Argatroban

Argatroban is used to treat Thrombosis and Coronary heart disease, and can cause a wide range of different side effects.

Overview:

Argatroban is an anticoagulant used to break up unwanted blood clots that form in the body. It was developed in Japan and is currently produced by GlaxoSmithKline under the name Argatroban. Other brand names for the drug include Argatroban NovaPlus and Premier Pro RX Argatroban.

Conditions Treated:

  • Thrombosis (the formation of blood clots in veins or arteries)
  • Heparin induced thrombocytopenia (a condition caused by heparin therapy, a means of treating thrombosis)
  • Coronary heart disease

Type of Medicine:

  • Anticoagulant/Thrombin inhibitor

Side Effects:

Argatroban can cause a wide range of different side effects, including sweating and internal bleeding. Argatroban therapy can be hard on the body, and it is important for patients to contact their doctor immediately as soon as they experience any side effects. The most common side effects of argatroban therapy can include:

  • Bleeding from the bladder/blood in a patient's urine
  • Blurred vision
  • Chest pain
  • Confusion
  • Dizziness
  • Faintness or lightheadedness, especially immediately after getting up from a seated or prone position
  • Unconsciousness
  • Fever
  • Lack of a pulse
  • Lack of a blood pressure
  • Stopping of the heart
  • Sweating
  • Unconsciousness
  • Unusual tiredness or weakness

Some of argatroban’s less common side effects can include:

  • Arm pain
  • Back pain
  • Jaw pain
  • Bloody or blackened stools
  • Chest tightness
  • Constipation
  • Coughing
  • Hoarseness
  • Coughing or spitting up blood
  • Irregular heartbeat
  • Nausea
  • Painful or irregular urination
  • Heart palpitations
  • Severe stomach pain
  • Severe abdominal pain
  • Vomiting
  • Vomiting blood
  • Vomiting a material that resembles coffee grounds (coagulated blood)

In rarer cases, patients may experience symptoms than can include:

  • Abdominal pain or or swelling
  • Back aches
  • Blue extremities, such as lips or fingertips
  • Changes in skin color, paleness
  • Rogue coldness in the extremities, such as the hands and feet
  • Coughing which may produce a pink frothy sputum
  • Diarrhea
  • Unusual shortness of breath, wheezing
  • Unusual sweating
  • Indigestion
  • Loss of appetite
  • Pain, redness, or swelling of the patient's legs
  • Pains in the chest, groin, or calves
  • Passing of gas
  • Sudden and/or extreme headaches
  • Sudden loss of coordination
  • Sudden onset of slurred speech
  • Sudden vision changes
  • Swelling of the legs or ankles

This is not necessarily a complete list of side effects. Patients should contact their doctor if they experience any unusual effects. Patients can report new side effects to the FDA at 1-800-FDA-1088.

Dosage:

For treatment of thrombosis, thromboembolic disorders, or heparin-induced thrombocytopenia:

2 mcg/kg/min (two micrograms per kilogram of bodyweight per minute) is usually the initial dose, building as needed (but not to exceed 10 mcg/kg/min) until a steady state of aPTT (activated partial thromboplastin time) can be maintained. The ideal aPTT range is 1.5 to three times what the patient’s initial aPTT range was.

The same procedure is followed in pediatric treatments, but many more variables are at play, and hard and fast numbers are impossible to give. Often time the treatment begins at .75 mcg/kg/min, and has been known to get as high as 2 mcg/kg/min in order to achieve the ideal aPTT.

Argatroban is metabolized by the liver, necessitating smaller doses for patients who suffer from hepatic impairment. In adults, a 0.5 mcg/kg/min constant infusion is usually used as the initial dose. In pediatric patients, the ideal initial dose is usually a 0.2 mcg/kg/min constant infusion.

For percutaneous coronary intervention (treatment of narrowed arteries in the heart which result from coronary heart disease):

A initial dose of 350 mcg/kg is usually delivered to the patient over the course of 3 to 5 minutes, along with a starting infusion of 25 mcg/kg/min. The dose will continue, being raised to as much as 30 mcg/kg/min and with additional infusions of 150 mcg/kg until the ideal ACT (activated clotting time, a measure of the blood’s ability to clot) is achieved. Henceforth, the treatment will be continued at the dose which achieves the ideal ACT.

Argatroban is metabolized by the liver. Patients with hepatic impairment will need to use a lower dose of argatroban to achieve the ideal ACT. Often times, because so much argatroban is needed for percutaneous coronary intervention, patients will use other methods to treat their symptoms.

Interactions:

Argatroban can interact with a whole host of drugs, in both major and minor ways. Many of the drugs which interact most severely with argatroban do so by raising the chances of severe hematic side effects. Any medicine which thins the blood or makes the patient more likely to bleed has the potential to interact with argatroban in a very negative way. The drugs listed below are known to interact seriously with argatroban. This is not necessarily a complete list of possible interactions, and patients should discuss all drugs, medications, or supplements they are taking with their doctor before receiving argatroban.

  • Ado-trastumuzab emtansine
  • Alteplase
  • Anistreplase
  • Apixaban
  • Ardeparin
  • Betrixaban
  • Bivalirudin
  • Cabozantinib
  • Cangrelor
  • Dabigatran
  • Deferasirox
  • Dalteparin
  • Danaparoid
  • Dasatanib
  • Defibrotide
  • Desirudin
  • Drotrecogin alfa
  • Edoxaban
  • Enoxaparin
  • Fondaparinux
  • Heparin (heparin can cause a condition argatroban is used to treat)
  • Heparin flush (heparin can cause a condition argatroban is used to treat)
  • Ibritumomab
  • Ibrutinib
  • Iodine i 131 tositumomab
  • Ipilimumab
  • Mifepristone
  • Omacetaxine
  • Panobinostat
  • Prasugrel
  • Prothrombin complex
  • Ramucirumab
  • Regorafenib
  • Reteplase
  • Rivaroxaban
  • Streptokinase
  • Temsirolimus
  • Tenecteplase
  • Tinzaparin
  • Tipranavir
  • Tositumomab
  • Urokinase
  • Vorapaxar

Similarly, the following medications are known to interact with argatroban primarily by increasing the risk of rogue bleeding. For many medications, patients should pay attention to their prothrombin levels (a protein and coagulating agent) if they choose to go ahead with receiving argatroban therapy while simultaneously taking any of the drugs listed below. This is not necessarily a complete list of drug interactions and patients should be sure to discuss all of the drugs, medications, and supplements they are taking with their doctor before receiving argatroban therapy.

  • Abciximab
  • Acetaminophen
  • Anagrelide
  • Anisindione
  • Aspirin
  • Baclofen
  • Bismuth subsalicylate
  • Benzoic acid
  • Bromfrenac
  • Bromfrenac opthalmic
  • Caffeine
  • Calcium
  • Capsaicin
  • Celecoxib
  • Chlorpheniramine
  • Choline salicylate
  • Cilostazol
  • Citalopram
  • Clomipramine
  • Clopidogrel
  • Collagenase clostridium histolyticum
  • Deoxycholic acid
  • Desvenlafaxine
  • Dexfenfluramine
  • Diclofenac
  • Diclofenac ophthalmic
  • Diphenhydramine
  • Dicumarol
  • Diflunisal
  • Dipyridamole
  • Dong quai
  • Doxycycline
  • Duloxetine
  • Epoprostenol
  • Eptifibatide
  • Escitalopram
  • Esomeprazole
  • Etodolac
  • Famotidine
  • Fenfluramine
  • Fenoprofen
  • Fluoxetine
  • Flurbiprofen
  • Fluvoxamine
  • Garlic
  • Ginger
  • Ginkgo
  • Ginger
  • Ginseng
  • Hemin
  • Horsechestnut
  • Hydrocortisone
  • Hyoscyamine
  • Ibuprofen
  • Icosapent
  • Iloprost
  • Indomethacin
  • Ketamine
  • Ketoprofen
  • Ketorolac
  • Lactobacillus casei
  • Lansoprazole
  • Levomilnacipran
  • Magnesium salicylate
  • Meclofenamate
  • Mefenamic acid
  • Meloxicam
  • Milnacipran
  • Nabumetone
  • Naproxen
  • Nepafenac ophthalmic
  • Nintedanib
  • Omega-3 polyunsaturated fatty acids
  • Oxaprozin
  • Paroxetine
  • Pentosan polysulfate sodium
  • Pentoxifylline
  • Phenylbutazone
  • Piroxicam
  • Protein c
  • Rofecoxib
  • Salsalate
  • Sertraline
  • Sibutramine
  • Sodium iodide i-123
  • Sodium iodide i-131
  • Sodium salicylate
  • Sodium thiosalicylate
  • Sugammadex
  • Sulfinpyrazone
  • Sulindac
  • Sunitinib
  • Suprofen ophthalmic
  • Ticagrelor
  • Ticlopidine
  • Tirofiban
  • Tolmetin
  • Treprostinil
  • Ubiquinone
  • Valdecoxib
  • Venlafaxine
  • Verteporfin
  • Vilazodone
  • Vitamin E
  • Vortioxetine
  • Warfarin

Warfarin and argatroban can be used to treat the same conditions. Warfarin is an oral anticoagulant, and patients are sometimes shifted from argatroban therapy to warfarin. In order to maintain the anticoagulant effects on the patient, the two are recommended to be taken concurrently for a period. There is no hard data at this time to suggest what the optimal period is for taking both argatroban and warfarin. In order to avoid adverse effects on the patient’s INR (a measure of the patient’s coagulating ability, with the intent to ensure that the patient retains some coagulating ability) a loading dose of warfarin is not usually administered. While the patient is receiving both argatroban and warfarin, they should be monitored by their doctor for signs of increased side effects and irregular INR.

In rare and minor cases, argatroban can interact with the following medications:

  • Clove
  • Capsicum
  • Chamomile
  • Fenugreek
  • Feverfew
  • Turmeric

Warnings:

Because it is delivered intravenously, argatroban’s greatest effects are hematological. Patients should be aware that argatroban therapy has caused patients to experience depleted hemoglobin levels, rogue episodes of bleeding (including from the groin) internal bleeding, and hemorrhages. Some patients suffered bleeding from their brachial artery, a high volume artery which if compromised puts the patient at risk of dying of blood loss. Patients suffered internal bleeding and hemorrhages in the intestine, the brain, and across a multitude of other organs.

One patient being treated for heparin-induced thrombocytopenia suffered a 4 day intracranial hemorrhage, even after ceasing argatroban therapy.

Argatroban therapy has also caused patients to experience hypertension and even cardiac arrest.

On top of the effects on the cardiovascular system, argatroban therapy has been known to cause pneumonia, fevers, urinary tract infections, and even cause sepsis.

Argatroban is metabolized by the liver. Patients with hepatic impairment should be given adjusted doses of the medicine. Patients with hepatic impairment, especially severe hepatic impairment should discuss with their doctor before receiving argatroban therapy. With dose adjustments to account for liver damage, argatroban therapy may be an ineffective way to treat the patient’s condition. Other anticoagulants exist which are metabolized by organs that are not the liver.

Argatroban is a class b drug for pregnancy risk. Argatroban poses no known risk to human fetuses. Women who are pregnant should consult with their doctor before receiving argatroban therapy.

Patients who are actively bleeding or who are healing from a wound should not receive argatroban therapy. Argatroban is an anticoagulant, and impedes the patient’s body’s ability to close the wound.

Additionally, patients who have conditions or diseases that make them predisposed to bleeding should exercise caution when considering receiving argatroban therapy. Patients should consult with their doctor before receiving argatroban therapy.

Storage:

Argatroban is typically administered by trained medical professionals. Situations where the patient would have to store the drug him/herself would be rare.

With that said, argatroban should be stored at a controlled room temperature of 68 to 77 degrees Fahrenheit or at a refrigerated temperature of 5 to 41 degrees Fahrenheit. Argatroban should be stored away from direct sunlight.

Summary:

Argatroban is a powerful, specialized drug which can greatly help patients with specific conditions. However, because it is an anticoagulant, it can have serious effects on a patient’s blood flow, especially on the patient’s body’s ability to control that blood flow. Patients who are considering argatroban therapy should be prepared to be constantly vigilant during the period of time they are treated, and respect the power that the drug has. A handful of the compounds argatroban interacts with are spices like clove and turmeric, so patients should exercise added caution when cooking or eating out.

As with any drug or treatment, the patient should discuss all facets of the treatment beforehand, including any preconditions the patient might have and any/all drugs or supplements the patient is taking.

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Last Reviewed:
December 25, 2017
Last Updated:
December 22, 2017
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