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Refludan (Berlex Labs)

Refludan (Berlex Labs) - General Information

Refludan (Berlex Labs) is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells.

 

Pharmacology of Refludan (Berlex Labs)

Refludan (Berlex Labs) is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Refludan (Berlex Labs) requires no cofactor for its anticoagulant action.

 

Refludan (Berlex Labs) for patients

What is Refludan used for? Refludan is indicated for patients who have had a reaction to heparin that resulted in reduced platelets and associated blood clots, in order to prevent more clotting complications

Who should not be treated with Refludan? You should not be given Refludan if you are allergic to this drug or similar drugs.

Special Warnings for Refludan:

Bleeding is the most common complication of Refludan. If you have the following conditions, your risk of bleeding may be increased:

  • Recent puncture of large vessels or organ biopsy
  • Abnormality of blood vessels or organs
  • Recent "mini-stroke," stroke, brain surgery, or other central nervous system procedure
  • Uncontrolled severe high blood pressure
  • Infection of the heart lining (endocarditis)
  • Advanced kidney damage
  • Tendency to bleed
  • Recent major surgery
  • Recent major bleeding

General Precautions with Refludan:

  • Your doctor will monitor your treatment by using a test that measures the clotting time of your blood.
  • The dosage of Refludan may be decreased if you have liver or kidney disease.

What should I tell my doctor or health care provider?

Because certain other medications can interact with Refludan, and increase the risk of bleeding, review all medications that you are taking with your health care provider, including those that you take without a prescription. Other drugs that break up or dissolve clots, such as (rt-PA) or streptokinase, or drugs that prevent clots such as Coumadin, warfarin, or aspirin, can increase your risk of bleeding.

What are some possible side effects of Refludan? (This is NOT a complete list of side effects reported with Refludan. Your health care provider can discuss with you a more complete list of side effects.)

Bleeding was the most common adverse event reported during testing of the product. Bleeding can be severe.

Other side effects occurring in at least 2% of the people studied:

  • Abnormal liver function
  • Allergic skin reactions

For more detailed information about Refludan, ask your health care provider.

 

Refludan (Berlex Labs) Interactions

Concomitant treatment with thrombolytics (eg, rt-PA or streptokinase) may:

  • increase the risk of bleeding complications
  • considerably enhance the effect of REFLUDAN on aPTT prolongation

Concomitant treatment with coumarin derivatives (vitamin K antagonists) and drugs that affect platelet function may also increase the risk of bleeding.

 

Refludan (Berlex Labs) Contraindications

REFLUDAN is contraindicated in patients with known hypersensitivity to hirudins or to any of the components in REFLUDAN [lepirudin (rDNA) for injection].

 

Additional information about Refludan (Berlex Labs)

Refludan (Berlex Labs) Indication: For the treatment of heparin-induced thrombocytopenia
Mechanism Of Action: Refludan (Berlex Labs) forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Lepirudin
Synonyms: Hirudin variant-1
Drug Category: Anticoagulants; Antithrombotic Agents
Drug Type: Biotech; Approved

Other Brand Names containing Lepirudin: Refludan (Berlex Labs);
Absorption: Bioavailability is 100% following injection.
Toxicity (Overdose): In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
Protein Binding: Not Available
Biotransformation: Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, con-clusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug.
Half Life: Approximately 1.3 hours
Dosage Forms of Refludan (Berlex Labs): Powder, for solution Intravenous
Chemical IUPAC Name: (4S)-4-[[(2S)-1-[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S,3R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-5-amino-2-[[(2S)-4-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S,3S)-2-[[(2R)-2-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[2-[[(2S)-5-amino-2-[[2-[[(2R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2R)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-hydroxy-4-oxobutanoyl]amino]-3-sulfanylpropanoyl]amino]-3-hydroxybutanoyl]amino]-5-hydroxy-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]-3-sulfanylpropanoyl]amino]-4-methylpentanoyl]amino]-3-sulfanylpropanoyl]amino]-5-hydroxy-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]amino]-3-methylbutanoyl]amino]-3-sulfanylpropanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]-3-sulfanylpropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-4-hydroxy-4-oxobutanoyl]amino]acetyl]amino]-5-hydroxy-5-oxopentanoyl]amino]hexanoyl]amino]-4-oxobutanoyl]amino]-5-oxopentanoyl]amino]-3-sulfanylpropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxybutanoyl]amino]acetyl]amino]-5-hydroxy-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-(3H-imidazol-4-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-hydroxy-4-oxobutanoyl]amino]acetyl]amino]-4-hydroxy-4-oxobutanoyl]amino]-3-cyclohexylpropanoyl]amino]-5-hydroxy-5-oxopentanoyl]amino]-5-hydroxy-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-hydroxy-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-hydroxy-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid
Chemical Formula: C287H446N80O111S6
Lepirudin on Wikipedia: https://en.wikipedia.org/wiki/Lepirudin
Organisms Affected: Humans and other mammals