Bivacs 10
(Bivaliurdin 0.75)

Drug Effects

Chemical Structure


Chemical Formula


C98H138N24O33

.

Iupac Name


d-Phenylalanyl-l-prolyl-l-arginyl
-l-prolylglycylglycylglycylglycyl-l-asparaginylglycyl
-l-alpha-aspartyl-l-phenylalanyl
-l-alpha-glutamyl-l-alpha-glutamyl-l-isoleucyl
-l-prolyl-l-alpha-glutamyl-l-alpha-glutamyl
-l-tyrosyl-l-leucine.

Usage


Bivalirudin is a type of "blood thinner" used instead of heparin to prevent blood clots during certain procedures used to open up the blood vessels in the heart (e.g., balloon angioplasty, coronary stent placement, percutaneous coronary intervention-PCI). It is usually used with aspirin.Bivalirudin works by blocking a certain natural substance (thrombin) that the body uses to form blood clots. Blood clots can cause a heart attackor cause the opened blood vessel in the heart to close back up.

Adverse Effect


  • Nausea, vomiting, heartburn, headache, or minor bleeding/irritation at the injection site may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Serious bleeding is the most common serious side effect. Tell your doctor immediately if any of these signs of serious bleeding occur: bleeding/bruising/swelling/oozing around the area where the procedure tube was placed, uncontrollednosebleed, fast/irregular heartbeat, pale/gray/bluish skin, pink/red urine, bloody/black/tarry stool, coughing up blood, vomit that looks like coffee grounds.Seek immediate medical attention if any of these signs of very serious bleeding occur: chest pain, vision problems, confusion, slurred speech, weakness on one side of the body.This medication may cause a decrease in blood platelets (thrombocytopenia). Tell your doctor immediately if you develop easy bleeding/bruising.A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects

Mechanism Action


Inhibits the action of thrombin by binding both to its catalytic site and to its anion-binding exosite. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.

Precaution


  • Before using bivalirudin, tell your doctor or pharmacist if you are allergic to it; or to other hirudins (e.g., lepirudin); or if you have any other allergies.This medication should not be used if you have certain medical conditions. 
  • Before using this medicine, consult your doctor or pharmacist if you have: current bleeding.Before using this medication, tell your doctor or pharmacist your medical history, especially of: recent major surgery/injury/other bleeding, stomach/intestinal problems (e.g., peptic ulcer, inflammatory bowel disease), bleeding problems (e.g., anemia, coagulopathy, thrombocytopenia), kidney disease, liver disease, stroke, very high uncontrolled blood pressure, tumor/blood vessel problem in the brain (e.g., aneurysm, AV malformation).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.
  • It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

Drug Interaction


Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: other "blood thinners" (e.g., warfarin), NSAIDs (e.g.,ibuprofennaproxen), anti-platelet drugs (e.g., dipyridamole, ticlopidine),tipranavir.Check all prescription and nonprescription medicine labels carefully since many contain pain relievers/fever reducers (NSAIDs such as ibuprofen, naproxen, or aspirin) that are similar to this drug.Bivalirudin is often used with other "blood thinners" such as aspirin and clopidogrel. Ask your doctor or pharmacist which medicines you need to take after leaving the hospital. Low-dose aspirin should be continued if prescribed by your doctor for heart attack or stroke prevention (usually at dosages of 81-325 milligrams a day). Consult your doctor or pharmacist for more details.This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

Pregnancy Category


Pregnancy Category B- Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women OR Animal studies have shown an adverse effect, but adequate and well-controlled studies in pregnant women have failed to demonstrate a risk to the fetus in any trimester.

Absorption


25 min (normal renal function); 57 min (severe renal impairment).

Distribution


Protein Bound: Minimal.

Metabolism


Angiomax is cleared from plasma by a combination of renal mechanisms and proteolytic cleavage.

Elemination


20% (urine).

References


  1.  Lincoff, A. M.; Bittl, J. A.; Harrington, R. A.; Feit, F.; Kleiman, N. S.; Jackman, J. D.; Sarembock, I. J.; Cohen, D. J.; Spriggs, D.; Ebrahimi, R.; Keren, G.; Carr, J.; Cohen, E. A.; Betriu, A.; Desmet, W.; Kereiakes, D. J.; Rutsch, W.; Wilcox, R. G.; De Feyter, P. J.; Vahanian, A.; Topol, E. J.; Replace-2, I. (2003). "Bivalirudin and provisional glycoprotein IIb/IIIa blockade compared with heparin and planned glycoprotein IIb/IIIa blockade during percutaneous coronary intervention: REPLACE-2 randomized trial". JAMA: the Journal of the American Medical Association 289 (7): 853–863. doi:10.1001/jama.289.7.853. PMID 12588269. 
  2.  "Annex 1 - Summary of Product Characteristics". www.themedicinescompany.com. The Medicines Company UK Ltd. March 2010. Retrieved 2 December 2011.
  3.  Zamora, Rolando; Forbes, Thomas; Hijazi, Ziyad; Qureshi, Athar; Ringewald, Jeremy; Rome, Jonathan; Vincent, Robert (2009). "Bivalirudin (Angiomax®) As a Procedural Anticoagulant in the Pediatric Population Undergoing Intravascular Procedures for Congenital Heart Disease". Catheterization and Cardiovascular Interventions 73 (S1): S8.
  4. a b Stone, G. W.; Witzenbichler, B.; Guagliumi, G.; Peruga, J. Z.; Brodie, B. R.; Dudek, D.; Kornowski, R.; Hartmann, F.; Gersh, B. J.; Pocock, S. J.; Dangas, G.; Wong, S. C.; Kirtane, A. J.; Parise, H.; Mehran, R.; Horizons-Ami Trial, I. (2008). "Bivalirudin during Primary PCI in Acute Myocardial Infarction". New England Journal of Medicine 358 (21): 2218–2230. doi:10.1056/NEJMoa0708191. PMID 18499566. 
  5. Mehran, R.; Lansky, A. J.; Witzenbichler, B.; Guagliumi, G.; Peruga, J. Z.; Brodie, B. R.; Dudek, D.; Kornowski, R.; Hartmann, F.; Gersh, B. J.; Pocock, S. J.; Wong, S. C.; Nikolsky, E.; Gambone, L.; Vandertie, L.; Parise, H.; Dangas, G. D.; Stone, G. W.; Horizons-Ami Trial, I. (2009). "Bivalirudin in patients undergoing primary angioplasty for acute myocardial infarction (HORIZONS-AMI): 1-year results of a randomised controlled trial". The Lancet 374 (9696): 1149–1159. doi:10.1016/S0140-6736(09)61484-7. PMID 19717185.