefore can only be used for acute HIT II and currently has no off-label uses for other conditions. Argatroban must not be administered if the patient has severe hepatic dysfunction or active bleeding caused by HIT II. Argatroban must not be administered to women during lactation. During pregnancy, the lowest possible dosage must be aimed for.

Risks and Side Effects

Argatroban is rich in side effects, the most common of which may be mild to severe bleeding. In these cases, immediate medical attention is essential. These include blood in the cough, sudden bruising under the skin, and blood in the urine or stool. Furthermore, patients may suffer from breathing difficulties as well as experience dryness in the mouth. Nausea is also a common side effect of Argatroban, with an incidence of up to 10%. Less common side effects include dizziness, confusion and possible fainting, as well as headache and speech or vision problems. Temporary numbness or urinary tract infections may also be a result of Argatroban side effects. Fever, joint pain and a permanent feeling of tiredness, as well as constipation or diarrhea may occur.However, these side effects occur very rarely, with a maximum frequency of 1%.